Ofloxacin
- Atc Codes:J01MA01#S01AX11#S02AA16
- CAS Codes:82419-36-1
- PHARMGKB ID:82419-36-1
Table of contents
- Brand Names
- Chemistry
- Pharmacologic Category
- Mechanism of Action
- Therapeutic Use
- Unlabeled Use
- Pregnancy and Lactation Implications
- Contraindications
- Warnings and Precautions
- Adverse Reactions
- Substrate of
- Inhibits
- Drug Interactions
- Nutrition/Nutraceutical Interactions
- Dosage
- Pharmacokinetics and Pharmacodynamics
- Special Considerations
Brand Names
Europe
Austria: Floxal, Ofloxacin, Tarivid; Belgium: Docofloxacine, Ofloxacine, Trafloxal, Tarivid; Bulgaria: Floxal, Medofloxine, Ofloxin, Oxacid, Uniflox-Unimed Pharma; Cyprus: Novecin, Oflox, Taravid; Czech Republic: Floxal, Ofloxacina, Ofloxin, Taroflox, Zanocin; Denmark: Exocin, Ofloxacin, Tarivid; Estonia: Ofloxin, Tarivid; Finland: Exocin, Tarivid; France: Exocine, Monoflocet, Oflocet, Ofloxacin; Germany: Floxal, Oflodura, Oflohexal, Oflox, Ofloxacin, Ofloxacine, Oxfloxacin, Tarivid; Greece: Cellin, Ermofan, Exocin, Grenis-Oflo, Hetacloxacin, Oflocollyre, Oflox, Tabrin, Urimax-Bros Ε.Π.Ε.; Hungary: Floxal, Grenis-Oflo, Oflogen, Ofloxacin, Tarivid, Zanocin; Ireland: Biravid, Exocin, Tarivid; Italy: Exocin, Oflocin; Netherlands: Ofloxacin, Ofloxacine, Tarivid, Trafloxal; Poland: Floxal, Oflodinex, Tarivid, Zanocin; Portugal: Bioquil, Exocin, Floxedol, Oflocet, Ofloxacina, Tarivid; Romania: Floxal, Ofloxacin, Ofloxin, Uniflox-Unimed Pharma, Zanocin; Slovakia: Medofloxine, Ofloxin, Tarivid, Taroflox; Spain: Exocín, Oflovir, Ofloxacino, Surnox, Tarivid; Sweden: Ofloxacin, Tarivid; UK: Exocin, Tarivid.
North America
Canada: Oflox; USA: Floxin, Ocuflox, Ofloxacin.
Latin America
Argentina: Floxil, Klonalflox, Newflox, Oflox, Ofloxacina, Otoflox; Brazil: Flogirax, Floxstat, Genoxacin, Nostil, Oflox, Ofloxacino; Mexico: Bactocin, Flonacin, Flosep, Floxil, Floxstat, Loxtev, Ocuflox, Ofloxacino, Oxken, Quiflural, Zanocin.
Asia
Japan: Libiget, Marromel, Ofloxacin, Ofloxat, Ofloxin, Oftector, Oftight, Oharaxin, Olcavit, Opool, Pharxacin, Tarifron, Tarivid, Tarixacin, Tarizart, Tatsumixin, Xatron.
Drug combinations
Chemistry
Ofloxacin: C~18~H~20~FN~3~O~4~. Mw: 361.37. (1) 7H-Pyrido[1,2,3-de]-1,4-benzoxazine-6-carboxylic acid, 9-fluoro-2,3-dihydro-3-methyl-10-(4-methyl-1-piperazinyl)-7-oxo-, (±)-; (2)(±)-9-Fluoro-2,3-dihydro-3-methyl-10-(4-methyl-1-piperazinyl)-7-oxo-7H-pyrido[1,2,3-de]-1,4-benzoxazine-6-carboxylic acid. CAS-82419-36-1 (1984).
Pharmacologic Category
Antibacterials; Quinolones. EENT Preparations; Antibacterials. (ATC-Code: J01MA01; S01AX11; S02AA16).
Mechanism of action
Ofloxacin inhibits bacterial DNA gyrase and topoisomerase IV. Usually bactericidal. Active in vitro against most Gram-negative aerobic bacteria, including Enterobacteriaceae and P. aeruginosa. Active in vitro against many Gram-positive aerobic bacteria, including penicillinase-producing, nonpenicillinase-producing, and some oxacillin-resistant staphylococci (previously known as methicillin-resistant staphylococci). Less active against Gram-positive than -negative bacteria. Active in vitro and in clinical infections against Gram-positive aerobic cocci such as S. aureus (oxacillin-susceptible (methicillin-susceptible) strains only), S. epidermidis (oxacillin-susceptible strains only), S. pneumoniae (penicillin-susceptible strains), S. pyogenes (group A β-hemolytic streptococci), S. saprophyticus, and Enterococcus faecalis. Also active in vitro against some other staphylococci (e.g. S. haemolyticus, S. hominis), some penicillin-resistant S. pneumoniae, viridans streptococci, groups C, F, and G streptococci, and nonenterococcal group D streptococci. Active against Gram-positive aerobic bacilli such as Bacillus anthracis, Corynebacterium oxacillin-resistant staphylococci, and Listeria monocytogenes (Nocardia asteroides usually resistant). Active in vitro and in clinical infections against Gram-negative aerobes such as Campylobacter jejuni, H. influenzae, H. parainfluenzae, M. catarrhalis, Ps. aeruginosa, and most Enterobacteriaceae (including Citrobacter, Edwardsiella, Enterobacter, E. coli, Klebsiella, M. morganii, P. mirabilis, P. vulgaris, Providencia, Salmonella, Shigella, Serratia, Yersinia enterocolitica). Also active in vitro against Acinetobacter, Aeromonas, Brucella, Francisella tularensis, Legionella pneumophila, Vibrio, and Yersinia pestis. Burkholderia cepacia resistant. Active in vitro and in clinical infections against other organisms such as C. pneumoniae, M. pneumoniae, M. tuberculosis, and other mycobacteria. Strains of N. gonorrhoeae with decreased susceptibility to ofloxacin and other fluoroquinolones reported with increasing frequency. Generally less active against Gram-positive than Gram-negative bacteria. Inactive against fungi and viruses. Some cross-resistance occurs between ofloxacin and other fluoroquinolones.
Therapeutic use
Acute exacerbations of chronic bronchitis, community-acquired pneumonia, skin and skin structure infections, urethral and cervical gonorrhea, urethritis and cervicitis (nongonococcal), mixed infections of urethra and cervix, pelvic inflammatory disease, cystitis, urinary tract infections, prostatitis. Superficial ocular infections. Otitis externa, chronic suppurative otitis media, acute otitis media.
Pregnancy and lactiation implications
Increased risk of teratogenic effects not observed in animals or humans; however, due to cartilage damage in immature animals, ofloxacin should only be used during pregnancy if safer option not available. Serum concentrations of ofloxacin may be lower during pregnancy than in nonpregnant patients. Enters breast milk (not recommended in nursing women).
Unlabeled use
Epididymitis (nongonococcal), leprosy, traveler’s diarrhea.
Contraindications
Hypersensitivity to ofloxacin or other members of quinolone group, such as nalidixic acid, oxolinic acid, cinoxacin, norfloxacin, and ciprofloxacin. Hypersensitivity to any component of the formulation.
Warnings and precautions
Fluoroquinolones may prolong QTc interval (avoid use in history of QTc prolongation, uncorrected hypokalemia, hypomagnesemia, or concurrent administration of other medications known to prolong the QT interval). Tremor, restlessness, confusion, and very rarely hallucinations or seizures may occur (caution in known or suspected CNS disorder). Fluoroquinolones associated with development of serious, and sometimes fatal, hypoglycemia (most often in elderly patients with diabetes). Hyperglycemia also reported. Severe hypersensitivity reactions, including anaphylaxis, occurred with quinolone therapy. Use of quinolones linked to peripheral neuropathy (rare). May cause moderate-to-severe phototoxicity reactions. Prolonged use may result in fungal or bacterial superinfection, including C. difficile-associated diarrhea and pseudomembranous colitis. There have been reports of tendon inflammation and/or rupture with quinolone antibiotics (higher risk if concurrent corticosteroids, organ transplant recipients, and in patients >60 years of age). Use with caution in hepatic impairment. Some quinolones may exacerbate myasthenia gravis; use with caution (rare, potentially life-threatening weakness of respiratory muscles may occur). Use with caution in renal impairment (may increase risk of tendon rupture), in rheumatoid arthritis (may increase risk of tendon rupture), and in risk of seizures (CNS disorders or concurrent therapy with medications which may lower seizure threshold; higher risk with concomitant NSAID therapy). All patients should be tested for syphilis. Hemolytic reactions may (rarely) occur with quinolone use in latent or actual G6PD deficiency. Some quinolones may produce false-positive urine screening result for opiates using commercially-available immunoassay kits.