Category Archive Drugs A-Z

Ofloxacin is a quinolone/fluoroquinolone antibiotic. Ofloxacin 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. Ofloxacin is a broad-spectrum antibiotic that is active against both Gram-positive and Gram-negative bacteria.

Mechanism of Action of Ofloxacin

Ofloxacin is a quinolone antimicrobial agent. The mechanism of action of ofloxacin and other fluoroquinolone antimicrobials involves inhibition of bacterial topoisomerase IV and DNA gyrase (both of which are type II topoisomerases), enzymes required for DNA replication, transcription, repair and recombination. Ofloxacin has in vitro activity against a wide range of gram-negative and gram-positive microorganisms. Ofloxacin is often bactericidal at concentrations equal to or slightly greater than inhibitory concentrations. Fluoroquinolones, including ofloxacin, differ in chemical structure and mode of action from aminoglycosides, macrolides and beta-lactam antibiotics, including penicillins. Fluoroquinolones may, therefore, be active against bacteria resistant to these antimicrobials. Resistance to ofloxacin due to spontaneous mutation in vitro is a rare occurrence . Although cross-resistance has been observed between ofloxacin and some other fluoroquinolones, some microorganisms resistant to other fluoroquinolones may be susceptible to ofloxacin.

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Quinolones are widely used in infection therapy due to their good antimicrobial characteristics. However, there potential joint chondrotoxicity on immature animals has stood in the way of the therapeutic application of these agents, the exact mechanism of which is still unclear. This study was undertaken to investigate the role of oxidative damage in ofloxacin (one typical quinolones)-induced arthropathy. Chondrocytes from juvenile rabbit joints were incubated with ofloxacin at concentrations of 0, 5, 10, 20, 40 and 80 ug/mL, respectively. The extent of oxidative damage was assessed by measuring the reactive oxygen species level, activities of antioxidant enzymes, and oxidative damage to some macromolecules. It was observed that ofloxacin induced a concentration-dependent increase in intracellular reactive oxygen species production, which may be an early mediator of ofloxacin cytotoxicity. Similarly, ofloxacin resulted in a significant lipid peroxidation, revealed by a concentration-dependent increase in the level of thiobarbituric acid reactive substances. At the same time, ofloxacin induced DNA damage in a concentration-dependent manner for 24 hr measured by comet assay, which may be a cause for overproduction of reactive oxygen species. Furthermore, antioxidant enzyme activities, such as glutathione peroxidase (GPx), catalase and superoxide dismutase (SOD), were rapidly decreased after treatment with ofloxacin. In addition, SOD decline and reactive oxygen species production were strongly inhibited, and the loss in cell viability was partly abated by additional glutathione (GSH), N-acetylcysteine (NAC) and dithiothreitol (DTT). In conclusion, these results clearly demonstrated that ofloxacin could induce oxidative stress, lipid peroxidation and DNA oxidative damage to chondrocytes.

Indications of Ofloxacin

• For the treatment of infections (respiratory tract, kidney, skin, soft tissue, UTI), urethral and cervical gonorrhoea.
• Bladder Infection
• Anthrax
• Anthrax Prophylaxis
• Bone infection
• Conjunctivitis
• Epididymitis
• Hansen’s Disease
• Nongonococcal urethritis
• Otitis Externa
• Prostatitis
• Skin and Subcutaneous Tissue Bacterial Infections
• Spontaneous Bacterial Peritonitis (SBP)
• Travelers’ Diarrhea
• Ulcerative keratitis
• Acute Pelvic inflammatory disease
• Acute, uncomplicated Gonorrhea
• Chronic suppurative Otitis media
• Uncomplicated Cystitis
• Bronchitis
• Campylobacter Gastroenteritis
• Cervicitis
• Chancroid
• Chlamydia Infection
• Epididymitis, Non-Specific
• Epididymitis, Sexually Transmitted
• Gonococcal Infection, Disseminated
• Gonococcal Infection, Uncomplicated
• Joint Infection
• Kidney Infections
• Methicillin-Resistant Staphylococcus Aureus Infection
• Mycobacterium avium-intracellulare, Treatment
• Nongonococcal Urethritis
• Pelvic Inflammatory Disease
• Cervicitis
• Community Acquired Pneumonia (CAP)
• Plague
• Pneumonia
• Prostatitis
• Salmonella Enteric Fever
• Salmonella Gastroenteritis
• Shigellosis
• Skin or Soft Tissue Infection
• Traveler’s Diarrhea
• Tuberculosis, Active
• Urinary Tract Infection

Therapeutic Indications

• Ofloxacin is used in the treatment of acute pelvic inflammatory disease (PID) caused by susceptible C. trachomatis or N. gonorrhoeae, but should not be used if QRNG may be involved or if in vitro susceptibility cannot be tested.
• Ofloxacin is used in adults for the treatment of nongonococcal urethritis and cervicitis caused by Chlamydia trachomatis.
• Ofloxacin is used in adults for the treatment of uncomplicated urinary tract infections (UTIs) (cystitis) caused by susceptible gram-negative bacteria, including Citrobacter diversus,  Enterobacter aerogenes,  Escherichia coli, Klebsiella pneumoniae, … Proteus mirabilis, or Pseudomonas aeruginosa.
• The drug also has been effective in a limited number of adults when used orally for the treatment of uncomplicated urinary tract infections caused by susceptible gram-positive bacteria, including Staphylococcus aureus, S. epidermidis, S. saprophyticus, Enterococcus faecalis (formerly Streptococcus faecalis), viridans streptococci, or Streptococcus agalactiae (group B streptococci). However, because of concerns about emergence of resistant strains of certain gram-positive bacteria (e.g., staphylococci) secondary to widespread use of quinolones, such use should be selective.
• Ofloxacin is used in adults for the treatment of pyelonephritis and other complicated urinary tract infections caused by susceptible gram-negative bacteria, including … C. freundii, Enterobacter, M. morganii,rettgeri. As with other anti-infectives, ofloxacin is more effective in the treatment of uncomplicated UTIs than in complicated infections.
• Ofloxacin is used in adults for the treatment of pyelonephritis and other complicated urinary tract infections caused by susceptible gram-negative bacteria, including C. diversus, E. coli, K. pneumoniae P. mirabilis,Ps. aeruginosa. As with other anti-infectives, ofloxacin is more effective in the treatment of uncomplicated UTIs than in complicated infections. /Included in US product label/
• Ofloxacin is used in adults for the treatment of uncomplicated urinary tract infections (UTIs) (cystitis) caused by susceptible gram-negative bacteria, including … C. freundii,E. cloacae Morganella morganii,
• Ofloxacin is used in adults for the treatment of lower respiratory tract infections, including community-acquired pneumonia (CAP) and acute exacerbations of chronic bronchitis caused by susceptible Haemophilus influenzae or Streptococcus pneumoniae.
• Ofloxacin has been used alone with some success for the treatment of acute exacerbations of bronchopulmonary Ps. aeruginosa infections in adults with cystic fibrosis.
• Ofloxacin also has been effective when used for the treatment of lower respiratory tract infections caused by susceptible Moraxella catarrhalis, S. aureus, viridans streptococci, Enterobacteriaceae, or Ps. aeruginosa.
• Oral ofloxacin has been used in the treatment of Helicobacter pylori infection and duodenal ulcer disease.
• Oral ofloxacin is used for the short-term treatment of travelers’ diarrhea or for the prevention of travelers’ diarrhea in adults traveling for relatively short periods of time to high-risk areas.
• Oral ofloxacin is used for the treatment of shigellosis caused by susceptible Shigella.
• Oral ofloxacin has been effective when used in adults for the treatment of infectious diarrhea caused by susceptible strains of enterotoxigenic E. coli or Shigella.
• Although efficacy of ofloxacin in the treatment of bone and joint infections has not been definitely established, oral ofloxacin has been effective when used in adults for the treatment of mild to moderate bone and joint infections, including osteomyelitis, caused by susceptible Escherichia coli, Enterobacter, Klebsiella oxytoca, K. pneumoniae, Proteus mirabilis, Pseudomonas aeruginosa, Serratia, Staphylococcus aureus, or S. epidermidis.
• Oral ofloxacin has been effective when used alone or in conjunction with amikacin for the treatment of postoperative sternotomy wound or soft tissue infections caused by M. fortuitum. The drug also has been used effectively in a few patients for the treatment of M. fortuitum pulmonary or urinary tract infections.
• Ofloxacin is used as an alternative agent in multiple-drug regimens used for the treatment of multibacillary lepros and also is used in a single-dose rifampin-based multiple-drug regimen for the treatment of single-lesion paucibacillary leprosy
• Fluoroquinolones, including ofloxacin, have been used in multiple-drug regimens for the treatment of active tuberculosis, usually in patients with infections caused by Mycobacterium tuberculosis resistant to first-line agents and in patients intolerant of some first-line agents. Although the potential role of fluoroquinolones and the optimal length of therapy have not been fully defined, the CDC, ATS, and IDSA state that use of fluoroquinolones as alternative agents for the treatment of active tuberculosis can be considered in patients with relapse, treatment failure, or M. tuberculosis resistant to isoniazid and or rifampin or when first-line drugs cannot be tolerated. These experts state that fluoroquinolones should not be considered first-line agents for the treatment of tuberculosis caused by M. tuberculosis susceptible to first-line agents.
• Oral ofloxacin has been recommended as one of several treatment options for the treatment of Legionnaires’ disease.
• Ofloxacin is used for the treatment of epididymitis most likely caused by sexually transmitted enteric bacteria (e.g., E. coli) or when culture or nucleic acid amplification tests are negative for N. gonorrhoeae.
• Oral ofloxacin has been used as follow-up therapy in the treatment of disseminated gonococcal infections caused by susceptible N. gonorrhoeae.
• Oral ofloxacin has been used in men and women for the treatment of acute, uncomplicated urethral and endocervical gonorrhea caused by susceptible Neisseria gonorrhoeae. Although fluoroquinolones (ciprofloxacin, levofloxacin, ofloxacin) were previously considered drugs of choice for the treatment of uncomplicated gonorrhea, the CDC currently states that fluoroquinolones should not be used for the treatment of gonorrhea or any associated infections that may involve Neisseria gonorrhoeae (e.g., pelvic inflammatory disease (PID), epididymitis). Neisseria gonorrhoeae with decreased susceptibility to fluoroquinolones (quinolone-resistant N. gonorrhoeae; QRNG) has been reported with increasing frequency worldwide and is widespread in the US.
• The CDC and others state that ofloxacin can be considered an alternative agent for the treatment of urogenital chlamydial infections caused by C. trachomatis.
• Oral ofloxacin has been used effectively for selective decontamination of the GI tract in granulocytopenic patients. It has been suggested that the drug may be particularly useful for prophylaxis of infection in these patients since it reduces or eradicates gram-negative bacteria from fecal flora but generally does not affect normal anaerobic fecal flora. Oral ofloxacin has been used with some success alone or in conjunction with other anti-infectives for prophylaxis of infection in neutropenic patients with leukemia or other malignancies and for empiric anti-infective therapy in febrile granulocytopenic patients.
• Oral ofloxacin has been effective when used in adults for the treatment of typhoid fever (enteric fever) caused by susceptible strains of Salmonella typhi, including chloramphenicol-resistant strains. However, the precise role of fluoroquinolones compared with other anti-infectives in the treatment of typhoid fever remains to be established.
• Ofloxacin has been used successfully in a limited number of patients for the treatment of various rickettsial infections.
• Fluoroquinolones (e.g., ciprofloxacin, levofloxacin, ofloxacin) have been suggested as alternative agents for the treatment of plague caused by Yersinia pestis and also have been recommended for postexposure prophylaxis following a high risk exposure to Yersinia pestis, including exposure in the context of biologic warfare or bioterrorism. The recommendation for use of fluoroquinolones for treatment or prophylaxis of plague is based on results of in vitro and animal testing. Although human studies are not available, results of in vitro studies indicate that ofloxacin is active against Yersinia pestis and the drug has been effective for the treatment of murine plague infections.
• Ofloxacin otic solution is instilled into the ear canal in patients with tympanostomy tubes for the treatment of acute otitis media caused by susceptible S. aureus, S. pneumoniae, H. influenzae, Moraxella catarrhalis, or P. aeruginosa.
• Ofloxacin otic solution is instilled into the ear canal in patients with perforated tympanic membranes for the treatment of chronic suppurative otitis media (CSOM) caused by susceptible Staphylococcus aureus, Proteus mirabilis, or Pseudomonas aeruginosa. Because commercially available ofloxacin oticsolution is sterile, unlike ciprofloxacin and hydrocortisone otic suspension (which is nonsterile), the ofloxacin otic solution can be used in the treatment of otic infections even when the tympanic membrane is perforated.
• Ofloxacin otic solution is instilled into the ear canal for the treatment of otitis externa caused by susceptible Escherichia coli, Staphylococcus aureus or Pseudomonas aeruginosa.
• Ofloxacin ophthalmic solution is used for the treatment of conjunctivitis caused by susceptible Enterobacter cloacae, Haemophilus influenzae, Proteus mirabilis, Pseudomonas aeruginosa, Staphylococcus aureus, Staphylococcus epidermidis, or Streptococcus pneumoniae. /Included in US product label/
• Ofloxacin ophthalmic solution is used in the treatment of keratitis (corneal ulcers) caused by susceptible Pseudomonas aeruginosa, Propionibacterium acnes, Serratia marcescens, Staphylococcus aureus, S. epidermidis, or Streptococcus pneumoniae; the drug is designated an orphan drug by the US Food and Drug Administration (FDA) for this use. /Included in US product label/

Contra Indications of Ofloxacin

• 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.
• Allergy
• Avoid taking this medicine if you have a known allergy to it or any other fluoroquinolones.
• Avoid if you have a past history of tendinitis or tendon rupture after using this medicine.
• Myasthenia Gravis

Strengths:  200 mg ,400 mg

Uncomplicated Cystitis

• Due to E. coli or K. pneumoniae: 200 mg PO q12hr for 3 days
• Due to other approved pathogens: 200 mg PO q12hr for 7 days

Side Effects of Ofloxacin

The most common 

• Abdominal or stomach cramps and pain (severe)
• diarrhea (watery and severe), which may also be bloody
• pain, inflammation, or swelling in calves, shoulders, or hands
• allergic reactions like skin rash, itching or hives, swelling of the face, lips, or tongue
• pain, swelling, irritation where injected
• sweating
• skin color change, mild diarrhea
• mild nausea
• loss of appetite
• swelling of feet or legs
• chest pain
• constipation
• cough
• difficulty with breathing
• dizziness
• heartburn

More common

• Abdominal or stomach pain, discomfort, or tenderness
• chills or fever
• headache, severe and throbbing
• joint or back pain
• muscle aching or cramping
• muscle pains or stiffness
• chest pressure or squeezing pain in chest
• excessive sweating
• feeling of heaviness, pain, warmth and/or swelling in a leg or in the pelvis
• sudden tingling or coldness in an arm or leg
• sudden slow or difficult speech
• sudden drowsiness or need to sleep
• fast breathing
• sharp pain when taking a deep breath
• fast or slow heartbeat
• coughing up blood
• decreased amount of urine

Rare

• Anxiety
• change in vision
• seizures
• tremors
• weight loss
• chest pain or tightness
• confusion
• cough
• Agitation
• blurred vision
• chest pain or discomfort
• convulsions
• extra heartbeats
• hallucinations
• headache
• irritability
• lightheadedness
• mood or mental changes
• muscle pain or cramps

Drug Interactions of Ofloxacin

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

• antacids that contain aluminum, calcium, or magnesium
• birth control medications
• bismuth subsalicylate
• calcium supplements
• digoxin
• Rosuvastatin
• Duloxetine
• Albuterol
• Topiramate
• Carbamazepin
• Vitamin D3 (cholecalciferol)
• Alprazolam
• Cetirizine
• insulin
• iron supplements
• penicillin
• vitamin A derivatives (e.g. isotretinoin)
• warfarin
• zinc sulfate or gluconate

Pregnancy and Lactation of Ofloxacin

FDA pregnancy category C

Mechanism of Action of Levofloxacin

Levofloxacin is a broad-spectrum antibiotic that is active against both Gram-positive and Gram-negative bacteria. Like all quinolones, it functions by inhibiting the DNA gyrase and topoisomerase IV. Topoisomerase IV is necessary to separate DNA that has been replicated (doubled) prior to bacterial cell division. With the DNA not being separated, the process is stopped, and the bacterium cannot divide. DNA gyrase, on the other hand, is responsible for supercoiling the DNA, so that it will fit in the newly formed cells. Both mechanisms amount to killing the bacterium. Levofloxacin acts as a bactericide.

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Fluoroquinolones prolong the QT interval by blocking voltage-gated potassium channels, especially the rapid component of the delayed rectifier potassium current I(Kr), expressed by HERG (the human ether-a-go-go-related gene). According to the available case reports and clinical studies, moxifloxacin carries the greatest risk of QT prolongation from all available quinolones in clinical practice and it should be used with caution in patients with predisposing factors for Torsades de pointes (TdP).

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Levofloxacin is the L-isomer of the racemate, ofloxacin, a quinolone antimicrobial agent. The antibacterial activity of ofloxacin resides primarily in the L-isomer. The mechanism of action of levofloxacin and other fluoroquinolone antimicrobials involves inhibition of bacterial topoisomerase IV and DNA gyrase (both of which are type II topoisomerases), enzymes required for DNA replication, transcription, repair and recombination.

Indications of Levofloxacin

Levofloxacin is used to treat bacterial infections in adults. These include:

• Pneumonia
• Sinus infection
• Worsening of chronic bronchitis
• Skin infections
• Chronic prostate infection
• Urinary tract infections
• Pyelonephritis (kidney infection)
• Inhalational anthrax
• Plague
• Bacterial Infection
• Urinary Tract Infection
• Anthrax
• Anthrax Prophylaxis
• Bladder Infection
• Bronchitis
• Chlamydia Infection
• Epididymitis, Sexually Transmitted
• Gonococcal Infection, Disseminated
• Gonococcal Infection, Uncomplicated
• Kidney Infections
• Nongonococcal Urethritis
• Nosocomial Pneumonia
• Otitis Media
• Pelvic Inflammatory Disease
• Plague
• Sinusitis
• Skin or Soft Tissue Infection
• Streptococcal Infection
• Tuberculosis, Active
• For the treatment of bacterial conjunctivitis caused by susceptible strains of the following organisms: Corynebacterium species, Staphylococus aureus, Staphylococcus epidermidis, Streptococcus pneumoniae, Streptococcus (Groups C/F/G), Viridans group streptococci, Acinetobacter lwoffii, Haemophilus influenzae, Serratia marcescens.
• Indicated in adults for the treatment of Respiratory Tract Infections (RTIs), Urinary Tract ,Infections (UTIs);
• Skin and soft tissue infections (SSTIs);Anthrax curative treatment;Quinsair is indicated for the management of chronic pulmonary infections due to Pseudomonas aeruginosa in adult patients with cystic fibrosis. Consideration should be given to official guidance on the appropriate use of antibacterial agents.

Therapeutic Indications of Levofloxacin

• Levofloxacin is used for the treatment of acute bacterial sinusitis caused by susceptible Streptococcus pneumoniae, Haemophilus influenzae, or Moraxella catarrhalis.
• Levofloxacin is used for the treatment of community-acquired pneumonia caused by susceptible S. aureus (oxacillin-susceptible strains), S. pneumoniae (including penicillin-resistant strains (penicillinMIC of 2 ug/mL or greater)), H. influenzae, H. parainfluenzae, Klebsiella pneumoniae, Legionella pneumophila, M. catarrhalis, Chlamydophila pneumoniae (formerly Chlamydia pneumoniae), or Mycoplasma pneumoniae.
• Levofloxacin is used for the treatment of mild to moderate complicated urinary tract infections caused by susceptible E. faecalis, Enterobacter cloacae, E. coli, K. pneumoniae, P. mirabilis, or Ps. aeruginosa and acute pyelonephritis caused by susceptible E. coli, including cases with concurrent bacteremia.
• Levofloxacin is used for the treatment of mild to moderate uncomplicated urinary tract infections caused by susceptible E. coli, K. pneumoniae, or S. saprophyticus.
• Levofloxacin is used for the treatment of mild to moderate uncomplicated skin and skin structure infections caused by susceptible S. aureus (oxacillin-susceptible strains) or S. pyogenes (group A beta-hemolytic streptococci) and for the treatment of complicated skin and skin structure infections caused by susceptible S. aureus (oxacillin-susceptible strains), Enterococcus faecalis, S. pyogenes, or Proteus mirabilis.
• Levofloxacin is used for the treatment of nosocomial pneumonia caused by susceptible S. aureus (oxacillin-susceptible strains), S. pneumoniae, H. influenzae, Escherichia coli, K. pneumoniae, Ps. aeruginosa, or Serratia marcescens.
• Levofloxacin is used for the treatment of acute bacterial exacerbations of chronic bronchitis caused by susceptible Staphylococcus aureus (oxacillin-susceptible (methicillin-susceptible) strains), S. pneumoniae, H. influenzae, H. parainfluenzae, or M. catarrhalis.
• Levofloxacin is used for inhalational anthrax (postexposure) to reduce the incidence or progression of disease following exposure to aerosolized Bacillus anthracis.1 Although the efficacy of levofloxacin for postexposure prophylaxis to prevent inhalational anthrax has not been evaluated in human clinical trials, the drug is labeled by the US Food and Drug Administration (FDA) for this indication based on a surrogate end point derived from a primate model of inhalational anthrax that predicts clinical benefit based on plasma levofloxacin concentrations achievable in humans with recommended oral or IV dosages.
• Levofloxacin is used for the treatment of chronic prostatitis caused by susceptible E. coli, E. faecalis, or S. epidermidis (oxacillin-susceptible strains).
• Oral levofloxacin is used for short-term treatment of travelers’ diarrhea or for the prevention of travelers’ diarrhea in adults traveling for relatively short periods of time to high-risk areas.
• Fluoroquinolones (e.g., ciprofloxacin, levofloxacin, ofloxacin) have been suggested as alternative agents for the treatment of plague caused by Yersinia pestis and also have been recommended for postexposure prophylaxis following a high risk exposure to Y. pestis, including exposure in the context of biologic warfare or bioterrorism.
• Levofloxacin is recommended as an alternative for the treatment of acute pelvic inflammatory disease (PID), but should not be used if quinolone-resistant N. gonorrhoeae may be involved or if in vitro susceptibility cannot be tested.
• The CDC recommends oral levofloxacin as an alternative agent for the treatment of nongonococcal urethritis.
• Fluoroquinolones, including levofloxacin, have been used in multiple-drug regimens for the treatment of active tuberculosis, usually in patients with infections caused by Mycobacterium tuberculosis resistant to first-line agents and in patients intolerant of some first-line agents.
• Levofloxacin has been used in a limited of patients for the treatment of meningitis caused by susceptible organisms (e.g., Rhodococcus equi)64 and has been suggested as a possible alternative for use in conjunction with other anti-infectives for the treatment of meningitis caused by susceptible bacteria.
• Levofloxacin is used for the treatment of epididymitis most likely caused by sexually transmitted enteric bacteria (e.g., E. coli) or when culture or nucleic acid amplification tests are negative for N. gonorrhoeae.
• Levofloxacin has been used in the treatment of disseminated gonococcal infections caused by susceptible N. gonorrhoeae.
• Levofloxacin has been used for the treatment of uncomplicated gonorrhea caused by susceptible Neisseria gonorrhoeae. Although fluoroquinolones (ciprofloxacin, levofloxacin, ofloxacin) were previously considered drugs of choice for the treatment of uncomplicated gonorrhea, the CDC currently states that fluoroquinolones should not be used for the treatment of gonorrhea or any associated infections that may involve N. gonorrhoeae (e.g., pelvic inflammatory disease (PID), epididymitis).
• Levofloxacin is used as an alternative for treatment of native or prosthetic valve endocarditis caused by fastidious gram-negative bacilli known as the HACEK group (Actinobacillus actinomycetemcomitans, Cardiobacterium hominis, Eikenella corrodens, Haemophilus aphrophilus, H. influenzae, H. parainfluenzae, H. paraphrophilus, Kingella denitrificans, K. kingae).
• Although levofloxacin has not been evaluated in clinical trials for the treatment of chlamydial infections, levofloxacin is considered an alternative agent for the treatment of urogenital infections caused by C. trachomatis.
• Levofloxacin 0.5% ophthalmic solution is used for the treatment of conjunctivitis caused by susceptible strains of Acinetobacter lwoffii, Corynebacterium spp, Haemophilus influenzae, Serratia marcescens, Staphylococcus aureus, S. epidermidis, groups C, F, and G streptococci, viridans streptococci, or Streptococcus pneumoniae.

Contra-Indications of Levofloxacin

• 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.
• Allergy
• Avoid taking this medicine if you have a known allergy to it or any other fluoroquinolones.
• Avoid if you have a past history of tendinitis or tendon rupture after using this medicine.
• Myasthenia Gravis

Dosage of Levofloxacin

Strengths: 250 mg; 500 mg; 750 mg, 25 mg/mL; 750 mg/150 mL; 250 mg/50 mL; 500 mg/100 mL

Nosocomial Pneumonia

• 750 mg orally or IV every 24 hours for 7 to 14 days

Pneumonia

• For 7- to 14-day regimen: 500 mg orally or IV every 24 hours for 7 to 14 days
• For 5-day regimen: 750 mg orally or IV every 24 hours for 5 days

For the treatment of community-acquired pneumonia

• For 7- to 14-day regimen: Due to methicillin-susceptible S aureus, S pneumoniae (including MDRSP), H influenzae, H parainfluenzae, K pneumoniae, Moraxella catarrhalis, Chlamydophila pneumoniae, Legionella pneumophila, or Mycoplasma pneumonia
• For 5-day regimen: Due to S pneumoniae (excluding MDRSP), H influenzae, H parainfluenzae, M pneumoniae, or C pneumonia

Skin and Structure Infection

• Complicated infection: 750 mg orally or IV every 24 hours for 7 to 14 days
• Uncomplicated infection: 500 mg orally or IV every 24 hours for 7 to 10 days

Duration of Therapy

• Postexposure prophylaxis for B anthracis infection: 60 days

Systemic anthrax

• With possible/confirmed meningitis: At least 2 to 3 weeks or untilthe the patient is clinically stable (whichever is longer)
• When meningitis has been excluded: 2 weeks or until patient is clinically stable (whichever is longer)
• Patients exposed to aerosolized spores will require prophylaxis to complete an antimicrobial regimen of 60 days from onset of illness.

Cutaneous anthrax without systemic involvement

• Bioterrorism-related cases: 60 days
• Naturally-acquired cases: 7 to 10 days

Side Effects of Levofloxacin

The most common 

• Abdominal or stomach cramps and pain (severe)
• diarrhea (watery and severe), which may also be bloody
• pain, inflammation, or swelling in calves, shoulders, or hands
• allergic reactions like skin rash, itching or hives, swelling of the face, lips, or tongue
• pain, swelling, irritation where injected
• sweating
• skin color change, mild diarrhea
• mild nausea
• loss of appetite
• swelling of feet or legs
• chest pain
• constipation
• cough
• difficulty with breathing
• dizziness
• heartburn

More common

• Abdominal or stomach pain, discomfort, or tenderness
• chills or fever
• headache, severe and throbbing
• joint or back pain
• muscle aching or cramping
• muscle pains or stiffness
• chest pressure or squeezing pain in chest
• excessive sweating
• feeling of heaviness, pain, warmth and/or swelling in a leg or in the pelvis
• sudden tingling or coldness in an arm or leg
• sudden slow or difficult speech
• sudden drowsiness or need to sleep
• fast breathing
• sharp pain when taking a deep breath
• fast or slow heartbeat
• coughing up blood
• decreased amount of urine

Rare

• Anxiety
• change in vision
• seizures
• tremors
• weight loss
• chest pain or tightness
• confusion
• cough
• Agitation
• blurred vision
• chest pain or discomfort
• convulsions
• extra heartbeats
• hallucinations
• headache
• irritability
• lightheadedness
• mood or mental changes
• muscle pain or cramps

Drug Interactions of Levofloxacin

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

• antacids containing aluminum hydroxide, calcium, and magnesium hydroxide
• antihistamines (e.g., cetirizine,  hydroxyzine, loratadine)
• antipsychotics (e.g. clozapine, haloperidol, olanzapine, quetiapine, risperidone)
• “azole” antifungals (e.g., itraconazole, ketoconazole, voriconazole)
• calcium supplements and multivitamins containing calcium
• inhaled corticosteroids
• oral corticosteroids (e.g., dexamethasone, hydrocortisone, prednisone)
• diabetes medications (e.g., metformin, nateglinide, rosiglitazone)
• formoterol
• iron supplements and multivitamins containing iron (do not take within 2 hours of levofloxacin)
• macrolide antibiotics (e.g., clarithromycin, erythromycin)
• magnesium supplements (e.g., magnesium hydroxide, magnesium oxide, magnesium sulfate)
• multivitamins
• nilotinib
• nonsteroidal anti-inflammatory medications (e.g., diclofenac, ibuprofen, ketoprofen, naproxen)
• other quinolone antibiotics (e.g., ciprofloxacin, , ofloxacin)
• selective serotonin reuptake inhibitors (SSRIs; e.g., citalopram, duloxetine, fluoxetine, paroxetine, sertraline)
• serotonin antagonists (e.g., granisetron, ondansetron)
• sotalol
• theophyllines (e.g., aminophylline, oxtriphylline, theophylline)
• trimethoprim
• tricyclic antidepressants (e.g., amitriptyline, clomipramine, desipramine, trimipramine)
• tyrosine kinase inhibitors (e.g., dasatinib, imatinib, nilotinib, sunitinib)
• vardenafil
• warfarin

Pregnancy and Lactation of Levofloxacin

FDA Pregnancy Category B 

Pregnancy

Ciprofloxacin is a synthetic broad spectrum fluoroquinolone antibiotic. The chemical classification of ciprofloxacin is Quinolones. Ciprofloxacin binds to and inhibits bacterial DNA gyrase, an enzyme essential for DNA replication. This agent is more active against Gram-negative bacteria than Gram-positive bacteria.

Ciprofloxacin is a broad-spectrum antimicrobial carboxyfluoroquinoline.The bactericidal action of ciprofloxacin results from inhibition of the enzymes topoisomerase II (DNA gyrase) and topoisomerase IV, which are required for bacterial DNA replication, transcription, repair, strand supercoiling repair, and recombination. It is a second-generation fluoroquinolone with a broad spectrum of activity that usually results in the death of the bacteria.

Mechanism of Action of Ciprofloxacin 

Ciprofloxacin usually is bactericidal in action. Like other fluoroquinolone anti-infectives, ciprofloxacininhibits DNA synthesis in susceptible organisms via inhibition of the enzymatic activities of 2 members of the DNA topoisomerase class of enzymes, DNA gyrase and topoisomerase IV. DNA gyrase and topoisomerase IV have distinct essential roles in bacterial DNA replication. DNA gyrase, a type II DNA topoisomerase, was the first identified quinolone target; DNA gyrase is a tetramer composed of 2 GyrA and 2 GyrB subunits. DNA gyrase introduces negative superhelical twists in DNA, an activity important for initiation of DNA replication. DNA gyrase also facilitates DNA replication by removing positive super helical twists. Topoisomerase IV, another type II DNA topoisomerase, is composed of 2 ParC and 2 ParE subunits. DNA gyrase and topoisomerase IV are structurally related; ParC is homologous to GyrA and ParE is homologous to GyrB. Topoisomerase IV acts at the terminal states of DNA replication by allowing for separation of interlinked daughter chromosomes so that segregation into daughter cells can occur. Fluoroquinolones inhibit these topoisomerase enzymes by stabilizing either the DNA-DNA gyrase complex or the DNA-topoismerase IV complex; these stabilized complexes block movement of the DNA replication fork and thereby inhibit DNA replication resulting in cell death.

or

The mechanism by which ciprofloxacin’s inhibition of DNA gyrase or topoisomerase IV results in death in susceptible organisms has not been fully determined. Unlike beta-lactam anti-infectives, which are most active against susceptible bacteria when they are in the logarithmic phase of growth, studies using Escherichia coli and Pseudomonas aeruginosa indicate that ciprofloxacin can be bactericidal during both logarithmic and stationary phases of growth; this effect does not appear to occur with gram-positive bacteria (e.g., Staphylococcus aureus). In vitro studies indicate that ciprofloxacin concentrations that approximate the minimum inhibitory concentration (MIC) of the drug induce filamentation in susceptible organisms; high concentrations of the drug result in enlarged or elongated cells that may not be extensively filamented. Although the bactericidal effect of some fluoroquinolones (e.g., norfloxacin) evidently requires competent RNA and protein synthesis in the bacterial cell, and concurrent use of anti-infectives that affect protein synthesis (e.g., chloramphenicol, tetracyclines) or RNA synthesis (e.g., rifampin) inhibit the in vitro bactericidal activity of these drugs, the bactericidal effect of ciprofloxacin is only partially reduced in the presence of these anti-infectives. This suggests that ciprofloxacin has an additional mechanism of action that is independent of RNA and protein synthesis.

Indications of Ciprofloxacin 

• Urinary tract infections (UTI) caused by certain bacteria such as E. coli.
• Infectious diarrheas caused by E. coli, Campylobacter jejuni, and Shigella bacteria.
• Skin infections
• Lung or airway Infections, for example, TB (tuberculosis), pneumonic and septicemic plague due to Yersinia pestis (Y. pestis), lower respiratory tract infections, and chronic bronchitis)
• Bone and Joint Infections
• Anthrax patients with fever and low white blood cell counts, and intra-abdominal infections.
• Typhoid fever
• Cervical and urethral gonorrhea due to Neisseria gonorrhoeae
• Chronic bacterial prostatitis
• Acute uncomplicated cystitis
• Escherichia urinary tract infection
• Infectious diarrhea
• Neutropenia, Febrile
• Otitis Media (OM)
• Plague caused by Yersinia pestis
• Sinusitis, Acute
• Typhoid fever caused by Salmonella typhi
• Hospital-acquired bacterial pneumonia
• Inhaled anthrax caused by Bacillus anthracis
• Skin-structure infections
• Kidney infections in children
• Uncomplicated Gonorrhea caused by Neisseria gonorrhoeae
• Acute exacerbation of chronic bronchitis caused by Moraxella catarrhalis
• Complicated Intra-Abdominal Infections
• Conjunctivitis caused by Haemophilus influenzae
• Conjunctivitis caused by Staphylococcus epidermidis
• Corneal Ulcers caused by Serratia marcescens
• Corneal Ulcers caused by Staphylococcus aureus
• Corneal Ulcers caused by Staphylococcus epidermidis
• Corneal Ulcers caused by Streptococcus Pneumoniae
• Corneal Ulcers caused by Streptococcus Viridans Group
• Corneal Ulcers caused by pseudomonas aeruginosa
• Lower respiratory tract infection caused by Enterobacter cloacae
• Lower respiratory tract infection caused by Escherichia coli
• Lower respiratory tract infection caused by Haemophilus influenzae
• Lower respiratory tract infection caused by Haemophilus parainfluenzae
• Lower respiratory tract infection caused by Klebsiella pneumoniae
• Lower respiratory tract infection caused by Proteus mirabilis
• Lower respiratory tract infection caused by penicillin-susceptible Streptococcus pneumoniae
• UTI caused by Citrobacter diversus
• UTI caused by Citrobacter frendii
• UTI caused by Entercococcus faecalis
• UTI caused by Enterobacter cloacae
• UTI caused by Klebsiella pneumoniae
• UTI caused by Morganella morganii
• UTI caused by Proteus mirabilis
• UTI caused by Providencia rettgeri
• UTI caused by Pseudomonas aeruginosa
• UTI caused by Serratia marcescens
• UTI caused by methicillin-susceptible Staphylococcus epidermidis
• Acute otitis externa caused by Staphylococcus aureus
• Acute otittis externa caused by Pseudomonas aeruginosa
• Acute, uncomplicated Cystitis caused by Escherichia coli
• Acute, uncomplicated Cystitis caused by Staphylococcus saprophyticus
• Chronic Prostatitis caused by Escherichia coli
• Chronic Prostatitis caused by Proteus mirabilis
• Complicated Pyelonephritis caused by Escherichia coli
• Complicated UTI caused by Escherichia coli

For the treatment of the following infections caused by susceptible organisms: urinary tract infections, acute uncomplicated cystitis, chronic bacterial prostatitis, lower respiratory tract infections, acute sinusitis, skin and skin structure infections, bone and joint infections, complicated intra-abdominal infections (used in combination with metronidazole), infectious diarrhea, typhoid fever (enteric fever), uncomplicated cervical and urethral gonorrhea, and inhalational anthrax (post-exposure).

Therapeutic Indications of Ciprofloxacin 

• Ciprofloxacin (IV, conventional tablets, oral suspension) is used in adults for the treatment of bone and joint infections, including osteomyelitis, caused by susceptible E. cloacae,  Ps. aeruginosa, or S. marcescens.
• Ciprofloxacin (IV, conventional tablets, oral suspension) is used in adults for the treatment of bone and joint infections, including osteomyelitis, caused by susceptible E. aerogenes, E. coli, K. pneumoniae, M. morganii, P. mirabilis. The drug also has been used in adults for the treatment of bone and joint infections caused by susceptible S. aureus, S. epidermidis, other coagulase-negative staphylococci, or Enterococcus faecalis (formerly S. faecalis), but other anti-infectives generally are preferred for these infections. Although resistance to ciprofloxacin has been reported in some strains of oxacillin-resistant S. aureus, oral ciprofloxacin may be a useful alternative to parenteral anti-infectives for the treatment of infections caused by susceptible oxacillin-resistant staphylococci.
• Although only limited experience is available to date, ciprofloxacin is recommended by the American Heart Association (AHA) and Infectious Diseases Society of America (IDSA) as an alternative agent for the treatment of native or prosthetic valve endocarditis caused by fastidious gram-negative bacilli known as the HACEK group (Actinobacillus actinomycetemcomitans, Cardiobacterium hominis, Eikenella corrodens, Haemophilus aphrophilus, H. influenzae, H. parainfluenzae, H. paraphrophilus, Kingella denitrificans, K. kingae).
• Ciprofloxacin is used in adults or children for inhalational anthrax (postexposure) to reduce the incidence or progression of disease following suspected or confirmed exposure to aerosolized B. anthracis spores.
• Natural penicillins (e.g., oral penicillin V, IM penicillin G benzathine, IM penicillin G procaine) generally have been considered drugs of choice for the treatment of mild, uncomplicated cutaneous anthrax caused by susceptible strains of B. anthracis that occurs as the result of naturally occurring or endemic exposure to anthrax, although some clinicians suggest use of oral fluoroquinolones (ciprofloxacin, ofloxacin, levofloxacin), oral amoxicillin, or oral doxycycline if in vitro tests indicate susceptibility.
• A 60-day anti-infective regimen is recommended for postexposure prophylaxis in laboratory workers exposed to confirmed B. anthracis cultures; anti-infective prophylaxis is not necessary for unvaccinated workers employed in biosafety level 3 laboratories that maintain recommended conditions. Following a bioterrorism-related event, use of anti-infective prophylaxis in asymptomatic individuals in the general population is not indicated unless appropriate public health or law-enforcement agencies have ascertained that a risk of exposure to B. anthracis spores exists.699 In addition, the CDC states that postexposure prophylaxis is not indicated for the prevention of cutaneous anthrax, for autopsy personnel examining bodies infected with anthrax when appropriate isolation precautions and procedures are followed, for hospital personnel caring for patients with anthrax, or for individuals who routinely open or handle mail in the absence of a suspicious letter or credible threat.
• The possible benefits of postexposure prophylaxis against anthrax should be weighed against the possible risks to the fetus when choosing an anti-infective for postexposure prophylaxis in pregnant women. The CDC and other experts state that ciprofloxacin should be considered the drug of choice for initial postexposure prophylaxis in pregnant women exposed to B. anthracis spores and that, if in vitro studies indicate that the organism is susceptible to penicillin, then consideration can be given to changing the postexposure regimen to amoxicillin. Women who become pregnant while receiving anti-infective prophylaxis should continue the existing regimen and consult with a healthcare provider or public health official to discuss whether an alternative regimen might be more appropriate.
• Although ciprofloxacin generally is not recommended for use in infants and children, the benefits of ciprofloxacin prophylaxis outweigh the risks for inhalational anthrax (postexposure) and the drug may be used in children to reduce the incidence or progression of disease following exposure to aerosolized B. anthracis spores.
• Ciprofloxacin (IV, conventional tablets, oral suspension) is used for the treatment of clinically apparent inhalational anthrax, cutaneous anthrax, or GI and oropharyngeal anthrax, and for prophylaxis following ingestion of B. anthracis spores in contaminated meat.
• Ciprofloxacin (conventional tablets, oral suspension) is used in adults and children for inhalational anthrax (postexposure) to reduce the incidence or progression of disease following suspected or confirmed exposure to aerosolized Bacillus anthracis spores.
• Ciprofloxacin (IV, conventional tablets, oral suspension) is used in men for the treatment of recurrent urinary tract infections and chronic prostatitis caused by E. coli or P. mirabilis.
• Ciprofloxacin extended-release tablets containing ciprofloxacin hydrochloride are used only for the treatment of uncomplicated urinary tract infections (acute cystitis) caused by susceptible E. coli or K. pneumoniae in adults.
• Ciprofloxacin (IV, conventional tablets, oral suspension) is used in adults for the treatment of skin and skin structure infections caused by susceptible C. freundii, E. cloacae, E. coli, K. oxytoca, K. pneumoniae, M. morganii, P. mirabilis, P. vulgaris, P. stuartii, P. aeruginosa,  S. aureus (oxacillin-susceptible strains), S. epidermidis (oxacillin-susceptible strains), or S. pyogenes (group A beta-hemolytic streptococci). The drug has been effective in the treatment of cellulitis, abscesses, folliculitis, furunculosis, pyoderma, postoperative wound infections, and infected ulcers, burns, or wounds.
• Clinical improvement has occurred when oral ciprofloxacin was used alone for the treatment of acute exacerbations of bronchopulmonary Ps. aeruginosa infections in adults with cystic fibrosis.
• Ciprofloxacin is used for the treatment of nosocomial pneumonia, including hospital-acquired, ventilator-associated, and healthcare-associated pneumonia.
• IV ciprofloxacin is used for the treatment of nosocomial pneumonia caused by susceptible H. influenzae or K. pneumoniae and for the treatment of acute bacterial sinusitis caused by H. influenzae, S. pneumoniae (penicillin-susceptible strains), or M. catarrhalis. Ciprofloxacin (IV, conventional tablets, oral suspension) is used in adults for the treatment of respiratory tract infections, including bronchiectasis, bronchitis, lung abscess, and pneumonia, caused by susceptible  E. cloacae, E. coli, Haemophilus influenzae, H. parainfluenzae K. pneumoniae, P. mirabilis, Ps. aeruginosa, or S. pneumoniae (penicillin-susceptible strains).
• Oral or IV ciprofloxacin is used in the treatment of malignant otitis externa caused by Ps. aeruginosa.
• IV ciprofloxacin has been used with some success for the treatment of meningitis caused by gram-negative bacteria.
• Ciprofloxacin (IV initially followed by oral therapy with conventional tablets or oral suspension) is used in conjunction with oral metronidazole for the treatment of complicated intra-abdominal infections caused by E. coli, Ps. aeruginosa, P. mirabilis, K. pneumoniae, or Bacteroides fragilis.
• Ciprofloxacin (conventional tablets, oral suspension) has been used for the short-term treatment of travelers’ diarrhea or for the prevention of travelers’ diarrhea in adults traveling for relatively short periods of time to high-risk areas. The most common cause of travelers’ diarrhea worldwide is noninvasive enterotoxigenic strains of E. coli (ETEC), but travelers’ diarrhea also can be caused by various other bacteria including enteroaggregative E. coli (EAEC), Campylobacter jejuni, Shigella, Salmonella, A. hydrophila, Plesiomonas shigelloides, Yersinia enterocolitica, or V. parahaemolyticus or non-O-group V. cholerae. In some cases, travelers’ diarrhea is caused by a parasitic enteric pathogen (e.g., Giardia duodenalis (also known as G. lamblia or G. intestinalis), Cryptosporidium parvum, Cyclospora cayetanensis, Entamoeba histolytica, Dientamoeba fragilis) or a viral enteric pathogen (e.g., rotavirus, norovirus).
• Although GI infections caused by Yersinia enterocolitica or Y. pseudotuberculosis usually are self-limited and anti-infective therapy unnecessary, the American Academy of Pediatrics (AAP), US Centers for Disease Control and Prevention (CDC), IDSA, and others recommend use of anti-infectives in immunocompromised individuals or for the treatment of severe infections or when septicemia or other invasive disease occurs.
• Ciprofloxacin (conventional tablets, oral suspension) is used for the treatment of shigellosis caused by susceptible Shigella.
• Although co-trimoxazole generally is the drug of choice for GI infections caused by Cyclospora or Isospora, ciprofloxacin is recommended as an alternative. Ciprofloxacin may not be as effective, but may be useful for the treatment of these infections in patients who cannot tolerate co-trimoxazole.
• Ciprofloxacin (conventional tablets, oral suspension) is used in adults for the treatment of infectious diarrhea caused by susceptible strains of enterotoxigenic E. coli, Campylobacter fetus subsp. jejuni, Salmonella, Shigella (S. flexneri, S. boydii, S. sonnei, S. dysenteriae), or Vibrio.
• Ciprofloxacin is recommended for use in a multiple-drug regimen for the empiric treatment of culture-negative endocarditis.
• A single oral dose of ciprofloxacin (conventional tablets, oral suspension) has been used for the treatment of uncomplicated urethral, endocervical, rectal, or pharyngeal gonorrhea caused by susceptible Neisseria gonorrhoeae.
• Oral ciprofloxacin (administered with or without metronidazole) has been used for induction of remission of mildly to moderately active Crohns disease.
• Oral ciprofloxacin was used with some success in a limited number of women for the treatment of urethral and cervical infections caused by C. trachomatis or Mycoplasma hominis. The drug generally has been ineffective in both men and women for the treatment of urogenital infections caused by Ureaplasma urealyticum.
• Ciprofloxacin (conventional tablets, oral suspension) has been effective in men for the treatment of chancroid, genital ulcers caused by Haemophilus ducreyi.
• Ciprofloxacin is recommended as an alternative to penicillin G for the treatment of infections caused by Capnocytophaga canimorsus.
• Ciprofloxacin has been used in the treatment of brucellosis caused by Brucella melitensis, and some clinicians suggest that a regimen of ciprofloxacin and rifampin can be used as an alternative regimen for the treatment of the disease.
• Some clinicians suggest that fluoroquinolones (e.g., ciprofloxacin) may be an alternative to tetracyclines for the treatment of other Vibrio infections, including gastroenteritis or wound infections caused by V. parahaemolyticus or V. vulnificus.
• Ciprofloxacin is used for perioperative prophylaxis in high risk patients undergoing genitourinary surgery.
• Ciprofloxacin has been used for the treatment of cholera caused by Vibrio cholerae 01 or 0139 in adults or children.
• Ciprofloxacin (conventional tablets, oral suspension) is used in adults for the treatment of typhoid fever (enteric fever) caused by susceptible strains of Salmonella typhi, including chloramphenicol-resistant strains.
• Ciprofloxacin (IV, conventional tablets, oral suspension) is recommended as an alternative to aminoglycosides (streptomycin or gentamicin) for the treatment of tularemia caused by Francisella tularensis.
• Oral ciprofloxacin has been used effectively for selective decontamination of the GI tract in granulocytopenic patients or other debilitated patients (e.g., those with cirrhosis).
• Ciprofloxacin has been used with some success in a limited number of patients for the treatment of various rickettsial infections.
• Ciprofloxacin (IV, conventional tablets, oral suspension) is recommended as an alternative agent for the treatment of plague caused by Yersinia pestis and also is recommended for postexposure prophylaxis following a high-risk exposure to Y. pestis, including exposure in the context of biologic warfare or bioterrorism.
• Ciprofloxacin (conventional tablets, oral suspension) is used in adults to eliminate nasopharyngeal carriage of Neisseria meningitidis.
• Although resistance to ciprofloxacin has been reported in strains of oxacillin-resistant S. aureus, oral ciprofloxacin (750 mg every 12 hours for 7-28 days) has been used to temporarily eliminate oxacillin-resistant S. aureus colonization in patients with serious diseases who were at risk for infection.
• Oral ciprofloxacin (conventional tablets, oral suspension) has been used in the treatment of mycobacterial infections, including those caused by Mycobacterium tuberculosis, M. fortuitum, or M. avium complex (MAC).
• Although ciprofloxacin reportedly has some activity in vitro against Plasmodium falciparum, oral ciprofloxacin has been ineffective when used alone in the treatment of uncomplicated malaria caused by chloroquine-resistant P. falciparum.
• Ciprofloxacin has been effective for the treatment of Legionnaires’ Disease caused by Legionella pneumophila, and some clinicians suggest that ciprofloxacin may be considered a drug of choice for this infection, especially in immunocompromised patients (e.g., transplant recipients).
• Oral ciprofloxacin is considered an alternative agent for the treatment of granuloma inguinale (donovanosis) caused by Klebsiella granulomatis (formerly Calymmatobacterium granulomatis).
• Ciprofloxacin (IV, conventional tablets, oral suspension) has been used as an alternative agent for the treatment of disseminated gonococcal infections caused by susceptible N. gonorrhoeae.
• Ciprofloxacin has been used in the treatment of cat scratch disease caused by Bartonella henselae (formerly Rochalimaea henselae).
• Ciprofloxacin hydrochloride and dexamethasone otic suspension is applied to the ear canal and middle ear for the treatment of acute otitis media caused by susceptible strains of S. aureus, S. pneumoniae, H. influenzae, Moraxella catarrhalis, or Ps. aeruginosa in pediatric patients’ tympanostomy tubes.
• Ciprofloxacin hydrochloride and hydrocortisone otic suspension is applied to the ear canal for the treatment of acute bacterial otitis externa caused by susceptible strains of S. aureus, Ps. aeruginosa, or Proteus mirabilis.
• Ciprofloxacin ophthalmic solution is used in the treatment of conjunctivitis caused by susceptible Staphylococcus aureus , S. epidermidis, Streptococcus pneumoniae, or Haemophilus influenzae.
• Ciprofloxacin ophthalmic solution is used in the treatment of keratitis (corneal ulcer) caused by susceptible Pseudomonas aeruginosa, Serratia marcescens, Staphylococcus aureus, S. epidermidis, Streptococcus pneumoniae, or viridans streptococci,.

Contra Indications of Ciprofloxacin 

• 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.
• Allergy
• Avoid taking this medicine if you have a known allergy to it or any other fluoroquinolones.
• Avoid if you have a past history of tendinitis or tendon rupture after using this medicine.
• Myasthenia Gravis
• Use by those who are hypersensitive to any member of the quinolone class of antimicrobial agents
• Ciprofloxacin is also considered to be contraindicated in children (except for the indications outlined above), in pregnancy, to nursing mothers, and in people with epilepsy or other seizure disorders.

FDA pregnancy  risk category C

Cefuroxime is a semisynthetic, broad-spectrum, beta-lactamase-resistant, second-generation cephalosporin with antibacterial activity. Cefuroxime binds to and inactivates penicillin-binding proteins (PBPs) located on the inner membrane of the bacterial cell wall. PBPs are enzymes involved in the terminal stages of assembling the bacterial cell wall and in reshaping the cell wall during growth and division. Inactivation of PBPs interferes with the cross-linkage of peptidoglycan chains necessary for bacterial cell wall strength and rigidity. This results in the weakening of the bacterial cell wall and causes cell lysis.

By binding to specific penicillin-binding proteins (PBPs) located inside the bacterial cell wall, it 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 cefuroxime interferes with an autolysin inhibitor. This effect is bactericidal.

Mechanism of Action of Cefuroxime

Cefuroxime, a beta-lactam antibiotic similar to penicillins, inhibits the third and final stage of bacterial cell wall synthesis by preferentially binding to specific penicillin-binding proteins (PBPs) that are located inside the bacterial cell wall. Penicillin-binding proteins are responsible for several steps in the synthesis of the cell wall and are found in quantities of several hundred to several thousand molecules per bacterial cell. Penicillin-binding proteins vary among different bacterial species. Thus, the intrinsic activity of cefuroxime, as well as the other cephalosporins and penicillins against a particular organism, depends on their ability to gain access to and bind with the necessary PBP. Like all beta-lactam antibiotics, cefuroxime’s ability to interfere with PBP-mediated cell wall synthesis ultimately leads to cell lysis. Lysis is mediated by bacterial cell wall autolytic enzymes (i.e., autolysins). The relationship between PBPs and autolysins is unclear, but it is possible that the beta-lactam antibiotic interferes with an autolysin inhibitor. Cefuroxime possesses activity against both Gram-positive and Gram-negative bacteria. The drug retains antibacterial activity in the presence of certain beta-lactamases, both penicillinase, and cephalosporins; however hydrolysis by other beta-lactamases, alteration of the PBP, and decreases permeability results in resistance to cefuroxime.

Indications of Cefuroxime

For the treatment of many different types of bacterial infections such as bronchitis, sinusitis, tonsillitis, ear infections, skin infections, gonorrhea, and urinary tract infections.

• Acute bacterial exacerbation of chronic bronchitis
• Bacterial infections
• Bloodstream infections
• Bone and joint infections
• Gonorrhea
• Impetigo
• Pneumonia
• Urinary tract infection
• Skin or soft tissue infection
• Skin and structure infection
• Septicemia
• Meningitis
• Joint infection
• Osteomyelitis
• Surgical prophylaxis
• Tonsillitis/pharyngitis
• Sinusitis
• Intra abdominal infection
• Appendicitis
• Wound infection
• Lower respiratory tract infection maxillary sinusitis
• Otitis media bacterial
• Skin and subcutaneous tissue bacterial infections
• Pharyngitis
• Bladder infection
• Epiglottitis
• Kidney infections
• Otitis media
• Peritonitis
• Sepsis
• Skin and structure /soft tissue  infection

Cefuroxime is usually active against the following microorganisms in vitro.

* All methicillin-resistant S. aureus are resistant to cefuroxime.

Cefixime is a broad-spectrum, third-generation cephalosporin antibiotic derived semisynthetically from the marine fungus Cephalosporium acremonium with antibacterial activity. As does penicillin, the beta-lactam antibiotic cefixime inhibits bacterial cell wall synthesis by disrupting peptidoglycan synthesis, resulting in a reduction in bacterial cell wall stability and bacterial cell lysis. Stable in the presence of a variety of beta-lactamases, this agent is more active against gram-negative bacteria and less active against gram-positive bacteria compared to second-generation cephalosporins. Clinical efficacy has been demonstrated in infections caused by commonly occurring pathogens including Streptococcus pneumoniae, Streptococcus pyogenes, Escherichia coli, Proteus mirabilis, Klebsiella species, Haemophilus influenzae (beta-lactamase positive and negative), Branhamella catarrhalis (beta-lactamase positive and negative) and Enterobacter species. It is highly stable in the presence of beta-lactamase enzymes.

Mechanism of Action of Cefixime

Indications of Cefixime

• Urinary Tract Infection – e.g. cystitis, cystourethritis, uncomplicated pyelonephritis.
• Otitis Media – Otitis caused by Haemophilus influenzae, Moraxella catarrhalis and Streptococcus pyogenes.
• Uncomplicated urinary tract infections caused by Escherichia coli and Proteus mirabilis,
• Otitis media caused by Haemophilus influenzae (beta-lactamase positive and negative strains), Moraxella catarrhalis (most of which are beta-lactamase positive), and S. pyogenes,
• Pharyngitis and tonsillitis caused by S. pyogenes,
• Acute bronchitis and acute exacerbations of chronic bronchitis caused by Streptococcus pneumoniae and Haemophilus influenzae (beta-lactamase positive and negative strains), and
• Uncomplicated gonorrhea (cervical/urethral) caused by Neisseria gonorrhoeae (penicillinase- and non-penicillinase-producing strains).
• Tonsillitis
• Bronchitis
• Sinusitis.
• Pharyngitis caused by Streptococcus pyogenes.
• Pneumonia caused by Streptococcus pneumoniae and Haemophilus influenzae.
• Typhoid fever.
• Enteric fever
• Gonorrhea
• Osteomyelitis
• Prevention of Chronic Kidney Disease (CKD) / Renal Hypodysplasia, Nonsyndromic
• Cervicitis, Vaginitis
• Acute bronchitis and acute exacerbations of chronic bronchitis caused by Streptococcus pneumoniae and Haemophilus influenzae
• Gonococcal Infection – Uncomplicated or Disseminated

Contra-Indications of Cefixime

• Hemolytic anemia
• Liver problems
• Interstitial nephritis
• Subacute cutaneous lupus erythematosus
• Systemic lupus erythematosus
• Allergies cephalosporins & beta-lactams

Dosage of Cefixime

Strengths: 100 mg;  200 mg; 400 mg;100 mg/5 mL;

Urinary Tract Infection

• Uncomplicated infections: 400 mg orally once a day or 200 mg orally every 12 hours

Otitis Media

• Oral suspension, chewable tablets: 400 mg orally once a day or 200 mg orally every 12 hours

Tonsillitis/Pharyngitis

• 400 mg orally once a day or 200 mg orally every 12 hours

Bronchitis

• Acute exacerbations of chronic bronchitis: 400 mg orally once a day or 200 mg orally every 12 hours

Gonococcal Infection 

• Uncomplicated cervical/urethral infections: 400 mg orally as a single dose

Centers for Disease Control and Prevention (CDC) recommendations

• Uncomplicated infections of the cervix, urethra, or rectum: 400 mg orally as a single dose plus (azithromycin  or doxycycline) plus test-of-cure in 1 week

Pediatric Otitis Media

Oral suspension, chewable tablets

• 6 months to 12 years (weighing 45 kg or less): 8 mg/kg orally once a day or 4 mg/kg orally every 12 hours
• Children weighing more than 45 kg or older than 12 years: 400 mg orally once a day or 200 mg orally every 12 hours

Pediatric Urinary Tract Infection

Uncomplicated infections, 6 months to 12 years (weighing 45 kg or less)

• Oral suspension, chewable tablets: 8 mg/kg orally once a day or 4 mg/kg orally every 12 hours
• Children weighing more than 45 kg or older than 12 years: 400 mg orally once a day or 200 mg orally every 12 hours

Pediatric Tonsillitis/Pharyngitis

6 months to 12 years (weighing 45 kg or less)

• Oral suspension, chewable tablets: 8 mg/kg orally once a day or 4 mg/kg orally every 12 hours
• Children weighing more than 45 kg or older than 12 years: 400 mg orally once a day or 200 mg orally every 12 hours

Pediatric Bronchitis

Acute exacerbations of chronic bronchitis, 6 months to 12 years (weighing 45 kg or less)

• Oral suspension, chewable tablets: 8 mg/kg orally once a day or 4 mg/kg orally every 12 hours
• Children weighing more than 45 kg or older than 12 years: 400 mg orally once a day or 200 mg orally every 12 hours

Reconstitution Directions For Oral Suspension

Side Effects of Cefixime

The most common

• Diarrhea
• Abdominal pain
• Swelling of face, lips, eyelids, tongue, hands and feet
• Heartburn
• Indigestion
• skin color change, mild diarrhea
• mild nausea
• loss of appetite
• vaginal discharge and itching
• swelling of feet or legs
• chest pain
• constipation
• cough
• diarrhea or loose stools
• difficulty with breathing
• dizziness
• heartburn

More common

• Abdominal or stomach pain, discomfort, or tenderness
• chills or fever
• difficulty with moving
• a headache, severe and throbbing
• joint or back pain
• muscle aching or cramping
• muscle pains or stiffness
• chest pressure or squeezing pain in the chest
• excessive sweating
• feeling of heaviness, pain, warmth and/or swelling in a leg or in the pelvis
• sudden tingling or coldness in an arm or leg
• sudden slow or difficult speech
• sudden drowsiness or need to sleep
• fast breathing
• sharp pain when taking a deep breath
• fast or slow heartbeat
• coughing up blood
• rust colored urine
• decreased amount of urine

Rare

• Anxiety
• change in vision
• seizures
• abnormal or fast heart rate
• tremors
• weight loss
• chest pain or tightness
• confusion
• a cough
• Agitation
• arm, back, or jaw pain
• blurred vision
• chest pain or discomfort
• convulsions
• extra heartbeats
• fainting
• hallucinations
• headache
• irritability
• lightheadedness
• mood or mental changes
• muscle pain or cramps

Drug Interactions

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

• aminoglycoside antibiotics (e.g., gentamicin, tobramycin)
• probenecid
• cholera vaccine,
• amoxicillin
• BCG vaccine
• Aspirin Low Strength (aspirin) 
• Diphenhydramine
• Rosuvastatin
• Duloxetine
• Albuterol
• Topiramate
• Carbamazepine
• Vitamin D3 (cholecalciferol)
• Alprazolam
• Cetirizine
• Phenprocoumon
• Picosulfuric acid
• Warfarin

Pregnancy Catagory of Cefixime

FDA Pregnancy Category  B

Pregnancy

It is not known if cefoperazone is safe for use by pregnant women. This medication should not be used during pregnancy unless the benefits outweigh the risks. If you become pregnant while taking this medication, contact your doctor immediately.

Lactation

This medication may passes into breast milk. If you are a breastfeeding mother and are taking cefoperazone it may affect your baby. Talk to your doctor about whether you should continue breastfeeding.It is not known if cefoperazone is safe for children under 6 months of age.

Tolperisone is an oral centrally acting muscle relaxant. Tolperisone is a centrally acting muscle relaxant that has been used for the symptomatic treatment of spasticity and muscle spasm . Its precise mechanism is not completely understood, though it blocks sodium and calcium channels. It possesses a high affinity for nervous system tissue, reaching highest concentrations in brain stem, spinal cord and peripheral nerves. Based on existing clinical data, Tolperisone is not sedating and does not interact with alcohol.

Voltage-gated Na⁺ channels (VGSC, Na) are critically important for electrogenesis and nerve impulse conduction. Certain Na⁺ channel isoforms are predominantly expressed in peripheral sensory neurons associated with pain sensation, and the expression and functional properties of Na in peripheral sensory neurons can be dynamically regulated following axonal injury or peripheral inflammation.

Mechanism of Action of Tolperisone 

Being, centrally acting muscle relaxant, tolperisone acts at the level of spinal cord by blocking sodium channels and calcium channels. Tolperisone exerts its spinal reflex inhibitory action predominantly via a pre synaptic inhibition of the transmitter release from the primary afferent endings via a combined action on voltage-gated sodium and calcium channels.

Tolperisone increases the blood supply to skeletal muscles; this action is noteworthy since a muscle contracture may compress the small blood vessels and induce an ischemia leading to release of pain stimulating compounds.Tolperisone causes preferential antinociceptive activity against thermal stimulation that is likely to be attributed to its local anesthetic action.Tolperisone causes muscle relaxation by its action on central nervous system. It also leads to membrane stabilization & has analgesic activity. This muscle relaxation is dose dependant.

or

A heterogeneous group of drugs used to produce muscle relaxation, excepting the neuromuscular blocking agents. They have their primary clinical and therapeutic uses in the treatment of muscle spasm and immobility associated with strains, sprains, and injuries of the back and, to a lesser degree, injuries to the neck. They have been used also for the treatment of a variety of clinical conditions that have in common only the presence of skeletal muscle hyperactivity, for example, the muscle spasms that can occur in MULTIPLE SCLEROSIS.

Indications of Tolperisone 

Tolperisone is indicated for use in the treatment of pathologically increased tone of the cross-striated muscle caused by neurological diseases (damage of the pyramidal tract, multiple sclerosis, myelopathy, encephalomyelitis) and of spastic paralysis and other encephalopathies manifested with muscular dystonia.

Other possible uses include

• Investigated for use/treatment in neurologic disorders, spinal cord injuries, muscle spasm, back pain, and multiple sclerosis.
• Symptomatic treatment of post-stroke spasticity in adults.
• Spondylosis
• Spondylarthrosis
• Cervical and lumbar syndromes
• Arthrosis of the large joints
• Obliterating atherosclerosis of the extremity vessels
• Diabetic angiopathy
• Thromboangiitis obliterans
• Raynaud’s syndrome
• Low back pain syndrome6
• Painful reflex muscle spasm
• Post-cerebral stroke spasticity
• Neurolathyrism
• Trapezitis
• Rehabilitation programmes
• Periarthritis
• Muscle spasm,spasticity due to scliosis.
• Parkinson’s disease
• Paresthesia, muscle pain, coordination disorder, tremor, rigidity, dystonia, ataxia,  nystagmus, strabismus, dysarthria, epileptic seizure

Contra indications of Tolperisone 

• Allergy
• Myasthenia gravis
• Use in children
• Children
• History of allerg
• Hypersensitivity
• Lactation
• Pregnancy
• Renal impairement
• Liver didease

Dosage of Tolperisone 

Tolperisone (HCl)’s dosage details are as follows

Side Effects of Tolperisone 

The Most common

• Loss of muscle coordination
• Diarrhea
• Abdominal pain
• Swelling of face, lips, eyelids, tongue, hands and feet
• Heartburn
• Indigestion
• skin color change, mild diarrhea
• mild nausea
• loss of appetite
• vaginal discharge and itching
• swelling of feet or legs
• chest pain
• constipation
• Frequently passing urine ,Excitement
• Visual disturbance
• cough
• diarrhea or loose stools
• difficulty with breathing
• dizziness
• heartburn

Common

• Abdominal or stomach pain, discomfort, or tenderness
• chills or fever
• difficulty with moving
• headache, severe and throbbing
• joint or back pain
• muscle aching or cramping
• muscle pains or stiffness
• chest pressure or squeezing pain in chest
• excessive sweating
• feeling of heaviness, pain, warmth and/or swelling in a leg or in the pelvis
• sudden tingling or coldness in an arm or leg
• sudden slow or difficult speech
• sudden drowsiness or need to sleep
• fast breathing
• sharp pain when taking a deep breath
• fast or slow heartbeat
• coughing up blood

Rare

• Anxiety
• change in vision
• seizures
• abnormal or fast heart rate
• tremors
• weight loss
• chest pain or tightness
• confusion
• cough
• Agitation
• arm, back, or jaw pain
• blurred vision
• chest pain or discomfort
• convulsions
• extra heartbeats
• fainting
• hallucinations
• headache
• irritability
• lightheadedness
• mood or mental changes
• muscle pain or cramps

Drug Interactions of Tolperisone  

• Allopurinol
• Probenecid
• Methocarbamol
• Tetracyclines

Pregnancy & Lactation of Tolperisone 

TGA pregnancy category C ,FDA Pregnancy Catagory N (unknown)

Pregnancy

It is not known if tolperisone is safe and effective for use in pregnant women. Tell your doctor if you’re pregnant or plan to become pregnant.  Tolperisone should be used during pregnancy only if the potential benefit justifies the potential risk.

Call your doctor right away if you become pregnant while taking this drug.

Lactation

It isn’t known if tolperisone passes into breast milk. If it does, it may cause side effects in a child who is breastfed. Talk to your doctor if you breastfeed your child. You may need to decide whether to stop breastfeeding or stop taking this medication.

References

1. Show More

   • DrugBank
     http://www.drugbank.ca/drugs/DB06264
     http://www.drugbank.ca/drugs/DB06264#enzymes
   • EPA DSStox
     https://comptox.epa.gov/dashboard/dsstoxdb/results?search=DTXSID8023686
   • European Chemicals Agency (ECHA)
     https://echa.europa.eu/substance-information/-/substanceinfo/100.010.889
     https://echa.europa.eu/information-on-chemicals/cl-inventory-database/-/discli/details/54570
   • ClinicalTrials.gov
     https://clinicaltrials.gov/
   • EU Community Register of Medicinal Products
     https://ec.europa.eu/health/documents/community-register/html/ho24242.htm
   • NIST
     http://www.nist.gov/srd/nist1a.cfm
   • Springer Nature
     https://pubchem.ncbi.nlm.nih.gov/substance/341142192
   • WHO ATC
     https://www.whocc.no/atc/
     https://www.whocc.no/atc_ddd_index/
   • Wikipedia
     https://en.wikipedia.org/wiki/Tolperisone

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

   • MeSH
     https://www.ncbi.nlm.nih.gov/mesh/68014049
     http://www.nlm.nih.gov/mesh/meshhome.html
     https://www.ncbi.nlm.nih.gov/mesh/68009125
   • ChEBI
     http://www.ebi.ac.uk/chebi/userManualForward.do#ChEBI%20Ontology
   • KEGG
     http://www.genome.jp/kegg-bin/get_htext?br08303.keg
     http://www.genome.jp/kegg-bin/get_htext?br08330.keg
   • WIPO
     http://www.wipo.int/classifications/ipc/
   • ChEMBL
     https://www.ebi.ac.uk/chembl/target/browser

Baclofen’s mechanism of action is not fully understood, but it is believed that the drug works mainly at the level of the spinal cord to block polysynaptic afferent pathways and, to a lesser extent, monosynaptic afferent pathways. Baclofen may inhibit the transmission of impulses through these pathways by acting as an inhibitory neurotransmitter itself or by hyperpolarizing the primary afferent nerve terminals, which inhibits the release of excitatory neurotransmitters such as glutamate and aspartic acids. Because of large doses of baclofen cause CNS depression, it is postulated that the drug works at supraspinal sites as well. Baclofen has been described as a gamma-aminobutyric acid (GABA) agonist; the drug stimulates the GABA-B receptor. This leads to a decreased release of the neurotransmitters aspartate and glutamate and decreased excitatory input into alpha-motor neurons.

or

Baclofen is a direct agonist at GABAB receptors. The precise mechanism of action of Baclofen is not fully known. It is capable of inhibiting both monosynaptic and polysynaptic reflexes at the spinal level, possibly by hyperpolarization of afferent terminals, although actions at supraspinal sites may also occur and contribute to its clinical effect.

Indications of Baclofen

For Hiccup

• If the hiccup are reached the severe condition the beclofen 5 mg tab  twich daily for 7 day. It must be come in control gradually

Pediatric Cerebral Spasticity

4 years and older ; The starting screening dose for pediatric patients is the same as in adult patients, (50 mcg); however, for very small patients, a screening dose of 25 mcg may be tried first

Intra thecal screening

• Prior to pump implantation for chronic infusion, patients must show a positive response to an intrathecal bolus dose in a screening trial.
• First Screening Dose: 25 to 50 mcg (in a volume of 1 mL) administered into the intrathecal space by barbotage over at least 1 minute; observe patient for 4 to 8 hours for a positive response
• Second Screening Dose: (if no positive response to first screening dose): 75 mcg (in a volume of 1.5 mL) bolus dose administered 24 hours after the first screening dose; observe patient for 4 to 8 hours for a positive response
• Third Screening Dose: (if no positive response to second screening dose): 100 mcg (in a volume of 2 mL) bolus dose administered 24 hours after the second screening dose; observe patient for 4 to 8 hours for a positive response; if no positive response to third screening dose, the patient should not be considered for chronic intrathecal therapy.

Maintenance dose
The same dosing recommendations for adults with spasticity of cerebral origin are used in pediatric patients 4 years and older

• During periodic refills of the pump, the daily dose may be increased by 5% to 20%, but no more than 20%, to maintain adequate symptom control.
• The daily dose may be reduced by 10% to 20% if patients experience side effects.

Maintenance dosage for long term continious infusion

• Pediatric patients 4 to under 12 years may require a lower daily dose: 274 mcg/day, with a range of 24 to 1199 mcg/day
• Age 12 years and older: 22 to 1400 mcg/day, with most patients adequately maintained on 90 to 703 mcg/day; there is limited experience with daily doses greater than 1000 mcg/day

Side effects of Baclofen

More common

• Constipation
• Frequently passing urine
• Loss of muscle coordination
• sleepiness or unusual drowsiness
• clumsiness or unsteadiness
• dizziness
• drowsiness
• dry mouth
• false sense of well-being
• increased watering of mouth
• lightheadedness
• constipation;
• vision changes;
• breast swelling (in men or women); or
• decreased sex drive, impotence, or difficulty having an orgasm.
• blurred vision, tunnel vision, eye pain or swelling, or seeing halos around lights;
• restless muscle movements in your eyes, tongue, jaw, or neck;
• a light-headed feeling, like you might pass out;

Common

• Drowsiness and lightheadedness the day after taking the medicine.
• Confusion.
• Numbed emotions.
• Visual disturbances such as blurred vision or double vision.
• Shaky movements and unsteady walk (ataxia).
• Loss of memory (amnesia).
• Muscle weakness.
• Dizziness.
• Headache.
• Skin rashes.
• Disturbances of the gut such as diarrhoea, constipation, nausea, vomiting or abdominal pain.
• Difficulty in passing urine (urinary retention).
• Changes in sex drive.
• Low blood pressure (hypotension).
• Blood disorders.
• Unexpected aggression, restlessness or irritability (tell your doctor if you experience this).
• Nightmares or hallucinations (tell your doctor if you experience this).

Rare

• Convulsions (seizures)
• hallucinations (seeing or hearing things that are not there)
• increase in muscle spasm, cramping, or tightness
• mood or mental changes
• unusual nervousness or restlessness
• Blurred or double vision
• muscle weakness (severe)
• irritability
• lightheadedness
• mood or mental changes
• shortness of breath or unusually slow or troubled breathingg

Drug Interactions of Baclofen

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

• antihistamines (e.g., cetirizine, doxylamine, diphenhydramine, hydroxyzine, loratadine)
• antipsychotics (e.g., chlorpromazine, clozapine, haloperidol, olanzapine, quetiapine, risperidone)
• aripiprazole
• antidiabetes medications 
• barbiturates (e.g., butalbital, pentobarbital, phenobarbital)
• benzodiazepines (e.g., alprazolam, diazepam, lorazepam)
• carbamazepine
• gabapentin
• levodopa – carbidopa
• magnesium sulfate
• mirtazapine
• monoamine oxidase inhibitors (MAOIs; e.g. rasagiline, selegiline, phenelzine, rasagiline, selegiline, )
• other muscle relaxants
• phenytoin
• selective serotonin reuptake inhibitors (SSRIs; e.g., citalopram, duloxetine, fluoxetine, paroxetine, sertraline)
• tapentadol
• topiramate
• tramadol
• tricyclic antidepressants (e.g., desipramine, nortriptyline)

Pregnancy & Lactation of 

FDA Pregnancy Category C

Pregnancy

It is not known if baclofen is safe and effective for use in pregnant women. Tell your doctor if you’re pregnant or plan to become pregnant. Baclofen should be used during pregnancy only if the potential benefit justifies the potential risk.Call your doctor right away if you become pregnant while taking this drug.

Lactation

It isn’t known if baclofen passes into breast milk. If it does, it may cause side effects in a child who is breastfed. Talk to your doctor if you breastfeed your child. You may need to decide whether to stop breastfeeding or stop taking this medication.

References

1. Show More

   1. ChemIDplus

      https://chem.nlm.nih.gov/chemidplus/sid/0001134470
      https://chem.nlm.nih.gov/chemidplus/sid/0062594369
      https://chem.sis.nlm.nih.gov/chemidplus/chemidheavy.jsp

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

   2. DTP/NCI

      https://dtp.cancer.gov/dtpstandard/servlet/dwindex?searchtype=NSC&outputformat=html&searchlist=755906

      https://dtp.cancer.gov/dtpstandard/servlet/dwindex?searchtype=NSC&outputformat=html&searchlist=329137

   3. DrugBank

      http://www.drugbank.ca/drugs/DB00181
      http://www.drugbank.ca/drugs/DB00181#targets
      http://www.drugbank.ca/drugs/DB00181#transporters

   4. EPA DSStox

      https://comptox.epa.gov/dashboard/dsstoxdb/results?search=DTXSID5022641

      https://www.webmd.com/drugs/2/drug-8615/baclofen-oral/details/list-contraindications

   5. European Chemicals Agency (ECHA)

      https://echa.europa.eu/substance-information/-/substanceinfo/100.013.170

      https://echa.europa.eu/information-on-chemicals/cl-inventory-database/-/discli/details/89100

   6. Human Metabolome Database (HMDB)

      http://www.hmdb.ca/metabolites/HMDB0014327

   7. LiverTox

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

   8. NCIT

      https://ncit.nci.nih.gov/ncitbrowser/ConceptReport.jsp?dictionary=NCI_Thesaurus&ns=NCI_Thesaurus&code=C28858

   9. ClinicalTrials.gov

      https://clinicaltrials.gov/

   10. DailyMed

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

   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=KPYSYYIEGFHWSV-UHFFFAOYSA-N

       http://mona.fiehnlab.ucdavis.edu/spectra/browse?inchikey=KPYSYYIEGFHWSV-QMMMGPOBSA-N

   13. NIST

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

   14. PubMed Health

       http://www.ncbi.nlm.nih.gov/pubmedhealth/PMHT0000200/

       http://www.ncbi.nlm.nih.gov/pubmedhealth/PMHT0009201/

       http://www.ncbi.nlm.nih.gov/pubmedhealth/PMHT0009200/

   15. SpectraBase
       https://spectrabase.com/compound/6v5gDcCOwQy#GolOmpsL9kv
       https://spectrabase.com/compound/6v5gDcCOwQy#FhHrmY9QSEb
   16. Springer Nature
       Read more …

       https://pubchem.ncbi.nlm.nih.gov/substance/341309189

   17. WHO ATC

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

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

   18. Wikipedia

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

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

    

Gabapentin is a unique anticonvulsant that is used as adjunctive therapy in the management of epilepsy and for neuropathic pain syndromes. Therapy with gabapentin is not associated with serum aminotransferase elevations, but several cases of clinically apparent liver injury from gabapentin have been reported. Gabapentin is an Anti-epileptic Agent. The physiologic effect of gabapentin is by means of Decreased Central Nervous System Disorganized Electrical Activity.

Mechanism of Action of Gabapentin

Indications of Gabapentin

• For the management of postherpetic neuralgia in adults and as adjunctive therapy in the treatment of partial seizures with and without secondary generalization in patients over 12 years of age with epilepsy.
• Epilepsy and Treatment of peripheral neuropathic pain
• Treating diabetic peripheral neuropathy
• Treating postherpetic neuralgia
• Treating neuropathic pain associated with spinal cord injury.
• Fibromyalgia
• Pain, Neuropathic
• Postherpetic Neuralgia
• Partial onset seizure Epilepsy,
• Convulsion
• Ankylosing spondylitis
• Pain due to especially musculoskeletal system
• Lumbago
• Pain due to demyelination of nerve
• Paresthesia, itching, numbness or radiating pain.
• Pain due to nerve entrapment
• Low back pain
• PLID
• Polyarthralgia
• Muscles stiffness in nerve diseases
• Multiple joint pain
• Muscles stiffness in spinal
• Muscles stiffness in muscle diseases
• Trigeminal neuralgia
• A headache
• A toothache
• Muscular Aches
• a backache
• minor pain of arthritis temporarily reduces fever
• Polyarthralgia
• Muscles stiffness in nerve diseases
• Frozen shoulder

Therapeutic Indications of Gabapentin

• Neurontin is indicated for: Management of postherpetic neuralgia in adults.
• Neurontin is indicated for: Adjunctive therapy in the treatment of partial onset seizures, with and without secondary generalization, in adults and pediatric patients 3 years and older with epilepsy.
• Gabapentin enacarbil Extended-Release Tablets are indicated for the treatment of moderate-to-severe primary Restless Legs Syndrome (RLS) in adults.
• Gabapentin enacarbil Extended-Release Tablets are indicated for the management of postherpetic neuralgia (PHN) in adults.
• Gabapentin also has been used with some evidence of benefit for the relief of chronic neurogenic pain in a variety of conditions including trigeminal neuralgia, pain, and control of paroxysmal symptoms of multiple sclerosis, complex regional pain syndromes, HIV-related peripheral neuropathy, and neuropathic pain associated with cancer.
• Gabapentin is used for the treatment of pain associated with diabetic neuropathy.
• Gabapentin has been used for the management of vasomotor symptoms in women with breast cancer and in postmenopausal women.
• Therapy with the drug has improved both the frequency and severity of vasomotor symptoms (e.g., hot flushes or flashes) in these women.
• The possible role of gabapentin in the management of vasomotor symptoms associated with antiandrogenic therapy in men with prostate cancer remains to be established. Current evidence of efficacy is limited; well-designed, controlled studies are underway in this population.

Dosage of Gabapentin 

Strengths: 100 mg, 300 mg, 400 mg, 600 mg, 800 mg

Epilepsy

• Initial dose: 300 mg orally on day one, 300 mg orally 2 times a day on day two, then 300 mg orally 3 times a day on day three
• Maintenance dose: 300 to 600 mg orally 3 times a day
• Maximum dose: 3600 mg orally daily (in 3 divided doses)
• Maximum time between doses in the 3 times a day schedule should not exceed 12 hours

Postherpetic Neuralgia

• Initial dose: 300 mg orally on day one, 300 mg orally 2 times the day on day two, then 300 mg orally 3 times a day on day three
• Titrate up as needed for pain relief
• Maximum dose: 1800 mg per day (600 mg orally 3 times a day)

Recommended titration schedule

• Day 1: 300 mg orally with the evening meal
• Day 2: 600 mg orally with the evening meal
• Days 3 through 6: 900 mg orally with the evening meal
• Days 7 through 10: 1200 mg orally with the evening meal
• Days 11 through 14: 1500 mg orally with the evening meal
• Day 15: 1800 mg orally with the evening meal

Gabapentin enacarbil extended-release tablets 

• The recommended dosage is 600 mg orally 2 times a day. Therapy should be initiated at a dose of 600 mg orally in the morning for 3 days of therapy, then increased to 600 mg 2 times a day (1200 mg/day) on day four.

Pediatric Epilepsy

Less than 3 years: Not recommended

Greater than or equal to 3 and less than 12 years

• Starting Dose: Ranges from 10 to 15 mg/kg/day in 3 divided doses
• Effective Dose: Reached by upward titration over a period of approximately 3 days; the effective dose in patients 5 years of age and older is 25 to 35 mg/kg/day in divided doses (3 times a day).
• The effective dose in pediatric patients ages 3 and 4 years is 40 mg/kg/day and given in divided doses (3 times a day). Gabapentin may be administered as the oral solution, capsule, or tablet, or using combinations of these formulations. Dosages up to 50 mg/kg/day have been well tolerated in a long-term clinical study. The maximum time interval between doses should not exceed 12 hours.

Greater than 12 years

• Initial dose: 300 mg orally on day one, 300 mg orally 2 times a day on day two, then 300 mg orally 3 times a day on day three
• Maintenance dose: 900 to 1800 mg orally in 3 divided doses; the dose may be increased up to 1800 mg/day.
• Dosages up to 2400 mg/day have been well tolerated in long-term clinical studies.
• Doses of 3600 mg/day have also been administered to a small number of patients for a relatively short duration, and have been well tolerated. The maximum time between doses in the three times a day schedule should not exceed 12 hours.

Side Effects of Gabapentin

Common

• Disturbances of the gut such as diarrhea, constipation, nausea, vomiting or abdominal pain.
• Drowsiness and lightheadedness the day after taking the medicine.
• Confusion.
• Numbed emotions.
• Visual disturbances such as blurred vision or double vision.
• Shaky movements and unsteady walk (ataxia).
• Loss of memory (amnesia).
• Muscle weakness.
• Dizziness.
• A headache.
• Skin rashes.
• Difficulty in passing urine (urinary retention).
• Changes in sex drive.
• Low blood pressure (hypotension).
• Blood disorders.
• Unexpected aggression, restlessness or irritability (tell your doctor if you experience this).
• Nightmares or hallucinations (tell your doctor if you experience this).

Common

• Constipation
• Frequently passing urine
• Loss of muscle coordination
• sleepiness or unusual drowsiness
• clumsiness or unsteadiness
• dizziness
• drowsiness
• dry mouth
• false sense of well-being
• increased watering of mouth
• lightheadedness
• constipation;
• vision changes;
• breast swelling (in men or women); or
• decreased sex drive, impotence, or difficulty having an orgasm.
• blurred vision, tunnel vision, eye pain or swelling, or seeing halos around lights;
• restless muscle movements in your eyes, tongue, jaw, or neck;
• a light-headed feeling, like you might pass out;

Rare

• Convulsions (seizures)
• hallucinations (seeing or hearing things that are not there)
• increase in muscle spasm, cramping, or tightness
• mood or mental changes
• unusual nervousness or restlessness
• Blurred or double vision
• muscle weakness (severe)
• irritability
• lightheadedness
• mood or mental changes
• shortness of breath or unusually slow or troubled breathing

Drug Interactions of Gabapentin

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

• antacids containing magnesium or aluminum
• cimetidine
• tapentadol
• antihistamines (e.g., cetirizine, doxylamine, diphenhydramine, hydroxyzine, loratadine)
• antipsychotics (e.g., chlorpromazine, clozapine, haloperidol, olanzapine, quetiapine, risperidone
• barbiturates (e.g., butalbital, phenobarbital)
• benzodiazepines (e.g., alprazolam, diazepam, lorazepam)
• clonidine
• general anesthetics
• ketorolac
• mirtazapine
• muscle relaxants
• seizure medications (e.g., carbamazepine, phenytoin)
• selective serotonin reuptake inhibitors (SSRIs; e.g., citalopram, duloxetine, fluoxetine, paroxetine, sertraline)
• tapentadol
• thiazolidinediones (e.g., pioglitazone, rosiglitazone)
• tramadol
• tricyclic antidepressants (e.g., amitriptyline, clomipramine, desipramine, trimipramine)

Pregnancy& Lactation

 Pregnancy Category C 

Pregnancy

This medication should not be used during pregnancy unless the benefits outweigh the risks. If you become pregnant while taking this medication, contact your doctor immediately. Talk to your doctor if you’re pregnant or planning to become pregnant. This drug should only be used if the potential benefit justifies the potential risk to the fetus. Call your doctor if you become pregnant while taking this drug.

Lactation

Gabapentin may pass into breast milk and cause serious side effects in a breastfeeding child. Tell your doctor if you are breastfeeding. You should decide together if you should stop taking this drug or stop breastfeeding.

For children

Gabapentin has not been studied in children for the management of postherpetic neuralgia or restless legs syndrome. It should not be used in people younger than 18 years. This drug should not be used to treat partial seizures in children younger than 3 years.

References

1. Show More

   • DrugBank

     http://www.drugbank.ca/drugs/DB00996
     http://www.drugbank.ca/drugs/DB00996#targets
     http://www.drugbank.ca/drugs/DB00996#enzymes

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

   • HSDB

     https://toxnet.nlm.nih.gov/cgi-bin/sis/search/r?dbs+hsdb:@term+@rn+@rel+60142-96-3

   • ChemIDplus

     https://chem.nlm.nih.gov/chemidplus/sid/0060142963

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

   • DTP/NCI

     https://dtp.cancer.gov/dtpstandard/servlet/dwindex?searchtype=NSC&outputformat=html&searchlist=742194

     https://www.webmd.com/drugs/2/drug-14208-8217/gabapentin-oral/gabapentin-oral/details/list-contraindications

   • EPA DSStox

     https://comptox.epa.gov/dashboard/dsstoxdb/results?search=DTXSID0020074

   • European Chemicals Agency (ECHA)

     https://echa.europa.eu/substance-information/-/substanceinfo/100.056.415

     https://echa.europa.eu/information-on-chemicals/cl-inventory-database/-/discli/details/98676

   • Human Metabolome Database (HMDB)

     http://www.hmdb.ca/metabolites/HMDB0005015

   • ClinicalTrials.gov

     https://clinicaltrials.gov/

   • DailyMed

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

   • FDA Pharm Classes

     https://www.accessdata.fda.gov/spl/data/c3630367-1d10-4b28-a78f-1db79c2c99d5/c3630367-1d10-4b28-a78f-1db79c2c99d5.xml

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

   • LiverTox

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

   • NCIt

     https://ncit.nci.nih.gov/ncitbrowser/ConceptReport.jsp?dictionary=NCI_Thesaurus&ns=NCI_Thesaurus&code=C1108

   • FDA/SPL Indexing Data
     https://www.fda.gov/ForIndustry/DataStandards/SubstanceRegistrationSystem-UniqueIngredientIdentifierUNII/
   • EU Community Register of Medicinal Products

     https://ec.europa.eu/health/documents/community-register/html/ho2421.htm

   • FDA Medication Guides

     https://www.fda.gov/downloads/Drugs/DrugSafety/UCM245196.pdf

     https://www.accessdata.fda.gov/drugsatfda_docs/label/2017/020235s062,020882s045,021129s044lbl.pdf#page=32

   • FDA Orange Book
     https://www.fda.gov/Drugs/InformationOnDrugs/ucm129662.htm
   • MassBank of North America (MoNA)

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

   • NIST

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

   • PubMed Health

     http://www.ncbi.nlm.nih.gov/pubmedhealth/PMHT0010419/

   • Springer Nature
     Read more …
   • The Cambridge Structural Database
     http://www.ccdc.cam.ac.uk/pages/Home.aspx
   • WHO ATC

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

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

   • Wikipedia

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

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

2. 

Mechanism of Action of Pregabalin

Indications of Pregabalin

• Treating diabetic peripheral neuropathy
• Treating postherpetic neuralgia
• Treating neuropathic pain associated with spinal cord injury.
• Epilepsy and Treatment of peripheral neuropathic pain
• Treating diabetic peripheral neuropathy
• Treating postherpetic neuralgia
• Treating neuropathic pain associated with spinal cord injury.
• Fibromyalgia
• Pain, Neuropathic
• Postherpetic Neuralgia
• Partial onset seizure Epilepsy,
• Convulsion
• Ankylosing spondylitis
• Pain due to especially musculoskeletal system
• Lumbago
• Pain due to demyelination of nerve
• Paresthesia, itching, numbness or radiating pain.
• Pain due to nerve instrument
• Low back pain
• PLID
• Polyarthralgia
• Muscles stiffness in nerve diseases
• Multiple joint pain
• Muscles stiffness in spinal
• Muscles stiffness in muscle diseases
• Trigeminal neuralgia
• a headache
• a toothache
• muscular aches
• a backache
• minor pain of arthritis temporarily reduces fever
• Polyarthralgia
• Muscles stiffness in nerve diseases
• Frozen shoulder

Therapeutic Uses

• Pregabalin is indicated for the management of post-herpetic neuralgia.
• Pregabalin is indicated for the management of neuropathic pain associated with diabetic peripheral neuropathy.
• Pregabalin is indicated as an adjunctive therapy for adult patients with partial onset seizures.
• The U.S. Food and Drug Administration has approved Lyrica (pregabalin), the first drug to treat fibromyalgia, a disorder characterized by pain, fatigue and sleep problems.

Therapeutic Indications of Pregabalin

• Pregabalin is used for the management of neuropathic pain associated with diabetic peripheral neuropathy or spinal cord injury, and postherpetic neuralgia. It is not approved for the management of fibromyalgia or as adjunctive therapy for adult partial onset seizures.
• Neuropathic pain: Lyrica is indicated for the treatment of peripheral and central neuropathic pain in adults.
• Epilepsy: Lyrica is indicated as adjunctive therapy in adults with partial seizures with or without secondary generalization.
• Neuropathic pain, Pregabalin Accord is indicated for the treatment of peripheral and central neuropathic pain in adults.
• Epilepsy, Pregabalin Accord is indicated as adjunctive therapy in adults with partial seizures with or without secondary generalization.
• Generalized anxiety disorder; Pregabalin Accord is indicated for the treatment of generalized anxiety disorder (GAD) in adults.
• Epilepsy; Pregabalin Mylan is indicated as adjunctive therapy in adults with partial seizures with or without secondary generalization.
• Generalized Anxiety Disorder; Pregabalin Mylan is indicated for the treatment of Generalised Anxiety Disorder (GAD) in adults
• Neuropathic pain; Pregabalin Mylan Pharma is indicated for the treatment of peripheral and central neuropathic pain in adults.
• Epilepsy –  Pregabalin Mylan Pharma is indicated as adjunctive therapy in adults with partial seizures with or without secondary generalization.
• Generalized Anxiety Disorder –  Pregabalin Mylan Pharma is indicated for the treatment of Generalised Anxiety Disorder (GAD) in adults.
• Neuropathic pain Pregabalin Pfizer is indicated for the treatment of peripheral and central neuropathic pain in adults.
• Epilepsy, Pregabalin Pfizer is indicated as adjunctive therapy in adults with partial seizures with or without secondary generalization.
• Generalized Anxiety Disorder, Pregabalin Pfizer is indicated for the treatment of Generalised Anxiety Disorder (GAD) in adults.
• Neuropathic pain Pregabalin Sandoz is indicated for the treatment of peripheral and central neuropathic pain in adults.
• Epilepsy Pregabalin Sandoz is indicated as adjunctive therapy in adults with partial seizures with or without secondary generalization.
• Generalized Anxiety Disorder, Pregabalin Sandoz is indicated for the treatment of Generalised Anxiety Disorder (GAD) in adults.
• Epilepsy, Pregabalin Sandoz GmbH is indicated as adjunctive therapy in adults with partial seizures with or without secondary generalization.
• Generalized Anxiety Disorder, Pregabalin Sandoz GmbH is indicated for the treatment of Generalised Anxiety Disorder (GAD) in adults.
• Epilepsy, Pregabalin Zentiva is indicated as adjunctive therapy in adults with partial seizures with or without secondary generalization.
• Generalized anxiety disorder, Pregabalin Zentiva is indicated for the treatment of generalized anxiety disorder (GAD) in adults.
• Neuropathic pain, Pregabalin Zentiva k.s. is indicated for the treatment of peripheral and central neuropathic pain in adults.
• Epilepsy, Pregabalin Zentiva k.s. is indicated as adjunctive therapy in adults with partial seizures with or without secondary generalization.
• Generalized anxiety disorder, Pregabalin Zentiva k.s. is indicated for the treatment of generalized anxiety disorder (GAD) in adults.

Contra-Indications of Pregabalin

• Severely Decreased Platelets
• Having Thoughts of Suicide
• Persons to drug class common.
• Avoid abrupt withdrawal
• Renal impairment
• CHF class III, IV NYHA
• Angioedema risk
• Depression
• CNS depressant use
• Alcohol use
• The decrease in the Sharpness of Vision
• Atrioventricular Heart Block
• Chronic Heart Failure
• Suddenly serious symptoms of heart failure
• Rhabdomyolysis
• Drowsiness
• Dizziness
• Fluid Retention in the Legs
• Giant hives
• Moderate to Severe Kidney Impairment
• Muscle Pain or Tenderness with Increase Creatine Kinase
•  Pregnancy

Dosage of Pregabalin

Side Effects of Pregabalin

The most common

• Disturbances of the gut such as diarrhea, constipation, nausea, vomiting or abdominal pain.
• Drowsiness and lightheadedness the day after taking the medicine.
• Vertigo
• Confusion.
• Numbed emotions.
• Visual disturbances such as blurred vision or double vision.
• Shaky movements and unsteady walk (ataxia).
• Loss of memory (amnesia).
• Muscle weakness.
• Dizziness.
• A headache.
• Skin rashes.
• Difficulty in passing urine (urinary retention).
• Changes in sex drive.
• Low blood pressure (hypotension).
• Blood disorders.
• Unexpected aggression, restlessness or irritability (tell your doctor if you experience this).
• Nightmares or hallucinations (tell your doctor if you experience this).

Common

• Constipation
• Frequently passing urine
• Loss of muscle coordination
• sleepiness or unusual drowsiness
• clumsiness or unsteadiness
• dizziness
• drowsiness
• dry mouth
• false sense of well-being
• increased watering of mouth
• lightheadedness
• constipation;
• vision changes;
• breast swelling (in men or women); or
• decreased sex drive, impotence, or difficulty having an orgasm.
• blurred vision, tunnel vision, eye pain or swelling, or seeing halos around lights;
• restless muscle movements in your eyes, tongue, jaw, or neck;
• a light-headed feeling, like you, might pass out;

Rare

• Convulsions (seizures)
• hallucinations (seeing or hearing things that are not there)
• increase in muscle spasm, cramping, or tightness
• mood or mental changes
• unusual nervousness or restlessness
• Blurred or double vision
• muscle weakness (severe)
• irritability
• lightheadedness
• mood or mental changes
• shortness of breath or unusually slow or troubled breathing

Drug Interactions of Pregabalin

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

• antacids containing magnesium or aluminum
• cimetidine
• tapentadol
• antihistamines (e.g., cetirizine, doxylamine, diphenhydramine, hydroxyzine, loratadine)
• antipsychotics (e.g., chlorpromazine, clozapine, haloperidol, olanzapine, quetiapine, risperidone
• barbiturates (e.g., butalbital, phenobarbital)
• benzodiazepines (e.g., alprazolam, diazepam, lorazepam)
• clonidine
• general anesthetics
• ketorolac
• mirtazapine
• muscle relaxants
• seizure medications (e.g., carbamazepine, phenytoin)
• selective serotonin reuptake inhibitors (SSRIs; e.g., citalopram, duloxetine, fluoxetine, paroxetine, sertraline)
• tapentadol
• thiazolidinediones (e.g., pioglitazone, rosiglitazone)
• tramadol
• tricyclic antidepressants (e.g., amitriptyline, clomipramine, desipramine, trimipramine)

Pregnancy & Lactation of Pregabalin