Drug Detail

Ofloxacin

Last Updated June 10, 2016

Trade Names

Tarivid, Tafloc, Apex-Ofloxacin

Drug Classification

Fluoroquinolone broad-spectrum antimicrobial

Formulations

200 mg, 400 mg tablets; 200 mg/100 mL as hydrochloride for infusion

Indications and Pharmacology

Indication: treatment of mild to moderate infections caused by susceptible bacterial strains; potent gram-negative activity and active against mycobacteria. Used in treatment of multidrug-resistant tuberculosis in combination with other second-line drugs.

Mechanism of action: inhibition of topoisomerase IV and DNA gyrase enzymes, disrupting bacterial DNA replication, transcription, repair, recombination.

Pharmacokinetics: rapidly absorbed from gastrointestinal tract and widely distributed throughout body; Tmax 1-2 hrs, half-life ~ 9 hours.

Dosage

Adult Dose for Tuberculosis: 800 mg once daily or 400 mg twice daily.

Taking tablet formulation with food delays absorption but does not affect peak serum concentration. Liberal ingestion of fluids is encouraged but administration with multivitamins or dairy products should be avoided.*

Use in Renal or Hepatic Insufficiency:

  • Renal impairment: < 30 mL/min or for patients receiving haemodialysis: 600-800 mg orally 3 times per week.*
  • Reduced liver function: do not exceed maximum dose of 400 mg/day.

Use in Pregnancy and Breastfeeding: Pregnancy Category C; use only if benefits outweigh potential risk to the foetus. May be excreted in breast milk, with potential for serious adverse reactions in breast-fed infants.

Use in Children: 15-20 mg/kg/day, oral (safety not established)*

Maximum dose: 800 mg/day.

Warnings

Contraindicated in patients with hypersensitivity to ofloxacin or any other quinolone antimicrobials.

Associated with increased risk of tendinitis and tendon rupture, especially in patients > 60 years, taking corticosteroid drugs, or with kidney, heart, or lung transplantations.

Avoid use in those with myasthenia gravis, due to risk of exacerbated muscle weakness.

Anaphylactic and/or hypersensitivity reactions may occur after the first dose; fever, rash, severe dermatologic reactions, vasculitis, arthralgia, myalgia, serum sickness, allergic pneumonitis, renal toxicity, hepatic toxicity, anaemia, thrombocytopenia, leucopenia, and other haematologic abnormalities may occur after multiple doses.

Reports of other reactions and adverse events including central nervous system effects, Clostridium difficile–associated diarrhoea, peripheral neuropathy, prolongation of the QT interval, musculoskeletal disorders in paediatric patients, blood glucose disturbances, photosensitivity/phototoxicity, development of drug-resistant bacteria.

Safety and efficacy not established in paediatric patients, adolescents, or pregnant or lactating women.

Drug–Drug Interactions

Potentiation of hypoglycaemic actions of oral hypoglycaemia drugs (glyburide, glibenclamide) or insulin.

Possible increased QTc interval of electrocardiogram with concomitant class IA or class III antiarrhythmics.

Possible increase in half-life of ofloxacin with concomitant cimetidine.

Decreased absorption of ofloxacin with multivalent cation-containing products (eg, magnesium/aluminium antacids, sucralfate, didanosine chewable/buffered tablets or paediatric powder, highly buffered drugs, products containing calcium, zinc, or iron) within 2 hours.

Possible increased concentration or effects of concomitant medication: theophylline, warfarin, cyclosporine.

Possible increased risk of central nervous system stimulation and convulsive seizures with concomitant nonsteroidal antiinflammatory.

Possible false-positive urine screening tests for opiates.

Avoid coadministration with multivitamins.*

Possible increased concentration or effects of concomitant warfarin; monitor international normalised ratio and prothrombin time.*

Considerations for Special Populations

Elderly may have increased risk of severe hepatotoxicity, tendinopathy, especially with concomitant corticosteroid use, and prolongation of QT interval; may be more likely to have decreased renal function and may require dosage adjustment.

Diabetics receiving insulin or an oral hypoglycaemic drug should discontinue ofloxacin immediately in event of a hypoglycaemic reaction.

Use with caution in patients with predisposition to seizures or lower seizure threshold.

QT interval: use caution in patients with known QT prolongation, uncorrected hypokalemia or receiving class IA or class III antiarrhythmics; caution should be used in patients receiving other drugs known to prolong the QT interval or with congenital QT prolongation.

Reduced excretion in patients with severe liver function disorders; do not exceed maximum 400 mg/day.

See above for pregnancy and lactation.

Adverse Effects

Most common adverse events included nausea, diarrhoea, vomiting, rash, pruritus, headache, insomnia, dizziness, external genital pruritus, vaginitis, dysgeusia.

Other adverse events may include abdominal pain and cramps, chest pain, decreased appetite, dry mouth, dysgeusia, fatigue, flatulence, gastrointestinal distress, nervousness, pharyngitis, pruritus, fever, rash, sleep disorders, somnolence, trunk pain, vaginal discharge, visual disturbances, and constipation.

Additional adverse events seen with fluoroquinolone treatment include pain in extremities, convulsions, increased intracranial pressure, toxic psychosis, central nervous system events (nervousness, agitation, restlessness, drowsiness, anxiety, nightmares, paranoia, confusion, tremor, hallucination, depression, suicidal thoughts or acts), hypersensitivity reactions, cardiac disturbances (QT prolongation and torsades de points), hepatic necrosis, interstitial nephritis, blood disorders, pseudomembranous colitis, peripheral neuropathy, tendonitis and tendon ruptures, phototoxicity.

Seizures may occur in patients with underlying central nervous system disease.

*Information from Aurum Institute Drugs on the Go.
Information from US Prescribing Information.