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Identification
NameNicardipine
Accession NumberDB00622  (APRD00088)
TypeSmall Molecule
GroupsApproved
Description

A potent calcium channel blockader with marked vasodilator action. It has antihypertensive properties and is effective in the treatment of angina and coronary spasms without showing cardiodepressant effects. It has also been used in the treatment of asthma and enhances the action of specific antineoplastic agents. [PubChem]

Structure
Thumb
Synonyms
Cardene
Nicardipino
Nicardipinum
External Identifiers Not Available
Approved Prescription Products
NameDosageStrengthRouteLabellerMarketing StartMarketing End
Cardene 20mg Capsulescapsule20 mgoralHoffmann La Roche Limited1996-12-312001-07-19Canada
Cardene 30mg Capsulescapsule30 mgoralHoffmann La Roche Limited1998-01-212001-07-19Canada
Cardene Cap 30mgcapsule30 mgoralSyntex Inc.1990-12-311998-09-03Canada
Cardene I.V.injection, solution.1 mg/mLintravenousEKR Therapeutics, Inc.1992-01-30Not applicableUs
Cardene I.V.injection2.5 mg/mLintravenousEkr Therapeutics1992-01-30Not applicableUs
Cardene I.V.injection, solution.2 mg/mLintravenousEKR Therapeutics, Inc.1992-01-30Not applicableUs
Cardene I.V.injection, solution.2 mg/mLintravenousEKR Therapeutics, Inc.1992-01-30Not applicableUs
Cardene I.V.injection, solution.1 mg/mLintravenousEKR Therapeutics, Inc.1992-01-30Not applicableUs
Cardene IVinjection, solution.2 mg/mLintravenousChiesi USA, Inc.1992-01-30Not applicableUs
Cardene IVinjection, solution.2 mg/mLintravenousChiesi USA, Inc.1992-01-30Not applicableUs
Cardene IVinjection, solution.1 mg/mLintravenousChiesi USA, Inc.1992-01-30Not applicableUs
Cardene IVinjection, solution.1 mg/mLintravenousChiesi USA, Inc.1992-01-30Not applicableUs
Cardene SRcapsule, extended release30 mg/1oralCarilion Materials Management1992-02-21Not applicableUs
Nicardipine Hydrochlorideinjection2.5 mg/mLintravenousWest Ward Pharmaceuticals Corp2012-03-02Not applicableUs
Nicardipine Hydrochlorideinjection2.5 mg/mLintravenousSun Pharma Global Inc.2009-11-17Not applicableUs
Nicardipine Hydrochlorideinjection25 mg/10mLintravenousWest Ward Pharmaceuticals Corp2012-03-02Not applicableUs
Nicardipine Hydrochlorideinjection2.5 mg/mLintravenousWest Ward Pharmaceuticals Corp2012-03-02Not applicableUs
Approved Generic Prescription Products
NameDosageStrengthRouteLabellerMarketing StartMarketing End
Nicardipine Hydrochloridecapsule30 mg/1oralAvera Mc Kennan Hospital2015-07-16Not applicableUs
Nicardipine Hydrochloridecapsule30 mg/1oralAv Kare, Inc.2010-05-05Not applicableUs
Nicardipine Hydrochloridecapsule20 mg/1oralMylan Pharmaceuticals Inc.1996-07-19Not applicableUs
Nicardipine Hydrochloridecapsule30 mg/1oralCarilion Materials Management1996-07-19Not applicableUs
Nicardipine Hydrochloridecapsule20 mg/1oralAv Kare, Inc.2010-05-05Not applicableUs
Nicardipine Hydrochloridecapsule20 mg/1oralCarilion Materials Management1996-07-19Not applicableUs
Nicardipine Hydrochlorideinjection, solution2.5 mg/mLintravenousPharma Force, Inc.2009-11-17Not applicableUs
Nicardipine Hydrochlorideinjection, solution2.5 mg/mLintravenousMylan Institutional LLC2011-12-23Not applicableUs
Nicardipine Hydrochlorideinjection2.5 mg/mLintravenousEmcure Pharmaceuticals Ltd.2009-11-17Not applicableUs
Nicardipine Hydrochlorideinjection2.5 mg/mLintravenousWockhardt USA LLC.2009-11-09Not applicableUs
Nicardipine Hydrochlorideinjection2.5 mg/mLintravenousSandoz Inc.2010-09-27Not applicableUs
Nicardipine Hydrochlorideinjection2.5 mg/mLintravenousWockhardt Limited2009-11-09Not applicableUs
Nicardipine Hydrochlorideinjection2.5 mg/mLintravenousSandoz Inc.2009-11-17Not applicableUs
Nicardipine Hydrochloridecapsule30 mg/1oralEpic Pharma, LLC2010-05-05Not applicableUs
Nicardipine Hydrochlorideinjection, solution2.5 mg/mLintravenousAmerican Regent, Inc.2009-11-17Not applicableUs
Nicardipine Hydrochloridecapsule20 mg/1oralEpic Pharma, LLC2010-05-05Not applicableUs
Nicardipine Hydrochloridecapsule30 mg/1oralMylan Pharmaceuticals Inc.1996-07-19Not applicableUs
Approved Over the Counter ProductsNot Available
Unapproved/Other Products Not Available
International Brands
NameCompany
CardeneRoche
Brand mixturesNot Available
Salts
Name/CASStructureProperties
Nicardipine Hydrochloride
Thumb
  • InChI Key: AIKVCUNQWYTVTO-UHFFFAOYNA-N
  • Monoisotopic Mass: 515.182313414
  • Average Mass: 515.986
DBSALT000499
Categories
UNIICZ5312222S
CAS number55985-32-5
WeightAverage: 479.525
Monoisotopic: 479.205635675
Chemical FormulaC26H29N3O6
InChI KeyInChIKey=ZBBHBTPTTSWHBA-UHFFFAOYSA-N
InChI
InChI=1S/C26H29N3O6/c1-17-22(25(30)34-4)24(20-11-8-12-21(15-20)29(32)33)23(18(2)27-17)26(31)35-14-13-28(3)16-19-9-6-5-7-10-19/h5-12,15,24,27H,13-14,16H2,1-4H3
IUPAC Name
3-{2-[benzyl(methyl)amino]ethyl} 5-methyl 2,6-dimethyl-4-(3-nitrophenyl)-1,4-dihydropyridine-3,5-dicarboxylate
SMILES
COC(=O)C1=C(C)NC(C)=C(C1C1=CC(=CC=C1)[N+]([O-])=O)C(=O)OCCN(C)CC1=CC=CC=C1
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
  • Nitrobenzene
  • Dihydropyridinecarboxylic acid derivative
  • Phenylmethylamine
  • Benzylamine
  • Aralkylamine
  • Benzenoid
  • Dicarboxylic acid or derivatives
  • Monocyclic benzene moiety
  • Vinylogous amide
  • Alpha,beta-unsaturated carboxylic ester
  • Enoate ester
  • Methyl ester
  • Organic nitro compound
  • Tertiary aliphatic amine
  • Tertiary amine
  • Organic nitrite
  • C-nitro compound
  • Carboxylic acid ester
  • Azacycle
  • Organic 1,3-dipolar compound
  • Propargyl-type 1,3-dipolar organic compound
  • Allyl-type 1,3-dipolar organic compound
  • Organic oxoazanium
  • Enamine
  • Carboxylic acid derivative
  • Hydrocarbon derivative
  • Organic salt
  • Organooxygen compound
  • Organonitrogen compound
  • Carbonyl group
  • Amine
  • Organic zwitterion
  • Aromatic heteromonocyclic compound
Molecular FrameworkAromatic heteromonocyclic compounds
External DescriptorsNot Available
Pharmacology
IndicationUsed for the management of patients with chronic stable angina and for the treatment of hypertension.
PharmacodynamicsNicardipine, a dihydropyridine calcium-channel blocker, is used alone or with an angiotensin-converting enzyme inhibitor, to treat hypertension, chronic stable angina pectoris, and Prinzmetal's variant angina. Nicardipine is similar to other peripheral vasodilators. Nicardipine inhibits the influx of extra cellular calcium across the myocardial and vascular smooth muscle cell membranes possibly by deforming the channel, inhibiting ion-control gating mechanisms, and/or interfering with the release of calcium from the sarcoplasmic reticulum. The decrease in intracellular calcium inhibits the contractile processes of the myocardial smooth muscle cells, causing dilation of the coronary and systemic arteries, increased oxygen delivery to the myocardial tissue, decreased total peripheral resistance, decreased systemic blood pressure, and decreased afterload.
Mechanism of actionBy deforming the channel, inhibiting ion-control gating mechanisms, and/or interfering with the release of calcium from the sarcoplasmic reticulum, nicardipine inhibits the influx of extracellular calcium across the myocardial and vascular smooth muscle cell membranes The decrease in intracellular calcium inhibits the contractile processes of the myocardial smooth muscle cells, causing dilation of the coronary and systemic arteries, increased oxygen delivery to the myocardial tissue, decreased total peripheral resistance, decreased systemic blood pressure, and decreased afterload.
Related Articles
AbsorptionWhile nicardipine is completely absorbed, it is subject to saturable first pass metabolism and the systemic bioavailability is about 35% following a 30 mg oral dose at steady state.
Volume of distribution
  • 8.3 L/kg
Protein binding>95%
Metabolism

Nicardipine HCl is metabolized extensively by the liver.

Route of eliminationNicardipine has been shown to be rapidly and extensively metabolized by the liver.
Half life8.6 hours
Clearance
  • 0.4 L/hr∙kg [Following infusion]
ToxicityOral LD50 Rat = 184 mg/kg, Oral LD50 Mouse = 322 mg/kg
Affected organisms
  • Humans and other mammals
PathwaysNot Available
SNP Mediated EffectsNot Available
SNP Mediated Adverse Drug ReactionsNot Available
ADMET
Predicted ADMET features
PropertyValueProbability
Human Intestinal Absorption+0.932
Blood Brain Barrier-0.9549
Caco-2 permeable-0.83
P-glycoprotein substrateSubstrate0.8581
P-glycoprotein inhibitor IInhibitor0.9036
P-glycoprotein inhibitor IIInhibitor0.8253
Renal organic cation transporterNon-inhibitor0.7502
CYP450 2C9 substrateNon-substrate0.8296
CYP450 2D6 substrateNon-substrate0.5554
CYP450 3A4 substrateSubstrate0.7228
CYP450 1A2 substrateInhibitor0.9107
CYP450 2C9 inhibitorInhibitor0.8948
CYP450 2D6 inhibitorInhibitor0.8932
CYP450 2C19 inhibitorInhibitor0.8994
CYP450 3A4 inhibitorInhibitor0.7959
CYP450 inhibitory promiscuityHigh CYP Inhibitory Promiscuity0.8558
Ames testNon AMES toxic0.562
CarcinogenicityNon-carcinogens0.7262
BiodegradationNot ready biodegradable0.9604
Rat acute toxicity2.9030 LD50, mol/kg Not applicable
hERG inhibition (predictor I)Strong inhibitor0.7332
hERG inhibition (predictor II)Non-inhibitor0.7316
ADMET data is predicted using admetSAR, a free tool for evaluating chemical ADMET properties. (23092397 )
Pharmacoeconomics
Manufacturers
  • Ekr therapeutics inc
  • Amneal pharmaceutical
  • Barr laboratories inc
  • Mylan pharmaceuticals inc
  • Teva pharmaceuticals usa inc
  • Watson laboratories inc
  • Bedford laboratories div ben venue laboratories inc
  • Bioniche pharma usa llc
  • Exela pharma sciences
  • Navinta llc
  • Pharmaforce inc
  • Sun pharma global inc
  • Wockhardt ltd
Packagers
Dosage forms
FormRouteStrength
Capsuleoral20 mg
Capsuleoral30 mg
Injection, solutionintravenous.1 mg/mL
Injection, solutionintravenous.2 mg/mL
Capsule, extended releaseoral30 mg/1
Capsuleoral20 mg/1
Capsuleoral30 mg/1
Injectionintravenous2.5 mg/mL
Injectionintravenous25 mg/10mL
Injection, solutionintravenous2.5 mg/mL
Prices
Unit descriptionCostUnit
Cardene SR 60 60 mg 12 Hour Capsule Bottle142.91USD bottle
Nicardipine 25 mg/10 ml ampule25.01USD ml
Nicardipine 25 mg/10 ml vial10.42USD ml
Cardene SR 45 mg 12 Hour Capsule3.22USD capsule
Cardene sr 45 mg capsule2.9USD capsule
Cardene sr 60 mg capsule sa2.29USD capsule
Cardene SR 30 mg 12 Hour Capsule2.02USD capsule
Cardene sr 45 mg capsule sa1.91USD capsule
Cardene-dex 40 mg/200 ml iv1.35USD ml
Cardene-nacl 40 mg/200 ml iv1.35USD ml
Cardene 30 mg capsule1.28USD capsule
Cardene sr 30 mg capsule sa1.21USD capsule
Cardene sr 30 mg capsule0.87USD capsule
Cardene 20 mg capsule0.8USD capsule
NiCARdipine HCl 30 mg capsule0.68USD capsule
Cardene-dex 20 mg/200 ml soln0.67USD ml
Cardene-nacl 20 mg/200 ml soln0.67USD ml
Nicardipine 30 mg capsule0.66USD capsule
NiCARdipine HCl 20 mg capsule0.48USD capsule
Nicardipine 20 mg capsule0.46USD capsule
DrugBank does not sell nor buy drugs. Pricing information is supplied for informational purposes only.
Patents
Patent NumberPediatric ExtensionApprovedExpires (estimated)
US5164405 No1992-11-172009-11-17Us
US7612102 No2007-12-262027-12-26Us
US7659291 No2007-04-182027-04-18Us
US8455524 No2007-04-182027-04-18Us
Properties
StateSolid
Experimental Properties
PropertyValueSource
melting point136-138 °CPhysProp
water solubility2.2 mg/LNot Available
logP3.82SANGSTER (1993)
Predicted Properties
PropertyValueSource
Water Solubility0.00247 mg/mLALOGPS
logP4.34ALOGPS
logP3.56ChemAxon
logS-5.3ALOGPS
pKa (Strongest Basic)8.18ChemAxon
Physiological Charge1ChemAxon
Hydrogen Acceptor Count6ChemAxon
Hydrogen Donor Count1ChemAxon
Polar Surface Area113.69 Å2ChemAxon
Rotatable Bond Count11ChemAxon
Refractivity134.8 m3·mol-1ChemAxon
Polarizability49.95 Å3ChemAxon
Number of Rings3ChemAxon
Bioavailability1ChemAxon
Rule of FiveYesChemAxon
Ghose FilterYesChemAxon
Veber's RuleYesChemAxon
MDDR-like RuleYesChemAxon
Spectra
Mass Spec (NIST)Not Available
SpectraNot Available
References
Synthesis Reference

Takashi Sonobe, Hiroitsu Kawata, Masayoshi Aruga, Tadayoshi Ohmura, Satoru Yoneya, Chiharu Yamada, Yukio Kubota, “Composition for long acting nicardipine preparation and process of producing the composition.” U.S. Patent US4758437, issued March, 1979.

US4758437
General ReferencesNot Available
External Links
ATC CodesC08CA04
AHFS Codes
  • 24:28.08
PDB EntriesNot Available
FDA labelDownload (1.26 MB)
MSDSDownload (106 KB)
Interactions
Drug Interactions
Drug
AcetaminophenThe metabolism of Nicardipine can be increased when combined with Acetaminophen.
AfatinibThe serum concentration of Afatinib can be increased when it is combined with Nicardipine.
AldesleukinThe risk or severity of adverse effects can be increased when Aldesleukin is combined with Nicardipine.
AlfuzosinAlfuzosin may increase the hypotensive activities of Nicardipine.
AmifostineNicardipine may increase the hypotensive activities of Amifostine.
AmobarbitalThe metabolism of Nicardipine can be increased when combined with Amobarbital.
AprepitantThe serum concentration of Nicardipine can be increased when it is combined with Aprepitant.
AripiprazoleThe serum concentration of Aripiprazole can be increased when it is combined with Nicardipine.
AtosibanThe risk or severity of adverse effects can be increased when Nicardipine is combined with Atosiban.
Atracurium besylateNicardipine may increase the neuromuscular blocking activities of Atracurium besylate.
BepridilNicardipine may increase the hypotensive activities of Bepridil.
BexaroteneThe serum concentration of Nicardipine can be decreased when it is combined with Bexarotene.
BortezomibThe metabolism of Bortezomib can be decreased when combined with Nicardipine.
BosentanThe serum concentration of Nicardipine can be decreased when it is combined with Bosentan.
BosutinibThe serum concentration of Bosutinib can be increased when it is combined with Nicardipine.
Brentuximab vedotinThe serum concentration of Brentuximab vedotin can be increased when it is combined with Nicardipine.
BrexpiprazoleThe serum concentration of Brexpiprazole can be increased when it is combined with Nicardipine.
BrimonidineBrimonidine may increase the antihypertensive activities of Nicardipine.
ButabarbitalThe metabolism of Nicardipine can be increased when combined with Butabarbital.
ButalbitalThe metabolism of Nicardipine can be increased when combined with Butalbital.
ButethalThe metabolism of Nicardipine can be increased when combined with Butethal.
CaffeineThe metabolism of Nicardipine can be increased when combined with Caffeine.
Calcium AcetateThe therapeutic efficacy of Nicardipine can be decreased when used in combination with Calcium Acetate.
Calcium carbonateThe therapeutic efficacy of Nicardipine can be decreased when used in combination with Calcium carbonate.
Calcium ChlorideThe therapeutic efficacy of Nicardipine can be decreased when used in combination with Calcium Chloride.
Calcium citrateThe therapeutic efficacy of Nicardipine can be decreased when used in combination with Calcium citrate.
Calcium gluconateThe therapeutic efficacy of Nicardipine can be decreased when used in combination with Calcium gluconate.
CarbamazepineThe metabolism of Nicardipine can be increased when combined with Carbamazepine.
CarvedilolNicardipine may increase the hypotensive activities of Carvedilol.
CilostazolThe serum concentration of Cilostazol can be increased when it is combined with Nicardipine.
CimetidineThe serum concentration of Nicardipine can be increased when it is combined with Cimetidine.
Cisatracurium besylateNicardipine may increase the neuromuscular blocking activities of Cisatracurium besylate.
CitalopramThe serum concentration of Citalopram can be increased when it is combined with Nicardipine.
ClarithromycinThe metabolism of Nicardipine can be decreased when combined with Clarithromycin.
ClopidogrelThe therapeutic efficacy of Clopidogrel can be decreased when used in combination with Nicardipine.
CodeineThe therapeutic efficacy of Codeine can be decreased when used in combination with Nicardipine.
ColchicineThe serum concentration of Colchicine can be increased when it is combined with Nicardipine.
ConivaptanThe serum concentration of Nicardipine can be increased when it is combined with Conivaptan.
CyclosporineThe metabolism of Nicardipine can be decreased when combined with Cyclosporine.
Dabigatran etexilateThe serum concentration of the active metabolites of Dabigatran etexilate can be increased when Dabigatran etexilate is used in combination with Nicardipine.
DabrafenibThe serum concentration of Nicardipine can be decreased when it is combined with Dabrafenib.
DapoxetineDapoxetine may increase the orthostatic hypotensive activities of Nicardipine.
DasatinibThe serum concentration of Nicardipine can be increased when it is combined with Dasatinib.
DeferasiroxThe serum concentration of Nicardipine can be decreased when it is combined with Deferasirox.
DiazoxideDiazoxide may increase the hypotensive activities of Nicardipine.
DiclofenacThe serum concentration of Diclofenac can be increased when it is combined with Nicardipine.
DofetilideNicardipine may increase the QTc-prolonging activities of Dofetilide.
DoxazosinDoxazosin may increase the hypotensive activities of Nicardipine.
DoxorubicinThe serum concentration of Doxorubicin can be increased when it is combined with Nicardipine.
DronabinolThe serum concentration of Dronabinol can be increased when it is combined with Nicardipine.
DuloxetineNicardipine may increase the orthostatic hypotensive activities of Duloxetine.
EdoxabanThe serum concentration of Edoxaban can be increased when it is combined with Nicardipine.
EfavirenzThe serum concentration of Nicardipine can be decreased when it is combined with Efavirenz.
EliglustatThe serum concentration of Eliglustat can be increased when it is combined with Nicardipine.
ErythromycinThe metabolism of Nicardipine can be decreased when combined with Erythromycin.
EverolimusThe serum concentration of Everolimus can be increased when it is combined with Nicardipine.
FesoterodineThe serum concentration of the active metabolites of Fesoterodine can be increased when Fesoterodine is used in combination with Nicardipine.
FlibanserinThe serum concentration of Flibanserin can be increased when it is combined with Nicardipine.
FluconazoleThe serum concentration of Nicardipine can be increased when it is combined with Fluconazole.
FluvoxamineThe metabolism of Fluvoxamine can be decreased when combined with Nicardipine.
FosaprepitantThe serum concentration of Nicardipine can be increased when it is combined with Fosaprepitant.
FosphenytoinThe serum concentration of Fosphenytoin can be increased when it is combined with Nicardipine.
Fusidic AcidThe serum concentration of Nicardipine can be increased when it is combined with Fusidic Acid.
GoserelinNicardipine may increase the QTc-prolonging activities of Goserelin.
HeptabarbitalThe metabolism of Nicardipine can be increased when combined with Heptabarbital.
HexobarbitalThe metabolism of Nicardipine can be increased when combined with Hexobarbital.
HydrocodoneThe serum concentration of Hydrocodone can be increased when it is combined with Nicardipine.
IdelalisibThe serum concentration of Nicardipine can be increased when it is combined with Idelalisib.
ItraconazoleThe risk or severity of adverse effects can be increased when Itraconazole is combined with Nicardipine.
IvacaftorThe serum concentration of Nicardipine can be increased when it is combined with Ivacaftor.
KetoconazoleThe risk or severity of adverse effects can be increased when Ketoconazole is combined with Nicardipine.
LacosamideThe serum concentration of Lacosamide can be increased when it is combined with Nicardipine.
LedipasvirThe serum concentration of Ledipasvir can be increased when it is combined with Nicardipine.
LeuprolideNicardipine may increase the QTc-prolonging activities of Leuprolide.
LevodopaNicardipine may increase the orthostatic hypotensive activities of Levodopa.
LomitapideThe serum concentration of Lomitapide can be increased when it is combined with Nicardipine.
LuliconazoleThe serum concentration of Nicardipine can be increased when it is combined with Luliconazole.
Magnesium chlorideThe risk or severity of adverse effects can be increased when Nicardipine is combined with Magnesium chloride.
Magnesium citrateThe risk or severity of adverse effects can be increased when Nicardipine is combined with Magnesium citrate.
Magnesium hydroxideThe risk or severity of adverse effects can be increased when Nicardipine is combined with Magnesium hydroxide.
Magnesium oxideThe risk or severity of adverse effects can be increased when Nicardipine is combined with Magnesium oxide.
Magnesium salicylateThe risk or severity of adverse effects can be increased when Nicardipine is combined with Magnesium salicylate.
Magnesium SulfateThe risk or severity of adverse effects can be increased when Nicardipine is combined with Magnesium Sulfate.
MelatoninMelatonin may decrease the antihypertensive activities of Nicardipine.
MethohexitalThe metabolism of Nicardipine can be increased when combined with Methohexital.
MethylphenidateMethylphenidate may decrease the antihypertensive activities of Nicardipine.
MetoprololThe serum concentration of Metoprolol can be increased when it is combined with Nicardipine.
MifepristoneThe serum concentration of Nicardipine can be increased when it is combined with Mifepristone.
MitotaneThe serum concentration of Nicardipine can be decreased when it is combined with Mitotane.
MolsidomineMolsidomine may increase the hypotensive activities of Nicardipine.
MoxonidineMoxonidine may increase the hypotensive activities of Nicardipine.
NafcillinThe metabolism of Nicardipine can be increased when combined with Nafcillin.
NaloxegolThe serum concentration of Naloxegol can be increased when it is combined with Nicardipine.
NebivololThe serum concentration of Nebivolol can be increased when it is combined with Nicardipine.
NelfinavirThe metabolism of Nicardipine can be decreased when combined with Nelfinavir.
NetupitantThe serum concentration of Nicardipine can be increased when it is combined with Netupitant.
NicorandilNicorandil may increase the hypotensive activities of Nicardipine.
NimodipineThe serum concentration of Nimodipine can be increased when it is combined with Nicardipine.
NitroprussideNicardipine may increase the hypotensive activities of Nitroprusside.
ObinutuzumabNicardipine may increase the hypotensive activities of Obinutuzumab.
OspemifeneThe serum concentration of Ospemifene can be increased when it is combined with Nicardipine.
PalbociclibThe serum concentration of Nicardipine can be increased when it is combined with Palbociclib.
PancuroniumNicardipine may increase the neuromuscular blocking activities of Pancuronium.
PantoprazoleThe metabolism of Pantoprazole can be decreased when combined with Nicardipine.
ParecoxibThe serum concentration of Parecoxib can be increased when it is combined with Nicardipine.
PazopanibThe serum concentration of Pazopanib can be increased when it is combined with Nicardipine.
PentobarbitalThe metabolism of Nicardipine can be increased when combined with Pentobarbital.
PentoxifyllinePentoxifylline may increase the hypotensive activities of Nicardipine.
PhenelzinePhenelzine may increase the orthostatic hypotensive activities of Nicardipine.
PhenobarbitalThe metabolism of Nicardipine can be increased when combined with Phenobarbital.
PhenoxybenzaminePhenoxybenzamine may increase the hypotensive activities of Nicardipine.
PhentolaminePhentolamine may increase the hypotensive activities of Nicardipine.
PhenytoinThe serum concentration of Phenytoin can be increased when it is combined with Nicardipine.
PimozideThe serum concentration of Pimozide can be increased when it is combined with Nicardipine.
PosaconazoleThe risk or severity of adverse effects can be increased when Posaconazole is combined with Nicardipine.
PrazosinPrazosin may increase the hypotensive activities of Nicardipine.
PrimidoneThe metabolism of Nicardipine can be increased when combined with Primidone.
PropafenoneThe serum concentration of Nicardipine can be increased when it is combined with Propafenone.
PrucaloprideThe serum concentration of Prucalopride can be increased when it is combined with Nicardipine.
QuinineQuinine may increase the hypotensive activities of Nicardipine.
RamelteonThe serum concentration of Ramelteon can be increased when it is combined with Nicardipine.
RanolazineThe serum concentration of Ranolazine can be increased when it is combined with Nicardipine.
RifabutinThe serum concentration of Nicardipine can be decreased when it is combined with Rifabutin.
RifampicinThe serum concentration of Nicardipine can be decreased when it is combined with Rifampicin.
RifapentineThe serum concentration of Nicardipine can be decreased when it is combined with Rifapentine.
RifaximinThe serum concentration of Rifaximin can be increased when it is combined with Nicardipine.
RisperidoneNicardipine may increase the hypotensive activities of Risperidone.
RituximabNicardipine may increase the hypotensive activities of Rituximab.
RocuroniumNicardipine may increase the neuromuscular blocking activities of Rocuronium.
SaquinavirThe serum concentration of Nicardipine can be increased when it is combined with Saquinavir.
SecobarbitalThe metabolism of Nicardipine can be increased when combined with Secobarbital.
SildenafilThe metabolism of Sildenafil can be decreased when combined with Nicardipine.
SilodosinThe serum concentration of Silodosin can be increased when it is combined with Nicardipine.
SiltuximabThe serum concentration of Nicardipine can be decreased when it is combined with Siltuximab.
SimeprevirThe serum concentration of Nicardipine can be increased when it is combined with Simeprevir.
St. John's WortThe serum concentration of Nicardipine can be decreased when it is combined with St. John's Wort.
StiripentolThe serum concentration of Nicardipine can be increased when it is combined with Stiripentol.
SulfisoxazoleThe metabolism of Nicardipine can be decreased when combined with Sulfisoxazole.
TacrolimusThe serum concentration of Tacrolimus can be increased when it is combined with Nicardipine.
TadalafilTadalafil may increase the antihypertensive activities of Nicardipine.
TamoxifenThe serum concentration of the active metabolites of Tamoxifen can be reduced when Tamoxifen is used in combination with Nicardipine resulting in a loss in efficacy.
TamsulosinTamsulosin may increase the hypotensive activities of Nicardipine.
TelithromycinThe metabolism of Nicardipine can be decreased when combined with Telithromycin.
TerazosinTerazosin may increase the hypotensive activities of Nicardipine.
TesmilifeneThe serum concentration of Nicardipine can be decreased when it is combined with Tesmilifene.
ThioridazineThe serum concentration of Thioridazine can be increased when it is combined with Nicardipine.
TocilizumabThe serum concentration of Nicardipine can be decreased when it is combined with Tocilizumab.
TopotecanThe serum concentration of Topotecan can be increased when it is combined with Nicardipine.
TramadolThe therapeutic efficacy of Tramadol can be decreased when used in combination with Nicardipine.
TranylcypromineTranylcypromine may increase the orthostatic hypotensive activities of Nicardipine.
TreprostinilTreprostinil may increase the hypotensive activities of Nicardipine.
ValsartanThe risk or severity of adverse effects can be increased when Valsartan is combined with Nicardipine.
VardenafilVardenafil may increase the antihypertensive activities of Nicardipine.
VecuroniumNicardipine may increase the neuromuscular blocking activities of Vecuronium.
VerapamilThe serum concentration of Nicardipine can be increased when it is combined with Verapamil.
VincristineThe serum concentration of Vincristine can be increased when it is combined with Nicardipine.
VoriconazoleThe risk or severity of adverse effects can be increased when Voriconazole is combined with Nicardipine.
YohimbineYohimbine may decrease the antihypertensive activities of Nicardipine.
Food Interactions
  • Grapefruit and grapefruit juice should be avoided throughout treatment. Grapefruit can increase serum levels of this product.
  • Take without regard to meals.

Targets

Kind
Protein
Organism
Human
Pharmacological action
yes
Actions
inhibitor
General Function:
Voltage-gated 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. 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. 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. Bell DC, Butcher AJ, Berrow NS, Page KM, Brust PF, Nesterova A, Stauderman KA, Seabrook GR, Nurnberg B, Dolphin AC: Biophysical properties, pharmacology, and modulation of human, neuronal L-type (alpha(1D), Ca(V)1.3) voltage-dependent calcium currents. J Neurophysiol. 2001 Feb;85(2):816-27. [PubMed:11160515 ]
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. 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
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. 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 preference for cGMP as a substrate.
Gene Name:
PDE1B
Uniprot ID:
Q01064
Molecular Weight:
61379.235 Da
References
  1. 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:
Protein heterodimerization activity
Specific Function:
This alpha-adrenergic receptor mediates its action by association with G proteins that activate a phosphatidylinositol-calcium second messenger system. Its effect is mediated by G(q) and G(11) proteins. Nuclear ADRA1A-ADRA1B heterooligomers regulate phenylephrine(PE)-stimulated ERK signaling in cardiac myocytes.
Gene Name:
ADRA1A
Uniprot ID:
P35348
Molecular Weight:
51486.005 Da
References
  1. Thayer SA, Welcome M, Chhabra A, Fairhurst AS: Effects of dihydropyridine calcium channel blocking drugs on rat brain muscarinic and alpha-adrenergic receptors. Biochem Pharmacol. 1985 Jan 15;34(2):175-80. [PubMed:2981533 ]
Kind
Protein
Organism
Human
Pharmacological action
unknown
Actions
antagonist
General Function:
Protein heterodimerization activity
Specific Function:
This alpha-adrenergic receptor mediates its action by association with G proteins that activate a phosphatidylinositol-calcium second messenger system. Its effect is mediated by G(q) and G(11) proteins. Nuclear ADRA1A-ADRA1B heterooligomers regulate phenylephrine (PE)-stimulated ERK signaling in cardiac myocytes.
Gene Name:
ADRA1B
Uniprot ID:
P35368
Molecular Weight:
56835.375 Da
References
  1. Thayer SA, Welcome M, Chhabra A, Fairhurst AS: Effects of dihydropyridine calcium channel blocking drugs on rat brain muscarinic and alpha-adrenergic receptors. Biochem Pharmacol. 1985 Jan 15;34(2):175-80. [PubMed:2981533 ]
Kind
Protein
Organism
Human
Pharmacological action
unknown
Actions
antagonist
General Function:
Alpha1-adrenergic receptor activity
Specific Function:
This alpha-adrenergic receptor mediates its effect through the influx of extracellular calcium.
Gene Name:
ADRA1D
Uniprot ID:
P25100
Molecular Weight:
60462.205 Da
References
  1. Thayer SA, Welcome M, Chhabra A, Fairhurst AS: Effects of dihydropyridine calcium channel blocking drugs on rat brain muscarinic and alpha-adrenergic receptors. Biochem Pharmacol. 1985 Jan 15;34(2):175-80. [PubMed:2981533 ]
Kind
Protein
Organism
Human
Pharmacological action
unknown
Actions
antagonist
General Function:
Phosphatidylinositol phospholipase c activity
Specific Function:
The muscarinic acetylcholine receptor mediates various cellular responses, including inhibition of adenylate cyclase, breakdown of phosphoinositides and modulation of potassium channels through the action of G proteins. Primary transducing effect is Pi turnover.
Gene Name:
CHRM1
Uniprot ID:
P11229
Molecular Weight:
51420.375 Da
References
  1. Thayer SA, Welcome M, Chhabra A, Fairhurst AS: Effects of dihydropyridine calcium channel blocking drugs on rat brain muscarinic and alpha-adrenergic receptors. Biochem Pharmacol. 1985 Jan 15;34(2):175-80. [PubMed:2981533 ]
Kind
Protein
Organism
Human
Pharmacological action
unknown
Actions
antagonist
General Function:
G-protein coupled acetylcholine receptor activity
Specific Function:
The muscarinic acetylcholine receptor mediates various cellular responses, including inhibition of adenylate cyclase, breakdown of phosphoinositides and modulation of potassium channels through the action of G proteins. Primary transducing effect is adenylate cyclase inhibition. Signaling promotes phospholipase C activity, leading to the release of inositol trisphosphate (IP3); this then trigge...
Gene Name:
CHRM2
Uniprot ID:
P08172
Molecular Weight:
51714.605 Da
References
  1. Thayer SA, Welcome M, Chhabra A, Fairhurst AS: Effects of dihydropyridine calcium channel blocking drugs on rat brain muscarinic and alpha-adrenergic receptors. Biochem Pharmacol. 1985 Jan 15;34(2):175-80. [PubMed:2981533 ]
Kind
Protein
Organism
Human
Pharmacological action
unknown
Actions
antagonist
General Function:
Receptor activity
Specific Function:
The muscarinic acetylcholine receptor mediates various cellular responses, including inhibition of adenylate cyclase, breakdown of phosphoinositides and modulation of potassium channels through the action of G proteins. Primary transducing effect is Pi turnover.
Gene Name:
CHRM3
Uniprot ID:
P20309
Molecular Weight:
66127.445 Da
References
  1. Thayer SA, Welcome M, Chhabra A, Fairhurst AS: Effects of dihydropyridine calcium channel blocking drugs on rat brain muscarinic and alpha-adrenergic receptors. Biochem Pharmacol. 1985 Jan 15;34(2):175-80. [PubMed:2981533 ]
Kind
Protein
Organism
Human
Pharmacological action
unknown
Actions
antagonist
General Function:
Guanyl-nucleotide exchange factor activity
Specific Function:
The muscarinic acetylcholine receptor mediates various cellular responses, including inhibition of adenylate cyclase, breakdown of phosphoinositides and modulation of potassium channels through the action of G proteins. Primary transducing effect is inhibition of adenylate cyclase.
Gene Name:
CHRM4
Uniprot ID:
P08173
Molecular Weight:
53048.65 Da
References
  1. Thayer SA, Welcome M, Chhabra A, Fairhurst AS: Effects of dihydropyridine calcium channel blocking drugs on rat brain muscarinic and alpha-adrenergic receptors. Biochem Pharmacol. 1985 Jan 15;34(2):175-80. [PubMed:2981533 ]
Kind
Protein
Organism
Human
Pharmacological action
unknown
Actions
antagonist
General Function:
Phosphatidylinositol phospholipase c activity
Specific Function:
The muscarinic acetylcholine receptor mediates various cellular responses, including inhibition of adenylate cyclase, breakdown of phosphoinositides and modulation of potassium channels through the action of G proteins. Primary transducing effect is Pi turnover.
Gene Name:
CHRM5
Uniprot ID:
P08912
Molecular Weight:
60073.205 Da
References
  1. Thayer SA, Welcome M, Chhabra A, Fairhurst AS: Effects of dihydropyridine calcium channel blocking drugs on rat brain muscarinic and alpha-adrenergic receptors. Biochem Pharmacol. 1985 Jan 15;34(2):175-80. [PubMed:2981533 ]
Kind
Protein
Organism
Human
Pharmacological action
unknown
Actions
other/unknown
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. Thayer SA, Fairhurst AS: The interaction of dihydropyridine calcium channel blockers with calmodulin and calmodulin inhibitors. Mol Pharmacol. 1983 Jul;24(1):6-9. [PubMed:6865927 ]

Enzymes

Kind
Protein
Organism
Human
Pharmacological action
unknown
Actions
substrateinhibitorinducer
General Function:
Vitamin d3 25-hydroxylase activity
Specific Function:
Cytochromes P450 are a group of heme-thiolate monooxygenases. In liver microsomes, this enzyme is involved in an NADPH-dependent electron transport pathway. It performs a variety of oxidation reactions (e.g. caffeine 8-oxidation, omeprazole sulphoxidation, midazolam 1'-hydroxylation and midazolam 4-hydroxylation) of structurally unrelated compounds, including steroids, fatty acids, and xenobiot...
Gene Name:
CYP3A4
Uniprot ID:
P08684
Molecular Weight:
57342.67 Da
References
  1. 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
substrateinhibitor
General Function:
Steroid hydroxylase activity
Specific Function:
Responsible for the metabolism of many drugs and environmental chemicals that it oxidizes. It is involved in the metabolism of drugs such as antiarrhythmics, adrenoceptor antagonists, and tricyclic antidepressants.
Gene Name:
CYP2D6
Uniprot ID:
P10635
Molecular Weight:
55768.94 Da
References
  1. 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
inhibitorinducer
General Function:
Steroid hydroxylase activity
Specific Function:
Cytochromes P450 are a group of heme-thiolate monooxygenases. In liver microsomes, this enzyme is involved in an NADPH-dependent electron transport pathway. It oxidizes a variety of structurally unrelated compounds, including steroids, fatty acids, and xenobiotics. This enzyme contributes to the wide pharmacokinetics variability of the metabolism of drugs such as S-warfarin, diclofenac, phenyto...
Gene Name:
CYP2C9
Uniprot ID:
P11712
Molecular Weight:
55627.365 Da
References
  1. 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 a number of therapeutic agents such as the anticonvulsant drug S-mephenytoin, omeprazole, proguanil, certain barbiturates, diazepam, propranolol, citalopram and imipramine.
Gene Name:
CYP2C19
Uniprot ID:
P33261
Molecular Weight:
55930.545 Da
References
  1. Preissner S, Kroll K, Dunkel M, Senger C, Goldsobel G, Kuzman D, Guenther S, Winnenburg R, Schroeder M, Preissner R: SuperCYP: a comprehensive database on Cytochrome P450 enzymes including a tool for analysis of CYP-drug interactions. Nucleic Acids Res. 2010 Jan;38(Database issue):D237-43. doi: 10.1093/nar/gkp970. Epub 2009 Nov 24. [PubMed:19934256 ]
Kind
Protein
Organism
Human
Pharmacological action
unknown
Actions
substrateinhibitor
General Function:
Steroid hydroxylase activity
Specific Function:
Cytochromes P450 are a group of heme-thiolate monooxygenases. In liver microsomes, this enzyme is involved in an NADPH-dependent electron transport pathway. It oxidizes a variety of structurally unrelated compounds, including steroids, fatty acids, and xenobiotics. In the epoxidation of arachidonic acid it generates only 14,15- and 11,12-cis-epoxyeicosatrienoic acids. It is the principal enzyme...
Gene Name:
CYP2C8
Uniprot ID:
P10632
Molecular Weight:
55824.275 Da
References
  1. Preissner S, Kroll K, Dunkel M, Senger C, Goldsobel G, Kuzman D, Guenther S, Winnenburg R, Schroeder M, Preissner R: SuperCYP: a comprehensive database on Cytochrome P450 enzymes including a tool for analysis of CYP-drug interactions. Nucleic Acids Res. 2010 Jan;38(Database issue):D237-43. doi: 10.1093/nar/gkp970. Epub 2009 Nov 24. [PubMed:19934256 ]
Kind
Protein
Organism
Human
Pharmacological action
unknown
Actions
inducer
General Function:
Steroid hydroxylase activity
Specific Function:
Cytochromes P450 are a group of heme-thiolate monooxygenases. In liver microsomes, this enzyme is involved in an NADPH-dependent electron transport pathway. It oxidizes a variety of structurally unrelated compounds, including steroids, fatty acids, and xenobiotics. Acts as a 1,4-cineole 2-exo-monooxygenase.
Gene Name:
CYP2B6
Uniprot ID:
P20813
Molecular Weight:
56277.81 Da
References
  1. Preissner S, Kroll K, Dunkel M, Senger C, Goldsobel G, Kuzman D, Guenther S, Winnenburg R, Schroeder M, Preissner R: SuperCYP: a comprehensive database on Cytochrome P450 enzymes including a tool for analysis of CYP-drug interactions. Nucleic Acids Res. 2010 Jan;38(Database issue):D237-43. doi: 10.1093/nar/gkp970. Epub 2009 Nov 24. [PubMed:19934256 ]
Kind
Protein
Organism
Human
Pharmacological action
unknown
Actions
substrate
General Function:
Steroid hydroxylase activity
Specific Function:
Metabolizes several precarcinogens, drugs, and solvents to reactive metabolites. Inactivates a number of drugs and xenobiotics and also bioactivates many xenobiotic substrates to their hepatotoxic or carcinogenic forms.
Gene Name:
CYP2E1
Uniprot ID:
P05181
Molecular Weight:
56848.42 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:
Oxygen binding
Specific Function:
Cytochromes P450 are a group of heme-thiolate monooxygenases. In liver microsomes, this enzyme is involved in an NADPH-dependent electron transport pathway. It oxidizes a variety of structurally unrelated compounds, including steroids, fatty acids, and xenobiotics.
Gene Name:
CYP3A5
Uniprot ID:
P20815
Molecular Weight:
57108.065 Da
References
  1. Preissner S, Kroll K, Dunkel M, Senger C, Goldsobel G, Kuzman D, Guenther S, Winnenburg R, Schroeder M, Preissner R: SuperCYP: a comprehensive database on Cytochrome P450 enzymes including a tool for analysis of CYP-drug interactions. Nucleic Acids Res. 2010 Jan;38(Database issue):D237-43. doi: 10.1093/nar/gkp970. Epub 2009 Nov 24. [PubMed:19934256 ]

Transporters

Kind
Protein
Organism
Human
Pharmacological action
unknown
Actions
substrateinhibitor
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. Katoh M, Nakajima M, Yamazaki H, Yokoi T: Inhibitory potencies of 1,4-dihydropyridine calcium antagonists to P-glycoprotein-mediated transport: comparison with the effects on CYP3A4. Pharm Res. 2000 Oct;17(10):1189-97. [PubMed:11145223 ]
  2. Lentz KA, Polli JW, Wring SA, Humphreys JE, Polli JE: Influence of passive permeability on apparent P-glycoprotein kinetics. Pharm Res. 2000 Dec;17(12):1456-60. [PubMed:11303953 ]
  3. 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 ]
  4. Takara K, Sakaeda T, Tanigawara Y, Nishiguchi K, Ohmoto N, Horinouchi M, Komada F, Ohnishi N, Yokoyama T, Okumura K: Effects of 12 Ca2+ antagonists on multidrug resistance, MDR1-mediated transport and MDR1 mRNA expression. Eur J Pharm Sci. 2002 Aug;16(3):159-65. [PubMed:12128170 ]
  5. Schwab D, Fischer H, Tabatabaei A, Poli S, Huwyler J: Comparison of in vitro P-glycoprotein screening assays: recommendations for their use in drug discovery. J Med Chem. 2003 Apr 24;46(9):1716-25. [PubMed:12699389 ]
  6. Ibrahim S, Peggins J, Knapton A, Licht T, Aszalos A: Influence of antipsychotic, antiemetic, and Ca(2+) channel blocker drugs on the cellular accumulation of the anticancer drug daunorubicin: P-glycoprotein modulation. J Pharmacol Exp Ther. 2000 Dec;295(3):1276-83. [PubMed:11082465 ]
  7. Polli JW, Wring SA, Humphreys JE, Huang L, Morgan JB, Webster LO, Serabjit-Singh CS: Rational use of in vitro P-glycoprotein assays in drug discovery. J Pharmacol Exp Ther. 2001 Nov;299(2):620-8. [PubMed:11602674 ]
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Drug created on June 13, 2005 07:24 / Updated on May 24, 2016 02:06