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Identification
NameFelodipine
Accession NumberDB01023  (APRD00374)
TypeSmall Molecule
GroupsApproved, Investigational
Description

Felodipine is a long-acting 1,4-dihydropyridine calcium channel blocker (CCB)b. It acts primarily on vascular smooth muscle cells by stabilizing voltage-gated L-type calcium channels in their inactive conformation. By inhibiting the influx of calcium in smooth muscle cells, felodipine prevents calcium-dependent myocyte contraction and vasoconstriction. Felodipine is the most potent CCB in use and is unique in that it exhibits fluorescent activity. In addition to binding to L-type calcium channels, felodipine binds to a number of calcium-binding proteins, exhibits competitive antagonism of the mineralcorticoid receptor, inhibits the activity of calmodulin-dependent cyclic nucleotide phosphodiesterase, and blocks calcium influx through voltage-gated T-type calcium channels. Felodipine is used to treat mild to moderate essential hypertension.

Structure
Thumb
Synonyms
SynonymLanguageCode
(+-)-Ethyl methyl 4-(2,3-dichlorophenyl)-1,4-dihydro-2,6-dimethyl-3,5-pyridinedicarboxylateNot AvailableNot Available
3-Ethyl 5-methyl 4-(2,3-dichlorophenyl)-2,6-dimethyl-1,4-dihydro-3,5-pyridinedicarboxylateNot AvailableNot Available
4-(2,3-Dichlorophenyl)-1,4-dihydro-2,6-dimethyl-3,5-pyridinedicarboxylic acid ethyl methyl esterNot AvailableNot Available
FelodipinaSpanishINN
FelodipineNot AvailableINN, BAN, USAN
FelodipinumLatinINN
Prescription Products
NameDosageStrengthRouteLabellerMarketing StartMarketing End
Plendiltablet, extended release2.5 mgoralAstra Zeneca Lp1994-10-04Not AvailableUs 0a2ef1ad1c84951dc1392a8bbe1f3cb241c91ed59e44ad8268635315440d978c
Plendiltablet, extended release5 mgoralAstra Zeneca Lp1991-09-16Not AvailableUs 0a2ef1ad1c84951dc1392a8bbe1f3cb241c91ed59e44ad8268635315440d978c
Plendiltablet, extended release10 mgoralAstra Zeneca Lp1991-09-16Not AvailableUs 0a2ef1ad1c84951dc1392a8bbe1f3cb241c91ed59e44ad8268635315440d978c
Felodipineextended-release Tabletstablet, extended release2.5 mgoralRanbaxy Pharmaceuticals Inc2008-09-10Not AvailableUs 0a2ef1ad1c84951dc1392a8bbe1f3cb241c91ed59e44ad8268635315440d978c
Felodipineextended-release Tabletstablet, extended release5 mgoralRanbaxy Pharmaceuticals Inc2008-09-10Not AvailableUs 0a2ef1ad1c84951dc1392a8bbe1f3cb241c91ed59e44ad8268635315440d978c
Felodipineextended-release Tabletstablet, extended release10 mgoralRanbaxy Pharmaceuticals Inc2008-09-10Not AvailableUs 0a2ef1ad1c84951dc1392a8bbe1f3cb241c91ed59e44ad8268635315440d978c
Plendiltablet, extended release10 mgoralbryant ranch prepack1991-09-16Not AvailableUs 0a2ef1ad1c84951dc1392a8bbe1f3cb241c91ed59e44ad8268635315440d978c
Generic Prescription Products
NameDosageStrengthRouteLabellerMarketing StartMarketing End
Felodipinetablet, film coated, extended release2.5 mgoralMylan Pharmaceuticals Inc.2013-03-28Not AvailableUs 0a2ef1ad1c84951dc1392a8bbe1f3cb241c91ed59e44ad8268635315440d978c
Felodipinetablet, film coated, extended release5 mgoralMylan Pharmaceuticals Inc.2013-03-28Not AvailableUs 0a2ef1ad1c84951dc1392a8bbe1f3cb241c91ed59e44ad8268635315440d978c
Felodipinetablet, film coated, extended release10 mgoralMylan Pharmaceuticals Inc.2013-03-28Not AvailableUs 0a2ef1ad1c84951dc1392a8bbe1f3cb241c91ed59e44ad8268635315440d978c
Felodipinetablet, extended release2.5 mgoralQualitest Pharmaceuticals2009-03-31Not AvailableUs 0a2ef1ad1c84951dc1392a8bbe1f3cb241c91ed59e44ad8268635315440d978c
Felodipinetablet, extended release5 mgoralQualitest Pharmaceuticals2011-12-15Not AvailableUs 0a2ef1ad1c84951dc1392a8bbe1f3cb241c91ed59e44ad8268635315440d978c
Felodipinetablet, film coated, extended release10 mgoralQualitest Pharmaceuticals2011-12-15Not AvailableUs 0a2ef1ad1c84951dc1392a8bbe1f3cb241c91ed59e44ad8268635315440d978c
Felodipinetablet, film coated, extended release10 mgoralNcs Health Care Of Ky, Inc Dba Vangard Labs2009-11-16Not AvailableUs 0a2ef1ad1c84951dc1392a8bbe1f3cb241c91ed59e44ad8268635315440d978c
Felodipinetablet, film coated, extended release5 mgoralNcs Health Care Of Ky, Inc Dba Vangard Labs2009-11-16Not AvailableUs 0a2ef1ad1c84951dc1392a8bbe1f3cb241c91ed59e44ad8268635315440d978c
Felodipinetablet, extended release2.5 mgoralTorrent Pharmaceuticals Limited2011-11-28Not AvailableUs 0a2ef1ad1c84951dc1392a8bbe1f3cb241c91ed59e44ad8268635315440d978c
Felodipinetablet, extended release5 mgoralTorrent Pharmaceuticals Limited2011-11-28Not AvailableUs 0a2ef1ad1c84951dc1392a8bbe1f3cb241c91ed59e44ad8268635315440d978c
Felodipinetablet, extended release10 mgoralTorrent Pharmaceuticals Limited2011-11-28Not AvailableUs 0a2ef1ad1c84951dc1392a8bbe1f3cb241c91ed59e44ad8268635315440d978c
Felodipinetablet, extended release2.5 mgoralHeritage Pharmaceuticals Inc.2013-11-08Not AvailableUs 0a2ef1ad1c84951dc1392a8bbe1f3cb241c91ed59e44ad8268635315440d978c
Felodipinetablet, extended release5 mgoralHeritage Pharmaceuticals Inc.2013-11-08Not AvailableUs 0a2ef1ad1c84951dc1392a8bbe1f3cb241c91ed59e44ad8268635315440d978c
Felodipinetablet, extended release10 mgoralHeritage Pharmaceuticals Inc.2013-11-08Not AvailableUs 0a2ef1ad1c84951dc1392a8bbe1f3cb241c91ed59e44ad8268635315440d978c
Felodipinetablet, film coated, extended release2.5 mgoralAv Kare, Inc.2014-03-31Not AvailableUs 0a2ef1ad1c84951dc1392a8bbe1f3cb241c91ed59e44ad8268635315440d978c
Felodipinetablet, film coated, extended release5 mgoralAv Kare, Inc.2014-03-31Not AvailableUs 0a2ef1ad1c84951dc1392a8bbe1f3cb241c91ed59e44ad8268635315440d978c
Felodipinetablet, film coated, extended release10 mgoralAv Kare, Inc.2014-03-31Not AvailableUs 0a2ef1ad1c84951dc1392a8bbe1f3cb241c91ed59e44ad8268635315440d978c
Felodipinetablet, extended release5 mgoralREMEDYREPACK INC.2011-04-20Not AvailableUs 0a2ef1ad1c84951dc1392a8bbe1f3cb241c91ed59e44ad8268635315440d978c
Felodipinetablet, film coated, extended release5 mgoralMylan Institutional Inc.2008-05-01Not AvailableUs 0a2ef1ad1c84951dc1392a8bbe1f3cb241c91ed59e44ad8268635315440d978c
Felodipinetablet, film coated, extended release10 mgoralMylan Institutional Inc.2008-05-01Not AvailableUs 0a2ef1ad1c84951dc1392a8bbe1f3cb241c91ed59e44ad8268635315440d978c
Felodipinetablet, film coated, extended release2.5 mgoralMutual Pharmaceutical Company, Inc.2004-11-02Not AvailableUs 0a2ef1ad1c84951dc1392a8bbe1f3cb241c91ed59e44ad8268635315440d978c
Felodipinetablet, film coated, extended release5 mgoralMutual Pharmaceutical Company, Inc.2004-11-02Not AvailableUs 0a2ef1ad1c84951dc1392a8bbe1f3cb241c91ed59e44ad8268635315440d978c
Felodipinetablet, film coated, extended release10 mgoralMutual Pharmaceutical Company, Inc.2004-11-02Not AvailableUs 0a2ef1ad1c84951dc1392a8bbe1f3cb241c91ed59e44ad8268635315440d978c
Felodipinetablet, film coated, extended release2.5 mgoralRichmond Pharmaceuticals, Inc.2004-11-02Not AvailableUs 0a2ef1ad1c84951dc1392a8bbe1f3cb241c91ed59e44ad8268635315440d978c
Felodipinetablet, film coated, extended release5 mgoralRichmond Pharmaceuticals, Inc.2004-11-02Not AvailableUs 0a2ef1ad1c84951dc1392a8bbe1f3cb241c91ed59e44ad8268635315440d978c
Felodipinetablet, film coated, extended release10 mgoralRichmond Pharmaceuticals, Inc.2004-11-02Not AvailableUs 0a2ef1ad1c84951dc1392a8bbe1f3cb241c91ed59e44ad8268635315440d978c
Felodipinetablet, film coated2.5 mgoralPhysicians Total Care, Inc.2005-11-08Not AvailableUs 0a2ef1ad1c84951dc1392a8bbe1f3cb241c91ed59e44ad8268635315440d978c
Felodipinetablet, film coated, extended release10 mgoralPhysicians Total Care, Inc.2005-01-21Not AvailableUs 0a2ef1ad1c84951dc1392a8bbe1f3cb241c91ed59e44ad8268635315440d978c
Felodipinetablet, film coated, extended release5 mgoralPhysicians Total Care, Inc.2005-03-22Not AvailableUs 0a2ef1ad1c84951dc1392a8bbe1f3cb241c91ed59e44ad8268635315440d978c
Felodipinetablet, film coated, extended release5 mgoralPd Rx Pharmaceuticals, Inc.2004-11-02Not AvailableUs 0a2ef1ad1c84951dc1392a8bbe1f3cb241c91ed59e44ad8268635315440d978c
Felodipinetablet, film coated, extended release2.5 mgoralWockhardt Limited2010-12-05Not AvailableUs 0a2ef1ad1c84951dc1392a8bbe1f3cb241c91ed59e44ad8268635315440d978c
Felodipinetablet, film coated, extended release5 mgoralWockhardt Limited2010-12-05Not AvailableUs 0a2ef1ad1c84951dc1392a8bbe1f3cb241c91ed59e44ad8268635315440d978c
Felodipinetablet, film coated, extended release10 mgoralWockhardt Limited2010-12-05Not AvailableUs 0a2ef1ad1c84951dc1392a8bbe1f3cb241c91ed59e44ad8268635315440d978c
Felodipinetablet, film coated, extended release2.5 mgoralCitron Pharma LLC2013-01-17Not AvailableUs 0a2ef1ad1c84951dc1392a8bbe1f3cb241c91ed59e44ad8268635315440d978c
Felodipinetablet, film coated, extended release5 mgoralCitron Pharma LLC2013-01-17Not AvailableUs 0a2ef1ad1c84951dc1392a8bbe1f3cb241c91ed59e44ad8268635315440d978c
Felodipinetablet, film coated, extended release10 mgoralCitron Pharma LLC2013-01-17Not AvailableUs 0a2ef1ad1c84951dc1392a8bbe1f3cb241c91ed59e44ad8268635315440d978c
Felodipinetablet, film coated, extended release5 mgoralbryant ranch prepack2004-11-02Not AvailableUs 0a2ef1ad1c84951dc1392a8bbe1f3cb241c91ed59e44ad8268635315440d978c
Felodipinetablet, extended release2.5 mgoralbryant ranch prepack2011-11-28Not AvailableUs 0a2ef1ad1c84951dc1392a8bbe1f3cb241c91ed59e44ad8268635315440d978c
Felodipinetablet, film coated, extended release2.5 mgoralWOCKHARDT USA LLC2010-12-05Not AvailableUs 0a2ef1ad1c84951dc1392a8bbe1f3cb241c91ed59e44ad8268635315440d978c
Felodipinetablet, film coated, extended release5 mgoralWOCKHARDT USA LLC2010-12-05Not AvailableUs 0a2ef1ad1c84951dc1392a8bbe1f3cb241c91ed59e44ad8268635315440d978c
Felodipinetablet, film coated, extended release10 mgoralWOCKHARDT USA LLC2010-12-05Not AvailableUs 0a2ef1ad1c84951dc1392a8bbe1f3cb241c91ed59e44ad8268635315440d978c
Felodipinetablet, film coated, extended release2.5 mgoralAurobindo Pharma Limited2013-01-17Not AvailableUs 0a2ef1ad1c84951dc1392a8bbe1f3cb241c91ed59e44ad8268635315440d978c
Felodipinetablet, film coated, extended release5 mgoralAurobindo Pharma Limited2013-01-17Not AvailableUs 0a2ef1ad1c84951dc1392a8bbe1f3cb241c91ed59e44ad8268635315440d978c
Felodipinetablet, film coated, extended release10 mgoralAurobindo Pharma Limited2013-01-17Not AvailableUs 0a2ef1ad1c84951dc1392a8bbe1f3cb241c91ed59e44ad8268635315440d978c
Felodipinetablet, extended release5 mgoralAmerican Health Packaging2014-12-15Not AvailableUs 0a2ef1ad1c84951dc1392a8bbe1f3cb241c91ed59e44ad8268635315440d978c
Felodipinetablet, film coated, extended release2.5 mgoralCarilion Materials Management2004-11-02Not AvailableUs 0a2ef1ad1c84951dc1392a8bbe1f3cb241c91ed59e44ad8268635315440d978c
Felodipinetablet, film coated, extended release2.5 mgoralGlenmark Generics, Inc. USA2010-12-20Not AvailableUs 0a2ef1ad1c84951dc1392a8bbe1f3cb241c91ed59e44ad8268635315440d978c
Felodipinetablet, film coated, extended release5 mgoralGlenmark Generics, Inc. USA2010-12-20Not AvailableUs 0a2ef1ad1c84951dc1392a8bbe1f3cb241c91ed59e44ad8268635315440d978c
Felodipinetablet, film coated, extended release10 mgoralGlenmark Generics, Inc. USA2010-12-20Not AvailableUs 0a2ef1ad1c84951dc1392a8bbe1f3cb241c91ed59e44ad8268635315440d978c
Over the Counter ProductsNot Available
International Brands
NameCompany
Felodur ERNot Available
FelogardNot Available
PenedilNot Available
Plendil DepottabAstraZeneca
Plendil ERAstraZeneca
Plendil RetardAstraZeneca
RenedilSanofi-Aventis
SplendilNot Available
Brand mixtures
Brand NameIngredients
Lexxelfelodipine + enalapril maleate
SaltsNot Available
Categories
CAS number72509-76-3
WeightAverage: 384.254
Monoisotopic: 383.069113515
Chemical FormulaC18H19Cl2NO4
InChI KeyRZTAMFZIAATZDJ-UHFFFAOYSA-N
InChI
InChI=1S/C18H19Cl2NO4/c1-5-25-18(23)14-10(3)21-9(2)13(17(22)24-4)15(14)11-7-6-8-12(19)16(11)20/h6-8,15,21H,5H2,1-4H3
IUPAC Name
3-ethyl 5-methyl 4-(2,3-dichlorophenyl)-2,6-dimethyl-1,4-dihydropyridine-3,5-dicarboxylate
SMILES
CCOC(=O)C1=C(C)NC(C)=C(C1C1=C(Cl)C(Cl)=CC=C1)C(=O)OC
Taxonomy
DescriptionThis compound belongs to the class of organic compounds known as dihydropyridinecarboxylic acids and derivatives. These are compounds containing a dihydropyridine moiety bearing a carboxylic acid group.
KingdomOrganic compounds
Super ClassOrganoheterocyclic compounds
ClassPyridines and derivatives
Sub ClassHydropyridines
Direct ParentDihydropyridinecarboxylic acids and derivatives
Alternative Parents
Substituents
  • Dihydropyridinecarboxylic acid derivative
  • 1,2-dichlorobenzene
  • Halobenzene
  • Chlorobenzene
  • Benzenoid
  • Dicarboxylic acid or derivatives
  • Monocyclic benzene moiety
  • Aryl halide
  • Aryl chloride
  • Vinylogous amide
  • Alpha,beta-unsaturated carboxylic ester
  • Enoate ester
  • Methyl ester
  • Carboxylic acid ester
  • Azacycle
  • Enamine
  • Carboxylic acid derivative
  • Hydrocarbon derivative
  • Organooxygen compound
  • Organonitrogen compound
  • Organochloride
  • Organohalogen compound
  • Carbonyl group
  • Amine
  • Aromatic heteromonocyclic compound
Molecular FrameworkAromatic heteromonocyclic compounds
External DescriptorsNot Available
Pharmacology
IndicationFor the treatment of mild to moderate essential hypertension.
PharmacodynamicsFelodipine belongs to the dihydropyridine (DHP) class of calcium channel blockers (CCBs), the most widely used class of CCBs. There are at least five different types of calcium channels in Homo sapiens: L-, N-, P/Q-, R- and T-type. It was widely accepted that CCBs target L-type calcium channels, the major channel in muscle cells that mediates contraction; however, some studies have shown that felodipine also binds to and inhibits T-type calcium channels. T-type calcium channels are most commonly found on neurons, cells with pacemaker activity and on osteocytes. The pharmacologic significance of T-type calcium channel blockade is unknown. Felodipine also binds to calmodulin and inhibits calmodulin-dependent calcium release from the sarcoplasmic reticulum. The effect of this interaction appears to be minor. Another study demonstrated that felodipine attenuates the activity of calmodulin-dependent cyclic nucleotide phosphodiesterase (CaMPDE) by binding to the PDE-1B1 and PDE-1A2 enzyme subunits. CaMPDE is one of the key enzymes involved in cyclic nucleotides and calcium second messenger systems. Felodipine also acts as an antagonist to the mineralcorticoid receptor by competing with aldosterone for binding and blocking aldosterone-induced coactivator recruitment of the mineralcorticoid receptor. Felodipine is able to bind to skeletal and cardiac muscle isoforms of troponin C, one of the key regulatory proteins in muscle contraction. Though felodipine exhibits binding to many endogenous molecules, its vasodilatory effects are still thought to be brought about primarily through inhibition of voltage-gated L-type calcium channels. Similar to other DHP CCBs, felodipine binds directly to inactive calcium channels stabilizing their inactive conformation. Since arterial smooth muscle depolarizations are longer in duration than cardiac muscle depolarizations, inactive channels are more prevalent in smooth muscle cells. Alternative splicing of the alpha-1 subunit of the channel gives felodipine additional arterial selectivity. At therapeutic sub-toxic concentrations, felodipine has little effect on cardiac myocytes and conduction cells.
Mechanism of actionFelodipine decreases arterial smooth muscle contractility and subsequent vasoconstriction by inhibiting the influx of calcium ions through voltage-gated L-type calcium channels. It reversibly competes against nitrendipine and other DHP CCBs for DHP binding sites in vascular smooth muscle and cultured rabbit atrial cells. Calcium ions entering the cell through these channels bind to calmodulin. Calcium-bound calmodulin then binds to and activates myosin light chain kinase (MLCK). Activated MLCK catalyzes the phosphorylation of the regulatory light chain subunit of myosin, a key step in muscle contraction. Signal amplification is achieved by calcium-induced calcium release from the sarcoplasmic reticulum through ryanodine receptors. Inhibition of the initial influx of calcium decreases the contractile activity of arterial smooth muscle cells and results in vasodilation. The vasodilatory effects of felodipine result in an overall decrease in blood pressure. Felodipine may be used to treat mild to moderate essential hypertension.
AbsorptionIs completely absorbed from the gastrointestinal tract; however, extensive first-pass metabolism through the portal circulation results in a low systemic availability of 15%. Bioavailability is unaffected by food.
Volume of distribution
  • 10 L/kg
Protein binding99%, primarily to the albumin fraction.
Metabolism

Hepatic metabolism primarily via cytochrome P450 3A4. Six metabolites with no appreciable vasodilatory effects have been identified.

SubstrateEnzymesProduct
Felodipine
dehydrofelodipineDetails
Route of eliminationAlthough higher concentrations of the metabolites are present in the plasma due to decreased urinary excretion, these are inactive. Animal studies have demonstrated that felodipine crosses the blood-brain barrier and the placenta.
Half life17.5-31.5 hours in hypertensive patients; 19.1-35.9 hours in elderly hypertensive patients; 8.5-19.7 in healthy volunteers.
Clearance
  • 0.8 L/min [Young healthy subjects]
ToxicitySymptoms of overdose include excessive peripheral vasodilation with marked hypotension and possibly bradycardia. Oral rat LD50 is 1050 mg/kg.
Affected organisms
  • Humans and other mammals
Pathways
PathwayCategorySMPDB ID
Felodipine Metabolism PathwayDrug metabolismSMP00619
Felodipine Action PathwayDrug actionSMP00377
SNP Mediated EffectsNot Available
SNP Mediated Adverse Drug ReactionsNot Available
ADMET
Predicted ADMET features
PropertyValueProbability
Human Intestinal Absorption+0.9878
Blood Brain Barrier-0.83
Caco-2 permeable+0.8867
P-glycoprotein substrateSubstrate0.5149
P-glycoprotein inhibitor IInhibitor0.8563
P-glycoprotein inhibitor IINon-inhibitor0.8383
Renal organic cation transporterNon-inhibitor0.8664
CYP450 2C9 substrateNon-substrate0.8357
CYP450 2D6 substrateNon-substrate0.9116
CYP450 3A4 substrateSubstrate0.6954
CYP450 1A2 substrateInhibitor0.9106
CYP450 2C9 substrateInhibitor0.8948
CYP450 2D6 substrateNon-inhibitor0.9232
CYP450 2C19 substrateInhibitor0.8994
CYP450 3A4 substrateInhibitor0.7959
CYP450 inhibitory promiscuityHigh CYP Inhibitory Promiscuity0.9304
Ames testNon AMES toxic0.7849
CarcinogenicityNon-carcinogens0.7511
BiodegradationNot ready biodegradable0.9527
Rat acute toxicity2.4526 LD50, mol/kg Not applicable
hERG inhibition (predictor I)Weak inhibitor0.9455
hERG inhibition (predictor II)Non-inhibitor0.8734
Pharmacoeconomics
ManufacturersNot Available
Packagers
Dosage forms
FormRouteStrength
Tablet, extended releaseoral10 mg
Tablet, extended releaseoral2.5 mg
Tablet, extended releaseoral5 mg
Tablet, film coatedoral2.5 mg
Tablet, film coated, extended releaseoral10 mg
Tablet, film coated, extended releaseoral2.5 mg
Tablet, film coated, extended releaseoral5 mg
Prices
Unit descriptionCostUnit
Plendil 10 mg 24 Hour tablet3.17USD tablet
Plendil er 10 mg tablet3.05USD tablet
Plendil 10 mg tablet sa2.96USD tablet
Felodipine 10 mg 24 Hour tablet2.95USD tablet
Plendil er 2.5 mg tablet2.94USD tablet
Felodipine er 10 mg tablet2.72USD tablet
Plendil er 5 mg tablet2.6USD tablet
Plendil 5 mg 24 Hour tablet1.77USD tablet
Plendil 2.5 mg 24 Hour tablet1.76USD tablet
Felodipine 5 mg 24 Hour tablet1.67USD tablet
Plendil 2.5 mg tablet sa1.65USD tablet
Plendil 5 mg tablet sa1.65USD tablet
Felodipine 2.5 mg 24 Hour tablet1.57USD tablet
Felodipine er 2.5 mg tablet1.51USD tablet
Felodipine er 5 mg tablet1.51USD tablet
Renedil 10 mg Extended-Release Tablet1.22USD tablet
Plendil 10 mg Extended-Release Tablet1.15USD tablet
Renedil 5 mg Extended-Release Tablet0.81USD tablet
Plendil 5 mg Extended-Release Tablet0.77USD tablet
Sandoz Felodipine 10 mg Extended-Release Tablet0.73USD tablet
Renedil 2.5 mg Extended-Release Tablet0.6USD tablet
Plendil 2.5 mg Extended-Release Tablet0.57USD tablet
Sandoz Felodipine 5 mg Extended-Release Tablet0.48USD tablet
DrugBank does not sell nor buy drugs. Pricing information is supplied for informational purposes only.
PatentsNot Available
Properties
StateSolid
Experimental Properties
PropertyValueSource
melting point145 °CNot Available
water solubility19.7 mg/LNot Available
logP3.86SANGSTER (1994)
Caco2 permeability-4.64ADME Research, USCD
Predicted Properties
PropertyValueSource
Water Solubility0.00715 mg/mLALOGPS
logP4.36ALOGPS
logP3.44ChemAxon
logS-4.7ALOGPS
pKa (Strongest Basic)5.39ChemAxon
Physiological Charge0ChemAxon
Hydrogen Acceptor Count3ChemAxon
Hydrogen Donor Count1ChemAxon
Polar Surface Area64.63 Å2ChemAxon
Rotatable Bond Count6ChemAxon
Refractivity99.2 m3·mol-1ChemAxon
Polarizability38.04 Å3ChemAxon
Number of Rings2ChemAxon
Bioavailability1ChemAxon
Rule of FiveYesChemAxon
Ghose FilterYesChemAxon
Veber's RuleYesChemAxon
MDDR-like RuleYesChemAxon
Spectra
Mass Spec (NIST)Not Available
SpectraNot Available
References
Synthesis Reference

Vinay Sharma, “Preparation of micron-size felodipine particles by microfluidization.” U.S. Patent US20020086061, issued July 04, 2002.

US20020086061
General Reference
  1. Dunselman PH, Edgar B: Felodipine clinical pharmacokinetics. Clin Pharmacokinet. 1991 Dec;21(6):418-30. Pubmed
External Links
ATC CodesC08CA02
AHFS Codes
  • 24:28.08
PDB EntriesNot Available
FDA labelDownload (228 KB)
MSDSDownload (55.4 KB)
Interactions
Drug Interactions
Drug
AlfuzosinMay enhance the hypotensive effect of Antihypertensives.
AmifostineAntihypertensives may enhance the hypotensive effect of Amifostine.
AmobarbitalBarbiturates may increase the metabolism of Calcium Channel Blockers.
AprepitantMay increase the serum concentration of CYP3A4 Substrates.
AripiprazoleCYP3A4 Inhibitors (Weak) may increase the serum concentration of ARIPiprazole.
AtracuriumMay enhance the neuromuscular-blocking effect of Neuromuscular-Blocking Agents (Nondepolarizing).
BatimastatMay decrease the metabolism of Calcium Channel Blockers (Dihydropyridine).
BosentanMay decrease the serum concentration of CYP3A4 Substrates.
ButabarbitalBarbiturates may increase the metabolism of Calcium Channel Blockers.
ButalbitalBarbiturates may increase the metabolism of Calcium Channel Blockers.
ButethalMay increase the metabolism of Calcium Channel Blockers.
Calcium AcetateCalcium Salts may diminish the therapeutic effect of Calcium Channel Blockers.
Calcium carbonateCalcium Salts may diminish the therapeutic effect of Calcium Channel Blockers.
Calcium ChlorideCalcium Salts may diminish the therapeutic effect of Calcium Channel Blockers.
CarbamazepineMay increase the metabolism of Calcium Channel Blockers (Dihydropyridine).
CimetidineCimetidine may increase the serum concentration of Calcium Channel Blockers.
Cisatracurium BesylateMay enhance the neuromuscular-blocking effect of Neuromuscular-Blocking Agents (Nondepolarizing).
ClarithromycinMacrolide Antibiotics may decrease the metabolism of Calcium Channel Blockers.
ClopidogrelMay diminish the therapeutic effect of Clopidogrel. Exceptions: Clevidipine.
ConivaptanMay increase the serum concentration of CYP3A4 Substrates.
DabrafenibMay decrease the serum concentration of CYP3A4 Substrates.
DapoxetineMay enhance the orthostatic hypotensive effect of Calcium Channel Blockers.
DasatinibMay increase the serum concentration of CYP3A4 Substrates.
DeferasiroxMay decrease the serum concentration of CYP3A4 Substrates.
DiazoxideMay enhance the hypotensive effect of Antihypertensives.
DofetilideCYP3A4 Inhibitors (Weak) may increase the serum concentration of Dofetilide.
DoxazosinAlpha1-Blockers may enhance the hypotensive effect of Calcium Channel Blockers.
DuloxetineHypotensive Agents may enhance the orthostatic hypotensive effect of DULoxetine.
EfavirenzMay decrease the serum concentration of Calcium Channel Blockers.
FluconazoleFluconazole may increase the serum concentration of Calcium Channel Blockers. Exceptions: Clevidipine.
FosaprepitantMay increase the serum concentration of CYP3A4 Substrates.
FosphenytoinCalcium Channel Blockers may increase the serum concentration of Fosphenytoin.
HeptabarbitalMay increase the metabolism of Calcium Channel Blockers.
HexobarbitalMay increase the metabolism of Calcium Channel Blockers.
HydrocodoneCYP3A4 Inhibitors (Weak) may increase the serum concentration of Hydrocodone.
IsoflurophateMay decrease the metabolism of Calcium Channel Blockers (Dihydropyridine).
ItraconazoleMay increase the serum concentration of Felodipine.
IvacaftorMay increase the serum concentration of CYP3A4 Substrates.
LomitapideCYP3A4 Inhibitors (Weak) may increase the serum concentration of Lomitapide.
LULICONAZOLEMay increase the serum concentration of CYP3A4 Substrates.
Magnesium oxideMay enhance the adverse/toxic effect of Magnesium Salts. Magnesium Salts may enhance the hypotensive effect of Calcium Channel Blockers.
Magnesium salicylateMay enhance the adverse/toxic effect of Magnesium Salts. Magnesium Salts may enhance the hypotensive effect of Calcium Channel Blockers.
MelatoninMay diminish the antihypertensive effect of Calcium Channel Blockers (Dihydropyridine).
MethohexitalBarbiturates may increase the metabolism of Calcium Channel Blockers.
MethylphenidateMay diminish the antihypertensive effect of Antihypertensives.
MifepristoneMay increase the serum concentration of CYP3A4 Substrates.
MitotaneMay decrease the serum concentration of CYP3A4 Substrates.
NafcillinNafcillin may increase the metabolism of Calcium Channel Blockers. Exceptions: Clevidipine.
NitroprussideMay enhance the hypotensive effect of Nitroprusside.
ObinutuzumabAntihypertensives may enhance the hypotensive effect of Obinutuzumab.
PancuroniumMay enhance the neuromuscular-blocking effect of Neuromuscular-Blocking Agents (Nondepolarizing).
PentobarbitalBarbiturates may increase the metabolism of Calcium Channel Blockers.
PentoxifyllineMay enhance the hypotensive effect of Antihypertensives.
PhenobarbitalBarbiturates may increase the metabolism of Calcium Channel Blockers.
PhenoxybenzamineAlpha1-Blockers may enhance the hypotensive effect of Calcium Channel Blockers.
PhentolamineAlpha1-Blockers may enhance the hypotensive effect of Calcium Channel Blockers.
PhenytoinMay increase the serum concentration of Phenytoin.
PimozideCYP3A4 Inhibitors (Weak) may increase the serum concentration of Pimozide.
PosaconazoleAntifungal Agents (Azole Derivatives, Systemic) may enhance the adverse/toxic effect of Calcium Channel Blockers. Specifically, itraconazole may enhance the negative inotropic effects of verapamil or diltiazem. Antifungal Agents (Azole Derivatives, Systemic) may decrease the metabolism of Calcium Channel Blockers. Fluconazole and isavuconazonium likely exert weaker effects than other azoles and are addressed in separate monographs.
PrazosinAlpha1-Blockers may enhance the hypotensive effect of Calcium Channel Blockers.
PrimidoneMay increase the metabolism of Calcium Channel Blockers.
RifampicinRifamycin Derivatives may decrease the serum concentration of Calcium Channel Blockers. This primarily affects oral forms of calcium channel blockers.
RifapentineRifamycin Derivatives may decrease the serum concentration of Calcium Channel Blockers. This primarily affects oral forms of calcium channel blockers.
RisperidoneHypotensive Agents may enhance the hypotensive effect of RisperiDONE.
RituximabAntihypertensives may enhance the hypotensive effect of RiTUXimab.
RocuroniumMay enhance the neuromuscular-blocking effect of Neuromuscular-Blocking Agents (Nondepolarizing).
SecobarbitalBarbiturates may increase the metabolism of Calcium Channel Blockers.
SilodosinAlpha1-Blockers may enhance the hypotensive effect of Calcium Channel Blockers.
SiltuximabMay decrease the serum concentration of CYP3A4 Substrates.
SimeprevirMay decrease the metabolism of Calcium Channel Blockers (Dihydropyridine).
SulfisoxazoleMacrolide Antibiotics may decrease the metabolism of Calcium Channel Blockers.
TadalafilMay enhance the antihypertensive effect of Antihypertensives.
TamsulosinAlpha1-Blockers may enhance the hypotensive effect of Calcium Channel Blockers.
TelithromycinMacrolide Antibiotics may decrease the metabolism of Calcium Channel Blockers.
TerazosinAlpha1-Blockers may enhance the hypotensive effect of Calcium Channel Blockers.
TocilizumabMay decrease the serum concentration of CYP3A4 Substrates.
VardenafilMay enhance the antihypertensive effect of Antihypertensives.
VecuroniumMay enhance the neuromuscular-blocking effect of Neuromuscular-Blocking Agents (Nondepolarizing).
VoriconazoleAntifungal Agents (Azole Derivatives, Systemic) may enhance the adverse/toxic effect of Calcium Channel Blockers. Specifically, itraconazole may enhance the negative inotropic effects of verapamil or diltiazem. Antifungal Agents (Azole Derivatives, Systemic) may decrease the metabolism of Calcium Channel Blockers. Fluconazole and isavuconazonium likely exert weaker effects than other azoles and are addressed in separate monographs.
YohimbineMay diminish the antihypertensive effect of Antihypertensives.
Food Interactions
  • Grapefruit down regulates post-translational expression of CYP3A4, the major metabolizing enzyme of nifedipine. Grapefruit, in all forms (e.g. whole fruit, juice and rind), can significantly increase serum levels of nifedipine and may cause toxicity. Avoid grapefruit products while on this medication.
  • Take without regard to meals.

Targets

1. Voltage-dependent L-type calcium channel subunit alpha-1C

Kind: protein

Organism: Human

Pharmacological action: yes

Actions: inhibitor

Components

Name UniProt ID Details
Voltage-dependent L-type calcium channel subunit alpha-1C Q13936 Details

References:

  1. Chen X, Ji ZL, Chen YZ: TTD: Therapeutic Target Database. Nucleic Acids Res. 2002 Jan 1;30(1):412-5. Pubmed
  2. Furukawa T, Yamakawa T, Midera T, Sagawa T, Mori Y, Nukada T: Selectivities of dihydropyridine derivatives in blocking Ca(2+) channel subtypes expressed in Xenopus oocytes. J Pharmacol Exp Ther. 1999 Nov;291(2):464-73. Pubmed
  3. Striessnig, J. (2004). Ca 2+ channel blockers. In S. Offermanns, & W. Rosenthal (Eds.). Encyclopedic reference of molecular pharmacology (pp. 201-207). Berlin, Germany: Springer.
  4. Zahradnikova A, Minarovic I, Zahradnik I: Competitive and cooperative effects of Bay K8644 on the L-type calcium channel current inhibition by calcium channel antagonists. J Pharmacol Exp Ther. 2007 Aug;322(2):638-45. Epub 2007 May 2. Pubmed

2. Voltage-dependent calcium channel subunit alpha-2/delta-1

Kind: protein

Organism: Human

Pharmacological action: yes

Actions: inhibitor

Components

Name UniProt ID Details
Voltage-dependent calcium channel subunit alpha-2/delta-1 P54289 Details

References:

  1. Chen X, Ji ZL, Chen YZ: TTD: Therapeutic Target Database. Nucleic Acids Res. 2002 Jan 1;30(1):412-5. Pubmed
  2. Furukawa T, Yamakawa T, Midera T, Sagawa T, Mori Y, Nukada T: Selectivities of dihydropyridine derivatives in blocking Ca(2+) channel subtypes expressed in Xenopus oocytes. J Pharmacol Exp Ther. 1999 Nov;291(2):464-73. Pubmed
  3. Striessnig, J. (2004). Ca 2+ channel blockers. In S. Offermanns, & W. Rosenthal (Eds.). Encyclopedic reference of molecular pharmacology (pp. 201-207). Berlin, Germany: Springer.
  4. Zahradnikova A, Minarovic I, Zahradnik I: Competitive and cooperative effects of Bay K8644 on the L-type calcium channel current inhibition by calcium channel antagonists. J Pharmacol Exp Ther. 2007 Aug;322(2):638-45. Epub 2007 May 2. Pubmed

3. Voltage-dependent L-type calcium channel subunit beta-2

Kind: protein

Organism: Human

Pharmacological action: yes

Actions: inhibitor

Components

Name UniProt ID Details
Voltage-dependent L-type calcium channel subunit beta-2 Q08289 Details

References:

  1. Chen X, Ji ZL, Chen YZ: TTD: Therapeutic Target Database. Nucleic Acids Res. 2002 Jan 1;30(1):412-5. Pubmed
  2. Furukawa T, Yamakawa T, Midera T, Sagawa T, Mori Y, Nukada T: Selectivities of dihydropyridine derivatives in blocking Ca(2+) channel subtypes expressed in Xenopus oocytes. J Pharmacol Exp Ther. 1999 Nov;291(2):464-73. Pubmed
  3. Striessnig, J. (2004). Ca 2+ channel blockers. In S. Offermanns, & W. Rosenthal (Eds.). Encyclopedic reference of molecular pharmacology (pp. 201-207). Berlin, Germany: Springer.
  4. Zahradnikova A, Minarovic I, Zahradnik I: Competitive and cooperative effects of Bay K8644 on the L-type calcium channel current inhibition by calcium channel antagonists. J Pharmacol Exp Ther. 2007 Aug;322(2):638-45. Epub 2007 May 2. Pubmed

4. Voltage-dependent L-type calcium channel subunit alpha-1D

Kind: protein

Organism: Human

Pharmacological action: yes

Actions: inhibitor

Components

Name UniProt ID Details
Voltage-dependent L-type calcium channel subunit alpha-1D Q01668 Details

References:

  1. Sinnegger-Brauns MJ, Huber IG, Koschak A, Wild C, Obermair GJ, Einzinger U, Hoda JC, Sartori SB, Striessnig J: Expression and 1,4-dihydropyridine-binding properties of brain L-type calcium channel isoforms. Mol Pharmacol. 2009 Feb;75(2):407-14. Epub 2008 Nov 24. Pubmed

5. Voltage-dependent L-type calcium channel subunit alpha-1S

Kind: protein

Organism: Human

Pharmacological action: yes

Actions: inhibitor

Components

Name UniProt ID Details
Voltage-dependent L-type calcium channel subunit alpha-1S Q13698 Details

References:

  1. Peterson BZ, Catterall WA: Allosteric interactions required for high-affinity binding of dihydropyridine antagonists to Ca(V)1.1 Channels are modulated by calcium in the pore. Mol Pharmacol. 2006 Aug;70(2):667-75. Epub 2006 May 4. Pubmed

6. Voltage-dependent T-type calcium channel subunit alpha-1H

Kind: protein

Organism: Human

Pharmacological action: unknown

Actions: inhibitor

Components

Name UniProt ID Details
Voltage-dependent T-type calcium channel subunit alpha-1H O95180 Details

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
  2. Perez-Reyes E, Van Deusen AL, Vitko I: Molecular pharmacology of human Cav3.2 T-type Ca2+ channels: block by antihypertensives, antiarrhythmics, and their analogs. J Pharmacol Exp Ther. 2009 Feb;328(2):621-7. Epub 2008 Oct 30. Pubmed

7. Voltage-dependent calcium channel subunit alpha-2/delta-2

Kind: protein

Organism: Human

Pharmacological action: unknown

Actions: inhibitor

Components

Name UniProt ID Details
Voltage-dependent calcium channel subunit alpha-2/delta-2 Q9NY47 Details

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
  2. Perez-Reyes E, Van Deusen AL, Vitko I: Molecular pharmacology of human Cav3.2 T-type Ca2+ channels: block by antihypertensives, antiarrhythmics, and their analogs. J Pharmacol Exp Ther. 2009 Feb;328(2):621-7. Epub 2008 Oct 30. Pubmed

8. Calmodulin

Kind: protein

Organism: Human

Pharmacological action: unknown

Actions: other

Components

Name UniProt ID Details
Calmodulin P62158 Details

References:

  1. Bostrom SL, Westerlund C, Rochester S, Vogel HJ: Binding of a dihydropyridine felodipine-analogue to calmodulin and related calcium-binding proteins. Biochem Pharmacol. 1988 Oct 1;37(19):3723-8. Pubmed
  2. Johnson JD, Andrews CT, Khabbaza EJ, Mills JS: The interaction of felodipine with calcium-binding proteins. J Cardiovasc Pharmacol. 1987;10 Suppl 1:S53-9. Pubmed
  3. Lamers JM, Cysouw KJ, Verdouw PD: Slow calcium channel blockers and calmodulin. Effect of felodipine, nifedipine, prenylamine and bepridil on cardiac sarcolemmal calcium pumping ATPase. Biochem Pharmacol. 1985 Nov 1;34(21):3837-43. Pubmed
  4. Lamers JM, Verdouw PD, Mas-Oliva J: The effects of felodipine and bepridil on calcium-stimulated calmodulin binding and calcium pumping ATPase of cardiac sarcolemma before and after removal of endogenous calmodulin. Mol Cell Biochem. 1987 Dec;78(2):169-76. Pubmed
  5. Mills JS, Bailey BL, Johnson JD: Cooperativity among calmodulin’s drug binding sites. Biochemistry. 1985 Aug 27;24(18):4897-902. Pubmed
  6. Walsh MP, Sutherland C, Scott-Woo GC: Effects of felodipine (a dihydropyridine calcium channel blocker) and analogues on calmodulin-dependent enzymes. Biochem Pharmacol. 1988 Apr 15;37(8):1569-80. Pubmed

9. Calcium/calmodulin-dependent 3',5'-cyclic nucleotide phosphodiesterase 1B

Kind: protein

Organism: Human

Pharmacological action: unknown

Actions: inhibitor

Components

Name UniProt ID Details
Calcium/calmodulin-dependent 3',5'-cyclic nucleotide phosphodiesterase 1B Q01064 Details

References:

  1. Lamers JM, Cysouw KJ, Verdouw PD: Slow calcium channel blockers and calmodulin. Effect of felodipine, nifedipine, prenylamine and bepridil on cardiac sarcolemmal calcium pumping ATPase. Biochem Pharmacol. 1985 Nov 1;34(21):3837-43. Pubmed
  2. Sharma RK, Wang JH, Wu Z: Mechanisms of inhibition of calmodulin-stimulated cyclic nucleotide phosphodiesterase by dihydropyridine calcium antagonists. J Neurochem. 1997 Aug;69(2):845-50. Pubmed

10. Calcium/calmodulin-dependent 3',5'-cyclic nucleotide phosphodiesterase 1A

Kind: protein

Organism: Human

Pharmacological action: unknown

Actions: inhibitor

Components

Name UniProt ID Details
Calcium/calmodulin-dependent 3',5'-cyclic nucleotide phosphodiesterase 1A P54750 Details

References:

  1. Lamers JM, Cysouw KJ, Verdouw PD: Slow calcium channel blockers and calmodulin. Effect of felodipine, nifedipine, prenylamine and bepridil on cardiac sarcolemmal calcium pumping ATPase. Biochem Pharmacol. 1985 Nov 1;34(21):3837-43. Pubmed
  2. Sharma RK, Wang JH, Wu Z: Mechanisms of inhibition of calmodulin-stimulated cyclic nucleotide phosphodiesterase by dihydropyridine calcium antagonists. J Neurochem. 1997 Aug;69(2):845-50. Pubmed

11. Mineralocorticoid receptor

Kind: protein

Organism: Human

Pharmacological action: unknown

Actions: antagonist

Components

Name UniProt ID Details
Mineralocorticoid receptor P08235 Details

References:

  1. Dietz JD, Du S, Bolten CW, Payne MA, Xia C, Blinn JR, Funder JW, Hu X: A number of marketed dihydropyridine calcium channel blockers have mineralocorticoid receptor antagonist activity. Hypertension. 2008 Mar;51(3):742-8. Epub 2008 Feb 4. Pubmed

12. Troponin C, skeletal muscle

Kind: protein

Organism: Human

Pharmacological action: unknown

Actions: other

Components

Name UniProt ID Details
Troponin C, skeletal muscle P02585 Details

References:

  1. Bostrom SL, Westerlund C, Rochester S, Vogel HJ: Binding of a dihydropyridine felodipine-analogue to calmodulin and related calcium-binding proteins. Biochem Pharmacol. 1988 Oct 1;37(19):3723-8. Pubmed
  2. Berman HM, Westbrook J, Feng Z, Gilliland G, Bhat TN, Weissig H, Shindyalov IN, Bourne PE: The Protein Data Bank. Nucleic Acids Res. 2000 Jan 1;28(1):235-42. Pubmed

13. Troponin C, slow skeletal and cardiac muscles

Kind: protein

Organism: Human

Pharmacological action: unknown

Actions: other

Components

Name UniProt ID Details
Troponin C, slow skeletal and cardiac muscles P63316 Details

References:

  1. Bostrom SL, Westerlund C, Rochester S, Vogel HJ: Binding of a dihydropyridine felodipine-analogue to calmodulin and related calcium-binding proteins. Biochem Pharmacol. 1988 Oct 1;37(19):3723-8. Pubmed

Enzymes

1. Cytochrome P450 3A4

Kind: protein

Organism: Human

Pharmacological action: unknown

Actions: substrate inhibitor

Components

Name UniProt ID Details
Cytochrome P450 3A4 P08684 Details

References:

  1. AstraZeneca LP. Plendil® (felodipine) extended-release tablets prescribing information. Wilmington, DE; 2003 Nov.
  2. Flockhart DA. Drug Interactions: Cytochrome P450 Drug Interaction Table. Indiana University School of Medicine (2007). Accessed May 28, 2010.
  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. Epub 2009 Nov 24. Pubmed
  4. Galetin A, Clarke SE, Houston JB: Quinidine and haloperidol as modifiers of CYP3A4 activity: multisite kinetic model approach. Drug Metab Dispos. 2002 Dec;30(12):1512-22. Pubmed

2. Cytochrome P450 3A5

Kind: protein

Organism: Human

Pharmacological action: unknown

Actions: substrate

Components

Name UniProt ID Details
Cytochrome P450 3A5 P20815 Details

References:

  1. Flockhart DA. Drug Interactions: Cytochrome P450 Drug Interaction Table. Indiana University School of Medicine (2007). Accessed May 28, 2010.

3. Cytochrome P450 3A7

Kind: protein

Organism: Human

Pharmacological action: unknown

Actions: substrate

Components

Name UniProt ID Details
Cytochrome P450 3A7 P24462 Details

References:

  1. Flockhart DA. Drug Interactions: Cytochrome P450 Drug Interaction Table. Indiana University School of Medicine (2007). Accessed May 28, 2010.

4. Cytochrome P450 2C8

Kind: protein

Organism: Human

Pharmacological action: unknown

Actions: inhibitor

Components

Name UniProt ID Details
Cytochrome P450 2C8 P10632 Details

References:

  1. Schoch GA, Yano JK, Sansen S, Dansette PM, Stout CD, Johnson EF: Determinants of cytochrome P450 2C8 substrate binding: structures of complexes with montelukast, troglitazone, felodipine, and 9-cis-retinoic acid. J Biol Chem. 2008 Jun 20;283(25):17227-37. Epub 2008 Apr 15. Pubmed
  2. Walsky RL, Gaman EA, Obach RS: Examination of 209 drugs for inhibition of cytochrome P450 2C8. J Clin Pharmacol. 2005 Jan;45(1):68-78. Pubmed
  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. Epub 2009 Nov 24. Pubmed

5. Cytochrome P450 2C9

Kind: protein

Organism: Human

Pharmacological action: unknown

Actions: inhibitor

Components

Name UniProt ID Details
Cytochrome P450 2C9 P11712 Details

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. Epub 2009 Nov 24. Pubmed

6. Cytochrome P450 2D6

Kind: protein

Organism: Human

Pharmacological action: unknown

Actions: inhibitor

Components

Name UniProt ID Details
Cytochrome P450 2D6 P10635 Details

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. Epub 2009 Nov 24. Pubmed

Transporters

1. Multidrug resistance protein 1

Kind: protein

Organism: Human

Pharmacological action: unknown

Actions: inhibitor

Components

Name UniProt ID Details
Multidrug resistance protein 1 P08183 Details

References:

  1. Wang EJ, Casciano CN, Clement RP, Johnson WW: Active transport of fluorescent P-glycoprotein substrates: evaluation as markers and interaction with inhibitors. Biochem Biophys Res Commun. 2001 Nov 30;289(2):580-5. Pubmed

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Drug created on June 13, 2005 07:24 / Updated on January 15, 2014 09:42