Each 100 mL contains Ofloxacin 200 mg.
Pharmacology: Antimicrobial Activity: Ofloxacin is a fluoroquinolone antibacterial. It is used against Chlamydia trachomatis. It is also active against Mycobacterium leprae as well as M. tuberculosis and some other Mycobacterium spp. Ofloxacin is bactericidal and acts by inhibiting the A subunit of DNA gyrase (topoisomerase) which is essential in the reproduction of bacterial DNA. Among Gram-negative aerobic bacteria, Ofloxacin is active against Enterobacteriaceae, including Escherichia coli and Citrobacter, Enterobacter, Klebsiella, Proteus, Providencia, Salmonella, Serratia, Shigella, and Yersinia spp. It is also active against Pseudomonas aeruginosa but less so against other Pseudomonas spp. Haemophilus ducreyi, H. influenzae, Moraxella catarrhalis (Branhamella catarrhalis), Neisseria gonorrheae, and N. meningitides are all very sensitive, including beta-lactamase-producing strains of H. influenzae, M. catarrhalis, and N. gonorrheae. Other Gram-negative aerobic bacteria reported to be sensitive to Ofloxacin have included Acinetobacter spp., Campylobacter spp., Gardnerella vaginalis, Helicobacter pylori, Legionella spp., Pasteurella multocida, and Vibrio spp. Variable activity has been reported against Brucella melitensis. Among Gram-positive aerobic bacteria, Ofloxacin is active against staphylococci, including penicillinase-producing and penicillinase-nonproducing strains, and against some methicillin-resistant strains. Streptococci, in particular Streptococcus pneumoniae and enterococci, are less susceptible. Other Gram-positive bacteria sensitive to Ofloxacin are Corynebacterium spp. and Listeria monocytogenes. Most anaerobic bacteria, including Bacteroides fragilis and Clostridium difficile, are resistant to Ofloxacin, although some other Bacteroides and Clostridium spp. may be susceptible. Ofloxacin has some activity against mycobacteria, mycoplasmas, rickettsias, and the protozoan Plasmodium falciparum. Chlamydia trachomatis is not very susceptible and Nocardia asteroids and Ureaplasma urealyticum are usually considered to be resistant. The spirochaete Treponema palladium and fungi are also resistant. Acquired resistance: Resistant strains, particularly of Staph. aureus (including methicillin-resistant strains) and Ps. aeruginosa have emerged during treatment with Ofloxacin.
Pharmacokinetics: About 25% is bound to plasma proteins. Ofloxacin is widely distributed in body fluids, including the CSF, and tissue penetration is good. It crosses the placenta and is distributed into breast milk. Relatively high concentrations are achieved in bile. There is limited metabolism to desmethyl and N-oxide metabolites; desmethyl ofloxacin has moderate antibacterial activity. Ofloxacin is eliminated mainly by the kidneys. Excretion is by tubular secretion and glomerular filtration and 65 to 80% of a dose is excreted unchanged in the urine over 24 to 48 hours, resulting in high urinary concentrations. Less than 5% is excreted in the urine as metabolites. From 4 to 8% of a dose may be excreted in the feces. Only small amounts of ofloxacin are removed by haemodialysis.
Ofloxacin has been used in the treatment of a wide range of infections including anthrax, biliary-tract infections, infected bites and stings, bone and joint infections, cat scratch disease, chancroid, exacerbations of cystic fibrosis, gastro-enteritis (including travellers' diarrhea and campylobacter enteritis, cholera, salmonella enteritis, and shigellosis), gonorrhea, infections in immunocompromised patients (neutropenia), legionnaire's disease, otitis externa, otitis media, peritonitis, Q fever, lower respiratory-tract infections (including pseudomonal infections in cystic fibrosis, but excluding infections due to Streptococcus pneumoniae such as pneumococcal pneumonia), septicemia, skin infections (including soft-tissue infections), spotted fevers, typhoid and paratyphoid fever, typhus, and urinary-tract infections. Ofloxacin is also used for surgical infection prophylaxis. It has been tried in the treatment of opportunistic mycobacterial infections and tuberculosis; Ofloxacin may be used in the treatment of leprosy. It is also used in chlamydial infections including non-gonococcal urethritis.
The adult intravenous dose ranges from 200 mg daily to 400 mg twice daily depending on the severity and the nature of the infection. Lower doses maybe necessary in patients with impaired renal function. Following a normal initial dose, subsequent doses are halved to 100 to 200 mg daily or the usual dose is given every 24 hours in patient with a creatinine clearance of 20 to 50 mL per minute; the dose should be reduced to 100 mg every 24 hours when the creatinine clearance is less than 20 mL per minute. Patients on dialysis may be given 100 mg every 24 hours or as prescribed by a physician.
Ofloxacin should not be used in children, adolescents, pregnant women, or breast-feeding mothers. It should also be avoided in methicillin-resistant Staphylococcus aureus infections because of the high level of resistance.
Ofloxacin should be used with caution in patients with epilepsy or a history of CNS disorders. Tendon damage may occur rarely with fluoroquinolones and treatment should be discontinued if patients experience tendon pain, inflammation, or rupture. Care is necessary in patients with impaired hepatic or renal function, glucose-6-phosphate dehydrogenase deficiency, or myasthenia gravis. An adequate fluid intake should be maintained during treatment with ofloxacin and excessive alkalinity of the urine avoided because of the risk of crystalluria. Exposure to strong sunlight or sunlamps should also be avoided. The ability to drive or operate machinery may be impaired by ofloxacin, especially when alcohol is also taken.
The range of adverse effects associated with Ofloxacin and other fluoroquinolone antibacterials most often involve the gastrointestinal tract, CNS, or skin. Gastrointestinal disturbances include nausea, vomiting, diarrhea, abdominal pain, and dyspepsia and are the most frequent adverse effects. Pseudomembranous colitis has been reported rarely. Headache, dizziness, and restlessness are among the commonest effects on the CNS. Others include tremor, drowsiness, insomnia, nightmares, visual and other sensory disturbances and, more rarely, hallucinations, psychotic reactions, depression, and convulsions. Paraesthesia and peripheral neuropathy have occurred occasionally. In addition to rash and pruritus, hypersensitivity-type reactions affecting the skin have included, rarely, vasculitis, erythema multiforme, Stevens-Johnson syndrome, and toxic epidermal necrolysis. Photosensitivity has occurred. Anaphylaxis has been associated with ofloxacin and some other quinolone antibacterial. As with other quinolone antibacterial, reversible arthralgia has sometimes occurred and joint erosions have been documented in immature animals. Tendon damage has been reported. Other adverse effects reported with Ofloxacin include transient increases in serum creatinine or blood urea nitrogen and, occasionally acute renal failure secondary to interstitial nephritis; crystalluria; elevated liver enzyme values, jaundice, and hepatitis; hematological disturbances including eosinophilia, leucopenia, thrombocytopenia and, very rarely, hemolytic anemia or agranulocytosis; myalgia; gynaecomastia; and cardiovascular effects including tachycardia. As with other antibacterial, superinfection with organisms not very susceptible to ofloxacin is possible. Such as Candida
, Clostridium difficile
, and Streptococcus pneumoniae
. Pain and irritation may occur at the site of infusion accompanied rarely by phlebitis or thrombophlebitis. Sodium chloride adverse effects hypernatremia, hypotension, hyperchloremia and hypervolemia.
Fluoroquinolones are known to inhibit hepatic drug metabolism and may interfere with the clearance of drugs, such as theophylline that are metabolized by the liver. Cations like aluminum, magnesium, or iron reduce the absorption of Ofloxacin and related drugs when given concomitantly.
Analgesics: Concurrent administration with fenbufen with quinolones may increase the incidence of quinolone CNS adverse effects. Adverse neurological effects have also been reported in patients receiving naproxen and chloroquine when ciprofloxacin was administered, which abated when the antirheumatic drug were withdrawn. Ofloxacin also interacts with opioid analgesics; peak serum concentrations of Ofloxacin given by mouth pre-operatively were significantly reduced when intramuscular papaveretum was injected concomitantly. It is recommended that opioids should not be administered preoperatively to patients receiving Ofloxacin.
Antacids and metal ions: The absorption of Ofloxacin and other fluoroquinolones is reduced by antacids containing aluminum or magnesium and also by calcium iron and zinc salts. In addition, concomitant administration of antacids or oral iron preparations might antagonize the antibacterial activity of fluoroquinolones within the gut lumen. Dairy products with high calcium content might also interfere with the absorption of some fluoroquinolones. Enteral feeds, which contain cations, have also been found to reduce absorption of Ofloxacin.
Antimigraine drugs: It is recommended that the dosage of zolmitriptan be reduced when given concurrently with Ofloxacin.
Antineoplastics and immunosuppressant: Absorption of oral Ofloxacin appears to be reduced after cytotoxic chemotherapy.
Probenecid: The urinary excretion of ofloxacin and some other fluoroquinolones is reduced by the concomitant administration of probenecid.
Xanthines: Ofloxacin and other fluoroquinolones decrease the clearance of theophylline and caffeine from the body. Fluoroquiolones can be neurotoxic in their own right.
Store at temperatures not exceeding 30°C.
J01MA01 - ofloxacin ; Belongs to the class of fluoroquinolones. Used in the systemic treatment of infections.
Soln for IV infusion (bottle) 2 mg/mL x 100 mL x 1's.