Active ingredient: Ofloxacin - Brands, Medical Use, Clinical Data

Brands, Medical Use, Clinical Data

Drug Category

• Anti-bacterial Agents
• Anti-Infectives
• Quinolones

Dosage Forms

• Solution (IV injection)
• Tablet
• Opthalmic drops

Brands / Synonyms

Akilen; Baccidal; Bactocin; Danoflox; Effexin; Exocin; Exocine; Flobacin; Flodemex; Flotavid; Flovid; Floxal; Floxil; Floxin; Floxin Otic; Floxstat; Fugacin; Inoflox; Kinflocin; Kinoxacin; Liflox; Loxinter; Marfloxacin; Medofloxine; Mergexin; Novecin; Nufafloqo; O-Flox; Obide; Occidal; Ocuflox; Ofcin; Oflin; Oflocee; Oflocet; Oflocin; Oflodal; Oflodex; Oflodura; Oflox; Ofloxin; Ofus; Onexacin; Operan; Orocin; Otonil; Pharflox; Praxin; Puiritol; Qinolon; Qipro; Quinolon; Quotavil; Rilox; Sinflo; Tabrin; Taravid; Tariflox; Tarivid; Tarivid Eye Ear; Tarivid Otic; Telbit; Tructum; Uro Tarivid; Viotisone; Zanocin

Indications

For the treatment of infections (respiratory tract, kidney, skin, soft tissue, UTI), urethral and cervical gonorrhoea.

Pharmacology

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

Ofloxacin acts on DNA gyrase, an enzyme which, like human topoisomerase, prevents the excessive supercoiling of DNA during replication or transcription.

Absorption

Bioavailability of ofloxacin in the tablet formulation is approximately 98%

Toxicity

LD₅₀=5450 mg/kg (orally in mice)

Biotrnasformation / Drug Metabolism

Hepatic

Contraindications

FLOXIN (ofloxacin) is contraindicated in persons with a history of hypersensitivity associated with the use of ofloxacin or any member of the quinolone group of antimicrobial agents.

Drug Interactions

Antacids, Sucralfate, Metal Cations, Multivitamins: Quinolones form chelates with alkaline earth and transition metal cations. Administration of quinolones with antacids containing calcium, magnesium, or aluminum, with sucralfate, with divalent or trivalent cations such as iron, or with multivitamins containing zinc or with Videx®, (Didanosine), chewable/buffered tablets or the pediatric powder for oral solution may substantially interfere with the absorption of quinolones resulting in systemic levels considerably lower than desired. These agents should not be taken within the two-hour period before or within the two-hour period after ofloxacin administration. Caffeine: Interactions between ofloxacin and caffeine have not been detected.

Cimetidine: Cimetidine has demonstrated interference with the elimination of some quinolones. This interference has resulted in significant increases in half-life and AUC of some quinolones. The potential for interaction between ofloxacin and cimetidine has not been studied.

Cyclosporine: Elevated serum levels of cyclosporine have been reported with concomitant use of cyclosporine with some other quinolones. The potential for interaction between ofloxacin and cyclosporine has not been studied.

Drugs metabolized by Cytochrome P450 enzymes: Most quinolone antimicrobial drugs inhibit cytochrome P450 enzyme activity. This may result in a prolonged half-life for some drugs that are also metabolized by this system (e. g. , cyclosporine, theophylline/methylxanthines, warfarin) when co-administered with quinolones. The extent of this inhibition varies among different quinolones.

Non-steroidal anti-inflammatory drugs: The concomitant administration of a non-steroidal anti-inflammatory drug with a quinolone, including ofloxacin, may increase the risk of CNS stimulation and convulsive seizures.

Probenecid: The concomitant use of probenecid with certain other quinolones has been reported to affect renal tubular secretion. The effect of probenecid on the elimination of ofloxacin has not been studied.

Theophylline: Steady-state theophylline levels may increase when ofloxacin and theophylline are administered concurrently. As with other quinolones, concomitant administration of ofloxacin may prolong the half-life of theophylline, elevate serum theophylline levels, and increase the risk of theophylline-related adverse reactions. Theophylline levels should be closely monitored and theophylline dosage adjustments made, if appropriate, when ofloxacin is co-administered. Adverse reactions (including seizures) may occur with or without an elevation in the serum theophylline level.

Warfarin: Some quinolones have been reported to enhance the effects of the oral anticoagulant warfarin orits derivatives. Therefore, if a quinolone antimicrobial is administered concomitantly with warfarin or its derivatives, the prothrombin time or other suitable coagulation test should be closely monitored.

Antidiabetic agents (e. g. , insulin, glyburide/glibenclamide): Since disturbances of blood glucose, including hyperglycemia and hypoglycemia, have been reported in patients treated concurrently with quinolones and an antidiabetic agent, careful monitoring of blood glucose is recommended when these agents are used concomitantly.