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Nitazoxanide, Indications, Dosage, Side Effects, Interactions, Pregnancy

Nitazoxanide is a synthetic benzamide with antiprotozoal activity. Nitazoxanide exerts its antiprotozoal activity by interfering with the pyruvate ferredoxin/flavodoxin oxidoreductase dependent electron transfer reaction, which is essential to anaerobic energy metabolism. PFOR enzyme reduces nitazoxanide, thereby impairing the energy metabolism. However, interference with the PFOR enzyme-dependent electron transfer reaction may not be the only pathway by which nitazoxanide exhibits antiprotozoal activity. Nitazoxanide is active against Giardia lamblia and Cryptosporidium parvum.
Nitazoxanide is an antimicrobial with activity against several parasitic worms and protozoa that is used predominantly in the United States in the treatment of giardiasis and cryptosporidiosis. Nitazoxanide therapy has not been reported to cause serum aminotransferase elevations during therapy or clinically apparent liver injury.
Nitazoxanide is a broad-spectrum antiparasitic, antiparasitic and broad-spectrum antiviral drug synthetic nitrothiazolyl-salicylamide derivative and an anti-protozoal agent. It is approved for treatment of infectious diarrhea caused by Cryptosporidium parvum and Giardia lamblia in patients 1 year of age and older. Following oral administration it is rapidly hydrolyzed to its active metabolite, tizoxanide, which is 99% protein bound. Peak concentrations are observed 1–4 hours after administration. It is excreted in the urine, bile, and feces. Untoward effects include abdominal pain, vomiting, and diarrhea.

Mechanism of Action of Nitazoxanide

The antiprotozoal activity of nitazoxanide is believed to be due to interference with the pyruvate, ferredoxin oxidoreductase (PFOR) enzyme-dependent electron transfer reaction which is essential to anaerobic energy metabolism. Nitazoxanide is an antifolate containing the pyrrolopyrimidine-based nucleus that exerts its antineoplastic activity by disrupting folate-dependent metabolic processes essential for cell replication. In vitro studies have shown that nitazoxanide inhibits thymidylate synthase (TS), dihydrofolate reductase (DHFR), and glycinamide ribonucleotide formyltransferase (GARFT), all folate-dependent enzymes involved in the de novo biosynthesis of thymidine and purine nucleotides. Nitazoxanide is transported into cells by both the reduced folate carrier and membrane folate binding protein transport systems. Once in the cell, nitazoxanide is converted to polyglutamate forms by the enzyme folylpolyglutamate synthetase. The polyglutamate forms are retained in cells and are inhibitors of TS and GARFT. Polyglutamation is a time- and concentration-dependent process that occurs in tumor cells and, to a lesser extent, in normal tissues. Polyglutamated metabolites have an increased intracellular half-life resulting in prolonged drug action in malignant cells.

Indications of Nitazoxanide

  • Dwarf Tapeworm Infection (Hymenolepis nana)
  • Ascariasis
  • Amebiasis
  • Diarrhea with vomiting
  • Giardiasis
  • Ascariasis
  • Cestode infections
  • Clostridium difficile infection recurrence
  • Cryptosporidiosis infection
  • Diarrhea caused by Cryptosporidium parvum
  • Diarrhea caused by Giardia lamblia
  • Giardiasis
  • Trichuriasis
  • For the treatment of diarrhea in adults and children caused by the protozoa Giardia lamblia, and for the treatment of diarrhea in children caused by the protozoan, Cryptosporidium parvum.
  • Nitazoxanide has not been shown to be superior to placebo medication for the management of diarrhea caused by Cryptosporidium parvum in patients with HIV/immunodeficiency

Contra-Indications of Nitazoxanide

  • Nitazoxanide is contraindicated only in individuals who have experienced a hypersensitivity reaction to nitazoxanide or the inactive ingredients of a nitazoxanide formulation

Dosage of Nitazoxanide

 Strengths:  500 mg ,100 mg/5 mL

Amebiasis

  • 500 mg twice daily with food for 3 days.
  • 1000 mg twice daily with food for 14 days or until diarrhea resolves.

Cryptosporidiosis

  • 500 mg twice daily with food for 3 days.
  • 1000 mg twice daily with food for 14 days or until diarrhea resolves.

Giardiasis

  • 500 mg twice daily with food for 3 days.
  • 1000 mg twice daily with food for 14 days or until diarrhea resolves.

Cryptosporidiosis

  • 12 to 47 months: 100 mg (5 mL) by mouth with food every 12 hours for 3 days.
  • 4 to 11 years: 200 mg (10 mL) with food every 12 hours for 3 days.
  • Greater than or equal to 12 years: 500 mg twice daily with food for 3 days.

Pediatric Giardiasis

  • 12 to 47 months: 100 mg (5 mL) by mouth with food every 12 hours for 3 days.
  • 4 to 11 years: 200 mg (10 mL) with food every 12 hours for 3 days.
  • Greater than or equal to 12 years: 500 mg twice daily with food for 3 days.

Ascariasis

  • 2 to 3 years: 100 mg/5 mL
  • 4 to 11 years: 200 mg/10 mL

Hymenolepis nana 

  •  to 3 years: 100 mg/5 mL
  • 4 to 11 years: 200 mg/10 mL

Pediatric Amebiasis

  • 500 mg twice daily with food for 3 days.

Side Effects of Nitazoxanide

The most common side effects 

Common

Rare

Drug Interactions of Nitazoxanide

Nitazoxanide may interact with following drugs, supplements, & may change the efficacy of drugs

Pregnancy & Lactation of Nitazoxanide

 FDA Pregnancy Category B

Pregnancy

There are no data with nitazoxanide in human pregnancy to inform a drug-associated risk. Animal reproductive studies performed in rats and rabbits at doses up to 2 and 30 times the recommended daily human dose demonstrated no evidence of teratogenicity or fetotoxicity due to nitazoxanide.

Breastfeeding

There is no information about the presence of nitazoxanide in human milk, the effects on the breastfed infant, or the effects on milk production. The developmental and health benefits of breastfeeding should be considered along with the mother’s clinical need for nitazoxanide and any potential adverse effects on the breastfed infant from nitazoxanide or the mother’s underlying condition.


  1. References

    1. DrugBank

      http://www.drugbank.ca/drugs/DB00507
      http://www.drugbank.ca/drugs/DB00507#targets
      http://www.drugbank.ca/drugs/DB00507#carriers
      http://www.drugbank.ca/drugs/DB00507#enzymes

      https://www.drugs.com/cdi/nitazoxanide-tablets.html

    2. EPA DSStox

      https://comptox.epa.gov/dashboard/dsstoxdb/results?search=DTXSID5033757

    3. European Chemicals Agency (ECHA)
      https://echa.europa.eu/substance-information/-/substanceinfo/100.054.465
      https://echa.europa.eu/information-on-chemicals/cl-inventory-database/-/discli/details/49601
    4. Human Metabolome Database (HMDB)

      http://www.hmdb.ca/metabolites/HMDB0014649

      https://www.webmd.com/drugs/2/drug-64747/nitazoxanide-oral/details

    5. ClinicalTrials.gov

      https://clinicaltrials.gov/

    6. DailyMed

      https://dailymed.nlm.nih.gov/dailymed/search.cfm?labeltype=all&query=NITAZOXANIDE

    7. FDA Pharm Classes

      https://www.accessdata.fda.gov/spl/data/7df89280-455d-4761-bf82-f8ca7ca2f0f4/7df89280-455d-4761-bf82-f8ca7ca2f0f4.xml

      https://www.fda.gov/ForIndustry/DataStandards/StructuredProductLabeling/ucm162549.htm

    8. LiverTox

      https://livertox.nlm.nih.gov/Nitazoxanide.htm

    9. NCIt

      https://ncit.nci.nih.gov/ncitbrowser/ConceptReport.jsp?dictionary=NCI_Thesaurus&ns=NCI_Thesaurus&code=C47637

    10. FDA/SPL Indexing Data
      https://www.fda.gov/ForIndustry/DataStandards/SubstanceRegistrationSystem-UniqueIngredientIdentifierUNII/
    11. FDA Orange Book

      https://www.fda.gov/Drugs/InformationOnDrugs/ucm129662.htm

    12. MassBank of North America (MoNA)

      http://mona.fiehnlab.ucdavis.edu/spectra/browse?inchikey=YQNQNVDNTFHQSW-UHFFFAOYSA-N

    13. PubMed Health

      http://www.ncbi.nlm.nih.gov/pubmedhealth/PMHT0011421/

    14. Springer Nature Read more …
    15. The Cambridge Structural Database
      http://www.ccdc.cam.ac.uk/pages/Home.aspx
    16. WHO ATC
      https://www.whocc.no/atc/
      https://www.whocc.no/atc_ddd_index/
    17. Wikipedia

      https://en.wikipedia.org/wiki/Nitazoxanide

      https://pubchem.ncbi.nlm.nih.gov

 

Nitazoxanide

By

Metronidazole, Indications, Dosage, Side Effects, Interactions

Metronidazole is a synthetic nitroimidazole derivative with antiprotozoal and antibacterial activities. Although its mechanism of action is not fully elucidated, un-ionized metronidazole is readily taken up by obligate anaerobic organisms and is subsequently reduced by low-redox potential electron-transport proteins to an active, intermediate product. Reduced metronidazole causes DNA strand breaks, thereby inhibiting DNA synthesis and bacterial cell growth.

A metroimidazole is an antibiotic and antiprotozoal medication used to treat amebiasis; vaginitis; trichomonas infections; giardiasis; anaerobic bacteria; and treponemal infections. It has also been proposed as a radiation sensitizer for hypoxic cells.

Machanism of Action of Metronidazole

Metronidazole, a synthetic antibacterial and antiprotozoal agent of the nitroimidazole class, is used against protozoa such as Trichomonas vaginalis, amebiasis, and giardiasis. Metronidazole is extremely effective against anaerobic bacterial infections and is also used to treat Crohn’s disease, antibiotic-associated diarrhea, and rosacea.Metronidazole is a prodrug. Unionized metronidazole is selective for anaerobic bacteria due to their ability to intracellularly reduce metronidazole to its active form. This reduced metronidazole then covalently binds to DNA, disrupt its helical structure, inhibiting bacterial nucleic acid synthesis and resulting in bacterial cell death.

or

Metronidazole is bactericidal, amebicidal, and trichomonacidal in action. The exact mechanism of action of the drug has not been fully elucidated. Metronidazole is un-ionized at physiologic pH and is readily taken up by anaerobic organisms or cells. In susceptible organisms or cells, metronidazoleis reduced by low-redox-potential electron transport proteins (e.g., nitroreductases such as ferredoxin) to unidentified polar product(s) which lack the nitro group. The reduction product(s) appears to be responsible for the cytotoxic and antimicrobial effects of the drug which include disruption of DNA and inhibition of nucleic acid synthesis. Metronidazole is equally effective against dividing and nondividing cells.
or
In in vivo studies in rats given metronidazole in dosages of 2-4 mg/100 g of body weight, the drug reportedly inhibited the development of formalin-induced edema in the rat paw. In vitro in neutrophils, metronidazole has a dose-dependent inhibitory effect on generation of hydrogen peroxide and hydroxyl radicals, oxidants that may cause tissue injury at the site of inflammation. This antioxidant effect appears to be caused by a direct effect on neutrophil function and may contribute to the drug’s anti-inflammatory effect in vivo.

Indications of Metronidazole

  • Bacterial Vaginitis
  • Bacterial Infection
  • Amebiasis
  • Aspiration Pneumonia
  • Dental Abscess
  • Clostridium difficile-associated diarrhea and colitis,
  • Helicobacter pylori infection and duodenal ulcer disease, bacterial vaginosis,
  • Giardia lamblia gastro-enteritis, amebiasis
  • STD Prophylaxis
  • Bacteremia
  • Balantidium coli
  • Bone infection
  • Clostridial Infection
  • Crohn’s Disease, 
  • Deep Neck Infection
  • Dientamoeba fragilis
  • Diverticulitis
  • Dracunculiasis
  • Endocarditis
  • Giardiasis
  • Helicobacter Pylori Infection
  • Intraabdominal Infection
  • Joint Infection
  • Lemierre’s Syndrome
  • Meningitis
  • Nongonococcal Urethritis
  • Pelvic Inflammatory Disease
  • Peritonitis
  • Pneumonia
  • Pouchitis
  • Pseudomembranous Colitis
  • Skin or Soft Tissue Infection
  • Surgical Prophylaxis
  • Trichomoniasis
  • For the treatment of anaerobic infections and mixed infections, surgical prophylaxis requiring anaerobic coverage, Clostridium difficile-associated diarrhea and colitis, Helicobacter pylori infection and duodenal ulcer disease, bacterial vaginosis, Giardia lamblia gastro-enteritis, amebiasis caused by Entamoeba histolytica, acne rosacea (topical treatment), and Trichomonas infections.

Therapeutic Indications of Metronidazole

  • Oral metronidazole (extended release formulation) is used in the treatment of bacterial vaginosis caused by Gardnerella vaginalis, Mobiluncus spp, mycoplasma hominis and anaerobes (peptostreptococcus spp and Bacteroides spp).
  • Metronidazole is used in the treatment of periodontal infections caused by Bacteroides species.
  • Oral metronidazole is used in the treatment of giardiasis caused by Giardia lamblia.
  • Some studies indicate that metronidazole may be effective, in combination with bismuth subsalicylate or colloidal bismuth subcitrate, and other oral antibiotic therapy, such as ampicillin or amoxicillin, in the treatment of Helicobacter pylori-associated gastritis and duodenal ulcer. However, metronidazole resistance may occur, especially in patients who have been previously exposed to metronidazole.
  • Metronidazole is used in the treatment of dracunculiasis (guinea worm infection) caused by Dracunculus medinensis. It decreases the inflammation around the ulcer, increasing the ease of removing the worm.
  • Metronidazole is used in the treatment of antibiotic-associated diarrhea and colitis caused by Clostridium difficile.
  • Metronidazole is used in the treatment of inflammatory bowel disease.
  • Metronidazole is used in the treatment of Balantidium coli infection.
  • Oral metronidazole is indicated in the treatment of symptomatic and asymptomatic trichomoniasis, in males and females, caused by Trichomonas vaginalis.
  • Metronidazole is indicated in the treatment of skin and soft tissue infections caused by Bacteroides species, including the Bacteroides fragilis group. Clostridium species, Fusobacterium species, Peptococcus species, and Peptostreptococcus species.
  • Metronidazole is indicated in the treatment of bacterial septicemia caused by Bacteroides species, including the Bacteroides fragilis group, and Clostridium species.
  • Metronidazole is indicated in the treatment of lower respiratory tract infections, including pneumonia, emphysema, and lung abscess, caused by Bacteroides species, including the Bacteroides fragilis group.
  • Intravenous metronidazole is indicated for the prophylaxis of perioperative infections during colorectal surgery.
  • Metronidazole is indicated in the treatment of female pelvic infections, including endometritis, endomyometritis, tubo-ovarian abscess, and postsurgical vaginal cuff infections, caused by Bacteroides species, including the Bacteroides fragilis group, Clostridium species, Peptoccus species, and Peptostreptococcus species.
  • Metronidazole is indicated in the treatment of intra-abdominal infections, including peritonitis, intra-abdominal abscess, and liver abscess, caused by Bacteroides species, including the Bacteroides fragilis group, Clostridium species, Eubacterium species, Peptococcus species, and Peptostreptococcus species
  • Metronidazole is indicated in the treatment of endocarditis caused by Bacteroides species, including the Bacteroides fragilis group.
  • Metronidazole is indicated in the treatment of CNS infections, including meningitis, caused by Bacteroides species, including the Bacteroides fragilis group.
  • Metronidazole is indicated in the treatment of brain abscess caused by Bacteroides species, including the Bacteroides fragilis group.
  • Metronidazole is indicated in the treatment of bone and joint infections caused by Bacteroides species, including the Bacteroides fragilis group (Bacteroides fragilis, Bacteroides distasonis, Bacteroides ovatus, Bacteroides thetaiotaomicron, Bacteroides vulgatus).
  • Oral metronidazole is indicated in the treatment of acute intestinal amebiasis caused by Entamoeba histolytica. Metronidazole may not eradicate intestinal amebic infections, requiring treatment with a luminal amebicide.
  • Metronidazole is indicated in the treatment of extraintestinal amebiases, including amebic liver abscess, caused by Entamoeba histolytica. When used in the treatment of invasive amebiasis, metronidazole should be administered concurrently or sequentially with a luminal amebicide (eg, iodoquinol, paromomycin, tetracycline, diloxanide furoate). When used in the treatment of amebic liver abscesses, metronidazole therapy does not obviate the need for aspiration of the abscess.
  • Metronidazole is not effective against facultative anaerobes, obligate aerobes, Propionibacterium acnes, Actinomyces species, or Candida albicans.

Contra Indications of Metronidazole

Dosage of Metronidazole

Strengths:  250 mg;400 mg 375 mg; 500 mg; 750 mg; 500 mg/100 mL;

Bacterial Infection

IV

  • Loading dose: 15 mg/kg IV once infused over 1 hour
  • Maintenance dose: 7.5 mg/kg IV infused over 1 hour every 6 hours
  • Maximum dose: 4 g per day
  • Duration of therapy: 7 to 10 days

Oral ,Immediate-release Capsules and Tablets

  • 7.5 mg/kg orally every 6 hours
  • Maximum dose: 4 g per day
  • Duration of therapy: 7 to 10 days

Amebiasis

Acute Intestinal Amebiasis (Acute Amebic Dysentery)

  • Immediate-release capsules and tablets: 750 mg orally 3 times a day for 5 to 10 days

Amebic Liver Abscess

  • Immediate-release capsules and tablets: 500 to 750 mg orally 3 times a day for 5 to 10 days

Trichomoniasis

  • Immediate-release Capsules: 375 mg orally twice a day for 7 consecutive days

Immediate-release Tablets

  • One-day regimen: 2 g orally as a single dose or 1 g twice given in the same da
  • Seven-day regimen: 250 mg orally 3 times a day for 7 consecutive days

US CDC recommendations ,Immediate-release Tablets

  • Recommended regimen: 2 g orally as a single dose
  • Alternative regimen: 500 mg orally twice a day for 7 days

Trichomoniasis in HIV-infected women

  • Immediate-release tablets: 500 mg orally twice a day for 7 days

Treatment failure with single-dose therapy and reinfection is excluded

  • Immediate-release tablets: 500 mg orally twice a day for 7 days; for patients failing this regimen, 2 g orally once a day for 7 days should be considered

Helicobacter pylori Infection

Some experts recommend

  • Bismuth quadruple therapy: 250 mg orally 4 times a day
  • Clarithromycin-based triple therapy: 500 mg orally twice a day
  • Duration of therapy: 10 to 14 days

Pelvic Inflammatory Disease

US CDC recommendations
Mild to moderately severe acute pelvic inflammatory disease (PID)

  • Immediate-release tablets: 500 mg orally twice a day for 14 days

Bacterial Vaginosis

  • Extended-release Tablets: 750 mg orally once a day for 7 consecutive days

US CDC recommendations

  • Immediate-release tablets: 500 mg orally twice a day for 7 days

Intraabdominal Infection

IV

  • Loading dose: 15 mg/kg IV once infused over 1 hour
  • Maintenance dose: 7.5 mg/kg IV infused over 1 hour every 6 hours
  • Maximum dose: 4 g per day
  • Duration of therapy: 7 to 10 days

Oral

  • Immediate-release capsules and tablets: 7.5 mg/kg orally every 6 hours
  • Maximum dose: 4 g per day
  • Duration of therapy: 7 to 10 days

IDSA and SIS recommendations

  • Immediate-release tablets: 500 mg IV every 8 to 12 hours or 1500 mg IV every 24 hours

Peritonitis

IV

  • Loading dose: 15 mg/kg IV once infused over 1 hour
  • Maintenance dose: 7.5 mg/kg IV infused over 1 hour every 6 hours
  • Maximum dose: 4 g per day
  • Duration of therapy: 7 to 10 days

Oral

  • Immediate-release capsules and tablets: 7.5 mg/kg orally every 6 hours
  • Maximum dose: 4 g per day
  • Duration of therapy: 7 to 10 days

Liver Abscess

IV

  • Loading dose: 15 mg/kg IV once infused over 1 hour
  • Maintenance dose: 7.5 mg/kg IV infused over 1 hour every 6 hours
  • Maximum dose: 4 g per day
  • Duration of therapy: 7 to 10 days

Oral

  • Immediate-release capsules and tablets: 7.5 mg/kg orally every 6 hours
  • Maximum dose: 4 g per day
  • Duration of therapy: 7 to 10 days

Joint Infection

IV:
-Loading dose: 15 mg/kg IV once infused over 1 hour
-Maintenance dose: 7.5 mg/kg IV infused over 1 hour every 6 hours
-Maximum dose: 4 g per day
-Duration of therapy: 7 to 10 days

Oral

  • Immediate-release capsules and tablets: 7.5 mg/kg orally every 6 hours
  • Maximum dose: 4 g per day
  • Duration of therapy: 7 to 10 days

Osteomyelitis

IV

  • Loading dose: 15 mg/kg IV once infused over 1 hour
  • Maintenance dose: 7.5 mg/kg IV infused over 1 hour every 6 hours
  • Maximum dose: 4 g per day
  • Duration of therapy: 7 to 10 days

Oral

  • Immediate-release capsules and tablets: 7.5 mg/kg orally every 6 hours
  • Maximum dose: 4 g per day
  • Duration of therapy: 7 to 10 days

Pediatric Bacterial Infection

American Academy of Pediatrics (AAP) recommendations ,Neonates
7 days or less

  • Up to 2 kg: 7.5 mg/kg IV every 12 hours
  • Greater than 2 kg: 7.5 mg/kg IV every 8 hours

8 to 28 days

  • Up to 2 kg: 7.5 mg/kg IV every 12 hours
  • Greater than 2 kg: 7.5 mg/kg IV every 6 hours
  • Postmenstrual age less than 34 weeks: 7.5 mg/kg IV every 12 hours
  • Postmenstrual age 34 to 40 weeks: 7.5 mg/kg IV every 8 hours
  • Postmenstrual age greater than 40 weeks: 7.5 mg/kg IV every 6 hour

1 month or older

  • IV: 22.5 to 40 mg/kg/day IV in 3 divided doses
  • Maximum dose: 1.5 g/day

Oral

  • 30 to 50 mg/kg/day orally in 3 divided doses
  • Maximum dose: 2.25 g/day

Side Effects of Metronidazole

The most common side effects 

Common

Rare

Drug Interactions of Metronidazole

Metronidazole may interact with following drugs, supplements, & may change the efficacy of drugs

Pregnancy & Lactation of Metronidazole

FDA Pregnancy Category B 
Pregnancy

According to the manufacturer, oral metronidazole is contraindicated during the first trimester of pregnancy in patients with trichomoniasis. However, the CDC states that metronidazole can be used for trichomoniasis at any stage of pregnancy as studies have not demonstrated an association between metronidazole and teratogenic effects.

Lactation

Metronidazole is excreted into breast milk. Breastfeeding is not recommended during treatment with systemic products. While there is some systemic absorption from topical and vaginal products, plasma concentrations would be lower than demonstrated with systemic formulations; however, caution is still advised. Metronidazole is a mutagen in vitro and has been shown to be carcinogenic in animal studies. In general, increased oral and rectal Candida colonization and loose stools have been reported in infants exposed to metronidazole via breast milk.


  1. References

    1. DrugBank

      http://www.drugbank.ca/drugs/DB00916
      http://www.drugbank.ca/drugs/DB00916#enzymes
      http://www.drugbank.ca/drugs/DB00916#targets

      https://www.drugs.com/metronidazole.html

    2. HSDB

      https://toxnet.nlm.nih.gov/cgi-bin/sis/search/r?dbs+hsdb:@term+@rn+@rel+443-48-1

    3. Human Metabolome Database (HMDB)

      http://www.hmdb.ca/metabolites/HMDB0015052

    4. ChemIDplus
      https://chem.nlm.nih.gov/chemidplus/sid/0000443481
      https://chem.sis.nlm.nih.gov/chemidplus/chemidheavy.jsp
    5. DTP/NCI

      https://dtp.cancer.gov/dtpstandard/servlet/dwindex?searchtype=NSC&outputformat=html&searchlist=757118

      https://dtp.cancer.gov/dtpstandard/servlet/dwindex?searchtype=NSC&outputformat=html&searchlist=69587

      https://dtp.cancer.gov/dtpstandard/servlet/dwindex?searchtype=NSC&outputformat=html&searchlist=50364

    6. EPA DSStox

      https://comptox.epa.gov/dashboard/dsstoxdb/results?search=DTXSID2020892

    7. European Chemicals Agency (ECHA)

      https://echa.europa.eu/substance-information/-/substanceinfo/100.006.489

      https://echa.europa.eu/information-on-chemicals/cl-inventory-database/-/discli/details/122521

    8. FDA Pharm Classes

      https://www.accessdata.fda.gov/spl/data/9ef71064-51c2-477c-b844-6cd39b67edc2/9ef71064-51c2-477c-b844-6cd39b67edc2.xml
      htps://www.fda.gov/ForIndustry/DataStandards/StructuredProductLabeling/ucm162549.htm

    9. LiverTox

      https://livertox.nlm.nih.gov/Metronidazole.htm

    10. NCIT

      https://ncit.nci.nih.gov/ncitbrowser/ConceptReport.jsp?dictionary=NCI_Thesaurus&ns=NCI_Thesaurus&code=C651

    11. ClinicalTrials.gov

      https://clinicaltrials.gov/

    12. DailyMed

      https://dailymed.nlm.nih.gov/dailymed/search.cfm?labeltype=all&query=PYLERA

      https://dailymed.nlm.nih.gov/dailymed/search.cfm?labeltype=all&query=METRONIDAZOLE

    13. FDA/SPL Indexing Data
      https://www.fda.gov/ForIndustry/DataStandards/SubstanceRegistrationSystem-UniqueIngredientIdentifierUNII/
    14. https://www.webmd.com/drugs/2/drug-6426/metronidazole-oral/details/list-contraindications
    15. EU Community Register of Medicinal Products

      https://ec.europa.eu/health/documents/community-register/html/o875.htm

    16. EPA Office of Pesticide Programs
      . Read more.

      http://www.ipmcenters.org/Ecotox/index.cfm

    17. FAO/WHO Food Additive Evaluations (JECFA)

      http://apps.who.int/food-additives-contaminants-jecfa-database/chemical.aspx?chemID=1482

    18. FDA Orange Book
      https://www.fda.gov/Drugs/InformationOnDrugs/ucm129662.htm
    19. SpectraBase
      https://spectrabase.com/compound/JFkJwk2sULC#HdF0T41T3NE
      https://spectrabase.com/compound/JFkJwk2sULC#8GCabMZST1m
      https://spectrabase.com/compound/JFkJwk2sULC#EHGeI5roo5K
      https://spectrabase.com/compound/JFkJwk2sULC#HnBVDInEb9a
      https://spectrabase.com/compound/JFkJwk2sULC#10mqscbTcU2
      https://spectrabase.com/compound/JFkJwk2sULC#CPP8EpjmR63
      https://spectrabase.com/compound/JFkJwk2sULC#FYFVNyw5ei0
      https://spectrabase.com/compound/JFkJwk2sULC#5nJn4e6QFpk
      https://spectrabase.com/compound/JFkJwk2sULC#4JYqtYHPj1u
      https://spectrabase.com/compound/JFkJwk2sULC#2EhAYCZSIIE
      https://spectrabase.com/compound/JFkJwk2sULC#BzHCiCimee6
    20. MassBank of North America (MoNA)

      http://mona.fiehnlab.ucdavis.edu/spectra/browse?inchikey=VAOCPAMSLUNLGC-UHFFFAOYSA-N

    21. NIST

      http://www.nist.gov/srd/nist1a.cfm

    22. PubMed Health

      http://www.ncbi.nlm.nih.gov/pubmedhealth/PMHT0001181/

      http://www.ncbi.nlm.nih.gov/pubmedhealth/PMHT0011199/

      http://www.ncbi.nlm.nih.gov/pubmedhealth/PMHT0011192/

      http://www.ncbi.nlm.nih.gov/pubmedhealth/PMHT0011193/

      http://www.ncbi.nlm.nih.gov/pubmedhealth/PMHT0011195/

    23. Springer Nature more …
    24. The Cambridge Structural Database

      http://www.ccdc.cam.ac.uk/pages/Home.aspx

    25. WHO ATC

      https://www.whocc.no/atc/

      https://www.whocc.no/atc_ddd_index/

    26. Wikipedia

      https://en.wikipedia.org/wiki/Metronidazole

      https://pubchem.ncbi.nlm.nih.gov

 

ByRx Harun

Medication/Drugs; Disease Conditions, Treatment,

Medication/Drugs is any substance (other than food that provides nutritional support) that, when inhaled, injected, smoked, consumed, absorbed via a patch on the skin, or dissolved under the tongue causes a temporary physiological (and often psychological) change in the body.

In pharmacology, a drug is a chemical substance of known structure, other than a nutrient of an essential dietary ingredient, which, when administered to a living organism, produces a biological effect. A pharmaceutical drug, also called a medication or medicine, is a chemical substance used to treat, cure, prevent, or diagnose a disease or to promote well-being. Traditionally drugs were obtained through extraction from medicinal plants, but more recently also by organic synthesis.Pharmaceutical drugs may be used for a limited duration, or on a regular basis for chronic disorders.

This list contains the names of many medical problems and the names of drugs that may be used for their treatment. The drugs are listed either as a generic name or drug class name. Specific brands are not shown. You may use this tool to find brand name versions of generics. This list is intended only as a guide and is not meant to be 100% complete. Use it for general reference.
The inclusion of a drug does not mean it is necessarily an appropriate treatment for you. Also, the doctor may prescribe the treatment that is not listed, but according to your medical history is quite appropriate for your medical condition.
Condition Commonly Used Drugs
Acid Indigestion and Upset Stomach Antacids
Bismuth Subsalicylate
Histamine H2 Receptor Antagonists
Hyoscyamine
Proton Pump Inhibitors
Simethicone
Sodium Bicarbonate
Acne Anti-acne Cleansing (Topical)
Topical Antibiotics (Clindamycin, Erythromycin)
Oral Antibiotics(Tetracyclines, Metronidazole)
Azelaic Acid
Benzoyl Peroxide
Isotretinoin
Keratolytics
Retinoids (Topical)
Actinic Keratoses Fluorouracil
Masoprocol
Acute Myocardial Infarction Antithrombotic Agents
Nitroglycerin
Angiotensin Converting Enzyme (ACE) Inhibitors
Beta-Adrenergic Blockers
Angiotensin-Receptor Blockers
Thrombolytics
Addison’s Disease Adrenocorticoids (Systemic)
Aging Dehydroepiandrosterone (DHEA)
AIDS and HIV Infection Fusion Inhibitors
Non-Nucleoside Reverse Transcriptase Inhibitors
Nucleoside Reverse Transcriptase Inhibitors
Nucleotide Reverse Transcriptase Inhibitors
Protease Inhibitors
Alcohol Withdrawal Benzodiazepines
Beta-Adrenergic Blocking Agents
Carbamazepine
Disulfiram
Hydroxyzine
Lithium
Naltrexone
Thiamine
Phenobarbital
Allergies and Allergic Reactions Adrenocorticoids (Nasal Inhalation, Oral Inhalation, Systemic)
Antihistamines
Antihistamines, Non-sedating
Antihistamines, Phenothiazine-Derivative
Azelastine
Cromolyn
Decongestants (Ophthalmic)
Ephedrine
Hydroxyzine
Alopecia Dutasteride
Finasteride
Minoxidil
Altitube Illness Carbonic Anhydrase Inhibitors
Alzheimer’s Disease Cholinesterase Inhibitors
Memantine
Amebiasis Chloroquine
Iodoquinol
Metronidazole
Amenorrhea Bromocriptine
Progestins
Amyotrophic Lateral Sclerosis (ALS) Riluzole
Anemia Adrenocorticoids (Systemic)
Androgens
Cyclosporine
Folic Acid
Iron Supplements
Leucovorin
Vitamin B-12
Angina Antiplatelet Agents
Beta Adrenergic Blocking Agents
Calcium Channel Blockers
Ranolazine
Nitrates
Anorexia Calcium Carbonate
Calcium Gluconate
Potassium Chloride
Antidepressants, Tricyclic
Progestins
Fluoxetine
Anxiety Antidepressants (Tricyclic, SSRIs, SNRIs)
Barbiturates
Benzodiazepines
Beta Adrenergic Blocking Agents
Buspirone
Ergotamine, Beladonna and Phenobarbital
Haloperidol
Hydroxyzine
Loxapine
Meprobamate
Phenothiazines
Thiothixene
Appetite Stimulant Antihistamines
Dronabinol
Megestrol
Arthritis (Osteoarthritis, Rheumatoid Arthritis) Acetaminophen
Adrenocorticoids (Oral Inhalation, Systemic)
Anakinra
Antihistamines, Non-sedating
COX-2 Inhibitors
NSAIDs
Aspirin
Azathioprine
Bronchodilators, Adrenergic
Bronchodilators, Xanthine
Capsaicin
Chloroquine
Cyclosporine
Gold Compounds
Hydroxychloroquine
Leukotriene Modifiers
Methotrexate
Tumor Necrosis Factor Blockers
Asthma Adrenocorticoids (Nasal Inhalation, Oral Inhalation, Systemic)
Bronchodilators, Adrenergic
Bronchodilators, Xanthine
Cromolyn
Ephedrine
Ipratropium
Leukotriene Modifiers
Nedocromil
Theophylline
Athlete’s Foot Antibacterials
Antifungals (Topical)
Attention Deficit Hyperactivity Disorder (ADHD) Amphetamines
Atomoxetine
Dexmethylphenidate
Methylphenidate
Pemoline
Guanfacine
Clonidine
Autism Haloperidol
Bacterial Infections Acetohydroxamic Acid (AHA)
Antibiotics
Benign Prostate Hyperplasia (BPH) Alpha Adrenergic Receptor Blockers
Dutasteride
Finasteride
Bipolar Disorder Antipsychotics (Quetiapine, Olanzapine, Risperidone, Ziprasidone, Haloperidol)
Anticonvulsants (Carbamazepine, Divalproex, Valproate Acid)
Lithium
Bites and Stings Adrenocorticoids (Topical)
Anesthetics (Topical)
Bladder Inflammation Dimethyl Sulfoxide
Bladder Spasms Clidinium
Propantheline
Oxybutynin
Bleeding Antifibrinolytic Agents
Vitamin K
Blood Circulation Cyclandelate
Intermittent Claudication Agents
Isoxsuprine
Vitamin E
Blood Clots Anticoagulants (Oral)
Antiplatelets (Clopidogrel, Dipyridamole, Ticlopidine)
Aspirin
Bronchial Spasms Anticholinergics
Bronchodilators, Adrenergic
Bronchitis Bronchodilators, Xanthine
Dextromethorphan
Ipratropium
Cephalosporins
Fluoroquinolones
Macrolides
Sulfonamides
Tetracyclines
Bulimia Antidepressants, Tricyclic
Lithium
Selective Serotonin Reuptake Inhibitors (SSRIs)
Burns Anesthetics (Topical)
Zinc Supplements
Silver Sulfadiazine
Neomycin/Polymyxin B/Bacitracin topical
Bursitis Adrenocorticoids (Systemic)
NSAIDs
Aspirin
Cancer Adrenocorticoids (Systemic)
Aminoglutethimide
Androgens
Antiandrogens, Nonsteroidal
Antifungals, Azoles
Busulfan
Capecitabine
Cholarmbucil
Cyclophosphamide
Estramustine
Estrogens
Etoposide
Flutamide
Hydroxyurea
Imatinib
Levamisole
Lomustine
Melphalan
Mercaptopurine
Methotrexate
Mitotane
Paclitaxel
Procarbazine
Progestins
Tamoxifen
Testolactone
Thioguanine
Thyroid Hormones
Toremifene
Cancer Of The Skin Fluorouracil
Masoprocol
Mechlorethamine (Topical)
Canker Sores (Aphthous Ulcers) Amlexanox
Bioadherent
Anesthetics (Mucosal-Local)
Corticosteroids
Chickenpox Acyclovir
Acetaminophen
Antihistamines
Cholesterol, High Cholestyramine
Colestipol
Ezetimibe
Gemfibrozil
HMG-CoA Reductase Inhibitors
Neomycin (Oral)
Niacin
Raloxifene
Chronic Obstructive Pulmonary Disease (COPD) Adrenocorticoids (Systemic)
Bronchodilators, Adrenergic
Bronchodilators, Xanthine
Ipratropium
Tiotropium
Cirrhosis Colchicine
Cyclosporine
Thiamine (Vitamin B-1)
Colds and Cough Acetaminophen
Anticholinergics
Antihistamines
Antihistamines, Non-sedating
NSAIDs
Aspirin
Dextromethorphan
Ephedrine
Guaifenesin
Phenylephrine
Phenylephrine (Ophthalmic)
Pseudoephedrine
Colic Hyoscyamine
Simethicone
Congestion Bronchodilators, Adrenergic
Ephedrine
Oxymetazoline
Phenylephrine
Pseudoephedrine
Xylometazoline
Congestive Heart Failure Angiotensin-Converting Enzyme (ACE) Inhibitors
Digitalis Preparations
Beta-Adrenergic Blocking Agents
Beta-Adrenergic Blocking Agents and Thiazide
Diuretics, Loop
Diuretics, Potassium-Sparing
Diuretics, Potassium-Sparing and Hydrochlorothiazide
Diuretics, Thiazide
Nitrates
Conjunctivitis (Pink Eye) Antibacterials (Ophthalmic)
Antivirals (Ophthalmic)
Conjunctivitis, Seasonal Allergic NSAIDs (Ophthalmic)
Antiallergic Agents (Ophthalmic)
Constipation Laxatives, Bulk-Forming (Psyllium)
Laxatives, Osmotic (Lactulose)
Laxatives, Softener/Lubricant
Laxatives, Stimulant (Senna, Bisacodyl, Cascara Sagrada)
Lubiprostone, Linaclotide
Tegaserod
Contraception (Birth Control) Contraceptives, Oral and Skin
Contraceptives, Vaginal
Contraceptives, Vaginal (Spermicides)
Convulsions (Epilepsy, Seizures) Anticonvulsants, Hydantoin
Anticonvulsants, Succinimide
Barbiturates
Benzodiazepines
Carbamazepine
Divalproex
Felbamate
Gabapentin
Lamotrigine
Levetiracetam
Oxcarbazepine
Primidone
Topiramate
Valproic Acid
Zonisamide
Corneal Ulcers Antibacterials (Ophthalmic)
Cushing’s Disease Adrenocorticoids (Systemic)
Aminoglutethimide
Antifungals, Azoles
Metyrapone
Mitotane
Trilostane
Cystitis Phenazopyridine
Sulfonamides and Phenazopyridine
Nitrofurantoin
Fosfomycin
Fluoroquinolones
Cephalosporins
Penicillins
Dandruff Antifungals (Topical)
Antiseborrheics
Coal Tar
Dementia Buspirone
Cholinesterase Inhibitors
Ergoloid Mesylates
Memantine
Haloperidol
Depression Antidepressants
Ergoloid Mesylates
Loxapine
Maprotiline
Methylphenidate
Selegiline
Dermatitis Adrenocorticoids (Systemic)
Adrenocorticoids (Topical)
Anesthetics (Topical)
Antiseborrheics
Coal Tar
Colchicine
Dapsone
Keratolytics
Dermatomyositis Aminobenzoate Potassium
Diabetes Antidiabetic Agents
Diarrhea Attapulgite
Bismuth Subsalicylate
Charcoal Activated
Difenoxin and Atropine
Diphenoxylate and Atropine
Kaolin and Pectin
Kaolin, Pectin, Belladonna and Opium
Loperamide
Nitazoxanide
Paregoric
Dietary Supplements Calcium Supplements
Iron Supplements
Niacin
Vitamin A
Vitamin B-12
Vitamin C
Vitamin D
Vitamin E
Vitamin K
Digestive Spasms Clidinium
Difenoxin and Atropine
Dicyclomine
Hyoscyamine
Propantheline
Diverticulitis
Drowsiness Caffeine
Orphenadrine, Aspirin and Caffeine
Dry Eyes Protectant (Ophthalmic)
Ear Allergies Anti-Inflammatory Drugs, Steroidal (Otic)
Ear Infections (Otitis Media) Antibiotics for Otitis Media
Antibacterials (Otic)
Anti-Inflammatory Drugs, Steroidal (Otic)
Antipyrine
Phenylephrine
Ear Wax Antipyrine and Benzocaine (Otic)
Eczema Adrenocorticoids (Topical)
Antibacterials, Antifungals (Topical)
Coal Tar
Doxepin (Topical)
Keratolytics
Emphysema Adrenocorticoids (Systemic)
Bronchodilators, Adrenergic
Bronchodilators, Xanthine
Ipratropium
Tiotropium
Endometriosis Danazol
Nafarelin
Goserelin
Leuprolide
Oral Contraceptives
Erectile Dysfunction (Impotence) Alprostadil
Erectile Dysfunction Agents
Papaverine
Yohimbe
Esophagitis Histamine H2 Receptor Antagonists
Metoclopramide
Proton Pump Inhibitors
Estrogen Deficiency Estrogen
Eye Allergies Antiallergic Agents (Ophthalmic)
Eye Conditions Antibacterials (Ophthalmic)
Cromolyn
Cycloplegic, Mydriatic (Ophthalmic)
Cyclopentolate (Ophthalmic)
Decongestants (Ophthalmic)
Natamycin (Ophthalmic)
Phenylephrine (Ophthalmic)
Fatigue Caffeine
Fever Acetaminophen
NSAIDs
Aspirin
Barbiturates, Aspirin and Codeine
Chlorzoxazone and Acetaminophen
Narcotic Analgesics and Aspirin
Salicylates
Fibrocystic Breast Disease Danazol
Vitamin E
Fluid Retention (Edema, Swelling) Angiotensin Converting Enzyme (ACE) Inhibitors and Hydrochlorothiazide
Carbonic Anhydrase Inhibitors
Clonidine and Chlorthalidone
Diuretics, Loop
Diuretics, Potassium-Sparing
Diuretics, Thiazide
Guanethidine and Hydrochlorothiazide
Hydralazine and Hydrochlorothiazide
Indapamide
Methyldopa and Thiazide Diuretics
Reserpine, Hydralazine and Hydrochlorothiazide
Fungal Infections (Ringworm) Antifungals, Azoles
Antifungals, Topical
Griseofulvin
Nystatin
Gallstones Ursodiol
Gastroesophageal Reflux Histamine H2 Receptor Antagonists
Proton Pump Inhibitors
Sucralfate
Genital Warts (Condyloma Acuminatum) Podofilox
Imiquimod
Papillomavirus Vaccines
Giardiasis Furazolidone, Quinacrine, Metronidazole, Nitazoxanide, Tinidazole
Gingivitis and Gum Disease Chlorhexidine
Erythromycins
Penicillins
Tetracyclines
Glaucoma Antiglaucoma, Adrenergic Antagonists
Antiglaucoma, Anticholinesterases
Antiglaucoma, Beta Blockers
Antiglaucoma, Carbonic Anhydrase Inhibitors
Antiglaucoma, Cholinergic Agonists
Antiglaucoma, Prostaglandins
Carbonic Anhydrase Inhibitors
Gonorrhea Cephalosporins
Erythromycins
Fluoroquinolones
Macrolide Antibiotics
Penicillins
Tetracyclines
Gout Adrenocorticoids (Systemic)
Allopurinol
NSAIDs
Colchicine
Meloxicam
Probenecid
Probenecid and Colchicine
Sulfinpyrazone
Hair Loss (Baldness) Antharil (Topical)
Finasteride
Minoxidil (Topical)
Hay Fever Antiallergic Agents (Ophthalmic)
Antihistamines
Antihistamines, Non-sedating
Antihistamine, Phenothiazine-Derivative
Ephedrine
Guaifenesin
Hydroxyzine
Meclizine
Orphenadrine
Phenylephrine (Ophthalmic)
Headache (Cluster, Migraine, Sinus, Tension, Vascular) Acetaminophen, Fioricet
Antidepressants, Tricyclic
Antihistamines
NSAIDs
Aspirin
Barbiturates, Aspirin and Codeine
Beta Adrenergic Blocking Agents
Buspirone
Butorphanol
Caffeine
Calcium Channel Blockers
Clonidine
Divalproex
Ergotamine
Ergotamine, Belladonna and Phenobarbital
Isometheptene, Dichloralphenazone and Acetaminophen
Lithium
Methysergide
Monoamine Oxidase Inhibitors
Triptans
Heart Rhythm Disorders (Irregular Heartbeat) Amiodarone
Beta-Adrenergic Blocking Agents
Calcium Channel Blockers
Digitalis Preparations
Disopyramide
Dofetilide
Flecainide Acetate
Mexiletine
Moricizine
Procainamide
Propafenone
Quinidine
Tocainide
Heartburn (Indigestion) Antacids
Histamine H2 Receptor Antagonists
Proton Pump Inhibitors
Sodium Bicarbonate
Hemorrhoids Adrenocorticoids (Topical)
Anesthetics (Rectal)
Herpes Antivirals (Topical)
Antivirals for Herpes Virus
Hives (Urticaria) Antihistamines
Antihistamines, Non-sedating
Antihistamines, Phenothiazine-Derivative
Hydroxyzine
Huntington’s Haloperidol
Hypercalcemia Colesevelam
Colestipol
Dextrothyroxine
HMG-CoA Reductase Inhibitors
Hyperglycemia Acarbose
Metformin
Hypertension (High Blood Pressure)
Hyperthyroidism Antithyroid Drugs
Hypertriglyceridemia Fibrates
Gemfibrozil
Hypoglycemia Glucagon
Miglitol
Hypothyroidism Dextrothyroxine
Thyroid Hormones
Incontinence Tolterodine
Infertility Bromocriptine
Clomiphene
Danazol
Progestins
Inflammation Acetaminophen and Salicylates
NSAIDs
COX-2 Inhibitors
Aspirin
Mesalamine
Narcotic Analgesics and Aspirin
Salicylates
Inflammatory Bowel Disease (Colitis, Crohn’s Disease) Adrenocorticoids (Systemic)
Cyclosporine
Mesalamine
Metronidazole
Olsalazine
Influenza (Flu) Antivirals for Influenza
Antivirals for Influenza, Neuraminidase Inhibitors
Ribavirin
Insomnia Belladonna Alkaloids and Barbiturates
Chloral Hydrate
Melatonin
Meprobamate
Intermittent Claudication Intermittent Claudication Agents
Irritable Bowel Syndrome Tegaserod
Itching Adrenocorticoids (Topical)
Doxepin (Topical)
Jet Lag Melatonin
Jock Itch Antifungals (Topical)
Joint Pain NSAIDs
COX-2 Inhibitors
Aspirin
Probenecid and Colchicine
Kidney Stones Allopurinol
Cellulose Sodium Phosphate
Citrates
Diuretics, Thiazide
Penicillamine
Sodium Bicarbonate
Tiopronin
Labyrinthitis Antihistamines, Phenothiazine-Derivatives
Benzodiazepines
Meclizine
Leg Pain or Cramps Cyclandelate
Intermittent Claudication Agents
Orphenadrine
Pentoxifylline
Quinine
Leukemia Imatinib
Thioguanine
Lice Pediculicides
Lupus (Skin and Systemic) NSAIDs
COX-2 Inhibitors
Adrenocorticoids (Systemic)
Adrenocorticoids (Topical)
Hydroxychloroquine
Methotrexate
Quinacrine
Lyme Disease Cephalosporins
Erythromycins
Macrolide Antibiotics
Penicillins
Tetracyclines
Malabsorption Vitamin K
Quinacrine
Malaria Antimalarial
Atovaquone
Chloroquine
Hydroxychloroquine
Primaquine
Proguanil
Quinidine
Quinine
Sulfadoxine and Pyrimethamine
Male Hormone Deficiency Androgens
Melanoma Hydroxyurea
Levamisole
Melphalan
Meniere’s Disease Antihistamines
Benzodiazepines
Meclizine
Scopolamine (Hyoscine)
Menopause Estrogens
Progestins
Menstrual Cramps (Dysmenorrhea) NSAIDs
COX-2 Inhibitors
Contraceptives (Oral)
Menstruation, Excessive (Menorrhagia) Contraceptives, Oral
Danazol
Estrogens
Progestins
Mental and Emotional Disturbances Loxapine
Molindone
Rauwolfia Alkaloids
Risperidone
Motion Sickness Antihistamines
Antihistamines, Non-sedating
Antihistamines, Phenothiazine-Derivative
Clotrimazole
Cyclizine
Diphenidol
Meclizine
Scopolamine
Multiple Sclerosis Adrenocorticoids (Systemic)
Baclofen
Tizanidine
Muscle Cramp, Spasm, Strain Baclofen
Chlorzoxazone and Acetaminophen
Dantrolene
Muscle Relaxants, Skeletal (Cyclobenzaprine, Carisoprodol, Orphenadrine, Tizanidine)
Aspirin and Caffeine
Quinine
Myasthenia Gravis Adrenocorticoids (Systemic)
Antimyasthenics
Azathioprine
Cyclosporine
Narcolepsy Amphetamines
Methylphenidate
Modafinil
Narcotic Withdrawal Buprenorphine and Naloxone
Nasal Allergy Adrenocorticoids (Nasal Inhalation)
Nausea and Vomiting Antihistamines Phenothiazine-Derivative
Bismuth Subsalicylate
Diphenidol
Dronabinol
Hydroxyzine
Metoclopramide
Nabilone
Phenothiazines
Scopolamine
Trimethobenzamide
Neural Tube Defects (prevention) Folic Acid
Night Blindness Beta Carotene
Obesity Appetite Suppressants
Lorcaserin
Phentermine
Orlistat
Liraglutide
Bupropion and Naltrexone
Obsessive Compulsive Disorder Antidepressants, Tricyclic
Selective Serotonin Reuptake Inhibitors (SSRIs)
Ocular Hypertension Beta Adrenergic Blocking Agents (Ophthalmic)
Dorzolamide
Osteoporosis Alendronate
Bone Formation Agents
Calcitonin
Calcium Supplements
Estrogens
Raloxifene
Sodium Fluoride
Vitamin D
Overactive Bladder Tolterodine, Oxybutynin, Trospium, Darifenacin, Solifenacin
TCA (Imipramine, Doxepin)
Mirabegron
Overdose Ipecac
Paget’s Disease Alendronate
Colchicine
Etidronate
Pain Adjuvant Analgesics
Pain In Mouth Anesthetics (Mucosal-Local)
Panic Disorder Antidepressants, Tricyclic
Benzodiazepines
Monoamine Oxidase Inhibitors
Parasites Anthelmintics
Pentamidine
Parkinson’s Disease Antidyskinetics
Antihistamines
Antivirals for Influenza
Bromocriptine
Carbidopa and Levodopa
Levodopa
Orphenadrine
Pergolide
Selegiline
Tolcapone
Parkinson’s Tremors Antihistamines
Niacin
Pellagra
Peyronie’s Disease Aminobenzoate Potassium
Poisoning Charcoal Activated
Ipecac
Potassium Deficiency Potassium Supplements
Premature Labor Isoxsuprine
Ritodrine
Premenstrual Syndrome (PMS) Antidepressants, Tricyclic
NSAIDs
Buspirone
Calcium Supplements
Contraceptives, Oral and Skin
Danazol
Pyridoxine (Vitamin B-6)
Selective Serotonin Reuptake Inhibitors (SSRIs)
Vitamin E
Pressure Sores Benzoyl Peroxide
Psoriasis Adrenocorticoids (Topical)
Anthralin
Biologics for Psoriasis
Calcipotriene
Coal Tar
Cyclosporine
Keratolytics
Methotrexate
Psoralens
Retinoids (Oral)
Retinoids (Topical)
Psychosis Thiothixene
Psychotic Disorders Aripiprazole
Carbamazepine
Clozapine
Haloperidol
Loxapine
Molindone
Olanzapine
Phenothiazines
Quetiapine
Risperidone
Thiothixene
Ziprasidone
Rectal Fissures Anesthetics (Rectal)
Respiratory Syncytial Virus (RSV) Ribavirin
Rickets Vitamin D
Rosacea Antibacterials (Topical)
Metronidazole
Azelaic Acid
Tetracyclines
Scabies Pediculicides
Schizophrenia Aripiprazole
Carbamazepine
Clozapine
Haloperidol
Molindone
Olanzapine
Phenothiazines
Quetiapine
Risperidone
Scleroderma Aminobenzoate Potassium
Shingles Antivirals (Topical)
Antivirals for Herpes Virus
Capsaicin
Sickle Cell Disease Hydroxyurea
Sinusitis Cephalosporins
Macrolide Antibiotics
Penicillins
Penicillins and Beta Lactamase Inhibitors
Sulfonamides
Tetracyclines
Trimethoprim
Xylometazoline
Skin Disorders (Rashes) Antibacterials (Topical)
Antibacterials, Antifungals (Topical)
Anesthetics (Topical)
Cyclophosphamide
Isotretinoin
Neomycin (Topical)
Retinoids (Topical)
Skin Lines and Wrinkles Botulinum Toxin (Type A)
Sleep Apnea Antidepressants, Tricyclic
Modafinil
Armodafinil
Progestins
Theophylline
Smoking Cessation Varenicline
Bupropion
Clonidine
Nicotine Transdermal Systems
Sore Throat Anesthetics (Mucosal-Local)
Medicated Lozenges, Sprays, Gargles
Stroke Prevention Platelet Inhibitors
Sunburn Adrenocorticoids (Topical)
Anesthetics (Topical)
Tonsillitis Cephalosporins
Macrolide Antibiotics
Tourette’s Syndrome Antidyskinetics
Haloperidol
Toxoplasmosis Pyrimethamine
Leucovorin
Atovaquone, Dapsone
Transplantation, Organ (Antirejection) Azathioprine
Cyclosporine
Immunosuppressive Agents
Tremors Benzodiazepines
Beta-Adrenergic Blocking Agents
Trigeminal Neuralgia Baclofen
Carbamazepine
Lamotrigine
Tuberculosis Cycloserine
Ethionamide
Isoniazid
Rifamycins
Ulcers Antacids
Anticholinergics
Bismuth Subsalicylate
Glycopyrrolate
Histamine H2 Receptor Antagonists
Metronidazole
Proton Pump Inhibitors
Sodium Bicarbonate
Sucralfate
Tetracyclines
Ulcerative Colitis Olsalazine
Sulfasalazine
Urethra Spasms Clidinium
Propantheline
Urethritis Erythromycins
Fluoroquinolones
Macrolide Antibiotics
Phenazopyridine
Sulfonamides and Phenazopyridine
Tetracyclines
Urinary Frequency Oxybutynin
Tolterodine
Urinary Retention Antimyasthenics
Bethanechol
Urinary Tract Infection Acetohydroxamic Acid
Atropine, Hyoscyamine, Methenamine
Cephalosporins
Cinoxacin
Cycloserine
Flavoxate
Fluoroquinolones
Loracarbef
Methenamine
Penicillins
Penicillins and Beta Lactamase Inhibitors
Phenazopyridine
Sulfonamides
Trimethoprim
Tetracyclines
Urine Acidity Citrates
Vitamin C
Uveitis Anti-Inflammatory Drugs, Steroidal (Ophthalmic)
Vaginal Infections or Irritation Clindamycin
Estrogens
Metronidazole
Progestins
Vaginal Yeast Infections Antifungals (Vaginal)
Vertigo Meclizine
Niacin
Virus Infections Of The Eye Antivirals (Ophthalmic)
Vitamin Deficiency Pantothenic Acid
Riboflavin
Vitamin A
Vitamin B-12
Vitamin C
Vitamin D
Vitamin E
Vitamin K
Vitiligo Psoralens (Methoxsalen)
Corticosteroids
Tacrolimus
Warts Keratolytics
Retinoids (Topical)
Wilson’s Disease Penicillamine
Zinc Supplements
Worms Anthelmintics
Zinc Deficiency Zinc Supplements
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Antidiabetes Drugs; Indications, Side Effects, Drug Interactions

Antidiabetes drugs is used in diabetes treat diabetes mellitus by lowering glucose levels in the blood. With the exceptions of insulin, exenatide, liraglutide and pramlintide, all are administered orally and are thus also called oral hypoglycemic agentsor oral antihyperglycemic agents. There are different classes of anti-diabetic drugs, and their selection depends on the nature of the diabetes, age and situation of the person, as well as other factors.

Diabetes mellitus type 1 is a disease caused by the lack of insulin. Insulin must be used in Type I, which must be injected.

Diabetes mellitus type 2 is a disease of insulin resistance by cells. Type 2 diabetes mellitus is the most common type of diabetes. Treatments include (1) agents that increase the amount of insulin secreted by the pancreas, (2) agents that increase the sensitivity of target organs to insulin, and (3) agents that decrease the rate at which glucose is absorbed from the gastrointestinal tract.

List of Medications for Diabetes

  • Insulins
  • Insulin sensitizers (reduce insulin resistance)
    • Biguanides
    • Thiazolidinediones
  • Secretagogues (stimulate insulin release)
    • Sulfonylureas
    • Meglitinides
  • Agents that slow the digestive/absorptive process:
    • Alpha-Glucosidase Inhibitors
  • Glucagon-Like Peptide-1 (GLP-1) Agonists
  • Dipeptidyl Peptidase-4 (DPP-4) Inhibitors
  • Amylin Analogues
  • Sodium-Glucose Transporter-2 (SGLT-2) Inhibitors
  • Combination Products

This comprehensive listing includes antihyperglycemic agents that can be used for glycemic control in diabetes.

New Antihyperglycemics

Class Generic/Brand/Approval year
SGLT-2 inhibitor Canagliflozin (Invokana), 2013
DPP-4 inhibitor Alogliptin (Nesina, Vipidia), 2013
SGLT-2 inhibitor Dapagliflozin (Farxiga), 2014
SGLT-2 inhibitor Empagliflozin (Jardiance), 2014
GLP-1 receptor agonist Albiglutide (Tanzeum), 2014
GLP-1 receptor agonist Dulaglutide (Trulicity), 2014
Inhaled insulin powder Afrezza, 2014

Insulin preparations differ in how quickly they work, when they peak maximal activity, and how long they work. Insulins are available for intravenous, intramuscular, and subcutaneous administration.

Generic Brand Name
Rapid Acting Insulins
Insulin aspart Novolog
Insulin glulisine Apidra
Insulin lispro Humalog
Insulin human Afrezza Inhalation Powder
Short Acting Insulins
Regular insulin Humulin R, Novolin R
Intermediate Acting Insulins
Insulin NPH Hagedorn NPH , Humulin N, Novolin N
Long Acting Insulins
Insulin detemir Levemir
Insulin glargine Lantus
Premixed Insulins
Insulin aspart protamine/
insulin aspart		 NovoLog 50/50, NovoLog 70/30
Insulin lispro protamine/
insulin lispro		 Humalog 50/50, Humalog 75/25
Combination with Insulins
Insulin glargine /Lixisenatide Soliqua 100/33
Insulin degludec/Liraglutide Xultophy 100/3.6

Sensitizers

Sensitizers increase the sensitivity of target organs to insulin.

Biguanides

Biguanides improve peripheral glucose uptake and utilization.

Generic Brand Name
Metformin Glucophage, Glucophage XR, Glumetza, Riomet, Fortamet

Phenformin and Buformin were withdrawn due to lactic acidosis risk.

Thiazolidinediones (Glitazones)

Thiazolidinediones work through the improvement of insulin sensitivity by acting on adipose, muscle, and liver to increase glucose utilization and decrease glucose production.

Generic Brand Name
Rosiglitazone Avandia
Pioglitazone Actos

Secretagogues

Secretagogues increase insulin secretion by the pancreas.

Sulfonylureas

Sulfonylureas stimulate insulin secretion by inhibiting the K(ATP) channel complex of the pancreatic beta cells. Sulfonylureas are used to treat type II diabetes. These agents are not indicated for type I diabetes.

Generic Brand Name
First-generation
Acetohexamide Dymelor
Chlorpropamide Diabinese
Tolazamide Tolinase
Tolbutamide Orinase
Second-generation
Glipizide Glucotrol, Minidiab, Glibenese
Glyburide (glibenclamide) Diabeta, Micronase, Glynase, Daonil, Euglycon
Glimepiride Amaryl
Gliclazide Uni Diamicron
Glyclopyramide Deamelin-S
Gliquidone Glurenorm

Meglitinides

Meglitinide derivatives stimulate insulin secretion from pancreatic cells, lowering blood glucose levels.

Generic Brand Name
Nateglinide Starlix
Repaglinide Prandin, NovoNorm

Alpha-Glucosidase Inhibitors

Alpha-glucosidase inhibitors are not technically glucose lowering agents because they do not have a direct effect on insulin secretion or sensitivity. These medications slow the digestive and absorptive process, preventing postprandial glucose raise.

Generic Brand Name
Acarbose Precose, Glucobay
Miglitol Glyset
Voglibose Basen

Glucagon-Like Peptide 1 (GLP-1) Agonists

GLP-1 analogs normalize fasting and postprandial blood glucose levels without causing hypoglycemia . Also, GLP-1 analogs reduce food intake and promote modest weight loss.

Generic Brand Name
Short-acting GLP-1 analogs
Exenatide Byetta
Lixisenatide Lyxumia, Adlyxin
Long-acting GLP-1 analogs
Liraglutide Victoza
Prolonged-acting GLP-1 analogs
Albiglutide Tanzeum
Dulaglutide Trulicity
Exenatide once weekly Bydureon
Under development
Taspoglutide Phase III clinical trials

Dipeptidyl Peptidase-4 Inhibitors (Gliptins)

Dipeptidyl peptidase-4 (DPP-4) inhibitors inhibit DPP-4, the enzyme that inactivates incretin hormones GLP-1 and GIP.

Generic Brand Name
Alogliptin Nesina, Vipidia
Anagliptin Suiny
Linagliptin Trajenta
Saxagliptin Onglyza
Sitagliptin Januvia
Teneligliptin Tenelia
DPP-4 inhibitors under development
Dutogliptin
Gemigliptin

Amylin Analogues

Pramlintide is a synthetic form of amylin, a pancreatic peptide produced by β-cells. Amylin and pramlintide lower postprandial glucose by lowering postprandial glucagon and delaying gastric emptying. Pramlintide is indicated for Type 1 and Type 2 diabetics who use insulin.

Generic Brand Name
Pramlintide Symlin

Sodium-Glucose Cotransporter 2 (SGLT-2) inhibitors

SGLT-2 inhibitors are a new class of drugs for Type 2 diabetes with novel mechanism of action. SGLT-2 inhibitors block reabsorption of glucose in the kidneys, leading to excretion of glucose in urine. These glucose lowering medications work independently of insulin.

Generic Brand Name
Canagliflozin Invokana
Dapagliflozin Forxiga, Farxiga
Empagliflozin Jardiance
SGLT-2 inhibitors under development
Ertugliflozin
Ipragliflozin
Remogliflozin etabonate
Tofogliflozin

Other Anti-diabetic Drugs

Generic Brand Name
Dopamine agonist
Bromocriptine Parlodel, Cycloset
Bile acid sequestrant
Colesevelam Welchol, Cholestagel, Lodalis

Combinations

Generic Brand Name
Alogliptin + Metformin Kazano
Dapagliflozin + Metformin Xigduo XR
Glipizide + Metformin Metaglip
Glyburide + Metformin Glucovance
Linagliptin + Metformin Jentadueto
Pioglitazone + Metformin Actoplus Met, Actoplus Met XR
Repaglinide + Metformin Prandimet
Rosiglitazone + Metformin Avandamet
Saxagliptin + Metformin Kombiglyze XR
Sitagliptin + Metformin Janumet
Rosiglitazone + Glimepiride Avandaryl
Pioglitazone + Glimepiride Duetact
Alogliptin + Pioglitazone Oseni
Simvastatin + Sitagliptin Juvisync
Empagliflozin + Metformin Synjardy

Mechanism of Action of antidiabetes drugs

Antidiabetes drugs mechanisms of action differ from other classes of oral antihyperglycemic agents. Antidiabetes drugs decreases blood glucose levels by decreasing hepatic glucose production, decreasing intestinal absorption of glucose, and improving insulin sensitivity by increasing peripheral glucose uptake and utilization. These effects are mediated by the initial activation by  antidiabetes drugs of AMP-activated protein kinase (AMPK), a liver enzyme that plays an important role in insulin signaling, whole body energy balance, and the metabolism of glucose and fats. Activation of AMPK is required for antidiabetes drugs inhibitory effect on the production of glucose by liver cells. Increased peripheral utilization of glucose may be due to improved insulin binding to insulin receptors. Antidiabetes drugs administration also increases AMPK activity in skeletal muscle. AMPK is known to cause GLUT4 deployment to the plasma membrane, resulting in insulin-independent glucose uptake. The rare side effect, lactic acidosis, is thought to be caused by decreased liver uptake of serum lactate, one of the substrates of gluconeogenesis. In those with healthy renal function, the slight excess is simply cleared. However, those with severe renal impairment may accumulate clinically significant serum lactic acid levels. Other conditions that may precipitate lactic acidosis include severe hepatic disease and acute/decompensated heart failure.

Indications antidiabetes drugs

  • Diabetes, Type 2
  • Polycystic Ovary Syndrome
  • Diabetes, Type 3c
  • Insulin Resistance Syndrome
  • Female Infertility
  • For use as an adjunct to diet and exercise in adult patients (18 years and older) with NIDDM. May also be used for the management of metabolic and reproductive abnormalities associated with polycystic ovary syndrome (PCOS). Jentadueto is for the treatment of patients when both linagliptin and metformin is appropriate.

Side Effects of Antidiabetes Drugs

Most common

More common

Less common

  • Abnormal stools
  • bad, unusual, or unpleasant (after) taste
  • change in taste
  • difficulty with moving
  • discoloration of the fingernails or toenails
  • flu-like symptoms
  • joint pain
  • rash
  • runny nose
  • sneezing
  • stuffy nose
  • swollen joints

Drug Interactions of Antidiabetes Drugs

Antidiabetes drugs may interact with following drugs ,suppliments & may decrease the efficacy of drug

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Anti viral,Anti fungal, Anti helmintics drug.The latest classification

Anti viral, Anti fungal, Anti helmintics drug. Antiviral drugs are a class of medication used specifically for treating viral infections rather than bacterial ones. Most antivirals are used for specific viral infections, while a broad-spectrum antiviral is effective against a wide range of viruses. Unlike most antibiotics, antiviral drugs do not destroy their target pathogen; instead they inhibit their development.

Antiviral drugs are one class of antimicrobials, a larger group which also includes antibiotic (also termed antibacterial), antifungal and antiparasitic drugs, or antiviral drugs based on monoclonal antibodies. Most antivirals are considered relatively harmless to the host, and therefore can be used to treat infections. They should be distinguished from viricides, which are not medication but deactivate or destroy virus particles, either inside or outside the body. Natural antivirals are produced by some plants such as eucalyptus.

Anti-herpetic agents

Generic Brand Name
Acyclovir Zovirax, Sitavig
Brivudine Helpin
Docosanol Abreva
Famciclovir Famvir
Foscarnet Foscavir
Idoxuridine Herplex, Dendrid
Penciclovir Denavir
Trifluridine Viroptic
Valacyclovir Valtrex
Pritelivir Inhibitor of the viral helicase-primase enzyme complex, currently under investigation

Anti-influenza agents
Generic Brand Name
Adamantane Derivatives
Amantadine Symmetrel
Rimantadine Flumadine
Neuraminidase Inhibitors
Oseltamivir Tamiflu
Peramivir Rapivab
Zanamivir Relenza

Allylamines

Generic name Brand name
Amorolfin Locery® (nail lacquer)
Butenafine Lotrimin® Ultra (cream, spray), Mentax® (cream)
Naftifine Naftin® (cream, gel)
Terbinafine Lamisil® (cream, gel, spray, solution, oral granules, tablets)

Allylamines are synthetic antifungals with activity against a wide range of dermatophytes. Allylamines act via inhibition of the squalene epoxidase formation, which blocks the synthesis of ergosterol.

Allylamines (with the exception of terbinafine) are used as topical treatments. Oral terbinafine is extensively used for the treatment of onychomycosis (fungal infection of the nail). It acts at an earlier stage by inhibiting the formation of squalene epoxide, a precursor of lanosterol. Oral terbinafine is the first choice for treating infections of fingernails and toenails

Azoles

Generic name Brand name
Imidazoles
Bifonazole Canespor® (cream)
Butoconazole Femstat® 3 (vaginal cream), Gynazole® 1 (vaginal cream)
Clotrimazole Canesten ® (cream, solution), Clocreme® (cream), Cruex® (spray powder), Desenex® (cream) , Femcare® (vaginal), Fungoid® (solution), Gyne-Lotrimin® (cream), Gynix® (vaginal tablets), Lotrimin (cream), Mycelex® (solution, troches), Pedesil® (ointment), Trivagizole® (cream)
Econazole Ecoza® (foam), Spectazole® (cream)
Fenticonazole * Lomexin®, Gynoxin®
Ketoconazole Nizoral® (oral tablets, cream, shampoo), Extina® (foam), Ketodan (foam), Kuric® (cream), Xolegel® (gel)
Isoconazole* Icaden®, Travogen®
Luliconazole Luzu® (cream)
Miconazole Cavilon® (antifungal cream), Cruex® (spray), Desenex® (topical powder), Fungoid® (cream, tincture), Lotrimin® AF Athlete’s Foot Spray (deodorant powder, powder, liquid), Lotrimin® AF Athlete’s Foot powder, Lotrimin® AF Jock Itch spray powder, Micatin® (cream), Monistat® 1, Monistat® 3, Monistat® 7, Ting® (antifungal spray powder, spray liquid), Vagistat® 3, Zeasorb® AF (powder, lotion)
Omoconazole* Fongamil®
Oxiconazole Oxistat® (cream, lotion)
Sertaconazole Ertaczo® (cream)
Sulconazole Exelderm® (cream, solution)
Tioconazole Monistat® 1 Simple Therapy, Vagistat® 1
Terconazole Terazol® 3 (vaginal cream, vaginal suppositories), Terazol® 7 (vaginal cream), Terconazole® (vaginal cream, vaginal suppositories), Zazole® (vaginal cream, vaginal suppositories)
Triazoles
Albaconazole Under® investigation
Efinaconazole Jublia® (topical gel, solution)
Fluconazole Diflucan® (tablets, capsules, injection)
Isavuconazole Cresemba® (capsules, injection)
Itraconazole Sporanox® (capsules, oral solution, injection), Onmel® (tablets)
Posaconazole Noxafil® (tablets, oral suspension, injection)
Ravuconazole Under investigation
Terconazole Terazol® 3, Terazol® 7 (vaginal cream, vaginal suppositories)
Voriconazole Vfend® (oral suspension, injection)
Arylguanidines (Thiazoles)
Abafungin* Abasol® (cream, gel)
* Not available in U.S.

Azoles (imidazole and triazole derivatives) are a large group of synthetic antifungal agents. Azoles are essentially fungistatic, and have a relatively broad antifungal spectrum. The azole antifungals have many drug-drug interactions because of their interference with cytochrome P-450 enzymes.

Imidazoles are considered first-line agents for most dermatophyte infections. Topical formulations are widely used for the treatment of superficial fungal infections and vaginal candidiasis. Imidazoles are very toxic when taken orally, so they are available only as topical formulations.

Triazoles are generally used for prophylaxis and treatment of invasive fungal infections and systemic mycosis.

Arylguanidines are a novel class of synthetic antifungal drugs.

Summary of the use of topical antifungals used in the treatment of tinea corporis, cruris and pedis

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Polyenes

Generic name Brand name
Amphotericin B Fungilin® (lozenges, oral suspension)
Nystatin Nilstat® (oral drops, capsules, powder, tablets)
Natamycin (pimaricin)
Trichomycin (hachimycin)

The polyenes are naturally occurring compounds with a very broad antifungal spectrum. Polyenes act by binding to sterols in the fungal cell membrane, thereby interfering with membrane integrity and causing leakage of essential metabolites. Most polyenes are used topically, but intravenous amphotericin remains an important agent for the treatment of systemic fungal infections. The risk of nephrotoxicity limits the use of amphotericin B.

Echinocandins

Generic name Brand name
Anidulafungin Eraxisin® injection
Caspofungin Cancidas® injection
Micafungin Mycamine® injection

Echinocandins are the most recently developed class of antifungals. Echinocandins are used mainly for the treatment of severe, invasive Candida infections. Echinocandins are safer than other classes of antifungals and have a broad spectrum, and synergistic effect in combination therapy.

Miscellaneous Antifungal Drugs

Generic name Brand name
Thiocarbamates
Tolnaftate Tinactin®, Aftate®, Breezee®, Ting®
Antimetabolites
Flucytosine
Benzylamines
Butenafine Mentax® (cream), Lotrimin® (cream)
Other antifungals
Griseofulvin Gris-PEG® (tablets), Grifulvin® V (tablets), Grisactin®
Ciclopirox Ciclodan® (cream, solution, topical suspension), Loprox® (cream), Penlac® (solution, nail lacquer), Loprox® (topical suspension, gel, shampoo)
Selenium sulfide Selsun®, Exsel®
Tavaborole Kerydin®

Anthelmintics

Anthelmintics are agents that destroy or expel parasitic worms (helminths). Interestingly, most anthelmintics were developed for use in veterinary medicine.

Generic Brand Name
Bephenium
Diethylcarbamazine
Ivermectin Sklice, Stromectol, Ivomec, Mectizan
Niclosamide Niclocide
Piperazine
Praziquantel Biltricide
Pyrantel Antiminth, Aut, Cobantril, Helmex, Lombriareu, Trilombrin
Pyrvinium Vanuin, Viprynium
Benzimidazoles
Albendazole Albenza
Flubendazole Fluvermal
Mebendazole Mebendacin, Mebutar, Nemazole, Vermox
Thiabendazole Foldan, Mintezol, Minzolum, Triasox

Scabicides & Pediculicides

Scabicides are agents that kill scabies mites and mite eggs.
Pediculicides are agents used to kill head lice.

Generic Brand Name
Benzyl benzoate Ascabiol
Benzyl benzoate/disulfiram Tenutex
Lindane GBH, G-Well, Kwellada, Kwildane, PMS Lindane
Malathion Derbac, Ovide
Permethrin Acticin, Elimite
Pediculicides (only for lice infestations)
Benzyl alcohol Ulesfia
Piperonyl butoxide/pyrethrins Pronto Lice Kill System
Spinosad Natroba
Scabicides (only for scabies infestations)
Crotamiton Eurax

References

  1. “A global view of hepatitis C: Physician knowledge, opinions, and perceived barriers to care”. Hepatology. 57 (4): 1325–1332. doi:10.1002/hep.26246. PMC 3683983 Freely accessible. PMID 23315914.
  2.  “New Hepatitis C Drugs Are Very Costly And Unavailable To Many State Prisoners”. Health Affairs. 35 (10): 1893–1901. doi:10.1377/hlthaff.2016.0296. ISSN 0278-2715.
  3. Summary of Recommendations for Patients Who are Initiating Therapy for HCV Infection by HCV Genotype | Recommendations for Testing, Managing, and Treating Hepatitis C”. www.hcvguidelines.org.
  4. Sofosbuvir and Velpatasvir (Lexi-Drugs)”. online.lexi.com.
  5. “Ledipasvir and Sofosbuvir (Lexi-Drugs)”. online.lexi.com.
  6. Hill, A.; Khoo, S.; Fortunak, J.; Simmons, B.; Ford, N. (6 January 2014). “Minimum Costs for Producing Hepatitis C Direct-Acting Antivirals for Use in Large-Scale Treatment Access Programs in Developing Countries”. Clinical Infectious Diseases. 58 (7): 928–936. doi:10.1093/cid/ciu012. PMC 3952605 Freely accessible. PMID 24399087.
  7. Times, Los Angeles. “The FDA can single-handedly reduce drug price-gouging. Why is it waiting?”. latimes.com.
  8. “21 USC CHAPTER 9, SUBCHAPTER VIII: IMPORTS AND EXPORTS . §381”. uscode.house.gov.
  9. NIH-Industry Partnerships Frequently Asked Questions | National Center for Advancing Translational Sciences”. National Center for Advancing Translational Sciences.
  10. Center for Disease Control. Understanding How Vaccines Work. https://www.cdc.gov/vaccines/hcp/conversations/downloads/vacsafe-understand-color-office.pdf Reviewed February 2013. Accessed 20 October 2016.

Anti viral, Anti fungal, Anti helmintics

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Analgesic, Anti Depressant, Sleeping Pill, Latest Clasification

Analgesic/painkiller is any member of the group of drugs used to achieve analgesia, relief from pain. Analgesic drugs act in various ways on the peripheral and central nervous systems. They are distinct from anesthetics, which temporarily affected, and in some instances completely eliminate sensation. Analgesics include paracetamol (known in North America as acetaminophen or simply APAP), the nonsteroidal anti-inflammatory drugs (NSAIDs) such as the salicylates, and opioid drugs such as morphine and oxycodone.

When choosing analgesics, the severity and response to other medication determine the choice of agent; the World Health Organization (WHO) pain ladder specifies mild analgesics as its first step.

The number of analgesics and adjunct agents are available for addressing different pain conditions. Following is a complete list of pain medications which includes new drug approvals.

Analgesics and adjunct pain medications share their mechanism of action. They all deliver analgesic effect by interfering with the pain signaling cascade.

Non-Narcotic Analgesics

Generic Brand Name
Acetaminophen Tylenol

Non-Steroidal Anti-Inflammatory Drugs (NSAIDs)

Generic Brand Name
Bromfenac Prolensa, Bromday
Diclofenac Cataflam, Voltaren, Zipsor
Diflunisal Dolobid
Etodolac Lodine, Lodine XL
Fenoprofen Nalfon
Flurbiprofen Ansaid
Ibuprofen Advil, Cramp End, Dolgesic, Excedrin IB, Genpril, Haltran, Ibren, Ibu, Ibuprin, Ibuprohm, Ibu-Tab, Medipren, Midol IB, Motrin, Nuprin, Pamprin-IB, Q-Profen, Rufen, Trendar
Indomethacin Indocin, Indocin SR, Tivorbex
Ketoprofen Actron, Orudis, Oruvail
Ketorolac Toradol, Sprix
Meclofenamate Meclomen
Mefenamic Acid Ponstel
Meloxicam Mobic, Vivlodex
Nabumetone Relafen
Naproxen Aleve, Anaprox,
Anaprox DS, EC-Naprosyn, Naprelan, Naprosyn
Nepafenac Nevanac
Oxaprozin Daypro
Phenylbutazone Cotylbutazone
Piroxicam Feldene
Sulindac Clinoril
Tolmetin Tolectin, Tolectin DS

COX-2 Inhibitors

Generic Brand Name
Celecoxib Celebrex

Narcotic Pain Medications (Painkillers)

Generic Brand Name
Buprenorphine Buprenex, Butrans transdermal patch
Butorphanol Stadol
Codeine
Hydrocodone
Hydromorphone Dilaudid, Dilaudid-5, Dilaudid-HP, Hydrostat IR, Exalgo ER
Levorphanol Levo-Dromoran
Meperidine Demerol
Methadone Dolophine, Methadose
Morphine Astramorph PF, AVINZA, Duramorph, Kadian,
M S Contin, MSIR, Oramorph SR, Rescudose, Roxanol
Nalbuphine Nubain
Oxycodone OxyContin, Roxicodone, Oxecta
Oxymorphone Numorphan
Pentazocine Talwin
Propoxyphene Cotanal-65, Darvon
Tapentadol Nucynta

Central Analgesics

Generic Brand Name
Tramadol Ultram
Tramadol and Acetaminophen Ultracet

Combinations

Generic Brand Name
Butalbital, Acetaminophen, and Caffeine Femcet, Fioricet, Esgic, Esgic-Plus
Butalbital, Aspirin, and Caffeine Fiorinal
Butalbital, acetaminophen, caffeine, and codeine Fioricet with Codeine
Hydrocodone and Ibuprofen Hydro seal IR, Vicoprofen
Morphine/Naltrexone Embeda
Oxycodone/Naltrexone Troxyca ER
Pentazocine/Naloxone Talwin NX
Narcotic Analgesics and Acetaminophen
Acetaminophen and Codeine Capital with Codeine, Margesic #3, Phenaphen with Codeine, Tylenol with Codeine
Dihydrocodeine, Acetaminophen, and Caffeine DHA plus
Hydrocodone and Acetaminophen Allay, Anexsia 5/500, Anexsia 7.5/650, Dolacet, Dolagesic, Duocet, Hycomed, Hydrocet, Hydrogesic, HY-PHEN, Lorcet 10/650, Lorcet-HD, Lortab, Panacet 5/500, Panlor, Stagesic, T-Gesic, Ugesic, Vicodin, Zydone
Oxycodone and Acetaminophen Endocet, Percocet, Roxicet, Roxilox, Tylox; Xartemis XR
Pentazocine and Acetaminophen Talacen
Propoxyphene and Acetaminophen Darvocet-N 50,
Darvocet-N 100, E-Lor, Propacet 100
Narcotic Analgesics and Aspirin
Aspirin, Caffeine, and Dihydrocodeine Synalgos-DC
Aspirin and Codeine Empirin with Codeine
Hydrocodone and Aspirin Damason-P, Lortab ASA, Panasal 5/500
Oxycodone and Aspirin Endodan, Percodan, Percodan-Demi, Roxiprin
Pentazocine and Aspirin Talwin Compound
Propoxyphene, Aspirin, and Caffeine Darvon Compound-65, PC-Cap, Propoxyphene Compound-65

Topical Analgesics

Generic Brand Name
Capsaicin ArthriCare, ARTH-RX, Axsain, Capsagel, Dura-Patch, Methacin, Qutenza, Zotrix, Zotrix-HP

Topical Anesthetics

While analgesics lessen the sensation of pain, anesthetics block all physical feelings, including pain.

Generic Brand Name
Benzocaine Americaine, Endocrine, Lagos
Benzocaine / Menthol Benzocol, Butyl Aminobenzoate, Dermoplast
Dibucaine Cinchocaine, Nupercainal Cream, Nupercainal Ointment
Lidocaine LidaMantle, Lidoderm, Lignocaine, Xylocaine
Lidocaine/ Prilocaine EMLA

Sleeping pill

Several different classes of medications are used to treat insomnia. This list includes both prescription and over-the-counter sedative-hypnotic medications.

Non-Benzodiazepine hypnotics (Z-Drugs)

Z-drugs are structurally unrelated to each other. These medications have largely replaced traditional benzodiazepines in the treatment of insomnia.

Generic Brand Name
Eszopiclone Lunesta
Zaleplon Sonata
Zolpidem Ambien, Intermezzo, Zolpimist
Zopiclone * Zimovane
* NOT approved in the US

Melatonin receptor agonists

Ramelteon is currently the only FDA-approved melatonin receptor agonist. Ramelteon is used for sleep onset insomnia and has little value for maintaining sleep.

Generic Brand Name
Ramelteon Rozerem

Orexin receptor antagonists

Orexin-receptor antagonists is a novel pharmacologic class of hypnotics. The first – and by far the only – member of this class was approved in 2014.

Generic Brand Name
Suvorexant Belsomra

Benzodiazepines

Benzodiazepine hypnotics are used for the short-term treatment of insomnia. Benzodiazepines produce sedative, hypnotic, anxiolytic, and muscle relaxant effects.

Benzodiazepines shorten sleep latency and reduce the number of awakenings and the time spent in the stage of wakefulness.

All benzodiazepines are controlled substances in schedule IV.

Generic Brand Name
Hypnotics
Brotizolam * Lendormin
Estazolam Prosom
Flurazepam Dalmane
Loprazolam* Dormonoct, Havlane, Sonin, Somnolent
Lormetazepam* Loramet, Noctamid
Nitrazepam* Cerson, Mogadon, Nitrazadon, Radedorm
Quazepam Doral
Temazepam Restoril
Triazolam Halcion
* NOT approved in the US
Anxiolytics (not approved as hypnotics)
Alprazolam Xanax
Bromazepam Lexotan
Chlordiazepoxide Librium
Clorazepate dipotassium Tranxene, Gen-Xene
Clonazepam Klonopin
Diazepam Valium
Lorazepam Ativan
Midazolam Versed
Oxazepam Serax

Sedating antidepressants

Sedating antidepressants are widely used for insomnia, but are not officially licensed for this indication. Currently doxepin is the only antidepressant approved by the U.S. FDA for the treatment of insomnia.

Generic Brand Name
Amitriptyline* Elavil, Endep, Vanatrip
Doxepin Silenor, Sinequan, Adapin
Mirtazapine* Remeron
Trazodone* Desyrel, Oleptro, Trittico
* NOT FDA approved for insomnia

Barbiturates

Currently, barbiturates are not recommended for routine use for insomnia due to the high incidence of tolerance and dependence.

Generic Brand Name
Amobarbital Amytal Sodium
Butabarbital Butisol
Pentobarbital Nembutal
Phenobarbital
Secobarbital Seconal Sodium

Other sedative-hypnotic agents

Generic/Class Brand Name
Chloral hydrate
(sedative, hypnotic)		 Somnote, Noctec, Aquachloral
Dexmedetomidine Precedex, Dexdor, Dexdomitor
Ethchlorvynol Placidyl

Over-the-counter sleep aids

Most of the over-the-counter sleep aids contain sedating antihistamine (histamine type 1 receptor blocker).

Generic Brand Name
Diphenhydramine Benadryl
Doxylamine Unisom SleepTabs, Good Sense Sleep Aid

 

Dietary supplements, herbal products

Name Class
Melatonin the hormone secreted by the pineal gland, available as a dietary supplement
Kava herbal product
Passionflower herbal product
St. John’s Wort herbal product
Valerian herbal product

“Off-label” Sleep Aids

Generic Brand Name
Atypical antipsychotics
Olanzapine Zyprexa
Quetiapine Seroquel, Seroquel XR
Anticonvulsant
Gabapentin Neurontin
Tiagabine Gabitril
Antihistamines
Chlorpheniramine Antagonate, Chlor-Trimeton, Kloromin, Phenetron, Pyridamal 100, Teldrin
Hydroxyzine and its combinations Vistaril, Atarax
Promethazine Phenergan, Remsed
Trimeprazine Temaril, Vallergan

Psychostimulants

The two classes of psychostimulants indicated for the treatment of ADHD are methylphenidate and amphetamines. Stimulants function by increasing the amount of dopamine and noradrenaline in the brain and stimulating the central nervous system.

Stimulants are the most potent, and also the most effective class of ADHD medications. Stimulants are considered a first-line therapy for controlling ADHD symptoms unless there are contraindications that preclude their use. Methylphenidate and amphetamines are equally effective, with efficacy rates ranging from 70% to 90%

Stimulants are available in many different formulations including short-acting, intermediate-acting, and long-acting preparations.

Generic name Brand name
Amphetamine Dyanavel XR, Adzenys XR, Evoker
Amphetamine/ dextroamphetamine salts Adderall, Adderall XR
Dexmethylphenidate Focalin, Focalin XR, Dexedrine, Dextrostat, ProCentra, Zenzedi
Lisdexamfetamine Vyvanse
Methamphetamine Desoxyn
Methylphenidate Ritalin, Ritalin SR, Ritalin LA, Methylin, Methylin ER, Quillichew ER, Quillivant XR, Aptensio XR, Concerta ER, Metadate CD
Methylphenidate transdermal Daytrana

Non-Stimulants

Non-stimulant medications approved for the treatment of ADHD have the different mode of action compared to psychostimulants and are considered non-addictive with more favorable side effect profiles.

On the other hand, non-stimulants are generally less effective than stimulants in the treatment of ADHD. The non-stimulants are usually considered second- and third-line medications.

Atomoxetine is a selective norepinephrine reuptake inhibitor with a unique mechanism of action. Atomoxetine is thought to have minimal abuse potential and significantly fewer withdrawal symptoms than psychostimulants. The main drawback is that atomoxetine doesn’t directly influence dopamine and it may take several weeks before the drug elicits a therapeutic effect.

Two antihypertensive drugs (alpha-2 noradrenergic agonists) are approved by the FDA to treat ADHD. These drugs reduce activity in the central nervous system but are considered less effective than stimulants. Clonidine and guanfacine are considered relatively safe over the long-term.

Generic name Brand name
Selective Norepinephrine Reuptake Inhibitor
Atomoxetine Strattera
Alpha-2 Noradrenergic Agonists
Clonidine extended-release Kapvay
Guanfacine extended-release Intuniv

“Off-label” Medications

There are several medications used to treat attention-deficit hyperactivity disorder “off-label”. While they are not approved for this disease, these medications can improve productivity, concentration, and overall cognitive function. Additionally, many are used as an augmentation strategy to treat patients that have comorbid depression or other disorders.

Generic name Brand name
Short-acting forms Alpha-2 Noradrenergic Agonists
Clonidine Catapres
Guanfacine Tenex
Antipsychotics
Aripiprazole Abilify
Olanzapine Zyprexa
Quetiapine Seroque
Risperidone Risperdal
Ziprasidone Geodon
Wakefulness-promoting eugeroic() drugs
Armodafinil Nuvigil
Modafinil Nuvigil
Antidepressants
Desipramine Norpramin
Imipramine Tofranil
Bupropion Wellbutrin SR, Wellbutrin XL

ADHD medications under investigation

Generic name, Class Brand name
Vortioxetine
(serotonin modulator and stimulator)		 Brintellix, Trintellix
Centanafadine
(serotonin-norepinephrine-dopamine reuptake inhibitor)
Dasotraline
(serotonin-norepinephrine-dopamine reuptake inhibitor )
Metadoxine

Antidepressants:

Common features of all antidepressants:

  • 1. All antidepressants work by increasing the levels of neurotransmitters (chemical messengers) in the brain.
  • 2. Antidepressants are NOT controlled substances.
  • 3. Antidepressants improve depressive symptoms at about the same rate.

New Antidepressants

Generic Name Brand Name
Vortioxetine (serotonin modulator and stimulator) Brintellix, approved September 2013
Levomilnacipran (SNRI) Fetzima, approved July 2013
Vilazodone (SSRI) Viibryd, approved January 2011

SSRIs (Selective Serotonin Reuptake Inhibitors)

Generic Brand Name
Citalopram Celexa
Escitalopram Lexapro, Cipralex
Fluoxetine Prozac, Sarafem; Pexeva
Fluvoxamine Luvox
Paroxetine Paxil, Paxil CR
Sertraline Zoloft

Selective serotonin reuptake inhibitors are the most widely prescribed antidepressants. SSRIs selectively inhibit the reuptake of serotonin resulting in increased serotonin concentration in the brain.
Main beneficial features of SSRIs over older antidepressants (MAOIs and TCAs):

  • Low overdose toxicity potential.
  • Low risk of severe systemic adverse effects, especially anticholinergic and cardiovascular side effects.

The major drawbacks of SSRIs:

  • Sexual dysfunction, which is the most common SSRI-induced side effect that leads to drug discontinuation.

Tricyclics (TCA)

Generic Brand Name
Amitriptyline Elavil, Endep, Levante
Amoxapine Asendin
Clomipramine Anafranil
Desipramine Norpramin, Pertofrane
Dosulepin Prothiaden, Thaden
Doxepin Adapin, Sinequan
Imipramine Tofranil
Lofepramine Gamanil, Lomont
Maprotiline Deprilept, Ludiomil, Psymion
Mianserin Bolvidon, Norval, Tolvan
Nortriptyline Pamelor
Protriptyline Vivactil
Trimipramine Surmontil

Tricyclic antidepressants represent the oldest class of drugs for depression. Currently, TCAs are considered second-line antidepressants in cases when SSRIs are ineffective or as adjunct therapy with newer drugs. TCAs act as non-selective inhibitors of the reuptake of serotonin and norepinephrine.

Advantages of TCAs:

  • Proven efficacy.
  • Low cost.

Drawbacks of TCAs:

  • Adverse effects such as orthostatic hypotension, anticholinergic effects, cardiovascular effects (arrhythmias and tachycardia).
  • Overdose toxicity.

SNRIs (Serotonin and Noradrenaline Reuptake Inhibitors)

Generic Brand Name
Desvenlafaxine Pristiq
Duloxetine Cymbalta
Levomilnacipran Fetzima
Milnacipran Savella
Venlafaxine Effexor, Effexor XR

Unlike SSRI antidepressants SNRIs block the reuptake of both serotonin and noradrenaline. Generally, SNRIs have side effect profile as SSRIs but are more likely to produce anticholinergic side effects.

NaSSA (Noradrenergic and Specific Serotonergic Antidepressant)

Generic Brand Name
Mirtazapine Remeron, Remeron SolTab

Mirtazapine enhances the presynaptic release of serotonin and norepinephrine in the brain. It works via antagonist activity in the presynaptic alpha 2-adrenergic receptors.

NDRIs (Norepinephrine and Dopamine Reuptake Inhibitors)

Generic Brand Name
Bupropion Wellbutrin, Wellbutrin SR, Wellbutrin XL, Zyban; Aplenzin

`

Generic Brand Name
Atomoxetine (Norepinephrine Reuptake Inhibitor) Strattera
Agomelatine (5-HT2C receptor antagonist) Valdoxan
Buspirone
(5HT1A receptor agonist)		 Buspar
Nefazodone
(5HT2-receptor antagonist)		 Nefadar, Serzone
Tandospirone (azapirone, 5HT1A receptor agonist) Sediel
Tianeptine
(Serotonin reuptake enhancer)		 Stablon
Trazodone
(5HT2-receptor antagonist, triazolopyridine-derivative)		 Desyrel, Apo-Trazodone, Oleptro
Reboxetine
(Norepinephrine Reuptake Inhibitor)		 Edronax, Vestra
Viloxazine (Norepinephrine Reuptake Inhibitor) Vivian
Vilazodone
(Selective serotonin reuptake inhibitor, Serotonin 5HT 1A receptor agonist)		 Viibryd
Serotonin Modulator and Stimulator
Vortioxetine Brintellix
Combinations
Fluoxetine/Olanzapine
(SSRI/antipsychotic)		 Symbyax
Amitriptyline/Perphenazine
(TCA/antipsychotic)		 Etrafon, Triavil

MAOIs (Monoamine Oxidase Inhibitors)

Generic Brand Name
Isocarboxazid Marplan
Moclobemide Manerix
Phenelzine Nardil
Tranylcypromine Parnate
Selegiline Emsam (transdermal patch)

 

Monoamine Oxidase Inhibitors (MAOIs) are irreversible inhibitors of the enzyme monoamine oxidase. MAOIs inactivate neurotransmitters norepinephrine, serotonin, and dopamine. Currently, MAOIs have a place in treating Parkinson’s disease, atypical depression, as well as depression that does not respond to other antidepressant drugs.

The main dangers of MAOIs:

  • Dietary restrictions. MAOIs have potentially lethal interactions with foods and drugs containing tyramine. Foods containing tyramine include cheese, smoked meats, and red wine.
  • Potential to cause a hypertensive crisis and serotonin syndrome.
  • Risk of orthostatic hypotension

Advantages of MAOIs:

  • Effective for atypical depression.
  • Highly effective for mood and anxiety disorders.
  • Minimal anticholinergic and antihistamine effects.
  • Inexpensive.

Mood Stabilizers

Some mood stabilizers used to treat depressive symptoms are:

Generic Brand Name
Lithium Eskalith, Lithane, Lithobid
Quetiapine Seroquel, Xeroquel, Ketipinor

Atypical antipsychotics

Certain atypical antipsychotics licensed to treat depression are:

Generic Brand Name
Brexpiprazole Rexulti
By

Antihypertensive Drugs, Uses, Side Effects, Drug Interactions

Antihypertensive drugs are a class of drugs that are used to treat hypertension (high blood pressure). Antihypertensives drugs therapy seeks to prevent the complications of high blood pressure, such as stroke and myocardial infarction. Evidence suggests that reduction of the blood pressure by 5 mmHg can decrease the risk of stroke by 34%, of ischaemic heart disease by 21%, and reduce the likelihood of dementia, heart failure, and mortality from cardiovascular disease. There are many classes of antihypertensives, which lower blood pressure by different means. Among the most important and most widely used drugs are thiazide diuretics, calcium channel blockers, ACE inhibitors, angiotensin II receptor antagonists (ARBs), and beta blockers.

Includes therapeutic agents that can be used for lowering of blood pressure.

Alpha-Blockers (Antihypertensive)

Alpha blockers, also called alpha-adrenergic antagonists, dilate blood vessels by blocking postsynaptic alpha1-adrenergic receptors. Alpha blockers are generally not recommended as initial therapy.

Generic Brand Name
Doxazosin Cardura, Carduran
Prazosin Minipress, Minipress XL
Terazosin Hytrin

Alpha-2 Agonists, Central-Acting

Alpha-2 adrenergic receptor agonists work by stimulating alpha-2 receptors and decreasing sympathetic activity, which leads to decreased blood pressure and heart rate.

Generic Brand Name
Clonidine Catapres, Catapres TTS (patch), Dixarit, Duraclon, Jenloga, Kapvay, Nexiclon XR
Guanabenz Wytensin
Guanfacine Intuniv, Tenex
Methyldopa Aldomet
Lofexidine Britlofex

Aldosterone Antagonists, Selective

Generic Brand Name
Eplerenone Inspra

Angiotensin II Receptor Blockers

Angiotensin receptor blockers work by blocking the effects of hormone angiotensin II (type 1 receptor). As a result, blood vessels dilate and blood pressure is reduced.

Generic Brand Name
Azilsartan Edarbi
Candesartan Atacand
Eprosartan Teveten
Irbesartan Avapro
Losartan Cozaar
Olmesartan Benicar
Telmisartan Micardis
Valsartan Diovan

ACE (Angiotensin Converting Enzyme) Inhibitors

ACE inhibitors remain the initial treatment of choice for hypertension. This class of drugs blocks the conversion of angiotensin I to angiotensin II by inhibiting angiotensin-converting enzyme (ACE), thus preventing constriction of blood vessels.

Generic Brand Name
Benazepril Lotensin
Captopril Capoten
Enalapril Vasotec
Fosinopril Monopril
Lisinopril Prinivil
Moexipril Univasc
Perindopril Aceon
Quinapril Accupril
Ramipril Altace
Trandolapril Mavik

Beta-blockers

Beta-blockers produce antihypertensive action by reducing heart rate and cardiac output. Currently beta-blockers are not recommended as first-line treatment due to the risk of stroke and new-onset of type 2 diabetes when compared to other medications

Generic Brand Name
Beta-blockers with alpha activity
Carvedilol Coreg, Coreg CR
Labetalol Trandate
Beta-blockers with intrinsic sympathomimetic activity
Acebutolol Sectral
Pindolol Visken
Penbutolol Levatol
Beta-1 cardioselective beta-blockers
Atenolol Tenormin
Betaxolol Kerlone
Bisoprolol Zebeta
Celiprolol Selectol
Metoprolol Lopressor, Toprol XL
Nebivolol Bystolic
Sotalol Betapace, Betapace AF, Sorine
Nonselective beta-blockers
Nadolol Corgard
Propranolol Inderal LA, InnoPran XL
Timolol Blocadren

Calcium Channel Blockers

Calcium channel blockers decrease the entry of calcium into the cells of the heart and blood vessels. By blocking the entry of calcium, this class of drugs reduces heart rate and contractility and dilates arteries.

Generic Brand Name
Amlodipine Norvasc, Lotrel
Bepridil Vascor
Clevidipine Cleviprex
Diltiazem Calan, Calan SR, Cardizem, Covera HS, Isoptin SR, Verelan, Verelan PM
Felodipine Plendil
Lacidipine Caldine, Lacimen, Lacipil, Midotens, Motens
Lercanidipine Lercadip, Zanidip
Levamlodipine EsCordi Cor, Esam, Eslo, S-Amlip
Isradipine DynaCirc, DynaCirc CR
Nicardipine Cardene SR
Nifedipine Adalat, Nifediac, Nifedical, Procardia
Nimodipine Nimotop
Nisoldipine Sular
Verapamil Calan, Calan SR, Covera-HS, Isoptin SR, Verelan, Verelan PM

Diuretics, Loop

Loop diuretics lower blood pressure by reducing blood volume. These medications inhibit the sodium-potassium-chloride cotransporter in the thick ascending limb of the loop of Henle. Loop diuretics promote water loss and increase sodium excretion.

Generic Brand Name
Bumetanide Bumex
Ethacrynic acid Edecrin
Furosemide Lasix
Piretanide
Torsemide Demadex

Diuretics, Potassium-Sparing

Potassium-sparing diuretics work by leaving more potassium in the blood, as a result more sodium and water are excreted in the urine. Potassium-sparing diuretics are weak antihypertensives when used alone.

Generic Brand Name
Amiloride Midamore
Spironolactone Aldactone
Triamterene Dyrenium

Diuretics, Thiazide

Thiazide diuretics reduce sodium absorption from the distal tubule segment of the kidney. Thiazide diuretics are known to worsen insulin sensitivity and elevate serum total cholesterol levels

Generic Brand Name
Bendroflumethiazide Aprinox
Chlorothiazide Diuril
Chlorthalidone Hygroton
Indapamide Lozol
Hydrochlorothiazide Hydrodiuril
Methyclothiazide Enduron
Metolazone Zaroxolyn, Diulo, Mykrox

Peripheral Adrenergic Inhibitors

These medications are rarely used unless other medications don’t help.

Generic Brand Name
Guanadrel Hylorel
Guanethidine Ismelin
Reserpine Serpasil

Renin Inhibitors

Renin inhibitors act by inhibiting the activity of renin, the enzyme responsible for angiotensin II levels.

Generic Brand Name
Aliskiren Tekturna

Vasodilators

Vasodilators work by dilating arterioles. However, vasodilatation by itself causes increased sympathetic outflow to the heart, leading to tachycardia and increased contraction.

Generic Brand Name
Diazoxide Proglycem
Hydralazine Apresoline, Dralzine
Minoxidil Loniten
Nitroprusside Nipride, Nitropress, Sodium Nitroprusside

Antihypertensive Combinations

Generic Brand Name
Alpha blockers and diuretics
Prazosin/Polythiazide Minizide
ACE inhibitors and Diuretics
Benazepril Lotensin HCT
Captopril Capozide
Enalapril Vaseretic
Fosinopril Monopril HCT
Lisinopril Prinzide, Zestoretic
Moexipril Uniretic
Quinapril Accuretic
Angiotensin ll Antagonists and Diuretics
Candesartan Atacand HCT
Eprosartan Teveten HCT
Irbesartan Avalide
Losartan Hyzaar
Olmesartan Benicar HCT
Telmisartan Micardis HCT
Valsartan Diovan HCT
Beta-blockers and Diuretics
Atenolol/Chlorthalidone Tenoretic
Bisoprolol Ziac
Metoprolol Lopressor HCT
Nadolol/Bendroflumethiazide Corzide
Propranolol Inderide
Timolol Timolide
Calcium channel blockers and ACE inhibitors
Amlodipine/Benzapril Lotrel
Amlodipine/Perindopril Prestalia
Diltiazem/Enalapril Teczem
Felodipine/Enalapril Lexxel
Lercanidipine/Enalapril Carmen ACE, Coripren
Verapamil/Trandolapril Tarka
Calcium channel blockers and Angiotensin II receptor antagonist
Amlodipine/Olmesartan Azor
Amlodipine/Olmesartan Tribenzor
Amlodipine/Telmisartan Twynsta
Amlodipine/Valsartan Exforge
Amlodipine/Valsartan Exforge HCT
Centrally acting drugs and Diuretics
Methyldopa Aldoril
Reserpine/Chlorothiazide Diupres
Reserpine Hydropres
Diuretic combinations
Amiloride Moduretic
Spironolactone Aldactone
Triamterene Dyazide, Maxzide
Clonidine/Chlorthalidone Combipres
Hydralazine Apresazide
Methyldopa Aldoril
Prazosin/Polythiazide Minizide
Other combinations
Amlodipine/Atorvastatin Caduet
Amlodipine/Aliskiren Tekamlo
Amlodipine/Aliskiren Amturnide
Aliskiren/HCTZ Tekturna HCT
Aliskiren/Valsartan Valturna
Nebivolol/Valsartan Byvalson

Blood pressure medications

Telmisartan affects the renin-angiotensin-aldosterone. You shouldn’t take this drug with other medicines that affect this system. These drugs include:

  • aliskiren. Telmisartan and aliskiren shouldn’t be used together in adults with diabetes or moderate kidney disease.
  • angiotensin receptor blockers (ARBs), such as:
    • candesartan (Atacand, Atacand HCT)
    • eprosartan (Teveten)
    • irbesartan (Avapro, Avalide)
    • losartan (Cozaar, Hyzaar)
    • olmesartan (Benicar, Benicar HCT, Tribenzor, Azor)
    • valsartan (Diovan, Diovan HCT, Exforge, Exforge HCT)
    • azilsartan (Edarbi, Edarbyclor)
  • angiotensin-converting enzyme (ACE) inhibitors, such as:
    • benazepril (Lotensin, Lotrel, Lotensin HCT)
    • captopril
    • enalapril (Vasotec, Epaned)
    • fosinopril (Monopril)
    • lisinopril (Prinivil, Zestril, Prinzide, Zestoretic)
    • moexipril (Uniretic)
    • perindopril (Aceon)
    • quinapril (Accupril, Accuretic)
    • ramipril (Altace)
    • trandolapril (Mavik, Tarka)

Mechanism of Action of Antihypertensives Drugs

Antihypertensive drug competes with sympathomimetic neurotransmitters such as catecholamines for binding at beta(1)-adrenergic receptors in the heart, inhibiting sympathetic stimulation. This results in a reduction in resting heart rate, cardiac output, systolic and diastolic blood pressure, and reflex orthostatic hypotension.

Antihypertensive drugs is classified as a non-cardioselective sympatholytic beta blocker that crosses the blood–brain barrier. It is lipid soluble and also has sodium channel blocking effects.  Antihypertensive drugs is a non-selective beta blocker; that is, it blocksthe action of epinephrine (adrenaline) and norepinephrine (noradrenaline) at both β1– and β2-adrenergic receptors. It has little intrinsic sympathomimetic activity, but has strong membrane stabilizing activity (only at high blood concentrations, e.g. overdose). Antihypertensive drugs is able to cross the blood–brain barrier and exert effects in the central nervous system in addition to its peripheral activity.

In addition to blockade of adrenergic receptors, Antihypertensive drugs has very weak inhibitory effects on the norepinephrine transporter and/or weakly stimulates norepinephrine release (i.e., the concentration of norepinephrine is increased in the synapse).Since propranolol blocks β-adrenoceptors, the increase in synaptic norepinephrine only results in α-adrenoceptor activation, with the α1-adrenoceptor being particularly important for effects observed in animal models. Therefore, it can be looked upon as a weak indirect α1-adrenoceptor agonist in addition to potent β-adrenoceptor antagonist.In addition to its effects on the adrenergic system, there is evidence that indicates that antihypertensive drugs may act as a weak antagonist of certain serotonin receptors, namely the 5-HT1A, 5-HT1B, and 5-HT2Breceptors.The latter may be involved in the effectiveness of propranolol in the treatment of migraine at high doses

or

Antihypertensive drugs competes with sympathomimetic neurotransmitters such as catecholamines for binding at beta(1)-adrenergic receptors in the heart, inhibiting sympathetic stimulation. This results in a reduction in resting heart rate, cardiac output, systolic and diastolic blood pressure, and reflex orthostatic hypotension.

Indications of Antihypertensive drugs

Cardiovascular

Psychiatric

Antihypertensive drugs is occasionally used to treat performance anxiety.Evidence to support its use in other anxiety disorders is poor.Some experimentation has been conducted in other psychiatric areas

Others

  • Essential tremor. Evidence for use for akathisia however is insufficient
  • Migraine and cluster headache prevention and in primary exertional headache
  • Hyperhidrosis (excessive sweating)
  • Proliferating infantile hemangioma
  • Glaucoma
  • Thyrotoxicosis by deiodinase inhibition
  • Akathisia caused by antipsychotic use
  • Angina Pectoris
  • Cardiovascular Mortality
  • Gastroesophageal variceal hemorrhage prophylaxis
  • Hemangiomas
  • High Blood Pressure (Hypertension)
  • Idiopathic hypertrophic subaortic stenosis
  • Migraines
  • Nonvalvular Atrial Fibrillation
  • Obstructive Hypertrophic Cardiomyopathy
  • Performance Anxiety
  • Pheochromocytomas
  • Supraventricular Arrhythmias
  • Tachyarrhythmia caused by Digitalis intoxication
  • Tachyarrhythmia caused by catecholamine excess
  • Thyroid Crisis
  • Thyrotoxicosis
  • Tremor caused by lithium
  • Tremor, Essential
  • Ventricular Tachycardia

Contra Indications of Antihypertensive drugs

Antihypertensive drugs may be contraindicated in people with

Side Effects of Antihypertensive drugs

The most common

Common

Rare

Drug Interactions of Antihypertensive drugs

Antihypertensive drugs may interact with following drugs, supplyments, & may change the efficacy of drugs

This medication may interfere with certain laboratory tests (including glaucoma screening test, cardiovascular stress testing using arbutamine), possibly causing false test results. Make sure laboratory personnel and all your doctors know you use this drug.

References

  1. https://www.ncbi.nlm.nih.gov/pubmedhealth/PMHT0025447/
  2. https://en.wikipedia.org/wiki/Antihypertensive_drug
By

Tetracycline, Uses, Dosage, Side effects, Interactions, Pregnancy

Tetracycline is a broad-spectrum naphthacene antibiotic produced semisynthetically from chlortetracycline, an antibiotic isolated from the bacterium Streptomyces aureofaciens. In bacteria, tetracycline binds to the 30S ribosomal subunit, interferes with the binding of aminoacyl-tRNA to the mRNA-ribosome complex, thereby inhibiting protein synthesis.

Tetracycline is a broad spectrum polyketide antibiotic produced by the Streptomyces genus of Actinobacteria. It exerts a bacteriostatic effect on bacteria by binding reversible to the bacterial 30S ribosomal subunit and blocking incoming aminoacyl tRNA from binding to the ribosome acceptor site.

Machanism of Action of Tetracycline

Tetracycline passively diffuses through porin channels in the bacterial membrane and reversibly binds to the 30S ribosomal subunit, preventing binding of tRNA to the mRNA-ribosome complex, and thus interfering with protein synthesis.

Tetracycline is a short-acting antibiotic that inhibits bacterial growth by inhibiting translation. It binds to the 30S ribosomal subunit and prevents the amino-acyl tRNA from binding to the A site of the ribosome. It also binds to some extent to the 50S ribosomal subunit. This binding is reversible in nature. Additionally tetracycline may alter the cytoplasmic membrane of bacteria causing leakage of intracellular contents, such as nucleotides, from the cell.

The hepatotoxic effects of tetracycline (I), rolitetracycline, and doxycycline were studied in male and female mice. All antibiotics (25-100 ug/g) increased the amount of unconjugated and total bilirubin. This effect was most pronounced after tetracycline, which also reduced the level of conjugated bilirubin. All drugs increased serum transaminase enzyme levels; this effect was more pronounced in females.

Indications of Tetracycline

  • Bacterial Infection
  • Bladder Infection
  • Acne
  • Bronchitis
  • Brucellosis
  • Bullous Pemphigoid
  • Chlamydia Infection
  • Ehrlichiosis
  • Epididymitis, Sexually Transmitted
  • Gonococcal Infection, Uncomplicated
  • Helicobacter Pylori Infection
  • Lyme Disease, Arthritis
  • Lyme Disease, Erythema Chronicum Migrans
  • Lyme Disease, Neurologic
  • Lymphogranuloma Venereum
  • Nongonococcal Urethritis
  • Ocular Rosacea
  • Ornithosis
  • Pelvic Inflammatory Disease
  • Pemphigoid
  • Pemphigus
  • Pneumonia
  • Psittacosis
  • Rheumatoid Arthritis
  • Rickettsial Infection
  • Syphilis, Early
  • Syphilis, Latent
  • Tertiary Syphilis
  • Upper Respiratory Tract Infection

Used to treat bacterial infections such as Rocky Mountain spotted fever, typhus fever, tick fevers, Q fever, rickettsialpox and Brill-Zinsser disease. May be used to treat infections caused by Chlamydiae spp., B. burgdorferi (Lyme disease), and upper respiratory infections caused by typical (S. pneumoniae, H. influenzae, and M. catarrhalis) and atypical organisms (C. pneumoniae, M. pneumoniae, L. pneumophila). May also be used to treat acne. Tetracycline may be an alternative drug for people who are allergic to penicillin.

Therapeutic Indications of Tetracycline

  • Tetracycline hydrochloride ointment is used in the prophylaxis of minor bacterial skin infections and in the treatment of dermal ulcer.
  • Tetracycline hydrochloride ointment is indicated in the topical treatment of minor skin infections caused by streptococci, staphylococci, and other susceptible organisms.
  • Tetracycline hydrochloride for topical solution is indicated for the topical treatment of acne vulgaris. It may be effective in grades II and III acne, which are characterized by inflammatory lesions such as papules and pustules.
  • Ophthalmic tetracycline is used in the treatment of chlamydia infections and ocular rosacea.
  • Ophthalmic tetracycline is used in the treatment of bacterial blepharitis, blepharoconjunctivitis, bacterial conjunctivitis, bacterial keratitis, bacterial keratoconjunctivitis, and meibomianitis.
  • Ophthalmic tetracycline is indicated in the treatment of trachoma caused by Chlamydia trachomatis. It should be used concurrently with oral tetracyclines.
  • Ophthalmic tetracycline is indicated in the prophylaxis of ophthalmia neonatorum caused by Neisseria gonorrhoea and Chlamydia trachomatis.
  • phthalmic tetracycline is indicated in the treatment of superficial ocular infections caused by Staphylococcus aureus, streptococci including Streptococcus epidermicus (Streptococcus pyogenes) and Staphylococcus pneumonia (Diplococcus pneumonia), Neisseria gonorrhoea, and Escherichia coli.
  • The intrapleural administration of tetracycline solution as a sclerosing agent for the treatment of recurrent malignant pleural effusions is discussed. The usual dose is 500 mg tetracycline hydrochloride diluted in 30-50 ml saline, instilled via a chest tube into the pleural space. Side effects have not been a problem. Considering the effective control rate, toxicity, availability and ease of administration, intrapleural tetracycline appears safe and effective and is considered the first choice for local therapy.
  • Standardized enamel and dentin specimens were impregnated in aqueous solutions of tetracycline HCl, oxytetracycline HCl or doxycyline HCl, rinsed in water, and stored dry for 200 days. Another series of specimens were impregnated in solutions of doxycyline HCl and then rinsed in tap water for varying periods up to 35 days.

Contra Indications of Tetracycline

  • History of severe hypersensitivity (e.g. anaphylactic reaction) to any other type of betalactam antibacterial agent (penicillins, monobactams and carbapenems).
  • Hemolytic anemia
  • Liver problems
  • Interstitial nephritis
  • Subacute cutaneous lupus erythematosus
  • Systemic lupus erythematosus
  • Tetracycline use should be avoided in pregnant or lactating women, and in children with developing teeth because they may result in permanent staining (dark yellow-gray teeth with a darker horizontal band that goes across the top and bottom rows of teeth), and possibly affect the growth of teeth and bones.
  • Usage during the first 12 weeks of pregnancy does not appear to increase the risk of any major birth defects. There may be a small increased risk for minor birth defects such as an inguinal hernia, but the number of reports is too small to be sure if there actually is any risk.

Dosage of Tetracycline 

Acne

  • 500 mg orally twice a day for 2 weeks or more, depending on the nature and severity of the infection

Bronchitis

  • 500 mg orally every 6 hours for 7 to 10 days, depending on the nature and severity of the infection; may be given for 4 to 5 days a week during winter months as prophylaxis against chronic infectious bronchitis

Brucellosis

  • 500 mg orally 4 times a day for 3 weeks given with streptomycin 1 g IM twice a day the first week and once a day the second week

Chlamydia Infection

  • Uncomplicated urethral, endocervical, or rectal infection: 500 mg orally 4 times a day for at least 7 days
  • The patient’s sexual partner(s) should also be evaluated/treated.
  • Oral doxycycline therapy is preferred by the Centers for Disease Control and Prevention (CDC) for the treatment of chlamydial infections in nonpregnant patients.

Helicobacter pylori Infection

  • 500 mg orally every 6 hours for 14 days given in conjunction with bismuth, metronidazole, and an H2 blocker

Lyme Disease Arthritis

  • 500 mg orally every 6 hours for 14 to 30 days, depending on the nature and severity of the infection

Lyme Disease Carditis

  • 500 mg orally every 6 hours for 14 to 30 days, depending on the nature and severity of the infection

Lyme Disease  Erythema Chronicum Migrans

  • 500 mg orally every 6 hours for 10 to 30 days, depending on the nature and severity of the infection

Pneumonia

  • 500 mg orally every 6 hours for 10 to 21 days, depending on the nature and severity of the infection

Upper Respiratory Tract Infection

  • 500 mg orally every 6 hours for 7 to 10 days, depending on the nature and severity of the infection

Psittacosis

  • 500 mg orally 4 times a day; initial treatment with IV doxycycline may be necessary for seriously ill patients
  • Duration: Treatment should continue at least 10 to 14 days after fever subsides to prevent relapse

Nongonococcal Urethritis

  • 500 mg orally every 6 hours for 7 days

Gonococcal Infection

  • 500 mg orally 4 times a day for 7 days

Cystitis

  • 500 mg orally every 6 hours for 3 to 7 days, depending on the nature and severity of the infection; recommended if no alternatives exist

Side Effects of Tetracycline 

The most common side effects 

More common

Rare

Drug Interactions of Tetracycline

Tetracycline may interact with following drugs, suppliments, & may change the efficacy of drugs

Pregnancy & Lactation of Tetracycline 

FDA Pregnancy Category D 

Pregnancy

Tetracycline is classified pregnancy category D. All tetracyclines have a detrimental effect on the skeletal development and bone growth of the fetus or child. They should not be used in the second half of pregnancy unless benefits from treatment outweigh the risks to the fetus, and their use should be considered only with extreme caution.

Lactation

Tetracyclines also have a serious effect on the dentin and enamel of developing teeth, causing permanent yellow or brown discoloration and enamel hypoplasia. Except when other therapy is ineffective, use in neonates, infants, and children to the age of 8 years, should be avoided.Tetracyclines are distributed in small amounts into breast milk. In general, manufacturers recommend that tetracycline antibiotics not be used in breast feeding mothers due to a theoretical risk of causing teeth discoloration, enamel hypoplasia,

References

By

Amoxicillin, Uses, Dosage, Side Effects, Interactions, Pregnancy

Amoxicillin Anhydrous is the anhydrous form of a broad-spectrum, semisynthetic aminopenicillin antibiotic with bactericidal activity. Amoxicillin binds to and inactivates penicillin-binding proteins (PBPs) located on the inner membrane of the bacterial cell wall. Inactivation of PBPs interferes with the cross-linkage of peptidoglycan chains necessary for bacterial cell wall strength and rigidity. This interrupts bacterial cell wall synthesis and results in the weakening of the bacterial cell wall and causes cell lysis.

A broad-spectrum semisynthetic antibiotic similar to ampicillin except that its resistance to gastric acid permits higher serum levels with oral administration. Amoxicillin is commonly prescribed with clauvanic acid (a beta lactamase inhibitor) as it is susceptible to beta-lacatamase degradation.

Mechanism of Action of Amoxicillin

Amoxicillin is a moderate-spectrum antibiotic active against a wide range of Gram-positive, and a limited range of Gram-negative organisms.Penicillins acylate the penicillin-sensitive transpeptidase C-terminal domain by opening the lactam ring. This inactivation of the enzyme prevents the formation of a cross-link of two linear peptidoglycan strands, inhibiting the third and last stage of bacterial cell wall synthesis. Cell lysis is then mediated by bacterial cell wall autolytic enzymes such as autolysins; it is possible that amoxicllin interferes with an autolysin inhibitor.  It is usually the drug of choice within the class because it is better absorbed, following oral administration, than other beta-lactam antibiotics. Amoxicillin is susceptible to degradation by β-lactamase-producing bacteria, and so may be given with clavulanic acid to increase its susceptability. The incidence of β-lactamase-producing resistant organisms, including E. coli, appears to be increasing. Amoxicillin is sometimes combined with clavulanic acid, a β-lactamase inhibitor, to increase the spectrum of action against Gram-negative organisms, and to overcome bacterial antibiotic resistance mediated through β-lactamase production.

or

Amoxicillin binds to penicillin-binding protein 1A (PBP-1A) located inside the bacterial cell well. Penicillins acylate the penicillin-sensitive transpeptidase C-terminal domain by opening the lactam ring. This inactivation of the enzyme prevents the formation of a cross-link of two linear peptidoglycan strands, inhibiting the third and last stage of bacterial cell wall synthesis. Cell lysis is then mediated by bacterial cell wall autolytic enzymes such as autolysins; it is possible that amoxicllin interferes with an autolysin inhibitor.
The penicillins and their metabolites are potent immunogens because of their ability to combine with proteins and act as haptens for acute antibody-mediated reactions. The most frequent (about 95 percent) or “major” determinant of penicillin allergy is the penicilloyl determinant produced by opening the beta-lactam ring of the penicillin. This allows linkage of the penicillin to protein at the amide group. “Minor” determinants (less frequent) are the other metabolites formed, including native penicillin and penicilloic acids.

Indication of Amoxicillin

  • Amoxicillin is used to treat infections due to bacteria that are susceptible to the effects of amoxicillin.
  • Common bacterial infections that amoxicillin is used for include infections of the
    • middle ear,
    • tonsils,
    • throat,
    • larynx (laryngitis),
    • bronchi (bronchitis),
    • Lungs (pneumonia),
    • urinary tract, and
    • skin.
  • It also is used to treat gonorrhea
  • Bacterial Endocarditis Prophylaxis
  • Chlamydia Infection
  • Helicobacter pylori Infection
  • Lyme Disease – Arthritis
  • Lyme Disease – Carditis
  • Lyme Disease – Erythema Chronicum Migrans
  • Lyme Disease
  • Dental abscesses (as addition to surgical management).
  • Typhoid and paratyphoid fever.
  • Pneumonia
  • throat infections
  • tonsillitis
  • typhoid
  • Bronchitis
  • Sinusitis
  • Dental abscess with spreading cellulitis
  • Prosthetic joint infections
  • Helicobacter pylori eradication
  • Urinary Tract Infection
  • Tonsillitis/Pharyngitis
  • Skin and Structure Infection
  • Cutaneous Bacillus anthracis
  • Anthrax Prophylaxis
  • For the treatment of infections of the ear, nose, and throat, the genitourinary tract, the skin and skin structure, and the lower respiratory tract due to susceptible (only b-lactamase-negative) strains of Streptococcus spp. (a- and b-hemolytic strains only), S. pneumoniae, Staphylococcus spp., H. influenzae, E. coli, P. mirabilis, or E. faecalis. Also for the treatment of acute, uncomplicated gonorrhea (ano-genital and urethral infections) due to N. gonorrhoeae (males and females).
  • The product is indicated for use in clinical cases of mastitis including cases associated with infections with the following major pathogens – Staphylococci (including beta-lactamase producing strains) Streptococci (including S. agalactiae, S. dysgalactiae and S. uberis), Escherichia coli (including beta-lactamase producing strains
  • Treatment and prophylaxis of several bacterial infections

Therapeutic Indications

  • Infections of the Ear, Nose, and Throat: Amoxicillin capsules are indicated in the treatment of infections due to susceptible (ONLY beta-lactamase-negative) isolates of Streptococcus species. (alpha- and beta-hemolytic isolates only), Streptococcus pneumoniae, Staphylococcus spp., or Haemophilus influenzae.
  • Infections of the Genitourinary Tract: Amoxicillin capsules are indicated in the treatment of infections due to susceptible (ONLY beta-lactamase-negative) isolates of Escherichia coli, Proteus mirabilis, or Enterococcus faecalis.
  • Infections of the Skin and Skin Structure: Amoxicillin capsules are indicated in the treatment of infections due to susceptible (ONLY beta-lactamase-negative) isolates of Streptococcus spp. (alpha- and beta-hemolytic isolates only), Staphylococcus spp., or E. coli
  • Infections of the Lower Respiratory Tract: Amoxicillin capsules are indicated in the treatment of infections due to susceptible (ONLY beta-lactamase-negative) isolates of Streptococcus spp. (alpha- and beta-hemolytic isolates only), S. pneumoniae, Staphylococcus spp., or H. influenzae.
  • Amoxicillin capsules in combination with clarithromycin plus lansoprazole as triple therapy, is indicated for the treatment of patients with Helicobacter pylori infection and duodenal ulcer disease (active or 1-year history of a duodenal ulcer) to eradicate H. pylori. Eradication of H. pylori has been shown to reduce the risk of duodenal ulcer recurrence.
  • Oral amoxicillin has been shown to be effective for the treatment of acute, uncomplicated urinary tract infections (UTIs) in some women when given as a single dose.
  • Amoxicillin and ampicillin have been used orally for the treatment of uncomplicated gonorrhea and disseminated gonococcal infections caused by nonpenicillinase-producing strains of N. gonorrhoeae; however, penicillins are no longer recommended for the treatment of uncomplicated or disseminated gonococcal infections and are not included in current CDC guidelines for treatment of the disease.
  • Ampicillin and amoxicillin are used in adults or children for the treatment of typhoid fever (enteric fever) caused by susceptible strains of Salmonella typhi.
  • Amoxicillin is considered a drug of choice for the treatment of erythema migrans and certain other manifestations of early or late Lyme disease.
  • Oral amoxicillin is recommended by the CDC and other clinicians for the treatment of uncomplicated urethral, endocervical, or rectal infections caused by Chlamydia trachomatis in pregnant women who cannot tolerate erythromycins; however, experience with amoxicillin therapy in this infection is limited.
  • Amoxicillin and ampicillin are used for prophylaxis in adults and children who have certain cardiac conditions that put them at high or moderate risk of enterococcal endocarditis and who are undergoing certain GI, biliary, or genitourinary tract surgery or instrumentation likely to cause transient bacteremia and increase their risk of developing enterococcal endocarditis.
  • Amoxicillin and ampicillin are used for prophylaxis of bacterial endocarditis in adults and children with congenital heart disease, rheumatic or other acquired valvular heart dysfunction (even after valvular surgery), prosthetic heart valves (including bioprosthetic and allograft valves), surgically constructed systemic pulmonary shunts or conduits, hypertrophic cardiomyopathy, mitral valve prolapse with valvular regurgitation and/or thickened leaflets, or previous bacterial endocarditis (even in the absence of heart disease) who undergo certain dental and upper respiratory tract procedures likely to cause transient bacteremia and increase the risk of endocarditis caused by viridans streptococci or certain GI, biliary, or genitourinary procedures likely to cause transient bacteremia and increase the risk of enterococcal endocarditis.
  • Amoxicillin and ampicillin are the preferred anti-infectives for prophylaxis of bacterial endocarditis in patients undergoing certain dental and upper respiratory tract procedures who have cardiac conditions that put them at high or moderate risk of endocarditis.
  • Amoxicillin is used as an alternative agent for postexposure prophylaxis following exposure to Bacillus anthracis spores, for the treatment of anthrax when a parenteral regimen is not available (e.g., when there are supply or logistic problems because large numbers of individuals require treatment in a mass casualty setting), and for the treatment of cutaneous anthrax.
  • Amoxicillin and clavulanate potassium is a fixed combination of amoxicillin trihydrate (an aminopenicillin antibiotic) and the potassium salt of clavulanic acid (a beta-lactamase inhibitor); clavulanic acid synergistically expands amoxicillin’s spectrum of activity against many strains of beta-lactamase-producing bacteria.

Active aganist

Gram-positive aerobes:

Enterococcus faecalis

Beta-hemolytic streptococci (Groups A, B, C and G)

Listeria monocytogenes
Species for which acquired resistance may be a problem
Gram-negative aerobes:

Escherichia coli

Haemophilus influenzae

Helicobacter pylori

Proteus mirabilis

Salmonella typhi

Salmonella paratyphi

Pasteurella multocida
Gram-positive aerobes:

Coagulase negative staphylococcus

Staphylococcus aureus

Streptococcus pneumoniae

Viridans group streptococcus
Gram-positive anaerobes:

Clostridium spp.
Gram-negative anaerobes:

Fusobacterium spp.
Other:

Borrelia burgdorferi
Inherently resistant organisms7
Gram-positive aerobes:

Enterococcus faecium†
Gram-negative aerobes:

Acinetobacter spp.

Enterobacter spp.

Klebsiella spp.

Pseudomonas spp.
Gram-negative anaerobes:

Bacteroides spp. (many strains of Bacteroides fragilis are resistant).
Others:

Chlamydia spp.

Mycoplasma spp.

Legionella spp

Contra Indications of Amoxicillin

  • History of severe hypersensitivity (e.g. anaphylactic reaction) to any other type of betalactam antibacterial agent (penicillins, monobactams and carbapenems).
  • Hemolytic anemia
  • Liver problems
  • Interstitial nephritis
  • Subacute cutaneous lupus erythematosus
  • Systemic lupus erythematosus
  • use should be avoided in pregnant or lactating women, and in children with developing teeth because they may result in permanent staining (dark yellow-gray teeth with a darker horizontal band that goes across the top and bottom rows of teeth), and possibly affect the growth of teeth and bones.

Dosage of Amoxicillin

Strengths: 125 mg; 200 mg; 400 mg; 500 mg, 875 mg;600 mg; 775 mg 200 mg/5 mL; 400 mg/5 mL;

Bacterial Endocarditis Prophylaxis

American Heart Association (AHA) recommendations

  • Immediate-release: 2 g orally as a single dose 30 to 60 minutes prior to procedure

Chlamydia Infection

US CDC recommendations

  • 500 mg orally 3 times a day for 7 days in pregnant patients as an alternative to azithromycin

Helicobacter pylori Infection

Immediate-release

  • Dual Therapy: 1 g orally every 8 hours for 14 days in combination with lansoprazole
  • Triple Therapy: 1 g orally every 12 hours for 14 days in combination with clarithromycin and lansoprazole

Pneumonia

Immediate-release

  • Mild, moderate, or severe infection: 500 mg orally every 8 hours or 875 mg every 12 hours

IDSA and American Thoracic Society (ATS) recommendations ,Pneumonia

  • Immediate-release: 1 g orally 3 times a day

Bronchitis

Immediate-release

  • Mild, moderate, or severe infection: 500 mg orally every 8 hours or 875 mg every 12 hours

IDSA and American Thoracic Society (ATS) recommendations ,Pneumonia

  • Immediate-release: 1 g orally 3 times a day

Sinusitis

Immediate-release

  • Mild to moderate infection: 250 mg orally every 8 hours or 500 mg every 12 hours
  • Severe infection: 500 mg orally every 8 hours or 875 mg every 12 hours

Urinary Tract Infection

Immediate-release

  • Mild to moderate infection: 250 mg orally every 8 hours or 500 mg every 12 hours
  • Severe infection: 500 mg orally every 8 hours or 875 mg every 12 hours

Tonsillitis/Pharyngitis

Extended-release

  • 775 mg orally once a day within 1 hour after a meal for 10 days

Skin and Structure Infection

Immediate-release

  • Mild to moderate infection: 250 mg orally every 8 hours or 500 mg every 12 hours
  • Severe infection: 500 mg orally every 8 hours or 875 mg every 12 hours

Pediatric Skin or Soft Tissue Infection

Immediate-Release Formulations ,Mild, Moderate, or Severe Infection

  • 3 months or younger: Up to 30 mg/kg/day orally in divided doses every 12 hours

Immediate-Release Formulations:Mild to Moderate Infection:4 months or older

  • Less than 40 kg: 20 mg/kg/day orally in divided doses every 8 hours or 25 mg/kg/day in divided doses every 12 hours
  • At least 40 kg: 250 mg orally every 8 hours or 500 mg every 12 hours

Severe Infection ;4 months or older

  • Less than 40 kg: 40 mg/kg/day orally in divided doses every 8 hours or 45 mg/kg/day in divided doses every 12 hours
  • At least 40 kg: 500 mg orally every 8 hours or 875 mg every 12 hours.

Immediate-Release Formulations;Mild to Moderate Infection4 months or older

  • Less than 40 kg: 20 mg/kg/day orally in divided doses every 8 hours or 25 mg/kg/day in divided doses every 12 hours
  • At least 40 kg: 250 mg orally every 8 hours or 500 mg every 12 hours

Severe Infection 4 months or older

  • Less than 40 kg: 40 mg/kg/day orally in divided doses every 8 hours or 45 mg/kg/day in divided doses every 12 hours
  • At least 40 kg: 500 mg orally every 8 hours or 875 mg every 12 hours

Urinary Tract Infection

Immediate-Release Formulations ,Mild, Moderate, or Severe Infection

  • 3 months or younger: Up to 30 mg/kg/day orally in divided doses every 12 hours

Pediatric Pneumonia

Immediate-Release Formulations ,Mild, Moderate, or Severe infection

  • 3 months or younger: Up to 30 mg/kg/day orally in divided doses every 12 hours

4 months or older

  • Less than 40 kg: 40 mg/kg/day orally in divided doses every 8 hours or 45 mg/kg/day in divided doses every 12 hours
  • At least 40 kg: 500 mg orally every 8 hours or 875 mg every 12 hours

IDSA and the Pediatric Infectious Diseases Society recommendatio ,Immediate-release formulations ,4 months or older

  • Empiric therapy for presumed bacterial pneumonia: 90 mg/kg/day orally in 2 divided doses; maximum 4 g/day
  • Streptococcus pneumoniae (penicillin minimum inhibitory concentration of 2 mcg/mL or less): 90 mg/kg/day orally in 2 divided doses or 45 mg/kg/day in 3 divided doses
  • Group A Streptococcus: 50 to 75 mg/kg/day orally in 2 divided doses
  • Haemophilus influenza typeable (A to F) or nontypeable: 75 to 100 mg/kg/day orally in 3 divided doses

Pediatric Dose for Bronchitis

Immediate-Release Formulations:Mild, Moderate, or Severe infection

  • 3 months or younger: Up to 30 mg/kg/day orally in divided doses every 12 hours

4 months or older

  • Less than 40 kg: 40 mg/kg/day orally in divided doses every 8 hours or 45 mg/kg/day in divided doses every 12 hours
  • At least 40 kg: 500 mg orally every 8 hours or 875 mg every 12 hours

IDSA and the Pediatric Infectious Diseases Society recommendations
Immediate-release formulations:4 months or older

  • Empiric therapy for presumed bacterial pneumonia: 90 mg/kg/day orally in 2 divided doses; maximum 4 g/day
  • Streptococcus pneumoniae (penicillin minimum inhibitory concentration of 2 mcg/mL or less): 90 mg/kg/day orally in 2 divided doses or 45 mg/kg/day in 3 divided doses
  • Group A Streptococcus: 50 to 75 mg/kg/day orally in 2 divided doses
  • Haemophilus influenza typeable (A to F) or nontypeable: 75 to 100 mg/kg/day orally in 3 divided doses

Tonsillitis/Pharyngitis

12 years or older

  • Extended-release: 775 mg orally once a day within 1 hour after a meal for 10 days

IDSA recommendations

  • Immediate-release: 50 mg/kg (maximum 1000 mg) orally once a day or 25 mg/kg (maximum 500 mg) twice a day

Side Effects of Amoxicillin

The most common side effects 

More common

Rare

Drug Interactions of Amoxicillin

Amoxicillin may interact with following drugs, supplements, & may change the efficacy of drugs

Pregnancy & Lactation Amoxicillin

FDA Pregnancy Category B

Pregnancy

Animal studies do not indicate direct or indirect harmful effects with respect to reproductive toxicity. Limited data on the use of amoxicillin during pregnancy in humans do not indicate an increased risk of congenital malformations. Amoxicillin may be used in pregnancy when the potential benefits outweigh the potential risks associated with treatment.

Lactation

Amoxicillin is excreted into breast milk in small quantities with the possible risk of sensitization. Consequently, diarrhea and fungus infection of the mucous membranes are possible in the breastfed infant, so that breastfeeding might have to be discontinued. Amoxicillin should only be used during breastfeeding after benefit/risk assessment by the physician in charge. There are no data on the effects of amoxicillin on fertility in humans. Reproductive studies in animals have shown no effects on fertility.

References

    1. DrugBank

      http://www.drugbank.ca/drugs/DB01060
      http://www.drugbank.ca/drugs/DB01060#targets
      http://www.drugbank.ca/drugs/DB01060#transporters
      http://www.drugbank.ca/drugs/DB01060#enzymes

    2. HSDB
      https://toxnet.nlm.nih.gov/cgi-bin/sis/search/r?dbs+hsdb:@term+@rn+@rel+26787-78-0
    3. Human Metabolome Database (HMDB)

      http://www.hmdb.ca/metabolites/HMDB0015193

    4. ChemIDplus

      https://chem.nlm.nih.gov/chemidplus/sid/0026787780
      https://chem.sis.nlm.nih.gov/chemidplus/chemidheavy.jsp

    5. EPA DSStox

      https://comptox.epa.gov/dashboard/dsstoxdb/results?search=DTXSID3037044

    6. European Chemicals Agency (ECHA)

      https://echa.europa.eu/substance-information/-/substanceinfo/100.043.625

      https://echa.europa.eu/information-on-chemicals/cl-inventory-database/-/discli/details/24225

    7. ClinicalTrials.gov

      https://clinicaltrials.gov/

    8. DailyMed

      https://dailymed.nlm.nih.gov/dailymed/search.cfm?labeltype=all&query=LANSOPRAZOLE,+AMOXICILLIN+AND+CLARITHROMYCIN

      https://dailymed.nlm.nih.gov/dailymed/search.cfm?labeltype=all&query=AMOXICILLIN
      https://dailymed.nlm.nih.gov/dailymed/search.cfm?labeltype=all&query=AMOXICILLIN+AND+CLAVULANATE+POTASSIUM

    9. FDA Pharm Classes

      https://www.accessdata.fda.gov/spl/data/ae9c98f1-deb9-4d84-990a-bfd055609ab6/ae9c98f1-deb9-4d84-990a-bfd055609ab6.xml

      https://www.fda.gov/ForIndustry/DataStandards/StructuredProductLabeling/ucm162549.htm

    10. LiverTox

      https://livertox.nlm.nih.gov/Amoxicillin.htm

    11. NCIT

      https://ncit.nci.nih.gov/ncitbrowser/ConceptReport.jsp?dictionary=NCI_Thesaurus&ns=NCI_Thesaurus&code=C87367

    12. FDA/SPL Indexing Data

      https://www.fda.gov/ForIndustry/DataStandards/SubstanceRegistrationSystem-UniqueIngredientIdentifierUNII/

    13. EU Community Register of Medicinal Products

      https://ec.europa.eu/health/documents/community-register/html/vo20021.htm

      https://ec.europa.eu/health/documents/community-register/html/ho25661.htm

      https://ec.europa.eu/health/documents/community-register/html/vo3102.htm

    14. FAO/WHO Food Additive Evaluations (JECFA)

      http://apps.who.int/food-additives-contaminants-jecfa-database/chemical.aspx?chemID=6066

    15. FDA Center for Food Safety and Applied Nutrition (CFSAN)

      https://www.fda.gov/Food/IngredientsPackagingLabeling/FoodAdditivesIngredients/ucm091048.htm

    16. FDA Orange Book
      https://www.fda.gov/Drugs/InformationOnDrugs/ucm129662.htm
    17. PubMed Health

      http://www.ncbi.nlm.nih.gov/pubmedhealth/PMHT0008968/

      http://www.ncbi.nlm.nih.gov/pubmedhealth/PMHT0011640/

    18. Springer Nature
      Read more …
    19. WHO ATC

      https://www.whocc.no/atc/

      https://www.whocc.no/atc_ddd_index/

    20. Wikipedia

      https://en.wikipedia.org/wiki/Amoxicillin

      https://pubchem.ncbi.nlm.nih.gov

     

By

Flucloxacillin, Uses, Dosage, Side Effects, Interactions, Pregnancy

Flucloxacillin is a narrow-spectrum, semisynthetic isoxazolyl penicillin with antibacterial activity. Floxacillin binds to and inactivates penicillin-binding proteins (PBPs) located on the inner membrane of the bacterial cell wall. Inactivation of PBPs interferes with the cross-linkage of peptidoglycan chains necessary for bacterial cell wall strength and rigidity. This interrupts bacterial cell wall synthesis and results in the weakening of the bacterial cell wall, eventually causing cell lysis.
Flucloxacillin is only found in individuals that have used or taken this drug. It is an antibiotic analog of cloxacillin. By binding to specific penicillin-binding proteins (PBPs) located inside the bacterial cell wall, flucloxacillin inhibits the third and last stage of bacterial cell wall synthesis. Cell lysis is then mediated by bacterial cell wall autolytic enzymes such as autolysins; it is possible that flucloxacillin interferes with an autolysin inhibitor.
Flucloxacillin (INN) or floxacillin is a narrow-spectrum beta-lactam antibiotic of the penicillin class. It is used to treat infections caused by susceptible Gram-positive bacteria.Flucloxacillin is a narrow-spectrum, semisynthetic isoxazolyl penicillin with antibacterial activity. Floxacillin binds to and inactivates penicillin-binding proteins (PBPs) located on the inner membrane of the bacterial cell wall. Inactivation of PBPs interferes with the cross-linkage of peptidoglycan chains necessary for bacterial cell wall strength and rigidity. This interrupts bacterial cell wall synthesis and results in the weakening of the bacterial cell wall, eventually causing cell lysis.

Mechanism of Action of Flucloxacillin

Flucloxacillin is a penicillin beta-lactam antibiotic used in the treatment of bacterial infections caused by susceptible, usually gram-positive, organisms. The name “penicillin” can either refer to several variants of penicillin available, or to the group of antibiotics derived from the penicillins. Flucloxacillin has in vitro activity against gram-positive and gram-negative aerobic and anaerobic bacteria. The bactericidal activity of Flucloxacillin results from the inhibition of cell wall synthesis and is mediated through flucloxacillin binding to penicillin binding proteins (PBPs). Flucloxacillin is stable against hydrolysis by a variety of beta-lactamases, including penicillinases, and cephalosporinases and extended spectrum beta-lactamases.By binding to specific penicillin-binding proteins (PBPs) located inside the bacterial cell wall, flucloxacillin inhibits the third and last stage of bacterial cell wall synthesis. Cell lysis is then mediated by bacterial cell wall autolytic enzymes such as autolysins; it is possible that flucloxacillin interferes with an autolysin inhibitor.

Or

By binding to specific penicillin-binding proteins (PBPs) located inside the bacterial cell wall, flucloxacillin inhibits the third and last stage of bacterial cell wall synthesis. Cell lysis is then mediated by bacterial cell wall autolytic enzymes such as autolysins; it is possible that flucloxacillininterferes with an autolysin inhibitor.

Indications of Flucloxacillin

It is most commonly used to treat infections.

  • Chest, ear, nose and throat (e.g. tonsillitis, sinusitis, pneumonia)
  • Skin and soft tissue (e.g. boils, burns, wounds, abscesses, infected eczema, infected acne)
  • Staphylococcal skin infections and cellulitis – including impetigo, otitis externa, folliculitis, boils, carbuncles, and mastitis
  • Pneumonia 
  • Osteomyelitis, septic arthritis
  • Septicaemia
  • Empirical treatment for endocarditis
  • Surgical prophylaxis
  • Other infections including those of the heart (endocarditis), bones and joints (osteomyelitis), membranes of the brain (meningitis), guts (enteritis), blood (septicaemia), and the kidney, bladder or urethra
  • Lung abscess
  • Empyema
  • Respiratory tract infections:
  • Osteomyelitis
  • Enteritis
  • Endocarditis
  • Septicaemia
  • Meningitis
  • Urinary tract infection
  • Used to treat bacterial infection by susceptible microorganisms.
  • Other infections caused by flucloxacillin-sensitive organisms

Contra Indications of Flucloxacillin

  • History of severe hypersensitivity (e.g. anaphylactic reaction) to any other type of betalactam antibacterial agent (penicillins, monobactams and carbapenems).
  • Hemolytic anemia
  • Liver problems
  • Interstitial nephritis
  • Subacute cutaneous lupus erythematosus
  • Systemic lupus erythematosus
  • use should be avoided in pregnant or lactating women, and in children with developing teeth because they may result in permanent staining (dark yellow-gray teeth with a darker horizontal band that goes across the top and bottom rows of teeth), and possibly affect the growth of teeth and bones.

Dosage of Flucloxacillin

Strengths: 125 mg; 200 mg; 250 mg ;400 mg;500 mg,  875 mg   125 mg/5 mL; 50 mg/mL; 250 mg/5 mL; ; 200 mg/5 mL; 400 mg/5 mL; 600 mg;

Bacterial Endocarditis

American Heart Association (AHA) recommendations

  • Immediate-release: 2 g orally as a single dose 30 to 60 minutes prior to procedure

Helicobacter pylori Infection

Immediate-release

  • Dual Therapy: 1 g orally every 8 hours for 14 days in combination with lansoprazole
  • Triple Therapy: 1 g orally every 12 hours for 14 days in combination with clarithromycin and lansoprazole

Pneumonia

Immediate-release

  • Mild, moderate, or severe infection: 500 mg orally every 8 hours or 875 mg every 12 hours

IDSA and American Thoracic Society (ATS) recommendations, Pneumonia

  • Immediate-release: 1 g orally 3 times a day

Bronchitis

Immediate-release

  • Mild, moderate, or severe infection: 500 mg orally every 8 hours or 875 mg every 12 hours

Sinusitis

Immediate-release

  • Mild to moderate infection: 250 mg orally every 8 hours or 500 mg every 12 hours
  • Severe infection: 500 mg orally every 8 hours or 875 mg every 12 hours

Urinary Tract Infection

Immediate-release

  • Mild to moderate infection: 250 mg orally every 8 hours or 500 mg every 12 hours
  • Severe infection: 500 mg orally every 8 hours or 875 mg every 12 hours

Tonsillitis/Pharyngitis

Extended-release

  • 775 mg orally once a day within 1 hour after a meal for 10 days

IDSA recommendations

  • Immediate-release: 1000 mg orally once a day or 500 mg orally twice a day

Skin and Structure Infection

Immediate-release

  • Mild to moderate infection: 250 mg orally every 8 hours or 500 mg every 12 hours
  • Severe infection: 500 mg orally every 8 hours or 875 mg every 12 hours

IDSA recommendations

  • Immediate-release: 500 mg orally 3 times a day for 7 to 10 days

Pediatric 

Sinusitis

Immediate-Release Formulations ,Mild, Moderate, or Severe Infection

  • 3 months or younger: Up to 30 mg/kg/day orally in divided doses every 12 hours

Immediate-Release Formulations, Mild to Moderate Infection ,4 months or older

  • Less than 40 kg: 20 mg/kg/day orally in divided doses every 8 hours or 25 mg/kg/day in divided doses every 12 hours
  • At least 40 kg: 250 mg orally every 8 hours or 500 mg every 12 hours

Severe Infection, 4 months or older

  • Less than 40 kg: 40 mg/kg/day orally in divided doses every 8 hours or 45 mg/kg/day in divided doses every 12 hours
  • At least 40 kg: 500 mg orally every 8 hours or 875 mg every 12 hours

Skin or Soft Tissue Infection

Immediate-Release Formulations , Mild, Moderate, or Severe Infection
3 months or younger: Up to 30 mg/kg/day orally in divided doses every 12 hours

Immediate-Release Formulations,Mild to Moderate Infection ,4 months or older

  • Less than 40 kg: 20 mg/kg/day orally in divided doses every 8 hours or 25 mg/kg/day in divided doses every 12 hours
  • At least 40 kg: 250 mg orally every 8 hours or 500 mg every 12 hours

Severe Infection, 4 months or older

  • Less than 40 kg: 40 mg/kg/day orally in divided doses every 8 hours or 45 mg/kg/day in divided doses every 12 hours
  • At least 40 kg: 500 mg orally every 8 hours or 875 mg every 12 hours

Urinary Tract Infection

  • Immediate-Release Formulations, Mild, Moderate, or Severe Infection
  • 3 months or younger: Up to 30 mg/kg/day orally in divided doses every 12 hours

Side Effects of Flucloxacillin

The most common side effects 

More common

Rare

Drug Interactions of  Flucloxacillin

Flucloxacillin may interact with following drugs, supplements, & may change the efficacy of drugs

Pregnancy & Lactation of Flucloxacillin

FDA Pregnancy Category B

Pregnancy

Animal studies with flucloxacillin have shown no teratogenic effects. The product has been in clinical use since 1970 and the limited number of reported cases of use in human pregnancy have shown no evidence of untoward effects. The decision to administer any drug during pregnancy should be taken with the utmost care. Therefore flucloxacillin should only be used in pregnancy when the potential benefits outweigh the potential risks associated with treatment.

Lactation

Trace quantities of flucloxacillin can be detected in breast milk. The possibility of hypersensitivity reactions must be considered in breastfeeding infants. Therefore flucloxacillin should only be administered to a breastfeeding mother when the potential benefits outweigh the potential risks associated with the treatment.

References

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Gemifloxacin, Uses, Dosage, Side Effects, Interactions, Pregnancy

Gemifloxacin is a fluoroquinolone antibiotic with the antimicrobial property. Gemifloxacin enters bacterial cells by diffusion through integral membrane porin pathway before targeting both DNA gyrase and topoisomerase IV, two enzymes critical for DNA replication and repair. This agent binds to the DNA/DNA-gyrase complex and inhibits the A subunits of the enzyme thereby preventing the bacterial chromosome from rejoining. This interferes with DNA replication and repair processes as well as transcription and ultimately leads to bacterial cell death. Gemifloxacin targets at both Gram-positive, -negative and atypical human pathogens.
or
Gemifloxacin is a fourth generation, an oral fluoroquinolone antibiotic used in the therapy of mild-to-moderate respiratory tract infections caused by susceptible organisms. Gemifloxacin has been linked to rare instances of acute liver injury.
or
Gemifloxacin is an oral broad-spectrum quinolone antibacterial agent used in the treatment of acute bacterial exacerbation of chronic bronchitis and mild-to-moderate pneumonia. Gemifloxacin acts by inhibiting DNA synthesis through the inhibition of both DNA gyrase and topoisomerase IV, which are essential for bacterial growth.

Mechanism of Action of Gemifloxacin

Gemifloxacin is a quinolone/fluoroquinolone antibiotic. Gemifloxacin is bactericidal and its mode of action depends on blocking of bacterial DNA replication by binding itself to an enzyme called DNA gyrase, which allows the untwisting required to replicate one DNA double helix into two. Notably, the drug has 100 times higher affinity for bacterial DNA gyrase than for mammalian. Gemifloxacin is a broad-spectrum antibiotic that is active against both Gram-positive and Gram-negative bacteria.

Like other fluoroquinolone anti-infective agents, gemifloxacin inhibits DNA synthesis in susceptible organisms via inhibition of type II DNA topoisomerases (DNA gyrase, topoisomerase IV). However, unlike many other fluoroquinolones, gemifloxacin targets both DNA gyrase and topoisomerase IV in susceptible S. pneumoniae. Although cross-resistance can occur between gemifloxacin and other fluoroquinolones, gemifloxacin may be active against some strains of S. pneumoniae resistant to ciprofloxacin and other fluoroquinolones.
or
The fluroquinolone gemifloxacin was examined for its capacity to modulate secretion of cytokines by human monocytes stimulated with lipopolysaccharide (LPS). Monocytes from six male and two female healthy volunteers were stimulated with LPS, exposed to gemifloxacin and the amounts of secreted IL-1 alpha, IL-1 beta, IL-6, IL-10 and TNF-alpha measured at 3, 6 and 24 h. The results revealed that LPS alone increased secretion of each cytokine significantly. Treatment of the LPS-stimulated monocytes with gemifloxacin resulted in a significant inhibition (p < 0.01) of secretion of each of the cytokines from monocytes of the eight volunteers. Nuclear extracts of the human monocyte cell line, THP-1, were used in the electrophoretic mobility shift assay to determine whether gemifloxacin affects nuclear factor-kappa B (NF-kappa B) activation. In addition, RNA from THP-1 cells was used in Northern blots to determine whether inhibition of secretion of IL-1 beta and TNF-alpha by gemifloxacin occurred at the transcription or translation level. Whereas LPS induced a rapid increase in NF-kappa B activation, gemifloxacin alone did not. Gemifloxacin did not affect the kinetics or decrease the extent of activation. Northern blots indicated that the inhibitory activity of gemifloxacin occurred post-transcription. Thus, gemifloxacin may modulate the immune response by altering secretion of cytokines by human monocytes. Although the concentrations of gemifloxacin used were higher than those observed in the serum of human volunteers treated with the dose under clinical development, it should be taken into consideration that concentrations at tissue and intracellular levels may be considerably higher than serum concentrations.

Indications of Gemifloxacin

  • Acute Bacterial Exacerbation of Chronic Bronchitis (ABECB)
  • Bacterial Infections
  • Community-Acquired Pneumonia (CAP)
  • Gonorrhea
  • Multidrug-resistant Streptococcus pneumoniae infection
  • Bacterial rhinosinusitis
  • Bronchitis
  • Pneumonia
  • Strep Throat

Contra Indications of Gemifloxacin

  • Acute Bacterial Exacerbation of Chronic Bronchitis
  • Bacterial Infections
  • Community-Acquired Pneumonia 
  • Gonorrhea
  • Multidrug-resistant Streptococcus pneumoniae infection
  • Bacterial rhinosinusitis
  • Bronchitis
  • Pneumonia
  • Strep Throat
  • For the treatment of bacterial infection caused by susceptible strains such as S. pneumoniae, H. influenzae, H. parainfluenzae, or M. catarrhalis, S. pneumoniae (including multi-drug resistant strains ), M. pneumoniae, C. pneumoniae, or K. pneumoniae.

Dosage of Gemifloxacin

Strengths: 320 mg

Bronchitis

  • 320 mg orally once a day for 5 days

 Pneumonia

  • 320 mg orally once a day
  • Due to known/suspected S pneumoniae, H influenzae, Mycoplasma pneumoniae, or Chlamydophila pneumoniae infection: 5 days
  • Due to known/suspected multi-drug resistant S pneumoniae (MDRSP), Klebsiella pneumoniae, or M catarrhalis infection: 7 days

Side Effects of Gemifloxacin

The most common side effects 

More common

Rare

Drug Interactions of Gemifloxacin

Gemifloxacin may interact with following drugs, supplements, & may change the efficacy of drugs

Pregnancy & Lactation of Gemifloxacin

FDA pregnancy category  C

Pregnancy

This drug should not be used during pregnancy unless the benefit outweighs the risk to the fetus; safety has not been established during pregnancy.

Lactation

Cartilage erosion and arthropathy have been observed in immature animals giving rise to concern over toxic effects in the developing joints of nursing infants; however, some studies suggest the risk is low. Absorption of the small amounts of fluoroquinolones in milk may be blocked by the calcium in milk; data insufficient to prove or disprove. A nursing mother was administered a single 320 mg oral tablet. A single breast milk sample was collected 3 hours after dosing; milk drug level was about 0.9 mg/L.

References

 

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Gatifloxacin, Uses, Dosage, Side Effects, Interactions, Pregnancy

Gatifloxacin is a synthetic 8-methoxyfluoroquinolone with antibacterial activity against a wide range of gram-negative and gram-positive microorganisms. Gatifloxacin exerts its effect through inhibition of DNA gyrase, an enzyme involved in DNA replication, transcription and repair, and inhibition of topoisomerase IV, an enzyme involved in the partitioning of chromosomal DNA during bacterial cell division.
Gatifloxacin is an antibiotic of the fourth-generation fluoroquinolone family, that like other members of that family, inhibits the bacterial enzymes DNA gyrase and topoisomerase IV. Bristol-Myers Squibb introduced Gatifloxacin in 1999 under the proprietary name Tequin for the treatment of respiratory tract infections, having licensed the medication from Kyorin Pharmaceutical Company of Japan. Allergan produces an eye-drop formulation called Zymar. Gatifloxacin is available as tablets and in various aqueous solutions for intravenous therapy.

Mechanism of Action of Gatifloxacin

Gatifloxacin is a synthetic broad-spectrum 8-methoxyfluoroquinolone antibacterial agent for oral or intravenous administration. is bactericidal and its mode of action depends on blocking of bacterial DNA replication by binding itself to an enzyme called DNA gyrase, which allows the untwisting required to replicate one DNA double helix into two. Notably the drug has 100 times higher affinity for bacterial DNA gyrase than for mammalian. Gatifloxacin is a broad-spectrum antibiotic that is active against both Gram-positive and Gram-negative bacteria. It should be used only to treat or prevent infections that are proven or strongly suspected to be caused by bacteria.

or

The bactericidal action of Gatifloxacin results from inhibition of the enzymes topoisomerase II (DNA gyrase) and topoisomerase IV, which are required for bacterial DNA replication, transcription, repair, and recombination.

Indications of Gatifloxacin

  • Ophthalmic Surgery
  • Conjunctivitis
  • Conjunctivitis, Bacterial
  • For the treatment of bronchitis,
  • Sinusitis,
  • Community-acquired pneumonia,
  • Skin infections (abscesses, wounds) caused by S. pneumoniae, H. influenzae, S. aureus, M. pneumoniae, C. pneumoniae, L. pneumophila, S. pyogenes
  • For the treatment of bronchitis, sinusitis, community-acquired pneumonia, and skin infections (abscesses, wounds) caused by S. pneumoniae, H. influenzae, S. aureus, M. pneumoniae, C. pneumoniae, L. pneumophila, S. pyogenes
  • Infections when due to gatifloxacin-susceptible pathogens: community-acquired pneumonia (mild to moderate) and complicated urinary tract infections (excluding prostatitis and epididymitis.

Contra-Indications of Gatifloxacin

  • History of severe hypersensitivity (e.g. anaphylactic reaction) to any other type of beta-lactam antibacterial agent (penicillins, monobactams, and carbapenems).
  • Hemolytic anemia
  • Liver problems
  • Interstitial nephritis
  • Subacute cutaneous lupus erythematosus
  • Systemic lupus erythematosus
  • use should be avoided in pregnant or lactating women, and in children with developing teeth because they may result in permanent staining (dark yellow-gray teeth with a darker horizontal band that goes across the top and bottom rows of teeth), and possibly affect the growth of teeth and bones.

Dosage of Gatifloxacin

Strengths: 0.5%; 0.3%

Bacterial Conjunctivitis

0.3% solution

  • Days 1 and 2: Instill 1 drop in the affected eye(s) every 2 hours while awake, up to 8 times a day.
  • Days 3 through 7: Instill 1 drop in the affected eye(s) up to 4 times a day while awake.

0.5% solution

  • Day 1: Instill 1 drop in the affected eye(s) every 2 hours while awake, up to 8 times a day.
  • Days 2 through 7: Instill 1 drop in the affected eye(s) 2 to 4 times a day while awake.

Bacterial Conjunctivitis

1 year or older, 0.3% solution

  • Days 1 and 2: Instill 1 drop in the affected eye(s) every 2 hours while awake, up to 8 times a day.
  • Days 3 through 7: Instill 1 drop in the affected eye(s) up to 4 times a day while awake.

0.5% solution

  • Day 1: Instill 1 drop in the affected eye(s) every 2 hours while awake, up to 8 times a day.
  • Days 2 through 7: Instill 1 drop in the affected eye(s) 2 to 4 times a day while awake.

Pediatric Bacterial Conjunctivitis

1 year or older; 0.3% solution

  • Days 1 and 2: Instill 1 drop in the affected eye(s) every 2 hours while awake, up to 8 times a day.
  • Days 3 through 7: Instill 1 drop in the affected eye(s) up to 4 times a day while awake.

0.5% solution

  • Day 1: Instill 1 drop in the affected eye(s) every 2 hours while awake, up to 8 times a day.
  • Days 2 through 7: Instill 1 drop in the affected eye(s) 2 to 4 times a day while awake.

Side Effects of Gatifloxacin

The most common side effects 

More common

Rare

Drug Interactions of Gatifloxacin

Gatifloxacin may interact with following drugs, supplements, & may change the efficacy of drugs

Pregnancy & Lactation of Gatifloxacin

 FDA Pregnancy Category C

Pregnancy

There are no data available on gatifloxacin ophthalmic use in pregnancy to inform a drug-associated risk. However, animal data have shown that administration of oral gatifloxacin throughout organogenesis and during late gestation through lactation did not produce adverse maternal, fetal, or neonatal effects at clinically relevant doses.

Breastfeeding

There are no data available regarding the presence of gatifloxacin in human milk, the effect of gatifloxacin on breastfeeding infants, or the effect of gatifloxacin on milk production. Animal data have shown that gatifloxacin is excreted in breast milk following oral administration;

References

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