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Identification
NameAmiodarone
Accession NumberDB01118  (APRD00288)
TypeSmall Molecule
GroupsApproved, Investigational
Description

An antianginal and antiarrhythmic drug. It increases the duration of ventricular and atrial muscle action by inhibiting Na,K-activated myocardial adenosine triphosphatase. There is a resulting decrease in heart rate and in vascular resistance. [PubChem]

Structure
Thumb
Synonyms
2-Butyl-3-(3,5-diiodo-4-(2-diethylaminoethoxy)benzoyl)benzofuran
2-Butyl-3-benzofuranyl 4-(2-(diethylamino)ethoxy)-3,5-diiodophenyl ketone
2-N-Butyl-3',5'-diiodo-4'-N-diethylaminoethoxy-3-benzoylbenzofuran
Amiodarona
Amiodarone
Amiodaronum
External Identifiers Not Available
Approved Prescription Products
NameDosageStrengthRouteLabellerMarketing StartMarketing End
Amiodaronetablet200 mgoralSanis Health Inc2011-06-10Not applicableCanada
Amiodaronetablet200 mgoralSivem Pharmaceuticals Ulc2012-06-10Not applicableCanada
Amiodaronetablet200 mgoralSorres Pharma Inc2009-06-232014-06-20Canada
Amiodarone for Injection 50mg/mlsolution50 mgintravenousTeva Canada Limited2004-04-21Not applicableCanada
Amiodarone Hydrochloride for Injectionliquid50 mgintravenousSandoz Canada Incorporated2000-06-14Not applicableCanada
Amiodarone Hydrochloride for Injectionsolution50 mgintravenousHospira Healthcare Corporation2002-08-29Not applicableCanada
Amiodarone Hydrochloride for Injectionsolution50 mgintravenousFresenius Kabi Canada Ltd2002-04-23Not applicableCanada
Amiodarone Hydrochloride Injectionsolution50 mgintravenousMylan Pharmaceuticals Ulc2012-10-24Not applicableCanada
Amiodarone Omegasolution50 mgintravenousOmega Laboratories LtdNot applicableNot applicableCanada
Amiodarone Syringesolution50 mgintravenousSandoz Canada Incorporated2015-08-12Not applicableCanada
Ava-amiodaronetablet200 mgoralAvanstra Inc2011-09-152014-08-21Canada
Cordaronetablet200 mg/1oralWyeth Pharmaceuticals Inc., a subsidiary of Pfizer Inc.1985-12-01Not applicableUs
Cordaronetablet200 mgoralPfizer Canada Inc1994-12-31Not applicableCanada
Cordarone Intravenous - Liq IV 50mg/mlliquid50 mgintravenousWyeth Ayerst Canada Inc.1995-12-312003-04-17Canada
Cordarone Tab 200mgtablet200 mgoralAyerst Laboratories1986-12-311996-09-10Canada
Dom-amiodaronetablet200 mgoralDominion Pharmacal2004-04-15Not applicableCanada
Dom-amiodaronetablet100 mgoralDominion PharmacalNot applicableNot applicableCanada
Jamp-amiodaronesolution50 mgintravenousJamp Pharma CorporationNot applicableNot applicableCanada
Mylan-amiodaronetablet200 mgoralMylan Pharmaceuticals Ulc1999-08-04Not applicableCanada
Mylan-amiodarone Sterile Concentrate, BPsolution50 mgintravenousMylan Pharmaceuticals UlcNot applicableNot applicableCanada
Nexteroneinjection, solution1.8 mg/mLintravenousBaxter Healthcare Corporation2010-11-16Not applicableUs
Nexteroneinjection, solution1.5 mg/mLintravenousBaxter Healthcare Corporation2010-11-16Not applicableUs
Ntp-amiodaronetablet200 mgoralTeva Canada LimitedNot applicableNot applicableCanada
Nu-amiodaronetablet200 mgoralNu Pharm IncNot applicableNot applicableCanada
Pendo-amiodaronetablet200 mgoralPendopharm Division Of De Pharmascience IncNot applicableNot applicableCanada
PHL-amiodaronetablet100 mgoralPharmel IncNot applicableNot applicableCanada
PHL-amiodaronetablet200 mgoralPharmel Inc2002-05-27Not applicableCanada
PMS-amiodaronetablet100 mgoralPharmascience Inc2007-04-03Not applicableCanada
PMS-amiodaronetablet200 mgoralPharmascience Inc2000-07-28Not applicableCanada
Pro-amiodarone - 200tablet200 mgoralPro Doc Limitee2008-07-04Not applicableCanada
Ratio-amiodaronetablet200 mgoralRatiopharm Inc Division Of Teva Canada Limited1999-05-122014-09-19Canada
Ratio-amiodarone I.V.liquid50 mgintravenousRatiopharm Inc Division Of Teva Canada Limited2000-09-272008-08-01Canada
Riva-amiodaronetablet200 mgoralLaboratoire Riva Inc2003-03-05Not applicableCanada
Sandoz Amiodaronetablet200 mgoralSandoz Canada Incorporated2001-08-21Not applicableCanada
Teva-amiodaronetablet200 mgoralTeva Canada Limited1999-03-29Not applicableCanada
Approved Generic Prescription Products
NameDosageStrengthRouteLabellerMarketing StartMarketing End
Amiodarone HCltablet400 mg/1oralLibertas Pharma, Inc.2013-01-01Not applicableUs
Amiodarone HCltablet200 mg/1oralLibertas Pharma, Inc.2013-01-01Not applicableUs
Amiodarone Hydrochloridetablet200 mg/1oralREMEDYREPACK INC.2011-04-12Not applicableUs
Amiodarone Hydrochlorideinjection, solution50 mg/mLintravenousPhysicians Total Care, Inc.2006-12-11Not applicableUs
Amiodarone Hydrochloridetablet200 mg/1oralTeva Pharmaceuticals USA Inc1998-11-30Not applicableUs
Amiodarone Hydrochloridetablet200 mg/1oralCardinal Health1998-11-30Not applicableUs
Amiodarone Hydrochloridetablet200 mg/1oralZydus Pharmaceuticals (USA) Inc.2009-08-10Not applicableUs
Amiodarone Hydrochloridetablet200 mg/1oralTaro Pharmaceuticals U.S.A., Inc.2001-03-30Not applicableUs
Amiodarone Hydrochlorideinjection, solution50 mg/mLintravenousHospira, Inc.2013-11-25Not applicableUs
Amiodarone Hydrochloridetablet200 mg/1oralREMEDYREPACK INC.2015-05-15Not applicableUs
Amiodarone Hydrochloridetablet200 mg/1oralREMEDYREPACK INC.2014-08-01Not applicableUs
Amiodarone Hydrochlorideinjection, solution50 mg/mLintravenousMylan Institutional LLC2002-10-14Not applicableUs
Amiodarone Hydrochloridetablet200 mg/1oralLake Erie Medical DBA Quality Care Products LLC1998-11-30Not applicableUs
Amiodarone Hydrochloridetablet200 mg/1oralApotex Corp2008-11-06Not applicableUs
Amiodarone Hydrochloridetablet200 mg/1oralCadila Healthcare Limited2009-08-10Not applicableUs
Amiodarone Hydrochloridetablet200 mg/1oralPhysicians Total Care, Inc.2002-04-22Not applicableUs
Amiodarone Hydrochlorideinjection, solution50 mg/mLintravenousSagent Pharmaceuticals2013-07-15Not applicableUs
Amiodarone Hydrochloridetablet200 mg/1oralGolden State Medical Supply, Inc.2001-03-30Not applicableUs
Amiodarone Hydrochloridetablet400 mg/1oralAv Kare, Inc.2016-03-18Not applicableUs
Amiodarone Hydrochloridetablet200 mg/1oralState of Florida DOH Central Pharmacy2014-11-01Not applicableUs
Amiodarone Hydrochloridetablet200 mg/1oralRebel Distributors Corp2009-08-10Not applicableUs
Amiodarone Hydrochlorideinjection50 mg/mLintravenousWockhardt Limited2008-10-30Not applicableUs
Amiodarone Hydrochloridetablet400 mg/1oralTaro Pharmaceuticals U.S.A., Inc.2002-11-29Not applicableUs
Amiodarone Hydrochloridetablet200 mg/1oralMc Kesson Packaging A Business Unit Of Mc Kesson Corporation2008-03-01Not applicableUs
Amiodarone Hydrochlorideinjection50 mg/mLintravenousGENERAL INJECTABLES AND VACCINES, INC.2014-09-02Not applicableUs
Amiodarone Hydrochloridetablet200 mg/1oralNcs Health Care Of Ky, Inc Dba Vangard Labs1998-12-23Not applicableUs
Amiodarone Hydrochlorideinjection50 mg/mLintravenousWockhardt Limited2008-10-30Not applicableUs
Amiodarone Hydrochloridetablet200 mg/1oralMc Kesson Contract Packaging2012-01-03Not applicableUs
Amiodarone Hydrochloridetablet300 mg/1oralTaro Pharmaceuticals U.S.A., Inc.2003-12-02Not applicableUs
Amiodarone Hydrochloridetablet200 mg/1oralEon Labs, Inc.1998-12-23Not applicableUs
Amiodarone Hydrochlorideinjection, solution50 mg/mLintravenousHospira, Inc.2002-10-18Not applicableUs
Amiodarone Hydrochlorideinjection, solution50 mg/mLintravenousAPP Pharmaceuticals, LLC2003-01-28Not applicableUs
Amiodarone Hydrochlorideinjection, solution, concentrate50 mg/mLintravenousGeneral Injectables & Vaccines, Inc.2010-03-01Not applicableUs
Amiodarone Hydrochloridetablet200 mg/1oralMylan Institutional Inc.1999-11-01Not applicableUs
Amiodarone Hydrochloridetablet200 mg/1oralAmerican Health Packaging2009-09-25Not applicableUs
Amiodarone Hydrochloridetablet200 mg/1oralCardinal Health2009-09-25Not applicableUs
Amiodarone Hydrochlorideinjection, solution50 mg/mLintravenousWest ward Pharmaceutical Corp2008-02-25Not applicableUs
Amiodarone Hydrochloridetablet100 mg/1oralTaro Pharmaceuticals U.S.A., Inc.2001-03-30Not applicableUs
Amiodarone Hydrochlorideinjection, solution50 mg/mLintravenousHospira, Inc.2013-11-25Not applicableUs
Amiodarone Hydrochlorideinjection, solution50 mg/mLintravenousREMEDYREPACK INC.2015-08-19Not applicableUs
Amiodarone Hydrochlorideinjection, solution50 mg/mLintravenousGeneral Injectables & Vaccines, Inc2012-06-06Not applicableUs
Apo-amiodarone Tabletstablet200 mgoralApotex Inc2003-09-05Not applicableCanada
Paceronetablet200 mg/1oralAphena Pharma Solutions Tennessee, Llc2011-01-19Not applicableUs
Paceronetablet200 mg/1oralPhysicians Total Care, Inc.2008-10-22Not applicableUs
Paceronetablet200 mg/1oralUpsher Smith Laboratories, Inc.2011-01-19Not applicableUs
Paceronetablet400 mg/1oralUpsher Smith Laboratories, Inc.2000-06-30Not applicableUs
Paceronetablet200 mg/1oralRx Pak Division Of Mc Kesson Corporation2014-04-28Not applicableUs
Paceronetablet100 mg/1oralUpsher Smith Laboratories, Inc.2011-01-19Not applicableUs
Paceronetablet200 mg/1oralCardinal Health2011-01-19Not applicableUs
Paceronetablet200 mg/1oralAvera Mc Kennan Hospital2015-09-02Not applicableUs
Approved Over the Counter ProductsNot Available
Unapproved/Other Products
NameDosageStrengthRouteLabellerMarketing StartMarketing End
Amiodarone HClinjection, solution1.8 mg/mLintravenousCantrell Drug Company2011-08-01Not applicableUs
International Brands
NameCompany
Amio-Aqueous IVNot Available
AratacNot Available
ArycorNot Available
AtlansilNot Available
TachyraNot Available
Brand mixturesNot Available
Salts
Name/CASStructureProperties
Amiodarone Hydrochloride
Thumb
  • InChI Key: ITPDYQOUSLNIHG-UHFFFAOYSA-N
  • Monoisotopic Mass: 681.000358378
  • Average Mass: 681.773
DBSALT000355
Categories
UNIIN3RQ532IUT
CAS number1951-25-3
WeightAverage: 645.3116
Monoisotopic: 645.023680639
Chemical FormulaC25H29I2NO3
InChI KeyInChIKey=IYIKLHRQXLHMJQ-UHFFFAOYSA-N
InChI
InChI=1S/C25H29I2NO3/c1-4-7-11-22-23(18-10-8-9-12-21(18)31-22)24(29)17-15-19(26)25(20(27)16-17)30-14-13-28(5-2)6-3/h8-10,12,15-16H,4-7,11,13-14H2,1-3H3
IUPAC Name
{2-[4-(2-butyl-1-benzofuran-3-carbonyl)-2,6-diiodophenoxy]ethyl}diethylamine
SMILES
CCCCC1=C(C(=O)C2=CC(I)=C(OCCN(CC)CC)C(I)=C2)C2=CC=CC=C2O1
Taxonomy
DescriptionThis compound belongs to the class of organic compounds known as benzofurans. These are organic compounds containing a benzene ring fused to a furan. Furan is a five-membered aromatic ring with four carbon atoms and one oxygen atom.
KingdomOrganic compounds
Super ClassOrganoheterocyclic compounds
ClassBenzofurans
Sub ClassNot Available
Direct ParentBenzofurans
Alternative Parents
Substituents
  • Benzofuran
  • Acetophenone
  • Aryl ketone
  • 3-aroylfuran
  • Phenol ether
  • Benzoyl
  • Iodobenzene
  • Halobenzene
  • Alkyl aryl ether
  • Benzenoid
  • Monocyclic benzene moiety
  • Aryl iodide
  • Aryl halide
  • Heteroaromatic compound
  • Furan
  • Tertiary aliphatic amine
  • Tertiary amine
  • Ketone
  • Oxacycle
  • Ether
  • Hydrocarbon derivative
  • Organooxygen compound
  • Organonitrogen compound
  • Organoiodide
  • Organohalogen compound
  • Amine
  • Aromatic heteropolycyclic compound
Molecular FrameworkAromatic heteropolycyclic compounds
External Descriptors
Pharmacology
IndicationIntravenously, for initiation of treatment and prophylaxis of frequently recurring ventricular fibrillation and hemodynamically unstable ventricular tachycardia in patients refractory to other therapy. Orally, for the treatment of life-threatening recurrent ventricular arrhythmias such as recurrent ventricular fibrillation and recurrent hemodynamically unstable ventricular tachycardia.
PharmacodynamicsAmiodarone belongs to a class of drugs called Vaughan-Williams Class III antiarrhythmic agents. It is used in the treatment of a wide range of cardiac tachyarhthmias, including both ventricular and supraventricular (atrial) arrhythmias. After intravenous administration in man, amiodarone relaxes vascular smooth muscle, reduces peripheral vascular resistance (afterload), and slightly increases cardiac index. Amiodarone prolongs phase 3 of the cardiac action potential. It has numerous other effects however, including actions that are similar to those of antiarrhythmic classes Ia, II, and IV. Amiodarone shows beta blocker-like and calcium channel blocker-like actions on the SA and AV nodes, increases the refractory period via sodium- and potassium-channel effects, and slows intra-cardiac conduction of the cardiac action potential, via sodium-channel effects.
Mechanism of actionThe antiarrhythmic effect of amiodarone may be due to at least two major actions. It prolongs the myocardial cell-action potential (phase 3) duration and refractory period and acts as a noncompetitive a- and b-adrenergic inhibitor.
Related Articles
AbsorptionSlow and variable (about 20 to 55% of an oral dose is absorbed).
Volume of distributionNot Available
Protein binding>96%
Metabolism

Amiodarone is extensively metabolized in the liver via CYP2C8 (under 1% unchanged in urine), and can effect the metabolism of numerous other drugs. The major metabolite of amiodarone is desethylamiodarone (DEA), which also has antiarrhythmic properties. The metabolism of amiodarone is inhibited by grapefruit juice, leading to elevated serum levels of amiodarone.

SubstrateEnzymesProduct
Amiodarone
N-desethylamiodaroneDetails
Route of eliminationAmiodarone is eliminated primarily by hepatic metabolism and biliary excretion and there is negligible excretion of amiodarone or DEA in urine.
Half life58 days (range 15-142 days)
Clearance
  • 90-158 mL/h/kg [Healthy with a single dose IV (5 mg/kg over 15 min)]
  • 100 mL/h/kg [Normal subjects > 65 yrs]
  • 150 mL/h/kg [younger subjects]
  • 220 and 440 mL/h/kg [patients with VT and VF]
ToxicityIntravenous, mouse: LD50 = 178 mg/kg. Some side effects have a significant mortality rate: specifically, hepatitis, exacerbation of asthma and congestive failure, and pneumonitis.
Affected organisms
  • Humans and other mammals
Pathways
PathwayCategorySMPDB ID
Amiodarone Action PathwayDrug actionSMP00665
SNP Mediated EffectsNot Available
SNP Mediated Adverse Drug Reactions
Interacting Gene/EnzymeSNP RS IDAllele nameDefining changeAdverse ReactionReference(s)
Potassium voltage-gated channel subfamily H member 2
Gene symbol: KCNH2
UniProt: Q12809
Not AvailableMiRP1KCNE2Channels formed with mutant MiRP1 subunits and HERG showed slower activation, faster deactivation, and increased drug sensitivity and is associated with cardiac arrhythmia.10219239
ADMET
Predicted ADMET features
PropertyValueProbability
Human Intestinal Absorption+1.0
Blood Brain Barrier+0.8615
Caco-2 permeable+0.66
P-glycoprotein substrateSubstrate0.8044
P-glycoprotein inhibitor IInhibitor0.8563
P-glycoprotein inhibitor IIInhibitor0.8388
Renal organic cation transporterInhibitor0.5099
CYP450 2C9 substrateNon-substrate0.7959
CYP450 2D6 substrateSubstrate0.8918
CYP450 3A4 substrateSubstrate0.7188
CYP450 1A2 substrateInhibitor0.9106
CYP450 2C9 inhibitorInhibitor0.8948
CYP450 2D6 inhibitorInhibitor0.8931
CYP450 2C19 inhibitorNon-inhibitor0.9025
CYP450 3A4 inhibitorNon-inhibitor0.8309
CYP450 inhibitory promiscuityHigh CYP Inhibitory Promiscuity0.8615
Ames testNon AMES toxic0.5661
CarcinogenicityNon-carcinogens0.7696
BiodegradationNot ready biodegradable1.0
Rat acute toxicity2.6539 LD50, mol/kg Not applicable
hERG inhibition (predictor I)Strong inhibitor0.5932
hERG inhibition (predictor II)Inhibitor0.7638
ADMET data is predicted using admetSAR, a free tool for evaluating chemical ADMET properties. (23092397 )
Pharmacoeconomics
ManufacturersNot Available
Packagers
Dosage forms
FormRouteStrength
Injectionintravenous50 mg/mL
Injection, solutionintravenous50 mg/mL
Injection, solution, concentrateintravenous50 mg/mL
Tabletoral300 mg/1
Liquidintravenous50 mg
Solutionintravenous50 mg
Tabletoral200 mg/1
Tabletoral200 mg
Injection, solutionintravenous1.5 mg/mL
Injection, solutionintravenous1.8 mg/mL
Tabletoral100 mg/1
Tabletoral400 mg/1
Tabletoral100 mg
Prices
Unit descriptionCostUnit
Amiodarone hcl powder38.98USD g
Pacerone 100 mg tablet7.58USD tablet
Pacerone 400 mg tablet7.43USD tablet
Amiodarone hcl 400 mg tablet6.32USD tablet
Cordarone 200 mg tablet4.78USD tablet
Pacerone 200 mg tablet3.53USD tablet
Amiodarone hcl 200 mg tablet3.37USD tablet
Cordarone 200 mg Tablet2.32USD tablet
Apo-Amiodarone 200 mg Tablet1.3USD tablet
Mylan-Amiodarone 200 mg Tablet1.3USD tablet
Novo-Amiodarone 200 mg Tablet1.3USD tablet
Pms-Amiodarone 200 mg Tablet1.3USD tablet
Ratio-Amiodarone 200 mg Tablet1.3USD tablet
Sandoz Amiodarone 200 mg Tablet1.3USD tablet
Amiodarone 150 mg/3 ml vial0.83USD ml
Pms-Amiodarone 100 mg Tablet0.72USD tablet
Amiodarone 900 mg/18 ml vial0.59USD ml
Amiodarone 450 mg/9 ml vial0.57USD ml
DrugBank does not sell nor buy drugs. Pricing information is supplied for informational purposes only.
Patents
Patent NumberPediatric ExtensionApprovedExpires (estimated)
US5134127 No1993-01-232010-01-23Us
US6869939 No2002-05-042022-05-04Us
US7635773 No2009-03-132029-03-13Us
Properties
StateSolid
Experimental Properties
PropertyValueSource
melting point156Tondeur, R. and Binon, F.; U.S. Patent 3,248,401; April 26,1966; assigned to Societe Beige de I'Azote et des Produits Chimiques du Marly, SA, Belgium.
water solubilityLowNot Available
logP7.57AVDEEF,A (1997)
Predicted Properties
PropertyValueSource
Water Solubility0.00476 mg/mLALOGPS
logP7.24ALOGPS
logP7.64ChemAxon
logS-5.1ALOGPS
pKa (Strongest Basic)8.47ChemAxon
Physiological Charge1ChemAxon
Hydrogen Acceptor Count3ChemAxon
Hydrogen Donor Count0ChemAxon
Polar Surface Area42.68 Å2ChemAxon
Rotatable Bond Count11ChemAxon
Refractivity145.05 m3·mol-1ChemAxon
Polarizability56.78 Å3ChemAxon
Number of Rings3ChemAxon
Bioavailability0ChemAxon
Rule of FiveYesChemAxon
Ghose FilterYesChemAxon
Veber's RuleYesChemAxon
MDDR-like RuleYesChemAxon
Spectra
Mass Spec (NIST)Not Available
SpectraNot Available
References
Synthesis Reference

DrugSyn.org

US3248401
General References
  1. DELTOUR G, BINON F, TONDEUR R, GOLDENBERG C, HENAUX F, SION R, DERAY E, CHARLIER R: [Studies in the benzofuran series. VI. Coronary-dilating activity of alkylated and aminoalkylated derivatives of 3-benzoylbenzofuran]. Arch Int Pharmacodyn Ther. 1962 Sep 1;139:247-54. [PubMed:14026835 ]
  2. CHARLIER R, DELTOUR G, TONDEUR R, BINON F: [Studies in the benzofuran series. VII. Preliminary pharmacological study of 2-butyl-3-(3,5-diiodo-4-beta-N-diethylaminoethoxybenzoyl)-benzofuran]. Arch Int Pharmacodyn Ther. 1962 Sep 1;139:255-64. [PubMed:14020244 ]
  3. Singh BN, Vaughan Williams EM: The effect of amiodarone, a new anti-anginal drug, on cardiac muscle. Br J Pharmacol. 1970 Aug;39(4):657-67. [PubMed:5485142 ]
  4. Rosenbaum MB, Chiale PA, Halpern MS, Nau GJ, Przybylski J, Levi RJ, Lazzari JO, Elizari MV: Clinical efficacy of amiodarone as an antiarrhythmic agent. Am J Cardiol. 1976 Dec;38(7):934-44. [PubMed:793369 ]
  5. Rosenbaum MB, Chiale PA, Haedo A, Lazzari JO, Elizari MV: Ten years of experience with amiodarone. Am Heart J. 1983 Oct;106(4 Pt 2):957-64. [PubMed:6613843 ]
External Links
ATC CodesC01BD01
AHFS Codes
  • 24:04.04.20
PDB EntriesNot Available
FDA labelDownload (545 KB)
MSDSDownload (51.8 KB)
Interactions
Drug Interactions
Drug
AbirateroneThe serum concentration of Amiodarone can be increased when it is combined with Abiraterone.
AcebutololAmiodarone may increase the bradycardic activities of Acebutolol.
AcenocoumarolAmiodarone may increase the anticoagulant activities of Acenocoumarol.
AfatinibThe serum concentration of Afatinib can be increased when it is combined with Amiodarone.
Agalsidase betaThe therapeutic efficacy of Agalsidase beta can be decreased when used in combination with Amiodarone.
AprepitantThe serum concentration of Amiodarone can be increased when it is combined with Aprepitant.
ArtesunateThe serum concentration of the active metabolites of Artesunate can be reduced when Artesunate is used in combination with Amiodarone resulting in a loss in efficacy.
AtazanavirThe serum concentration of Amiodarone can be increased when it is combined with Atazanavir.
AtenololAmiodarone may increase the bradycardic activities of Atenolol.
AtorvastatinThe metabolism of Atorvastatin can be decreased when combined with Amiodarone.
AzithromycinAzithromycin may increase the QTc-prolonging activities of Amiodarone.
BepridilBepridil may increase the bradycardic activities of Amiodarone.
BetaxololAmiodarone may increase the bradycardic activities of Betaxolol.
BexaroteneThe serum concentration of Amiodarone can be decreased when it is combined with Bexarotene.
BisoprololAmiodarone may increase the bradycardic activities of Bisoprolol.
BoceprevirThe serum concentration of Amiodarone can be increased when it is combined with Boceprevir.
BosentanThe serum concentration of Amiodarone can be decreased when it is combined with Bosentan.
BosutinibThe serum concentration of Bosutinib can be increased when it is combined with Amiodarone.
Brentuximab vedotinThe serum concentration of Brentuximab vedotin can be increased when it is combined with Amiodarone.
BretyliumBretylium may increase the bradycardic activities of Amiodarone.
BrexpiprazoleThe serum concentration of Brexpiprazole can be increased when it is combined with Amiodarone.
CarteololAmiodarone may increase the bradycardic activities of Carteolol.
CarvedilolThe serum concentration of Carvedilol can be increased when it is combined with Amiodarone.
CeritinibAmiodarone may increase the bradycardic activities of Ceritinib.
CholestyramineThe bioavailability of Amiodarone can be decreased when combined with Cholestyramine.
CimetidineThe serum concentration of Amiodarone can be increased when it is combined with Cimetidine.
CitalopramCitalopram may increase the QTc-prolonging activities of Amiodarone.
ClopidogrelThe serum concentration of the active metabolites of Clopidogrel can be reduced when Clopidogrel is used in combination with Amiodarone resulting in a loss in efficacy.
CobicistatThe serum concentration of Amiodarone can be increased when it is combined with Cobicistat.
CodeineThe therapeutic efficacy of Codeine can be decreased when used in combination with Amiodarone.
ColchicineThe serum concentration of Colchicine can be increased when it is combined with Amiodarone.
ColesevelamThe bioavailability of Amiodarone can be decreased when combined with Colesevelam.
ColestipolThe bioavailability of Amiodarone can be decreased when combined with Colestipol.
ConivaptanThe serum concentration of Amiodarone can be increased when it is combined with Conivaptan.
CyclophosphamideThe risk or severity of adverse effects can be increased when Cyclophosphamide is combined with Amiodarone.
CyclosporineThe metabolism of Cyclosporine can be decreased when combined with Amiodarone.
Dabigatran etexilateThe serum concentration of Dabigatran etexilate can be increased when it is combined with Amiodarone.
DabrafenibThe serum concentration of Amiodarone can be decreased when it is combined with Dabrafenib.
DaclatasvirDaclatasvir may increase the bradycardic activities of Amiodarone.
DarunavirThe serum concentration of Amiodarone can be increased when it is combined with Darunavir.
DeferasiroxThe serum concentration of Amiodarone can be decreased when it is combined with Deferasirox.
DicoumarolAmiodarone may increase the anticoagulant activities of Dicoumarol.
DigoxinThe serum concentration of Digoxin can be increased when it is combined with Amiodarone.
DiltiazemDiltiazem may increase the bradycardic activities of Amiodarone.
DisopyramideAmiodarone may increase the QTc-prolonging activities of Disopyramide.
DofetilideDofetilide may increase the QTc-prolonging activities of Amiodarone.
DoxorubicinThe serum concentration of Doxorubicin can be increased when it is combined with Amiodarone.
DronabinolThe serum concentration of Dronabinol can be increased when it is combined with Amiodarone.
EdoxabanThe serum concentration of Edoxaban can be increased when it is combined with Amiodarone.
EsmololAmiodarone may increase the bradycardic activities of Esmolol.
EtravirineThe serum concentration of Amiodarone can be decreased when it is combined with Etravirine.
EverolimusThe serum concentration of Everolimus can be increased when it is combined with Amiodarone.
FesoterodineThe serum concentration of the active metabolites of Fesoterodine can be increased when Fesoterodine is used in combination with Amiodarone.
FingolimodFingolimod may increase the arrhythmogenic activities of Amiodarone.
FlecainideAmiodarone may increase the QTc-prolonging activities of Flecainide.
FlibanserinThe serum concentration of Flibanserin can be increased when it is combined with Amiodarone.
FluconazoleThe metabolism of Amiodarone can be decreased when combined with Fluconazole.
FluvastatinThe metabolism of Fluvastatin can be decreased when combined with Amiodarone.
FluvoxamineThe metabolism of Fluvoxamine can be decreased when combined with Amiodarone.
FosamprenavirThe serum concentration of Amiodarone can be increased when it is combined with Fosamprenavir.
FosaprepitantThe serum concentration of Amiodarone can be increased when it is combined with Fosaprepitant.
FosphenytoinFosphenytoin may increase the QTc-prolonging activities of Amiodarone.
Fusidic AcidThe serum concentration of Amiodarone can be increased when it is combined with Fusidic Acid.
GoserelinGoserelin may increase the QTc-prolonging activities of Amiodarone.
HydrocodoneThe serum concentration of Hydrocodone can be increased when it is combined with Amiodarone.
IdelalisibThe serum concentration of Amiodarone can be increased when it is combined with Idelalisib.
IndinavirThe serum concentration of Amiodarone can be increased when it is combined with Indinavir.
IvabradineIvabradine may increase the QTc-prolonging activities of Amiodarone.
IvacaftorThe serum concentration of Amiodarone can be increased when it is combined with Ivacaftor.
LabetalolAmiodarone may increase the bradycardic activities of Labetalol.
LacosamideAmiodarone may increase the atrioventricular blocking (AV block) activities of Lacosamide.
LedipasvirThe serum concentration of Ledipasvir can be increased when it is combined with Amiodarone.
LeuprolideLeuprolide may increase the QTc-prolonging activities of Amiodarone.
LidocaineThe serum concentration of Lidocaine can be increased when it is combined with Amiodarone.
LomitapideThe serum concentration of Lomitapide can be increased when it is combined with Amiodarone.
LopinavirLopinavir may increase the QTc-prolonging activities of Amiodarone.
LoratadineThe serum concentration of Loratadine can be increased when it is combined with Amiodarone.
LovastatinThe metabolism of Lovastatin can be decreased when combined with Amiodarone.
LuliconazoleThe serum concentration of Amiodarone can be increased when it is combined with Luliconazole.
MetoprololThe serum concentration of Metoprolol can be increased when it is combined with Amiodarone.
MifepristoneMifepristone may increase the QTc-prolonging activities of Amiodarone.
MipomersenAmiodarone may increase the hepatotoxic activities of Mipomersen.
MitotaneThe serum concentration of Amiodarone can be decreased when it is combined with Mitotane.
NadololAmiodarone may increase the bradycardic activities of Nadolol.
NaloxegolThe serum concentration of Naloxegol can be increased when it is combined with Amiodarone.
NebivololThe serum concentration of Nebivolol can be increased when it is combined with Amiodarone.
NelfinavirThe serum concentration of Amiodarone can be increased when it is combined with Nelfinavir.
NetupitantThe serum concentration of Amiodarone can be increased when it is combined with Netupitant.
NicotineThe metabolism of Nicotine can be decreased when combined with Amiodarone.
NimodipineThe serum concentration of Nimodipine can be increased when it is combined with Amiodarone.
OctreotideOctreotide may increase the bradycardic activities of Amiodarone.
OrlistatOrlistat can cause a decrease in the absorption of Amiodarone resulting in a reduced serum concentration and potentially a decrease in efficacy.
PalbociclibThe serum concentration of Amiodarone can be increased when it is combined with Palbociclib.
PazopanibThe serum concentration of Pazopanib can be increased when it is combined with Amiodarone.
PenbutololAmiodarone may increase the bradycardic activities of Penbutolol.
PhenytoinThe serum concentration of Amiodarone can be decreased when it is combined with Phenytoin.
PimozideThe serum concentration of Pimozide can be increased when it is combined with Amiodarone.
PindololAmiodarone may increase the bradycardic activities of Pindolol.
PorfimerAmiodarone may increase the photosensitizing activities of Porfimer.
ProcainamideAmiodarone may increase the QTc-prolonging activities of Procainamide.
PropafenoneThe risk or severity of adverse effects can be increased when Amiodarone is combined with Propafenone.
PropranololAmiodarone may increase the bradycardic activities of Propranolol.
PrucaloprideThe serum concentration of Prucalopride can be increased when it is combined with Amiodarone.
QuinidineAmiodarone may increase the QTc-prolonging activities of Quinidine.
RifampicinThe serum concentration of the active metabolites of Amiodarone can be reduced when Amiodarone is used in combination with Rifampicin resulting in a loss in efficacy.
RifaximinThe serum concentration of Rifaximin can be increased when it is combined with Amiodarone.
RitonavirThe serum concentration of Amiodarone can be increased when it is combined with Ritonavir.
RosiglitazoneThe metabolism of Amiodarone can be decreased when combined with Rosiglitazone.
RosuvastatinThe metabolism of Rosuvastatin can be decreased when combined with Amiodarone.
RuxolitinibRuxolitinib may increase the bradycardic activities of Amiodarone.
SaquinavirSaquinavir may increase the QTc-prolonging activities of Amiodarone.
SildenafilThe metabolism of Sildenafil can be decreased when combined with Amiodarone.
SilodosinThe serum concentration of Silodosin can be increased when it is combined with Amiodarone.
SiltuximabThe serum concentration of Amiodarone can be decreased when it is combined with Siltuximab.
SimeprevirThe serum concentration of Amiodarone can be increased when it is combined with Simeprevir.
SimvastatinThe metabolism of Simvastatin can be decreased when combined with Amiodarone.
Sodium Iodide I-131The therapeutic efficacy of Sodium Iodide I-131 can be decreased when used in combination with Amiodarone.
SofosbuvirSofosbuvir may increase the bradycardic activities of Amiodarone.
St. John's WortThe serum concentration of Amiodarone can be decreased when it is combined with St. John's Wort.
StiripentolThe serum concentration of Amiodarone can be increased when it is combined with Stiripentol.
TamoxifenThe serum concentration of the active metabolites of Tamoxifen can be reduced when Tamoxifen is used in combination with Amiodarone resulting in a loss in efficacy.
TegafurThe serum concentration of the active metabolites of Tegafur can be reduced when Tegafur is used in combination with Amiodarone resulting in a loss in efficacy.
TelaprevirThe risk or severity of adverse effects can be increased when Telaprevir is combined with Amiodarone.
TesmilifeneThe serum concentration of Amiodarone can be decreased when it is combined with Tesmilifene.
ThioridazineThe serum concentration of Thioridazine can be increased when it is combined with Amiodarone.
TimololAmiodarone may increase the bradycardic activities of Timolol.
TipranavirThe serum concentration of Amiodarone can be increased when it is combined with Tipranavir.
TizanidineThe serum concentration of Tizanidine can be increased when it is combined with Amiodarone.
TocilizumabThe serum concentration of Amiodarone can be decreased when it is combined with Tocilizumab.
TofacitinibTofacitinib may increase the bradycardic activities of Amiodarone.
TopotecanThe serum concentration of Topotecan can be increased when it is combined with Amiodarone.
TramadolThe therapeutic efficacy of Tramadol can be decreased when used in combination with Amiodarone.
TrimethoprimThe metabolism of Amiodarone can be decreased when combined with Trimethoprim.
VerapamilThe serum concentration of Amiodarone can be increased when it is combined with Verapamil.
VerteporfinAmiodarone may increase the photosensitizing activities of Verteporfin.
VincristineThe serum concentration of Vincristine can be increased when it is combined with Amiodarone.
WarfarinAmiodarone may increase the anticoagulant activities of Warfarin.
Food Interactions
  • Grapefruit and grapefruit juice should be avoided throughout treatment.
  • Grapefruit can significantly increase serum levels of this product.
  • Take without regard to meals.

Targets

Kind
Protein
Organism
Human
Pharmacological action
yes
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. Chen X, Ji ZL, Chen YZ: TTD: Therapeutic Target Database. Nucleic Acids Res. 2002 Jan 1;30(1):412-5. [PubMed:11752352 ]
  2. Wang SP, Wang JA, Luo RH, Cui WY, Wang H: Potassium channel currents in rat mesenchymal stem cells and their possible roles in cell proliferation. Clin Exp Pharmacol Physiol. 2008 Sep;35(9):1077-84. doi: 10.1111/j.1440-1681.2008.04964.x. Epub 2008 May 25. [PubMed:18505444 ]
  3. Varro A, Biliczki P, Iost N, Virag L, Hala O, Kovacs P, Matyus P, Papp JG: Theoretical possibilities for the development of novel antiarrhythmic drugs. Curr Med Chem. 2004 Jan;11(1):1-11. [PubMed:14754422 ]
  4. Waldhauser KM, Brecht K, Hebeisen S, Ha HR, Konrad D, Bur D, Krahenbuhl S: Interaction with the hERG channel and cytotoxicity of amiodarone and amiodarone analogues. Br J Pharmacol. 2008 Oct;155(4):585-95. doi: 10.1038/bjp.2008.287. Epub 2008 Jul 7. [PubMed:18604229 ]
Kind
Protein
Organism
Human
Pharmacological action
yes
Actions
antagonist
General Function:
Receptor signaling protein activity
Specific Function:
Beta-adrenergic receptors mediate the catecholamine-induced activation of adenylate cyclase through the action of G proteins. This receptor binds epinephrine and norepinephrine with approximately equal affinity. Mediates Ras activation through G(s)-alpha- and cAMP-mediated signaling.
Gene Name:
ADRB1
Uniprot ID:
P08588
Molecular Weight:
51322.1 Da
References
  1. Doggrell SA, Brown L: Present and future pharmacotherapy for heart failure. Expert Opin Pharmacother. 2002 Jul;3(7):915-30. [PubMed:12083991 ]
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-1H gives rise to T-type calcium currents. T-type calcium channels belong to the "low-v...
Gene Name:
CACNA1H
Uniprot ID:
O95180
Molecular Weight:
259160.2 Da
References
  1. Cohen CJ, Spires S, Van Skiver D: Block of T-type Ca channels in guinea pig atrial cells by antiarrhythmic agents and Ca channel antagonists. J Gen Physiol. 1992 Oct;100(4):703-28. [PubMed:1281221 ]
  2. Lewalter T, Pittrow D, Goette A, Kirch W, Hohnloser S: [Clinical pharmacology and electrophysiological properties of dronedarone]. Dtsch Med Wochenschr. 2010 Mar;135 Suppl 2:S43-7. doi: 10.1055/s-0030-1249208. Epub 2010 Mar 10. [PubMed:20221978 ]
Kind
Protein
Organism
Human
Pharmacological action
yes
Actions
inhibitor
General Function:
Voltage-gated calcium channel activity
Specific Function:
The alpha-2/delta subunit of voltage-dependent calcium channels regulates calcium current density and activation/inactivation kinetics of the calcium channel. Acts as a regulatory subunit for P/Q-type calcium channel (CACNA1A), N-type (CACNA1B), L-type (CACNA1C OR CACNA1D) and possibly T-type (CACNA1G). Overexpression induces apoptosis.
Gene Name:
CACNA2D2
Uniprot ID:
Q9NY47
Molecular Weight:
129816.095 Da
References
  1. Cohen CJ, Spires S, Van Skiver D: Block of T-type Ca channels in guinea pig atrial cells by antiarrhythmic agents and Ca channel antagonists. J Gen Physiol. 1992 Oct;100(4):703-28. [PubMed:1281221 ]
  2. Lewalter T, Pittrow D, Goette A, Kirch W, Hohnloser S: [Clinical pharmacology and electrophysiological properties of dronedarone]. Dtsch Med Wochenschr. 2010 Mar;135 Suppl 2:S43-7. doi: 10.1055/s-0030-1249208. Epub 2010 Mar 10. [PubMed:20221978 ]

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. Elsherbiny ME, El-Kadi AO, Brocks DR: The metabolism of amiodarone by various CYP isoenzymes of human and rat, and the inhibitory influence of ketoconazole. J Pharm Pharm Sci. 2008;11(1):147-59. [PubMed:18445370 ]
  3. 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 ]
  4. Ohyama K, Nakajima M, Nakamura S, Shimada N, Yamazaki H, Yokoi T: A significant role of human cytochrome P450 2C8 in amiodarone N-deethylation: an approach to predict the contribution with relative activity factor. Drug Metab Dispos. 2000 Nov;28(11):1303-10. [PubMed:11038157 ]
  5. Drug Interactions: Cytochrome P450 Drug Interaction Table [Link]
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 ]
  3. Ohyama K, Nakajima M, Nakamura S, Shimada N, Yamazaki H, Yokoi T: A significant role of human cytochrome P450 2C8 in amiodarone N-deethylation: an approach to predict the contribution with relative activity factor. Drug Metab Dispos. 2000 Nov;28(11):1303-10. [PubMed:11038157 ]
  4. Website [Link]
Kind
Protein
Organism
Human
Pharmacological action
unknown
Actions
substrateinhibitor
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. 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:
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 ]
  3. Drug Interactions: Cytochrome P450 Drug Interaction Table [Link]
Kind
Protein
Organism
Human
Pharmacological action
unknown
Actions
substrateinhibitor
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. 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
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:
Vitamin d 24-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:
CYP1A1
Uniprot ID:
P04798
Molecular Weight:
58164.815 Da
References
  1. Elsherbiny ME, El-Kadi AO, Brocks DR: The metabolism of amiodarone by various CYP isoenzymes of human and rat, and the inhibitory influence of ketoconazole. J Pharm Pharm Sci. 2008;11(1):147-59. [PubMed:18445370 ]
  2. Preissner S, Kroll K, Dunkel M, Senger C, Goldsobel G, Kuzman D, Guenther S, Winnenburg R, Schroeder M, Preissner R: SuperCYP: a comprehensive database on Cytochrome P450 enzymes including a tool for analysis of CYP-drug interactions. Nucleic Acids Res. 2010 Jan;38(Database issue):D237-43. doi: 10.1093/nar/gkp970. Epub 2009 Nov 24. [PubMed:19934256 ]
Kind
Protein
Organism
Human
Pharmacological action
unknown
Actions
inhibitor
General Function:
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. 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
inhibitor
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
inhibitor
General Function:
Steroid hydroxylase activity
Specific Function:
Exhibits a high coumarin 7-hydroxylase activity. Can act in the hydroxylation of the anti-cancer drugs cyclophosphamide and ifosphamide. Competent in the metabolic activation of aflatoxin B1. Constitutes the major nicotine C-oxidase. Acts as a 1,4-cineole 2-exo-monooxygenase. Possesses low phenacetin O-deethylation activity.
Gene Name:
CYP2A6
Uniprot ID:
P11509
Molecular Weight:
56501.005 Da

Transporters

Kind
Protein
Organism
Human
Pharmacological action
unknown
Actions
inhibitorinducer
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. Schuetz EG, Beck WT, Schuetz JD: Modulators and substrates of P-glycoprotein and cytochrome P4503A coordinately up-regulate these proteins in human colon carcinoma cells. Mol Pharmacol. 1996 Feb;49(2):311-8. [PubMed:8632764 ]
  2. Katoh M, Nakajima M, Yamazaki H, Yokoi T: Inhibitory effects of CYP3A4 substrates and their metabolites on P-glycoprotein-mediated transport. Eur J Pharm Sci. 2001 Feb;12(4):505-13. [PubMed:11231118 ]
  3. Yasuda K, Lan LB, Sanglard D, Furuya K, Schuetz JD, Schuetz EG: Interaction of cytochrome P450 3A inhibitors with P-glycoprotein. J Pharmacol Exp Ther. 2002 Oct;303(1):323-32. [PubMed:12235267 ]
  4. Tiberghien F, Loor F: Ranking of P-glycoprotein substrates and inhibitors by a calcein-AM fluorometry screening assay. Anticancer Drugs. 1996 Jul;7(5):568-78. [PubMed:8862725 ]
  5. Kim RB, Wandel C, Leake B, Cvetkovic M, Fromm MF, Dempsey PJ, Roden MM, Belas F, Chaudhary AK, Roden DM, Wood AJ, Wilkinson GR: Interrelationship between substrates and inhibitors of human CYP3A and P-glycoprotein. Pharm Res. 1999 Mar;16(3):408-14. [PubMed:10213372 ]
Comments
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Drug created on June 13, 2005 07:24 / Updated on July 29, 2016 01:53