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Identification
NameVerapamil
Accession NumberDB00661  (APRD00335)
TypeSmall Molecule
GroupsApproved
Description

A calcium channel blocker that is a class IV anti-arrhythmia agent. [PubChem]

Structure
Thumb
Synonyms
Calan
Calan sr
Covera-hs
CP-16533-1
CP-165331
D-365
Iproveratril
Isoptin
Isoptin sr
Tarka
Vérapamil
Verapamil
Verapamilo
Verapamilum
Verelan
External Identifiers
  • CP 16533-1
  • D 365
Prescription Products
NameDosageStrengthRouteLabellerMarketing StartMarketing End
Alti-verapamil - 120mgtablet120 mgoralAltimed Pharma Inc.1990-12-312004-08-03Canada
Alti-verapamil - 80mgtablet80 mgoralAltimed Pharma Inc.1990-12-312004-08-03Canada
Calantablet, film coated80 mg/1oralG.D. Searle LLC Division of Pfizer Inc1984-09-102016-04-23Us
Calantablet, film coated120 mg/1oralG.D. Searle LLC Division of Pfizer Inc1984-09-102016-04-23Us
Calan SRtablet, film coated, extended release180 mg/1oralG.D. Searle LLC Division of Pfizer Inc1989-12-152016-04-23Us
Calan SRtablet, film coated, extended release120 mg/1oralG.D. Searle LLC Division of Pfizer Inc1991-03-062016-04-23Us
Calan SRtablet, film coated, extended release240 mg/1oralG.D. Searle LLC Division of Pfizer Inc1986-12-162016-04-23Us
Covera-HStablet, extended release240 mg/1oralG.D. Searle LLC Division of Pfizer Inc1996-02-262016-04-23Us
Covera-HStablet, extended release180 mg/1oralG.D. Searle LLC Division of Pfizer Inc1996-02-262016-04-23Us
Covera-HStablet (extended-release)240 mgoralPfizer Canada Inc1997-11-132013-02-15Canada
Covera-HStablet (extended-release)180 mgoralPfizer Canada Inc1997-11-132013-02-15Canada
Dom-verapamil SR 240mg Tabletstablet (extended-release)240 mgoralDominion Pharmacal1999-12-16Not applicableCanada
Isoptin Inj 2.5mg/mlliquid2.5 mgintravenousAbbott Laboratories, Limited1984-12-312007-07-31Canada
Isoptin SRtablet (extended-release)240 mgoralBgp Pharma Ulc1988-12-31Not applicableCanada
Isoptin SRtablet (extended-release)180 mgoralBgp Pharma Ulc1994-04-21Not applicableCanada
Isoptin SRtablet (extended-release)120 mgoralBgp Pharma Ulc1991-12-31Not applicableCanada
Isoptin Tab 120mgtablet120 mgoralAbbott Laboratories, Limited1982-12-312007-07-31Canada
Isoptin Tab 80mgtablet80 mgoralAbbott Laboratories, Limited1982-12-312007-07-31Canada
Med Verapamil Tabletstablet120 mgoralMedican Pharma Incorporated1999-03-082011-03-29Canada
Med Verapamil Tabletstablet80 mgoralMedican Pharma Incorporated1999-03-082011-03-29Canada
Mylan-verapamiltablet120 mgoralMylan Pharmaceuticals Ulc1998-05-11Not applicableCanada
Mylan-verapamiltablet80 mgoralMylan Pharmaceuticals Ulc1998-05-25Not applicableCanada
Mylan-verapamil SRtablet (extended-release)180 mgoralMylan Pharmaceuticals Ulc1996-12-31Not applicableCanada
Mylan-verapamil SRtablet (extended-release)240 mgoralMylan Pharmaceuticals UlcNot applicableNot applicableCanada
Mylan-verapamil SRtablet (extended-release)180 mgoralMylan Pharmaceuticals UlcNot applicableNot applicableCanada
Mylan-verapamil SRtablet (extended-release)120 mgoralMylan Pharmaceuticals UlcNot applicableNot applicableCanada
Mylan-verapamil SRtablet (extended-release)240 mgoralMylan Pharmaceuticals Ulc1996-12-31Not applicableCanada
Mylan-verapamil SRtablet (extended-release)120 mgoralMylan Pharmaceuticals Ulc1996-12-31Not applicableCanada
Novo-veramiltablet120 mgoralTeva Canada Limited1989-12-31Not applicableCanada
Novo-veramiltablet80 mgoralTeva Canada Limited1989-12-31Not applicableCanada
Novo-veramil SRtablet (extended-release)240 mgoralTeva Canada Limited1996-12-31Not applicableCanada
Nu-verap SRtablet (extended-release)240 mgoralNu Pharm Inc2004-07-192012-09-04Canada
Nu-verap SRtablet (extended-release)180 mgoralNu Pharm IncNot applicableNot applicableCanada
Nu-verap SRtablet (extended-release)120 mgoralNu Pharm IncNot applicableNot applicableCanada
Nu-verap Tab 120mgtablet120 mgoralNu Pharm Inc1990-12-312012-09-04Canada
Nu-verap Tab 80mgtablet80 mgoralNu Pharm Inc1990-12-312012-09-04Canada
Penta-verapamil - 120mgtablet120 mgoralPentapharm Ltd.1997-06-252004-07-30Canada
Penta-verapamil - 80mgtablet80 mgoralPentapharm Ltd.1997-06-252004-07-30Canada
PHL-verapamil SRtablet (extended-release)240 mgoralPharmel Inc2002-05-31Not applicableCanada
PMS-verapamil SRtablet (extended-release)240 mgoralPharmascience Inc1999-09-01Not applicableCanada
Pro-verapamil SRtablet (extended-release)180 mgoralPro Doc Limitee2009-06-15Not applicableCanada
Pro-verapamil SRtablet (extended-release)120 mgoralPro Doc Limitee2009-06-15Not applicableCanada
Pro-verapamil SRtablet (extended-release)240 mgoralPro Doc Limitee2008-07-09Not applicableCanada
Riva-verapamil SRtablet (extended-release)240 mgoralLaboratoire Riva Inc2005-09-14Not applicableCanada
Taro-verapamil Tab 120mgtablet120 mgoralTaro Pharmaceuticals Inc1993-12-312000-08-31Canada
Taro-verapamil Tab 80mgtablet80 mgoralTaro Pharmaceuticals Inc1993-12-312000-08-31Canada
Verapamil Hydrochloridecapsule, extended release300 mg/1oralKremers Urban Pharmaceuticals Inc.1998-11-252016-04-05Us
Verapamil Hydrochloridecapsule, delayed release pellets360 mg/1oralActavis Pharma, Inc.1990-05-292016-04-23Us
Verapamil Hydrochloridecapsule, delayed release pellets240 mg/1oralActavis Pharma, Inc.1990-05-292016-04-23Us
Verapamil Hydrochloridecapsule, delayed release pellets360 mg/1oralbryant ranch prepack1990-05-292016-04-05Us
Verapamil Hydrochloridecapsule, extended release200 mg/1oralKremers Urban Pharmaceuticals Inc.1998-11-252016-04-05Us
Verapamil Hydrochloridecapsule, delayed release pellets180 mg/1oralActavis Pharma, Inc.1990-05-292016-04-23Us
Verapamil Hydrochloridecapsule, extended release100 mg/1oralKremers Urban Pharmaceuticals Inc.1998-11-252016-04-05Us
Verapamil Hydrochloridecapsule, delayed release pellets120 mg/1oralActavis Pharma, Inc.1990-05-292016-04-23Us
Verapamil Hydrochloridecapsule, delayed release pellets360 mg/1oralPhysicians Total Care, Inc.2009-02-122016-04-05Us
Verapamil Hydrochloridetablet, film coated, extended release240 mg/1oralState of Florida DOH Central Pharmacy2009-07-012016-04-05Us
Verapamil Hydrochloridecapsule, delayed release pellets180 mg/1oralCarilion Materials Management1990-05-292016-04-05Us
Verapamil Hydrochloridetablet, film coated, extended release120 mg/1oralState of Florida DOH Central Pharmacy2009-07-012016-04-05Us
Verapamil Hydrochloridecapsule, delayed release pellets120 mg/1oralPreferred Pharmaceuticals, Inc.2012-07-242016-04-05Us
Verapamil Hydrochloride Injection 2.5mg/mlsolution2.5 mgintravenousHospira Healthcare Corporation1994-12-31Not applicableCanada
Verapamil Hydrochloride Injection USPliquid2.5 mgintravenousSandoz Canada Incorporated1995-12-31Not applicableCanada
Verapamil Injection 2.5mg/mlliquid2.5 mgintravenousNovopharm Limited1994-12-312005-08-10Canada
Verapamil SRtablet (extended-release)240 mgoralSorres Pharma Inc2009-06-222014-06-20Canada
Verapamil Tab 80mgtablet80 mgoralPro Doc Limitee1990-12-312012-07-23Canada
Verapamil-120 Tabtablet120 mgoralPro Doc Limitee1990-12-312009-07-23Canada
Verelancapsule, delayed release pellets120 mg/1oralUCB, Inc.1990-05-292016-04-23Us
Verelancapsule, delayed release pellets360 mg/1oralKremers Urban Pharmaceuticals Inc.1990-05-292016-04-05Us
Verelancapsule, delayed release pellets180 mg/1oralUCB, Inc.1990-05-292016-04-23Us
Verelancapsule, delayed release pellets240 mg/1oralKremers Urban Pharmaceuticals Inc.1990-05-292016-04-05Us
Verelancapsule, delayed release pellets180 mg/1oralKremers Urban Pharmaceuticals Inc.1990-05-292016-04-05Us
Verelancapsule (sustained-release)120 mgoralRecro Gainesville Llc1994-12-31Not applicableCanada
Verelancapsule (sustained-release)180 mgoralRecro Gainesville Llc1994-12-31Not applicableCanada
Verelancapsule, delayed release pellets120 mg/1oralKremers Urban Pharmaceuticals Inc.1990-05-292016-04-05Us
Verelancapsule, delayed release pellets360 mg/1oralPhysicians Total Care, Inc.2003-06-122016-04-05Us
Verelancapsule, delayed release pellets240 mg/1oralPhysicians Total Care, Inc.2004-08-122016-04-05Us
Verelancapsule (sustained-release)240 mgoralRecro Gainesville Llc1994-12-31Not applicableCanada
Verelancapsule, delayed release pellets360 mg/1oralUCB, Inc.1990-05-292016-04-23Us
Verelancapsule, delayed release pellets240 mg/1oralUCB, Inc.1990-05-292016-04-23Us
Verelan PMcapsule, extended release300 mg/1oralbryant ranch prepack1998-11-252016-04-05Us
Verelan PMcapsule, extended release300 mg/1oralUCB, Inc.1998-11-252016-04-23Us
Verelan PMcapsule, extended release200 mg/1oralUCB, Inc.1998-11-252016-04-23Us
Verelan PMcapsule, extended release100 mg/1oralUCB, Inc.1998-11-252016-04-23Us
Verelan PMcapsule, extended release300 mg/1oralKremers Urban Pharmaceuticals Inc.1998-11-252016-04-05Us
Verelan PMcapsule, extended release200 mg/1oralKremers Urban Pharmaceuticals Inc.1998-11-252016-04-05Us
Verelan PMcapsule, extended release100 mg/1oralKremers Urban Pharmaceuticals Inc.1998-11-252016-04-05Us
Generic Prescription Products
NameDosageStrengthRouteLabellerMarketing StartMarketing End
Apo-verap SRtablet (extended-release)240 mgoralApotex Inc2003-04-24Not applicableCanada
Apo-verap SRtablet (extended-release)180 mgoralApotex Inc2003-04-24Not applicableCanada
Apo-verap SRtablet (extended-release)120 mgoralApotex Inc2003-04-24Not applicableCanada
Apo-verap Tab 80mgtablet80 mgoralApotex Inc1989-12-31Not applicableCanada
Apo-verap Tablet 120mgtablet120 mgoralApotex Inc1989-12-31Not applicableCanada
Verapamiltablet, film coated, extended release120 mg/1oralSt Marys Medical Park Pharmacy2014-04-212016-04-05Us
Verapamiltablet, extended release180 mg/1oralPd Rx Pharmaceuticals, Inc.2011-08-052016-04-05Us
Verapamiltablet, film coated, extended release180 mg/1oralSt Marys Medical Park Pharmacy2013-02-052016-04-05Us
Verapamiltablet, film coated, extended release180 mg/1oralUnit Dose Services2012-11-192016-04-05Us
Verapamiltablet, film coated, extended release240 mg/1oralApotex Corp.2012-11-192016-04-05Us
Verapamiltablet, film coated, extended release240 mg/1oralAmerican Health Packaging2014-01-142016-04-30Us
Verapamiltablet, film coated, extended release180 mg/1oralApotex Corp.2012-11-192016-04-05Us
Verapamiltablet, film coated, extended release180 mg/1oralAmerican Health Packaging2014-01-142015-12-31Us
Verapamiltablet, film coated, extended release120 mg/1oralAmerican Health Packaging2014-01-142016-03-31Us
Verapamiltablet, film coated, extended release120 mg/1oralApotex Corp.2012-11-192016-04-05Us
Verapamil Hydrochloridetablet, film coated, extended release240 mg/1oralPhysicians Total Care, Inc.2000-05-092016-04-05Us
Verapamil Hydrochloridetablet, film coated, extended release240 mg/1oralGolden State Medical Supply, Inc2014-12-042016-04-05Us
Verapamil Hydrochloridetablet, film coated80 mg/1oralActavis Pharma, Inc.1986-10-012016-04-23Us
Verapamil Hydrochloridetablet, extended release240 mg/1oralSun Pharmaceutical Industries, Inc.2012-01-012016-04-05Us
Verapamil Hydrochloridetablet, extended release240 mg/1oralPreferred Pharmaceuticals, Inc.2013-09-262016-04-05Us
Verapamil Hydrochloridetablet, film coated120 mg/1oralbryant ranch prepack1986-10-012016-04-05Us
Verapamil Hydrochloridetablet, film coated120 mg/1oralActavis Pharma, Inc.1986-10-012016-04-23Us
Verapamil Hydrochloridetablet, extended release180 mg/1oralPd Rx Pharmaceuticals, Inc.2012-01-012016-04-05Us
Verapamil Hydrochloridetablet, film coated120 mg/1oralBlenheim Pharmacal, Inc.2013-12-172016-04-05Us
Verapamil Hydrochloridetablet, film coated, extended release180 mg/1oralNcs Health Care Of Ky, Inc Dba Vangard Labs2012-02-232016-04-23Us
Verapamil Hydrochloridetablet, film coated, extended release180 mg/1oralMylan Institutional Inc.1998-11-152016-04-05Us
Verapamil Hydrochloridetablet80 mg/1oralREMEDYREPACK INC.2011-11-162016-04-05Us
Verapamil Hydrochlorideinjection, solution2.5 mg/mLintravenousHospira, Inc.1998-10-202016-04-23Us
Verapamil Hydrochloridetablet, film coated120 mg/1oralPhysicians Total Care, Inc.1996-02-052016-04-05Us
Verapamil Hydrochloridetablet, extended release240 mg/1oralPd Rx Pharmaceuticals, Inc.2012-01-012016-04-05Us
Verapamil Hydrochlorideinjection, solution2.5 mg/mLintravenousGeneral Injectables & Vaccines, Inc2010-03-012016-04-05Us
Verapamil Hydrochloridetablet, film coated, extended release120 mg/1oralTeva Pharmaceuticals USA Inc2014-03-102016-04-23Us
Verapamil Hydrochloridecapsule, extended release120 mg/1oralMylan Institutional Inc.1999-10-012016-04-05Us
Verapamil Hydrochloridetablet, extended release180 mg/1oralSun Pharmaceutical Industries, Inc.2012-01-012016-04-05Us
Verapamil Hydrochlorideinjection, solution2.5 mg/mLintravenousCardinal Health2011-03-252016-04-05Us
Verapamil Hydrochloridetablet, film coated, extended release180 mg/1oralbryant ranch prepack2010-04-202016-04-05Us
Verapamil Hydrochloridetablet120 mg/1oralREMEDYREPACK INC.2011-12-132016-04-05Us
Verapamil Hydrochloridetablet, film coated, extended release240 mg/1oralBlenheim Pharmacal, Inc.2010-08-202016-04-05Us
Verapamil Hydrochloridetablet, film coated, extended release120 mg/1oralMylan Institutional Inc.1998-04-172016-04-05Us
Verapamil Hydrochloridetablet, extended release180 mg/1oralREMEDYREPACK INC.2011-08-242016-04-05Us
Verapamil Hydrochlorideinjection, solution2.5 mg/mLintravenousHospira, Inc.1987-05-062016-04-23Us
Verapamil Hydrochloridetablet, film coated80 mg/1oralPhysicians Total Care, Inc.1995-04-242016-04-05Us
Verapamil Hydrochloridetablet, film coated, extended release180 mg/1oralMylan Pharmaceuticals Inc.1997-09-222016-04-23Us
Verapamil Hydrochlorideinjection, solution2.5 mg/mLintravenousGeneral Injectables & Vaccines, Inc2010-09-012016-04-05Us
Verapamil Hydrochloridetablet, extended release120 mg/1oralSun Pharmaceutical Industries, Inc.2012-01-012016-04-05Us
Verapamil Hydrochloridetablet, film coated, extended release240 mg/1oralCardinal Health2009-09-172016-04-05Us
Verapamil Hydrochloridetablet, film coated, extended release240 mg/1oralbryant ranch prepack1992-08-012016-04-05Us
Verapamil Hydrochloridetablet, film coated, extended release180 mg/1oralGolden State Medical Supply, Inc2014-12-042016-04-05Us
Verapamil Hydrochloridetablet, film coated, extended release180 mg/1oralGlenmark Pharmaceuticals Inc., Usa2011-08-052016-04-05Us
Verapamil Hydrochloridetablet40 mg/1oralHeritage Pharmaceuticals Inc.2011-01-072016-04-05Us
Verapamil Hydrochloridetablet, film coated, extended release240 mg/1oralBlenheim Pharmacal, Inc.2011-02-152016-04-05Us
Verapamil Hydrochloridetablet, film coated, extended release240 mg/1oralMylan Institutional Inc.1996-04-152016-04-05Us
Verapamil Hydrochloridetablet, extended release240 mg/1oralREMEDYREPACK INC.2011-12-072016-04-05Us
Verapamil Hydrochlorideinjection, solution2.5 mg/mLintravenousHospira, Inc.1987-05-062016-04-23Us
Verapamil Hydrochloridetablet, film coated120 mg/1oralA S Medication Solutions Llc1986-10-012016-04-05Us
Verapamil Hydrochloridetablet, film coated, extended release120 mg/1oralMylan Pharmaceuticals Inc.1997-02-252016-04-23Us
Verapamil Hydrochloridetablet120 mg/1oralREMEDYREPACK INC.2014-06-272016-04-05Us
Verapamil Hydrochloridetablet, film coated, extended release240 mg/1oralPd Rx Pharmaceuticals, Inc.2009-09-172016-04-05Us
Verapamil Hydrochloridetablet, film coated80 mg/1oralCardinal Health1986-10-012016-04-05Us
Verapamil Hydrochloridetablet, film coated, extended release120 mg/1oralGolden State Medical Supply, Inc2014-12-042016-04-05Us
Verapamil Hydrochloridetablet, film coated, extended release120 mg/1oralGlenmark Pharmaceuticals Inc., Usa2011-08-052016-04-05Us
Verapamil Hydrochloridetablet120 mg/1oralHeritage Pharmaceuticals Inc.2011-01-072016-04-05Us
Verapamil Hydrochloridetablet, film coated120 mg/1oralMajor Pharmaceuticals1986-10-012016-04-05Us
Verapamil Hydrochloridetablet, film coated, extended release120 mg/1oralUnit Dose Services2011-08-052016-04-05Us
Verapamil Hydrochloridetablet80 mg/1oralREMEDYREPACK INC.2011-08-082016-04-05Us
Verapamil Hydrochloridecapsule, extended release240 mg/1oralMylan Pharmaceuticals Inc.1999-05-192016-04-23Us
Verapamil Hydrochloridetablet, extended release180 mg/1oralState of Florida DOH Central Pharmacy2014-11-012016-04-05Us
Verapamil Hydrochloridetablet, film coated, extended release240 mg/1oralMylan Pharmaceuticals Inc.1996-03-252016-04-23Us
Verapamil Hydrochloridetablet, film coated, extended release120 mg/1oralREMEDYREPACK INC.2013-05-152016-04-05Us
Verapamil Hydrochloridecapsule, extended release200 mg/1oralPhysicians Total Care, Inc.2010-05-172016-04-05Us
Verapamil Hydrochloridetablet, film coated80 mg/1oralClinical Solutions Wholesale1986-10-012016-04-05Us
Verapamil Hydrochloridetablet, film coated, extended release240 mg/1oralGlenmark Pharmaceuticals Inc., Usa2009-09-172016-04-05Us
Verapamil Hydrochloridetablet, extended release180 mg/1oralREMEDYREPACK INC.2011-07-252016-04-05Us
Verapamil Hydrochloridecapsule, extended release180 mg/1oralMylan Pharmaceuticals Inc.1999-05-192016-04-23Us
Verapamil Hydrochloridetablet, film coated, extended release120 mg/1oralState of Florida DOH Central Pharmacy2009-07-012016-04-05Us
Verapamil Hydrochloridetablet, film coated120 mg/1oralMylan Pharmaceuticals Inc.2012-08-152016-04-23Us
Verapamil Hydrochloridetablet, film coated, extended release240 mg/1oralREMEDYREPACK INC.2013-05-142016-04-05Us
Verapamil Hydrochloridetablet, film coated120 mg/1oralPd Rx Pharmaceuticals, Inc.2011-05-042016-04-05Us
Verapamil Hydrochloridecapsule, extended release300 mg/1oralPhysicians Total Care, Inc.2007-12-202016-04-05Us
Verapamil Hydrochloridetablet, film coated, extended release240 mg/1oralSt Marys Medical Park Pharmacy2013-05-222016-04-05Us
Verapamil Hydrochloridetablet, film coated40 mg/1oralClinical Solutions Wholesale1993-06-292016-04-05Us
Verapamil Hydrochloridetablet, film coated40 mg/1oralCarilion Materials Management1993-06-292016-04-05Us
Verapamil Hydrochloridetablet80 mg/1oralHeritage Pharmaceuticals Inc.2011-01-072016-04-05Us
Verapamil Hydrochloridetablet, film coated80 mg/1oralMajor Pharmaceuticals1986-10-012016-04-05Us
Verapamil Hydrochloridecapsule, extended release120 mg/1oralMylan Pharmaceuticals Inc.1999-05-192016-04-23Us
Verapamil Hydrochloridetablet, film coated, extended release120 mg/1oralState of Florida DOH Central Pharmacy2014-01-012016-04-05Us
Verapamil Hydrochloridetablet, film coated80 mg/1oralMylan Pharmaceuticals Inc.2012-08-152016-04-23Us
Verapamil Hydrochloridetablet240 mg/1oralREMEDYREPACK INC.2012-10-022016-04-05Us
Verapamil Hydrochlorideinjection, solution2.5 mg/mLintravenousCardinal Health2011-03-252016-04-05Us
Verapamil Hydrochloridetablet, film coated, extended release120 mg/1oralPhysicians Total Care, Inc.2000-11-282016-04-05Us
Verapamil Hydrochloridetablet, film coated, extended release240 mg/1oralClinical Solutions Wholesale2009-09-172016-04-05Us
Verapamil Hydrochloridetablet, film coated, extended release240 mg/1oralA S Medication Solutions2009-09-172016-04-01Us
Verapamil Hydrochloridetablet, film coated, extended release240 mg/1oralRebel Distributors Corp2010-04-202016-04-05Us
Verapamil Hydrochloridetablet, film coated120 mg/1oralNcs Health Care Of Ky, Inc Dba Vangard Labs1986-10-012016-04-23Us
Verapamil Hydrochloridetablet, film coated, extended release240 mg/1oralUnit Dose Services2009-09-172016-04-05Us
Verapamil Hydrochloridecapsule, extended release120 mg/1oralREMEDYREPACK INC.2010-11-222016-04-05Us
Verapamil Hydrochlorideinjection, solution2.5 mg/mLintravenousCardinal Health2011-03-252016-04-05Us
Verapamil Hydrochloridetablet, film coated, extended release180 mg/1oralPhysicians Total Care, Inc.1996-01-152016-04-05Us
Verapamil Hydrochloridetablet, film coated120 mg/1oralClinical Solutions Wholesale1986-10-012016-04-05Us
Verapamil Hydrochloridetablet120 mg/1oralRebel Distributors Corp1996-02-052016-04-05Us
Verapamil Hydrochloridetablet, film coated80 mg/1oralNcs Health Care Of Ky, Inc Dba Vangard Labs1986-10-012016-04-23Us
Verapamil Hydrochloridetablet120 mg/1oralA S Medication Solutions Llc2011-01-072016-04-05Us
Verapamil Hydrochloridetablet, film coated, extended release240 mg/1oralAphena Pharma Solutions Tennessee, Llc1996-03-252016-04-05Us
Verapamil Hydrochloridetablet, film coated, extended release180 mg/1oralState of Florida DOH Central Pharmacy2009-07-012016-04-05Us
Verapamil Hydrochloridetablet, film coated, extended release240 mg/1oralTeva Pharmaceuticals USA Inc2014-04-072016-04-23Us
Verapamil Hydrochloridetablet, film coated, extended release180 mg/1oralREMEDYREPACK INC.2013-03-142016-04-05Us
Verapamil Hydrochloridetablet, film coated, extended release240 mg/1oralCardinal Health2012-07-122016-04-05Us
Verapamil Hydrochloridecapsule, extended release100 mg/1oralPhysicians Total Care, Inc.2008-08-072016-04-05Us
Verapamil Hydrochloridetablet, film coated, extended release180 mg/1oralClinical Solutions Wholesale2011-08-052016-04-05Us
Verapamil Hydrochloridetablet, film coated, extended release240 mg/1oralPreferred Pharmaceuticals, Inc.2012-06-042016-04-05Us
Verapamil Hydrochloridetablet, film coated, extended release120 mg/1oralbryant ranch prepack1997-10-102016-04-05Us
Verapamil Hydrochloridetablet, film coated40 mg/1oralActavis Pharma, Inc.1993-06-292016-04-23Us
Verapamil Hydrochloridetablet80 mg/1oralRebel Distributors Corp1995-04-242016-04-05Us
Verapamil Hydrochloridetablet, film coated, extended release240 mg/1oralNcs Health Care Of Ky, Inc Dba Vangard Labs2012-02-232016-04-23Us
Verapamil Hydrochloridetablet, film coated, extended release240 mg/1oralLake Erie Medical DBA Quality Care Products LLC2009-09-172016-04-05Us
Verapamil Hydrochloridetablet, film coated, extended release180 mg/1oralAphena Pharma Solutions Tennessee, Llc1997-09-222016-04-05Us
Verapamil Hydrochloridetablet, film coated, extended release240 mg/1oralState of Florida DOH Central Pharmacy2009-07-012016-04-05Us
Verapamil Hydrochloridetablet, film coated, extended release180 mg/1oralTeva Pharmaceuticals USA Inc2014-01-292016-04-23Us
Verapamil Hydrochloridetablet, extended release240 mg/301oralNorthwind Pharmaceuticals2014-05-272016-04-05Us
Verapamil Hydrochloride PMcapsule, extended release100 mg/1oralMylan Pharmaceuticals Inc.2007-08-092016-04-23Us
Verapamil Hydrochloride PMcapsule, extended release100 mg/1oralAvera Mc Kennan Hospital2015-06-252016-04-05Us
Verapamil Hydrochloride PMcapsule, extended release300 mg/1oralMylan Pharmaceuticals Inc.2007-08-092016-04-23Us
Verapamil Hydrochloride PMcapsule, extended release200 mg/1oralMylan Pharmaceuticals Inc.2007-08-092016-04-23Us
Over the Counter ProductsNot Available
International Brands
NameCompany
BosoptinBosnalijek
IsoptinAbbott
VerisopGerard
VerminRatiopharm
VerminePharmasant
VerogalidIvax
Verogalid ERIvax
VerpamilMylan
VertabTrinity-Chiesi
VetrimilCCPC
ZolveraRosemont
Brand mixtures
NameLabellerIngredients
TarkaAbb Vie Inc.
Trandolapril and Verapamil HydrochlorideGlenmark Pharmaceuticals Inc., Usa
Trandolapril and Verapamil Hydrochloride ERGreenstone LLC
Salts
Name/CASStructureProperties
Verapamil Hydrochloride
152-11-4
Thumb
  • InChI Key: DOQPXTMNIUCOSY-UHFFFAOYNA-N
  • Monoisotopic Mass: 490.259835453
  • Average Mass: 491.063
DBSALT000534
Categories
UNIICJ0O37KU29
CAS number52-53-9
WeightAverage: 454.6016
Monoisotopic: 454.283157714
Chemical FormulaC27H38N2O4
InChI KeyInChIKey=SGTNSNPWRIOYBX-UHFFFAOYSA-N
InChI
InChI=1S/C27H38N2O4/c1-20(2)27(19-28,22-10-12-24(31-5)26(18-22)33-7)14-8-15-29(3)16-13-21-9-11-23(30-4)25(17-21)32-6/h9-12,17-18,20H,8,13-16H2,1-7H3
IUPAC Name
2-(3,4-dimethoxyphenyl)-5-{[2-(3,4-dimethoxyphenyl)ethyl](methyl)amino}-2-(propan-2-yl)pentanenitrile
SMILES
COC1=C(OC)C=C(CCN(C)CCCC(C#N)(C(C)C)C2=CC(OC)=C(OC)C=C2)C=C1
Taxonomy
DescriptionThis compound belongs to the class of organic compounds known as phenylbutylamines. These are compounds containing a phenylbutylamine moiety, which consists of a phenyl group substituted at the fourth carbon by an butan-1-amine.
KingdomOrganic compounds
Super ClassBenzenoids
ClassBenzene and substituted derivatives
Sub ClassPhenylbutylamines
Direct ParentPhenylbutylamines
Alternative Parents
Substituents
  • Phenylbutylamine
  • O-dimethoxybenzene
  • Dimethoxybenzene
  • Phenylpropane
  • Phenethylamine
  • Benzyl-cyanide
  • Methoxybenzene
  • Phenol ether
  • Anisole
  • Aralkylamine
  • Alkyl aryl ether
  • Tertiary aliphatic amine
  • Tertiary amine
  • Nitrile
  • Carbonitrile
  • Ether
  • Hydrocarbon derivative
  • Organooxygen compound
  • Organonitrogen compound
  • Amine
  • Aromatic homomonocyclic compound
Molecular FrameworkAromatic homomonocyclic compounds
External DescriptorsNot Available
Pharmacology
IndicationFor the treatment of hypertension, angina, and cluster headache prophylaxis.
PharmacodynamicsVerapamil is an L-type calcium channel blocker that also has antiarrythmic activity. The R-enantiomer is more effective at reducing blood pressure compared to the S-enantiomer. However, the S-enantiomer is 20 times more potent than the R-enantiomer at prolonging the PR interval in treating arrhythmias.
Mechanism of actionVerapamil inhibits voltage-dependent calcium channels. Specifically, its effect on L-type calcium channels in the heart causes a reduction in ionotropy and chronotropy, thuis reducing heart rate and blood pressure. Verapamil's mechanism of effect in cluster headache is thought to be linked to its calcium-channel blocker effect, but which channel subtypes are involved is presently not known.
Related Articles
Absorption90%
Volume of distributionNot Available
Protein binding90%
Metabolism
SubstrateEnzymesProduct
Verapamil
O-Desmethylverapamil (D-702)Details
Verapamil
Verapamil metabolite D-617Details
Verapamil
NorverapamilDetails
Verapamil
O-Desmethylverapamil (D-703)Details
O-Desmethylverapamil (D-702)
Verapamil metabolite D-620Details
Verapamil metabolite D-617
Verapamil metabolite D-620Details
Verapamil metabolite D-617
Not Available
Verapamil metabolite PR-25Details
Norverapamil
Verapamil metabolite D-715 (PR-22)Details
Norverapamil
Verapamil metabolite D-620Details
Route of eliminationApproximately 70% of an administered dose is excreted as metabolites in the urine and 16% or more in the feces within 5 days. About 3% to 4% is excreted in the urine as unchanged drug.
Half life2.8-7.4 hours
ClearanceNot Available
ToxicityLD50=8 mg/kg (i.v. in mice)
Affected organisms
  • Humans and other mammals
Pathways
PathwayCategorySMPDB ID
Verapamil Action PathwayDrug actionSMP00375
SNP Mediated Effects
Interacting Gene/EnzymeSNP RS IDAllele nameDefining changeEffectReference(s)
Beta-1 adrenergic receptor
Gene symbol: ADRB1
UniProt: P08588
rs1801253 Not AvailableG > CBetter response to drug therapy22192668
SNP Mediated Adverse Drug ReactionsNot Available
ADMET
Predicted ADMET features
PropertyValueProbability
Human Intestinal Absorption+0.9371
Blood Brain Barrier+0.6323
Caco-2 permeable+0.738
P-glycoprotein substrateSubstrate0.7874
P-glycoprotein inhibitor IInhibitor0.9056
P-glycoprotein inhibitor IIInhibitor0.855
Renal organic cation transporterInhibitor0.6259
CYP450 2C9 substrateNon-substrate0.8029
CYP450 2D6 substrateNon-substrate0.8706
CYP450 3A4 substrateSubstrate0.7657
CYP450 1A2 substrateNon-inhibitor0.9553
CYP450 2C9 inhibitorNon-inhibitor0.9071
CYP450 2D6 inhibitorNon-inhibitor0.9231
CYP450 2C19 inhibitorNon-inhibitor0.9026
CYP450 3A4 inhibitorInhibitor0.796
CYP450 inhibitory promiscuityLow CYP Inhibitory Promiscuity0.9181
Ames testNon AMES toxic0.8393
CarcinogenicityNon-carcinogens0.6463
BiodegradationNot ready biodegradable1.0
Rat acute toxicity3.4137 LD50, mol/kg Not applicable
hERG inhibition (predictor I)Weak inhibitor0.7687
hERG inhibition (predictor II)Inhibitor0.8188
ADMET data is predicted using admetSAR, a free tool for evaluating chemical ADMET properties. (23092397 )
Pharmacoeconomics
Manufacturers
  • Mylan pharmaceuticals inc
  • Elan drug delivery inc
  • Gd searle llc
  • Fsc laboratories inc
  • Abraxis pharmaceutical products
  • Bedford laboratories div ben venue laboratories inc
  • Hospira inc
  • International medication system
  • Luitpold pharmaceuticals inc
  • Marsam pharmaceuticals llc
  • Smith and nephew solopak div smith and nephew
  • Solopak medical products inc
  • Ranbaxy laboratories inc
  • Glenmark generics ltd
  • Ivax pharmaceuticals inc sub teva pharmaceuticals usa
  • Par pharmaceutical inc
  • Pliva inc
  • Actavis elizabeth llc
  • Heritage pharmaceuticals inc
  • Mutual pharmaceutical co inc
  • Sandoz inc
  • Warner chilcott div warner lambert co
  • Watson laboratories inc
Packagers
Dosage forms
FormRouteStrength
Tabletoral80 mg
Tablet, film coatedoral120 mg/1
Tablet, film coatedoral80 mg/1
Tablet, film coated, extended releaseoral120 mg/1
Tablet, film coated, extended releaseoral180 mg/1
Tablet, film coated, extended releaseoral240 mg/1
Tablet, extended releaseoral180 mg/1
Tablet, extended releaseoral240 mg/1
Tabletoral120 mg
Tablet (extended-release)oral120 mg
Tablet (extended-release)oral180 mg
Tablet (extended-release)oral240 mg
Tablet (extended-release)oral
Tablet, film coated, extended releaseoral
Capsule, extended releaseoral120 mg/1
Capsule, extended releaseoral180 mg/1
Capsule, extended releaseoral240 mg/1
Injection, solutionintravenous2.5 mg/mL
Tabletoral120 mg/1
Tabletoral240 mg/1
Tabletoral40 mg/1
Tabletoral80 mg/1
Tablet, extended releaseoral120 mg/1
Tablet, extended releaseoral240 mg/301
Tablet, film coatedoral40 mg/1
Solutionintravenous2.5 mg
Liquidintravenous2.5 mg
Capsule (sustained-release)oral120 mg
Capsule (sustained-release)oral180 mg
Capsule (sustained-release)oral240 mg
Capsule, delayed release pelletsoral120 mg/1
Capsule, delayed release pelletsoral180 mg/1
Capsule, delayed release pelletsoral240 mg/1
Capsule, delayed release pelletsoral360 mg/1
Capsule, extended releaseoral100 mg/1
Capsule, extended releaseoral200 mg/1
Capsule, extended releaseoral300 mg/1
Prices
Unit descriptionCostUnit
Verelan 360 mg 24 Hour Capsule6.82USD capsule
Verelan 360 mg cap pellet6.73USD pellet
Verelan pm 300 mg cap pellet5.87USD pellet
Verelan 240 mg 24 Hour Capsule4.76USD capsule
Verelan 240 mg cap pellet4.58USD pellet
Verelan 180 mg 24 Hour Capsule4.22USD capsule
Verelan 180 mg cap pellet4.06USD pellet
Verelan pm 200 mg cap pellet4.04USD pellet
Verelan 120 mg cap pellet3.87USD pellet
Verapamil HCl CR 300 mg 24 Hour Capsule3.82USD capsule
Isoptin sr 240 mg tablet3.32USD tablet
Verapamil hcl powder3.24USD g
Calan SR 240 mg Controlled Release Tabs3.15USD tab
Isoptin SR 240 mg Controlled Release Tabs3.14USD tab
Verelan pm 100 mg cap pellet3.13USD pellet
Calan sr 240 mg caplet3.09USD caplet
Covera-HS 240 mg 24 Hour tablet3.09USD tablet
Covera-hs 240 mg tablet sa2.97USD tablet
Isoptin sr 180 mg tablet2.9USD tablet
Calan SR 180 mg Controlled Release Tabs2.8USD tab
Isoptin SR 180 mg Controlled Release Tabs2.74USD tab
Calan sr 180 mg caplet2.7USD caplet
Verapamil HCl CR 200 mg 24 Hour Capsule2.62USD capsule
Isoptin sr 120 mg tablet2.29USD tablet
Calan SR 120 mg Controlled Release Tabs2.27USD tab
Covera-HS 180 mg 24 Hour tablet2.2USD tablet
Isoptin SR 120 mg Controlled Release Tabs2.16USD tab
Calan sr 120 mg caplet2.13USD caplet
Covera-hs 180 mg tablet sa2.11USD tablet
Verapamil HCl CR 360 mg 24 Hour Capsule2.1USD capsule
Verapamil HCl CR 100 mg 24 Hour Capsule2.04USD capsule
Isoptin Sr 240 mg Sustained-Release Tablet2.03USD tablet
Calan sr 240 mg caplet sa1.77USD caplet
Verapamil HCl CR 240 mg 24 Hour Capsule1.69USD capsule
Verapamil HCl CR 240 mg Controlled Release Tabs1.6USD tab
Calan 120 mg tablet1.56USD tablet
Isoptin Sr 180 mg Sustained-Release Tablet1.52USD tablet
Verapamil HCl CR 180 mg 24 Hour Capsule1.5USD capsule
Calan sr 180 mg caplet sa1.46USD caplet
Verapamil HCl CR 120 mg 24 Hour Capsule1.43USD capsule
Verapamil HCl CR 180 mg Controlled Release Tabs1.41USD tab
Isoptin Sr 120 mg Sustained-Release Tablet1.34USD tablet
Calan 80 mg tablet1.25USD tablet
Verapamil 2.5 mg/ml vial1.18USD ml
Verapamil HCl CR 120 mg Controlled Release Tabs1.12USD tab
Apo-Verap Sr 240 mg Sustained-Release Tablet0.91USD tablet
Mylan-Verapamil Sr 240 mg Sustained-Release Tablet0.91USD tablet
Novo-Veramil Sr 240 mg Sustained-Release Tablet0.91USD tablet
Pms-Verapamil Sr 240 mg Sustained-Release Tablet0.91USD tablet
Calan 40 mg tablet0.76USD tablet
Apo-Verap Sr 120 mg Sustained-Release Tablet0.72USD tablet
Mylan-Verapamil Sr 120 mg Sustained-Release Tablet0.72USD tablet
Verapamil HCl 120 mg tablet0.71USD tablet
Apo-Verap Sr 180 mg Sustained-Release Tablet0.69USD tablet
Mylan-Verapamil Sr 180 mg Sustained-Release Tablet0.69USD tablet
Verapamil HCl 80 mg tablet0.56USD tablet
Apo-Verap 120 mg Tablet0.45USD tablet
Mylan-Verapamil 120 mg Tablet0.45USD tablet
Nu-Verap 120 mg Tablet0.45USD tablet
Verapamil 120 mg tablet0.39USD tablet
Verapamil 80 mg tablet0.31USD tablet
Verapamil HCl 40 mg tablet0.29USD tablet
Apo-Verap 80 mg Tablet0.29USD tablet
Mylan-Verapamil 80 mg Tablet0.29USD tablet
Nu-Verap 80 mg Tablet0.29USD tablet
Verapamil 40 mg tablet0.28USD tablet
DrugBank does not sell nor buy drugs. Pricing information is supplied for informational purposes only.
Patents
Patent NumberPediatric ExtensionApprovedExpires (estimated)
US5785994 No1992-10-222009-10-22Us
US6096339 No1997-04-042017-04-04Us
Properties
StateLiquid
Experimental Properties
PropertyValueSource
melting point< 25 °CPhysProp
boiling point243-246 °C at 1.00E-02 mm HgPhysProp
water solubility4.47 mg/LNot Available
logP3.79HANSCH,C ET AL. (1995)
Caco2 permeability-4.58ADME Research, USCD
pKa8.92SANGSTER (1994)
Predicted Properties
PropertyValueSource
Water Solubility0.00394 mg/mLALOGPS
logP5.23ALOGPS
logP5.04ChemAxon
logS-5.1ALOGPS
pKa (Strongest Basic)9.68ChemAxon
Physiological Charge1ChemAxon
Hydrogen Acceptor Count6ChemAxon
Hydrogen Donor Count0ChemAxon
Polar Surface Area63.95 Å2ChemAxon
Rotatable Bond Count13ChemAxon
Refractivity132.65 m3·mol-1ChemAxon
Polarizability51.7 Å3ChemAxon
Number of Rings2ChemAxon
Bioavailability0ChemAxon
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, Positive (Annotated)splash10-0u08z00000-6a46ea2d5eed6d8b01ebView in MoNA
LC-MS/MSLC-MS/MS Spectrum - Quattro_QQQ 25V, Positive (Annotated)splash10-g70zx00000-80d342090a0be3344e82View in MoNA
LC-MS/MSLC-MS/MS Spectrum - Quattro_QQQ 40V, Positive (Annotated)splash10-0zmgi00000-2def387c7c93ab211423View in MoNA
LC-MS/MSLC-MS/MS Spectrum - LC-ESI-QQ (API3000, Applied Biosystems) 10V, Positivesplash10-0000z00000-4cde9a4b3a4f83d16afcView in MoNA
LC-MS/MSLC-MS/MS Spectrum - LC-ESI-QQ (API3000, Applied Biosystems) 20V, Positivesplash10-0000z00000-980b47834e505d54a0e6View in MoNA
LC-MS/MSLC-MS/MS Spectrum - LC-ESI-QQ (API3000, Applied Biosystems) 30V, Positivesplash10-0z18x00000-ae024239c46b33917426View in MoNA
LC-MS/MSLC-MS/MS Spectrum - LC-ESI-QQ (API3000, Applied Biosystems) 40V, Positivesplash10-0z24000000-81d1159b3102cff76218View in MoNA
LC-MS/MSLC-MS/MS Spectrum - LC-ESI-QQ (API3000, Applied Biosystems) 50V, Positivesplash10-1z20000000-d9c344fee7b45b4030e6View in MoNA
LC-MS/MSLC-MS/MS Spectrum - LC-ESI-IT (LC/MSD Trap XCT, Agilent Technologies) , Positivesplash10-0z5g000000-070bdb975910e9aae99cView in MoNA
LC-MS/MSLC-MS/MS Spectrum - LC-ESI-IT (LC/MSD Trap XCT, Agilent Technologies) , Positivesplash10-0cz0000000-f41d80462c5d06c4f001View in MoNA
LC-MS/MSLC-MS/MS Spectrum - LC-ESI-IT (LC/MSD Trap XCT, Agilent Technologies) , Positivesplash10-8zv0000000-9a2ab0bcab33f7eaac6bView in MoNA
LC-MS/MSLC-MS/MS Spectrum - LC-ESI-IT (LC/MSD Trap XCT, Agilent Technologies) , Positivesplash10-0z01000000-252a9989a8511cb2db80View in MoNA
LC-MS/MSLC-MS/MS Spectrum - LC-ESI-IT (LC/MSD Trap XCT, Agilent Technologies) , Positivesplash10-0z00000000-4fd6ca2c6c19c3bbf8f0View in MoNA
MSMass Spectrum (Electron Ionization)splash10-ek5z000000-b5e0b9e0caac5cb57222View in MoNA
1D NMR1H NMR SpectrumNot Available
2D NMR[1H,13C] 2D NMR SpectrumNot Available
References
Synthesis Reference

Philippe Baudier, Arthur De Boeck, Jacques Fossion, “Novel galenic forms of verapamil, their preparation and medicines containing said novel galenic forms.” U.S. Patent US4859469, issued April, 1987.

US4859469
General References
  1. Bellamy WT: P-glycoproteins and multidrug resistance. Annu Rev Pharmacol Toxicol. 1996;36:161-83. [PubMed:8725386 ]
External Links
ATC CodesC08DA01C08DA51C09BB10
AHFS Codes
  • 24:28.92
PDB EntriesNot Available
FDA labelDownload (1.9 MB)
MSDSDownload (73.5 KB)
Interactions
Drug Interactions
Drug
AbirateroneThe serum concentration of Verapamil can be increased when it is combined with Abiraterone.
AcetaminophenThe metabolism of Verapamil can be increased when combined with Acetaminophen.
Acetylsalicylic acidVerapamil may increase the anticoagulant activities of Acetylsalicylic acid.
AfatinibThe serum concentration of Afatinib can be increased when it is combined with Verapamil.
AldesleukinThe risk or severity of adverse effects can be increased when Aldesleukin is combined with Verapamil.
AlfuzosinAlfuzosin may increase the hypotensive activities of Verapamil.
AliskirenThe serum concentration of Aliskiren can be increased when it is combined with Verapamil.
AmifostineVerapamil may increase the hypotensive activities of Amifostine.
AmiodaroneThe serum concentration of Amiodarone can be increased when it is combined with Verapamil.
AmlodipineAmlodipine may increase the hypotensive activities of Verapamil.
AmobarbitalThe metabolism of Verapamil can be increased when combined with Amobarbital.
ApixabanThe serum concentration of Apixaban can be increased when it is combined with Verapamil.
AprepitantThe serum concentration of Verapamil can be increased when it is combined with Aprepitant.
AripiprazoleThe serum concentration of Aripiprazole can be increased when it is combined with Verapamil.
AtorvastatinThe serum concentration of Verapamil can be increased when it is combined with Atorvastatin.
AtosibanThe risk or severity of adverse effects can be increased when Verapamil is combined with Atosiban.
Atracurium besylateVerapamil may increase the neuromuscular blocking activities of Atracurium besylate.
AvanafilThe serum concentration of Avanafil can be increased when it is combined with Verapamil.
AzithromycinThe serum concentration of Verapamil can be increased when it is combined with Azithromycin.
BatimastatThe metabolism of Verapamil can be decreased when combined with Batimastat.
BendroflumethiazideThe serum concentration of Bendroflumethiazide can be increased when it is combined with Verapamil.
BexaroteneThe serum concentration of Verapamil can be decreased when it is combined with Bexarotene.
BosentanThe serum concentration of Verapamil can be decreased when it is combined with Bosentan.
BosutinibThe serum concentration of Bosutinib can be increased when it is combined with Verapamil.
Brentuximab vedotinThe serum concentration of Brentuximab vedotin can be increased when it is combined with Verapamil.
BretyliumBretylium may increase the bradycardic activities of Verapamil.
BrexpiprazoleThe serum concentration of Brexpiprazole can be increased when it is combined with Verapamil.
BrimonidineBrimonidine may increase the antihypertensive activities of Verapamil.
BudesonideThe serum concentration of Budesonide can be increased when it is combined with Verapamil.
BuspironeThe metabolism of Buspirone can be decreased when combined with Verapamil.
ButabarbitalThe metabolism of Verapamil can be increased when combined with Butabarbital.
ButalbitalThe metabolism of Verapamil can be increased when combined with Butalbital.
ButethalThe metabolism of Verapamil can be increased when combined with Butethal.
CaffeineThe metabolism of Verapamil can be increased when combined with Caffeine.
Calcium AcetateThe therapeutic efficacy of Verapamil can be decreased when used in combination with Calcium Acetate.
Calcium carbonateThe therapeutic efficacy of Verapamil can be decreased when used in combination with Calcium carbonate.
Calcium ChlorideThe therapeutic efficacy of Verapamil can be decreased when used in combination with Calcium Chloride.
Calcium citrateThe therapeutic efficacy of Verapamil can be decreased when used in combination with Calcium citrate.
Calcium gluconateThe therapeutic efficacy of Verapamil can be decreased when used in combination with Calcium gluconate.
CarbamazepineThe serum concentration of Carbamazepine can be increased when it is combined with Verapamil.
CarfilzomibThe serum concentration of Carfilzomib can be increased when it is combined with Verapamil.
CarvedilolThe serum concentration of Carvedilol can be increased when it is combined with Verapamil.
CeritinibVerapamil may increase the bradycardic activities of Ceritinib.
CetirizineThe serum concentration of Cetirizine can be increased when it is combined with Verapamil.
CilostazolThe serum concentration of Cilostazol can be increased when it is combined with Verapamil.
CimetidineThe serum concentration of Verapamil can be increased when it is combined with Cimetidine.
CiprofloxacinThe serum concentration of Ciprofloxacin can be increased when it is combined with Verapamil.
Cisatracurium besylateVerapamil may increase the neuromuscular blocking activities of Cisatracurium besylate.
ClarithromycinThe serum concentration of Verapamil can be increased when it is combined with Clarithromycin.
ClonidineClonidine may increase the atrioventricular blocking (AV block) activities of Verapamil.
ClopidogrelThe therapeutic efficacy of Clopidogrel can be decreased when used in combination with Verapamil.
CobicistatThe serum concentration of Verapamil can be increased when it is combined with Cobicistat.
ColchicineThe serum concentration of Colchicine can be increased when it is combined with Verapamil.
ConivaptanThe serum concentration of Verapamil can be increased when it is combined with Conivaptan.
CrizotinibThe serum concentration of Crizotinib can be increased when it is combined with Verapamil.
CyclosporineThe serum concentration of Cyclosporine can be increased when it is combined with Verapamil.
Dabigatran etexilateThe serum concentration of the active metabolites of Dabigatran etexilate can be increased when Dabigatran etexilate is used in combination with Verapamil.
DabrafenibThe serum concentration of Verapamil can be decreased when it is combined with Dabrafenib.
DaclatasvirThe serum concentration of Verapamil can be increased when it is combined with Daclatasvir.
DantroleneDantrolene may increase the hyperkalemic activities of Verapamil.
DapoxetineThe serum concentration of Dapoxetine can be increased when it is combined with Verapamil.
DarunavirThe serum concentration of Verapamil can be increased when it is combined with Darunavir.
DasatinibThe serum concentration of Verapamil can be increased when it is combined with Dasatinib.
DaunorubicinThe serum concentration of Daunorubicin can be increased when it is combined with Verapamil.
DeferasiroxThe serum concentration of Verapamil can be decreased when it is combined with Deferasirox.
DesloratadineThe serum concentration of Desloratadine can be increased when it is combined with Verapamil.
DexamethasoneThe serum concentration of Dexamethasone can be increased when it is combined with Verapamil.
DiazoxideDiazoxide may increase the hypotensive activities of Verapamil.
DigoxinVerapamil may increase the atrioventricular blocking (AV block) activities of Digoxin.
DiltiazemThe serum concentration of Diltiazem can be increased when it is combined with Verapamil.
DipyridamoleThe serum concentration of Verapamil can be increased when it is combined with Dipyridamole.
DisopyramideThe risk or severity of adverse effects can be increased when Verapamil is combined with Disopyramide.
DocetaxelThe serum concentration of Docetaxel can be increased when it is combined with Verapamil.
DofetilideThe serum concentration of Dofetilide can be increased when it is combined with Verapamil.
DomperidoneThe serum concentration of Domperidone can be increased when it is combined with Verapamil.
DoxazosinDoxazosin may increase the hypotensive activities of Verapamil.
DoxorubicinThe serum concentration of Doxorubicin can be increased when it is combined with Verapamil.
DronabinolThe serum concentration of Dronabinol can be increased when it is combined with Verapamil.
DronedaroneVerapamil may increase the atrioventricular blocking (AV block) activities of Dronedarone.
DrospirenoneThe serum concentration of Drospirenone can be increased when it is combined with Verapamil.
DuloxetineVerapamil may increase the orthostatic hypotensive activities of Duloxetine.
EdoxabanThe serum concentration of Edoxaban can be increased when it is combined with Verapamil.
EfavirenzThe serum concentration of Verapamil can be decreased when it is combined with Efavirenz.
EletriptanThe serum concentration of Eletriptan can be increased when it is combined with Verapamil.
EliglustatThe serum concentration of Eliglustat can be increased when it is combined with Verapamil.
EplerenoneThe serum concentration of Eplerenone can be increased when it is combined with Verapamil.
ErythromycinThe serum concentration of Verapamil can be increased when it is combined with Erythromycin.
EsmololEsmolol may increase the bradycardic activities of Verapamil.
EstradiolThe serum concentration of Estradiol can be increased when it is combined with Verapamil.
EthanolThe serum concentration of Ethanol can be increased when it is combined with Verapamil.
EtoposideThe serum concentration of Etoposide can be increased when it is combined with Verapamil.
EverolimusThe serum concentration of Everolimus can be increased when it is combined with Verapamil.
FentanylThe serum concentration of Fentanyl can be increased when it is combined with Verapamil.
FexofenadineThe bioavailability of Fexofenadine can be increased when combined with Verapamil.
FingolimodVerapamil may increase the bradycardic activities of Fingolimod.
FlecainideThe risk or severity of adverse effects can be increased when Verapamil is combined with Flecainide.
FlibanserinThe serum concentration of Flibanserin can be increased when it is combined with Verapamil.
FluconazoleThe serum concentration of Verapamil can be increased when it is combined with Fluconazole.
FlunisolideThe metabolism of Flunisolide can be decreased when combined with Verapamil.
FosamprenavirThe serum concentration of Fosamprenavir can be increased when it is combined with Verapamil.
FosaprepitantThe serum concentration of Verapamil can be increased when it is combined with Fosaprepitant.
FosphenytoinThe serum concentration of Fosphenytoin can be increased when it is combined with Verapamil.
Fusidic AcidThe serum concentration of Verapamil can be increased when it is combined with Fusidic Acid.
HalofantrineThe serum concentration of Halofantrine can be increased when it is combined with Verapamil.
HeptabarbitalThe metabolism of Verapamil can be increased when combined with Heptabarbital.
HexobarbitalThe metabolism of Verapamil can be increased when combined with Hexobarbital.
HydrocodoneThe serum concentration of Hydrocodone can be increased when it is combined with Verapamil.
HydrocortisoneThe serum concentration of Hydrocortisone can be increased when it is combined with Verapamil.
IbrutinibThe serum concentration of Ibrutinib can be increased when it is combined with Verapamil.
IdarubicinThe serum concentration of Idarubicin can be increased when it is combined with Verapamil.
IdelalisibThe serum concentration of Verapamil can be increased when it is combined with Idelalisib.
IfosfamideThe serum concentration of the active metabolites of Ifosfamide can be reduced when Ifosfamide is used in combination with Verapamil resulting in a loss in efficacy.
ImatinibThe serum concentration of Imatinib can be increased when it is combined with Verapamil.
IndinavirThe serum concentration of Indinavir can be increased when it is combined with Verapamil.
IrinotecanThe serum concentration of Irinotecan can be increased when it is combined with Verapamil.
IsoflurophateThe metabolism of Verapamil can be decreased when combined with Isoflurophate.
ItraconazoleThe serum concentration of Verapamil can be increased when it is combined with Itraconazole.
IvabradineThe serum concentration of Ivabradine can be increased when it is combined with Verapamil.
IvacaftorThe serum concentration of Ivacaftor can be increased when it is combined with Verapamil.
IvermectinThe serum concentration of Ivermectin can be increased when it is combined with Verapamil.
KetoconazoleThe serum concentration of Verapamil can be increased when it is combined with Ketoconazole.
LacosamideVerapamil may increase the atrioventricular blocking (AV block) activities of Lacosamide.
LapatinibThe serum concentration of Lapatinib can be increased when it is combined with Verapamil.
LedipasvirThe serum concentration of Ledipasvir can be increased when it is combined with Verapamil.
LevodopaVerapamil may increase the orthostatic hypotensive activities of Levodopa.
LithiumVerapamil may increase the neurotoxic activities of Lithium.
LomitapideThe serum concentration of Lomitapide can be increased when it is combined with Verapamil.
LoperamideThe serum concentration of Loperamide can be increased when it is combined with Verapamil.
LopinavirThe serum concentration of Lopinavir can be increased when it is combined with Verapamil.
LoratadineThe serum concentration of Loratadine can be increased when it is combined with Verapamil.
LovastatinThe serum concentration of Lovastatin can be increased when it is combined with Verapamil.
LuliconazoleThe serum concentration of Verapamil can be increased when it is combined with Luliconazole.
LurasidoneThe serum concentration of Lurasidone can be increased when it is combined with Verapamil.
Magnesium chlorideThe risk or severity of adverse effects can be increased when Verapamil is combined with Magnesium chloride.
Magnesium citrateThe risk or severity of adverse effects can be increased when Verapamil is combined with Magnesium citrate.
Magnesium hydroxideThe risk or severity of adverse effects can be increased when Verapamil is combined with Magnesium hydroxide.
Magnesium oxideThe risk or severity of adverse effects can be increased when Verapamil is combined with Magnesium oxide.
Magnesium salicylateThe risk or severity of adverse effects can be increased when Verapamil is combined with Magnesium salicylate.
Magnesium SulfateThe risk or severity of adverse effects can be increased when Verapamil is combined with Magnesium Sulfate.
MefloquineThe serum concentration of Verapamil can be increased when it is combined with Mefloquine.
MetforminThe therapeutic efficacy of Metformin can be decreased when used in combination with Verapamil.
MethohexitalThe metabolism of Verapamil can be increased when combined with Methohexital.
MethotrexateThe serum concentration of Methotrexate can be increased when it is combined with Verapamil.
MethylphenidateMethylphenidate may decrease the antihypertensive activities of Verapamil.
MidodrineVerapamil may increase the bradycardic activities of Midodrine.
MifepristoneThe serum concentration of Verapamil can be increased when it is combined with Mifepristone.
MirabegronThe serum concentration of Verapamil can be increased when it is combined with Mirabegron.
MitomycinThe serum concentration of Mitomycin can be increased when it is combined with Verapamil.
MitotaneThe serum concentration of Verapamil can be decreased when it is combined with Mitotane.
MolsidomineMolsidomine may increase the hypotensive activities of Verapamil.
MorphineThe serum concentration of Morphine can be increased when it is combined with Verapamil.
MoxonidineMoxonidine may increase the hypotensive activities of Verapamil.
NadololVerapamil may increase the hypotensive activities of Nadolol.
NafcillinThe metabolism of Verapamil can be increased when combined with Nafcillin.
NaloxegolThe serum concentration of Naloxegol can be increased when it is combined with Verapamil.
NelfinavirThe serum concentration of Nelfinavir can be increased when it is combined with Verapamil.
NetupitantThe serum concentration of Verapamil can be increased when it is combined with Netupitant.
NicardipineThe serum concentration of Nicardipine can be increased when it is combined with Verapamil.
NicorandilNicorandil may increase the hypotensive activities of Verapamil.
NilotinibThe serum concentration of Verapamil can be increased when it is combined with Nilotinib.
NimodipineThe serum concentration of Nimodipine can be increased when it is combined with Verapamil.
NintedanibThe serum concentration of Nintedanib can be increased when it is combined with Verapamil.
NitroprussideVerapamil may increase the hypotensive activities of Nitroprusside.
NorgestimateThe serum concentration of Norgestimate can be increased when it is combined with Verapamil.
ObinutuzumabVerapamil may increase the hypotensive activities of Obinutuzumab.
OctreotideOctreotide may increase the bradycardic activities of Verapamil.
OlaparibThe serum concentration of Olaparib can be increased when it is combined with Verapamil.
OndansetronThe serum concentration of Ondansetron can be increased when it is combined with Verapamil.
OxycodoneThe risk or severity of adverse effects can be increased when Verapamil is combined with Oxycodone.
PaclitaxelThe serum concentration of Paclitaxel can be increased when it is combined with Verapamil.
PalbociclibThe serum concentration of Verapamil can be increased when it is combined with Palbociclib.
PaliperidoneThe serum concentration of Paliperidone can be increased when it is combined with Verapamil.
PancuroniumVerapamil may increase the neuromuscular blocking activities of Pancuronium.
PazopanibThe serum concentration of Pazopanib can be increased when it is combined with Verapamil.
PentobarbitalThe metabolism of Verapamil can be increased when combined with Pentobarbital.
PentoxifyllinePentoxifylline may increase the hypotensive activities of Verapamil.
PhenelzinePhenelzine may increase the hypotensive activities of Verapamil.
PhenobarbitalThe metabolism of Verapamil can be increased when combined with Phenobarbital.
PhenoxybenzaminePhenoxybenzamine may increase the hypotensive activities of Verapamil.
PhentolaminePhentolamine may increase the hypotensive activities of Verapamil.
PhenytoinThe serum concentration of Phenytoin can be increased when it is combined with Verapamil.
PimecrolimusThe metabolism of Pimecrolimus can be decreased when combined with Verapamil.
PimozideThe serum concentration of Pimozide can be increased when it is combined with Verapamil.
PosaconazoleThe risk or severity of adverse effects can be increased when Posaconazole is combined with Verapamil.
PrazosinPrazosin may increase the hypotensive activities of Verapamil.
PrimidoneThe metabolism of Verapamil can be increased when combined with Primidone.
ProgesteroneThe serum concentration of Verapamil can be increased when it is combined with Progesterone.
PropafenoneThe serum concentration of Propafenone can be increased when it is combined with Verapamil.
PropranololThe serum concentration of Verapamil can be increased when it is combined with Propranolol.
PrucaloprideThe serum concentration of Prucalopride can be increased when it is combined with Verapamil.
QuinidineQuinidine may increase the hypotensive activities of Verapamil.
QuinineThe serum concentration of Quinine can be increased when it is combined with Verapamil.
RanitidineThe serum concentration of Ranitidine can be increased when it is combined with Verapamil.
RanolazineThe serum concentration of Ranolazine can be increased when it is combined with Verapamil.
RegorafenibRegorafenib may increase the bradycardic activities of Verapamil.
ReserpineThe serum concentration of Verapamil can be increased when it is combined with Reserpine.
RifabutinThe serum concentration of Verapamil can be decreased when it is combined with Rifabutin.
RifampicinThe serum concentration of Verapamil can be decreased when it is combined with Rifampicin.
RifapentineThe serum concentration of Verapamil can be decreased when it is combined with Rifapentine.
RifaximinThe serum concentration of Rifaximin can be increased when it is combined with Verapamil.
RiociguatThe serum concentration of Riociguat can be increased when it is combined with Verapamil.
RisperidoneThe serum concentration of Risperidone can be increased when it is combined with Verapamil.
RitonavirThe serum concentration of Ritonavir can be increased when it is combined with Verapamil.
RituximabVerapamil may increase the hypotensive activities of Rituximab.
RivaroxabanThe serum concentration of Rivaroxaban can be increased when it is combined with Verapamil.
RocuroniumVerapamil may increase the neuromuscular blocking activities of Rocuronium.
RolapitantThe serum concentration of Verapamil can be increased when it is combined with Rolapitant.
RuxolitinibRuxolitinib may increase the bradycardic activities of Verapamil.
SalmeterolThe serum concentration of Salmeterol can be increased when it is combined with Verapamil.
SaquinavirThe serum concentration of Verapamil can be increased when it is combined with Saquinavir.
SaxagliptinThe serum concentration of Saxagliptin can be increased when it is combined with Verapamil.
SecobarbitalThe metabolism of Verapamil can be increased when combined with Secobarbital.
SilodosinThe serum concentration of Silodosin can be increased when it is combined with Verapamil.
SiltuximabThe serum concentration of Verapamil can be decreased when it is combined with Siltuximab.
SimeprevirThe serum concentration of Simeprevir can be increased when it is combined with Verapamil.
SimvastatinThe serum concentration of Simvastatin can be increased when it is combined with Verapamil.
SirolimusThe serum concentration of Sirolimus can be increased when it is combined with Verapamil.
SitagliptinThe serum concentration of Sitagliptin can be increased when it is combined with Verapamil.
SofosbuvirThe serum concentration of Sofosbuvir can be increased when it is combined with Verapamil.
SonidegibThe serum concentration of Sonidegib can be increased when it is combined with Verapamil.
St. John's WortThe serum concentration of Verapamil can be decreased when it is combined with St. John&#39;s Wort.
StiripentolThe serum concentration of Verapamil can be increased when it is combined with Stiripentol.
SufentanilSufentanil may increase the bradycardic activities of Verapamil.
SulfisoxazoleThe serum concentration of Verapamil can be increased when it is combined with Sulfisoxazole.
SunitinibThe serum concentration of Verapamil can be increased when it is combined with Sunitinib.
SuvorexantThe serum concentration of Suvorexant can be increased when it is combined with Verapamil.
TacrolimusThe metabolism of Tacrolimus can be decreased when combined with Verapamil.
TadalafilTadalafil may increase the antihypertensive activities of Verapamil.
TamoxifenThe serum concentration of Verapamil can be increased when it is combined with Tamoxifen.
TamsulosinTamsulosin may increase the hypotensive activities of Verapamil.
TelaprevirThe serum concentration of Telaprevir can be increased when it is combined with Verapamil.
TelithromycinTelithromycin may increase the bradycardic activities of Verapamil.
TemsirolimusThe serum concentration of Temsirolimus can be increased when it is combined with Verapamil.
TeniposideThe serum concentration of Teniposide can be increased when it is combined with Verapamil.
TerazosinTerazosin may increase the hypotensive activities of Verapamil.
TesmilifeneThe serum concentration of Verapamil can be decreased when it is combined with Tesmilifene.
TipranavirThe serum concentration of Verapamil can be decreased when it is combined with Tipranavir.
TizanidineThe serum concentration of Tizanidine can be increased when it is combined with Verapamil.
TocilizumabThe serum concentration of Verapamil can be decreased when it is combined with Tocilizumab.
TofacitinibTofacitinib may increase the bradycardic activities of Verapamil.
TolvaptanThe serum concentration of Tolvaptan can be increased when it is combined with Verapamil.
TopotecanThe serum concentration of Topotecan can be increased when it is combined with Verapamil.
TrabectedinThe serum concentration of Trabectedin can be increased when it is combined with Verapamil.
TranylcypromineTranylcypromine may increase the hypotensive activities of Verapamil.
TreprostinilTreprostinil may increase the hypotensive activities of Verapamil.
UlipristalThe serum concentration of Ulipristal can be increased when it is combined with Verapamil.
ValsartanThe risk or severity of adverse effects can be increased when Valsartan is combined with Verapamil.
VandetanibThe serum concentration of Verapamil can be increased when it is combined with Vandetanib.
VardenafilVardenafil may increase the antihypertensive activities of Verapamil.
VecuroniumVerapamil may increase the neuromuscular blocking activities of Vecuronium.
VemurafenibThe serum concentration of Vemurafenib can be increased when it is combined with Verapamil.
VilazodoneThe serum concentration of Vilazodone can be increased when it is combined with Verapamil.
VinblastineThe serum concentration of Vinblastine can be increased when it is combined with Verapamil.
VincristineThe serum concentration of Vincristine can be increased when it is combined with Verapamil.
VindesineThe serum concentration of Vindesine can be increased when it is combined with Verapamil.
VoriconazoleThe risk or severity of adverse effects can be increased when Voriconazole is combined with Verapamil.
YohimbineYohimbine may decrease the antihypertensive activities of Verapamil.
ZopicloneThe serum concentration of Zopiclone can be increased when it is combined with Verapamil.
ZuclopenthixolThe serum concentration of Zuclopenthixol can be increased when it is combined with Verapamil.
Food Interactions
  • Avoid alcohol.
  • Avoid excessive quantities of coffee or tea (Caffeine).
  • Avoid natural licorice.
  • Avoid taking with grapefruit juice.
  • Take with food.

Targets

Kind
Protein
Organism
Human
Pharmacological action
yes
Actions
inhibitor
General Function:
Voltage-gated calcium channel activity
Specific Function:
Voltage-sensitive calcium channels (VSCC) mediate the entry of calcium ions into excitable cells and are also involved in a variety of calcium-dependent processes, including muscle contraction, hormone or neurotransmitter release, gene expression, cell motility, cell division and cell death. The isoform alpha-1C gives rise to L-type calcium currents. Long-lasting (L-type) calcium channels belon...
Gene Name:
CACNA1C
Uniprot ID:
Q13936
Molecular Weight:
248974.1 Da
References
  1. Dilmac N, Hilliard N, Hockerman GH: Molecular determinants of frequency dependence and Ca2+ potentiation of verapamil block in the pore region of Cav1.2. Mol Pharmacol. 2004 Nov;66(5):1236-47. Epub 2004 Jul 30. [PubMed:15286207 ]
  2. Morel N, Buryi V, Feron O, Gomez JP, Christen MO, Godfraind T: The action of calcium channel blockers on recombinant L-type calcium channel alpha1-subunits. Br J Pharmacol. 1998 Nov;125(5):1005-12. [PubMed:9846638 ]
  3. Patel MK, Clunn GF, Lymn JS, Austin O, Hughes AD: Effect of serum withdrawal on the contribution of L-type calcium channels (CaV1.2) to intracellular Ca2+ responses and chemotaxis in cultured human vascular smooth muscle cells. Br J Pharmacol. 2005 Jul;145(6):811-7. [PubMed:15880143 ]
  4. Tfelt-Hansen P, Tfelt-Hansen J: Verapamil for cluster headache. Clinical pharmacology and possible mode of action. Headache. 2009 Jan;49(1):117-25. doi: 10.1111/j.1526-4610.2008.01298.x. [PubMed:19125880 ]
Kind
Protein
Organism
Human
Pharmacological action
yes
Actions
inhibitor
General Function:
Voltage-gated calcium channel activity involved sa node cell action potential
Specific Function:
Voltage-sensitive calcium channels (VSCC) mediate the entry of calcium ions into excitable cells and are also involved in a variety of calcium-dependent processes, including muscle contraction, hormone or neurotransmitter release, gene expression, cell motility, cell division and cell death. The isoform alpha-1D gives rise to L-type calcium currents. Long-lasting (L-type) calcium channels belon...
Gene Name:
CACNA1D
Uniprot ID:
Q01668
Molecular Weight:
245138.75 Da
References
  1. Tfelt-Hansen P, Tfelt-Hansen J: Verapamil for cluster headache. Clinical pharmacology and possible mode of action. Headache. 2009 Jan;49(1):117-25. doi: 10.1111/j.1526-4610.2008.01298.x. [PubMed:19125880 ]
Kind
Protein
Organism
Human
Pharmacological action
yes
Actions
inhibitor
General Function:
Voltage-gated calcium channel activity
Specific Function:
Voltage-sensitive calcium channels (VSCC) mediate the entry of calcium ions into excitable cells and are also involved in a variety of calcium-dependent processes, including muscle contraction, hormone or neurotransmitter release, gene expression, cell motility, cell division and cell death. The isoform alpha-1F gives rise to L-type calcium currents. Long-lasting (L-type) calcium channels belon...
Gene Name:
CACNA1F
Uniprot ID:
O60840
Molecular Weight:
220675.9 Da
References
  1. Tfelt-Hansen P, Tfelt-Hansen J: Verapamil for cluster headache. Clinical pharmacology and possible mode of action. Headache. 2009 Jan;49(1):117-25. doi: 10.1111/j.1526-4610.2008.01298.x. [PubMed:19125880 ]
Kind
Protein
Organism
Human
Pharmacological action
yes
Actions
inhibitor
General Function:
Voltage-gated calcium channel activity
Specific Function:
Voltage-sensitive calcium channels (VSCC) mediate the entry of calcium ions into excitable cells and are also involved in a variety of calcium-dependent processes, including muscle contraction, hormone or neurotransmitter release, gene expression, cell motility, cell division and cell death. The isoform alpha-1S gives rise to L-type calcium currents. Long-lasting (L-type) calcium channels belon...
Gene Name:
CACNA1S
Uniprot ID:
Q13698
Molecular Weight:
212348.1 Da
References
  1. Tfelt-Hansen P, Tfelt-Hansen J: Verapamil for cluster headache. Clinical pharmacology and possible mode of action. Headache. 2009 Jan;49(1):117-25. doi: 10.1111/j.1526-4610.2008.01298.x. [PubMed:19125880 ]
Kind
Protein
Organism
Human
Pharmacological action
yes
Actions
inhibitor
General Function:
Voltage-gated calcium channel activity
Specific Function:
The beta subunit of voltage-dependent calcium channels contributes to the function of the calcium channel by increasing peak calcium current, shifting the voltage dependencies of activation and inactivation, modulating G protein inhibition and controlling the alpha-1 subunit membrane targeting.
Gene Name:
CACNB1
Uniprot ID:
Q02641
Molecular Weight:
65712.995 Da
References
  1. Tfelt-Hansen P, Tfelt-Hansen J: Verapamil for cluster headache. Clinical pharmacology and possible mode of action. Headache. 2009 Jan;49(1):117-25. doi: 10.1111/j.1526-4610.2008.01298.x. [PubMed:19125880 ]
Kind
Protein
Organism
Human
Pharmacological action
yes
Actions
inhibitor
General Function:
Voltage-gated calcium channel activity
Specific Function:
The beta subunit of voltage-dependent calcium channels contributes to the function of the calcium channel by increasing peak calcium current, shifting the voltage dependencies of activation and inactivation, modulating G protein inhibition and controlling the alpha-1 subunit membrane targeting.
Gene Name:
CACNB2
Uniprot ID:
Q08289
Molecular Weight:
73579.925 Da
References
  1. Tfelt-Hansen P, Tfelt-Hansen J: Verapamil for cluster headache. Clinical pharmacology and possible mode of action. Headache. 2009 Jan;49(1):117-25. doi: 10.1111/j.1526-4610.2008.01298.x. [PubMed:19125880 ]
Kind
Protein
Organism
Human
Pharmacological action
yes
Actions
inhibitor
General Function:
Voltage-gated calcium channel activity
Specific Function:
The beta subunit of voltage-dependent calcium channels contributes to the function of the calcium channel by increasing peak calcium current, shifting the voltage dependencies of activation and inactivation, modulating G protein inhibition and controlling the alpha-1 subunit membrane targeting.
Gene Name:
CACNB3
Uniprot ID:
P54284
Molecular Weight:
54531.425 Da
References
  1. Tfelt-Hansen P, Tfelt-Hansen J: Verapamil for cluster headache. Clinical pharmacology and possible mode of action. Headache. 2009 Jan;49(1):117-25. doi: 10.1111/j.1526-4610.2008.01298.x. [PubMed:19125880 ]
Kind
Protein
Organism
Human
Pharmacological action
yes
Actions
inhibitor
General Function:
Voltage-gated calcium channel activity
Specific Function:
The beta subunit of voltage-dependent calcium channels contributes to the function of the calcium channel by increasing peak calcium current, shifting the voltage dependencies of activation and inactivation, modulating G protein inhibition and controlling the alpha-1 subunit membrane targeting.
Gene Name:
CACNB4
Uniprot ID:
O00305
Molecular Weight:
58168.625 Da
References
  1. Tfelt-Hansen P, Tfelt-Hansen J: Verapamil for cluster headache. Clinical pharmacology and possible mode of action. Headache. 2009 Jan;49(1):117-25. doi: 10.1111/j.1526-4610.2008.01298.x. [PubMed:19125880 ]
Kind
Protein
Organism
Human
Pharmacological action
unknown
Actions
inhibitor
General Function:
Voltage-gated calcium channel activity
Specific Function:
Voltage-sensitive calcium channels (VSCC) mediate the entry of calcium ions into excitable cells and are also involved in a variety of calcium-dependent processes, including muscle contraction, hormone or neurotransmitter release, gene expression, cell motility, cell division and cell death. Isoform alpha-1I gives rise to T-type calcium currents. T-type calcium channels belong to the "low-volta...
Gene Name:
CACNA1I
Uniprot ID:
Q9P0X4
Molecular Weight:
245100.8 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 ]
Kind
Protein
Organism
Human
Pharmacological action
unknown
Actions
inhibitor
General Function:
Scaffold protein binding
Specific Function:
Voltage-sensitive calcium channels (VSCC) mediate the entry of calcium ions into excitable cells and are also involved in a variety of calcium-dependent processes, including muscle contraction, hormone or neurotransmitter release, gene expression, cell motility, cell division and cell death. The isoform alpha-1G gives rise to T-type calcium currents. T-type calcium channels belong to the "low-v...
Gene Name:
CACNA1G
Uniprot ID:
O43497
Molecular Weight:
262468.62 Da
References
  1. Tfelt-Hansen P, Tfelt-Hansen J: Verapamil for cluster headache. Clinical pharmacology and possible mode of action. Headache. 2009 Jan;49(1):117-25. doi: 10.1111/j.1526-4610.2008.01298.x. [PubMed:19125880 ]
  2. Chen X, Ji ZL, Chen YZ: TTD: Therapeutic Target Database. Nucleic Acids Res. 2002 Jan 1;30(1):412-5. [PubMed:11752352 ]
  3. Freeze BS, McNulty MM, Hanck DA: State-dependent verapamil block of the cloned human Ca(v)3.1 T-type Ca(2+) channel. Mol Pharmacol. 2006 Aug;70(2):718-26. Epub 2006 May 12. [PubMed:16699084 ]
Kind
Protein
Organism
Human
Pharmacological action
unknown
Actions
inhibitor
General Function:
Voltage-gated calcium channel activity
Specific Function:
Voltage-sensitive calcium channels (VSCC) mediate the entry of calcium ions into excitable cells and are also involved in a variety of calcium-dependent processes, including muscle contraction, hormone or neurotransmitter release, gene expression, cell motility, cell division and cell death. The isoform alpha-1B gives rise to N-type calcium currents. N-type calcium channels belong to the 'high-...
Gene Name:
CACNA1B
Uniprot ID:
Q00975
Molecular Weight:
262493.84 Da
References
  1. Tfelt-Hansen P, Tfelt-Hansen J: Verapamil for cluster headache. Clinical pharmacology and possible mode of action. Headache. 2009 Jan;49(1):117-25. doi: 10.1111/j.1526-4610.2008.01298.x. [PubMed:19125880 ]
Kind
Protein
Organism
Human
Pharmacological action
unknown
Actions
inhibitor
General Function:
Voltage-gated calcium channel activity
Specific Function:
Voltage-sensitive calcium channels (VSCC) mediate the entry of calcium ions into excitable cells and are also involved in a variety of calcium-dependent processes, including muscle contraction, hormone or neurotransmitter release, gene expression, cell motility, cell division and cell death. The isoform alpha-1A gives rise to P and/or Q-type calcium currents. P/Q-type calcium channels belong to...
Gene Name:
CACNA1A
Uniprot ID:
O00555
Molecular Weight:
282362.39 Da
References
  1. Tfelt-Hansen P, Tfelt-Hansen J: Verapamil for cluster headache. Clinical pharmacology and possible mode of action. Headache. 2009 Jan;49(1):117-25. doi: 10.1111/j.1526-4610.2008.01298.x. [PubMed:19125880 ]
Kind
Protein
Organism
Human
Pharmacological action
unknown
Actions
inhibitor
General Function:
Voltage-gated potassium channel activity involved in ventricular cardiac muscle cell action potential repolarization
Specific Function:
Pore-forming (alpha) subunit of voltage-gated inwardly rectifying potassium channel. Channel properties are modulated by cAMP and subunit assembly. Mediates the rapidly activating component of the delayed rectifying potassium current in heart (IKr). Isoforms USO have no channel activity by themself, but modulates channel characteristics by forming heterotetramers with other isoforms which are r...
Gene Name:
KCNH2
Uniprot ID:
Q12809
Molecular Weight:
126653.52 Da
References
  1. Duan JJ, Ma JH, Zhang PH, Wang XP, Zou AR, Tu DN: Verapamil blocks HERG channel by the helix residue Y652 and F656 in the S6 transmembrane domain. Acta Pharmacol Sin. 2007 Jul;28(7):959-67. [PubMed:17588331 ]
  2. Cheng HC, Incardona J, McCullough B: Isolated perfused and paced guinea pig heart to test for drug-induced changes of the QT interval. J Pharmacol Toxicol Methods. 2006 Nov-Dec;54(3):278-87. Epub 2006 Feb 28. [PubMed:16507347 ]
  3. Schneider J, Hauser R, Andreas JO, Linz K, Jahnel U: Differential effects of human ether-a-go-go-related gene (HERG) blocking agents on QT duration variability in conscious dogs. Eur J Pharmacol. 2005 Apr 4;512(1):53-60. [PubMed:15814090 ]
  4. Ridley JM, Dooley PC, Milnes JT, Witchel HJ, Hancox JC: Lidoflazine is a high affinity blocker of the HERG K(+)channel. J Mol Cell Cardiol. 2004 May;36(5):701-5. [PubMed:15135665 ]
  5. Shimizu W, Aiba T, Antzelevitch C: Specific therapy based on the genotype and cellular mechanism in inherited cardiac arrhythmias. Long QT syndrome and Brugada syndrome. Curr Pharm Des. 2005;11(12):1561-72. [PubMed:15892662 ]
  6. Tfelt-Hansen P, Tfelt-Hansen J: Verapamil for cluster headache. Clinical pharmacology and possible mode of action. Headache. 2009 Jan;49(1):117-25. doi: 10.1111/j.1526-4610.2008.01298.x. [PubMed:19125880 ]
Kind
Protein
Organism
Human
Pharmacological action
unknown
Actions
other
General Function:
Voltage-gated sodium channel activity involved in sa node cell action potential
Specific Function:
This protein mediates the voltage-dependent sodium ion permeability of excitable membranes. Assuming opened or closed conformations in response to the voltage difference across the membrane, the protein forms a sodium-selective channel through which Na(+) ions may pass in accordance with their electrochemical gradient. It is a tetrodotoxin-resistant Na(+) channel isoform. This channel is respon...
Gene Name:
SCN5A
Uniprot ID:
Q14524
Molecular Weight:
226937.475 Da
References
  1. Milberg P, Reinsch N, Osada N, Wasmer K, Monnig G, Stypmann J, Breithardt G, Haverkamp W, Eckardt L: Verapamil prevents torsade de pointes by reduction of transmural dispersion of repolarization and suppression of early afterdepolarizations in an intact heart model of LQT3. Basic Res Cardiol. 2005 Jul;100(4):365-71. Epub 2005 Jun 10. [PubMed:15944809 ]
Kind
Protein
Organism
Human
Pharmacological action
unknown
Actions
inhibitor
General Function:
Voltage-gated potassium channel activity
Specific Function:
This receptor is controlled by G proteins. Inward rectifier potassium channels are characterized by a greater tendency to allow potassium to flow into the cell rather than out of it. Their voltage dependence is regulated by the concentration of extracellular potassium; as external potassium is raised, the voltage range of the channel opening shifts to more positive voltages. The inward rectific...
Gene Name:
KCNJ11
Uniprot ID:
Q14654
Molecular Weight:
43540.375 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 ]
  2. Yamada S, Kane GC, Behfar A, Liu XK, Dyer RB, Faustino RS, Miki T, Seino S, Terzic A: Protection conferred by myocardial ATP-sensitive K+ channels in pressure overload-induced congestive heart failure revealed in KCNJ11 Kir6.2-null mutant. J Physiol. 2006 Dec 15;577(Pt 3):1053-65. Epub 2006 Oct 12. [PubMed:17038430 ]
  3. Shigeto M, Katsura M, Matsuda M, Ohkuma S, Kaku K: Nateglinide and mitiglinide, but not sulfonylureas, induce insulin secretion through a mechanism mediated by calcium release from endoplasmic reticulum. J Pharmacol Exp Ther. 2007 Jul;322(1):1-7. Epub 2007 Apr 4. [PubMed:17409272 ]
Kind
Protein
Organism
Human
Pharmacological action
unknown
Actions
other/unknown
General Function:
Serotonin:sodium symporter activity
Specific Function:
Serotonin transporter whose primary function in the central nervous system involves the regulation of serotonergic signaling via transport of serotonin molecules from the synaptic cleft back into the pre-synaptic terminal for re-utilization. Plays a key role in mediating regulation of the availability of serotonin to other receptors of serotonergic systems. Terminates the action of serotonin an...
Gene Name:
SLC6A4
Uniprot ID:
P31645
Molecular Weight:
70324.165 Da
References
  1. Tatsumi M, Groshan K, Blakely RD, Richelson E: Pharmacological profile of antidepressants and related compounds at human monoamine transporters. Eur J Pharmacol. 1997 Dec 11;340(2-3):249-58. [PubMed:9537821 ]
  2. Brown NL, Sirugue O, Worcel M: The effects of some slow channel blocking drugs on high affinity serotonin uptake by rat brain synaptosomes. Eur J Pharmacol. 1986 Apr 9;123(1):161-5. [PubMed:2940099 ]

Enzymes

Kind
Protein
Organism
Human
Pharmacological action
unknown
Actions
substrateinhibitor
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. Zhou SF, Zhou ZW, Yang LP, Cai JP: Substrates, inducers, inhibitors and structure-activity relationships of human Cytochrome P450 2C9 and implications in drug development. Curr Med Chem. 2009;16(27):3480-675. Epub 2009 Sep 1. [PubMed:19515014 ]
  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 ]
  3. Ekins S, Bravi G, Wikel JH, Wrighton SA: Three-dimensional-quantitative structure activity relationship analysis of cytochrome P-450 3A4 substrates. J Pharmacol Exp Ther. 1999 Oct;291(1):424-33. [PubMed:10490933 ]
  4. Drug Interactions: Cytochrome P450 Drug Interaction Table [Link]
Kind
Protein
Organism
Human
Pharmacological action
unknown
Actions
substrateinhibitor
General Function:
Oxygen binding
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.
Gene Name:
CYP3A5
Uniprot ID:
P20815
Molecular Weight:
57108.065 Da
References
  1. Zhou SF, Zhou ZW, Yang LP, Cai JP: Substrates, inducers, inhibitors and structure-activity relationships of human Cytochrome P450 2C9 and implications in drug development. Curr Med Chem. 2009;16(27):3480-675. Epub 2009 Sep 1. [PubMed:19515014 ]
  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 ]
  3. Drug Interactions: Cytochrome P450 Drug Interaction Table [Link]
Kind
Protein
Organism
Human
Pharmacological action
unknown
Actions
substrateinhibitor
General Function:
Oxygen binding
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.
Gene Name:
CYP3A7
Uniprot ID:
P24462
Molecular Weight:
57525.03 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 ]
  2. Drug Interactions: Cytochrome P450 Drug Interaction Table [Link]
Kind
Protein
Organism
Human
Pharmacological action
unknown
Actions
substrate
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. 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 ]
  2. Drug Interactions: Cytochrome P450 Drug Interaction Table [Link]
Kind
Protein
Organism
Human
Pharmacological action
unknown
Actions
substrateinhibitor
General Function:
Steroid 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 oxidizes a variety of structurally unrelated compounds, including steroids, fatty acids, and xenobiotics. This enzyme contributes to the wide pharmacokinetics variability of the metabolism of drugs such as S-warfarin, diclofenac, phenyto...
Gene Name:
CYP2C9
Uniprot ID:
P11712
Molecular Weight:
55627.365 Da
References
  1. Zhou SF, Zhou ZW, Yang LP, Cai JP: Substrates, inducers, inhibitors and structure-activity relationships of human Cytochrome P450 2C9 and implications in drug development. Curr Med Chem. 2009;16(27):3480-675. Epub 2009 Sep 1. [PubMed:19515014 ]
  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
substrate
General Function:
Steroid 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 oxidizes a variety of structurally unrelated compounds, including steroids, fatty acids, and xenobiotics. In the epoxidation of arachidonic acid it generates only 14,15- and 11,12-cis-epoxyeicosatrienoic acids. It is the principal enzyme...
Gene Name:
CYP2C8
Uniprot ID:
P10632
Molecular Weight:
55824.275 Da
References
  1. Zhou SF, Zhou ZW, Yang LP, Cai JP: Substrates, inducers, inhibitors and structure-activity relationships of human Cytochrome P450 2C9 and implications in drug development. Curr Med Chem. 2009;16(27):3480-675. Epub 2009 Sep 1. [PubMed:19515014 ]
  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
substrate
General Function:
Steroid hydroxylase activity
Specific Function:
Responsible for the metabolism of a number of therapeutic agents such as the anticonvulsant drug S-mephenytoin, omeprazole, proguanil, certain barbiturates, diazepam, propranolol, citalopram and imipramine.
Gene Name:
CYP2C19
Uniprot ID:
P33261
Molecular Weight:
55930.545 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 ]
Kind
Protein
Organism
Human
Pharmacological action
unknown
Actions
substrate
General Function:
Steroid 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 oxidizes a variety of structurally unrelated compounds, including steroids, fatty acids, and xenobiotics.
Gene Name:
CYP2C18
Uniprot ID:
P33260
Molecular Weight:
55710.075 Da
References
  1. Zhou SF, Zhou ZW, Yang LP, Cai JP: Substrates, inducers, inhibitors and structure-activity relationships of human Cytochrome P450 2C9 and implications in drug development. Curr Med Chem. 2009;16(27):3480-675. Epub 2009 Sep 1. [PubMed:19515014 ]
Kind
Protein
Organism
Human
Pharmacological action
unknown
Actions
substrateinducer
General Function:
Steroid 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 oxidizes a variety of structurally unrelated compounds, including steroids, fatty acids, and xenobiotics. Acts as a 1,4-cineole 2-exo-monooxygenase.
Gene Name:
CYP2B6
Uniprot ID:
P20813
Molecular Weight:
56277.81 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 ]
Kind
Protein
Organism
Human
Pharmacological action
unknown
Actions
inhibitor
General Function:
Steroid hydroxylase activity
Specific Function:
Responsible for the metabolism of many drugs and environmental chemicals that it oxidizes. It is involved in the metabolism of drugs such as antiarrhythmics, adrenoceptor antagonists, and tricyclic antidepressants.
Gene Name:
CYP2D6
Uniprot ID:
P10635
Molecular Weight:
55768.94 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
substrateinhibitorinducer
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. Perloff MD, von Moltke LL, Fahey JM, Daily JP, Greenblatt DJ: Induction of P-glycoprotein expression by HIV protease inhibitors in cell culture. AIDS. 2000 Jun 16;14(9):1287-9. [PubMed:10894301 ]
  2. Romiti N, Tramonti G, Chieli E: Influence of different chemicals on MDR-1 P-glycoprotein expression and activity in the HK-2 proximal tubular cell line. Toxicol Appl Pharmacol. 2002 Sep 1;183(2):83-91. [PubMed:12387747 ]
  3. Choo EF, Leake B, Wandel C, Imamura H, Wood AJ, Wilkinson GR, Kim RB: Pharmacological inhibition of P-glycoprotein transport enhances the distribution of HIV-1 protease inhibitors into brain and testes. Drug Metab Dispos. 2000 Jun;28(6):655-60. [PubMed:10820137 ]
  4. Kawahara I, Kato Y, Suzuki H, Achira M, Ito K, Crespi CL, Sugiyama Y: Selective inhibition of human cytochrome P450 3A4 by N-[2(R)-hydroxy-1(S)-indanyl]-5-[2(S)-(1, 1-dimethylethylaminocarbonyl)-4-[(furo[2, 3-b]pyridin-5-yl)methyl]piperazin-1-yl]-4(S)-hydroxy-2(R)-phenylmethy lpentanamide and P-glycoprotein by valspodar in gene transfectant systems. Drug Metab Dispos. 2000 Oct;28(10):1238-43. [PubMed:10997946 ]
  5. Fujita R, Ishikawa M, Takayanagi M, Takayanagi Y, Sasaki K: Enhancement of doxorubicin activity in multidrug-resistant cells by mefloquine. Methods Find Exp Clin Pharmacol. 2000 Jun;22(5):281-4. [PubMed:11031728 ]
  6. Gao J, Murase O, Schowen RL, Aube J, Borchardt RT: A functional assay for quantitation of the apparent affinities of ligands of P-glycoprotein in Caco-2 cells. Pharm Res. 2001 Feb;18(2):171-6. [PubMed:11405287 ]
  7. Wang EJ, Casciano CN, Clement RP, Johnson WW: Active transport of fluorescent P-glycoprotein substrates: evaluation as markers and interaction with inhibitors. Biochem Biophys Res Commun. 2001 Nov 30;289(2):580-5. [PubMed:11716514 ]
  8. Leonessa F, Kim JH, Ghiorghis A, Kulawiec RJ, Hammer C, Talebian A, Clarke R: C-7 analogues of progesterone as potent inhibitors of the P-glycoprotein efflux pump. J Med Chem. 2002 Jan 17;45(2):390-8. [PubMed:11784143 ]
  9. Tang F, Horie K, Borchardt RT: Are MDCK cells transfected with the human MDR1 gene a good model of the human intestinal mucosa? Pharm Res. 2002 Jun;19(6):765-72. [PubMed:12134945 ]
  10. Zhang S, Morris ME: Effects of the flavonoids biochanin A, morin, phloretin, and silymarin on P-glycoprotein-mediated transport. J Pharmacol Exp Ther. 2003 Mar;304(3):1258-67. [PubMed:12604704 ]
  11. Horie K, Tang F, Borchardt RT: Isolation and characterization of Caco-2 subclones expressing high levels of multidrug resistance protein efflux transporter. Pharm Res. 2003 Feb;20(2):161-8. [PubMed:12636153 ]
  12. Schwab D, Fischer H, Tabatabaei A, Poli S, Huwyler J: Comparison of in vitro P-glycoprotein screening assays: recommendations for their use in drug discovery. J Med Chem. 2003 Apr 24;46(9):1716-25. [PubMed:12699389 ]
  13. van der Sandt IC, Blom-Roosemalen MC, de Boer AG, Breimer DD: Specificity of doxorubicin versus rhodamine-123 in assessing P-glycoprotein functionality in the LLC-PK1, LLC-PK1:MDR1 and Caco-2 cell lines. Eur J Pharm Sci. 2000 Sep;11(3):207-14. [PubMed:11042226 ]
  14. Ibrahim S, Peggins J, Knapton A, Licht T, Aszalos A: Influence of antipsychotic, antiemetic, and Ca(2+) channel blocker drugs on the cellular accumulation of the anticancer drug daunorubicin: P-glycoprotein modulation. J Pharmacol Exp Ther. 2000 Dec;295(3):1276-83. [PubMed:11082465 ]
  15. Wang EJ, Casciano CN, Clement RP, Johnson WW: Evaluation of the interaction of loratadine and desloratadine with P-glycoprotein. Drug Metab Dispos. 2001 Aug;29(8):1080-3. [PubMed:11454724 ]
  16. Weiss J, Dormann SM, Martin-Facklam M, Kerpen CJ, Ketabi-Kiyanvash N, Haefeli WE: Inhibition of P-glycoprotein by newer antidepressants. J Pharmacol Exp Ther. 2003 Apr;305(1):197-204. [PubMed:12649369 ]
  17. Wils P, Phung-Ba V, Warnery A, Lechardeur D, Raeissi S, Hidalgo IJ, Scherman D: Polarized transport of docetaxel and vinblastine mediated by P-glycoprotein in human intestinal epithelial cell monolayers. Biochem Pharmacol. 1994 Oct 7;48(7):1528-30. [PubMed:7945455 ]
  18. Hait WN, Gesmonde JF, Murren JR, Yang JM, Chen HX, Reiss M: Terfenadine (Seldane): a new drug for restoring sensitivity to multidrug resistant cancer cells. Biochem Pharmacol. 1993 Jan 26;45(2):401-6. [PubMed:8094615 ]
  19. Pouliot JF, L'Heureux F, Liu Z, Prichard RK, Georges E: Reversal of P-glycoprotein-associated multidrug resistance by ivermectin. Biochem Pharmacol. 1997 Jan 10;53(1):17-25. [PubMed:8960059 ]
  20. Kuhnel JM, Perrot JY, Faussat AM, Marie JP, Schwaller MA: Functional assay of multidrug resistant cells using JC-1, a carbocyanine fluorescent probe. Leukemia. 1997 Jul;11(7):1147-55. [PubMed:9205004 ]
  21. Kim AE, Dintaman JM, Waddell DS, Silverman JA: Saquinavir, an HIV protease inhibitor, is transported by P-glycoprotein. J Pharmacol Exp Ther. 1998 Sep;286(3):1439-45. [PubMed:9732409 ]
  22. Bebawy M, Morris MB, Roufogalis BD: A continuous fluorescence assay for the study of P-glycoprotein-mediated drug efflux using inside-out membrane vesicles. Anal Biochem. 1999 Mar 15;268(2):270-7. [PubMed:10075817 ]
  23. Golstein PE, Boom A, van Geffel J, Jacobs P, Masereel B, Beauwens R: P-glycoprotein inhibition by glibenclamide and related compounds. Pflugers Arch. 1999 Apr;437(5):652-60. [PubMed:10087141 ]
  24. Jonsson O, Behnam-Motlagh P, Persson M, Henriksson R, Grankvist K: Increase in doxorubicin cytotoxicity by carvedilol inhibition of P-glycoprotein activity. Biochem Pharmacol. 1999 Dec 1;58(11):1801-6. [PubMed:10571255 ]
  25. Eagling VA, Profit L, Back DJ: Inhibition of the CYP3A4-mediated metabolism and P-glycoprotein-mediated transport of the HIV-1 protease inhibitor saquinavir by grapefruit juice components. Br J Clin Pharmacol. 1999 Oct;48(4):543-52. [PubMed:10583025 ]
  26. Choi CH, Kim JH, Kim SH: Reversal of P-glycoprotein-mediated MDR by 5,7,3',4',5'-pentamethoxyflavone and SAR. Biochem Biophys Res Commun. 2004 Jul 30;320(3):672-9. [PubMed:15240100 ]
  27. Honda Y, Ushigome F, Koyabu N, Morimoto S, Shoyama Y, Uchiumi T, Kuwano M, Ohtani H, Sawada Y: Effects of grapefruit juice and orange juice components on P-glycoprotein- and MRP2-mediated drug efflux. Br J Pharmacol. 2004 Dec;143(7):856-64. Epub 2004 Oct 25. [PubMed:15504753 ]
  28. Hu K, Morris ME: Effects of benzyl-, phenethyl-, and alpha-naphthyl isothiocyanates on P-glycoprotein- and MRP1-mediated transport. J Pharm Sci. 2004 Jul;93(7):1901-11. [PubMed:15176077 ]
  29. Lee BH, Lee CO, Kwon MJ, Yi KY, Yoo SE, Choi SU: Differential effects of the optical isomers of KR30031 on cardiotoxicity and on multidrug resistance reversal activity. Anticancer Drugs. 2003 Feb;14(2):175-81. [PubMed:12569305 ]
  30. Nagy H, Goda K, Fenyvesi F, Bacso Z, Szilasi M, Kappelmayer J, Lustyik G, Cianfriglia M, Szabo G Jr: Distinct groups of multidrug resistance modulating agents are distinguished by competition of P-glycoprotein-specific antibodies. Biochem Biophys Res Commun. 2004 Mar 19;315(4):942-9. [PubMed:14985103 ]
  31. Petri N, Tannergren C, Rungstad D, Lennernas H: Transport characteristics of fexofenadine in the Caco-2 cell model. Pharm Res. 2004 Aug;21(8):1398-404. [PubMed:15359574 ]
  32. Baltes S, Gastens AM, Fedrowitz M, Potschka H, Kaever V, Loscher W: Differences in the transport of the antiepileptic drugs phenytoin, levetiracetam and carbamazepine by human and mouse P-glycoprotein. Neuropharmacology. 2007 Feb;52(2):333-46. Epub 2006 Oct 10. [PubMed:17045309 ]
  33. Santoni-Rugiu E, Silverman JA: Functional characterization of the rat mdr1b encoded P-glycoprotein: not all inducing agents are substrates. Carcinogenesis. 1997 Nov;18(11):2255-63. [PubMed:9395229 ]
  34. Sieczkowski E, Lehner C, Ambros PF, Hohenegger M: Double impact on p-glycoprotein by statins enhances doxorubicin cytotoxicity in human neuroblastoma cells. Int J Cancer. 2010 May 1;126(9):2025-35. doi: 10.1002/ijc.24885. [PubMed:19739078 ]
  35. Chiu LY, Ko JL, Lee YJ, Yang TY, Tee YT, Sheu GT: L-type calcium channel blockers reverse docetaxel and vincristine-induced multidrug resistance independent of ABCB1 expression in human lung cancer cell lines. Toxicol Lett. 2010 Feb 15;192(3):408-18. doi: 10.1016/j.toxlet.2009.11.018. Epub 2009 Nov 26. [PubMed:19944135 ]
  36. Karlsson JE, Heddle C, Rozkov A, Rotticci-Mulder J, Tuvesson O, Hilgendorf C, Andersson TB: High-activity p-glycoprotein, multidrug resistance protein 2, and breast cancer resistance protein membrane vesicles prepared from transiently transfected human embryonic kidney 293-epstein-barr virus nuclear antigen cells. Drug Metab Dispos. 2010 Apr;38(4):705-14. doi: 10.1124/dmd.109.028886. Epub 2010 Jan 13. [PubMed:20071452 ]
  37. Jutabha P, Wempe MF, Anzai N, Otomo J, Kadota T, Endou H: Xenopus laevis oocytes expressing human P-glycoprotein: probing trans- and cis-inhibitory effects on [3H]vinblastine and [3H]digoxin efflux. Pharmacol Res. 2010 Jan;61(1):76-84. doi: 10.1016/j.phrs.2009.07.002. Epub 2009 Jul 21. [PubMed:19631272 ]
  38. Kugawa F, Suzuki T, Miyata M, Tomono K, Tamanoi F: Construction of a model cell line for the assay of MDR1 (multi drug resistance gene-1) substrates/inhibitors using HeLa cells. Pharmazie. 2009 May;64(5):296-300. [PubMed:19530439 ]
  39. Dahan A, Amidon GL: Small intestinal efflux mediated by MRP2 and BCRP shifts sulfasalazine intestinal permeability from high to low, enabling its colonic targeting. Am J Physiol Gastrointest Liver Physiol. 2009 Aug;297(2):G371-7. doi: 10.1152/ajpgi.00102.2009. Epub 2009 Jun 18. [PubMed:19541926 ]
  40. Noguchi K, Kawahara H, Kaji A, Katayama K, Mitsuhashi J, Sugimoto Y: Substrate-dependent bidirectional modulation of P-glycoprotein-mediated drug resistance by erlotinib. Cancer Sci. 2009 Sep;100(9):1701-7. doi: 10.1111/j.1349-7006.2009.01213.x. Epub 2009 May 12. [PubMed:19493273 ]
  41. Dahan A, Sabit H, Amidon GL: The H2 receptor antagonist nizatidine is a P-glycoprotein substrate: characterization of its intestinal epithelial cell efflux transport. AAPS J. 2009 Jun;11(2):205-13. doi: 10.1208/s12248-009-9092-5. Epub 2009 Mar 25. [PubMed:19319690 ]
  42. Pauli-Magnus C, von Richter O, Burk O, Ziegler A, Mettang T, Eichelbaum M, Fromm MF: Characterization of the major metabolites of verapamil as substrates and inhibitors of P-glycoprotein. J Pharmacol Exp Ther. 2000 May;293(2):376-82. [PubMed:10773005 ]
  43. Polli JW, Wring SA, Humphreys JE, Huang L, Morgan JB, Webster LO, Serabjit-Singh CS: Rational use of in vitro P-glycoprotein assays in drug discovery. J Pharmacol Exp Ther. 2001 Nov;299(2):620-8. [PubMed:11602674 ]
  44. Adachi Y, Suzuki H, Sugiyama Y: Comparative studies on in vitro methods for evaluating in vivo function of MDR1 P-glycoprotein. Pharm Res. 2001 Dec;18(12):1660-8. [PubMed:11785684 ]
  45. Troutman MD, Thakker DR: Novel experimental parameters to quantify the modulation of absorptive and secretory transport of compounds by P-glycoprotein in cell culture models of intestinal epithelium. Pharm Res. 2003 Aug;20(8):1210-24. [PubMed:12948019 ]
  46. Faassen F, Vogel G, Spanings H, Vromans H: Caco-2 permeability, P-glycoprotein transport ratios and brain penetration of heterocyclic drugs. Int J Pharm. 2003 Sep 16;263(1-2):113-22. [PubMed:12954186 ]
  47. Dagenais C, Graff CL, Pollack GM: Variable modulation of opioid brain uptake by P-glycoprotein in mice. Biochem Pharmacol. 2004 Jan 15;67(2):269-76. [PubMed:14698039 ]
  48. Borgnia MJ, Eytan GD, Assaraf YG: Competition of hydrophobic peptides, cytotoxic drugs, and chemosensitizers on a common P-glycoprotein pharmacophore as revealed by its ATPase activity. J Biol Chem. 1996 Feb 9;271(6):3163-71. [PubMed:8621716 ]
  49. Collett A, Tanianis-Hughes J, Hallifax D, Warhurst G: Predicting P-glycoprotein effects on oral absorption: correlation of transport in Caco-2 with drug pharmacokinetics in wild-type and mdr1a(-/-) mice in vivo. Pharm Res. 2004 May;21(5):819-26. [PubMed:15180340 ]
  50. Tfelt-Hansen P, Tfelt-Hansen J: Verapamil for cluster headache. Clinical pharmacology and possible mode of action. Headache. 2009 Jan;49(1):117-25. doi: 10.1111/j.1526-4610.2008.01298.x. [PubMed:19125880 ]
Kind
Protein
Organism
Human
Pharmacological action
unknown
Actions
inhibitor
General Function:
Secondary active organic cation transmembrane transporter activity
Specific Function:
Translocates a broad array of organic cations with various structures and molecular weights including the model compounds 1-methyl-4-phenylpyridinium (MPP), tetraethylammonium (TEA), N-1-methylnicotinamide (NMN), 4-(4-(dimethylamino)styryl)-N-methylpyridinium (ASP), the endogenous compounds choline, guanidine, histamine, epinephrine, adrenaline, noradrenaline and dopamine, and the drugs quinine...
Gene Name:
SLC22A1
Uniprot ID:
O15245
Molecular Weight:
61153.345 Da
References
  1. Zhang L, Dresser MJ, Gray AT, Yost SC, Terashita S, Giacomini KM: Cloning and functional expression of a human liver organic cation transporter. Mol Pharmacol. 1997 Jun;51(6):913-21. [PubMed:9187257 ]
  2. Zhang L, Schaner ME, Giacomini KM: Functional characterization of an organic cation transporter (hOCT1) in a transiently transfected human cell line (HeLa). J Pharmacol Exp Ther. 1998 Jul;286(1):354-61. [PubMed:9655880 ]
Kind
Protein
Organism
Human
Pharmacological action
unknown
Actions
inhibitor
General Function:
Organic anion transmembrane transporter activity
Specific Function:
May act as an inducible transporter in the biliary and intestinal excretion of organic anions. Acts as an alternative route for the export of bile acids and glucuronides from cholestatic hepatocytes (By similarity).
Gene Name:
ABCC3
Uniprot ID:
O15438
Molecular Weight:
169341.14 Da
References
  1. Zeng H, Chen ZS, Belinsky MG, Rea PA, Kruh GD: Transport of methotrexate (MTX) and folates by multidrug resistance protein (MRP) 3 and MRP1: effect of polyglutamylation on MTX transport. Cancer Res. 2001 Oct 1;61(19):7225-32. [PubMed:11585759 ]
Kind
Protein
Organism
Human
Pharmacological action
unknown
Actions
inhibitor
General Function:
Atpase activity, coupled to transmembrane movement of substances
Specific Function:
May be an organic anion pump relevant to cellular detoxification.
Gene Name:
ABCC4
Uniprot ID:
O15439
Molecular Weight:
149525.33 Da
References
  1. Chen ZS, Lee K, Walther S, Raftogianis RB, Kuwano M, Zeng H, Kruh GD: Analysis of methotrexate and folate transport by multidrug resistance protein 4 (ABCC4): MRP4 is a component of the methotrexate efflux system. Cancer Res. 2002 Jun 1;62(11):3144-50. [PubMed:12036927 ]
  2. Bai J, Lai L, Yeo HC, Goh BC, Tan TM: Multidrug resistance protein 4 (MRP4/ABCC4) mediates efflux of bimane-glutathione. Int J Biochem Cell Biol. 2004 Feb;36(2):247-57. [PubMed:14643890 ]
Kind
Protein
Organism
Human
Pharmacological action
unknown
Actions
inhibitor
General Function:
Symporter activity
Specific Function:
Sodium-ion dependent, high affinity carnitine transporter. Involved in the active cellular uptake of carnitine. Transports one sodium ion with one molecule of carnitine. Also transports organic cations such as tetraethylammonium (TEA) without the involvement of sodium. Also relative uptake activity ratio of carnitine to TEA is 11.3.
Gene Name:
SLC22A5
Uniprot ID:
O76082
Molecular Weight:
62751.08 Da
References
  1. Ohashi R, Tamai I, Yabuuchi H, Nezu JI, Oku A, Sai Y, Shimane M, Tsuji A: Na(+)-dependent carnitine transport by organic cation transporter (OCTN2): its pharmacological and toxicological relevance. J Pharmacol Exp Ther. 1999 Nov;291(2):778-84. [PubMed:10525100 ]
  2. Ohashi R, Tamai I, Nezu Ji J, Nikaido H, Hashimoto N, Oku A, Sai Y, Shimane M, Tsuji A: Molecular and physiological evidence for multifunctionality of carnitine/organic cation transporter OCTN2. Mol Pharmacol. 2001 Feb;59(2):358-66. [PubMed:11160873 ]
Kind
Protein
Organism
Human
Pharmacological action
unknown
Actions
inhibitor
General Function:
Transporter activity
Specific Function:
Involved in the ATP-dependent secretion of bile salts into the canaliculus of hepatocytes.
Gene Name:
ABCB11
Uniprot ID:
O95342
Molecular Weight:
146405.83 Da
References
  1. Wang EJ, Casciano CN, Clement RP, Johnson WW: Fluorescent substrates of sister-P-glycoprotein (BSEP) evaluated as markers of active transport and inhibition: evidence for contingent unequal binding sites. Pharm Res. 2003 Apr;20(4):537-44. [PubMed:12739759 ]
Kind
Protein
Organism
Human
Pharmacological action
unknown
Actions
inhibitor
General Function:
Transporter activity
Specific Function:
Mediates export of organic anions and drugs from the cytoplasm. Mediates ATP-dependent transport of glutathione and glutathione conjugates, leukotriene C4, estradiol-17-beta-o-glucuronide, methotrexate, antiviral drugs and other xenobiotics. Confers resistance to anticancer drugs. Hydrolyzes ATP with low efficiency.
Gene Name:
ABCC1
Uniprot ID:
P33527
Molecular Weight:
171589.5 Da
References
  1. Lespine A, Dupuy J, Orlowski S, Nagy T, Glavinas H, Krajcsi P, Alvinerie M: Interaction of ivermectin with multidrug resistance proteins (MRP1, 2 and 3). Chem Biol Interact. 2006 Feb 25;159(3):169-79. Epub 2005 Dec 27. [PubMed:16384552 ]
Kind
Protein
Organism
Human
Pharmacological action
unknown
Actions
inhibitor
General Function:
Sodium-independent organic anion transmembrane transporter activity
Specific Function:
Mediates the Na(+)-independent transport of organic anions such as sulfobromophthalein (BSP) and conjugated (taurocholate) and unconjugated (cholate) bile acids (By similarity). Selectively inhibited by the grapefruit juice component naringin.
Gene Name:
SLCO1A2
Uniprot ID:
P46721
Molecular Weight:
74144.105 Da
References
  1. Cvetkovic M, Leake B, Fromm MF, Wilkinson GR, Kim RB: OATP and P-glycoprotein transporters mediate the cellular uptake and excretion of fexofenadine. Drug Metab Dispos. 1999 Aug;27(8):866-71. [PubMed:10421612 ]
  2. Shitara Y, Sugiyama D, Kusuhara H, Kato Y, Abe T, Meier PJ, Itoh T, Sugiyama Y: Comparative inhibitory effects of different compounds on rat oatpl (slc21a1)- and Oatp2 (Slc21a5)-mediated transport. Pharm Res. 2002 Feb;19(2):147-53. [PubMed:11883641 ]
Kind
Protein
Organism
Human
Pharmacological action
unknown
Actions
inhibitor
General Function:
Atpase activity, coupled to transmembrane movement of substances
Specific Function:
ATP-dependent transporter probably involved in cellular detoxification through lipophilic anion extrusion.
Gene Name:
ABCC10
Uniprot ID:
Q5T3U5
Molecular Weight:
161627.375 Da
References
  1. Chen ZS, Hopper-Borge E, Belinsky MG, Shchaveleva I, Kotova E, Kruh GD: Characterization of the transport properties of human multidrug resistance protein 7 (MRP7, ABCC10). Mol Pharmacol. 2003 Feb;63(2):351-8. [PubMed:12527806 ]
Kind
Protein
Organism
Human
Pharmacological action
unknown
Actions
inhibitor
General Function:
Organic anion transmembrane transporter activity
Specific Function:
Mediates hepatobiliary excretion of numerous organic anions. May function as a cellular cisplatin transporter.
Gene Name:
ABCC2
Uniprot ID:
Q92887
Molecular Weight:
174205.64 Da
References
  1. Tang F, Horie K, Borchardt RT: Are MDCK cells transfected with the human MRP2 gene a good model of the human intestinal mucosa? Pharm Res. 2002 Jun;19(6):773-9. [PubMed:12134946 ]
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 ]
  2. Wu X, George RL, Huang W, Wang H, Conway SJ, Leibach FH, Ganapathy V: Structural and functional characteristics and tissue distribution pattern of rat OCTN1, an organic cation transporter, cloned from placenta. Biochim Biophys Acta. 2000 Jun 1;1466(1-2):315-27. [PubMed:10825452 ]
Kind
Protein
Organism
Human
Pharmacological action
unknown
Actions
inhibitor
General Function:
Xenobiotic-transporting atpase activity
Specific Function:
High-capacity urate exporter functioning in both renal and extrarenal urate excretion. Plays a role in porphyrin homeostasis as it is able to mediates the export of protoporhyrin IX (PPIX) both from mitochondria to cytosol and from cytosol to extracellular space, and cellular export of hemin, and heme. Xenobiotic transporter that may play an important role in the exclusion of xenobiotics from t...
Gene Name:
ABCG2
Uniprot ID:
Q9UNQ0
Molecular Weight:
72313.47 Da
References
  1. Ozvegy-Laczka C, Hegedus T, Varady G, Ujhelly O, Schuetz JD, Varadi A, Keri G, Orfi L, Nemet K, Sarkadi B: High-affinity interaction of tyrosine kinase inhibitors with the ABCG2 multidrug transporter. Mol Pharmacol. 2004 Jun;65(6):1485-95. [PubMed:15155841 ]
Kind
Protein
Organism
Human
Pharmacological action
unknown
Actions
inhibitor
General Function:
Sodium-independent organic anion transmembrane transporter activity
Specific Function:
Mediates the Na(+)-independent uptake of organic anions such as pravastatin, taurocholate, methotrexate, dehydroepiandrosterone sulfate, 17-beta-glucuronosyl estradiol, estrone sulfate, prostaglandin E2, thromboxane B2, leukotriene C3, leukotriene E4, thyroxine and triiodothyronine. Involved in the clearance of bile acids and organic anions from the liver.
Gene Name:
SLCO1B1
Uniprot ID:
Q9Y6L6
Molecular Weight:
76447.99 Da
References
  1. Oostendorp RL, van de Steeg E, van der Kruijssen CM, Beijnen JH, Kenworthy KE, Schinkel AH, Schellens JH: Organic anion-transporting polypeptide 1B1 mediates transport of Gimatecan and BNP1350 and can be inhibited by several classic ATP-binding cassette (ABC) B1 and/or ABCG2 inhibitors. Drug Metab Dispos. 2009 Apr;37(4):917-23. doi: 10.1124/dmd.108.024901. Epub 2009 Jan 12. [PubMed:19139163 ]
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Drug created on June 13, 2005 07:24 / Updated on April 29, 2016 02:28