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Identification
NameLevofloxacin
Accession NumberDB01137  (APRD00477, DB06085)
TypeSmall Molecule
GroupsApproved, Investigational
Description

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

Structure
Thumb
Synonyms
(-)-Ofloxacin
(3S)-(-)-9-Fluoro-3-methyl-10-(4-methyl-1-piperazinyl)-7-oxo-2,3-dihydro-7H-pyrido[1,2,3-de][1,4]benzoxazine-6-carboxylic acid
(S)-(-)-9-Fluoro-3-methyl-10-(4-methyl-1-piperazinyl)-7-oxo-2,3-dihydro-7H-pyrido[1,2,3-de][1,4]benzooxazine-6-carboxylic acid
(S)-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
(S)-Ofloxacin
L-ofloxacin
Levofloxacine
Levofloxacino
Levofloxacinum
Ofloxacin S-(-)-form
External Identifiers
  • MP-376
Approved Prescription Products
NameDosageStrengthRouteLabellerMarketing StartMarketing End
Act Levofloxacintablet750 mgoralActavis Pharma Company2009-06-24Not applicableCanada
Act Levofloxacintablet500 mgoralActavis Pharma Company2009-06-24Not applicableCanada
Act Levofloxacintablet250 mgoralActavis Pharma Company2009-06-24Not applicableCanada
Auro-levofloxacintablet750 mgoralAuro Pharma Inc2016-04-12Not applicableCanada
Auro-levofloxacintablet500 mgoralAuro Pharma Inc2016-04-12Not applicableCanada
Auro-levofloxacintablet250 mgoralAuro Pharma Inc2016-04-12Not applicableCanada
Ava-levofloxacintablet500 mgoralAvanstra Inc2011-09-152014-08-21Canada
Ava-levofloxacintablet250 mgoralAvanstra Inc2011-09-152014-08-21Canada
Dom-levofloxacintablet500 mgoralDominion PharmacalNot applicableNot applicableCanada
Dom-levofloxacintablet250 mgoralDominion PharmacalNot applicableNot applicableCanada
Dom-levofloxacintablet750 mgoralDominion PharmacalNot applicableNot applicableCanada
Iquixsolution15 mg/mLophthalmicVistakon Pharmaceuticals LLC2004-06-01Not applicableUs
Levaquintablet, film coated750 mg/1oralPhysicians Total Care, Inc.2005-08-02Not applicableUs
Levaquininjection, solution5 mg/mLintravenousJanssen Pharmaceuticals, Inc.1996-12-20Not applicableUs
Levaquintablet, film coated250 mg/1oralRed Pharm Drug Inc.1996-12-20Not applicableUs
Levaquinsolution25 mg/mLoralPatriot Pharmaceuticals, Inc.2013-07-01Not applicableUs
Levaquintablet, film coated500 mg/1oralCardinal Health1996-12-20Not applicableUs
Levaquintablet, film coated500 mg/1oralA S Medication Solutions1996-12-20Not applicableUs
Levaquintablet, film coated250 mg/1oralPhysicians Total Care, Inc.2000-05-12Not applicableUs
Levaquininjection, solution5 mg/mLintravenousJanssen Pharmaceuticals, Inc.1996-12-20Not applicableUs
Levaquintablet, film coated750 mg/1oralRed Pharm Drug Inc.1996-12-20Not applicableUs
Levaquintablet, film coated500 mg/1oralPhysicians Total Care, Inc.2000-05-11Not applicableUs
Levaquintablet, film coated500 mg/1oralLake Erie Medical DBA Quality Care Products LLC2011-01-27Not applicableUs
Levaquintablet, film coated500 mg/1oralRed Pharm Drug Inc.1996-12-20Not applicableUs
Levaquintablet, film coated750 mg/1oralJanssen Pharmaceuticals, Inc.1996-12-20Not applicableUs
Levaquintablet, film coated250 mg/1oralREMEDYREPACK INC.2013-04-11Not applicableUs
Levaquintablet, film coated500 mg/1oralbryant ranch prepack1996-12-20Not applicableUs
Levaquintablet, film coated500 mg/1oralJanssen Pharmaceuticals, Inc.1996-12-20Not applicableUs
Levaquintablet, film coated500 mg/1oralREMEDYREPACK INC.2013-04-10Not applicableUs
Levaquintablet, film coated500 mg/1oralPd Rx Pharmaceuticals, Inc.1996-12-20Not applicableUs
Levaquintablet, film coated250 mg/1oralJanssen Pharmaceuticals, Inc.1996-12-20Not applicableUs
Levaquintablet, film coated500 mg/1oralPd Rx Pharmaceuticals, Inc.1996-12-20Not applicableUs
Levaquintablet, film coated750 mg/1oralPd Rx Pharmaceuticals, Inc.1996-12-20Not applicableUs
Levaquinsolution25 mg/mLoralJanssen Pharmaceuticals, Inc.2004-10-21Not applicableUs
Levaquintablet, film coated750 mg/1oralRebel Distributors Corp1996-12-20Not applicableUs
Levaquintablet, film coated250 mg/1oralCardinal Health1996-12-20Not applicableUs
Levaquininjection, solution5 mg/mLintravenousJanssen Pharmaceuticals, Inc.1996-12-20Not applicableUs
Levaquintablet, film coated500 mg/1oralRebel Distributors Corp1996-12-20Not applicableUs
Levaquintablet, film coated750 mg/1oralCardinal Health1996-12-20Not applicableUs
Levaquintablet250 mgoralJanssen Inc1997-11-282014-10-27Canada
Levaquin 25mg/mlsolution25 mgintravenousJanssen Inc1998-01-292006-08-04Canada
Levaquin 500mgtablet500 mgoralJanssen Inc1997-11-282015-04-02Canada
Levaquin 5mg/mlsolution5 mgintravenousJanssen Inc1997-11-282014-03-19Canada
Levaquin 750mgtablet750 mgoralJanssen Inc2004-01-302015-03-27Canada
Levofloxacintablet500 mgoralPro Doc Limitee2013-11-28Not applicableCanada
Levofloxacintablet750 mgoralCobalt Pharmaceuticals CompanyNot applicableNot applicableCanada
Levofloxacintablet500 mgoralCobalt Pharmaceuticals CompanyNot applicableNot applicableCanada
Levofloxacintablet250 mgoralCobalt Pharmaceuticals CompanyNot applicableNot applicableCanada
Levofloxacin In 5% Dextrose Injectionsolution5 mgintravenousHospira Healthcare Corporation2011-12-23Not applicableCanada
Levofloxacin Injectionsolution5 mgintravenousTeva Canada LimitedNot applicableNot applicableCanada
Mylan-levofloxacintablet250 mgoralMylan Pharmaceuticals Ulc2009-06-24Not applicableCanada
Mylan-levofloxacintablet500 mgoralMylan Pharmaceuticals Ulc2009-06-24Not applicableCanada
Ntp-levofloxacintablet750 mgoralTeva Canada LimitedNot applicableNot applicableCanada
Ntp-levofloxacintablet500 mgoralTeva Canada LimitedNot applicableNot applicableCanada
Ntp-levofloxacintablet250 mgoralTeva Canada LimitedNot applicableNot applicableCanada
PHL-levofloxacintablet250 mgoralPharmel IncNot applicableNot applicableCanada
PHL-levofloxacintablet500 mgoralPharmel IncNot applicableNot applicableCanada
PHL-levofloxacintablet750 mgoralPharmel IncNot applicableNot applicableCanada
PMS-levofloxacintablet750 mgoralPharmascience Inc2009-06-24Not applicableCanada
PMS-levofloxacintablet500 mgoralPharmascience Inc2009-06-24Not applicableCanada
PMS-levofloxacintablet250 mgoralPharmascience Inc2009-06-24Not applicableCanada
Quinsairsolution240 mginhalationRaptor Pharmaceuticals IncNot applicableNot applicableCanada
Quixinsolution5 mg/mLophthalmicVistakon Pharmaceuticals LLC2000-10-01Not applicableUs
Sandoz Levofloxacintablet750 mgoralSandoz Canada Incorporated2009-06-24Not applicableCanada
Sandoz Levofloxacintablet500 mgoralSandoz Canada Incorporated2009-06-24Not applicableCanada
Sandoz Levofloxacintablet250 mgoralSandoz Canada Incorporated2009-06-24Not applicableCanada
Teva-levofloxacintablet500 mgoralTeva Canada Limited2004-11-30Not applicableCanada
Teva-levofloxacintablet250 mgoralTeva Canada Limited2004-11-30Not applicableCanada
Teva-levofloxacintablet750 mgoralTeva Canada Limited2009-06-24Not applicableCanada
Approved Generic Prescription Products
NameDosageStrengthRouteLabellerMarketing StartMarketing End
Apo-levofloxacintablet250 mgoralApotex Inc2009-06-24Not applicableCanada
Apo-levofloxacintablet500 mgoralApotex Inc2009-06-24Not applicableCanada
Apo-levofloxacintablet750 mgoralApotex Inc2009-06-24Not applicableCanada
Levofloxacintablet, film coated750 mg/1oralPd Rx Pharmaceuticals, Inc.2011-06-20Not applicableUs
Levofloxacintablet, film coated500 mg/1oralSTAT Rx USA LLC2011-08-13Not applicableUs
Levofloxacininjection, solution5 mg/mLintravenousClaris Lifesciences Inc.2013-07-01Not applicableUs
Levofloxacintablet, film coated500 mg/1oralBlenheim Pharmacal, Inc.2013-11-13Not applicableUs
Levofloxacintablet, film coated750 mg/1oralMacleods Pharmaceuticals Limited2012-03-22Not applicableUs
Levofloxacintablet500 mg/1oralMajor Pharmaceuticals2011-06-23Not applicableUs
Levofloxacintablet, film coated500 mg/1oralDr. Reddy's Laboratories Limited2011-06-20Not applicableUs
Levofloxacintablet, film coated500 mg/1oralNorthwind Pharmaceuticals2014-03-03Not applicableUs
Levofloxacintablet500 mg/1oralNew Horizon Rx Group, LLC2013-08-25Not applicableUs
Levofloxacintablet, film coated500 mg/1oralPd Rx Pharmaceuticals, Inc.2011-06-20Not applicableUs
Levofloxacintablet, film coated250 mg/1oralCardinal Health2013-12-01Not applicableUs
Levofloxacintablet250 mg/1oralMajor Pharmaceuticals2011-06-23Not applicableUs
Levofloxacintablet, film coated750 mg/1oralDr. Reddy's Laboratories Limited2011-06-20Not applicableUs
Levofloxacintablet250 mg/1oralWest ward Pharmaceutical Corp2011-06-21Not applicableUs
Levofloxacininjection5 mg/mLintravenousFresenius Kabi USA, LLC2013-06-20Not applicableUs
Levofloxacintablet, film coated250 mg/1oralTeva Pharmaceuticals USA Inc2011-06-20Not applicableUs
Levofloxacintablet, film coated750 mg/1oralDIRECT RX2015-01-01Not applicableUs
Levofloxacintablet, film coated250 mg/1oralAmerican Health Packaging2011-07-01Not applicableUs
Levofloxacintablet250 mg/1oralHikma Pharmaceutical2011-06-21Not applicableUs
Levofloxacintablet500 mg/1oralWockhardt USA LLC.2011-06-20Not applicableUs
Levofloxacintablet, film coated500 mg/1oralbryant ranch prepack2011-06-20Not applicableUs
Levofloxacintablet, film coated750 mg/1oralPreferred Pharmaceuticals, Inc.2011-06-20Not applicableUs
Levofloxacintablet, film coated500 mg/1oralMacleods Pharmaceuticals Limited2012-03-22Not applicableUs
Levofloxacintablet, film coated500 mg/1oralAmerican Health Packaging2011-07-01Not applicableUs
Levofloxacintablet, film coated500 mg/1oralREMEDYREPACK INC.2016-01-07Not applicableUs
Levofloxacininjection, solution5 mg/mLintravenousSagent Pharmaceuticals2011-12-05Not applicableUs
Levofloxacinsolution5 mg/mLophthalmicAkorn Inc.2011-03-01Not applicableUs
Levofloxacintablet, film coated500 mg/1oralPd Rx Pharmaceuticals, Inc.2011-06-20Not applicableUs
Levofloxacinsolution/ drops5 mg/mLtopicalPACK Pharmaceuticals, LLC2010-12-20Not applicableUs
Levofloxacininjection, solution5 mg/mLintravenousClaris Lifesciences Inc.2013-07-01Not applicableUs
Levofloxacintablet, film coated500 mg/1oralBlenheim Pharmacal, Inc.2015-07-15Not applicableUs
Levofloxacintablet, film coated250 mg/1oralDr. Reddy's Laboratories Limited2011-06-20Not applicableUs
Levofloxacintablet, film coated250 mg/1oralNorthwind Pharmaceuticals2015-05-14Not applicableUs
Levofloxacintablet, film coated500 mg/1oralClinical Solutions Wholesale2011-06-20Not applicableUs
Levofloxacintablet, film coated750 mg/1oralCardinal Health2013-12-01Not applicableUs
Levofloxacintablet, film coated750 mg/1oralSandoz Inc2011-06-20Not applicableUs
Levofloxacintablet500 mg/1oralWest ward Pharmaceutical Corp2011-06-21Not applicableUs
Levofloxacintablet, film coated750 mg/1oralProficient Rx LP2012-11-10Not applicableUs
Levofloxacintablet750 mg/1oralDIRECT RX2015-01-01Not applicableUs
Levofloxacintablet, film coated750 mg/1oralAurobindo Pharma Limited2011-06-20Not applicableUs
Levofloxacintablet250 mg/1oralWockhardt USA LLC.2011-06-20Not applicableUs
Levofloxacintablet, film coated500 mg/1oralH.J. Harkins Company, Inc.2011-11-22Not applicableUs
Levofloxacintablet, film coated750 mg/1oralZydus Pharmaceuticals (USA) Inc.2012-11-10Not applicableUs
Levofloxacintablet, film coated250 mg/1oralMacleods Pharmaceuticals Limited2012-03-22Not applicableUs
Levofloxacinsolution25 mg/mLoralDepartment Of State Health Services, Pharmacy Branch2011-06-21Not applicableUs
Levofloxacininjection, solution5 mg/mLintravenousSagent Pharmaceuticals2011-06-20Not applicableUs
Levofloxacintablet, film coated250 mg/1oralPd Rx Pharmaceuticals, Inc.2011-06-20Not applicableUs
Levofloxacintablet750 mg/1oralTorrent Pharmaceuticals Limited2011-06-20Not applicableUs
Levofloxacininjection, solution5 mg/mLintravenousClaris Lifesciences Inc.2013-07-01Not applicableUs
Levofloxacintablet, film coated750 mg/1oralBlenheim Pharmacal, Inc.2013-11-15Not applicableUs
Levofloxacintablet, film coated750 mg/1oralPhysicians Total Care, Inc.2011-06-22Not applicableUs
Levofloxacintablet, film coated500 mg/1oralUnit Dose Services2011-06-20Not applicableUs
Levofloxacintablet, film coated750 mg/1oralCitron Pharma LLC2011-06-20Not applicableUs
Levofloxacintablet, film coated500 mg/1oralCardinal Health2013-12-01Not applicableUs
Levofloxacintablet, film coated500 mg/1oralSandoz Inc2011-06-20Not applicableUs
Levofloxacintablet750 mg/1oralWest ward Pharmaceutical Corp2011-06-21Not applicableUs
Levofloxacintablet, film coated750 mg/1oralProficient Rx LP2011-06-20Not applicableUs
Levofloxacintablet, film coated500 mg/1oralDIRECT RX2015-01-01Not applicableUs
Levofloxacintablet, film coated500 mg/1oralAurobindo Pharma Limited2011-06-20Not applicableUs
Levofloxacintablet, film coated750 mg/1oralBoca Pharmacal, LLC2012-08-17Not applicableUs
Levofloxacintablet750 mg/1oralPreferred Pharmaceuticals, Inc.2013-02-04Not applicableUs
Levofloxacintablet, film coated500 mg/1oralZydus Pharmaceuticals (USA) Inc.2012-11-10Not applicableUs
Levofloxacintablet250 mg/1oralAidarex Pharmaceuticals LLC2011-06-20Not applicableUs
Levofloxacininjection, solution750 mg/150mLintravenousAuro Medics Pharma Llc2016-02-10Not applicableUs
Levofloxacininjection, solution25 mg/mLintravenousSagent Pharmaceuticals2012-01-05Not applicableUs
Levofloxacintablet, film coated500 mg/1oralPhysicians Total Care, Inc.2011-06-22Not applicableUs
Levofloxacinsolution25 mg/mLoralHi Tech Pharmacal Co., Inc.2011-06-21Not applicableUs
Levofloxacintablet, film coated500 mg/1oralCitron Pharma LLC2011-06-20Not applicableUs
Levofloxacintablet250 mg/1oralCardinal Health2011-06-23Not applicableUs
Levofloxacintablet, film coated250 mg/1oralSandoz Inc2011-06-20Not applicableUs
Levofloxacininjection, solution250 mg/50mLintravenousWest ward Pharmaceutical Corp2011-09-16Not applicableUs
Levofloxacintablet, film coated500 mg/1oralProficient Rx LP2011-06-20Not applicableUs
Levofloxacintablet, film coated750 mg/1oralREMEDYREPACK INC.2015-05-20Not applicableUs
Levofloxacintablet, film coated250 mg/1oralAurobindo Pharma Limited2011-06-20Not applicableUs
Levofloxacintablet, film coated500 mg/1oralBoca Pharmacal, LLC2012-08-17Not applicableUs
Levofloxacintablet, film coated500 mg/1oralPreferred Pharmaceuticals, Inc.2011-08-12Not applicableUs
Levofloxacintablet, film coated250 mg/1oralZydus Pharmaceuticals (USA) Inc.2012-11-10Not applicableUs
Levofloxacintablet750 mg/1oralAidarex Pharmaceuticals LLC2011-06-20Not applicableUs
Levofloxacininjection, solution500 mg/100mLintravenousAuro Medics Pharma Llc2016-02-10Not applicableUs
Levofloxacininjection25 mg/mLintravenousHeritage Pharmaceuticals Inc.2013-02-04Not applicableUs
Levofloxacintablet, film coated750 mg/1oralPd Rx Pharmaceuticals, Inc.2011-06-20Not applicableUs
Levofloxacintablet500 mg/1oralTorrent Pharmaceuticals Limited2011-06-20Not applicableUs
Levofloxacininjection, solution25 mg/mLintravenousClaris Lifesciences Inc.2013-07-01Not applicableUs
Levofloxacintablet, film coated500 mg/1oralBlenheim Pharmacal, Inc.2013-09-05Not applicableUs
Levofloxacininjection, solution5 mg/mLintravenousSandoz Inc2011-07-07Not applicableUs
Levofloxacininjection, solution500 mg/100mLintravenousWest ward Pharmaceutical Corp2011-09-16Not applicableUs
Levofloxacintablet, film coated750 mg/1oralProficient Rx2011-06-20Not applicableUs
Levofloxacintablet, film coated500 mg/1oralJubilant Cadista Pharmaceuticals Inc.2012-12-02Not applicableUs
Levofloxacintablet, film coated750 mg/1oralCadila Healthcare Limited2012-11-10Not applicableUs
Levofloxacintablet, film coated250 mg/1oralBoca Pharmacal, LLC2012-08-17Not applicableUs
Levofloxacintablet750 mg/1oralPreferred Pharmaceuticals, Inc.2013-03-27Not applicableUs
Levofloxacintablet, film coated750 mg/1oralLupin Pharmaceuticals, Inc.2011-06-20Not applicableUs
Levofloxacintablet, film coated750 mg/1oralREMEDYREPACK INC.2016-04-14Not applicableUs
Levofloxacintablet500 mg/1oralAidarex Pharmaceuticals LLC2011-06-20Not applicableUs
Levofloxacininjection, solution250 mg/50mLintravenousAuro Medics Pharma Llc2016-02-10Not applicableUs
Levofloxacintablet, film coated750 mg/1oralRebel Distributors Corp2011-06-20Not applicableUs
Levofloxacintablet, film coated500 mg/1oralPd Rx Pharmaceuticals, Inc.2011-06-20Not applicableUs
Levofloxacintablet250 mg/1oralTorrent Pharmaceuticals Limited2011-06-20Not applicableUs
Levofloxacintablet, film coated500 mg/1oralLake Erie Medical DBA Quality Care Products LLC2011-06-20Not applicableUs
Levofloxacintablet, film coated750 mg/1oralMajor Pharmaceuticals2013-12-01Not applicableUs
Levofloxacintablet, film coated250 mg/1oralPhysicians Total Care, Inc.2011-09-15Not applicableUs
Levofloxacinsolution/ drops5 mg/mLophthalmicHi Tech Pharmacal Co., Inc.2011-02-10Not applicableUs
Levofloxacintablet, film coated250 mg/1oralCitron Pharma LLC2011-06-20Not applicableUs
Levofloxacintablet500 mg/1oralCardinal Health2011-06-23Not applicableUs
Levofloxacintablet, film coated500 mg/1oralCadila Healthcare Limited2012-11-10Not applicableUs
Levofloxacintablet, film coated500 mg/1oralReady Meds2011-06-20Not applicableUs
Levofloxacintablet, film coated750 mg/1oralPreferred Pharmaceuticals, Inc.2013-11-14Not applicableUs
Levofloxacintablet, film coated500 mg/1oralLupin Pharmaceuticals, Inc.2011-06-20Not applicableUs
Levofloxacininjection, solution5 mg/mLintravenousWG Critical Care, LLC2016-04-14Not applicableUs
Levofloxacintablet, film coated750 mg/1oralCamber Pharmaceuticals, Inc.2015-01-09Not applicableUs
Levofloxacintablet, film coated500 mg/1oralProficient Rx LP2012-03-22Not applicableUs
Levofloxacintablet, film coated500 mg/1oralRebel Distributors Corp2011-06-20Not applicableUs
Levofloxacintablet, film coated750 mg/1oralAv Kare, Inc.2013-07-12Not applicableUs
Levofloxacintablet, film coated500 mg/1oralApotheca Inc.2012-03-22Not applicableUs
Levofloxacintablet, film coated250 mg/1oralLake Erie Medical DBA Quality Care Products LLC2011-06-20Not applicableUs
Levofloxacintablet, film coated500 mg/1oralMajor Pharmaceuticals2013-12-01Not applicableUs
Levofloxacintablet, film coated250 mg/1oralREMEDYREPACK INC.2013-12-31Not applicableUs
Levofloxacintablet, film coated500 mg/1oralMedsource Pharmaceuticals2011-06-20Not applicableUs
Levofloxacintablet750 mg/1oralWockhardt Limited2011-06-20Not applicableUs
Levofloxacintablet750 mg/1oralCardinal Health2011-06-23Not applicableUs
Levofloxacininjection, solution5 mg/mLintravenousSandoz Inc2011-07-07Not applicableUs
Levofloxacininjection, solution750 mg/150mLintravenousWest ward Pharmaceutical Corp2011-09-16Not applicableUs
Levofloxacintablet, film coated500 mg/1oralProficient Rx2011-06-20Not applicableUs
Levofloxacintablet, film coated250 mg/1oralJubilant Cadista Pharmaceuticals Inc.2012-12-02Not applicableUs
Levofloxacininjection, solution5 mg/mLintravenousWG Critical Care, LLC2016-04-14Not applicableUs
Levofloxacintablet, film coated500 mg/1oralCamber Pharmaceuticals, Inc.2015-01-09Not applicableUs
Levofloxacintablet, film coated750 mg/1oralCentral Texas Community Health Centers2012-03-22Not applicableUs
Levofloxacintablet, film coated250 mg/1oralRebel Distributors Corp2011-06-20Not applicableUs
Levofloxacintablet, film coated500 mg/1oralAv Kare, Inc.2013-07-12Not applicableUs
Levofloxacintablet, film coated750 mg/1oralBlenheim Pharmacal, Inc.2015-03-26Not applicableUs
Levofloxacintablet, film coated500 mg/1oralLake Erie Medical DBA Quality Care Products LLC2011-06-20Not applicableUs
Levofloxacintablet, film coated250 mg/1oralMajor Pharmaceuticals2013-12-01Not applicableUs
Levofloxacintablet, film coated500 mg/1oralREMEDYREPACK INC.2013-09-19Not applicableUs
Levofloxacintablet, film coated500 mg/1oralPd Rx Pharmaceuticals, Inc.2012-03-22Not applicableUs
Levofloxacintablet500 mg/1oralWockhardt Limited2011-06-20Not applicableUs
Levofloxacininjection, solution, concentrate750 mg/30mLintravenousAuro Medics Pharma Llc2013-01-24Not applicableUs
Levofloxacininjection, solution5 mg/mLintravenousSandoz Inc2011-07-07Not applicableUs
Levofloxacintablet, film coated750 mg/1oralTeva Pharmaceuticals USA Inc2011-06-20Not applicableUs
Levofloxacintablet, film coated500 mg/1oralDIRECT RX2015-01-01Not applicableUs
Levofloxacintablet750 mg/1oralHikma Pharmaceutical2011-06-21Not applicableUs
Levofloxacintablet, film coated250 mg/1oralCadila Healthcare Limited2012-11-10Not applicableUs
Levofloxacintablet250 mg/1oralbryant ranch prepack2011-06-20Not applicableUs
Levofloxacintablet, film coated750 mg/1oralPreferred Pharmaceuticals, Inc.2015-01-08Not applicableUs
Levofloxacintablet, film coated250 mg/1oralLupin Pharmaceuticals, Inc.2011-06-20Not applicableUs
Levofloxacintablet, film coated250 mg/1oralAv Kare, Inc.2013-07-12Not applicableUs
Levofloxacintablet, film coated500 mg/1oralBlenheim Pharmacal, Inc.2014-01-14Not applicableUs
Levofloxacintablet, film coated750 mg/1oralLake Erie Medical DBA Quality Care Products LLC2011-06-21Not applicableUs
Levofloxacintablet750 mg/1oralMajor Pharmaceuticals2011-06-23Not applicableUs
Levofloxacintablet, film coated250 mg/1oralREMEDYREPACK INC.2013-03-08Not applicableUs
Levofloxacintablet, film coated500 mg/1oralPd Rx Pharmaceuticals, Inc.2012-03-22Not applicableUs
Levofloxacintablet250 mg/1oralWockhardt Limited2011-06-20Not applicableUs
Levofloxacininjection, solution, concentrate500 mg/20mLintravenousAuro Medics Pharma Llc2013-01-24Not applicableUs
Levofloxacininjection, solution5 mg/mLintravenousHospira, Inc.2015-09-03Not applicableUs
Levofloxacintablet, film coated500 mg/1oralTeva Pharmaceuticals USA Inc2011-06-20Not applicableUs
Levofloxacintablet, film coated250 mg/1oralDIRECT RX2014-01-01Not applicableUs
Levofloxacintablet500 mg/1oralHikma Pharmaceutical2011-06-21Not applicableUs
Levofloxacintablet750 mg/1oralWockhardt USA LLC.2011-06-20Not applicableUs
Levofloxacintablet, film coated750 mg/1oralbryant ranch prepack2011-06-20Not applicableUs
Levofloxacintablet, film coated500 mg/1oralPreferred Pharmaceuticals, Inc.2011-06-20Not applicableUs
Levofloxacintablet, film coated750 mg/1oralAmerican Health Packaging2011-07-01Not applicableUs
Levofloxacininjection, solution5 mg/mLintravenousWG Critical Care, LLC2016-04-14Not applicableUs
Levofloxacintablet, film coated250 mg/1oralCamber Pharmaceuticals, Inc.2015-01-09Not applicableUs
Levofloxacininjection25 mg/mLintravenousAkorn, Inc.2011-07-01Not applicableUs
Approved Over the Counter ProductsNot Available
Unapproved/Other Products Not Available
International Brands
NameCompany
CravitNot Available
ElequineNot Available
FloxelNot Available
LeroxacinNot Available
LevokacinNot Available
LevoxNot Available
LevoxacinNot Available
MosardalNot Available
NofaxinNot Available
ReskuinNot Available
TavanicNot Available
Brand mixturesNot Available
Salts
Name/CASStructureProperties
Levofloxacin hemihydrate
138199-71-0
Thumb
  • InChI Key: SUIQUYDRLGGZOL-RCWTXCDDSA-N
  • Monoisotopic Mass: 740.298133282
  • Average Mass: 740.762
DBSALT001001
Categories
UNIIRIX4E89Y14
CAS number100986-85-4
WeightAverage: 361.3675
Monoisotopic: 361.143784348
Chemical FormulaC18H20FN3O4
InChI KeyInChIKey=GSDSWSVVBLHKDQ-JTQLQIEISA-N
InChI
InChI=1S/C18H20FN3O4/c1-10-9-26-17-14-11(16(23)12(18(24)25)8-22(10)14)7-13(19)15(17)21-5-3-20(2)4-6-21/h7-8,10H,3-6,9H2,1-2H3,(H,24,25)/t10-/m0/s1
IUPAC Name
(2S)-7-fluoro-2-methyl-6-(4-methylpiperazin-1-yl)-10-oxo-4-oxa-1-azatricyclo[7.3.1.0⁵,¹³]trideca-5(13),6,8,11-tetraene-11-carboxylic acid
SMILES
C[[email protected]]1COC2=C3N1C=C(C(O)=O)C(=O)C3=CC(F)=C2N1CCN(C)CC1
Taxonomy
DescriptionThis compound belongs to the class of organic compounds known as quinoline carboxylic acids. These are quinolines in which the quinoline ring system is substituted by a carboxyl group at one or more positions.
KingdomOrganic compounds
Super ClassOrganoheterocyclic compounds
ClassQuinolines and derivatives
Sub ClassQuinoline carboxylic acids
Direct ParentQuinoline carboxylic acids
Alternative Parents
Substituents
  • Quinoline-3-carboxylic acid
  • N-arylpiperazine
  • Fluoroquinolone
  • Hydroxyquinoline
  • Dihydroquinolone
  • Aminoquinoline
  • Dihydroquinoline
  • Benzoxazine
  • Pyridine carboxylic acid or derivatives
  • Pyridine carboxylic acid
  • Dialkylarylamine
  • N-alkylpiperazine
  • N-methylpiperazine
  • Fluorobenzene
  • Alkyl aryl ether
  • Benzenoid
  • Pyridine
  • Piperazine
  • 1,4-diazinane
  • Aryl halide
  • Aryl fluoride
  • Heteroaromatic compound
  • Vinylogous amide
  • Tertiary aliphatic amine
  • Tertiary amine
  • Oxacycle
  • Azacycle
  • Monocarboxylic acid or derivatives
  • Ether
  • Carboxylic acid
  • Carboxylic acid derivative
  • Hydrocarbon derivative
  • Organooxygen compound
  • Organonitrogen compound
  • Organofluoride
  • Organohalogen compound
  • Carbonyl group
  • Amine
  • Aromatic heteropolycyclic compound
Molecular FrameworkAromatic heteropolycyclic compounds
External Descriptors
Pharmacology
IndicationFor the treatment of bacterial conjunctivitis caused by susceptible strains of the following organisms: Corynebacterium species, Staphylococus aureus, Staphylococcus epidermidis, Streptococcus pneumoniae, Streptococcus (Groups C/F/G), Viridans group streptococci, Acinetobacter lwoffii, Haemophilus influenzae, Serratia marcescens.
PharmacodynamicsLevofloxacin, a fluoroquinolone antiinfective, is the optically active L-isomer of ofloxacin. Levofloxacin is used to treat bacterial conjunctivitis, sinusitis, chronic bronchitis, community-acquired pneumonia and pneumonia caused by penicillin-resistant strains of Streptococcus pneumoniae, skin and skin structure infections, complicated urinary tract infections and acute pyelonephritis.
Mechanism of actionLevofloxacin inhibits bacterial type II topoisomerases, topoisomerase IV and DNA gyrase. Levofloxacin, like other fluoroquinolones, inhibits the A subunits of DNA gyrase, two subunits encoded by the gyrA gene. This results in strand breakage on a bacterial chromosome, supercoiling, and resealing; DNA replication and transcription is inhibited.
Related Articles
AbsorptionAbsorption of ofloxacin after single or multiple doses of 200 to 400 mg is predictable, and the amount of drug absorbed increases proportionately with the dose.
Volume of distributionNot Available
Protein binding24-38% (to plasma proteins)
Metabolism

Mainly excreted as unchanged drug (87%); undergoes limited metabolism in humans.

Route of eliminationMainly excreted as unchanged drug in the urine.
Half life6-8 hours
ClearanceNot Available
ToxicitySide effects include disorientation, dizziness, drowsiness, hot and cold flashes, nausea, slurring of speech, swelling and numbness in the face
Affected organisms
  • Enteric bacteria and other eubacteria
PathwaysNot Available
SNP Mediated EffectsNot Available
SNP Mediated Adverse Drug ReactionsNot Available
ADMET
Predicted ADMET features
PropertyValueProbability
Human Intestinal AbsorptionNot AvailableNot Available
Blood Brain BarrierNot AvailableNot Available
Caco-2 permeableNot AvailableNot Available
P-glycoprotein substrateNot AvailableNot Available
P-glycoprotein inhibitor INot AvailableNot Available
P-glycoprotein inhibitor IINot AvailableNot Available
Renal organic cation transporterNot AvailableNot Available
CYP450 2C9 substrateNot AvailableNot Available
CYP450 2D6 substrateNot AvailableNot Available
CYP450 3A4 substrateNot AvailableNot Available
CYP450 1A2 substrateNot AvailableNot Available
CYP450 2C9 inhibitorNot AvailableNot Available
CYP450 2D6 inhibitorNot AvailableNot Available
CYP450 2C19 inhibitorNot AvailableNot Available
CYP450 3A4 inhibitorNot AvailableNot Available
CYP450 inhibitory promiscuityNot AvailableNot Available
Ames testNot AvailableNot Available
CarcinogenicityNot AvailableNot Available
BiodegradationNot AvailableNot Available
Rat acute toxicityNot AvailableNot applicable
hERG inhibition (predictor I)Not AvailableNot Available
hERG inhibition (predictor II)Not AvailableNot Available
ADMET data is predicted using admetSAR, a free tool for evaluating chemical ADMET properties. (23092397 )
Pharmacoeconomics
ManufacturersNot Available
Packagers
Dosage forms
FormRouteStrength
Solutionophthalmic15 mg/mL
Solutionoral25 mg/mL
Solutionintravenous25 mg
Injectionintravenous25 mg/mL
Injectionintravenous5 mg/mL
Injection, solutionintravenous25 mg/mL
Injection, solutionintravenous250 mg/50mL
Injection, solutionintravenous5 mg/mL
Injection, solutionintravenous500 mg/100mL
Injection, solutionintravenous750 mg/150mL
Injection, solution, concentrateintravenous500 mg/20mL
Injection, solution, concentrateintravenous750 mg/30mL
Solutionophthalmic5 mg/mL
Solution/ dropsophthalmic5 mg/mL
Solution/ dropstopical5 mg/mL
Tabletoral250 mg/1
Tabletoral500 mg/1
Tabletoral750 mg/1
Tablet, film coatedoral250 mg/1
Tablet, film coatedoral500 mg/1
Tablet, film coatedoral750 mg/1
Solutionintravenous5 mg
Tabletoral250 mg
Tabletoral500 mg
Solutioninhalation240 mg
Tabletoral750 mg
Prices
Unit descriptionCostUnit
Iquix 1.5% Solution 5ml Bottle81.68USD bottle
Levofloxacin hemihydr 100% powder42.69USD g
Levaquin 750 mg tablet28.06USD each
Levaquin 750 mg leva-pak tablet27.51USD tablet
Levaquin 500 mg tablet16.57USD tablet
Iquix 1.5% eye drops15.71USD ml
Levaquin 250 mg tablet13.71USD tablet
Quixin 0.5% eye drops12.21USD ml
Quixin 0.5% Solution11.4USD ml
Levaquin i.v. 25 mg/ml vial1.94USD ml
Levaquin 500 mg/100 ml d5w0.44USD ml
DrugBank does not sell nor buy drugs. Pricing information is supplied for informational purposes only.
Patents
Patent NumberPediatric ExtensionApprovedExpires (estimated)
US5053407 No1993-12-202010-12-20Us
US6806256 Yes2002-08-262022-08-26Us
Properties
StateSolid
Experimental Properties
PropertyValueSource
water solubilityInsolubleNot Available
logP2.1Not Available
Predicted Properties
PropertyValueSource
Water Solubility1.44 mg/mLALOGPS
logP-0.02ALOGPS
logP0.65ChemAxon
logS-2.4ALOGPS
pKa (Strongest Acidic)5.45ChemAxon
pKa (Strongest Basic)6.2ChemAxon
Physiological Charge-1ChemAxon
Hydrogen Acceptor Count7ChemAxon
Hydrogen Donor Count1ChemAxon
Polar Surface Area73.32 Å2ChemAxon
Rotatable Bond Count2ChemAxon
Refractivity94.94 m3·mol-1ChemAxon
Polarizability36.69 Å3ChemAxon
Number of Rings4ChemAxon
Bioavailability1ChemAxon
Rule of FiveYesChemAxon
Ghose FilterYesChemAxon
Veber's RuleYesChemAxon
MDDR-like RuleYesChemAxon
Spectra
Mass Spec (NIST)Not Available
Spectra
Spectrum TypeDescriptionSplash Key
LC-MS/MSLC-MS/MS Spectrum - Quattro_QQQ 10V, N/A (Annotated)splash10-00gm-1315975420-b0c4e6cdef799fda69b4View in MoNA
LC-MS/MSLC-MS/MS Spectrum - Quattro_QQQ 25V, N/A (Annotated)splash10-0abc-3459425420-e8a4ecd2f8aea93fa660View in MoNA
LC-MS/MSLC-MS/MS Spectrum - Quattro_QQQ 40V, N/A (Annotated)splash10-0h9p-3513893500-1d5c8069419fa2c37ebbView in MoNA
1D NMR1H NMR SpectrumNot Available
2D NMR[1H,13C] 2D NMR SpectrumNot Available
References
Synthesis Reference

Valerie Niddam-Hildesheim, “Preparation of levofloxacin and forms thereof.” U.S. Patent US20030130507, issued July 10, 2003.

US20030130507
General ReferencesNot Available
External Links
ATC CodesA02BD10J01MA12J01RA05S01AE05
AHFS Codes
  • 08:12.18
PDB EntriesNot Available
FDA labelDownload (139 KB)
MSDSNot Available
Interactions
Drug Interactions
Drug
Aluminum hydroxideAluminum hydroxide can cause a decrease in the absorption of Levofloxacin resulting in a reduced serum concentration and potentially a decrease in efficacy.
Calcium carbonateCalcium carbonate can cause a decrease in the absorption of Levofloxacin resulting in a reduced serum concentration and potentially a decrease in efficacy.
CitalopramLevofloxacin may increase the QTc-prolonging activities of Citalopram.
DicoumarolLevofloxacin may increase the anticoagulant activities of Dicoumarol.
DidanosineThe serum concentration of Didanosine can be decreased when it is combined with Levofloxacin.
DofetilideLevofloxacin may increase the QTc-prolonging activities of Dofetilide.
FludrocortisoneThe risk or severity of adverse effects can be increased when Fludrocortisone is combined with Levofloxacin.
GoserelinGoserelin may increase the QTc-prolonging activities of Levofloxacin.
InfliximabInfliximab may increase the neuroexcitatory activities of Levofloxacin.
Insulin HumanLevofloxacin may increase the hypoglycemic activities of Insulin Regular.
Iron DextranThe serum concentration of Levofloxacin can be decreased when it is combined with Iron Dextran.
IvabradineIvabradine may increase the QTc-prolonging activities of Levofloxacin.
LanthanumThe serum concentration of Levofloxacin can be decreased when it is combined with Lanthanum.
LeuprolideLeuprolide may increase the QTc-prolonging activities of Levofloxacin.
Magnesium oxideMagnesium oxide can cause a decrease in the absorption of Levofloxacin resulting in a reduced serum concentration and potentially a decrease in efficacy.
Magnesium SulfateThe serum concentration of Levofloxacin can be decreased when it is combined with Magnesium Sulfate.
MifepristoneMifepristone may increase the QTc-prolonging activities of Levofloxacin.
Mycophenolic acidThe serum concentration of Mycophenolic acid can be decreased when it is combined with Levofloxacin.
OctreotideOctreotide may increase the QTc-prolonging activities of Levofloxacin.
Picosulfuric acidThe therapeutic efficacy of Sodium picosulfate can be decreased when used in combination with Levofloxacin.
PorfimerLevofloxacin may increase the photosensitizing activities of Porfimer.
ProbenecidThe serum concentration of Levofloxacin can be increased when it is combined with Probenecid.
QuinaprilThe serum concentration of Levofloxacin can be decreased when it is combined with Quinapril.
SevelamerSevelamer can cause a decrease in the absorption of Levofloxacin resulting in a reduced serum concentration and potentially a decrease in efficacy.
Strontium ranelateThe serum concentration of Levofloxacin can be decreased when it is combined with Strontium ranelate.
SucralfateThe serum concentration of Levofloxacin can be decreased when it is combined with Sucralfate.
TacrolimusLevofloxacin may increase the QTc-prolonging activities of Tacrolimus.
VareniclineThe serum concentration of Varenicline can be increased when it is combined with Levofloxacin.
VerteporfinLevofloxacin may increase the photosensitizing activities of Verteporfin.
Food Interactions
  • Take without regard to meals. Take with water, drink lliberally. Taking this product with orange juice can result in reduced quinolone plasma levels.

Targets

Kind
Protein
Organism
Haemophilus influenzae (strain ATCC 51907 / DSM 11121 / KW20 / Rd)
Pharmacological action
yes
Actions
inhibitor
General Function:
Dna topoisomerase type ii (atp-hydrolyzing) activity
Specific Function:
DNA gyrase negatively supercoils closed circular double-stranded DNA in an ATP-dependent manner and also catalyzes the interconversion of other topological isomers of double-stranded DNA rings, including catenanes and knotted rings.
Gene Name:
gyrA
Uniprot ID:
P43700
Molecular Weight:
97817.145 Da
References
  1. Overington JP, Al-Lazikani B, Hopkins AL: How many drug targets are there? Nat Rev Drug Discov. 2006 Dec;5(12):993-6. [PubMed:17139284 ]
  2. Imming P, Sinning C, Meyer A: Drugs, their targets and the nature and number of drug targets. Nat Rev Drug Discov. 2006 Oct;5(10):821-34. [PubMed:17016423 ]
  3. Schmitz FJ, Hofmann B, Hansen B, Scheuring S, Luckefahr M, Klootwijk M, Verhoef J, Fluit A, Heinz HP, Kohrer K, Jones ME: Relationship between ciprofloxacin, ofloxacin, levofloxacin, sparfloxacin and moxifloxacin (BAY 12-8039) MICs and mutations in grlA, grlB, gyrA and gyrB in 116 unrelated clinical isolates of Staphylococcus aureus. J Antimicrob Chemother. 1998 Apr;41(4):481-4. [PubMed:9598779 ]
  4. Brisse S, Milatovic D, Fluit AC, Verhoef J, Martin N, Scheuring S, Kohrer K, Schmitz FJ: Comparative in vitro activities of ciprofloxacin, clinafloxacin, gatifloxacin, levofloxacin, moxifloxacin, and trovafloxacin against Klebsiella pneumoniae, Klebsiella oxytoca, Enterobacter cloacae, and Enterobacter aerogenes clinical isolates with alterations in GyrA and ParC proteins. Antimicrob Agents Chemother. 1999 Aug;43(8):2051-5. [PubMed:10428935 ]
  5. Messina C, Cafiso V, Campanile F, Santagati M, Stefani S: Rapid method for detection of gyrA and grlA mutations in unrelated strains of Staphylococci susceptible and resistant to levofloxacin. New Microbiol. 2001 Oct;24(4):347-53. [PubMed:11718372 ]
Kind
Protein
Organism
Haemophilus influenzae (strain ATCC 51907 / DSM 11121 / KW20 / Rd)
Pharmacological action
yes
Actions
inhibitor
General Function:
Dna topoisomerase type ii (atp-hydrolyzing) activity
Specific Function:
Topoisomerase IV is essential for chromosome segregation. It relaxes supercoiled DNA. Performs the decatenation events required during the replication of a circular DNA molecule.
Gene Name:
parC
Uniprot ID:
P43702
Molecular Weight:
83366.24 Da
References
  1. Overington JP, Al-Lazikani B, Hopkins AL: How many drug targets are there? Nat Rev Drug Discov. 2006 Dec;5(12):993-6. [PubMed:17139284 ]
  2. Imming P, Sinning C, Meyer A: Drugs, their targets and the nature and number of drug targets. Nat Rev Drug Discov. 2006 Oct;5(10):821-34. [PubMed:17016423 ]
  3. Zheng X, Johnson C, Lu Y, Yanagihara R, Hollingshead S, Crain M, Benjamin W Jr, Waites KB: Clinical isolates of Streptococcus pneumoniae resistant to levofloxacin contain mutations in both gyrA and parC genes. Int J Antimicrob Agents. 2001 Oct;18(4):373-8. [PubMed:11691571 ]
  4. Schafer J, Hovde LB, Simonson D, Rotschafer JC: In vitro pharmacodynamics of moxifloxacin versus levofloxacin against 4 strains of Streptococcus pneumoniae: 1 wild type, 2 first-step parC mutants, and 1 pump mutant. Diagn Microbiol Infect Dis. 2008 Feb;60(2):155-61. Epub 2007 Oct 29. [PubMed:17910998 ]
  5. Deryke CA, Du X, Nicolau DP: Evaluation of bacterial kill when modelling the bronchopulmonary pharmacokinetic profile of moxifloxacin and levofloxacin against parC-containing isolates of Streptococcus pneumoniae. J Antimicrob Chemother. 2006 Sep;58(3):601-9. Epub 2006 Jul 19. [PubMed:16857688 ]
Kind
Protein
Organism
Human
Pharmacological action
yes
Actions
inhibitor
General Function:
Ubiquitin binding
Specific Function:
Control of topological states of DNA by transient breakage and subsequent rejoining of DNA strands. Topoisomerase II makes double-strand breaks. Essential during mitosis and meiosis for proper segregation of daughter chromosomes. May play a role in regulating the period length of ARNTL/BMAL1 transcriptional oscillation (By similarity).
Gene Name:
TOP2A
Uniprot ID:
P11388
Molecular Weight:
174383.88 Da
References
  1. Chen X, Ji ZL, Chen YZ: TTD: Therapeutic Target Database. Nucleic Acids Res. 2002 Jan 1;30(1):412-5. [PubMed:11752352 ]

Enzymes

Kind
Protein
Organism
Human
Pharmacological action
unknown
Actions
inhibitor
General Function:
Oxidoreductase activity, acting on paired donors, with incorporation or reduction of molecular oxygen, reduced flavin or flavoprotein as one donor, and incorporation of one atom of oxygen
Specific Function:
Cytochromes P450 are a group of heme-thiolate monooxygenases. In liver microsomes, this enzyme is involved in an NADPH-dependent electron transport pathway. It oxidizes a variety of structurally unrelated compounds, including steroids, fatty acids, and xenobiotics. Most active in catalyzing 2-hydroxylation. Caffeine is metabolized primarily by cytochrome CYP1A2 in the liver through an initial N...
Gene Name:
CYP1A2
Uniprot ID:
P05177
Molecular Weight:
58293.76 Da
References
  1. Bellon A, Perez-Garcia G, Coverdale JH, Chacko RC: Seizures associated with levofloxacin: case presentation and literature review. Eur J Clin Pharmacol. 2009 Oct;65(10):959-62. doi: 10.1007/s00228-009-0717-5. Epub 2009 Aug 26. [PubMed:19707748 ]
  2. Preissner S, Kroll K, Dunkel M, Senger C, Goldsobel G, Kuzman D, Guenther S, Winnenburg R, Schroeder M, Preissner R: SuperCYP: a comprehensive database on Cytochrome P450 enzymes including a tool for analysis of CYP-drug interactions. Nucleic Acids Res. 2010 Jan;38(Database issue):D237-43. doi: 10.1093/nar/gkp970. Epub 2009 Nov 24. [PubMed:19934256 ]
Kind
Protein
Organism
Human
Pharmacological action
unknown
Actions
inhibitor
General Function:
Vitamin d3 25-hydroxylase activity
Specific Function:
Cytochromes P450 are a group of heme-thiolate monooxygenases. In liver microsomes, this enzyme is involved in an NADPH-dependent electron transport pathway. It performs a variety of oxidation reactions (e.g. caffeine 8-oxidation, omeprazole sulphoxidation, midazolam 1'-hydroxylation and midazolam 4-hydroxylation) of structurally unrelated compounds, including steroids, fatty acids, and xenobiot...
Gene Name:
CYP3A4
Uniprot ID:
P08684
Molecular Weight:
57342.67 Da
References
  1. Preissner S, Kroll K, Dunkel M, Senger C, Goldsobel G, Kuzman D, Guenther S, Winnenburg R, Schroeder M, Preissner R: SuperCYP: a comprehensive database on Cytochrome P450 enzymes including a tool for analysis of CYP-drug interactions. Nucleic Acids Res. 2010 Jan;38(Database issue):D237-43. doi: 10.1093/nar/gkp970. Epub 2009 Nov 24. [PubMed:19934256 ]

Transporters

Kind
Protein
Organism
Human
Pharmacological action
unknown
Actions
substrateinhibitor
General Function:
Xenobiotic-transporting atpase activity
Specific Function:
Energy-dependent efflux pump responsible for decreased drug accumulation in multidrug-resistant cells.
Gene Name:
ABCB1
Uniprot ID:
P08183
Molecular Weight:
141477.255 Da
References
  1. Ito T, Yano I, Tanaka K, Inui KI: Transport of quinolone antibacterial drugs by human P-glycoprotein expressed in a kidney epithelial cell line, LLC-PK1. J Pharmacol Exp Ther. 1997 Aug;282(2):955-60. [PubMed:9262363 ]
  2. Yamaguchi H, Yano I, Hashimoto Y, Inui KI: Secretory mechanisms of grepafloxacin and levofloxacin in the human intestinal cell line caco-2. J Pharmacol Exp Ther. 2000 Oct;295(1):360-6. [PubMed:10992002 ]
  3. Yamaguchi H, Yano I, Saito H, Inui K: Effect of cisplatin-induced acute renal failure on bioavailability and intestinal secretion of quinolone antibacterial drugs in rats. Pharm Res. 2004 Feb;21(2):330-8. [PubMed:15032316 ]
Kind
Protein
Organism
Human
Pharmacological action
unknown
Actions
substrate
General Function:
Sodium-independent organic anion transmembrane transporter activity
Specific Function:
Involved in the renal elimination of endogenous and exogenous organic anions. Functions as organic anion exchanger when the uptake of one molecule of organic anion is coupled with an efflux of one molecule of endogenous dicarboxylic acid (glutarate, ketoglutarate, etc). Mediates the sodium-independent uptake of 2,3-dimercapto-1-propanesulfonic acid (DMPS) (By similarity). Mediates the sodium-in...
Gene Name:
SLC22A6
Uniprot ID:
Q4U2R8
Molecular Weight:
61815.78 Da
References
  1. Uwai Y, Okuda M, Takami K, Hashimoto Y, Inui K: Functional characterization of the rat multispecific organic anion transporter OAT1 mediating basolateral uptake of anionic drugs in the kidney. FEBS Lett. 1998 Nov 6;438(3):321-4. [PubMed:9827570 ]
Kind
Protein
Organism
Human
Pharmacological action
unknown
Actions
inhibitor
General Function:
Quaternary ammonium group transmembrane transporter activity
Specific Function:
Mediates tubular uptake of organic compounds from circulation. Mediates the influx of agmatine, dopamine, noradrenaline (norepinephrine), serotonin, choline, famotidine, ranitidine, histamin, creatinine, amantadine, memantine, acriflavine, 4-[4-(dimethylamino)-styryl]-N-methylpyridinium ASP, amiloride, metformin, N-1-methylnicotinamide (NMN), tetraethylammonium (TEA), 1-methyl-4-phenylpyridiniu...
Gene Name:
SLC22A2
Uniprot ID:
O15244
Molecular Weight:
62579.99 Da
References
  1. Urakami Y, Akazawa M, Saito H, Okuda M, Inui K: cDNA cloning, functional characterization, and tissue distribution of an alternatively spliced variant of organic cation transporter hOCT2 predominantly expressed in the human kidney. J Am Soc Nephrol. 2002 Jul;13(7):1703-10. [PubMed:12089365 ]
  2. Okuda M, Urakami Y, Saito H, Inui K: Molecular mechanisms of organic cation transport in OCT2-expressing Xenopus oocytes. Biochim Biophys Acta. 1999 Mar 4;1417(2):224-31. [PubMed:10082798 ]
Kind
Protein
Organism
Human
Pharmacological action
unknown
Actions
inhibitor
General Function:
Symporter activity
Specific Function:
Sodium-ion dependent, low affinity carnitine transporter. Probably transports one sodium ion with one molecule of carnitine. Also transports organic cations such as tetraethylammonium (TEA) without the involvement of sodium. Relative uptake activity ratio of carnitine to TEA is 1.78. A key substrate of this transporter seems to be ergothioneine (ET).
Gene Name:
SLC22A4
Uniprot ID:
Q9H015
Molecular Weight:
62154.48 Da
References
  1. Yabuuchi H, Tamai I, Nezu J, Sakamoto K, Oku A, Shimane M, Sai Y, Tsuji A: Novel membrane transporter OCTN1 mediates multispecific, bidirectional, and pH-dependent transport of organic cations. J Pharmacol Exp Ther. 1999 May;289(2):768-73. [PubMed:10215651 ]
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Drug created on June 13, 2005 07:24 / Updated on May 29, 2016 03:21