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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
(+-)-Ethyl methyl 4-(2,3-dichlorophenyl)-1,4-dihydro-2,6-dimethyl-3,5-pyridinedicarboxylate
3-Ethyl 5-methyl 4-(2,3-dichlorophenyl)-2,6-dimethyl-1,4-dihydro-3,5-pyridinedicarboxylate
4-(2,3-Dichlorophenyl)-1,4-dihydro-2,6-dimethyl-3,5-pyridinedicarboxylic acid ethyl methyl ester
Felodipina
Felodipine
Felodipinum
External Identifiers Not Available
Approved Prescription Products
NameDosageStrengthRouteLabellerMarketing StartMarketing End
Felodipineextended-release Tabletstablet, extended release10 mg/1oralRanbaxy Pharmaceuticals Inc2008-09-10Not applicableUs
Felodipineextended-release Tabletstablet, extended release5 mg/1oralRanbaxy Pharmaceuticals Inc2008-09-10Not applicableUs
Felodipineextended-release Tabletstablet, extended release2.5 mg/1oralRanbaxy Pharmaceuticals Inc2008-09-10Not applicableUs
Plendiltablet, extended release2.5 mg/1oralAstra Zeneca Lp1994-10-04Not applicableUs
Plendiltablet, extended release10 mg/1oralbryant ranch prepack1991-09-16Not applicableUs
Plendiltablet, extended release10 mg/1oralAstra Zeneca Lp1991-09-16Not applicableUs
Plendiltablet, extended release5 mg/1oralAstra Zeneca Lp1991-09-16Not applicableUs
Plendil 10 mgtablet (extended-release)10 mgoralAstrazeneca Canada Inc1992-12-31Not applicableCanada
Plendil 2.5 mgtablet (extended-release)2.5 mgoralAstrazeneca Canada Inc1994-12-31Not applicableCanada
Plendil 5 mgtablet (extended-release)5 mgoralAstrazeneca Canada Inc1992-12-31Not applicableCanada
Renediltablet (extended-release)10 mgoralSanofi Aventis Canada Inc1997-05-282014-06-23Canada
Renediltablet (extended-release)5 mgoralSanofi Aventis Canada Inc1997-04-212014-06-23Canada
Renediltablet (extended-release)2.5 mgoralSanofi Aventis Canada Inc1997-03-242014-06-23Canada
Renedil Srt 10mgtablet (extended-release)10 mgoralHoechst Roussel Canada Inc.1994-12-311999-08-11Canada
Renedil Srt 10mgtablet (extended-release)10 mgoralHoechst Canada Inc.1992-12-311996-08-29Canada
Renedil Srt 2.5mgtablet (extended-release)2.5 mgoralHoechst Roussel Canada Inc.1994-12-311999-08-11Canada
Renedil Srt 2.5mgtablet (extended-release)2.5 mgoralHoechst Canada Inc.1994-12-311997-08-05Canada
Renedil Srt 5mgtablet (extended-release)5 mgoralHoechst Roussel Canada Inc.1994-12-311999-08-11Canada
Renedil Srt 5mgtablet (extended-release)5 mgoralHoechst Canada Inc.1992-12-311996-08-29Canada
Sandoz Felodipinetablet (extended-release)10 mgoralSandoz Canada Incorporated2006-08-15Not applicableCanada
Sandoz Felodipinetablet (extended-release)5 mgoralSandoz Canada Incorporated2006-08-15Not applicableCanada
Approved Generic Prescription Products
NameDosageStrengthRouteLabellerMarketing StartMarketing End
Apo-felodipinetablet (extended-release)2.5 mgoralApotex IncNot applicableNot applicableCanada
Apo-felodipinetablet (extended-release)10 mgoralApotex IncNot applicableNot applicableCanada
Apo-felodipinetablet (extended-release)5 mgoralApotex IncNot applicableNot applicableCanada
Felodipinetablet, film coated, extended release5 mg/1oralWockhardt Limited2010-12-05Not applicableUs
Felodipinetablet, film coated, extended release2.5 mg/1oralRichmond Pharmaceuticals, Inc.2004-11-02Not applicableUs
Felodipinetablet, film coated, extended release10 mg/1oralMedsource Pharmaceuticals2010-12-20Not applicableUs
Felodipinetablet, film coated, extended release10 mg/1oralGlenmark Pharmaceuticals Inc., Usa2010-12-20Not applicableUs
Felodipinetablet, film coated, extended release10 mg/1oralWOCKHARDT USA LLC2010-12-05Not applicableUs
Felodipinetablet, film coated, extended release10 mg/1oralAv Kare, Inc.2014-03-312016-01-15Us
Felodipinetablet, film coated, extended release10 mg/1oralWockhardt Limited2010-12-05Not applicableUs
Felodipinetablet, extended release2.5 mg/1oralTorrent Pharmaceuticals Limited2011-11-28Not applicableUs
Felodipinetablet, film coated, extended release2.5 mg/1oralMylan Pharmaceuticals Inc.2013-03-28Not applicableUs
Felodipinetablet, film coated, extended release5 mg/1oralGlenmark Pharmaceuticals Inc., Usa2010-12-20Not applicableUs
Felodipinetablet, film coated, extended release5 mg/1oralWOCKHARDT USA LLC2010-12-05Not applicableUs
Felodipinetablet, film coated, extended release5 mg/1oralAv Kare, Inc.2014-03-312016-01-15Us
Felodipinetablet, film coated, extended release5 mg/1oralNcs Health Care Of Ky, Inc Dba Vangard Labs2009-11-16Not applicableUs
Felodipinetablet, film coated, extended release2.5 mg/1oralWockhardt Limited2010-12-05Not applicableUs
Felodipinetablet, film coated, extended release10 mg/1oralMutual Pharmaceutical Company, Inc.2004-11-02Not applicableUs
Felodipinetablet, film coated, extended release2.5 mg/1oralGlenmark Pharmaceuticals Inc., Usa2010-12-20Not applicableUs
Felodipinetablet, film coated, extended release2.5 mg/1oralWOCKHARDT USA LLC2010-12-05Not applicableUs
Felodipinetablet, film coated, extended release2.5 mg/1oralAv Kare, Inc.2014-03-312016-01-15Us
Felodipinetablet, film coated, extended release10 mg/1oralNcs Health Care Of Ky, Inc Dba Vangard Labs2009-11-16Not applicableUs
Felodipinetablet, film coated, extended release5 mg/1oralPd Rx Pharmaceuticals, Inc.2004-11-02Not applicableUs
Felodipinetablet, film coated, extended release5 mg/1oralMutual Pharmaceutical Company, Inc.2004-11-02Not applicableUs
Felodipinetablet, film coated, extended release5 mg/1oralPhysicians Total Care, Inc.2005-03-22Not applicableUs
Felodipinetablet, film coated, extended release2.5 mg/1oralMutual Pharmaceutical Company, Inc.2004-11-02Not applicableUs
Felodipinetablet, film coated, extended release2.5 mg/1oralCarilion Materials Management2004-11-02Not applicableUs
Felodipinetablet, extended release2.5 mg/1oralbryant ranch prepack2011-11-28Not applicableUs
Felodipinetablet, extended release10 mg/1oralHeritage Pharmaceuticals Inc.2013-11-08Not applicableUs
Felodipinetablet, film coated, extended release10 mg/1oralQualitest Pharmaceuticals2011-12-15Not applicableUs
Felodipinetablet, film coated, extended release10 mg/1oralPhysicians Total Care, Inc.2005-01-21Not applicableUs
Felodipinetablet, film coated, extended release10 mg/1oralMylan Institutional Inc.2008-05-01Not applicableUs
Felodipinetablet, extended release5 mg/1oralAmerican Health Packaging2014-12-15Not applicableUs
Felodipinetablet, film coated, extended release5 mg/1oralbryant ranch prepack2004-11-02Not applicableUs
Felodipinetablet, extended release5 mg/1oralHeritage Pharmaceuticals Inc.2013-11-08Not applicableUs
Felodipinetablet, extended release5 mg/1oralQualitest Pharmaceuticals2011-12-15Not applicableUs
Felodipinetablet, film coated2.5 mg/1oralPhysicians Total Care, Inc.2005-11-08Not applicableUs
Felodipinetablet, film coated, extended release5 mg/1oralMylan Institutional Inc.2008-05-01Not applicableUs
Felodipinetablet, film coated, extended release5 mg/1oralCarilion Materials Management2010-12-20Not applicableUs
Felodipinetablet, film coated, extended release10 mg/1oralAurobindo Pharma Limited2013-01-17Not applicableUs
Felodipinetablet, film coated, extended release10 mg/1oralCitron Pharma LLC2013-01-17Not applicableUs
Felodipinetablet, extended release2.5 mg/1oralHeritage Pharmaceuticals Inc.2013-11-08Not applicableUs
Felodipinetablet, extended release2.5 mg/1oralQualitest Pharmaceuticals2009-03-31Not applicableUs
Felodipinetablet, film coated, extended release10 mg/1oralRichmond Pharmaceuticals, Inc.2004-11-02Not applicableUs
Felodipinetablet, extended release5 mg/1oralREMEDYREPACK INC.2011-04-20Not applicableUs
Felodipinetablet, film coated, extended release5 mg/1oralAurobindo Pharma Limited2013-01-17Not applicableUs
Felodipinetablet, film coated, extended release5 mg/1oralCitron Pharma LLC2013-01-17Not applicableUs
Felodipinetablet, extended release10 mg/1oralTorrent Pharmaceuticals Limited2011-11-28Not applicableUs
Felodipinetablet, film coated, extended release10 mg/1oralMylan Pharmaceuticals Inc.2013-03-28Not applicableUs
Felodipinetablet, film coated, extended release5 mg/1oralRichmond Pharmaceuticals, Inc.2004-11-02Not applicableUs
Felodipinetablet, extended release5 mg/1oralMedsource Pharmaceuticals2011-11-28Not applicableUs
Felodipinetablet, film coated, extended release2.5 mg/1oralAurobindo Pharma Limited2013-01-17Not applicableUs
Felodipinetablet, film coated, extended release2.5 mg/1oralCitron Pharma LLC2013-01-17Not applicableUs
Felodipinetablet, extended release5 mg/1oralTorrent Pharmaceuticals Limited2011-11-28Not applicableUs
Felodipinetablet, film coated, extended release5 mg/1oralMylan Pharmaceuticals Inc.2013-03-28Not applicableUs
Approved Over the Counter ProductsNot Available
Unapproved/Other Products Not Available
International Brands
NameCompany
Felodur ERNot Available
FelogardNot Available
PenedilNot Available
Plendil DepottabAstraZeneca
Plendil ERAstraZeneca
Plendil RetardAstraZeneca
SplendilNot Available
Brand mixtures
NameLabellerIngredients
Altace Plus Felodipine 2.5mg + 2.5mgSanofi Aventis Canada Inc
Altace Plus Felodipine 5mg + 5mgSanofi Aventis Canada Inc
SaltsNot Available
Categories
UNIIOL961R6O2C
CAS number72509-76-3
WeightAverage: 384.254
Monoisotopic: 383.069113515
Chemical FormulaC18H19Cl2NO4
InChI KeyInChIKey=RZTAMFZIAATZDJ-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.
Related Articles
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 Action PathwayDrug actionSMP00377
Felodipine Metabolism PathwayDrug metabolismSMP00619
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 inhibitorInhibitor0.8948
CYP450 2D6 inhibitorNon-inhibitor0.9232
CYP450 2C19 inhibitorInhibitor0.8994
CYP450 3A4 inhibitorInhibitor0.7959
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
ADMET data is predicted using admetSAR, a free tool for evaluating chemical ADMET properties. (23092397 )
Pharmacoeconomics
ManufacturersNot Available
Packagers
Dosage forms
FormRouteStrength
Tabletoral
Tablet, film coatedoral2.5 mg/1
Tablet, film coated, extended releaseoral10 mg/1
Tablet, film coated, extended releaseoral2.5 mg/1
Tablet, film coated, extended releaseoral5 mg/1
Tablet, extended releaseoral10 mg/1
Tablet, extended releaseoral2.5 mg/1
Tablet, extended releaseoral5 mg/1
Tablet (extended-release)oral10 mg
Tablet (extended-release)oral2.5 mg
Tablet (extended-release)oral5 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 References
  1. Dunselman PH, Edgar B: Felodipine clinical pharmacokinetics. Clin Pharmacokinet. 1991 Dec;21(6):418-30. [PubMed:1782737 ]
External Links
ATC CodesC08CA02C09BB05
AHFS Codes
  • 24:28.08
PDB EntriesNot Available
FDA labelDownload (228 KB)
MSDSDownload (55.4 KB)
Interactions
Drug Interactions
Drug
AcetaminophenThe metabolism of Felodipine can be increased when combined with Acetaminophen.
AldesleukinThe risk or severity of adverse effects can be increased when Aldesleukin is combined with Felodipine.
AlfuzosinAlfuzosin may increase the hypotensive activities of Felodipine.
AmifostineFelodipine may increase the hypotensive activities of Amifostine.
AmobarbitalThe metabolism of Felodipine can be increased when combined with Amobarbital.
AmodiaquineThe serum concentration of Amodiaquine can be increased when it is combined with Felodipine.
AprepitantThe serum concentration of Felodipine can be increased when it is combined with Aprepitant.
AripiprazoleThe serum concentration of Aripiprazole can be increased when it is combined with Felodipine.
AtosibanThe risk or severity of adverse effects can be increased when Felodipine is combined with Atosiban.
Atracurium besylateFelodipine may increase the neuromuscular blocking activities of Atracurium besylate.
BepridilFelodipine may increase the hypotensive activities of Bepridil.
BexaroteneThe serum concentration of Felodipine can be decreased when it is combined with Bexarotene.
BosentanThe serum concentration of Felodipine can be decreased when it is combined with Bosentan.
BrimonidineBrimonidine may increase the antihypertensive activities of Felodipine.
ButabarbitalThe metabolism of Felodipine can be increased when combined with Butabarbital.
ButalbitalThe metabolism of Felodipine can be increased when combined with Butalbital.
ButethalThe metabolism of Felodipine can be increased when combined with Butethal.
CaffeineThe metabolism of Felodipine can be increased when combined with Caffeine.
Calcium AcetateThe therapeutic efficacy of Felodipine can be decreased when used in combination with Calcium Acetate.
Calcium carbonateThe therapeutic efficacy of Felodipine can be decreased when used in combination with Calcium carbonate.
Calcium ChlorideThe therapeutic efficacy of Felodipine can be decreased when used in combination with Calcium Chloride.
Calcium citrateThe therapeutic efficacy of Felodipine can be decreased when used in combination with Calcium citrate.
Calcium gluconateThe therapeutic efficacy of Felodipine can be decreased when used in combination with Calcium gluconate.
CarbamazepineThe metabolism of Felodipine can be increased when combined with Carbamazepine.
CimetidineThe serum concentration of Felodipine can be increased when it is combined with Cimetidine.
Cisatracurium besylateFelodipine may increase the neuromuscular blocking activities of Cisatracurium besylate.
ClarithromycinThe metabolism of Felodipine can be decreased when combined with Clarithromycin.
ClopidogrelThe therapeutic efficacy of Clopidogrel can be decreased when used in combination with Felodipine.
ConivaptanThe serum concentration of Felodipine can be increased when it is combined with Conivaptan.
CyclosporineThe metabolism of Felodipine can be decreased when combined with Cyclosporine.
DabrafenibThe serum concentration of Felodipine can be decreased when it is combined with Dabrafenib.
DapoxetineDapoxetine may increase the orthostatic hypotensive activities of Felodipine.
DasatinibThe serum concentration of Felodipine can be increased when it is combined with Dasatinib.
DeferasiroxThe serum concentration of Felodipine can be decreased when it is combined with Deferasirox.
DiazoxideDiazoxide may increase the hypotensive activities of Felodipine.
DoxazosinDoxazosin may increase the hypotensive activities of Felodipine.
DuloxetineFelodipine may increase the orthostatic hypotensive activities of Duloxetine.
EfavirenzThe serum concentration of Felodipine can be decreased when it is combined with Efavirenz.
ErythromycinThe metabolism of Felodipine can be decreased when combined with Erythromycin.
FluconazoleThe serum concentration of Felodipine can be increased when it is combined with Fluconazole.
FosaprepitantThe serum concentration of Felodipine can be increased when it is combined with Fosaprepitant.
FosphenytoinThe serum concentration of Fosphenytoin can be increased when it is combined with Felodipine.
Fusidic AcidThe serum concentration of Felodipine can be increased when it is combined with Fusidic Acid.
HeptabarbitalThe metabolism of Felodipine can be increased when combined with Heptabarbital.
HexobarbitalThe metabolism of Felodipine can be increased when combined with Hexobarbital.
IdelalisibThe serum concentration of Felodipine can be increased when it is combined with Idelalisib.
ItraconazoleThe serum concentration of Felodipine can be increased when it is combined with Itraconazole.
IvacaftorThe serum concentration of Felodipine can be increased when it is combined with Ivacaftor.
KetoconazoleThe serum concentration of Felodipine can be increased when it is combined with Ketoconazole.
LevodopaFelodipine may increase the orthostatic hypotensive activities of Levodopa.
LuliconazoleThe serum concentration of Felodipine can be increased when it is combined with Luliconazole.
Magnesium chlorideThe risk or severity of adverse effects can be increased when Felodipine is combined with Magnesium chloride.
Magnesium citrateThe risk or severity of adverse effects can be increased when Felodipine is combined with Magnesium citrate.
Magnesium hydroxideThe risk or severity of adverse effects can be increased when Felodipine is combined with Magnesium hydroxide.
Magnesium oxideThe risk or severity of adverse effects can be increased when Felodipine is combined with Magnesium oxide.
Magnesium salicylateThe risk or severity of adverse effects can be increased when Felodipine is combined with Magnesium salicylate.
Magnesium SulfateThe risk or severity of adverse effects can be increased when Felodipine is combined with Magnesium Sulfate.
MelatoninMelatonin may decrease the antihypertensive activities of Felodipine.
MethohexitalThe metabolism of Felodipine can be increased when combined with Methohexital.
MethylphenidateMethylphenidate may decrease the antihypertensive activities of Felodipine.
MifepristoneThe serum concentration of Felodipine can be increased when it is combined with Mifepristone.
MitotaneThe serum concentration of Felodipine can be decreased when it is combined with Mitotane.
MolsidomineMolsidomine may increase the hypotensive activities of Felodipine.
MoxonidineMoxonidine may increase the hypotensive activities of Felodipine.
NafcillinThe metabolism of Felodipine can be increased when combined with Nafcillin.
NelfinavirThe metabolism of Felodipine can be decreased when combined with Nelfinavir.
NetupitantThe serum concentration of Felodipine can be increased when it is combined with Netupitant.
NicorandilNicorandil may increase the hypotensive activities of Felodipine.
NitroprussideFelodipine may increase the hypotensive activities of Nitroprusside.
ObinutuzumabFelodipine may increase the hypotensive activities of Obinutuzumab.
PalbociclibThe serum concentration of Felodipine can be increased when it is combined with Palbociclib.
PancuroniumFelodipine may increase the neuromuscular blocking activities of Pancuronium.
PentobarbitalThe metabolism of Felodipine can be increased when combined with Pentobarbital.
PentoxifyllinePentoxifylline may increase the hypotensive activities of Felodipine.
PhenelzinePhenelzine may increase the hypotensive activities of Felodipine.
PhenobarbitalThe metabolism of Felodipine can be increased when combined with Phenobarbital.
PhenoxybenzaminePhenoxybenzamine may increase the hypotensive activities of Felodipine.
PhentolaminePhentolamine may increase the hypotensive activities of Felodipine.
PhenytoinThe serum concentration of Phenytoin can be increased when it is combined with Felodipine.
PosaconazoleThe risk or severity of adverse effects can be increased when Posaconazole is combined with Felodipine.
PrazosinPrazosin may increase the hypotensive activities of Felodipine.
PrimidoneThe metabolism of Felodipine can be increased when combined with Primidone.
QuinineQuinine may increase the hypotensive activities of Felodipine.
RifabutinThe serum concentration of Felodipine can be decreased when it is combined with Rifabutin.
RifampicinThe serum concentration of Felodipine can be decreased when it is combined with Rifampicin.
RifapentineThe serum concentration of Felodipine can be decreased when it is combined with Rifapentine.
RisperidoneFelodipine may increase the hypotensive activities of Risperidone.
RituximabFelodipine may increase the hypotensive activities of Rituximab.
RocuroniumFelodipine may increase the neuromuscular blocking activities of Rocuronium.
SecobarbitalThe metabolism of Felodipine can be increased when combined with Secobarbital.
SilodosinSilodosin may increase the hypotensive activities of Felodipine.
SiltuximabThe serum concentration of Felodipine can be decreased when it is combined with Siltuximab.
SimeprevirThe serum concentration of Felodipine can be increased when it is combined with Simeprevir.
St. John's WortThe serum concentration of Felodipine can be decreased when it is combined with St. John's Wort.
StiripentolThe serum concentration of Felodipine can be increased when it is combined with Stiripentol.
SulfisoxazoleThe metabolism of Felodipine can be decreased when combined with Sulfisoxazole.
TacrolimusThe serum concentration of Tacrolimus can be increased when it is combined with Felodipine.
TadalafilTadalafil may increase the antihypertensive activities of Felodipine.
TamsulosinTamsulosin may increase the hypotensive activities of Felodipine.
TelithromycinThe metabolism of Felodipine can be decreased when combined with Telithromycin.
TerazosinTerazosin may increase the hypotensive activities of Felodipine.
TocilizumabThe serum concentration of Felodipine can be decreased when it is combined with Tocilizumab.
TorasemideThe metabolism of Torasemide can be decreased when combined with Felodipine.
TranylcypromineTranylcypromine may increase the hypotensive activities of Felodipine.
TreprostinilTreprostinil may increase the hypotensive activities of Felodipine.
ValsartanThe risk or severity of adverse effects can be increased when Valsartan is combined with Felodipine.
VardenafilVardenafil may increase the antihypertensive activities of Felodipine.
VecuroniumFelodipine may increase the neuromuscular blocking activities of Vecuronium.
VoriconazoleThe risk or severity of adverse effects can be increased when Voriconazole is combined with Felodipine.
YohimbineYohimbine may decrease the antihypertensive activities of Felodipine.
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

Kind
Protein
Organism
Human
Pharmacological action
yes
Actions
inhibitor
General Function:
Voltage-gated calcium channel activity
Specific Function:
Voltage-sensitive calcium channels (VSCC) mediate the entry of calcium ions into excitable cells and are also involved in a variety of calcium-dependent processes, including muscle contraction, hormone or neurotransmitter release, gene expression, cell motility, cell division and cell death. The isoform alpha-1C gives rise to L-type calcium currents. Long-lasting (L-type) calcium channels belon...
Gene Name:
CACNA1C
Uniprot ID:
Q13936
Molecular Weight:
248974.1 Da
References
  1. Chen X, Ji ZL, Chen YZ: TTD: Therapeutic Target Database. Nucleic Acids Res. 2002 Jan 1;30(1):412-5. [PubMed:11752352 ]
  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:10525060 ]
  3. 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:17475903 ]
  4. Striessnig, J. (2004). Ca 2+ channel blockers. In Encyclopedic reference of molecular pharmacology (pp. 201-207). Berlin: Springer. [ISBN:9783540298328 ]
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. Plays an important role in excitation-contraction coupling (By similarity).
Gene Name:
CACNA2D1
Uniprot ID:
P54289
Molecular Weight:
124566.93 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. 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:10525060 ]
  3. 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:17475903 ]
  4. Striessnig, J. (2004). Ca 2+ channel blockers. In Encyclopedic reference of molecular pharmacology (pp. 201-207). Berlin: Springer. [ISBN:9783540298328 ]
Kind
Protein
Organism
Human
Pharmacological action
yes
Actions
inhibitor
General Function:
Voltage-gated calcium channel activity
Specific Function:
The beta subunit of voltage-dependent calcium channels contributes to the function of the calcium channel by increasing peak calcium current, shifting the voltage dependencies of activation and inactivation, modulating G protein inhibition and controlling the alpha-1 subunit membrane targeting.
Gene Name:
CACNB2
Uniprot ID:
Q08289
Molecular Weight:
73579.925 Da
References
  1. Chen X, Ji ZL, Chen YZ: TTD: Therapeutic Target Database. Nucleic Acids Res. 2002 Jan 1;30(1):412-5. [PubMed:11752352 ]
  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:10525060 ]
  3. 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:17475903 ]
  4. Striessnig, J. (2004). Ca 2+ channel blockers. In Encyclopedic reference of molecular pharmacology (pp. 201-207). Berlin: Springer. [ISBN:9783540298328 ]
Kind
Protein
Organism
Human
Pharmacological action
yes
Actions
inhibitor
General Function:
Voltage-gated calcium channel activity involved sa node cell action potential
Specific Function:
Voltage-sensitive calcium channels (VSCC) mediate the entry of calcium ions into excitable cells and are also involved in a variety of calcium-dependent processes, including muscle contraction, hormone or neurotransmitter release, gene expression, cell motility, cell division and cell death. The isoform alpha-1D gives rise to L-type calcium currents. Long-lasting (L-type) calcium channels belon...
Gene Name:
CACNA1D
Uniprot ID:
Q01668
Molecular Weight:
245138.75 Da
References
  1. 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. doi: 10.1124/mol.108.049981. Epub 2008 Nov 24. [PubMed:19029287 ]
Kind
Protein
Organism
Human
Pharmacological action
yes
Actions
inhibitor
General Function:
Voltage-gated calcium channel activity
Specific Function:
Voltage-sensitive calcium channels (VSCC) mediate the entry of calcium ions into excitable cells and are also involved in a variety of calcium-dependent processes, including muscle contraction, hormone or neurotransmitter release, gene expression, cell motility, cell division and cell death. The isoform alpha-1S gives rise to L-type calcium currents. Long-lasting (L-type) calcium channels belon...
Gene Name:
CACNA1S
Uniprot ID:
Q13698
Molecular Weight:
212348.1 Da
References
  1. 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:16675661 ]
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. 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. doi: 10.1124/jpet.108.145672. Epub 2008 Oct 30. [PubMed:18974361 ]
Kind
Protein
Organism
Human
Pharmacological action
unknown
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. 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. doi: 10.1124/jpet.108.145672. Epub 2008 Oct 30. [PubMed:18974361 ]
Kind
Protein
Organism
Human
Pharmacological action
unknown
Actions
other
General Function:
Titin binding
Specific Function:
Calmodulin mediates the control of a large number of enzymes, ion channels, aquaporins and other proteins by Ca(2+). Among the enzymes to be stimulated by the calmodulin-Ca(2+) complex are a number of protein kinases and phosphatases. Together with CCP110 and centrin, is involved in a genetic pathway that regulates the centrosome cycle and progression through cytokinesis.
Gene Name:
CALM1
Uniprot ID:
P62158
Molecular Weight:
16837.47 Da
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:3178884 ]
  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:2442519 ]
  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:2933041 ]
  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:2964559 ]
  5. Mills JS, Bailey BL, Johnson JD: Cooperativity among calmodulin's drug binding sites. Biochemistry. 1985 Aug 27;24(18):4897-902. [PubMed:4074665 ]
  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:2833901 ]
Kind
Protein
Organism
Human
Pharmacological action
unknown
Actions
inhibitor
General Function:
Metal ion binding
Specific Function:
Cyclic nucleotide phosphodiesterase with a dual-specificity for the second messengers cAMP and cGMP, which are key regulators of many important physiological processes. Has a preference for cGMP as a substrate.
Gene Name:
PDE1B
Uniprot ID:
Q01064
Molecular Weight:
61379.235 Da
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:2933041 ]
  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:9231746 ]
Kind
Protein
Organism
Human
Pharmacological action
unknown
Actions
inhibitor
General Function:
Metal ion binding
Specific Function:
Cyclic nucleotide phosphodiesterase with a dual-specificity for the second messengers cAMP and cGMP, which are key regulators of many important physiological processes. Has a higher affinity for cGMP than for cAMP.
Gene Name:
PDE1A
Uniprot ID:
P54750
Molecular Weight:
61251.38 Da
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:2933041 ]
  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:9231746 ]
Kind
Protein
Organism
Human
Pharmacological action
unknown
Actions
antagonist
General Function:
Zinc ion binding
Specific Function:
Receptor for both mineralocorticoids (MC) such as aldosterone and glucocorticoids (GC) such as corticosterone or cortisol. Binds to mineralocorticoid response elements (MRE) and transactivates target genes. The effect of MC is to increase ion and water transport and thus raise extracellular fluid volume and blood pressure and lower potassium levels.
Gene Name:
NR3C2
Uniprot ID:
P08235
Molecular Weight:
107066.575 Da
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. doi: 10.1161/HYPERTENSIONAHA.107.103580. Epub 2008 Feb 4. [PubMed:18250364 ]
Kind
Protein
Organism
Human
Pharmacological action
unknown
Actions
other
General Function:
Calcium ion binding
Specific Function:
Troponin is the central regulatory protein of striated muscle contraction. Tn consists of three components: Tn-I which is the inhibitor of actomyosin ATPase, Tn-T which contains the binding site for tropomyosin and Tn-C. The binding of calcium to Tn-C abolishes the inhibitory action of Tn on actin filaments.
Gene Name:
TNNC2
Uniprot ID:
P02585
Molecular Weight:
18121.895 Da
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:3178884 ]
  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:10592235 ]
Kind
Protein
Organism
Human
Pharmacological action
unknown
Actions
other
General Function:
Troponin t binding
Specific Function:
Troponin is the central regulatory protein of striated muscle contraction. Tn consists of three components: Tn-I which is the inhibitor of actomyosin ATPase, Tn-T which contains the binding site for tropomyosin and Tn-C. The binding of calcium to Tn-C abolishes the inhibitory action of Tn on actin filaments.
Gene Name:
TNNC1
Uniprot ID:
P63316
Molecular Weight:
18402.36 Da
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:3178884 ]

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. 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. 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:12433827 ]
  3. Drug Interactions: Cytochrome P450 Drug Interaction Table [Link]
Kind
Protein
Organism
Human
Pharmacological action
unknown
Actions
substrate
General Function:
Oxygen binding
Specific Function:
Cytochromes P450 are a group of heme-thiolate monooxygenases. In liver microsomes, this enzyme is involved in an NADPH-dependent electron transport pathway. It oxidizes a variety of structurally unrelated compounds, including steroids, fatty acids, and xenobiotics.
Gene Name:
CYP3A5
Uniprot ID:
P20815
Molecular Weight:
57108.065 Da
References
  1. Drug Interactions: Cytochrome P450 Drug Interaction Table [Link]
Kind
Protein
Organism
Human
Pharmacological action
unknown
Actions
substrate
General Function:
Oxygen binding
Specific Function:
Cytochromes P450 are a group of heme-thiolate monooxygenases. In liver microsomes, this enzyme is involved in an NADPH-dependent electron transport pathway. It oxidizes a variety of structurally unrelated compounds, including steroids, fatty acids, and xenobiotics.
Gene Name:
CYP3A7
Uniprot ID:
P24462
Molecular Weight:
57525.03 Da
References
  1. Drug Interactions: Cytochrome P450 Drug Interaction Table [Link]
Kind
Protein
Organism
Human
Pharmacological action
unknown
Actions
inhibitor
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. 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. doi: 10.1074/jbc.M802180200. Epub 2008 Apr 15. [PubMed:18413310 ]
  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:15601807 ]
  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 ]
Kind
Protein
Organism
Human
Pharmacological action
unknown
Actions
inhibitor
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. Preissner S, Kroll K, Dunkel M, Senger C, Goldsobel G, Kuzman D, Guenther S, Winnenburg R, Schroeder M, Preissner R: SuperCYP: a comprehensive database on Cytochrome P450 enzymes including a tool for analysis of CYP-drug interactions. Nucleic Acids Res. 2010 Jan;38(Database issue):D237-43. doi: 10.1093/nar/gkp970. Epub 2009 Nov 24. [PubMed:19934256 ]
Kind
Protein
Organism
Human
Pharmacological action
unknown
Actions
inhibitor
General Function:
Steroid hydroxylase activity
Specific Function:
Responsible for the metabolism of many drugs and environmental chemicals that it oxidizes. It is involved in the metabolism of drugs such as antiarrhythmics, adrenoceptor antagonists, and tricyclic antidepressants.
Gene Name:
CYP2D6
Uniprot ID:
P10635
Molecular Weight:
55768.94 Da
References
  1. Preissner S, Kroll K, Dunkel M, Senger C, Goldsobel G, Kuzman D, Guenther S, Winnenburg R, Schroeder M, Preissner R: SuperCYP: a comprehensive database on Cytochrome P450 enzymes including a tool for analysis of CYP-drug interactions. Nucleic Acids Res. 2010 Jan;38(Database issue):D237-43. doi: 10.1093/nar/gkp970. Epub 2009 Nov 24. [PubMed:19934256 ]

Transporters

Kind
Protein
Organism
Human
Pharmacological action
unknown
Actions
inhibitor
General Function:
Xenobiotic-transporting atpase activity
Specific Function:
Energy-dependent efflux pump responsible for decreased drug accumulation in multidrug-resistant cells.
Gene Name:
ABCB1
Uniprot ID:
P08183
Molecular Weight:
141477.255 Da
References
  1. Wang EJ, Casciano CN, Clement RP, Johnson WW: Active transport of fluorescent P-glycoprotein substrates: evaluation as markers and interaction with inhibitors. Biochem Biophys Res Commun. 2001 Nov 30;289(2):580-5. [PubMed:11716514 ]
Comments
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Drug created on June 13, 2005 07:24 / Updated on April 15, 2016 16:02