MOA : It functions by inhibiting DNA gyrase, a type II topoisomerase, and topoisomerase IV,enzymes necessary to separate bacterial DNA, thereby inhibiting cell division
Pharmacology & Brands Available:
As Ofloas®, Opera Pharma (K) Ltd
Oflox®, Cosmos Limited
Ofloxacin® , Metro
Ofla-OD®, Psm Pharmaceuticals Limited
Oflomac®, Macleods Pharmaceuticals Limited
Ojen®, Jenburkt Pharmaceuticals Ltd
Toflox®, Lincoln Pharmaceuticals Ltd
Zofex®, Claris Otsuka Private Limited
Ofloxacin is a second-generation fluoroquinolone, being a broader-spectrum analog of norfloxacin, and was synthesized and developed by scientists at Daiichi Seiyaku.
It was first approved for marketing in Japan in 1985 for oral administration, and Daiichi marketed it there under the brand name Tarvid. Daiichi, working with Johnson & Johnson, obtained FDA approval in December 1990 under the brand name Floxin
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.
Ofloxacin is almost completely absorbed after oral administration plasma protein-bound 32 %. Maximal blood levels occur 1-3 hours after dosing and the elimination half-life is 4-6 hours. Ofloxacin is primarily excreted unchanged in the urine.
- Acute bacterial exacerbations of COPD
- Community-acquired pneumonia
- Uncomplicated skin and skin structure infections
- Nongonococcal urethritis and cervicitis
- Mixed Infections of the urethra and cervix
- Acute pelvic inflammatory disease
- Uncomplicated cystitis
- Complicated urinary tract infections
- Acute, uncomplicated urethral and cervical gonorrhea.
- Ofloxacin has not been shown to be effective in the treatment of syphilis.
Ofloxacin is contraindicated in patients with known hypersensitivity to quinolones or any of the tablet excipients, children, growing adolescents, pregnant or breastfeeding women.
ADVERSE EFFECTS :
Nausea, vomiting, headache, sleep disorders etc.
PRECAUTIONS AND WARNINGS:
Patients being treated with ofloxacin should not expose themselves unnecessarily to strong sunlight and should avoid UV rays (sun lamps, solaria). Caution is recommended if the drug is to be used in psychotic patients or in patients with a history of psychiatric disease. Administration of antibiotics, especially if prolonged, may lead to the proliferation of resistant micro-organisms. The patient’s condition must, therefore, be checked at regular intervals. If a secondary infection occurs, appropriate measures must be taken.
DOSAGE AND ADMINISTRATION :
The dosage range in adults is 200 mg daily to 400 mg twice daily depending on the severity and nature of the infection. Up to 400 mg may be given as a single dose. preferably in the morning, larger doses should be given as two divided doses
Lower urinary tract infection: 200-400 mg daily.
Upper urinary tract infection 200-400 mg daily increasing, if necessary to 400 mg twice a day. Lower respiratory tract infection: 400 mg daily increasing, 1f necessary to 400 mg twice daily. Uncomplicated urethral and cervical Gonorrhea A single dose of 400 mg.
Nongonococcal urethritis and cervicitis: 400 mg daily in single or divided doses. Skin and soft tissue infections: 400 mg twice daily. Typhoid: 400mg 800 mg daily or as directed by the physician.
CNS symptoms such as confusion, dizziness, impairment of consciousness and convulsive seizures as well as gastrointestinal reactions such as nausea and mucosal erosions.
Treatment in the ease of overdose Steps to remove any unabsorbed ofloxacin e. g gastric lavage, administration of adsorbents and Sodium sulphate, if possible during the first 30 minutes, are recommended; antacids are recommended for protection of the gastric mucosa. Elimination of ofloxacin may be increased by forced diuresis.
Drug may interact with theophylline, other antibiotics, anticoagulants (blood thinners like warfarin and nicoumalone), NSAIDs (e. g ibuprofen, naproxen, aspirin), diabetes medication, live vaccines, quinapril, didanosine, vitamins/minerals (e.g magnesium, aluminium, calcium, iron, zinc), sucralfate, Antacids like cimetidine, cyclosporine, bismuth subsalicylate.