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Identification
NameNimodipine
Accession NumberDB00393  (APRD00612)
TypeSmall Molecule
GroupsApproved
Description

Nimodipine is a 1,4-dihydropyridine calcium channel blocker. 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, nimodipine prevents calcium-dependent smooth muscle contraction and subsequent vasoconstriction. Compared to other calcium channel blocking agents, nimodipine exhibits greater effects on cerebral circulation than on peripheral circulation. Nimodipine is used to as an adjunct to improve the neurologic outcome following subarachnoid hemorrhage from ruptured intracranial aneurysm.

Structure
Thumb
Synonyms
2,6-Dimethyl-4-(3'-nitrophenyl)-1,4-dihydropyridine-3,5-dicarboxylic acid 3-beta-methoxyethyl ester 5-isopropyl ester
BAY e 9736
Isopropyl 2-methoxyethyl 1,4-dihydro-2,6-dimethyl-4-(3-nitrophenyl)-3,5-pyridinedicarboxylate
Isopropyl 2-methoxyethyl 1,4-dihydro-2,6-dimethyl-4-(m-nitrophenyl)-3,5-pyridinedicarboxylate
Nimodipine
Nimodipino
Nimodipinum
Nimotop
Periplum
External Identifiers Not Available
Approved Prescription Products
NameDosageStrengthRouteLabellerMarketing StartMarketing End
Nimotoptablet30 mgoralBayer Inc2009-07-24Not applicableCanada
Nimotop - Cap 30mgcapsule30 mgoralBayer Inc1989-12-312009-08-06Canada
Nimotop Cap 30mgcapsule30 mgoralMiles Canada Inc. Pharmaceutical Division1989-12-311996-10-02Canada
Nimotop I.V.-0.2mg/mlliquid.2 mgintravenousBayer Inc1996-10-082000-09-19Canada
Nimotop IV 0.2mg/mlliquid0.2 mgintravenousMiles Canada Inc. Pharmaceutical Division1992-12-312000-08-01Canada
Nymalizesolution60 mg/20mLoralArbor Pharmaceuticals2013-06-03Not applicableUs
Approved Generic Prescription Products
NameDosageStrengthRouteLabellerMarketing StartMarketing End
Nimodipinecapsule, liquid filled30 mg/1oralHeritage2008-03-21Not applicableUs
Nimodipinecapsule, liquid filled30 mg/1oralAmerican Health Packaging2015-02-15Not applicableUs
Nimodipinecapsule, liquid filled30 mg/1oralAscend Laboratories, LLC2015-01-01Not applicableUs
Nimodipinecapsule30 mg/1oralANI Pharmaceuticals, Inc.2015-11-01Not applicableUs
Nimodipinecapsule, liquid filled30 mg/1oralGolden State Medical Supply, Inc.2008-03-21Not applicableUs
Nimodipinecapsule30 mg/1oralCaraco Pharmaceutical Laboratories, Ltd.2007-06-28Not applicableUs
Nimodipinecapsule, liquid filled30 mg/1oralMajor Pharmaceuticals2015-01-01Not applicableUs
Nimodipinecapsule30 mg/1oralCardinal Health2007-06-28Not applicableUs
Nimodipinecapsule, liquid filled30 mg/1oralCardinal Health2008-03-21Not applicableUs
Approved Over the Counter ProductsNot Available
Unapproved/Other Products Not Available
International Brands
NameCompany
PeriplumNot Available
Brand mixturesNot Available
SaltsNot Available
Categories
UNII57WA9QZ5WH
CAS number66085-59-4
WeightAverage: 418.4403
Monoisotopic: 418.174001196
Chemical FormulaC21H26N2O7
InChI KeyInChIKey=UIAGMCDKSXEBJQ-UHFFFAOYSA-N
InChI
InChI=1S/C21H26N2O7/c1-12(2)30-21(25)18-14(4)22-13(3)17(20(24)29-10-9-28-5)19(18)15-7-6-8-16(11-15)23(26)27/h6-8,11-12,19,22H,9-10H2,1-5H3
IUPAC Name
3-(2-methoxyethyl) 5-propan-2-yl 2,6-dimethyl-4-(3-nitrophenyl)-1,4-dihydropyridine-3,5-dicarboxylate
SMILES
COCCOC(=O)C1=C(C)NC(C)=C(C1C1=CC(=CC=C1)[N+]([O-])=O)C(=O)OC(C)C
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
  • Benzenoid
  • Dicarboxylic acid or derivatives
  • Monocyclic benzene moiety
  • Vinylogous amide
  • Alpha,beta-unsaturated carboxylic ester
  • Enoate ester
  • Organic nitro compound
  • 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
  • Ether
  • Enamine
  • Dialkyl ether
  • 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
IndicationFor use as an adjunct to improve neurologic outcome following subarachnoid hemorrhage (SAH) from ruptured intracranial berry aneurysms by reducing the incidence and severity of ischemic deficits.
PharmacodynamicsNimodipine belongs to the class of pharmacological agents known as calcium channel blockers. Nimodipine is indicated for the improvement of neurological outcome by reducing the incidence and severity of ischemic deficits in patients with subarachnoid hemorrhage from ruptured congenital aneurysms who are in good neurological condition post-ictus (e.g., Hunt and Hess Grades I-III). The contractile processes of smooth muscle cells are dependent upon calcium ions, which enter these cells during depolarization as slow ionic transmembrane currents. Nimodipine inhibits calcium ion transfer into these cells and thus inhibits contractions of vascular smooth muscle. In animal experiments, nimodipine had a greater effect on cerebral arteries than on arteries elsewhere in the body perhaps because it is highly lipophilic, allowing it to cross the blood brain barrier.
Mechanism of actionAlthough the precise mechanism of action is not known, nimodipine blocks intracellular influx of calcium through voltage-dependent and receptor-operated slow calcium channels across the membranes of myocardial, vascular smooth muscle, and neuronal cells. Nimodipine binds specifically to L-type voltage-gated calcium channels. The inhibition of calcium ion transfer results in the inhibition of vascular smooth muscle contraction. Evidence suggests that the dilation of small cerebral resistance vessels, with a resultant increase in collateral circulation, and/or a direct effect involving the prevention of calcium overload in neurons may be responsible for nimodipine's clinical effect in patients with subarachnoid hemorrhage.
Related Articles
AbsorptionIn humans, nimodipine is rapidly absorbed after oral administration, and peak concentrations are generally attained within one hour. Bioavailability is 100% following intravenous administration and 3-30% following oral administration due to extensive first-pass metabolism.
Volume of distributionNot Available
Protein binding95% bound to plasma protein
Metabolism

Hepatic metabolism via CYP 3A4.

Route of eliminationNimodipine is eliminated almost exclusively in the form of metabolites and less than 1% is recovered in the urine as unchanged drug. Numerous metabolites, all of which are either inactive or considerably less active than the parent compound, have been identified.
Half life1.7-9 hours
ClearanceNot Available
ToxicitySymptoms of overdosage would be expected to be related to cardiovascular effects such as excessive peripheral vasodilation with marked systemic hypotension.
Affected organisms
  • Humans and other mammals
Pathways
PathwayCategorySMPDB ID
Nimodipine Action PathwayDrug actionSMP00380
SNP Mediated EffectsNot Available
SNP Mediated Adverse Drug ReactionsNot Available
ADMET
Predicted ADMET features
PropertyValueProbability
Human Intestinal Absorption+0.9387
Blood Brain Barrier-0.9358
Caco-2 permeable-0.5838
P-glycoprotein substrateSubstrate0.752
P-glycoprotein inhibitor IInhibitor0.9287
P-glycoprotein inhibitor IIInhibitor0.9098
Renal organic cation transporterNon-inhibitor0.8178
CYP450 2C9 substrateNon-substrate0.8151
CYP450 2D6 substrateNon-substrate0.9118
CYP450 3A4 substrateSubstrate0.7571
CYP450 1A2 substrateInhibitor0.9108
CYP450 2C9 inhibitorInhibitor0.8949
CYP450 2D6 inhibitorNon-inhibitor0.9231
CYP450 2C19 inhibitorInhibitor0.8994
CYP450 3A4 inhibitorInhibitor0.8248
CYP450 inhibitory promiscuityHigh CYP Inhibitory Promiscuity0.8557
Ames testNon AMES toxic0.5976
CarcinogenicityNon-carcinogens0.6953
BiodegradationNot ready biodegradable0.8797
Rat acute toxicity2.5326 LD50, mol/kg Not applicable
hERG inhibition (predictor I)Weak inhibitor0.6468
hERG inhibition (predictor II)Non-inhibitor0.8734
ADMET data is predicted using admetSAR, a free tool for evaluating chemical ADMET properties. (23092397 )
Pharmacoeconomics
Manufacturers
  • Banner pharmacaps inc
  • Barr laboratories inc
  • Sun pharmaceutical industries inc
  • Bayer pharmaceuticals corp
Packagers
Dosage forms
FormRouteStrength
Capsuleoral30 mg/1
Capsule, liquid filledoral30 mg/1
Tabletoral30 mg
Capsuleoral30 mg
Liquidintravenous.2 mg
Liquidintravenous0.2 mg
Solutionoral60 mg/20mL
Prices
Unit descriptionCostUnit
NiMODipine 100 30 mg capsule Box952.07USD box
Nimotop 30 mg capsule9.87USD capsule
Nimodipine 30 mg capsule9.69USD capsule
DrugBank does not sell nor buy drugs. Pricing information is supplied for informational purposes only.
PatentsNot Available
Properties
StateSolid
Experimental Properties
PropertyValueSource
melting point125 °CNot Available
logP3.05MASUMOTO,K ET AL. (1995)
Predicted Properties
PropertyValueSource
Water Solubility0.012 mg/mLALOGPS
logP3.41ALOGPS
logP2.54ChemAxon
logS-4.5ALOGPS
pKa (Strongest Basic)5.41ChemAxon
Physiological Charge0ChemAxon
Hydrogen Acceptor Count6ChemAxon
Hydrogen Donor Count1ChemAxon
Polar Surface Area119.68 Å2ChemAxon
Rotatable Bond Count10ChemAxon
Refractivity112.38 m3·mol-1ChemAxon
Polarizability43.17 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 ReferenceNot Available
General References
  1. Janjua N, Mayer SA: Cerebral vasospasm after subarachnoid hemorrhage. Curr Opin Crit Care. 2003 Apr;9(2):113-9. [PubMed:12657973 ]
  2. Allen GS, Ahn HS, Preziosi TJ, Battye R, Boone SC, Boone SC, Chou SN, Kelly DL, Weir BK, Crabbe RA, Lavik PJ, Rosenbloom SB, Dorsey FC, Ingram CR, Mellits DE, Bertsch LA, Boisvert DP, Hundley MB, Johnson RK, Strom JA, Transou CR: Cerebral arterial spasm--a controlled trial of nimodipine in patients with subarachnoid hemorrhage. N Engl J Med. 1983 Mar 17;308(11):619-24. [PubMed:6338383 ]
  3. Belfort MA, Anthony J, Saade GR, Allen JC Jr: A comparison of magnesium sulfate and nimodipine for the prevention of eclampsia. N Engl J Med. 2003 Jan 23;348(4):304-11. [PubMed:12540643 ]
  4. Kim JH, Park IS, Park KB, Kang DH, Hwang SH: Intraarterial nimodipine infusion to treat symptomatic cerebral vasospasm after aneurysmal subarachnoid hemorrhage. J Korean Neurosurg Soc. 2009 Sep;46(3):239-44. doi: 10.3340/jkns.2009.46.3.239. Epub 2009 Sep 30. [PubMed:19844625 ]
  5. Tomassoni D, Lanari A, Silvestrelli G, Traini E, Amenta F: Nimodipine and its use in cerebrovascular disease: evidence from recent preclinical and controlled clinical studies. Clin Exp Hypertens. 2008 Nov;30(8):744-66. doi: 10.1080/10641960802580232. [PubMed:19021025 ]
  6. Vergouwen MD, Vermeulen M, Roos YB: Effect of nimodipine on outcome in patients with traumatic subarachnoid haemorrhage: a systematic review. Lancet Neurol. 2006 Dec;5(12):1029-32. [PubMed:17110283 ]
External Links
ATC CodesC08CA06
AHFS Codes
  • 24:28.08
PDB EntriesNot Available
FDA labelDownload (504 KB)
MSDSDownload (73.3 KB)
Interactions
Drug Interactions
Drug
AcetaminophenThe metabolism of Nimodipine can be increased when combined with Acetaminophen.
AldesleukinThe risk or severity of adverse effects can be increased when Aldesleukin is combined with Nimodipine.
AlfuzosinAlfuzosin may increase the hypotensive activities of Nimodipine.
AlprazolamThe serum concentration of Nimodipine can be increased when it is combined with Alprazolam.
AmifostineNimodipine may increase the hypotensive activities of Amifostine.
AmiodaroneThe serum concentration of Nimodipine can be increased when it is combined with Amiodarone.
AmlodipineThe serum concentration of Nimodipine can be increased when it is combined with Amlodipine.
AmobarbitalThe metabolism of Nimodipine can be increased when combined with Amobarbital.
AprepitantThe serum concentration of Nimodipine can be increased when it is combined with Aprepitant.
ArmodafinilThe serum concentration of Nimodipine can be decreased when it is combined with Armodafinil.
AtazanavirThe serum concentration of Nimodipine can be increased when it is combined with Atazanavir.
AtorvastatinThe serum concentration of Nimodipine can be increased when it is combined with Atorvastatin.
AtosibanThe risk or severity of adverse effects can be increased when Nimodipine is combined with Atosiban.
Atracurium besylateNimodipine may increase the neuromuscular blocking activities of Atracurium besylate.
BepridilNimodipine may increase the hypotensive activities of Bepridil.
BexaroteneThe serum concentration of Nimodipine can be decreased when it is combined with Bexarotene.
BicalutamideThe serum concentration of Nimodipine can be increased when it is combined with Bicalutamide.
BoceprevirThe serum concentration of Nimodipine can be increased when it is combined with Boceprevir.
BosentanThe serum concentration of Nimodipine can be decreased when it is combined with Bosentan.
BrimonidineBrimonidine may increase the antihypertensive activities of Nimodipine.
ButabarbitalThe metabolism of Nimodipine can be increased when combined with Butabarbital.
ButalbitalThe metabolism of Nimodipine can be increased when combined with Butalbital.
ButethalThe metabolism of Nimodipine can be increased when combined with Butethal.
CaffeineThe metabolism of Nimodipine can be increased when combined with Caffeine.
CalcitriolThe serum concentration of Nimodipine can be decreased when it is combined with Calcitriol.
Calcium AcetateThe therapeutic efficacy of Nimodipine can be decreased when used in combination with Calcium Acetate.
Calcium carbonateThe therapeutic efficacy of Nimodipine can be decreased when used in combination with Calcium carbonate.
Calcium ChlorideThe therapeutic efficacy of Nimodipine can be decreased when used in combination with Calcium Chloride.
Calcium citrateThe therapeutic efficacy of Nimodipine can be decreased when used in combination with Calcium citrate.
Calcium gluconateThe therapeutic efficacy of Nimodipine can be decreased when used in combination with Calcium gluconate.
CarbamazepineThe serum concentration of Nimodipine can be decreased when it is combined with Carbamazepine.
CeritinibThe serum concentration of Nimodipine can be increased when it is combined with Ceritinib.
CilostazolThe serum concentration of Nimodipine can be increased when it is combined with Cilostazol.
CimetidineThe serum concentration of Nimodipine can be increased when it is combined with Cimetidine.
CiprofloxacinThe serum concentration of Nimodipine can be increased when it is combined with Ciprofloxacin.
Cisatracurium besylateNimodipine may increase the neuromuscular blocking activities of Cisatracurium besylate.
ClarithromycinThe serum concentration of Nimodipine can be increased when it is combined with Clarithromycin.
ClobazamThe serum concentration of Nimodipine can be decreased when it is combined with Clobazam.
ClopidogrelThe therapeutic efficacy of Clopidogrel can be decreased when used in combination with Nimodipine.
ClotrimazoleThe serum concentration of Nimodipine can be increased when it is combined with Clotrimazole.
CobicistatThe serum concentration of Nimodipine can be increased when it is combined with Cobicistat.
ConivaptanThe serum concentration of Nimodipine can be increased when it is combined with Conivaptan.
CrizotinibThe serum concentration of Nimodipine can be increased when it is combined with Crizotinib.
CyclosporineThe serum concentration of Nimodipine can be increased when it is combined with Cyclosporine.
DabrafenibThe serum concentration of Nimodipine can be decreased when it is combined with Dabrafenib.
DanazolThe serum concentration of Nimodipine can be increased when it is combined with Danazol.
DapoxetineDapoxetine may increase the orthostatic hypotensive activities of Nimodipine.
DarunavirThe serum concentration of Nimodipine can be increased when it is combined with Darunavir.
DasatinibThe serum concentration of Nimodipine can be increased when it is combined with Dasatinib.
DeferasiroxThe serum concentration of Nimodipine can be decreased when it is combined with Deferasirox.
DelavirdineThe serum concentration of Nimodipine can be increased when it is combined with Delavirdine.
DesvenlafaxineThe serum concentration of Nimodipine can be decreased when it is combined with Desvenlafaxine.
DexamethasoneThe serum concentration of Nimodipine can be decreased when it is combined with Dexamethasone.
DiazoxideDiazoxide may increase the hypotensive activities of Nimodipine.
DicloxacillinThe serum concentration of Nimodipine can be decreased when it is combined with Dicloxacillin.
DiltiazemThe serum concentration of Nimodipine can be increased when it is combined with Diltiazem.
DoxazosinDoxazosin may increase the hypotensive activities of Nimodipine.
DronedaroneThe serum concentration of Nimodipine can be increased when it is combined with Dronedarone.
DuloxetineNimodipine may increase the orthostatic hypotensive activities of Duloxetine.
EfavirenzThe serum concentration of Nimodipine can be decreased when it is combined with Efavirenz.
EnzalutamideThe serum concentration of Nimodipine can be decreased when it is combined with Enzalutamide.
ErythromycinThe metabolism of Nimodipine can be decreased when combined with Erythromycin.
Eslicarbazepine acetateThe serum concentration of Nimodipine can be decreased when it is combined with Eslicarbazepine acetate.
EstradiolThe serum concentration of Nimodipine can be decreased when it is combined with Estradiol.
EtravirineThe serum concentration of Nimodipine can be decreased when it is combined with Etravirine.
ExemestaneThe serum concentration of Nimodipine can be decreased when it is combined with Exemestane.
FelbamateThe serum concentration of Nimodipine can be decreased when it is combined with Felbamate.
FluconazoleThe serum concentration of Nimodipine can be increased when it is combined with Fluconazole.
FluoxetineThe serum concentration of Nimodipine can be increased when it is combined with Fluoxetine.
FluvoxamineThe serum concentration of Nimodipine can be increased when it is combined with Fluvoxamine.
FosamprenavirThe serum concentration of Nimodipine can be increased when it is combined with Fosamprenavir.
FosaprepitantThe serum concentration of Nimodipine can be increased when it is combined with Fosaprepitant.
FosphenytoinThe serum concentration of Nimodipine can be decreased when it is combined with Fosphenytoin.
Fusidic AcidThe serum concentration of Nimodipine can be increased when it is combined with Fusidic Acid.
Glycerol PhenylbutyrateThe serum concentration of Nimodipine can be increased when it is combined with Glycerol Phenylbutyrate.
GriseofulvinThe serum concentration of Nimodipine can be decreased when it is combined with Griseofulvin.
HeptabarbitalThe metabolism of Nimodipine can be increased when combined with Heptabarbital.
HexobarbitalThe metabolism of Nimodipine can be increased when combined with Hexobarbital.
HydrocortisoneThe serum concentration of Nimodipine can be decreased when it is combined with Hydrocortisone.
IdelalisibThe serum concentration of Nimodipine can be increased when it is combined with Idelalisib.
IloperidoneThe serum concentration of Nimodipine can be increased when it is combined with Iloperidone.
ImatinibThe serum concentration of Nimodipine can be increased when it is combined with Imatinib.
IndinavirThe serum concentration of Nimodipine can be increased when it is combined with Indinavir.
IsavuconazoniumThe serum concentration of Nimodipine can be decreased when it is combined with Isavuconazonium.
IsoniazidThe serum concentration of Nimodipine can be increased when it is combined with Isoniazid.
ItraconazoleThe serum concentration of Nimodipine can be increased when it is combined with Itraconazole.
IvacaftorThe serum concentration of Nimodipine can be increased when it is combined with Ivacaftor.
KetoconazoleThe serum concentration of Nimodipine can be increased when it is combined with Ketoconazole.
LapatinibThe serum concentration of Nimodipine can be increased when it is combined with Lapatinib.
LevodopaNimodipine may increase the orthostatic hypotensive activities of Levodopa.
LomitapideThe serum concentration of Nimodipine can be increased when it is combined with Lomitapide.
LuliconazoleThe serum concentration of Nimodipine can be increased when it is combined with Luliconazole.
LurasidoneThe serum concentration of Nimodipine can be increased when it is combined with Lurasidone.
Magnesium chlorideThe risk or severity of adverse effects can be increased when Nimodipine is combined with Magnesium chloride.
Magnesium citrateThe risk or severity of adverse effects can be increased when Nimodipine is combined with Magnesium citrate.
Magnesium hydroxideThe risk or severity of adverse effects can be increased when Nimodipine is combined with Magnesium hydroxide.
Magnesium oxideThe risk or severity of adverse effects can be increased when Nimodipine is combined with Magnesium oxide.
Magnesium salicylateThe risk or severity of adverse effects can be increased when Nimodipine is combined with Magnesium salicylate.
Magnesium SulfateThe risk or severity of adverse effects can be increased when Nimodipine is combined with Magnesium Sulfate.
Medroxyprogesterone acetateThe serum concentration of Nimodipine can be decreased when it is combined with Medroxyprogesterone Acetate.
MelatoninMelatonin may decrease the antihypertensive activities of Nimodipine.
MethohexitalThe metabolism of Nimodipine can be increased when combined with Methohexital.
MethylphenidateMethylphenidate may decrease the antihypertensive activities of Nimodipine.
MetyraponeThe serum concentration of Nimodipine can be decreased when it is combined with Metyrapone.
MifepristoneThe serum concentration of Nimodipine can be increased when it is combined with Mifepristone.
MitotaneThe serum concentration of Nimodipine can be decreased when it is combined with Mitotane.
ModafinilThe serum concentration of Nimodipine can be decreased when it is combined with Modafinil.
MolsidomineMolsidomine may increase the hypotensive activities of Nimodipine.
MoxonidineMoxonidine may increase the hypotensive activities of Nimodipine.
NafcillinThe metabolism of Nimodipine can be increased when combined with Nafcillin.
NefazodoneThe serum concentration of Nimodipine can be increased when it is combined with Nefazodone.
NelfinavirThe serum concentration of Nimodipine can be increased when it is combined with Nelfinavir.
NetupitantThe serum concentration of Nimodipine can be increased when it is combined with Netupitant.
NevirapineThe serum concentration of Nimodipine can be decreased when it is combined with Nevirapine.
NicardipineThe serum concentration of Nimodipine can be increased when it is combined with Nicardipine.
NicorandilNicorandil may increase the hypotensive activities of Nimodipine.
NilotinibThe serum concentration of Nimodipine can be increased when it is combined with Nilotinib.
NitroprussideNimodipine may increase the hypotensive activities of Nitroprusside.
ObinutuzumabNimodipine may increase the hypotensive activities of Obinutuzumab.
OritavancinThe serum concentration of Nimodipine can be decreased when it is combined with Oritavancin.
OxcarbazepineThe serum concentration of Nimodipine can be decreased when it is combined with Oxcarbazepine.
PaclitaxelThe serum concentration of Nimodipine can be decreased when it is combined with Paclitaxel.
PalbociclibThe serum concentration of Nimodipine can be increased when it is combined with Palbociclib.
PancuroniumNimodipine may increase the neuromuscular blocking activities of Pancuronium.
PazopanibThe serum concentration of Nimodipine can be increased when it is combined with Pazopanib.
PentobarbitalThe metabolism of Nimodipine can be increased when combined with Pentobarbital.
PentoxifyllinePentoxifylline may increase the hypotensive activities of Nimodipine.
PerampanelThe serum concentration of Nimodipine can be decreased when it is combined with Perampanel.
PhenelzinePhenelzine may increase the hypotensive activities of Nimodipine.
PhenobarbitalThe serum concentration of Nimodipine can be decreased when it is combined with Phenobarbital.
PhenoxybenzaminePhenoxybenzamine may increase the hypotensive activities of Nimodipine.
PhentolaminePhentolamine may increase the hypotensive activities of Nimodipine.
PhenytoinThe serum concentration of Nimodipine can be decreased when it is combined with Phenytoin.
PioglitazoneThe serum concentration of Nimodipine can be decreased when it is combined with Pioglitazone.
PosaconazoleThe serum concentration of Nimodipine can be increased when it is combined with Posaconazole.
PrazosinPrazosin may increase the hypotensive activities of Nimodipine.
PrednisoneThe serum concentration of Nimodipine can be decreased when it is combined with Prednisone.
PrimidoneThe serum concentration of Nimodipine can be decreased when it is combined with Primidone.
PropofolThe serum concentration of Nimodipine can be increased when it is combined with Propofol.
QuinidineThe serum concentration of Quinidine can be decreased when it is combined with Nimodipine.
QuinineQuinine may increase the hypotensive activities of Nimodipine.
RanolazineThe serum concentration of Nimodipine can be increased when it is combined with Ranolazine.
RifabutinThe serum concentration of Nimodipine can be decreased when it is combined with Rifabutin.
RifampicinThe serum concentration of Nimodipine can be decreased when it is combined with Rifampicin.
RifapentineThe serum concentration of Nimodipine can be decreased when it is combined with Rifapentine.
RisperidoneNimodipine may increase the hypotensive activities of Risperidone.
RitonavirThe serum concentration of Nimodipine can be increased when it is combined with Ritonavir.
RituximabNimodipine may increase the hypotensive activities of Rituximab.
RocuroniumNimodipine may increase the neuromuscular blocking activities of Rocuronium.
RufinamideThe serum concentration of Nimodipine can be decreased when it is combined with Rufinamide.
SaquinavirThe serum concentration of Nimodipine can be increased when it is combined with Saquinavir.
SecobarbitalThe metabolism of Nimodipine can be increased when combined with Secobarbital.
SilodosinSilodosin may increase the hypotensive activities of Nimodipine.
SiltuximabThe serum concentration of Nimodipine can be decreased when it is combined with Siltuximab.
SimeprevirThe serum concentration of Nimodipine can be increased when it is combined with Simeprevir.
St. John's WortThe serum concentration of Nimodipine can be decreased when it is combined with St. John's Wort.
StiripentolThe serum concentration of Nimodipine can be increased when it is combined with Stiripentol.
SulfisoxazoleThe metabolism of Nimodipine can be decreased when combined with Sulfisoxazole.
TacrolimusThe serum concentration of Tacrolimus can be increased when it is combined with Nimodipine.
TadalafilTadalafil may increase the antihypertensive activities of Nimodipine.
TamsulosinTamsulosin may increase the hypotensive activities of Nimodipine.
TelaprevirThe serum concentration of Nimodipine can be increased when it is combined with Telaprevir.
TelithromycinThe serum concentration of Nimodipine can be increased when it is combined with Telithromycin.
TerazosinTerazosin may increase the hypotensive activities of Nimodipine.
TerbinafineThe serum concentration of Nimodipine can be decreased when it is combined with Terbinafine.
TicagrelorThe serum concentration of Nimodipine can be increased when it is combined with Ticagrelor.
TiclopidineThe serum concentration of Nimodipine can be increased when it is combined with Ticlopidine.
TocilizumabThe serum concentration of Nimodipine can be decreased when it is combined with Tocilizumab.
TopiramateThe serum concentration of Nimodipine can be decreased when it is combined with Topiramate.
TrametinibThe serum concentration of Nimodipine can be decreased when it is combined with Trametinib.
TranylcypromineTranylcypromine may increase the hypotensive activities of Nimodipine.
TreprostinilTreprostinil may increase the hypotensive activities of Nimodipine.
ValsartanThe risk or severity of adverse effects can be increased when Valsartan is combined with Nimodipine.
VardenafilVardenafil may increase the antihypertensive activities of Nimodipine.
VecuroniumNimodipine may increase the neuromuscular blocking activities of Vecuronium.
VemurafenibThe serum concentration of Nimodipine can be decreased when it is combined with Vemurafenib.
VerapamilThe serum concentration of Nimodipine can be increased when it is combined with Verapamil.
VoriconazoleThe serum concentration of Nimodipine can be increased when it is combined with Voriconazole.
YohimbineYohimbine may decrease the antihypertensive activities of Nimodipine.
Food Interactions
  • Grapefruit down regulates post-translational expression of CYP3A4, the major metabolizing enzyme of nimodipine. Grapefruit, in all forms (e.g. whole fruit, juice and rind), can significantly increase serum levels of nimodipine and may cause toxicity. Avoid grapefruit products while on this medication.
  • Take at the same time each day, with or without food, but always in the same manner.

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. Marchetti C, Usai C: High affinity block by nimodipine of the internal calcium elevation in chronically depolarized rat cerebellar granule neurons. Neurosci Lett. 1996 Mar 29;207(2):77-80. [PubMed:8731425 ]
  3. Weant KA, Ramsey CN 3rd, Cook AM: Role of intraarterial therapy for cerebral vasospasm secondary to aneurysmal subarachnoid hemorrhage. Pharmacotherapy. 2010 Apr;30(4):405-17. doi: 10.1592/phco.30.4.405. [PubMed:20334460 ]
  4. Dong CJ, Guo Y, Agey P, Wheeler L, Hare WA: Nimodipine enhancement of alpha2 adrenergic modulation of NMDA receptor via a mechanism independent of Ca2+ channel blocking. Invest Ophthalmol Vis Sci. 2010 Aug;51(8):4174-80. doi: 10.1167/iovs.09-4613. Epub 2010 Mar 24. [PubMed:20335610 ]
  5. Kim JH, Park IS, Park KB, Kang DH, Hwang SH: Intraarterial nimodipine infusion to treat symptomatic cerebral vasospasm after aneurysmal subarachnoid hemorrhage. J Korean Neurosurg Soc. 2009 Sep;46(3):239-44. doi: 10.3340/jkns.2009.46.3.239. Epub 2009 Sep 30. [PubMed:19844625 ]
  6. Kumar R, Mehra R, Ray SB: L-type calcium channel blockers, morphine and pain: Newer insights. Indian J Anaesth. 2010 Mar;54(2):127-31. doi: 10.4103/0019-5049.63652. [PubMed:20661350 ]
  7. Keyrouz SG, Diringer MN: Clinical review: Prevention and therapy of vasospasm in subarachnoid hemorrhage. Crit Care. 2007;11(4):220. [PubMed:17705883 ]
  8. 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 ]
  2. Weant KA, Ramsey CN 3rd, Cook AM: Role of intraarterial therapy for cerebral vasospasm secondary to aneurysmal subarachnoid hemorrhage. Pharmacotherapy. 2010 Apr;30(4):405-17. doi: 10.1592/phco.30.4.405. [PubMed:20334460 ]
  3. Dong CJ, Guo Y, Agey P, Wheeler L, Hare WA: Nimodipine enhancement of alpha2 adrenergic modulation of NMDA receptor via a mechanism independent of Ca2+ channel blocking. Invest Ophthalmol Vis Sci. 2010 Aug;51(8):4174-80. doi: 10.1167/iovs.09-4613. Epub 2010 Mar 24. [PubMed:20335610 ]
  4. Kim JH, Park IS, Park KB, Kang DH, Hwang SH: Intraarterial nimodipine infusion to treat symptomatic cerebral vasospasm after aneurysmal subarachnoid hemorrhage. J Korean Neurosurg Soc. 2009 Sep;46(3):239-44. doi: 10.3340/jkns.2009.46.3.239. Epub 2009 Sep 30. [PubMed:19844625 ]
  5. Kumar R, Mehra R, Ray SB: L-type calcium channel blockers, morphine and pain: Newer insights. Indian J Anaesth. 2010 Mar;54(2):127-31. doi: 10.4103/0019-5049.63652. [PubMed:20661350 ]
  6. Keyrouz SG, Diringer MN: Clinical review: Prevention and therapy of vasospasm in subarachnoid hemorrhage. Crit Care. 2007;11(4):220. [PubMed:17705883 ]
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-1F gives rise to L-type calcium currents. Long-lasting (L-type) calcium channels belon...
Gene Name:
CACNA1F
Uniprot ID:
O60840
Molecular Weight:
220675.9 Da
References
  1. Weant KA, Ramsey CN 3rd, Cook AM: Role of intraarterial therapy for cerebral vasospasm secondary to aneurysmal subarachnoid hemorrhage. Pharmacotherapy. 2010 Apr;30(4):405-17. doi: 10.1592/phco.30.4.405. [PubMed:20334460 ]
  2. Dong CJ, Guo Y, Agey P, Wheeler L, Hare WA: Nimodipine enhancement of alpha2 adrenergic modulation of NMDA receptor via a mechanism independent of Ca2+ channel blocking. Invest Ophthalmol Vis Sci. 2010 Aug;51(8):4174-80. doi: 10.1167/iovs.09-4613. Epub 2010 Mar 24. [PubMed:20335610 ]
  3. Kim JH, Park IS, Park KB, Kang DH, Hwang SH: Intraarterial nimodipine infusion to treat symptomatic cerebral vasospasm after aneurysmal subarachnoid hemorrhage. J Korean Neurosurg Soc. 2009 Sep;46(3):239-44. doi: 10.3340/jkns.2009.46.3.239. Epub 2009 Sep 30. [PubMed:19844625 ]
  4. Kumar R, Mehra R, Ray SB: L-type calcium channel blockers, morphine and pain: Newer insights. Indian J Anaesth. 2010 Mar;54(2):127-31. doi: 10.4103/0019-5049.63652. [PubMed:20661350 ]
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 ]
  2. Weant KA, Ramsey CN 3rd, Cook AM: Role of intraarterial therapy for cerebral vasospasm secondary to aneurysmal subarachnoid hemorrhage. Pharmacotherapy. 2010 Apr;30(4):405-17. doi: 10.1592/phco.30.4.405. [PubMed:20334460 ]
  3. Dong CJ, Guo Y, Agey P, Wheeler L, Hare WA: Nimodipine enhancement of alpha2 adrenergic modulation of NMDA receptor via a mechanism independent of Ca2+ channel blocking. Invest Ophthalmol Vis Sci. 2010 Aug;51(8):4174-80. doi: 10.1167/iovs.09-4613. Epub 2010 Mar 24. [PubMed:20335610 ]
  4. Kim JH, Park IS, Park KB, Kang DH, Hwang SH: Intraarterial nimodipine infusion to treat symptomatic cerebral vasospasm after aneurysmal subarachnoid hemorrhage. J Korean Neurosurg Soc. 2009 Sep;46(3):239-44. doi: 10.3340/jkns.2009.46.3.239. Epub 2009 Sep 30. [PubMed:19844625 ]
  5. Kumar R, Mehra R, Ray SB: L-type calcium channel blockers, morphine and pain: Newer insights. Indian J Anaesth. 2010 Mar;54(2):127-31. doi: 10.4103/0019-5049.63652. [PubMed:20661350 ]
  6. Keyrouz SG, Diringer MN: Clinical review: Prevention and therapy of vasospasm in subarachnoid hemorrhage. Crit Care. 2007;11(4):220. [PubMed:17705883 ]
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:
CACNB1
Uniprot ID:
Q02641
Molecular Weight:
65712.995 Da
References
  1. Weant KA, Ramsey CN 3rd, Cook AM: Role of intraarterial therapy for cerebral vasospasm secondary to aneurysmal subarachnoid hemorrhage. Pharmacotherapy. 2010 Apr;30(4):405-17. doi: 10.1592/phco.30.4.405. [PubMed:20334460 ]
  2. Dong CJ, Guo Y, Agey P, Wheeler L, Hare WA: Nimodipine enhancement of alpha2 adrenergic modulation of NMDA receptor via a mechanism independent of Ca2+ channel blocking. Invest Ophthalmol Vis Sci. 2010 Aug;51(8):4174-80. doi: 10.1167/iovs.09-4613. Epub 2010 Mar 24. [PubMed:20335610 ]
  3. Kim JH, Park IS, Park KB, Kang DH, Hwang SH: Intraarterial nimodipine infusion to treat symptomatic cerebral vasospasm after aneurysmal subarachnoid hemorrhage. J Korean Neurosurg Soc. 2009 Sep;46(3):239-44. doi: 10.3340/jkns.2009.46.3.239. Epub 2009 Sep 30. [PubMed:19844625 ]
  4. Kumar R, Mehra R, Ray SB: L-type calcium channel blockers, morphine and pain: Newer insights. Indian J Anaesth. 2010 Mar;54(2):127-31. doi: 10.4103/0019-5049.63652. [PubMed:20661350 ]
  5. Keyrouz SG, Diringer MN: Clinical review: Prevention and therapy of vasospasm in subarachnoid hemorrhage. Crit Care. 2007;11(4):220. [PubMed:17705883 ]
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. Weant KA, Ramsey CN 3rd, Cook AM: Role of intraarterial therapy for cerebral vasospasm secondary to aneurysmal subarachnoid hemorrhage. Pharmacotherapy. 2010 Apr;30(4):405-17. doi: 10.1592/phco.30.4.405. [PubMed:20334460 ]
  3. Kim JH, Park IS, Park KB, Kang DH, Hwang SH: Intraarterial nimodipine infusion to treat symptomatic cerebral vasospasm after aneurysmal subarachnoid hemorrhage. J Korean Neurosurg Soc. 2009 Sep;46(3):239-44. doi: 10.3340/jkns.2009.46.3.239. Epub 2009 Sep 30. [PubMed:19844625 ]
  4. Kumar R, Mehra R, Ray SB: L-type calcium channel blockers, morphine and pain: Newer insights. Indian J Anaesth. 2010 Mar;54(2):127-31. doi: 10.4103/0019-5049.63652. [PubMed:20661350 ]
  5. Keyrouz SG, Diringer MN: Clinical review: Prevention and therapy of vasospasm in subarachnoid hemorrhage. Crit Care. 2007;11(4):220. [PubMed:17705883 ]
  6. 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:
CACNB3
Uniprot ID:
P54284
Molecular Weight:
54531.425 Da
References
  1. Weant KA, Ramsey CN 3rd, Cook AM: Role of intraarterial therapy for cerebral vasospasm secondary to aneurysmal subarachnoid hemorrhage. Pharmacotherapy. 2010 Apr;30(4):405-17. doi: 10.1592/phco.30.4.405. [PubMed:20334460 ]
  2. Dong CJ, Guo Y, Agey P, Wheeler L, Hare WA: Nimodipine enhancement of alpha2 adrenergic modulation of NMDA receptor via a mechanism independent of Ca2+ channel blocking. Invest Ophthalmol Vis Sci. 2010 Aug;51(8):4174-80. doi: 10.1167/iovs.09-4613. Epub 2010 Mar 24. [PubMed:20335610 ]
  3. Kim JH, Park IS, Park KB, Kang DH, Hwang SH: Intraarterial nimodipine infusion to treat symptomatic cerebral vasospasm after aneurysmal subarachnoid hemorrhage. J Korean Neurosurg Soc. 2009 Sep;46(3):239-44. doi: 10.3340/jkns.2009.46.3.239. Epub 2009 Sep 30. [PubMed:19844625 ]
  4. Kumar R, Mehra R, Ray SB: L-type calcium channel blockers, morphine and pain: Newer insights. Indian J Anaesth. 2010 Mar;54(2):127-31. doi: 10.4103/0019-5049.63652. [PubMed:20661350 ]
  5. Keyrouz SG, Diringer MN: Clinical review: Prevention and therapy of vasospasm in subarachnoid hemorrhage. Crit Care. 2007;11(4):220. [PubMed:17705883 ]
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:
CACNB4
Uniprot ID:
O00305
Molecular Weight:
58168.625 Da
References
  1. Weant KA, Ramsey CN 3rd, Cook AM: Role of intraarterial therapy for cerebral vasospasm secondary to aneurysmal subarachnoid hemorrhage. Pharmacotherapy. 2010 Apr;30(4):405-17. doi: 10.1592/phco.30.4.405. [PubMed:20334460 ]
  2. Dong CJ, Guo Y, Agey P, Wheeler L, Hare WA: Nimodipine enhancement of alpha2 adrenergic modulation of NMDA receptor via a mechanism independent of Ca2+ channel blocking. Invest Ophthalmol Vis Sci. 2010 Aug;51(8):4174-80. doi: 10.1167/iovs.09-4613. Epub 2010 Mar 24. [PubMed:20335610 ]
  3. Kim JH, Park IS, Park KB, Kang DH, Hwang SH: Intraarterial nimodipine infusion to treat symptomatic cerebral vasospasm after aneurysmal subarachnoid hemorrhage. J Korean Neurosurg Soc. 2009 Sep;46(3):239-44. doi: 10.3340/jkns.2009.46.3.239. Epub 2009 Sep 30. [PubMed:19844625 ]
  4. Kumar R, Mehra R, Ray SB: L-type calcium channel blockers, morphine and pain: Newer insights. Indian J Anaesth. 2010 Mar;54(2):127-31. doi: 10.4103/0019-5049.63652. [PubMed:20661350 ]
  5. Keyrouz SG, Diringer MN: Clinical review: Prevention and therapy of vasospasm in subarachnoid hemorrhage. Crit Care. 2007;11(4):220. [PubMed:17705883 ]
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
agonist
General Function:
Transcription regulatory region dna binding
Specific Function:
Ligand-activated transcriptional activator. Binds to the XRE promoter region of genes it activates. Activates the expression of multiple phase I and II xenobiotic chemical metabolizing enzyme genes (such as the CYP1A1 gene). Mediates biochemical and toxic effects of halogenated aromatic hydrocarbons. Involved in cell-cycle regulation. Likely to play an important role in the development and matu...
Gene Name:
AHR
Uniprot ID:
P35869
Molecular Weight:
96146.705 Da
References
  1. Hu W, Sorrentino C, Denison MS, Kolaja K, Fielden MR: Induction of cyp1a1 is a nonspecific biomarker of aryl hydrocarbon receptor activation: results of large scale screening of pharmaceuticals and toxicants in vivo and in vitro. Mol Pharmacol. 2007 Jun;71(6):1475-86. Epub 2007 Feb 27. [PubMed:17327465 ]

Enzymes

Kind
Protein
Organism
Human
Pharmacological action
unknown
Actions
substrate
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
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. 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 ]
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Drug created on June 13, 2005 07:24 / Updated on April 15, 2016 15:51