Floxstat - General Information:A synthetic fluoroquinolone (fluoroquinolones) antibacterial agent that inhibits the supercoiling activity of bacterial DNA gyrase, halting DNA replication. [PubChem]
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Pharmacology:Floxstat is a quinolone/fluoroquinolone antibiotic. Floxstat 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. Floxstat is a broad-spectrum antibiotic that is active against both Gram-positive and Gram-negative bacteria.
Floxstat for patients
Patients should be advised:
- to drink fluids liberally;
- that mineral supplements, vitamins with iron or minerals, calcium- , aluminum-, or magnesium-based
antacids, sucralfate or Videx®, (Didanosine), chewable/buffered tablets or the pediatric powder for
oral solution should not be taken within the two-hour period before or within the two-hour period after
taking ofloxacin (See Drug Interactions);
- that ofloxacin can be taken without regard to meals;
- that ofloxacin may cause neurologic adverse effects (e. g. , dizziness, lightheadedness) and that
patients should know how they react to ofloxacin before they operate an automobile or machinery or
engage in activities requiring mental alertness and coordination
- to discontinue treatment and inform their physician if they experience pain, inflammation, or rupture
of a tendon, and to rest and refrain from exercise until the diagnosis of tendinitis or tendon rupture
has been confidently excluded;
- that ofloxacin may be associated with hypersensitivity reactions, even following the first dose, to
discontinue the drug at the first sign of a skin rash, hives or other skin reactions, a rapid heartbeat,
difficulty in swallowing or breathing, any swelling suggesting angioedema (e. g. , swelling of the lips,
tongue, face; tightness of the throat, hoarseness), or any other symptom of an allergic reaction
- to avoid excessive sunlight or artificial ultraviolet light while receiving ofloxacin and to discontinue
therapy if phototoxicity (e. g. , skin eruption) occurs;
- that if they are diabetic and are being treated with insulin or an oral hypoglycemic drug, to discontinue
ofloxacin immediately if a hypoglycemic reaction occurs and consult a physician
- that convulsions have been reported in patients taking quinolones, including ofloxacin, and to notify their
physician before taking this drug if there is a history of this condition.
Antacids, Sucralfate, Metal Cations, Multivitamins: Quinolones form chelates with alkaline earth and transition metal cations. Administration of quinolones with antacids containing calcium, magnesium, or aluminum, with sucralfate, with divalent or trivalent cations such as iron, or with multivitamins containing zinc or with Videx®, (Didanosine), chewable/buffered tablets or the pediatric powder for oral solution may substantially interfere with the absorption of quinolones resulting in systemic levels considerably lower than desired. These agents should not be taken within the two-hour period before or within the two-hour period after ofloxacin administration. Caffeine: Interactions between ofloxacin and caffeine have not been detected.
Cimetidine: Cimetidine has demonstrated interference with the elimination of some quinolones. This interference has resulted in significant increases in half-life and AUC of some quinolones. The potential for interaction between ofloxacin and cimetidine has not been studied.
Cyclosporine: Elevated serum levels of cyclosporine have been reported with concomitant use of cyclosporine with some other quinolones. The potential for interaction between ofloxacin and cyclosporine has not been studied.
Drugs metabolized by Cytochrome P450 enzymes: Most quinolone antimicrobial drugs inhibit cytochrome P450 enzyme activity. This may result in a prolonged half-life for some drugs that are also metabolized by this system (e. g. , cyclosporine, theophylline/methylxanthines, warfarin) when co-administered with quinolones. The extent of this inhibition varies among different quinolones.
Non-steroidal anti-inflammatory drugs: The concomitant administration of a non-steroidal anti-inflammatory drug with a quinolone, including ofloxacin, may increase the risk of CNS stimulation and convulsive seizures.
Probenecid: The concomitant use of probenecid with certain other quinolones has been reported to affect renal tubular secretion. The effect of probenecid on the elimination of ofloxacin has not been studied.
Theophylline: Steady-state theophylline levels may increase when ofloxacin and theophylline are administered concurrently. As with other quinolones, concomitant administration of ofloxacin may prolong the half-life of theophylline, elevate serum theophylline levels, and increase the risk of theophylline-related adverse reactions. Theophylline levels should be closely monitored and theophylline dosage adjustments made, if appropriate, when ofloxacin is co-administered. Adverse reactions (including seizures) may occur with or without an elevation in the serum theophylline level.
Warfarin: Some quinolones have been reported to enhance the effects of the oral anticoagulant warfarin orits derivatives. Therefore, if a quinolone antimicrobial is administered concomitantly with warfarin or its derivatives, the prothrombin time or other suitable coagulation test should be closely monitored.
Antidiabetic agents (e. g. , insulin, glyburide/glibenclamide): Since disturbances of blood glucose, including hyperglycemia and hypoglycemia, have been reported in patients treated concurrently with quinolones and an antidiabetic agent, careful monitoring of blood glucose is recommended when these agents are used concomitantly.
FLOXIN (ofloxacin) is contraindicated in persons with a history of hypersensitivity associated with the use of ofloxacin or any member of the quinolone group of antimicrobial agents.
Additional information about FloxstatFloxstat Indication: For the treatment of infections (respiratory tract, kidney, skin, soft tissue, UTI), urethral and cervical gonorrhoea.
Mechanism Of Action: Floxstat acts on DNA gyrase, an enzyme which, like human topoisomerase, prevents the excessive supercoiling of DNA during replication or transcription.
Drug Interactions: Aluminium Formation of non-absorbable complexes
Bismuth Formation of non-absorbable complexes
Calcium Formation of non-absorbable complexes
Iron Formation of non-absorbable complexes
Magnesium oxide Formation of non-absorbable complexes
Magnesium Formation of non-absorbable complexes
Sucralfate Formation of non-absorbable complexes
Zinc Formation of non-absorbable complexes
Warfarin The quinolone increases the anticoagulant effect
Acenocoumarol The quinolone increases the anticoagulant effect
Dicumarol The quinolone increases the anticoagulant effect
Anisindione The quinolone increases the anticoagulant effect
Dihydroquinidine barbiturate Increased risk of cardiotoxicity and arrhythmias
Quinidine Increased risk of cardiotoxicity and arrhythmias
Quinidine barbiturate Increased risk of cardiotoxicity and arrhythmias
Foscarnet Increased risk of convulsions
Procainamide The quinolone increases the effect of procainamide
Food Interactions: Not Available
Generic Name: Ofloxacin
Synonyms: Not Available
Drug Category: Anti-Bacterial Agents; Anti-Infectives; Quinolones
Drug Type: Small Molecule; Approved
Other Brand Names containing Ofloxacin: Akilen; Baccidal; Bactocin; Danoflox; Effexin; Exocin; Exocine; Flobacin; Flodemex; Flotavid; Flovid; Floxal; Floxil; Floxstat; Fugacin; Inoflox; Kinflocin; Kinoxacin; Liflox; Loxinter; Marfloxacin; Medofloxine; Mergexin; Novecin; Nufafloqo; O-Flox; Obide; Occidal; Ofcin; Oflin; Oflocee; Oflocet; Oflocin; Oflodal; Oflodex; Oflodura; Oflox; Ofloxin; Ofus; Onexacin; Operan; Orocin; Otonil; Pharflox; Praxin; Puiritol; Qinolon; Qipro; Quinolon; Quotavil; Rilox; Sinflo; Tabrin; Taravid; Tariflox; Tarivid; Telbit; Tructum; Uro Tarivid; Viotisone; Zanocin; Floxin;
Absorption: Bioavailability of ofloxacin in the tablet formulation is approximately 98%
Toxicity (Overdose): LD50=5450 mg/kg (orally in mice)
Protein Binding: 32%
Half Life: 9 hours
Dosage Forms of Floxstat: Tablet Oral
Chemical IUPAC Name: (+/-)-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
Chemical Formula: C18H20FN3O4
Ofloxacin on Wikipedia: http://en.wikipedia.org/wiki/Ofloxacin
Organisms Affected: Enteric bacteria and other eubacteria
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