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Identification
NameAtorvastatin
Accession NumberDB01076  (APRD00055)
TypeSmall Molecule
GroupsApproved
Description

Atorvastatin (Lipitor) is a member of the drug class known as statins. It is used for lowering cholesterol. Atorvastatin is a competitive inhibitor of hydroxymethylglutaryl-coenzyme A (HMG-CoA) reductase, the rate-determining enzyme in cholesterol biosynthesis via the mevalonate pathway. HMG-CoA reductase catalyzes the conversion of HMG-CoA to mevalonate. Atorvastatin acts primarily in the liver. Decreased hepatic cholesterol levels increases hepatic uptake of cholesterol and reduces plasma cholesterol levels.

Structure
Thumb
Synonyms
Lipovastatinklonal
External Identifiers Not Available
Prescription Products
NameDosageStrengthRouteLabellerMarketing StartMarketing End
Act Atorvastatintablet80 mgoralActavis Pharma Company2010-05-19Not applicableCanada
Act Atorvastatintablet40 mgoralActavis Pharma Company2010-05-19Not applicableCanada
Act Atorvastatintablet20 mgoralActavis Pharma Company2010-05-19Not applicableCanada
Act Atorvastatintablet10 mgoralActavis Pharma Company2010-05-19Not applicableCanada
Atorvastatintablet80 mgoralSanis Health Inc2010-05-27Not applicableCanada
Atorvastatintablet40 mgoralApotex Inc2013-01-07Not applicableCanada
Atorvastatintablet10 mgoralRatiopharm Inc Division Of Teva Canada Limited2010-05-192013-06-27Canada
Atorvastatintablet10 mgoralRanbaxy Pharmaceuticals Canada Inc.Not applicableNot applicableCanada
Atorvastatintablet20 mgoralRatiopharm Inc Division Of Teva Canada Limited2010-05-192013-06-27Canada
Atorvastatintablet20 mgoralRanbaxy Pharmaceuticals Canada Inc.Not applicableNot applicableCanada
Atorvastatintablet40 mgoralSanis Health Inc2010-05-27Not applicableCanada
Atorvastatintablet20 mgoralApotex Inc2013-01-07Not applicableCanada
Atorvastatintablet80 mgoralActavis Pharma CompanyNot applicableNot applicableCanada
Atorvastatintablet20 mgoralSanis Health Inc2010-05-27Not applicableCanada
Atorvastatintablet80 mgoralSivem Pharmaceuticals Ulc2012-06-26Not applicableCanada
Atorvastatintablet10 mgoralApotex Inc2013-01-07Not applicableCanada
Atorvastatintablet40 mgoralActavis Pharma CompanyNot applicableNot applicableCanada
Atorvastatintablet10 mgoralSanis Health Inc2010-05-27Not applicableCanada
Atorvastatintablet40 mgoralSivem Pharmaceuticals Ulc2012-06-26Not applicableCanada
Atorvastatintablet20 mgoralActavis Pharma CompanyNot applicableNot applicableCanada
Atorvastatintablet80 mgoralPro Doc Limitee2010-05-21Not applicableCanada
Atorvastatintablet20 mgoralSivem Pharmaceuticals Ulc2012-06-26Not applicableCanada
Atorvastatintablet10 mgoralActavis Pharma CompanyNot applicableNot applicableCanada
Atorvastatintablet40 mgoralPro Doc Limitee2010-05-21Not applicableCanada
Atorvastatintablet10 mgoralSivem Pharmaceuticals Ulc2012-06-26Not applicableCanada
Atorvastatintablet80 mgoralRatiopharm Inc Division Of Teva Canada Limited2010-05-192013-06-27Canada
Atorvastatintablet80 mgoralRanbaxy Pharmaceuticals Canada Inc.Not applicableNot applicableCanada
Atorvastatintablet20 mgoralPro Doc Limitee2010-05-21Not applicableCanada
Atorvastatintablet40 mgoralRanbaxy Pharmaceuticals Canada Inc.Not applicableNot applicableCanada
Atorvastatintablet10 mgoralPro Doc Limitee2010-05-21Not applicableCanada
Atorvastatintablet80 mgoralApotex Inc2013-01-07Not applicableCanada
Atorvastatintablet40 mgoralRatiopharm Inc Division Of Teva Canada Limited2010-05-192013-06-27Canada
Atorvastatin Calciumtablet, film coated10 mg/1oralCardinal Health2012-01-162016-04-05Us
Atorvastatin Calciumtablet, film coated20 mg/1oralAphena Pharma Solutions Tennessee, Llc2011-11-302016-04-05Us
Atorvastatin Calciumtablet, film coated80 mg/1oralLegacy Pharmaceutical Packaging, Llc2011-11-302016-04-05Us
Atorvastatin Calciumtablet, film coated80 mg/1oralWatson Laboratories, Inc.2011-11-302016-04-23Us
Atorvastatin Calciumtablet, film coated40 mg/1oralAmerican Health Packaging2013-07-052016-04-05Us
Atorvastatin Calciumtablet, film coated20 mg/1oralLegacy Pharmaceutical Packaging2011-11-302016-04-05Us
Atorvastatin Calciumtablet, film coated40 mg/1oralCardinal Health2012-01-022016-04-05Us
Atorvastatin Calciumtablet, film coated80 mg/1oralAphena Pharma Solutions Tennessee, Llc2011-11-302016-04-05Us
Atorvastatin Calciumtablet, film coated40 mg/1oralLegacy Pharmaceutical Packaging, Llc2011-11-302016-04-05Us
Atorvastatin Calciumtablet, film coated40 mg/1oralWatson Laboratories, Inc.2011-11-302016-04-23Us
Atorvastatin Calciumtablet, film coated20 mg/1oralAmerican Health Packaging2013-07-052016-04-05Us
Atorvastatin Calciumtablet, film coated80 mg/1oralGreenstone LLC2011-11-302016-04-05Us
Atorvastatin Calciumtablet, film coated40 mg/1oralGreenstone LLC2011-11-302016-04-05Us
Atorvastatin Calciumtablet, film coated40 mg/1oralAphena Pharma Solutions Tennessee, Llc2011-11-302016-04-05Us
Atorvastatin Calciumtablet, film coated20 mg/1oralLegacy Pharmaceutical Packaging, Llc2011-11-302016-04-05Us
Atorvastatin Calciumtablet, film coated20 mg/1oralWatson Laboratories, Inc.2011-11-302016-04-23Us
Atorvastatin Calciumtablet, film coated10 mg/1oralAmerican Health Packaging2013-07-052016-04-05Us
Atorvastatin Calciumtablet, film coated20 mg/1oralGreenstone LLC2011-11-302016-04-05Us
Atorvastatin Calciumtablet, film coated10 mg/1oralRebel Distributors Corp2011-11-302016-04-05Us
Atorvastatin Calciumtablet, film coated10 mg/1oralLegacy Pharmaceutical Packaging, Llc2013-01-012016-04-05Us
Atorvastatin Calciumtablet, film coated10 mg/1oralWatson Laboratories, Inc.2011-11-302016-04-23Us
Atorvastatin Calciumtablet, film coated10 mg/1oralGreenstone LLC2013-01-012016-04-05Us
Atorvastatin Calciumtablet, film coated80 mg/1oralRebel Distributors Corp1996-12-172016-04-05Us
Atorvastatin Calciumtablet, film coated80 mg/1oralLegacy Pharmaceutical Packaging2011-11-302016-04-05Us
Atorvastatin Calciumtablet, film coated80 mg/1oralKAISER FOUNDATION HOSPITALS2013-11-052016-04-23Us
Atorvastatin Calciumtablet, film coated40 mg/1oralRebel Distributors Corp1996-12-172016-04-05Us
Atorvastatin Calciumtablet, film coated40 mg/1oralLegacy Pharmaceutical Packaging2011-11-302016-04-05Us
Atorvastatin Calciumtablet, film coated20 mg/1oralbryant ranch prepack2011-11-302016-04-05Us
Atorvastatin Calciumtablet, film coated20 mg/1oralState of Florida DOH Central Pharmacy2014-01-012016-04-05Us
Atorvastatin Calciumtablet, film coated20 mg/1oralCardinal Health2012-01-162016-04-05Us
Atorvastatin Calciumtablet, film coated40 mg/1oralRebel Distributors Corp1996-12-172016-04-05Us
Atorvastatin Calciumtablet, film coated20 mg/1oralLegacy Pharmaceutical Packaging2011-11-302016-04-05Us
Atorvastatin Calciumtablet, film coated10 mg/1oralLegacy Pharmaceutical Packaging2011-11-302016-04-05Us
Atorvastatin Calciumtablet, film coated40 mg/1oralLegacy Pharmaceutical Packaging2011-11-302016-04-05Us
Atorvastatin-10tablet10 mgoralSivem Pharmaceuticals Ulc2013-10-23Not applicableCanada
Atorvastatin-10tablet10 mgoralPro Doc Limitee2010-06-012011-07-27Canada
Atorvastatin-20tablet20 mgoralSivem Pharmaceuticals Ulc2013-10-23Not applicableCanada
Atorvastatin-20tablet20 mgoralPro Doc Limitee2010-06-012011-07-27Canada
Atorvastatin-40tablet40 mgoralSivem Pharmaceuticals Ulc2013-10-23Not applicableCanada
Atorvastatin-40tablet40 mgoralPro Doc Limitee2010-06-012011-07-27Canada
Atorvastatin-80tablet80 mgoralSivem Pharmaceuticals Ulc2013-10-23Not applicableCanada
Atorvastatin-80tablet80 mgoralPro Doc Limitee2010-06-012011-07-27Canada
Auro-atorvastatintablet10 mgoralAuro Pharma Inc2013-06-13Not applicableCanada
Auro-atorvastatintablet80 mgoralAuro Pharma Inc2013-06-13Not applicableCanada
Auro-atorvastatintablet40 mgoralAuro Pharma Inc2013-06-13Not applicableCanada
Auro-atorvastatintablet20 mgoralAuro Pharma Inc2013-06-13Not applicableCanada
Ava-atorvastatintablet20 mgoralAvanstra Inc2011-11-282014-08-21Canada
Ava-atorvastatintablet10 mgoralAvanstra Inc2011-11-282014-08-21Canada
Ava-atorvastatintablet80 mgoralAvanstra Inc2011-11-282014-08-21Canada
Ava-atorvastatintablet40 mgoralAvanstra Inc2011-11-282014-08-21Canada
Dom-atorvastatintablet40 mgoralDominion Pharmacal2013-08-09Not applicableCanada
Dom-atorvastatintablet20 mgoralDominion Pharmacal2013-08-09Not applicableCanada
Dom-atorvastatintablet80 mgoralDominion PharmacalNot applicableNot applicableCanada
Dom-atorvastatintablet40 mgoralDominion Pharmacal2010-12-17Not applicableCanada
Dom-atorvastatintablet10 mgoralDominion Pharmacal2013-08-09Not applicableCanada
Dom-atorvastatintablet20 mgoralDominion Pharmacal2010-12-17Not applicableCanada
Dom-atorvastatintablet10 mgoralDominion Pharmacal2010-12-17Not applicableCanada
Dom-atorvastatintablet80 mgoralDominion PharmacalNot applicableNot applicableCanada
Gd-atorvastatintablet40 mgoralGenmed A Division Of Pfizer Canada Inc2010-05-20Not applicableCanada
Gd-atorvastatintablet20 mgoralGenmed A Division Of Pfizer Canada Inc2010-05-20Not applicableCanada
Gd-atorvastatintablet10 mgoralGenmed A Division Of Pfizer Canada Inc2010-05-20Not applicableCanada
Gd-atorvastatintablet80 mgoralGenmed A Division Of Pfizer Canada Inc2010-05-20Not applicableCanada
Jamp-atorvastatintablet20 mgoralJamp Pharma Corporation2012-09-10Not applicableCanada
Jamp-atorvastatintablet40 mgoralJamp Pharma Corporation2012-09-10Not applicableCanada
Jamp-atorvastatintablet10 mgoralJamp Pharma Corporation2012-09-10Not applicableCanada
Jamp-atorvastatintablet80 mgoralJamp Pharma Corporation2012-09-10Not applicableCanada
Lipitortablet, film coated20 mg/1oralPhysicians Total Care, Inc2004-03-122016-04-05Us
Lipitortablet, film coated40 mg/1oralLake Erie Medical & Surgical Supply DBA Quality Care Products LLC2012-03-052016-04-05Us
Lipitortablet, film coated10 mg/1oralPHARMAKON, LLC2010-12-012016-04-05Us
Lipitortablet, film coated10 mg/1oralbryant ranch prepack1996-12-172016-04-05Us
Lipitortablet, film coated40 mg/1oralPhysicians Total Care, Inc2000-07-062016-04-05Us
Lipitortablet, film coated10 mg/1oralParke Davis Div Of Pfizer Inc1996-12-172016-04-23Us
Lipitortablet, film coated20 mg/1oralbryant ranch prepack1996-12-172016-04-05Us
Lipitortablet, film coated10 mg/1oralPhysicians Total Care, Inc1997-05-052016-04-05Us
Lipitortablet, film coated20 mg/1oralLake Erie Medical & Surgical Supply DBA Quality Care Products LLC2012-03-052016-04-05Us
Lipitortablet, film coated80 mg/1oralA S Medication Solutions Llc2002-04-082016-04-05Us
Lipitortablet, film coated10 mg/1oralLake Erie Medical & Surgical Supply DBA Quality Care Products LLC2012-03-052016-04-05Us
Lipitortablet, film coated80 mg/1oralCardinal Health2000-04-072016-04-05Us
Lipitortablet, film coated40 mg/1oralA S Medication Solutions Llc1998-06-082016-04-05Us
Lipitortablet, film coated20 mg/1oralREMEDYREPACK INC.2013-05-142016-03-16Us
Lipitortablet, film coated40 mg/1oralCardinal Health1996-12-172016-04-05Us
Lipitortablet, film coated40 mg/1oralAphena Pharma Solutions Tennessee, Llc1996-12-172016-04-05Us
Lipitortablet80 mgoralPfizer Canada Inc2001-06-29Not applicableCanada
Lipitortablet, film coated20 mg/1oralA S Medication Solutions Llc1997-03-112016-04-05Us
Lipitortablet, film coated10 mg/1oralREMEDYREPACK INC.2013-06-042016-04-05Us
Lipitortablet, film coated20 mg/1oralCardinal Health1996-12-172016-04-05Us
Lipitortablet, film coated80 mg/1oralAphena Pharma Solutions Tennessee, Llc2000-04-072016-04-05Us
Lipitortablet40 mgoralPfizer Canada Inc1997-03-05Not applicableCanada
Lipitortablet, film coated10 mg/1oralA S Medication Solutions Llc1997-03-112016-04-05Us
Lipitortablet, film coated80 mg/1oralPHARMAKON, LLC2010-12-012016-04-05Us
Lipitortablet, film coated10 mg/1oralPd Rx Pharmaceuticals, Inc.1996-12-172016-04-05Us
Lipitortablet, film coated10 mg/1oralCardinal Health1996-12-172016-04-05Us
Lipitortablet, film coated80 mg/1oralParke Davis Div Of Pfizer Inc2000-04-072016-04-23Us
Lipitortablet20 mgoralPfizer Canada Inc1997-03-05Not applicableCanada
Lipitortablet, film coated40 mg/1oralPHARMAKON, LLC2010-12-012016-04-05Us
Lipitortablet, film coated40 mg/1oralPd Rx Pharmaceuticals, Inc.1996-12-172016-04-05Us
Lipitortablet, film coated40 mg/1oralParke Davis Div Of Pfizer Inc1996-12-172016-04-23Us
Lipitortablet, film coated80 mg/1oralbryant ranch prepack2000-04-072016-04-05Us
Lipitortablet10 mgoralPfizer Canada Inc1997-03-05Not applicableCanada
Lipitortablet, film coated80 mg/1oralLake Erie Medical & Surgical Supply DBA Quality Care Products LLC2012-03-052016-04-05Us
Lipitortablet, film coated20 mg/1oralPHARMAKON, LLC2010-12-012016-04-05Us
Lipitortablet, film coated20 mg/1oralPd Rx Pharmaceuticals, Inc.1996-12-172016-04-05Us
Lipitortablet, film coated80 mg/1oralPhysicians Total Care, Inc2006-01-112016-04-05Us
Lipitortablet, film coated40 mg/1oralRebel Distributors Corp1996-12-172016-04-05Us
Lipitortablet, film coated20 mg/1oralParke Davis Div Of Pfizer Inc1996-12-172016-04-23Us
Lipitortablet, film coated40 mg/1oralbryant ranch prepack1996-12-172016-04-05Us
Mylan-atorvastatintablet20 mgoralMylan Pharmaceuticals Ulc2011-10-17Not applicableCanada
Mylan-atorvastatintablet10 mgoralMylan Pharmaceuticals Ulc2011-10-17Not applicableCanada
Mylan-atorvastatintablet80 mgoralMylan Pharmaceuticals Ulc2014-06-03Not applicableCanada
Mylan-atorvastatintablet40 mgoralMylan Pharmaceuticals Ulc2014-06-03Not applicableCanada
Mylan-atorvastatintablet20 mgoralMylan Pharmaceuticals Ulc2014-06-03Not applicableCanada
Mylan-atorvastatintablet80 mgoralMylan Pharmaceuticals Ulc2011-10-17Not applicableCanada
Mylan-atorvastatintablet10 mgoralMylan Pharmaceuticals Ulc2014-06-03Not applicableCanada
Mylan-atorvastatintablet40 mgoralMylan Pharmaceuticals Ulc2011-10-17Not applicableCanada
Novo-atorvastatintablet80 mgoralNovopharm Limited2010-05-192015-10-26Canada
Novo-atorvastatintablet40 mgoralNovopharm Limited2010-05-192015-10-26Canada
Novo-atorvastatintablet20 mgoralNovopharm Limited2010-05-192015-10-26Canada
Novo-atorvastatintablet10 mgoralNovopharm Limited2010-05-192015-10-26Canada
Ntp-atorvastatintablet80 mgoralTeva Canada LimitedNot applicableNot applicableCanada
Ntp-atorvastatintablet40 mgoralTeva Canada LimitedNot applicableNot applicableCanada
Ntp-atorvastatintablet20 mgoralTeva Canada LimitedNot applicableNot applicableCanada
Ntp-atorvastatintablet10 mgoralTeva Canada LimitedNot applicableNot applicableCanada
PMS-atorvastatintablet40 mgoralPharmascience Inc2010-05-19Not applicableCanada
PMS-atorvastatintablet80 mgoralPharmascience Inc2010-05-19Not applicableCanada
PMS-atorvastatintablet20 mgoralPharmascience Inc2010-05-19Not applicableCanada
PMS-atorvastatintablet10 mgoralPharmascience Inc2010-05-19Not applicableCanada
PMS-atorvastatintablet80 mgoralPharmascience IncNot applicableNot applicableCanada
PMS-atorvastatintablet80 mgoralPharmascience Inc2013-03-26Not applicableCanada
PMS-atorvastatintablet40 mgoralPharmascience IncNot applicableNot applicableCanada
PMS-atorvastatintablet40 mgoralPharmascience Inc2013-03-26Not applicableCanada
PMS-atorvastatintablet20 mgoralPharmascience IncNot applicableNot applicableCanada
PMS-atorvastatintablet20 mgoralPharmascience Inc2013-03-26Not applicableCanada
PMS-atorvastatintablet10 mgoralPharmascience IncNot applicableNot applicableCanada
PMS-atorvastatintablet10 mgoralPharmascience Inc2013-03-26Not applicableCanada
Q-gen Atorvastatintablet10 mgoralQ Gen Pharmaceuticals IncNot applicableNot applicableCanada
Q-gen Atorvastatintablet20 mgoralQ Gen Pharmaceuticals IncNot applicableNot applicableCanada
Q-gen Atorvastatintablet80 mgoralQ Gen Pharmaceuticals IncNot applicableNot applicableCanada
Q-gen Atorvastatintablet40 mgoralQ Gen Pharmaceuticals IncNot applicableNot applicableCanada
Ran-atorvastatintablet80 mgoralRanbaxy Pharmaceuticals Canada Inc.2010-05-20Not applicableCanada
Ran-atorvastatintablet40 mgoralRanbaxy Pharmaceuticals Canada Inc.2010-05-20Not applicableCanada
Ran-atorvastatintablet20 mgoralRanbaxy Pharmaceuticals Canada Inc.2010-05-20Not applicableCanada
Ran-atorvastatintablet10 mgoralRanbaxy Pharmaceuticals Canada Inc.2010-05-20Not applicableCanada
Ratio-atorvastatintablet10 mgoralTeva Canada Limited2010-05-19Not applicableCanada
Ratio-atorvastatintablet80 mgoralTeva Canada Limited2010-05-19Not applicableCanada
Ratio-atorvastatintablet40 mgoralTeva Canada Limited2010-05-19Not applicableCanada
Ratio-atorvastatintablet20 mgoralTeva Canada Limited2010-05-19Not applicableCanada
Rbx-atorvastatintablet20 mgoralRanbaxy Pharmaceuticals Canada Inc.Not applicableNot applicableCanada
Rbx-atorvastatintablet10 mgoralRanbaxy Pharmaceuticals Canada Inc.Not applicableNot applicableCanada
Rbx-atorvastatintablet80 mgoralRanbaxy Pharmaceuticals Canada Inc.Not applicableNot applicableCanada
Rbx-atorvastatintablet40 mgoralRanbaxy Pharmaceuticals Canada Inc.Not applicableNot applicableCanada
Reddy-atorvastatintablet10 mgoralDr Reddys Laboratories Ltd2015-06-22Not applicableCanada
Reddy-atorvastatintablet80 mgoralDr Reddys Laboratories Ltd2015-06-22Not applicableCanada
Reddy-atorvastatintablet40 mgoralDr Reddys Laboratories Ltd2015-06-22Not applicableCanada
Reddy-atorvastatintablet20 mgoralDr Reddys Laboratories Ltd2015-06-22Not applicableCanada
Riva-atorvastatintablet80 mgoralLaboratoire Riva Inc2014-03-20Not applicableCanada
Riva-atorvastatintablet40 mgoralLaboratoire Riva Inc2014-03-20Not applicableCanada
Riva-atorvastatintablet20 mgoralLaboratoire Riva Inc2014-03-20Not applicableCanada
Riva-atorvastatintablet10 mgoralLaboratoire Riva Inc2014-03-20Not applicableCanada
Sandoz Atorvastatintablet80 mgoralSandoz Canada Incorporated2010-05-19Not applicableCanada
Sandoz Atorvastatintablet40 mgoralSandoz Canada Incorporated2010-05-19Not applicableCanada
Sandoz Atorvastatintablet20 mgoralSandoz Canada Incorporated2010-05-19Not applicableCanada
Sandoz Atorvastatintablet10 mgoralSandoz Canada Incorporated2010-05-19Not applicableCanada
Generic Prescription Products
NameDosageStrengthRouteLabellerMarketing StartMarketing End
Apo-atorvastatintablet10 mgoralApotex Inc2010-05-19Not applicableCanada
Apo-atorvastatintablet80 mgoralApotex Inc2010-05-19Not applicableCanada
Apo-atorvastatintablet40 mgoralApotex Inc2010-05-19Not applicableCanada
Apo-atorvastatintablet20 mgoralApotex Inc2010-05-19Not applicableCanada
Atorvastatin Calciumtablet20 mg/1oralNcs Health Care Of Ky, Inc Dba Vangard Labs2012-07-172016-04-23Us
Atorvastatin Calciumtablet, film coated20 mg/1oralMylan Pharmaceuticals Inc.2012-05-302016-04-23Us
Atorvastatin Calciumtablet80 mg/1oralDr. Reddy's Laboratories Limited2012-07-172016-04-05Us
Atorvastatin Calciumtablet20 mg/1oralState of Florida DOH Central Pharmacy2014-11-012016-04-05Us
Atorvastatin Calciumtablet, film coated10 mg/1oralbryant ranch prepack2012-05-292016-04-05Us
Atorvastatin Calciumtablet, film coated40 mg/1oralNorthwind Pharmaceuticals2014-04-032016-04-05Us
Atorvastatin Calciumtablet, film coated10 mg/1oralNorthwind Pharmaceuticals2015-08-252016-04-05Us
Atorvastatin Calciumtablet, film coated40 mg/1oralKremers Urban Pharmaceuticals Inc.2013-04-052016-04-05Us
Atorvastatin Calciumtablet, film coated10 mg/1oralUnit Dose Services2012-05-292016-04-05Us
Atorvastatin Calciumtablet, film coated40 mg/1oralAvera Mc Kennan Hospital2015-03-022016-04-05Us
Atorvastatin Calciumtablet, film coated80 mg/1oralCardinal Health2013-09-192016-04-05Us
Atorvastatin Calciumtablet, film coated40 mg/1oralLake Erie Medical DBA Quality Care Products LLC2013-07-092016-04-05Us
Atorvastatin Calciumtablet, film coated10 mg/1oralDispensing Solutions, Inc.2011-12-012016-04-05Us
Atorvastatin Calciumtablet, film coated20 mg/1oralbryant ranch prepack2012-05-292016-04-05Us
Atorvastatin Calciumtablet, film coated20 mg/1oralAphena Pharma Solutions Tennessee, Llc2012-05-292016-04-05Us
Atorvastatin Calciumtablet, film coated80 mg/1oralMajor Pharmaceuticals2014-10-312016-04-05Us
Atorvastatin Calciumtablet, film coated20 mg/1oralApotex Corp.2012-05-292016-04-05Us
Atorvastatin Calciumtablet, film coated10 mg/1oralClinical Solutions Wholesale, Llc2012-05-292016-04-05Us
Atorvastatin Calciumtablet, film coated80 mg/1oralLegacy Pharmaceutical Packaging2012-05-292016-04-05Us
Atorvastatin Calciumtablet, film coated10 mg/1oralState of Florida DOH Central Pharmacy2014-01-012016-04-05Us
Atorvastatin Calciumtablet, film coated40 mg/1oralProficient Rx LP2012-05-292016-04-05Us
Atorvastatin Calciumtablet, film coated40 mg/1oralApotex Corp.2012-05-292016-04-05Us
Atorvastatin Calciumtablet, film coated80 mg/1oralPreferred Pharmaceuticals Inc.2016-02-162016-04-05Us
Atorvastatin Calciumtablet, film coated20 mg/1oralLake Erie Medical DBA Quality Care Products LLC2013-07-092016-04-05Us
Atorvastatin Calciumtablet40 mg/1oralState of Florida DOH Central Pharmacy2014-11-012016-04-05Us
Atorvastatin Calciumtablet, film coated80 mg/1oralRanbaxy Pharmaceuticals Inc.2011-12-012016-04-05Us
Atorvastatin Calciumtablet, film coated10 mg/301oralNorthwind Pharmaceuticals2014-04-252016-04-05Us
Atorvastatin Calciumtablet, film coated20 mg/1oralKremers Urban Pharmaceuticals Inc.2013-04-052016-04-05Us
Atorvastatin Calciumtablet, film coated80 mg/1oralUnit Dose Services2012-05-292016-04-05Us
Atorvastatin Calciumtablet, film coated20 mg/1oralAvera Mc Kennan Hospital2015-03-052016-04-05Us
Atorvastatin Calciumtablet, film coated80 mg/1oralDispensing Solutions, Inc.2011-12-012016-04-05Us
Atorvastatin Calciumtablet, film coated40 mg/1oralAphena Pharma Solutions Tennessee, Llc2012-05-292016-04-05Us
Atorvastatin Calciumtablet, film coated40 mg/1oralMajor Pharmaceuticals2014-10-312016-04-05Us
Atorvastatin Calciumtablet, film coated10 mg/1oralApotex Corp.2012-05-292016-04-05Us
Atorvastatin Calciumtablet, film coated40 mg/1oralCardinal Health2013-07-092016-04-05Us
Atorvastatin Calciumtablet, film coated20 mg/1oralLegacy Pharmaceutical Packaging2012-05-292016-04-05Us
Atorvastatin Calciumtablet, film coated20 mg/1oralProficient Rx LP2012-05-292016-04-05Us
Atorvastatin Calciumtablet, film coated20 mg/1oralAidarex Pharmaceuticals LLC2011-12-012016-04-05Us
Atorvastatin Calciumtablet10 mg/1oralNcs Health Care Of Ky, Inc Dba Vangard Labs2012-07-172016-04-23Us
Atorvastatin Calciumtablet40 mg/1oralDr. Reddy's Laboratories Limited2012-07-172016-04-05Us
Atorvastatin Calciumtablet, film coated10 mg/1oralAvera Mc Kennan Hospital2015-03-052016-04-05Us
Atorvastatin Calciumtablet, film coated40 mg/1oralDispensing Solutions, Inc.2011-12-012016-04-05Us
Atorvastatin Calciumtablet, film coated80 mg/1oralAphena Pharma Solutions Tennessee, Llc2012-05-292016-04-05Us
Atorvastatin Calciumtablet, film coated20 mg/1oralMajor Pharmaceuticals2012-05-292016-04-05Us
Atorvastatin Calciumtablet, film coated80 mg/1oralGolden State Medical Supply, Inc.2012-05-292016-04-05Us
Atorvastatin Calciumtablet, film coated10 mg/1oralCardinal Health2013-07-092016-04-05Us
Atorvastatin Calciumtablet, film coated10 mg/1oralLegacy Pharmaceutical Packaging2012-05-292016-04-05Us
Atorvastatin Calciumtablet, film coated80 mg/1oralDIRECT RX2015-01-012016-04-05Us
Atorvastatin Calciumtablet, film coated80 mg/1oralSandoz Inc2012-05-292016-04-05Us
Atorvastatin Calciumtablet, film coated80 mg/1oralMylan Pharmaceuticals Inc.2013-09-192016-04-23Us
Atorvastatin Calciumtablet20 mg/1oralDr. Reddy's Laboratories Limited2012-07-172016-04-05Us
Atorvastatin Calciumtablet, film coated10 mg/1oralREMEDYREPACK INC.2013-10-072016-04-05Us
Atorvastatin Calciumtablet, film coated40 mg/1oralRanbaxy Pharmaceuticals Inc.2011-12-012016-04-05Us
Atorvastatin Calciumtablet, film coated80 mg/1oralMylan Institutional Inc.2014-01-232016-04-05Us
Atorvastatin Calciumtablet, film coated10 mg/1oralKremers Urban Pharmaceuticals Inc.2013-04-052016-04-05Us
Atorvastatin Calciumtablet, film coated80 mg/1oralPd Rx Pharmaceuticals, Inc.2013-04-052016-04-05Us
Atorvastatin Calciumtablet, film coated20 mg/1oralPd Rx Pharmaceuticals, Inc.2012-05-292016-04-05Us
Atorvastatin Calciumtablet, film coated10 mg/1oralMajor Pharmaceuticals2012-05-292016-04-05Us
Atorvastatin Calciumtablet, film coated40 mg/1oralGolden State Medical Supply, Inc.2012-05-292016-04-05Us
Atorvastatin Calciumtablet, film coated20 mg/1oralCardinal Health2013-07-092016-04-05Us
Atorvastatin Calciumtablet, film coated20 mg/1oralCarilion Materials Management2012-05-292016-04-05Us
Atorvastatin Calciumtablet, film coated80 mg/1oralSt Marys Medical Park Pharmacy2014-04-202016-04-05Us
Atorvastatin Calciumtablet, film coated40 mg/1oralSandoz Inc2012-05-292016-04-05Us
Atorvastatin Calciumtablet, film coated40 mg/1oralMylan Pharmaceuticals Inc.2013-09-192016-04-23Us
Atorvastatin Calciumtablet10 mg/1oralDr. Reddy's Laboratories Limited2012-07-172016-04-05Us
Atorvastatin Calciumtablet, film coated80 mg/1oralREMEDYREPACK INC.2013-07-312016-04-05Us
Atorvastatin Calciumtablet, film coated20 mg/1oralRanbaxy Pharmaceuticals Inc.2011-12-012016-04-05Us
Atorvastatin Calciumtablet, film coated40 mg/1oralMylan Institutional Inc.2014-01-292016-04-05Us
Atorvastatin Calciumtablet, film coated40 mg/1oralDIRECT RX2015-01-012016-04-05Us
Atorvastatin Calciumtablet, film coated10 mg/1oralPd Rx Pharmaceuticals, Inc.2011-12-012016-04-05Us
Atorvastatin Calciumtablet80 mg/1oralPreferred Pharmaceuticals, Inc.2015-04-202016-04-05Us
Atorvastatin Calciumtablet, film coated20 mg/1oralDispensing Solutions, Inc.2011-12-012016-04-05Us
Atorvastatin Calciumtablet, film coated10 mg/1oralPd Rx Pharmaceuticals, Inc.2012-05-292016-04-05Us
Atorvastatin Calciumtablet, film coated40 mg/1oralCardinal Health2014-10-312016-04-05Us
Atorvastatin Calciumtablet, film coated20 mg/1oralGolden State Medical Supply, Inc.2012-05-292016-04-05Us
Atorvastatin Calciumtablet, film coated10 mg/1oralCardinal Health2012-05-292016-04-05Us
Atorvastatin Calciumtablet, film coated80 mg/1oralAmerican Health Packaging2013-07-092016-04-05Us
Atorvastatin Calciumtablet, film coated40 mg/1oralSt Marys Medical Park Pharmacy2014-01-152016-04-05Us
Atorvastatin Calciumtablet, film coated20 mg/1oralSandoz Inc2012-05-292016-04-05Us
Atorvastatin Calciumtablet, film coated20 mg/1oralMylan Pharmaceuticals Inc.2013-09-192016-04-23Us
Atorvastatin Calciumtablet, film coated80 mg/1oralPhysicians Total Care, Inc.2011-12-022016-04-05Us
Atorvastatin Calciumtablet10 mg/1oralREMEDYREPACK INC.2013-05-152016-04-05Us
Atorvastatin Calciumtablet, film coated10 mg/1oralRanbaxy Pharmaceuticals Inc.2011-12-012016-04-05Us
Atorvastatin Calciumtablet, film coated20 mg/1oralMylan Institutional Inc.2014-01-292016-04-05Us
Atorvastatin Calciumtablet20 mg/1oralDIRECT RX2015-01-012016-04-05Us
Atorvastatin Calciumtablet, film coated80 mg/1oralAv Kare, Inc.2013-07-082016-04-05Us
Atorvastatin Calciumtablet, film coated20 mg/1oralPreferred Pharmaceuticals, Inc.2013-04-152016-04-05Us
Atorvastatin Calciumtablet, film coated10 mg/1oralDispensing Solutions, Inc.2011-12-012016-04-05Us
Atorvastatin Calciumtablet, film coated40 mg/1oralAmerican Health Packaging2013-07-092016-04-05Us
Atorvastatin Calciumtablet, film coated20 mg/1oralSt Marys Medical Park Pharmacy2014-04-202016-04-05Us
Atorvastatin Calciumtablet, film coated10 mg/1oralSandoz Inc2012-05-292016-04-05Us
Atorvastatin Calciumtablet, film coated10 mg/1oralMylan Pharmaceuticals Inc.2013-09-192016-04-23Us
Atorvastatin Calciumtablet, film coated40 mg/1oralPhysicians Total Care, Inc.2011-12-012016-04-05Us
Atorvastatin Calciumtablet, film coated20 mg/301oralNorthwind Pharmaceuticals2014-03-112016-04-05Us
Atorvastatin Calciumtablet, film coated10 mg/1oralProficient Rx LP2013-04-052016-04-05Us
Atorvastatin Calciumtablet, film coated10 mg/1oralMylan Institutional Inc.2014-01-302016-04-05Us
Atorvastatin Calciumtablet40 mg/1oralREMEDYREPACK INC.2015-06-052016-04-05Us
Atorvastatin Calciumtablet, film coated40 mg/1oralAv Kare, Inc.2013-07-082016-04-05Us
Atorvastatin Calciumtablet, film coated40 mg/1oralPreferred Pharmaceuticals, Inc.2013-04-152016-04-05Us
Atorvastatin Calciumtablet, film coated20 mg/1oralMed Vantx, Inc.2012-05-292016-04-05Us
Atorvastatin Calciumtablet, film coated40 mg/1oralPd Rx Pharmaceuticals, Inc.2012-05-292016-04-05Us
Atorvastatin Calciumtablet, film coated10 mg/1oralGolden State Medical Supply, Inc.2012-05-292016-04-05Us
Atorvastatin Calciumtablet, film coated80 mg/1oralCardinal Health2013-07-092016-04-05Us
Atorvastatin Calciumtablet80 mg/1oralNcs Health Care Of Ky, Inc Dba Vangard Labs2012-07-172016-04-23Us
Atorvastatin Calciumtablet, film coated80 mg/1oralMylan Pharmaceuticals Inc.2012-05-302016-04-23Us
Atorvastatin Calciumtablet, film coated20 mg/1oralPhysicians Total Care, Inc.2011-12-022016-04-05Us
Atorvastatin Calciumtablet, film coated80 mg/301oralNorthwind Pharmaceuticals2014-04-282016-04-05Us
Atorvastatin Calciumtablet, film coated80 mg/1oralProficient Rx LP2013-04-052016-04-05Us
Atorvastatin Calciumtablet, film coated40 mg/1oralUnit Dose Services2012-05-292016-04-05Us
Atorvastatin Calciumtablet20 mg/1oralREMEDYREPACK INC.2015-05-192016-04-05Us
Atorvastatin Calciumtablet, film coated20 mg/1oralAv Kare, Inc.2013-07-082016-04-05Us
Atorvastatin Calciumtablet, film coated10 mg/1oralPreferred Pharmaceuticals, Inc.2013-04-152016-04-05Us
Atorvastatin Calciumtablet, film coated40 mg/1oralbryant ranch prepack2012-05-292016-04-05Us
Atorvastatin Calciumtablet, film coated10 mg/1oralAidarex Pharmaceuticals LLC2012-05-292016-04-05Us
Atorvastatin Calciumtablet, film coated40 mg/1oralNew Horizon Rx Group, LLC2013-08-252016-04-05Us
Atorvastatin Calciumtablet, film coated40 mg/1oralInternational Laboratories, Inc.2014-06-012016-04-05Us
Atorvastatin Calciumtablet, film coated20 mg/1oralAmerican Health Packaging2013-07-092016-04-05Us
Atorvastatin Calciumtablet, film coated10 mg/1oralSt Marys Medical Park Pharmacy2014-04-202016-04-05Us
Atorvastatin Calciumtablet40 mg/1oralNcs Health Care Of Ky, Inc Dba Vangard Labs2012-07-172016-04-23Us
Atorvastatin Calciumtablet, film coated40 mg/1oralMylan Pharmaceuticals Inc.2012-05-302016-04-23Us
Atorvastatin Calciumtablet, film coated10 mg/1oralPhysicians Total Care, Inc.2011-12-022016-04-05Us
Atorvastatin Calciumtablet, film coated40 mg/1oralNorthwind Pharmaceuticals, LLC2014-10-082016-04-05Us
Atorvastatin Calciumtablet, film coated80 mg/1oralKremers Urban Pharmaceuticals Inc.2013-04-052016-04-05Us
Atorvastatin Calciumtablet, film coated20 mg/1oralUnit Dose Services2012-05-292016-04-05Us
Atorvastatin Calciumtablet, film coated80 mg/1oralCardinal Health2014-01-232016-04-05Us
Atorvastatin Calciumtablet, film coated10 mg/1oralAv Kare, Inc.2013-07-082016-04-05Us
Atorvastatin Calciumtablet, film coated20 mg/1oralDispensing Solutions, Inc.2011-12-012016-04-05Us
Atorvastatin Calciumtablet, film coated80 mg/1oralbryant ranch prepack2011-12-012016-04-05Us
Atorvastatin Calciumtablet, film coated40 mg/1oralBlenheim Pharmacal, Inc.2015-04-202016-04-05Us
Atorvastatin Calciumtablet, film coated20 mg/1oralClinical Solutions Wholesale, Llc2012-05-292016-04-05Us
Atorvastatin Calciumtablet, film coated40 mg/1oralState of Florida DOH Central Pharmacy2014-01-012016-04-05Us
Atorvastatin Calciumtablet, film coated10 mg/1oralAmerican Health Packaging2013-07-092016-04-05Us
Atorvastatin Calciumtablet, film coated80 mg/1oralApotex Corp.2012-05-292016-04-05Us
Atorvastatin Calciumtablet, film coated80 mg/1oralProficient Rx LP2012-05-292016-04-05Us
Over the Counter ProductsNot Available
International Brands
NameCompany
AtogalIngers (Czech Republic)
CardylPfizer (Spain)
FaboximFabop (Argentina)
HipolixanPasteur (Chile)
LipotropicDrugtech (Chile)
LiprimarPfizer (Hungary, Ukraine), Goedecke (Russia)
LowdenSaval (Chile)
NormalipQuesada (Argentina)
SincolIndeco (Argentina)
SortisPfizer (Austria, Czech Republic, Germany, Hungary, Poland, Portugal, Switzerland), Godecke (Germany), Parke, Davis (Germany)
TorvacardZentiva (Czech Republic, Hungary, Poland, Russia, Ukraine)
TorvastPfizer (Italy)
TotalipGuidotti (Italy)
TulipLek (Czech Republic, Russia), Wermar (Mexico), Sandoz (Poland, Ukraine), Pharmacia (Spain)
VastinaPenn (Argentina)
XanatorSieger (Greece)
XaratorParke, Davis (Italy)
ZurinelPrater (Chile)
Brand mixtures
NameLabellerIngredients
Amlodipine Besylate and Atorvastatin CalciumMylan Pharmaceuticals Inc.
Amlodipine Besylate/atorvastatin CalciumMylan Pharmaceuticals Inc.
Apo-amlodipine-atorvastatinApotex Inc
CaduetPfizer Laboratories Div Pfizer Inc
Gd-amlodipine/atorvastatinGenmed A Division Of Pfizer Canada Inc
LiptruzetMerck Sharp & Dohme Corp.
Mylan-amlodipine/atorvastatinMylan Pharmaceuticals Ulc
Pendo-amlodipine-atorvastatinPendopharm Division Of De Pharmascience Inc
PMS-amlodipine-atorvastatinPharmascience Inc
Salts
Name/CASStructureProperties
Atorvastatin Calcium
134523-03-8
Thumb
  • InChI Key: FQCKMBLVYCEXJB-ZUHSGPLBNA-L
  • Monoisotopic Mass: 1154.452941981
  • Average Mass: 1155.342
DBSALT000011
Atorvastatin calcium trihydrate
ThumbNot applicableDBSALT001499
Categories
UNIIA0JWA85V8F
CAS number134523-00-5
WeightAverage: 557.6319
Monoisotopic: 557.245175413
Chemical FormulaC33H34FN2O5
InChI KeyInChIKey=XUKUURHRXDUEBC-UHFFFAOYNA-M
InChI
InChI=1/C33H35FN2O5/c1-21(2)31-30(33(41)35-25-11-7-4-8-12-25)29(22-9-5-3-6-10-22)32(23-13-15-24(34)16-14-23)36(31)18-17-26(37)19-27(38)20-28(39)40/h3-16,21,26-27,37-38H,17-20H2,1-2H3,(H,35,41)(H,39,40)/p-1
IUPAC Name
7-[2-(4-fluorophenyl)-3-phenyl-4-(phenylcarbamoyl)-5-(propan-2-yl)-1H-pyrrol-1-yl]-3,5-dihydroxyheptanoate
SMILES
CC(C)C1=C(C(=O)NC2=CC=CC=C2)C(=C(N1CCC(O)CC(O)CC([O-])=O)C1=CC=C(F)C=C1)C1=CC=CC=C1
Taxonomy
DescriptionThis compound belongs to the class of organic compounds known as diphenylpyrroles. These are aromatic heterocyclic compounds with a structure based on a pyrrole ring linked to exactly two phenyl groups.
KingdomOrganic compounds
Super ClassOrganoheterocyclic compounds
ClassPyrroles
Sub ClassSubstituted pyrroles
Direct ParentDiphenylpyrroles
Alternative Parents
Substituents
  • 2,3-diphenylpyrrole
  • N-arylamide
  • Pyrrole-3-carboxylic acid or derivatives
  • Pyrrole-3-carboxamide
  • Halobenzene
  • Fluorobenzene
  • Beta-hydroxy acid
  • Benzenoid
  • Hydroxy acid
  • Monocyclic benzene moiety
  • Aryl halide
  • Aryl fluoride
  • Heteroaromatic compound
  • Vinylogous amide
  • Secondary carboxylic acid amide
  • Secondary alcohol
  • Carboxylic acid salt
  • Carboxamide group
  • Azacycle
  • Monocarboxylic acid or derivatives
  • Carboxylic acid
  • Carboxylic acid derivative
  • Hydrocarbon derivative
  • Organooxygen compound
  • Organonitrogen compound
  • Organofluoride
  • Organohalogen compound
  • Carbonyl group
  • Alcohol
  • Organic anion
  • Aromatic heteromonocyclic compound
Molecular FrameworkAromatic heteromonocyclic compounds
External DescriptorsNot Available
Pharmacology
IndicationMay be used as primary prevention in individuals with multiple risk factors for coronary heart disease (CHD) and as secondary prevention in individuals with CHD to reduce the risk of myocardial infarction (MI), stroke, angina, and revascularization procedures. May be used to reduce the risk of cardiovascular events in patients with acute coronary syndrome (ACS). May be used in the treatment of primary hypercholesterolemia and mixed dyslipidemia, homozygous familial hypercholesterolemia, primary dysbetalipoproteinemia, and/or hypertriglyeridemia as an adjunct to dietary therapy to decrease serum total and low-density lipoprotein cholesterol (LDL-C), apolipoprotein B (apoB), and triglyceride concentrations, while increasing high-density lipoprotein cholesterol (HDL-C) levels.
PharmacodynamicsAtorvastatin, a selective, competitive HMG-CoA reductase inhibitor, is used to lower serum total and LDL cholesterol, apoB, and triglyceride levels while increasing HDL cholesterol. High LDL-C, low HDL-C and high TG concentrations in the plasma are associated with increased risk of atherosclerosis and cardiovascular disease. The total cholesterol to HDL-C ratio is a strong predictor of coronary artery disease and high ratios are associated with higher risk of disease. Increased levels of HDL-C are associated with lower cardiovascular risk. By decreasing LDL-C and TG and increasing HDL-C, atorvastatin reduces the risk of cardiovascular morbidity and mortality. Atorvastatin has a unique structure, long half-life, and hepatic selectivity, explaining its greater LDL-lowering potency compared to other HMG-CoA reductase inhibitors.
Mechanism of actionAtorvastatin selectively and competitively inhibits the hepatic enzyme HMG-CoA reductase. As HMG-CoA reductase is responsible for converting HMG-CoA to mevalonate in the cholesterol biosynthesis pathway, this results in a subsequent decrease in hepatic cholesterol levels. Decreased hepatic cholesterol levels stimulates upregulation of hepatic LDL-C receptors which increases hepatic uptake of LDL-C and reduces serum LDL-C concentrations.
Related Articles
AbsorptionAtorvastatin is rapidly absorbed after oral administration with maximum plasma concentrations achieved in 1 to 2 hours. The absolute bioavailability of atorvastatin (parent drug) is approximately 14% and the systemic availability of HMG-CoA reductase inhibitory activity is approximately 30%. The low systemic bioavailability is due to presystemic clearance by gastrointestinal mucosa and first-pass metabolism in the liver.
Volume of distribution

381 L

Protein binding>98% bound to plasma proteins
Metabolism

Atorvastatin is extensively metabolized to ortho- and parahydroxylated derivatives and various beta-oxidation products. In vitro inhibition of HMG-CoA reductase by ortho- and parahydroxylated metabolites is equivalent to that of atorvastatin. Approximately 70% of circulating inhibitory activity for HMG-CoA reductase is attributed to active metabolites. CYP3A4 is also involved in the metabolism of atorvastatin.

SubstrateEnzymesProduct
Atorvastatin
para-hydroxyatorvastatinDetails
Atorvastatin
ortho-hydroxyatorvastatinDetails
para-hydroxyatorvastatin
Not Available
para-hydroxyatorvastatin lactoneDetails
ortho-hydroxyatorvastatin
Not Available
ortho-hydroxyatorvastatin lactoneDetails
Atorvastatin
Not Available
Atorvastatin lactoneDetails
Route of eliminationEliminated primarily in bile after hepatic and/or extrahepatic metabolism. Does not appear to undergo significant enterohepatic recirculation. Less than 2% of the orally administered dose is recovered in urine.
Half life14 hours, but half-life of HMG-CoA inhibitor activity is 20-30 hours due to longer-lived active metabolites
ClearanceNot Available
ToxicityGenerally well-tolerated. Side effects may include myalgia, constipation, asthenia, abdominal pain, and nausea. Other possible side effects include myotoxicity (myopathy, myositis, rhabdomyolysis) and hepatotoxicity. To avoid toxicity in Asian patients, lower doses should be considered.
Affected organisms
  • Humans and other mammals
PathwaysNot Available
SNP Mediated Effects
Interacting Gene/EnzymeSNP RS IDAllele nameDefining changeEffectReference(s)
Kinesin-like protein KIF6
Gene symbol: KIF6
UniProt: Q6ZMV9
rs20455 Not AvailableC AlleleImproved response to statin drugs18222353
3-hydroxy-3-methylglutaryl-coenzyme A reductase
Gene symbol: HMGCR
UniProt: P04035
rs17244841 Not AvailableT AlleleReduced response to statin drugs15199031
Multidrug resistance protein 1
Gene symbol: ABCB1
UniProt: P08183
rs1045642 MDR1*TT Allele (C3435T)Larger reduction in LDL and smaller increase in HDL cholesterol in females15081455
SNP Mediated Adverse Drug ReactionsNot Available
ADMET
Predicted ADMET features
PropertyValueProbability
Human Intestinal Absorption+0.8947
Blood Brain Barrier-0.7825
Caco-2 permeable-0.8956
P-glycoprotein substrateSubstrate0.5246
P-glycoprotein inhibitor IInhibitor0.7164
P-glycoprotein inhibitor IIInhibitor0.8724
Renal organic cation transporterNon-inhibitor0.8131
CYP450 2C9 substrateNon-substrate0.7887
CYP450 2D6 substrateNon-substrate0.9116
CYP450 3A4 substrateSubstrate0.6841
CYP450 1A2 substrateNon-inhibitor0.8551
CYP450 2C9 inhibitorNon-inhibitor0.719
CYP450 2D6 inhibitorNon-inhibitor0.9042
CYP450 2C19 inhibitorNon-inhibitor0.6191
CYP450 3A4 inhibitorNon-inhibitor0.6675
CYP450 inhibitory promiscuityHigh CYP Inhibitory Promiscuity0.6894
Ames testNon AMES toxic0.9133
CarcinogenicityNon-carcinogens0.7777
BiodegradationNot ready biodegradable0.9974
Rat acute toxicity2.5686 LD50, mol/kg Not applicable
hERG inhibition (predictor I)Weak inhibitor0.9904
hERG inhibition (predictor II)Non-inhibitor0.5101
ADMET data is predicted using admetSAR, a free tool for evaluating chemical ADMET properties. (23092397 )
Pharmacoeconomics
ManufacturersNot Available
Packagers
Dosage forms
FormRouteStrength
Tabletoral10 mg/1
Tabletoral20 mg/1
Tabletoral40 mg/1
Tabletoral80 mg/1
Tablet, film coatedoral10 mg/301
Tablet, film coatedoral20 mg/301
Tablet, film coatedoral80 mg/301
Tabletoral
Tablet, film coatedoral
Tabletoral10 mg
Tabletoral20 mg
Tabletoral40 mg
Tabletoral80 mg
Tablet, film coatedoral10 mg/1
Tablet, film coatedoral20 mg/1
Tablet, film coatedoral40 mg/1
Tablet, film coatedoral80 mg/1
Prices
Unit descriptionCostUnit
Lipitor 20 mg tablet5.0USD tablet
Lipitor 40 mg tablet5.0USD tablet
Lipitor 80 mg tablet5.0USD tablet
Lipitor 10 mg tablet3.5USD tablet
Lipitor 40 mg Tablet2.52USD tablet
Lipitor 80 mg Tablet2.52USD tablet
Lipitor 20 mg Tablet2.34USD tablet
Lipitor 10 mg Tablet1.87USD tablet
DrugBank does not sell nor buy drugs. Pricing information is supplied for informational purposes only.
Patents
Patent NumberPediatric ExtensionApprovedExpires (estimated)
CA2220018 No2001-04-172016-07-08Canada
CA2521776 No2006-04-252022-05-21Canada
US4681893 No1992-09-242009-09-24Us
US5969156 Yes1997-01-082017-01-08Us
US6455574 No1998-08-112018-08-11Us
USRE42461 Yes1997-04-252017-04-25Us
Properties
StateSolid
Experimental Properties
PropertyValueSource
melting point159.2-160.7 °CNot Available
water solubilitySodium salt soluble in water, 20.4 ug/mL (pH 2.1), 1.23 mg/mL (pH 6.0)Not Available
logP5.7Not Available
Predicted Properties
PropertyValueSource
Water Solubility0.000495 mg/mLALOGPS
logP4.41ALOGPS
logP5.39ChemAxon
logS-6.1ALOGPS
pKa (Strongest Acidic)4.33ChemAxon
pKa (Strongest Basic)-2.7ChemAxon
Physiological Charge-1ChemAxon
Hydrogen Acceptor Count5ChemAxon
Hydrogen Donor Count3ChemAxon
Polar Surface Area114.62 Å2ChemAxon
Rotatable Bond Count12ChemAxon
Refractivity169.04 m3·mol-1ChemAxon
Polarizability59.7 Å3ChemAxon
Number of Rings4ChemAxon
Bioavailability0ChemAxon
Rule of FiveYesChemAxon
Ghose FilterYesChemAxon
Veber's RuleYesChemAxon
MDDR-like RuleYesChemAxon
Spectra
Mass Spec (NIST)Not Available
SpectraNot Available
References
Synthesis Reference

Zlatko Pflaum, “Process for the preparation of amorphous atorvastatin.” U.S. Patent US20020183527, issued December 05, 2002.

US20020183527
General References
  1. Rouleau J: Improved outcome after acute coronary syndromes with an intensive versus standard lipid-lowering regimen: results from the Pravastatin or Atorvastatin Evaluation and Infection Therapy-Thrombolysis in Myocardial Infarction 22 (PROVE IT-TIMI 22) trial. Am J Med. 2005 Dec;118 Suppl 12A:28-35. [PubMed:16356805 ]
  2. Maggon K: Best-selling human medicines 2002-2004. Drug Discov Today. 2005 Jun 1;10(11):739-42. [PubMed:15922927 ]
External Links
ATC CodesC10AA05C10BA05C10BX03C10BX06C10BX08C10BX11
AHFS Codes
  • 24:06.08
PDB EntriesNot Available
FDA labelDownload (62 KB)
MSDSDownload (57.4 KB)
Interactions
Drug Interactions
Drug
AcipimoxAcipimox may increase the myopathic rhabdomyolysis activities of Atorvastatin.
AfatinibThe serum concentration of Afatinib can be increased when it is combined with Atorvastatin.
AliskirenThe serum concentration of Aliskiren can be increased when it is combined with Atorvastatin.
Aluminum hydroxideThe serum concentration of Atorvastatin can be decreased when it is combined with Aluminum hydroxide.
AmiodaroneThe metabolism of Atorvastatin can be decreased when combined with Amiodarone.
AprepitantThe serum concentration of Atorvastatin can be increased when it is combined with Aprepitant.
AripiprazoleThe serum concentration of Aripiprazole can be increased when it is combined with Atorvastatin.
AtazanavirThe serum concentration of Atorvastatin can be increased when it is combined with Atazanavir.
AzithromycinAzithromycin may increase the myopathic rhabdomyolysis activities of Atorvastatin.
BatimastatThe serum concentration of Atorvastatin can be increased when it is combined with Batimastat.
BexaroteneThe serum concentration of Atorvastatin can be decreased when it is combined with Bexarotene.
BezafibrateBezafibrate may increase the myopathic rhabdomyolysis activities of Atorvastatin.
BoceprevirThe serum concentration of Atorvastatin can be increased when it is combined with Boceprevir.
BosentanThe metabolism of Atorvastatin can be increased when combined with Bosentan.
BosutinibThe serum concentration of Bosutinib can be increased when it is combined with Atorvastatin.
Brentuximab vedotinThe serum concentration of Brentuximab vedotin can be increased when it is combined with Atorvastatin.
Calcium carbonateThe serum concentration of Atorvastatin can be decreased when it is combined with Calcium carbonate.
CholestyramineThe serum concentration of Atorvastatin can be decreased when it is combined with Cholestyramine.
CimetidineThe risk or severity of adverse effects can be increased when Atorvastatin is combined with Cimetidine.
CiprofibrateThe risk or severity of adverse effects can be increased when Ciprofibrate is combined with Atorvastatin.
ClarithromycinThe serum concentration of Atorvastatin can be increased when it is combined with Clarithromycin.
CobicistatThe serum concentration of Atorvastatin can be increased when it is combined with Cobicistat.
ColchicineColchicine may increase the myopathic rhabdomyolysis activities of Atorvastatin.
ColesevelamThe serum concentration of Atorvastatin can be decreased when it is combined with Colesevelam.
ColestipolThe serum concentration of Atorvastatin can be decreased when it is combined with Colestipol.
ConivaptanThe serum concentration of Atorvastatin can be increased when it is combined with Conivaptan.
CyclosporineThe serum concentration of Atorvastatin can be increased when it is combined with Cyclosporine.
Cyproterone acetateThe serum concentration of Atorvastatin can be increased when it is combined with Cyproterone acetate.
Dabigatran etexilateThe serum concentration of Dabigatran etexilate can be decreased when it is combined with Atorvastatin.
DabrafenibThe serum concentration of Atorvastatin can be decreased when it is combined with Dabrafenib.
DaclatasvirThe serum concentration of Atorvastatin can be increased when it is combined with Daclatasvir.
DanazolThe serum concentration of Atorvastatin can be increased when it is combined with Danazol.
DaptomycinThe risk or severity of adverse effects can be increased when Atorvastatin is combined with Daptomycin.
DarunavirThe serum concentration of Atorvastatin can be increased when it is combined with Darunavir.
DasatinibThe serum concentration of Atorvastatin can be increased when it is combined with Dasatinib.
DeferasiroxThe serum concentration of Atorvastatin can be decreased when it is combined with Deferasirox.
DigoxinThe serum concentration of Digoxin can be increased when it is combined with Atorvastatin.
DiltiazemThe serum concentration of Diltiazem can be increased when it is combined with Atorvastatin.
DofetilideThe serum concentration of Dofetilide can be increased when it is combined with Atorvastatin.
DoxorubicinThe serum concentration of Doxorubicin can be increased when it is combined with Atorvastatin.
DronedaroneThe serum concentration of Atorvastatin can be increased when it is combined with Dronedarone.
EdoxabanThe serum concentration of Edoxaban can be increased when it is combined with Atorvastatin.
EfavirenzThe serum concentration of Atorvastatin can be decreased when it is combined with Efavirenz.
EltrombopagThe serum concentration of Atorvastatin can be increased when it is combined with Eltrombopag.
ErythromycinThe serum concentration of Atorvastatin can be increased when it is combined with Erythromycin.
EtravirineThe serum concentration of Atorvastatin can be decreased when it is combined with Etravirine.
EverolimusThe serum concentration of Everolimus can be increased when it is combined with Atorvastatin.
FenofibrateThe risk or severity of adverse effects can be increased when Fenofibrate is combined with Atorvastatin.
FlibanserinThe serum concentration of Flibanserin can be increased when it is combined with Atorvastatin.
FluconazoleThe serum concentration of Atorvastatin can be increased when it is combined with Fluconazole.
FosamprenavirThe serum concentration of Atorvastatin can be increased when it is combined with Fosamprenavir.
FosaprepitantThe serum concentration of Atorvastatin can be increased when it is combined with Fosaprepitant.
FosphenytoinThe serum concentration of Atorvastatin can be decreased when it is combined with Fosphenytoin.
Fusidic AcidThe risk or severity of adverse effects can be increased when Fusidic Acid is combined with Atorvastatin.
GemfibrozilGemfibrozil may increase the myopathic rhabdomyolysis activities of Atorvastatin.
HydrocodoneThe serum concentration of Hydrocodone can be increased when it is combined with Atorvastatin.
IdelalisibThe serum concentration of Atorvastatin can be increased when it is combined with Idelalisib.
IndinavirThe serum concentration of Atorvastatin can be increased when it is combined with Indinavir.
IsoflurophateThe serum concentration of Atorvastatin can be increased when it is combined with Isoflurophate.
ItraconazoleThe serum concentration of Atorvastatin can be increased when it is combined with Itraconazole.
IvacaftorThe serum concentration of Atorvastatin can be increased when it is combined with Ivacaftor.
KetoconazoleThe risk or severity of adverse effects can be increased when Atorvastatin is combined with Ketoconazole.
LanthanumThe serum concentration of Lanthanum can be decreased when it is combined with Atorvastatin.
LedipasvirThe serum concentration of Ledipasvir can be increased when it is combined with Atorvastatin.
LomitapideThe serum concentration of Lomitapide can be increased when it is combined with Atorvastatin.
LuliconazoleThe serum concentration of Atorvastatin can be increased when it is combined with Luliconazole.
Magnesium oxideThe serum concentration of Atorvastatin can be decreased when it is combined with Magnesium oxide.
MidazolamThe serum concentration of Midazolam can be increased when it is combined with Atorvastatin.
MifepristoneThe serum concentration of Atorvastatin can be increased when it is combined with Mifepristone.
MitotaneThe serum concentration of Atorvastatin can be decreased when it is combined with Mitotane.
NaloxegolThe serum concentration of Naloxegol can be increased when it is combined with Atorvastatin.
NelfinavirThe serum concentration of Atorvastatin can be increased when it is combined with Nelfinavir.
NetupitantThe serum concentration of Atorvastatin can be increased when it is combined with Netupitant.
NiacinThe risk or severity of adverse effects can be increased when Niacin is combined with Atorvastatin.
NicotinamideThe risk or severity of adverse effects can be increased when Nicotinamide is combined with Atorvastatin.
NimodipineThe serum concentration of Nimodipine can be increased when it is combined with Atorvastatin.
PalbociclibThe serum concentration of Atorvastatin can be increased when it is combined with Palbociclib.
PazopanibThe serum concentration of Pazopanib can be increased when it is combined with Atorvastatin.
PhenytoinThe serum concentration of Atorvastatin can be decreased when it is combined with Phenytoin.
PimozideThe serum concentration of Pimozide can be increased when it is combined with Atorvastatin.
PosaconazoleThe serum concentration of Atorvastatin can be increased when it is combined with Posaconazole.
PrucaloprideThe serum concentration of Prucalopride can be increased when it is combined with Atorvastatin.
QuinineThe serum concentration of Atorvastatin can be increased when it is combined with Quinine.
RaltegravirRaltegravir may increase the myopathic rhabdomyolysis activities of Atorvastatin.
RanolazineThe serum concentration of Atorvastatin can be increased when it is combined with Ranolazine.
RifabutinThe serum concentration of Atorvastatin can be decreased when it is combined with Rifabutin.
RifaximinThe serum concentration of Rifaximin can be increased when it is combined with Atorvastatin.
RitonavirThe serum concentration of Atorvastatin can be increased when it is combined with Ritonavir.
SaquinavirThe serum concentration of Atorvastatin can be increased when it is combined with Saquinavir.
SilodosinThe serum concentration of Silodosin can be increased when it is combined with Atorvastatin.
SiltuximabThe serum concentration of Atorvastatin can be decreased when it is combined with Siltuximab.
SimeprevirThe serum concentration of Atorvastatin can be increased when it is combined with Simeprevir.
SpironolactoneThe risk or severity of adverse effects can be increased when Atorvastatin is combined with Spironolactone.
St. John's WortThe metabolism of Atorvastatin can be increased when combined with St. John's Wort.
StiripentolThe serum concentration of Atorvastatin can be increased when it is combined with Stiripentol.
TelaprevirThe serum concentration of Atorvastatin can be increased when it is combined with Telaprevir.
TelithromycinThe serum concentration of Atorvastatin can be increased when it is combined with Telithromycin.
TeriflunomideThe serum concentration of Atorvastatin can be increased when it is combined with Teriflunomide.
TesmilifeneThe serum concentration of Atorvastatin can be decreased when it is combined with Tesmilifene.
TicagrelorThe serum concentration of Atorvastatin can be increased when it is combined with Ticagrelor.
TipranavirThe serum concentration of Atorvastatin can be increased when it is combined with Tipranavir.
TocilizumabThe serum concentration of Atorvastatin can be decreased when it is combined with Tocilizumab.
TopotecanThe serum concentration of Topotecan can be increased when it is combined with Atorvastatin.
TrabectedinAtorvastatin may increase the myopathic rhabdomyolysis activities of Trabectedin.
VerapamilThe serum concentration of Verapamil can be increased when it is combined with Atorvastatin.
VincristineThe serum concentration of Vincristine can be increased when it is combined with Atorvastatin.
VoriconazoleThe serum concentration of Atorvastatin can be increased when it is combined with Voriconazole.
Food Interactions
  • Avoid alcohol.
  • Avoid drastic changes in dietary habit.
  • Avoid taking grapefruit or grapefruit juice throughout treatment. Grapefruit can significantly increase serum levels of this product.
  • Food may decrease maximum plasma levels and area under the curve, but this is clinically inconsequential according to the manufacturer.
  • Take with low fat meal.

Targets

Kind
Protein
Organism
Human
Pharmacological action
yes
Actions
inhibitor
General Function:
Nadph binding
Specific Function:
Transmembrane glycoprotein that is the rate-limiting enzyme in cholesterol biosynthesis as well as in the biosynthesis of nonsterol isoprenoids that are essential for normal cell function including ubiquinone and geranylgeranyl proteins.
Gene Name:
HMGCR
Uniprot ID:
P04035
Molecular Weight:
97475.155 Da
References
  1. Davidson MH: Rosuvastatin: a highly efficacious statin for the treatment of dyslipidaemia. Expert Opin Investig Drugs. 2002 Mar;11(3):125-41. [PubMed:12769127 ]
  2. Jafari M, Ebrahimi R, Ahmadi-Kashani M, Balian H, Bashir M: Efficacy of alternate-day dosing versus daily dosing of atorvastatin. J Cardiovasc Pharmacol Ther. 2003 Jun;8(2):123-6. [PubMed:12808485 ]
  3. Baxter JD, Webb P, Grover G, Scanlan TS: Selective activation of thyroid hormone signaling pathways by GC-1: a new approach to controlling cholesterol and body weight. Trends Endocrinol Metab. 2004 May-Jun;15(4):154-7. [PubMed:15109613 ]
  4. Maejima T, Yamazaki H, Aoki T, Tamaki T, Sato F, Kitahara M, Saito Y: Effect of pitavastatin on apolipoprotein A-I production in HepG2 cell. Biochem Biophys Res Commun. 2004 Nov 12;324(2):835-9. [PubMed:15474503 ]
  5. Bosel J, Gandor F, Harms C, Synowitz M, Harms U, Djoufack PC, Megow D, Dirnagl U, Hortnagl H, Fink KB, Endres M: Neuroprotective effects of atorvastatin against glutamate-induced excitotoxicity in primary cortical neurones. J Neurochem. 2005 Mar;92(6):1386-98. [PubMed:15748157 ]
  6. Chen X, Ji ZL, Chen YZ: TTD: Therapeutic Target Database. Nucleic Acids Res. 2002 Jan 1;30(1):412-5. [PubMed:11752352 ]
Kind
Protein
Organism
Human
Pharmacological action
no
Actions
inhibitor
General Function:
Virus receptor activity
Specific Function:
Cell surface glycoprotein receptor involved in the costimulatory signal essential for T-cell receptor (TCR)-mediated T-cell activation. Acts as a positive regulator of T-cell coactivation, by binding at least ADA, CAV1, IGF2R, and PTPRC. Its binding to CAV1 and CARD11 induces T-cell proliferation and NF-kappa-B activation in a T-cell receptor/CD3-dependent manner. Its interaction with ADA also ...
Gene Name:
DPP4
Uniprot ID:
P27487
Molecular Weight:
88277.935 Da
References
  1. Taldone T, Zito SW, Talele TT: Inhibition of dipeptidyl peptidase-IV (DPP-IV) by atorvastatin. Bioorg Med Chem Lett. 2008 Jan 15;18(2):479-84. Epub 2007 Dec 3. [PubMed:18068977 ]
Kind
Protein
Organism
Human
Pharmacological action
unknown
Actions
agonist
General Function:
Transcription regulatory region dna binding
Specific Function:
Ligand-activated transcriptional activator. Binds to the XRE promoter region of genes it activates. Activates the expression of multiple phase I and II xenobiotic chemical metabolizing enzyme genes (such as the CYP1A1 gene). Mediates biochemical and toxic effects of halogenated aromatic hydrocarbons. Involved in cell-cycle regulation. Likely to play an important role in the development and matu...
Gene Name:
AHR
Uniprot ID:
P35869
Molecular Weight:
96146.705 Da
References
  1. Hu W, Sorrentino C, Denison MS, Kolaja K, Fielden MR: Induction of cyp1a1 is a nonspecific biomarker of aryl hydrocarbon receptor activation: results of large scale screening of pharmaceuticals and toxicants in vivo and in vitro. Mol Pharmacol. 2007 Jun;71(6):1475-86. Epub 2007 Feb 27. [PubMed:17327465 ]
  2. Chauvin B, Drouot S, Barrail-Tran A, Taburet AM: Drug-drug interactions between HMG-CoA reductase inhibitors (statins) and antiviral protease inhibitors. Clin Pharmacokinet. 2013 Oct;52(10):815-31. doi: 10.1007/s40262-013-0075-4. [PubMed:23703578 ]

Enzymes

Kind
Protein
Organism
Human
Pharmacological action
unknown
Actions
substrateinhibitorinducer
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. Neuvonen PJ, Niemi M, Backman JT: Drug interactions with lipid-lowering drugs: mechanisms and clinical relevance. Clin Pharmacol Ther. 2006 Dec;80(6):565-81. [PubMed:17178259 ]
  2. Cohen LH, van Leeuwen RE, van Thiel GC, van Pelt JF, Yap SH: Equally potent inhibitors of cholesterol synthesis in human hepatocytes have distinguishable effects on different cytochrome P450 enzymes. Biopharm Drug Dispos. 2000 Dec;21(9):353-64. [PubMed:11523064 ]
  3. 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 ]
  4. 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 ]
  5. Jacobsen W, Kuhn B, Soldner A, Kirchner G, Sewing KF, Kollman PA, Benet LZ, Christians U: Lactonization is the critical first step in the disposition of the 3-hydroxy-3-methylglutaryl-CoA reductase inhibitor atorvastatin. Drug Metab Dispos. 2000 Nov;28(11):1369-78. [PubMed:11038166 ]
  6. Drug Interactions: Cytochrome P450 Drug Interaction Table [Link]
Kind
Protein
Organism
Human
Pharmacological action
unknown
Actions
substrate
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. Jacobsen W, Kuhn B, Soldner A, Kirchner G, Sewing KF, Kollman PA, Benet LZ, Christians U: Lactonization is the critical first step in the disposition of the 3-hydroxy-3-methylglutaryl-CoA reductase inhibitor atorvastatin. Drug Metab Dispos. 2000 Nov;28(11):1369-78. [PubMed:11038166 ]
  4. Drug Interactions: Cytochrome P450 Drug Interaction Table [Link]
Kind
Protein
Organism
Human
Pharmacological action
unknown
Actions
substrate
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. 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. 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. 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. Jacobsen W, Kuhn B, Soldner A, Kirchner G, Sewing KF, Kollman PA, Benet LZ, Christians U: Lactonization is the critical first step in the disposition of the 3-hydroxy-3-methylglutaryl-CoA reductase inhibitor atorvastatin. Drug Metab Dispos. 2000 Nov;28(11):1369-78. [PubMed:11038166 ]
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. Cohen LH, van Leeuwen RE, van Thiel GC, van Pelt JF, Yap SH: Equally potent inhibitors of cholesterol synthesis in human hepatocytes have distinguishable effects on different cytochrome P450 enzymes. Biopharm Drug Dispos. 2000 Dec;21(9):353-64. [PubMed:11523064 ]
Kind
Protein
Organism
Human
Pharmacological action
unknown
Actions
inhibitorinducer
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. Cohen LH, van Leeuwen RE, van Thiel GC, van Pelt JF, Yap SH: Equally potent inhibitors of cholesterol synthesis in human hepatocytes have distinguishable effects on different cytochrome P450 enzymes. Biopharm Drug Dispos. 2000 Dec;21(9):353-64. [PubMed:11523064 ]
  2. 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
inhibitor
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. Cohen LH, van Leeuwen RE, van Thiel GC, van Pelt JF, Yap SH: Equally potent inhibitors of cholesterol synthesis in human hepatocytes have distinguishable effects on different cytochrome P450 enzymes. Biopharm Drug Dispos. 2000 Dec;21(9):353-64. [PubMed:11523064 ]
Kind
Protein
Organism
Human
Pharmacological action
unknown
Actions
inducer
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. 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
substrate
General Function:
Steroid binding
Specific Function:
UDPGT is of major importance in the conjugation and subsequent elimination of potentially toxic xenobiotics and endogenous compounds. This isoform glucuronidates bilirubin IX-alpha to form both the IX-alpha-C8 and IX-alpha-C12 monoconjugates and diconjugate. Is also able to catalyze the glucuronidation of 17beta-estradiol, 17alpha-ethinylestradiol, 1-hydroxypyrene, 4-methylumbelliferone, 1-naph...
Gene Name:
UGT1A1
Uniprot ID:
P22309
Molecular Weight:
59590.91 Da
References
  1. Stormo C, Bogsrud MP, Hermann M, Asberg A, Piehler AP, Retterstol K, Kringen MK: UGT1A1*28 is associated with decreased systemic exposure of atorvastatin lactone. Mol Diagn Ther. 2013 Aug;17(4):233-7. doi: 10.1007/s40291-013-0031-x. [PubMed:23580084 ]
Kind
Protein
Organism
Human
Pharmacological action
unknown
Actions
substrate
General Function:
Retinoic acid binding
Specific Function:
UDPGT is of major importance in the conjugation and subsequent elimination of potentially toxic xenobiotics and endogenous compounds. Isoform 2 lacks transferase activity but acts as a negative regulator of isoform 1.
Gene Name:
UGT1A3
Uniprot ID:
P35503
Molecular Weight:
60337.835 Da
References
  1. Stormo C, Bogsrud MP, Hermann M, Asberg A, Piehler AP, Retterstol K, Kringen MK: UGT1A1*28 is associated with decreased systemic exposure of atorvastatin lactone. Mol Diagn Ther. 2013 Aug;17(4):233-7. doi: 10.1007/s40291-013-0031-x. [PubMed:23580084 ]
Kind
Protein
Organism
Human
Pharmacological action
unknown
Actions
substrate
General Function:
Glucuronosyltransferase activity
Specific Function:
UDPGT is of major importance in the conjugation and subsequent elimination of potentially toxic xenobiotics and endogenous compounds.Its unique specificity for 3,4-catechol estrogens and estriol suggests it may play an important role in regulating the level and activity of these potent and active estrogen metabolites. Is also active with androsterone, hyodeoxycholic acid and tetrachlorocatechol...
Gene Name:
UGT2B7
Uniprot ID:
P16662
Molecular Weight:
60694.12 Da
References
  1. http://www.pharmacologyweekly.com/content/pages/ugt-enzymes-medications-herbs-substrate-inhibitor-inducer

Transporters

Kind
Protein
Organism
Human
Pharmacological action
unknown
Actions
inhibitor
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. Wang E, Casciano CN, Clement RP, Johnson WW: HMG-CoA reductase inhibitors (statins) characterized as direct inhibitors of P-glycoprotein. Pharm Res. 2001 Jun;18(6):800-6. [PubMed:11474784 ]
  2. 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 ]
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. Hsiang B, Zhu Y, Wang Z, Wu Y, Sasseville V, Yang WP, Kirchgessner TG: A novel human hepatic organic anion transporting polypeptide (OATP2). Identification of a liver-specific human organic anion transporting polypeptide and identification of rat and human hydroxymethylglutaryl-CoA reductase inhibitor transporters. J Biol Chem. 1999 Dec 24;274(52):37161-8. [PubMed:10601278 ]
Kind
Protein
Organism
Human
Pharmacological action
unknown
Actions
substrateinhibitor
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. Hsiang B, Zhu Y, Wang Z, Wu Y, Sasseville V, Yang WP, Kirchgessner TG: A novel human hepatic organic anion transporting polypeptide (OATP2). Identification of a liver-specific human organic anion transporting polypeptide and identification of rat and human hydroxymethylglutaryl-CoA reductase inhibitor transporters. J Biol Chem. 1999 Dec 24;274(52):37161-8. [PubMed:10601278 ]
  2. Kameyama Y, Yamashita K, Kobayashi K, Hosokawa M, Chiba K: Functional characterization of SLCO1B1 (OATP-C) variants, SLCO1B1*5, SLCO1B1*15 and SLCO1B1*15+C1007G, by using transient expression systems of HeLa and HEK293 cells. Pharmacogenet Genomics. 2005 Jul;15(7):513-22. [PubMed:15970799 ]
Kind
Protein
Organism
Human
Pharmacological action
unknown
Actions
substrate
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. Knauer MJ, Urquhart BL, Meyer zu Schwabedissen HE, Schwarz UI, Lemke CJ, Leake BF, Kim RB, Tirona RG: Human skeletal muscle drug transporters determine local exposure and toxicity of statins. Circ Res. 2010 Feb 5;106(2):297-306. doi: 10.1161/CIRCRESAHA.109.203596. Epub 2009 Nov 25. [PubMed:19940267 ]
Kind
Protein
Organism
Human
Pharmacological action
unknown
Actions
substrate
General Function:
Organic anion transmembrane transporter activity
Specific Function:
Acts as a multispecific organic anion pump which can transport nucleotide analogs.
Gene Name:
ABCC5
Uniprot ID:
O15440
Molecular Weight:
160658.8 Da
References
  1. Knauer MJ, Urquhart BL, Meyer zu Schwabedissen HE, Schwarz UI, Lemke CJ, Leake BF, Kim RB, Tirona RG: Human skeletal muscle drug transporters determine local exposure and toxicity of statins. Circ Res. 2010 Feb 5;106(2):297-306. doi: 10.1161/CIRCRESAHA.109.203596. Epub 2009 Nov 25. [PubMed:19940267 ]
Kind
Protein
Organism
Human
Pharmacological action
unknown
Actions
substrate
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. Knauer MJ, Urquhart BL, Meyer zu Schwabedissen HE, Schwarz UI, Lemke CJ, Leake BF, Kim RB, Tirona RG: Human skeletal muscle drug transporters determine local exposure and toxicity of statins. Circ Res. 2010 Feb 5;106(2):297-306. doi: 10.1161/CIRCRESAHA.109.203596. Epub 2009 Nov 25. [PubMed:19940267 ]
Kind
Protein
Organism
Human
Pharmacological action
unknown
General Function:
Sodium-independent organic anion transmembrane transporter activity
Specific Function:
Mediates the Na(+)-independent transport of organic anions such as taurocholate, the prostaglandins PGD2, PGE1, PGE2, leukotriene C4, thromboxane B2 and iloprost.
Gene Name:
SLCO2B1
Uniprot ID:
O94956
Molecular Weight:
76709.98 Da
References
  1. Grube M, Kock K, Oswald S, Draber K, Meissner K, Eckel L, Bohm M, Felix SB, Vogelgesang S, Jedlitschky G, Siegmund W, Warzok R, Kroemer HK: Organic anion transporting polypeptide 2B1 is a high-affinity transporter for atorvastatin and is expressed in the human heart. Clin Pharmacol Ther. 2006 Dec;80(6):607-20. [PubMed:17178262 ]
Kind
Protein
Organism
Human
Pharmacological action
unknown
Actions
substrate
General Function:
Sodium-independent organic anion transmembrane transporter activity
Specific Function:
Mediates the Na(+)-independent uptake of organic anions such as 17-beta-glucuronosyl estradiol, taurocholate, triiodothyronine (T3), leukotriene C4, dehydroepiandrosterone sulfate (DHEAS), methotrexate and sulfobromophthalein (BSP). Involved in the clearance of bile acids and organic anions from the liver.
Gene Name:
SLCO1B3
Uniprot ID:
Q9NPD5
Molecular Weight:
77402.175 Da
References
  1. Klatt S, Fromm MF, Konig J: The influence of oral antidiabetic drugs on cellular drug uptake mediated by hepatic OATP family members. Basic Clin Pharmacol Toxicol. 2013 Apr;112(4):244-50. doi: 10.1111/bcpt.12031. Epub 2012 Dec 6. [PubMed:23121773 ]
Kind
Protein
Organism
Human
Pharmacological action
unknown
Actions
substrate
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. Becker ML, Elens LL, Visser LE, Hofman A, Uitterlinden AG, van Schaik RH, Stricker BH: Genetic variation in the ABCC2 gene is associated with dose decreases or switches to other cholesterol-lowering drugs during simvastatin and atorvastatin therapy. Pharmacogenomics J. 2013 Jun;13(3):251-6. doi: 10.1038/tpj.2011.59. Epub 2011 Dec 20. [PubMed:22186618 ]
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Drug created on June 13, 2005 07:24 / Updated on April 29, 2016 03:10