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A synthetic fluoroquinolone (fluoroquinolones) antibacterial agent that inhibits the supercoiling activity of bacterial DNA gyrase, halting DNA replication. [PubChem]

• Akorn inc
• Alcon inc
• Apotex inc
• Bausch and lomb inc
• Bausch and lomb pharmaceuticals inc
• Bedford laboratories div ben venue laboratories inc
• Daiichi pharmaceutical corp
• Dr reddys laboratories ltd
• Fdc ltd
• Hi tech pharmacal co inc
• Larken laboratories inc
• Novex pharma
• Ortho mcneil janssen pharmaceuticals inc
• Ortho mcneil pharmaceutical inc
• Pharmaforce inc
• Ranbaxy laboratories ltd
• Sandoz inc
• Teva pharmaceuticals usa inc

• Akorn Inc.
• Alcon Laboratories
• Allergan Inc.
• American Regent
• Apotex Inc.
• AQ Pharmaceuticals Inc.
• A-S Medication Solutions LLC
• Bausch & Lomb Inc.
• Cipla Ltd.
• Daiichi Sankyo
• Dispensing Solutions
• Diversified Healthcare Services Inc.
• Doctor Reddys Laboratories Ltd.
• Falcon Pharmaceuticals Ltd.
• H.J. Harkins Co. Inc.
• Hi Tech Pharmacal Co. Inc.
• Innoviant Pharmacy Inc.
• Janssen-Ortho Inc.
• Lake Erie Medical and Surgical Supply
• Novex Pharma
• Nucare Pharmaceuticals Inc.
• Ortho Mcneil Janssen Pharmaceutical Inc.
• Pacific Pharma Lp
• Pack Pharmaceuticals
• Par Pharmaceuticals
• PD-Rx Pharmaceuticals Inc.
• Pharmaceutical Utilization Management Program VA Inc.
• Pharmaforce Inc.
• Physicians Total Care Inc.
• Preferred Pharmaceuticals Inc.
• Prescript Pharmaceuticals
• Ranbaxy Laboratories
• Rebel Distributors Corp.
• Redpharm Drug
• Sandhills Packaging Inc.
• Santen Inc.
• Teva Pharmaceutical Industries Ltd.

Synthesis Reference	Not Available
General Reference	Not Available

Type	small molecule

Classes

Fluoroquinolones and Quinolones Aminoquinolines and Derivatives Hydroxyquinolines

Substructures

Hydroxy Compounds Acetates Phenols and Derivatives Aliphatic and Aryl Amines Pyridines and Derivatives Piperazines Fluoroquinolones and Quinolones Ethers Benzene and Derivatives Oxazines Aminoquinolines and Derivatives Carboxylic Acids and Derivatives Hydroxyquinolines Halobenzenes Heterocyclic compounds Aromatic compounds Anisoles (Iso)quinolines and Derivatives Aryl Halides Phenyl Esters Anilines

antibacterials 抗细菌;

Indication	For the treatment of infections (respiratory tract, kidney, skin, soft tissue, UTI), urethral and cervical gonorrhoea.
Pharmacodynamics	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.
Mechanism of action	Ofloxacin acts on DNA gyrase and toposiomerase IV, enzymes which, like human topoisomerase, prevents the excessive supercoiling of DNA during replication or transcription. By inhibiting their function, the drug thereby inhibits normal cell division.
Absorption	Bioavailability of ofloxacin in the tablet formulation is approximately 98%
Volume of distribution	Not Available
Protein binding	32%
Metabolism	Hepatic
Route of elimination	Elimination is mainly by renal excretion. Between 65% and 80% of an administered oral dose of ofloxacin is excreted unchanged via the kidneys within 48 hours of dosing. Four to eight percent of an ofloxacin dose is excreted in the feces. This indicates a small degree of biliary excretion of ofloxacin.
Half life	9 hours
Clearance	Not Available
Toxicity	LD50=5450 mg/kg (orally in mice)
Affected organisms	Enteric bacteria and other eubacteria
Pathways	Not Available

Properties
State	solid
Experimental Properties	Property Value Source melting point 254 dec °C PhysProp water solubility 28.3 mg/mL Not Available logP -0.39 HANSCH,C ET AL. (1995)
Predicted Properties	Property Value Source water solubility 1.44e+00 g/l ALOGPS logP -0.02 ALOGPS logP 0.65 ChemAxon logS -2.4 ALOGPS pKa (strongest acidic) 5.45 ChemAxon pKa (strongest basic) 6.2 ChemAxon physiological charge -1 ChemAxon hydrogen acceptor count 7 ChemAxon hydrogen donor count 1 ChemAxon polar surface area 73.32 ChemAxon rotatable bond count 2 ChemAxon refractivity 94.94 ChemAxon polarizability 36.69 ChemAxon

Drug	Interaction
Acenocoumarol	The quinolone antibiotic, ofloxacin, may increase the anticoagulant effect of acenocoumarol.
Aluminium	Formation of non-absorbable complexes
Anisindione	The quinolone antibiotic, ofloxacin, may increase the anticoagulant effect of anisindione.
Calcium	Formation of non-absorbable complexes
Calcium Acetate	Calcium salts such as calcium acetate may decrease the absorption of quinolone antibiotics such as ofloxacin. Of concern only with oral administration of both agents. Interactions can be minimized by administering oral quinolone at least 2 hours before, or 6 hours after, the dose of an oral calcium supplement. Monitor for decreased therapeutic effects of oral quinolones if administered with oral calcium supplements.
Dicumarol	The quinolone antibiotic, ofloxacin, may increase the anticoagulant effect of dicumarol.
Dihydroquinidine barbiturate	Increased risk of cardiotoxicity and arrhythmias
Foscarnet	Increased risk of convulsions
Iron	Formation of non-absorbable complexes
Iron Dextran	Formation of non-absorbable complexes
Magnesium	Formation of non-absorbable complexes
Magnesium oxide	Formation of non-absorbable complexes
Procainamide	Ofloxacin may increase the effect of procainamide.
Quinidine	Increased risk of cardiotoxicity and arrhythmias
Quinidine barbiturate	Increased risk of cardiotoxicity and arrhythmias
Sucralfate	Formation of non-absorbable complexes
Tacrine	The metabolism of Tacrine, a CYP1A2 substrate, may be reduced by strong CYP1A2 inhibitors such as Ofloxacin. Consider modifying therapy to avoid Tacrine toxicity. Monitor the efficacy and toxicity of Tacrine if Ofloxacin is initiated, discontinued or if the dose is changed.
Thiothixene	The strong CYP1A2 inhibitor, Ofloxacin, may decrease the metabolism and clearance of Thiothixene, a CYP1A2 substrate. Consider alternate therapy or monitor for changes in Thiothixene therapeutic and adverse effects if Ofloxacin is initiated, discontinued or dose changed.
Tizanidine	Ofloxacin may decrease the metabolism and clearance of Tizanidine. Consider alternate therapy or use caution during co-administration.
Warfarin	The quinolone antibiotic, ofloxacin, may increase the anticoagulant effect of warfarin.
Zinc	Formation of non-absorbable complexes

• Avoid high doses of caffeine.
• Take without regard to meals.