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Norfloxacin; Uses, Dosage, Side Effects, Interactions, Pregnan

Norfloxacin is a synthetic, broad-spectrum fluoroquinolone with antibacterial activity. Norfloxacin inhibits the activity of DNA gyrase, thereby blocking bacterial DNA replication. Norfloxacin concentrates in the renal tubules and bladder and is bactericidal against a wide range of aerobic gram-positive and gram-negative organisms.

Norfloxacin is a synthetic fluoroquinolone (FLUOROQUINOLONES) with broad-spectrum antibacterial activity against most gram-negative and gram-positive bacteria. Norfloxacin inhibits bacterial DNA GYRASE.

Norfloxacin is a Quinolone Antimicrobial. The chemical classification of norfloxacin is Quinolones.

Mechanism of Action of Norfloxacin

The bactericidal action of Norfloxacin results from inhibition of the enzymes topoisomerase II (DNA gyrase) and topoisomerase IV, which are required for bacterial DNA replication, transcription, repair, and recombination. Norfloxacinis a broad-spectrum antibiotic that is active against both gram-positive and gram-negative bacterias. The fluorine atom at the 6 position increases potency against gram-negative organisms, and the piperazine moiety at the 7 position is responsible for anti-pseudomonal activity

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).

Indications of Norfloxacin

For the treatment of urinary tract infection
Treatment of acute or chronic complicated pyelonephritis due to susceptible organisms
Uncomplicated urinary tract infections (including cystitis)
Complicated urinary tract infections (restricted use) ^[13]
Uncomplicated urethral and cervical gonorrhea (however this indication is no longer considered to be effective by some experts due to bacterial resistance) ^[14]^[15]
Prostatitis due to Escherichia coli.^[16]
Syphilis treatment – Norfloxacin has not been shown to be effective in the treatment of syphilis. Antimicrobial agents used in high doses for short periods of time to treat gonorrhea may mask or delay the symptoms of incubating syphilis.^[17]
Though the fluoroquinolones are sometimes used to treat typhoid and paratyphoid fever, it should be noted here that norfloxacin had more clinical failures than the other fluoroquinolones .^[18]
Cystitis
Gonococcal cervicitis
Infectious diarrhea
Pyelitis
Pyelonephritis
Spontaneous Bacterial Peritonitis (SBP)
Travelers’ Diarrhea
Urethritis gonococcal

Therapeutic Uses of Norfloxacin

Anti-Bacterial Agents; Enzyme Inhibitors; Nucleic Acid Synthesis InhibitorsOral norfloxacin is used for the treatment of prostatitis caused by E. coli.
Oral norfloxacin is used in adults for the treatment of complicated UTIs caused by susceptible E. coli, K. pneumoniae, P. mirabilis, Ps. aeruginosa, S. marcescens, or E. faecalis.
Oral norfloxacin is used in adults for the treatment of uncomplicated urinary tract infections (UTIs) (including cystitis) caused by susceptible Citrobacter freundii, Enterobacter aerogenes, E. cloacae, Escherichia coli, Klebsiella pneumoniae, Proteus mirabilis, P. vulgaris, … Pseudomonas aeruginosa. The drug also is used orally in adults for the treatment of uncomplicated UTIs caused by susceptible Staphylococcus aureus, S. epidermidis, S. saprophyticus, Streptococcus agalactiae (group B streptococci), or Enterococcus faecalis.
Oral norfloxacin has been used in adults 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).
Norfloxacin has been 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. 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, P. shigelloides, Yersinia enterocolitica, V. parahaemolyticus, or non-O-group V. cholerae.In some cases, travelers’ diarrhea is caused by parasitic enteric pathogens (e.g., Giardia duodenalis (also known as G. lamblia or G. intestinalis), Cryptosporidium parvum, Cyclospora cayetanensis, Entamoeba histolytica, Dientamoeba fragilis) or viral enteric pathogens (e.g., rotavirus, norovirus).
Oral norfloxacin is used for the treatment of shigellosis caused by susceptible Shigella. product
Norfloxacin has been effective when used in the treatment of cholera, including infections caused by Vibrio cholerae serotypes 01 or 0139.
Norfloxacin has been effective when used in adults for the treatment of gastroenteritis caused by susceptible enterotoxigenic E. coli, Aeromonas hydrophila, Plesiomonas shigelloides, Salmonella, Shigella (including Sh. boydii, Sh. dysenteriae, Sh. flexneri, Sh. sonnei), Vibrio cholerae, or V. parahaemolyticus.
Oral norfloxacin is used in adults for the treatment of uncomplicated urinary tract infections (UTIs) (including cystitis) caused by susceptible Morganella morganii, Providencia rettgeri or Serratia marcescens.

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Contra Indications of Norfloxacin

Clostridium difficile infection
Glucose-6-Phosphate Dehydrogenase (G6PD) Deficiency
Low amount of potassium in the blood
Acquired decrease of all cells in the blood
Anemia
Decreased Blood Platelets
Deficiency of Granulocytes a Type of White Blood Cell
Decreased white blood cells
Psychotic disorder
Lower Seizure Threshold
Pseudotumor cerebri
Peripheral neuropathy
Myasthenia Gravis
Disease of Inadequate Blood Flow to the Heart Muscle
Very Rapid Heartbeat – Torsades de Pointes
prolonged QT interval on EKG
Abnormal EKG with QT changes from Birth
Severe Hardening of the Arteries in the Brain
Severe renal impairment
Inflammation of the Tendon
Rupture of a Tendon
Hallucination
Seizures
Involuntary Quivering
abnormal liver function tests
High Pressure Within the Skull
Anemia from Pyruvate Kinase and G6PD Deficiencies
Lung Transplant
Heart Transplant
Allergies to Quinolones

Dosage of Norfloxacin

Strengths: 400 mg

Cystitis

400 mg orally every 12 hours

Duration of Therapy

Complicated urinary tract infections (UTIs):10 to 21 days
Uncomplicated UTIs (cystitis) due to Escherichia coli, Klebsiella pneumoniae, or Proteus mirabilis: 3 days
Uncomplicated UTIs due to other listed organisms: 7 to 10 days

Urinary Tract Infection

400 mg orally every 12 hours

Duration of Therapy

Complicated urinary tract infections (UTIs):10 to 21 days
Uncomplicated UTIs (cystitis) due to Escherichia coli, Klebsiella pneumoniae, or Proteus mirabilis: 3 days
Uncomplicated UTIs due to other listed organisms: 7 to 10 days

Prostatitis

400 mg orally every 12 hours for 28 days

Gonococcal Infection

800 mg orally once

Pyelonephritis

Some experts recommend

Mild infections: 400 mg orally every 12 hours for 14 days

Shigellosis

Infectious Diseases Society of America (IDSA) recommendations: 400 mg orally twice a day

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Duration of Therapy

Immunocompetent patients: 3 days
Immunocompromised patients: 7 to 10 days

Infectious Diarrhea

Infectious Diseases Society of America (IDSA) recommendations: 400 mg orally twice a day

Duration of Therapy

Immunocompetent patients: 3 days
Immunocompromised patients: 7 to 10 days

Salmonella Enteric Fever

IDSA recommendations: 400 mg orally twice a day

Duration of Therapy

Immunocompetent patients: 5 to 7 days
Immunocompromised patients: Up to 14 days (or longer if relapsing) may be required

Salmonella Gastroenteritis

IDSA recommendations: 400 mg orally twice a day

Duration of Therapy

Immunocompetent patients: 5 to 7 days
Immunocompromised patients: Up to 14 days (or longer if relapsing) may be required

Traveler’s Diarrhea

IDSA recommendations: 400 mg orally twice a day
Duration of Therapy: 24 hours to 3 days

Traveler’s Diarrhea Prophylaxis

IDSA recommendations: 400 mg orally once a day

Side Effects of Norfloxacin

The most common

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

Drug Interactions of Norfloxacin

Norfloxacin may interact with following drugs, supplements, & 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

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Pregnancy and Lactation of Norfloxacin

FDA pregnancy Risk Rategory 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.

Lactation

Norfloxacin may pass into breast milk. If you are a breast-feeding mother and are taking this medication, it may affect your baby. Talk to your doctor about whether you should continue breast-feeding. The safety and effectiveness of using this medication have not been established for children under 16 years of age.