Ofcin

Ofloxacin.

Pharmacology: Ofloxacin exerts its bactericidal action by inhibiting DNA gyrase, an enzyme necessary for bacterial DNA replication, in susceptible organisms.
Microbiology: Ofloxacin is active in vitro against many gram-positive aerobic bacteria, including penicillinase-producing, non-penicillinase-producing, and some methicillin-resistant staphylococci. It is also active in vitro against most gram-negative aerobic bacteria, including Enterobacteriaceae and Pseudomonas aeruginosa. It also has some activities in vitro against Chlamydia, Mycoplasma, Mycobacterium, Plasmodium and Rickettsia.
Ofloxacin has some activities against gram-positive and gram-negative anaerobic bacteria; however, high concentrations of the drug are generally required for in vitro inhibition and most of these organisms are considered resistant to the drug. This includes Clostridium and Bacteroides groups.
Pharmacokinetics: Ofloxacin is rapidly and almost completely absorbed from the gastrointestinal tract following oral administration. Peak serum concentrations are generally attained within 0.5-2 hrs. It is widely distributed into body tissues and fluids following oral administration, and is concentrated within neutrophils, achieving concentrations in these cells that may be up to 8 times greater than extracellular concentrations. Almost 80% of ofloxacin is excreted unchanged in urine and a small percentage of the dose is excreted in urine as metabolites and in feces. In healthy adults with normal renal function, its elimination half-life in the terminal phase averages 4-8 hrs, although renal impairment will increase its serum concentrations and prolong its half-life.

For the treatment of infections caused by susceptible strains of microorganisms in infections of the urinary tract, lower respiratory tract, skin and soft tissue, gonorrhoea and nongonococcal urethritis and cervicitis.

Urinary Tract Infections: 200-400 mg daily, preferably in the morning, and increased if necessary in upper urinary tract infections to 400 mg twice daily for 7-10 days.
Lower Respiratory Tract Infections: 400 mg daily, preferably in the morning, and increased if necessary to 400 mg twice daily for 7-14 days.
Skin and Soft Tissue Infections: 200-400 mg twice daily for 7 days.
Uncomplicated Gonorrhoea: 400 mg as a single dose.
Nongonococcal Urethritis and Cervicitis: 400 mg daily in single or divided doses for 7-10 days.
Renal Impairment: When creatinine clearance is 20-50 mL/min, the dosage should be reduced by ½ (100-200 mg). If creatinine clearance is <20 mL/min, 100 mg should be given every 24 hrs. In patients undergoing haemodialysis or peritoneal dialysis, 100 mg should be given every 24 hrs.
Liver Impairment: Dose of ofloxacin should be reduced accordingly in patients with impaired liver function.

Symptoms: Overdosage of ofloxacin would be expected to produce manifestations that are extensions of the adverse reactions reported with the drug, and may include nausea, vomiting, seizures, vertigo, dysgeusia and psychosis.
Treatment: If acute overdosage of ofloxacin occurs, the stomach should be emptied by inducing emesis or by gastric lavage. Supportive and symptomatic treatment should be initiated, and patient should be observed carefully while adequate hydration should be maintained. Since ofloxacin is not efficiently removed by haemodialysis or peritoneal dialysis, these procedures should not be relied on to enhance elimination of the drug from the body.

Patient who has shown previous hypersensitivity to ofloxacin or to other quinolone antibiotics.
Patients with a history of epilepsy or with a lowered seizure threshold.
Use in pregnancy & lactation: Ofloxacin is contraindicated in pregnant or breastfeeding women.
Use in children: Ofloxacin is contraindicated in children or growing adolescents.

Patients on ofloxacin should be cautioned to avoid excessive exposure to direct sunlight while receiving the drug. If photosensitivity occurs (eg, skin eruption), ofloxacin should be discontinued.
As with other antibiotics, use of ofloxacin may result in overgrowth of nonsusceptible organisms, especially enterococci or Candida. Resistant strains of some organisms (eg, Pseudomonas aeruginosa, staphylococci) have developed during ofloxacin therapy. Careful monitoring of the patient and periodic in vitro susceptibility tests are essential. If superinfection occurs, appropriate therapy should be instituted.
Ofloxacin should be used with caution in patients with renal or hepatic impairment because elimination of the drug is reduced in these patients.
Effects on the Ability to Drive or Operate Machinery: Adverse effects may affect performance of skilled tasks (eg, driving or handing machinery).
Use in the elderly: Dosage of ofloxacin does not need to be modified in geriatric patients with creatinine clearances >50 mL/min.

Ofloxacin is contraindicated in pregnant or breastfeeding women.

Ofloxacin is generally well tolerated, and adverse effects of the drug are similar to those reported with other quinolone antibiotics. The most frequent adverse effects involve the GI tract or the CNS, including nausea, diarrhea, vomiting, abdominal pain/discomfort, abdominal cramps, flatulence, constipation, dyspepsia, heartburn, decreased appetite, dry mouth, headache, insomnia, dizziness, nervousness and sleep disorders. Also reported are rash and pruritus, tachycardia, transient hypotension, hepatitis, cholestatic jaundice, interstitial nephritis, eosinophilia, leukocytosis, anemia.

Clinically important drug interactions of ofloxacin include those with antacids, sucralfate, oral antidiabetics, warfarin and theophylline. Both antacids and sucralfate decrease absorption of oral ofloxacin; effects of oral antidiabetics may be enhanced by ofloxacin; effects of warfarin on prothrombin time and theophylline level may be increased by ofloxacin. With high doses of quinolones, impairment of excretion and an increase in serum levels may occur when co-administered with other drugs that undergo renal tubular secretion, eg probenecid. Other drug interactions include those with aminoglycosides, β-lactam antibiotics and antimycobacterial agents.

Store at a temperature below 30°C. Protect from light and moisture. Keep in a tight container.
Shelf-Life: 3 years.

Quinolones

J01MA01 - ofloxacin ; Belongs to the class of fluoroquinolones. Used in the systemic treatment of infections.

B