Norfloxacin

Chemical structure of Norfloxacin: Norfloxacin in Kenya

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:

Brands of Norfloxacin in Kenya

Asnor® , Opera Pharma (K) Ltd
Carenorfcin® , Careplus Limited
Floxinor®, Biodeal Laboratories Ltd
Floxinox®, Dawa
Mediflox® , Medisel Kenya Ltd
Negaflox®, Zydus
Niflox®, Elys Chemical Industries Ltd
Norflogen® Tablets, Shanghai Agen International Trade Co.ltd,
Noflox®, Cosmos Limited
Norbactin®, Ranbaxy
Norfen®, Cadila pharm
Norfocin®, Mac’s
Norilet®,GSK
Norlab®, Lab & Allied Ltd
Normax®, Ipca Laboratories Limited
Normed®, Zest pharma
Uniflox®, Universal Corporation Limited
Uriflox®, Flamingo
Uruflox®, Gesto
Zeflox®, Emcure

It was patented in 1977 and approved for medical use in 1983

Indications

  • Uncomplicated urinary tract infections (including cystitis)
  • Complicated urinary tract infections (restricted use)
  • Uncomplicated urethral and cervical gonorrhoea (however this indication is no longer considered to be effective by some experts due to bacterial resistance)
  • Prostatitis due to Escherichia coli.
  • Syphilis treatment: Norfloxacin has not been shown to be effective in the treatment of syphilis. Antimicrobial agents used in high doses for short periods of time to treat gonorrhoea may mask or delay the symptoms of incubating syphilis.
  • In ophthalmology, Norfloxacin licensed use is limited to the treatment of conjunctival infections caused by susceptible bacteria
  • Norfloxacin is used for prevention of spontaneous bacterial peritonitis in cirrhotic patients who have a low ascites fluid protein level, impaired renal function, severe liver disease, have had a prior episode of spontaneous bacterial peritonitis, or oesophagal variceal bleeding

Contraindications

  • Norfloxacin is contraindicated in persons with a history of hypersensitivity, tendinitis, or tendon rupture associated with the use of norfloxacin or any member of the quinolone group of antimicrobial agents.”
  • Quinolones, including norfloxacin, have been shown in vitro to inhibit CYP1A2. Concomitant use with drugs metabolized by CYP1A2 (e.g., caffeine, clozapine, ropinirole, tacrine, theophylline, tizanidine) may result in increased substrate drug concentrations when given in usual doses. Patients taking any of these drugs concomitantly with norfloxacin should be carefully monitored.”
  • Concomitant administration with tizanidine is contraindicated

Adverse effects

  • Common side-effects include gastrointestinal effects such as nausea, vomiting, and diarrhoea, as well as headache and insomnia.
  • Exacerbation of the symptoms of the neurological disorder myasthenia gravis
  • The most severe form of tendinopathy associated with fluoroquinolone administration is tendon rupture, which in the great majority of cases involves the Achilles tendon.
  • Prolongation of the QT interval can lead to torsades de pointes, a life-threatening arrhythmia
  • Clostridium difficile-associated diarrhoea may occur in connection with the use of Norfloxacin
  • Peripheral neuropathy, which can be permanent.
  • Other nervous system effects include insomnia, restlessness, and rarely, seizure, convulsions, and psychosis    norfloxacin in Kenya

Drug Interactions

  • Quinolones, including norfloxacin, may enhance the effects of oral anticoagulants, including warfarin or its derivatives or similar agents
  • The use of NSAIDs (Non-Steroid Anti Inflammatory Drugs) while undergoing fluoroquinolone therapy is contraindicated due to the risk of severe CNS adverse reactions, including but not limited to seizure disorders
  • The use of norfloxacin concomitantly has also been associated with transient elevations in serum creatinine in patients receiving cyclosporine, on rare occasions, resulted in severe hypoglycemia with a sulfonylurea.
  • Renal tubular transport of methotrexate may be inhibited by concomitant administration of norfloxacin, potentially leading to increased plasma levels of methotrexate. This might increase the risk of methotrexate toxic reactions.
  • Current or past treatment with oral corticosteroids is associated with an increased risk of Achilles tendon rupture, especially in elderly patients who are also taking the fluoroquinolones
  • Coadministration of certain fluoroquinolones and other drugs primarily metabolized by CYP1A2 (e.g. theophylline, methylxanthines, tizanidine) results in increased plasma concentrations and could lead to clinically significant side effects of the coadministered drug.
  • The fluoroquinolones have also been shown to interfere with the metabolism of caffeine and the absorption of levothyroxine. The interference with the metabolism of caffeine may lead to the reduced clearance of caffeine and a prolongation of its serum half-life, resulting in a caffeine overdose.