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Identification
NameMibefradil
Accession NumberDB01388
TypeSmall Molecule
GroupsWithdrawn
DescriptionMibefradil was withdrawn from the market in 1998 because of potentially harmful interactions with other drugs.
Structure
Thumb
SynonymsNot Available
External Identifiers Not Available
Approved Prescription ProductsNot Available
Approved Generic Prescription ProductsNot Available
Approved Over the Counter ProductsNot Available
Unapproved/Other Products Not Available
International Brands
NameCompany
PosicorNot Available
Brand mixturesNot Available
SaltsNot Available
Categories
UNII27B90X776A
CAS number116644-53-2
WeightAverage: 495.6287
Monoisotopic: 495.289720302
Chemical FormulaC29H38FN3O3
InChI KeyHBNPJJILLOYFJU-VMPREFPWSA-N
InChI
InChI=1S/C29H38FN3O3/c1-20(2)28-23-12-11-22(30)18-21(23)13-14-29(28,36-27(34)19-35-4)15-17-33(3)16-7-10-26-31-24-8-5-6-9-25(24)32-26/h5-6,8-9,11-12,18,20,28H,7,10,13-17,19H2,1-4H3,(H,31,32)/t28-,29-/m0/s1
IUPAC Name
(1S,2S)-2-(2-{[3-(1H-1,3-benzodiazol-2-yl)propyl](methyl)amino}ethyl)-6-fluoro-1-(propan-2-yl)-1,2,3,4-tetrahydronaphthalen-2-yl 2-methoxyacetate
SMILES
COCC(=O)O[C@]1(CCN(C)CCCC2=NC3=CC=CC=C3N2)CCC2=C(C=CC(F)=C2)[C@@H]1C(C)C
Pharmacology
IndicationFor the treatment of angina and high blood pressure.
Structured Indications Not Available
PharmacodynamicsMibefradil belongs to a group of medicines called calcium channel blocking agents, or, more commonly, calcium channel blockers. Calcium channel blocking agents affect the movement of calcium into the cells of the heart and blood vessels. As a result, they relax blood vessels and increase the supply of blood and oxygen to the heart while reducing its workload. Mibefradil is a benzimidazoyl-substituted tetraline that selectively binds and inhibits T-type calcium channels.
Mechanism of actionMibefradil is a tetralol calcium channel blocking agent that inhibits the influx of calcium ions across both the T (low-voltage) and L (high-voltage) calcium channels of cardiac and vascular smooth muscle, with a greater selectivity for T channels. Vasodilation occurs in vascular smooth muscle, causing a decrease in peripheral vascular resistance and a resulting decrease in blood pressure. Mibefradil causes a slight increase in cardiac output during chronic dosing. Mibefradil slows sinus and atrioventricular (AV) node conduction, producing a slight reduction in heart rate and a slight increase in the PR interval. It has also been shown to slightly lengthen the corrected sinus node recovery time and AH interval and to raise the Wenckebach point. The mechanism by which mibefradil reduces angina is not known, but is thought to be attributed to a reduction in heart rate, total peripheral resistance (afterload), and the heart rate–systolic blood pressure product at any given level of exercise. The result of these effects is a decrease in cardiac workload and myocardial oxygen demand.
TargetKindPharmacological actionActionsOrganismUniProt ID
Voltage-dependent T-type calcium channel subunit alpha-1GProteinyes
inhibitor
HumanO43497 details
Voltage-dependent T-type calcium channel subunit alpha-1HProteinyes
inhibitor
HumanO95180 details
Voltage-dependent L-type calcium channel subunit alpha-1CProteinyes
inhibitor
HumanQ13936 details
Voltage-dependent L-type calcium channel subunit alpha-1DProteinyes
inhibitor
HumanQ01668 details
Voltage-dependent L-type calcium channel subunit alpha-1FProteinyes
inhibitor
HumanO60840 details
Voltage-dependent T-type calcium channel subunit alpha-1IProteinyes
inhibitor
HumanQ9P0X4 details
Voltage-dependent L-type calcium channel subunit alpha-1SProteinyes
inhibitor
HumanQ13698 details
Voltage-dependent L-type calcium channel subunit beta-1Proteinyes
inhibitor
HumanQ02641 details
Voltage-dependent L-type calcium channel subunit beta-2Proteinyes
inhibitor
HumanQ08289 details
Voltage-dependent L-type calcium channel subunit beta-3Proteinyes
inhibitor
HumanP54284 details
Voltage-dependent L-type calcium channel subunit beta-4Proteinyes
inhibitor
HumanO00305 details
Related Articles
AbsorptionBioavailability after a single dose is 70%. After multiple dosing, the proportion of mibefradil undergoing first-pass metabolism is reduced, resulting in a steady state bioavailability of approximately 90%. Food does not affect the rate or extent of absorption of mibefradil.
Volume of distributionNot Available
Protein binding≥ 99%, primarily to alpha 1-acid glycoprotein.
Metabolism

The two metabolic pathways that mibefradil undergoes are esterase-catalyzed hydrolysis of the ester side chain (producing an alcohol metabolite) and cytochrome P450 3A4-catalyzed oxidation (that becomes less important during chronic dosing). The pharmacologic effect of the metabolite is approximately 10% of that of the parent mibefradil.

Route of eliminationNot Available
Half life17 to 25 hours at steady state.
ClearanceNot Available
ToxicityNot Available
Affected organisms
  • Humans and other mammals
PathwaysNot Available
SNP Mediated EffectsNot Available
SNP Mediated Adverse Drug ReactionsNot Available
Interactions
Drug Interactions
DrugInteractionDrug group
2-HYDROXY-1,4-NAPHTHOQUINONEThe risk or severity of adverse effects can be increased when 2-HYDROXY-1,4-NAPHTHOQUINONE is combined with Mibefradil.Experimental
2-mercaptobenzothiazoleThe risk or severity of adverse effects can be increased when 2-mercaptobenzothiazole is combined with Mibefradil.Vet Approved
7,8-DICHLORO-1,2,3,4-TETRAHYDROISOQUINOLINE7,8-DICHLORO-1,2,3,4-TETRAHYDROISOQUINOLINE may increase the hypotensive activities of Mibefradil.Experimental
AcebutololThe serum concentration of Acebutolol can be increased when it is combined with Mibefradil.Approved
AcetaminophenThe serum concentration of Acetaminophen can be increased when it is combined with Mibefradil.Approved
Acetylsalicylic acidThe serum concentration of Acetylsalicylic acid can be increased when it is combined with Mibefradil.Approved, Vet Approved
AfatinibThe serum concentration of Afatinib can be increased when it is combined with Mibefradil.Approved
AldosteroneThe serum concentration of Aldosterone can be increased when it is combined with Mibefradil.Experimental
AlfuzosinAlfuzosin may increase the hypotensive activities of Mibefradil.Approved, Investigational
AliskirenMibefradil may increase the hypotensive activities of Aliskiren.Approved, Investigational
AlitretinoinThe serum concentration of Alitretinoin can be increased when it is combined with Mibefradil.Approved, Investigational
AlprenololAlprenolol may increase the hypotensive activities of Mibefradil.Approved, Withdrawn
AmbrisentanThe serum concentration of Ambrisentan can be increased when it is combined with Mibefradil.Approved, Investigational
AmifostineMibefradil may increase the hypotensive activities of Amifostine.Approved, Investigational
AmiodaroneThe metabolism of Mibefradil can be decreased when combined with Amiodarone.Approved, Investigational
AmitriptylineThe serum concentration of Amitriptyline can be increased when it is combined with Mibefradil.Approved
AmlodipineAmlodipine may increase the hypotensive activities of Mibefradil.Approved
AmobarbitalThe metabolism of Mibefradil can be increased when combined with Amobarbital.Approved, Illicit
AmorolfineThe risk or severity of adverse effects can be increased when Amorolfine is combined with Mibefradil.Approved
Amphotericin BThe risk or severity of adverse effects can be increased when Amphotericin B is combined with Mibefradil.Approved, Investigational
AN2690The risk or severity of adverse effects can be increased when AN2690 is combined with Mibefradil.Investigational
AnidulafunginThe risk or severity of adverse effects can be increased when Anidulafungin is combined with Mibefradil.Approved, Investigational
ApixabanThe serum concentration of Apixaban can be increased when it is combined with Mibefradil.Approved
AprepitantThe serum concentration of Mibefradil can be increased when it is combined with Aprepitant.Approved, Investigational
Arsenic trioxideThe serum concentration of Arsenic trioxide can be increased when it is combined with Mibefradil.Approved, Investigational
ArtemetherThe risk or severity of adverse effects can be increased when Artemether is combined with Mibefradil.Approved
AtazanavirThe metabolism of Mibefradil can be decreased when combined with Atazanavir.Approved, Investigational
AtenololThe serum concentration of Atenolol can be increased when it is combined with Mibefradil.Approved
AtomoxetineThe metabolism of Mibefradil can be decreased when combined with Atomoxetine.Approved
AtosibanThe risk or severity of adverse effects can be increased when Mibefradil is combined with Atosiban.Approved
Atracurium besylateMibefradil may increase the neuromuscular blocking activities of Atracurium besylate.Approved
AxitinibThe serum concentration of Axitinib can be increased when it is combined with Mibefradil.Approved, Investigational
Bafilomycin A1The risk or severity of adverse effects can be increased when Bafilomycin A1 is combined with Mibefradil.Experimental
BarbexacloneThe metabolism of Mibefradil can be increased when combined with Barbexaclone.Experimental
BarbitalThe metabolism of Mibefradil can be increased when combined with Barbital.Illicit
BenazeprilBenazepril may increase the hypotensive activities of Mibefradil.Approved, Investigational
BendroflumethiazideBendroflumethiazide may increase the hypotensive activities of Mibefradil.Approved
BenmoxinBenmoxin may increase the hypotensive activities of Mibefradil.Withdrawn
Benzoic AcidThe risk or severity of adverse effects can be increased when Benzoic Acid is combined with Mibefradil.Approved
BepridilBepridil may increase the hypotensive activities of Mibefradil.Approved, Withdrawn
BetamethasoneThe serum concentration of Betamethasone can be increased when it is combined with Mibefradil.Approved, Vet Approved
BetaxololBetaxolol may increase the hypotensive activities of Mibefradil.Approved
BethanidineBethanidine may increase the hypotensive activities of Mibefradil.Approved
BexaroteneThe serum concentration of Mibefradil can be decreased when it is combined with Bexarotene.Approved, Investigational
BifonazoleThe risk or severity of adverse effects can be increased when Bifonazole is combined with Mibefradil.Approved
BimatoprostBimatoprost may increase the hypotensive activities of Mibefradil.Approved, Investigational
BisoprololBisoprolol may increase the hypotensive activities of Mibefradil.Approved
BoceprevirThe metabolism of Mibefradil can be decreased when combined with Boceprevir.Approved
BortezomibThe metabolism of Mibefradil can be decreased when combined with Bortezomib.Approved, Investigational
BosentanThe serum concentration of Mibefradil can be decreased when it is combined with Bosentan.Approved, Investigational
BosutinibThe serum concentration of Bosutinib can be increased when it is combined with Mibefradil.Approved
Brentuximab vedotinThe serum concentration of Brentuximab vedotin can be increased when it is combined with Mibefradil.Approved
BretyliumBretylium may increase the hypotensive activities of Mibefradil.Approved
BrimonidineBrimonidine may increase the hypotensive activities of Mibefradil.Approved
BrimonidineBrimonidine may increase the antihypertensive activities of Mibefradil.Approved
BromocriptineThe serum concentration of Bromocriptine can be increased when it is combined with Mibefradil.Approved, Investigational
BucindololBucindolol may increase the hypotensive activities of Mibefradil.Investigational
BupranololMibefradil may increase the hypotensive activities of Bupranolol.Approved
ButenafineThe risk or severity of adverse effects can be increased when Butenafine is combined with Mibefradil.Approved
ButoconazoleThe risk or severity of adverse effects can be increased when Butoconazole is combined with Mibefradil.Approved
CabazitaxelThe serum concentration of Cabazitaxel can be increased when it is combined with Mibefradil.Approved
CaffeineThe serum concentration of Caffeine can be increased when it is combined with Mibefradil.Approved
CalciumThe therapeutic efficacy of Mibefradil can be decreased when used in combination with Calcium.Nutraceutical
Calcium AcetateThe therapeutic efficacy of Mibefradil can be decreased when used in combination with Calcium Acetate.Approved
Calcium carbonateThe therapeutic efficacy of Mibefradil can be decreased when used in combination with Calcium carbonate.Approved
Calcium ChlorideThe therapeutic efficacy of Mibefradil can be decreased when used in combination with Calcium Chloride.Approved
Calcium citrateThe therapeutic efficacy of Mibefradil can be decreased when used in combination with Calcium citrate.Approved
Calcium glubionateThe therapeutic efficacy of Mibefradil can be decreased when used in combination with Calcium glubionate.Approved
Calcium GluceptateThe therapeutic efficacy of Mibefradil can be decreased when used in combination with Calcium Gluceptate.Approved
Calcium gluconateThe therapeutic efficacy of Mibefradil can be decreased when used in combination with Calcium gluconate.Approved, Vet Approved
CamptothecinThe serum concentration of Camptothecin can be increased when it is combined with Mibefradil.Experimental
CanagliflozinThe serum concentration of Canagliflozin can be increased when it is combined with Mibefradil.Approved
CandesartanCandesartan may increase the hypotensive activities of Mibefradil.Approved
CandicidinThe risk or severity of adverse effects can be increased when Candicidin is combined with Mibefradil.Withdrawn
CandoxatrilCandoxatril may increase the hypotensive activities of Mibefradil.Experimental
CaptoprilCaptopril may increase the hypotensive activities of Mibefradil.Approved
CarbamazepineThe metabolism of Mibefradil can be increased when combined with Carbamazepine.Approved, Investigational
CarbomycinThe metabolism of Mibefradil can be decreased when combined with Carbomycin.Vet Approved
CarfilzomibThe serum concentration of Carfilzomib can be increased when it is combined with Mibefradil.Approved
CaroxazoneCaroxazone may increase the hypotensive activities of Mibefradil.Withdrawn
CarteololCarteolol may increase the hypotensive activities of Mibefradil.Approved
CarvedilolCarvedilol may increase the hypotensive activities of Mibefradil.Approved, Investigational
CaspofunginThe risk or severity of adverse effects can be increased when Caspofungin is combined with Mibefradil.Approved
CeliprololMibefradil may increase the hypotensive activities of Celiprolol.Approved, Investigational
CeritinibThe serum concentration of Mibefradil can be increased when it is combined with Ceritinib.Approved
CerivastatinThe serum concentration of Cerivastatin can be increased when it is combined with Mibefradil.Withdrawn
CeruleninThe risk or severity of adverse effects can be increased when Cerulenin is combined with Mibefradil.Approved
ChlorothiazideChlorothiazide may increase the hypotensive activities of Mibefradil.Approved, Vet Approved
ChloroxineThe risk or severity of adverse effects can be increased when Chloroxine is combined with Mibefradil.Approved
ChlorpromazineThe serum concentration of Chlorpromazine can be increased when it is combined with Mibefradil.Approved, Vet Approved
ChlorthalidoneChlorthalidone may increase the hypotensive activities of Mibefradil.Approved
CiclopiroxThe risk or severity of adverse effects can be increased when Ciclopirox is combined with Mibefradil.Approved, Investigational
CilazaprilCilazapril may increase the hypotensive activities of Mibefradil.Approved
CimetidineThe serum concentration of Mibefradil can be increased when it is combined with Cimetidine.Approved
CiprofloxacinThe serum concentration of Ciprofloxacin can be increased when it is combined with Mibefradil.Approved, Investigational
CisplatinThe serum concentration of Cisplatin can be increased when it is combined with Mibefradil.Approved
CitalopramThe serum concentration of Citalopram can be increased when it is combined with Mibefradil.Approved
ClarithromycinThe metabolism of Mibefradil can be decreased when combined with Clarithromycin.Approved
ClemastineThe metabolism of Mibefradil can be decreased when combined with Clemastine.Approved
ClobazamThe serum concentration of Clobazam can be increased when it is combined with Mibefradil.Approved, Illicit
ClomifeneThe serum concentration of Clomifene can be increased when it is combined with Mibefradil.Approved, Investigational
ClonidineThe serum concentration of Clonidine can be increased when it is combined with Mibefradil.Approved
ClopidogrelThe therapeutic efficacy of Clopidogrel can be decreased when used in combination with Mibefradil.Approved, Nutraceutical
ClotrimazoleThe risk or severity of adverse effects can be increased when Clotrimazole is combined with Mibefradil.Approved, Vet Approved
ClozapineThe serum concentration of Clozapine can be increased when it is combined with Mibefradil.Approved
CobicistatThe metabolism of Mibefradil can be decreased when combined with Cobicistat.Approved
CobimetinibThe serum concentration of Cobimetinib can be increased when it is combined with Mibefradil.Approved
ColchicineThe serum concentration of Colchicine can be increased when it is combined with Mibefradil.Approved
ConivaptanThe serum concentration of Mibefradil can be increased when it is combined with Conivaptan.Approved, Investigational
Conjugated Equine EstrogensThe serum concentration of Conjugated Equine Estrogens can be increased when it is combined with Mibefradil.Approved
CordycepinThe risk or severity of adverse effects can be increased when Cordycepin is combined with Mibefradil.Investigational
CrizotinibThe metabolism of Mibefradil can be decreased when combined with Crizotinib.Approved
CryptenamineCryptenamine may increase the hypotensive activities of Mibefradil.Approved
CyclosporineThe risk or severity of adverse effects can be increased when Cyclosporine is combined with Mibefradil.Approved, Investigational, Vet Approved
CyclothiazideCyclothiazide may increase the hypotensive activities of Mibefradil.Approved
Dabigatran etexilateThe serum concentration of the active metabolites of Dabigatran etexilate can be increased when Dabigatran etexilate is used in combination with Mibefradil.Approved
DabrafenibThe serum concentration of Mibefradil can be decreased when it is combined with Dabrafenib.Approved
DactinomycinThe serum concentration of Dactinomycin can be increased when it is combined with Mibefradil.Approved
DapagliflozinThe serum concentration of Dapagliflozin can be increased when it is combined with Mibefradil.Approved
DapoxetineDapoxetine may increase the orthostatic hypotensive activities of Mibefradil.Investigational
DarunavirThe metabolism of Mibefradil can be decreased when combined with Darunavir.Approved
DasatinibThe serum concentration of Mibefradil can be increased when it is combined with Dasatinib.Approved, Investigational
DaunorubicinThe serum concentration of Daunorubicin can be increased when it is combined with Mibefradil.Approved
DebrisoquinThe serum concentration of Debrisoquin can be increased when it is combined with Mibefradil.Approved
Decanoic AcidThe risk or severity of adverse effects can be increased when Decanoic Acid is combined with Mibefradil.Experimental
DeferasiroxThe serum concentration of Mibefradil can be decreased when it is combined with Deferasirox.Approved, Investigational
DelavirdineThe metabolism of Mibefradil can be decreased when combined with Delavirdine.Approved
DeserpidineMibefradil may increase the hypotensive activities of Deserpidine.Approved
DexamethasoneThe serum concentration of Mibefradil can be decreased when it is combined with Dexamethasone.Approved, Investigational, Vet Approved
DiazepamThe serum concentration of Diazepam can be increased when it is combined with Mibefradil.Approved, Illicit, Vet Approved
DiazoxideDiazoxide may increase the hypotensive activities of Mibefradil.Approved
DiethylstilbestrolThe serum concentration of Diethylstilbestrol can be increased when it is combined with Mibefradil.Approved
DigitoxinThe serum concentration of Digitoxin can be increased when it is combined with Mibefradil.Approved
DigoxinThe serum concentration of Digoxin can be increased when it is combined with Mibefradil.Approved
DihydralazineMibefradil may increase the hypotensive activities of Dihydralazine.Investigational
DihydroergotamineThe metabolism of Mibefradil can be decreased when combined with Dihydroergotamine.Approved
DihydrotestosteroneThe serum concentration of Dihydrotestosterone can be increased when it is combined with Mibefradil.Illicit
DiltiazemThe metabolism of Mibefradil can be decreased when combined with Diltiazem.Approved
DipyridamoleThe serum concentration of Dipyridamole can be increased when it is combined with Mibefradil.Approved
DocetaxelThe serum concentration of Docetaxel can be increased when it is combined with Mibefradil.Approved, Investigational
DomperidoneThe serum concentration of Domperidone can be increased when it is combined with Mibefradil.Approved, Investigational, Vet Approved
DorzolamideDorzolamide may increase the hypotensive activities of Mibefradil.Approved
DoxazosinDoxazosin may increase the hypotensive activities of Mibefradil.Approved
DoxorubicinThe serum concentration of Doxorubicin can be increased when it is combined with Mibefradil.Approved, Investigational
DoxycyclineThe metabolism of Mibefradil can be decreased when combined with Doxycycline.Approved, Investigational, Vet Approved
DronedaroneThe metabolism of Mibefradil can be decreased when combined with Dronedarone.Approved
EconazoleThe risk or severity of adverse effects can be increased when Econazole is combined with Mibefradil.Approved
EdoxabanThe serum concentration of Edoxaban can be increased when it is combined with Mibefradil.Approved
EfavirenzThe serum concentration of Mibefradil can be decreased when it is combined with Efavirenz.Approved, Investigational
EfinaconazoleThe risk or severity of adverse effects can be increased when Efinaconazole is combined with Mibefradil.Approved
EfonidipineMibefradil may increase the hypotensive activities of Efonidipine.Approved
EletriptanThe serum concentration of Eletriptan can be increased when it is combined with Mibefradil.Approved, Investigational
EnalaprilEnalapril may increase the hypotensive activities of Mibefradil.Approved, Vet Approved
EnalaprilatMibefradil may increase the hypotensive activities of Enalaprilat.Approved
EnzalutamideThe serum concentration of Mibefradil can be decreased when it is combined with Enzalutamide.Approved
EpinastineThe serum concentration of Epinastine can be increased when it is combined with Mibefradil.Approved, Investigational
EpoprostenolEpoprostenol may increase the hypotensive activities of Mibefradil.Approved
EprosartanEprosartan may increase the hypotensive activities of Mibefradil.Approved
ErlotinibThe serum concentration of Erlotinib can be increased when it is combined with Mibefradil.Approved, Investigational
ErythromycinThe metabolism of Mibefradil can be decreased when combined with Erythromycin.Approved, Vet Approved
Eslicarbazepine acetateThe serum concentration of Mibefradil can be decreased when it is combined with Eslicarbazepine acetate.Approved
EstradiolThe serum concentration of Estradiol can be increased when it is combined with Mibefradil.Approved, Investigational, Vet Approved
EstriolThe serum concentration of Estriol can be increased when it is combined with Mibefradil.Approved, Vet Approved
EstroneThe serum concentration of Estrone can be increased when it is combined with Mibefradil.Approved
Ethinyl EstradiolThe serum concentration of Ethinyl Estradiol can be increased when it is combined with Mibefradil.Approved
EtoposideThe serum concentration of Etoposide can be increased when it is combined with Mibefradil.Approved
EtravirineThe serum concentration of Mibefradil can be decreased when it is combined with Etravirine.Approved
EverolimusThe serum concentration of Everolimus can be increased when it is combined with Mibefradil.Approved
EzetimibeThe serum concentration of Ezetimibe can be increased when it is combined with Mibefradil.Approved
FelodipineFelodipine may increase the hypotensive activities of Mibefradil.Approved, Investigational
FenoldopamFenoldopam may increase the hypotensive activities of Mibefradil.Approved
FesoterodineThe serum concentration of the active metabolites of Fesoterodine can be increased when Fesoterodine is used in combination with Mibefradil.Approved
FexofenadineThe serum concentration of Fexofenadine can be increased when it is combined with Mibefradil.Approved
FidaxomicinThe serum concentration of Fidaxomicin can be increased when it is combined with Mibefradil.Approved
FluconazoleThe serum concentration of Mibefradil can be increased when it is combined with Fluconazole.Approved
FlucytosineThe risk or severity of adverse effects can be increased when Flucytosine is combined with Mibefradil.Approved
Fluticasone furoateThe serum concentration of Fluticasone furoate can be increased when it is combined with Mibefradil.Approved
FluvoxamineThe metabolism of Mibefradil can be decreased when combined with Fluvoxamine.Approved, Investigational
FosamprenavirThe metabolism of Mibefradil can be decreased when combined with Fosamprenavir.Approved
FosaprepitantThe serum concentration of Mibefradil can be increased when it is combined with Fosaprepitant.Approved
FosinoprilFosinopril may increase the hypotensive activities of Mibefradil.Approved
FosphenytoinThe serum concentration of Fosphenytoin can be increased when it is combined with Mibefradil.Approved
FurazolidoneFurazolidone may increase the hypotensive activities of Mibefradil.Approved, Vet Approved
Fusidic AcidThe serum concentration of Mibefradil can be increased when it is combined with Fusidic Acid.Approved
GefitinibThe serum concentration of Gefitinib can be increased when it is combined with Mibefradil.Approved, Investigational
GemcitabineThe serum concentration of Gemcitabine can be increased when it is combined with Mibefradil.Approved
GlyphosateThe risk or severity of adverse effects can be increased when Glyphosate is combined with Mibefradil.Experimental
GrazoprevirThe serum concentration of Grazoprevir can be increased when it is combined with Mibefradil.Approved
GrepafloxacinThe serum concentration of Grepafloxacin can be increased when it is combined with Mibefradil.Withdrawn
GriseofulvinThe risk or severity of adverse effects can be increased when Griseofulvin is combined with Mibefradil.Approved, Vet Approved
GuanabenzGuanabenz may increase the hypotensive activities of Mibefradil.Approved
GuanadrelGuanadrel may increase the hypotensive activities of Mibefradil.Approved
GuanethidineGuanethidine may increase the hypotensive activities of Mibefradil.Approved
GuanfacineGuanfacine may increase the hypotensive activities of Mibefradil.Approved, Investigational
HaloperidolThe serum concentration of Haloperidol can be increased when it is combined with Mibefradil.Approved
HaloproginThe risk or severity of adverse effects can be increased when Haloprogin is combined with Mibefradil.Approved, Withdrawn
HexamethoniumMibefradil may increase the hypotensive activities of Hexamethonium.Experimental
HexetidineThe risk or severity of adverse effects can be increased when Hexetidine is combined with Mibefradil.Approved
HexobarbitalThe metabolism of Mibefradil can be increased when combined with Hexobarbital.Approved
HydracarbazineHydracarbazine may increase the hypotensive activities of Mibefradil.Approved
HydralazineHydralazine may increase the hypotensive activities of Mibefradil.Approved
HydrochlorothiazideHydrochlorothiazide may increase the hypotensive activities of Mibefradil.Approved, Vet Approved
HydrocortisoneThe serum concentration of Hydrocortisone can be increased when it is combined with Mibefradil.Approved, Vet Approved
HydroflumethiazideHydroflumethiazide may increase the hypotensive activities of Mibefradil.Approved
IbuprofenThe serum concentration of Ibuprofen can be increased when it is combined with Mibefradil.Approved
IdelalisibThe serum concentration of Mibefradil can be increased when it is combined with Idelalisib.Approved
IloprostIloprost may increase the hypotensive activities of Mibefradil.Approved, Investigational
ImatinibThe metabolism of Mibefradil can be decreased when combined with Imatinib.Approved
ImidaprilMibefradil may increase the hypotensive activities of Imidapril.Investigational
ImipramineThe serum concentration of Imipramine can be increased when it is combined with Mibefradil.Approved
IndacaterolThe serum concentration of Indacaterol can be increased when it is combined with Mibefradil.Approved
IndapamideIndapamide may increase the hypotensive activities of Mibefradil.Approved
IndenololMibefradil may increase the hypotensive activities of Indenolol.Withdrawn
IndinavirThe metabolism of Mibefradil can be decreased when combined with Indinavir.Approved
IndomethacinThe serum concentration of Indomethacin can be increased when it is combined with Mibefradil.Approved, Investigational
IndoraminMibefradil may increase the hypotensive activities of Indoramin.Withdrawn
IproclozideIproclozide may increase the hypotensive activities of Mibefradil.Withdrawn
IproniazidIproniazid may increase the hypotensive activities of Mibefradil.Withdrawn
IrbesartanIrbesartan may increase the hypotensive activities of Mibefradil.Approved, Investigational
IrinotecanThe serum concentration of Irinotecan can be increased when it is combined with Mibefradil.Approved, Investigational
IsavuconazoniumThe metabolism of Mibefradil can be decreased when combined with Isavuconazonium.Approved, Investigational
IsocarboxazidIsocarboxazid may increase the hypotensive activities of Mibefradil.Approved
IsoconazoleThe risk or severity of adverse effects can be increased when Isoconazole is combined with Mibefradil.Approved
IsradipineThe metabolism of Mibefradil can be decreased when combined with Isradipine.Approved
ItraconazoleThe metabolism of Mibefradil can be decreased when combined with Itraconazole.Approved, Investigational
IvacaftorThe serum concentration of Mibefradil can be increased when it is combined with Ivacaftor.Approved
IvermectinThe serum concentration of Ivermectin can be increased when it is combined with Mibefradil.Approved, Vet Approved
JosamycinThe metabolism of Mibefradil can be decreased when combined with Josamycin.Approved
KetanserinMibefradil may increase the hypotensive activities of Ketanserin.Investigational
KetazolamThe serum concentration of Ketazolam can be increased when it is combined with Mibefradil.Approved
KetoconazoleThe metabolism of Mibefradil can be decreased when combined with Ketoconazole.Approved, Investigational
KitasamycinThe metabolism of Mibefradil can be decreased when combined with Kitasamycin.Experimental
LabetalolLabetalol may increase the hypotensive activities of Mibefradil.Approved
LacidipineMibefradil may increase the hypotensive activities of Lacidipine.Approved
LamivudineThe serum concentration of Lamivudine can be increased when it is combined with Mibefradil.Approved, Investigational
LamotrigineThe serum concentration of Lamotrigine can be increased when it is combined with Mibefradil.Approved, Investigational
LansoprazoleThe serum concentration of Lansoprazole can be increased when it is combined with Mibefradil.Approved, Investigational
LatanoprostLatanoprost may increase the hypotensive activities of Mibefradil.Approved, Investigational
LedipasvirThe serum concentration of Ledipasvir can be increased when it is combined with Mibefradil.Approved
LenalidomideThe serum concentration of Lenalidomide can be increased when it is combined with Mibefradil.Approved
LenvatinibThe serum concentration of Lenvatinib can be increased when it is combined with Mibefradil.Approved
LercanidipineLercanidipine may increase the hypotensive activities of Mibefradil.Approved, Investigational
LevetiracetamThe serum concentration of Levetiracetam can be increased when it is combined with Mibefradil.Approved, Investigational
LevofloxacinThe serum concentration of Levofloxacin can be increased when it is combined with Mibefradil.Approved, Investigational
LevomilnacipranThe serum concentration of Levomilnacipran can be increased when it is combined with Mibefradil.Approved
LinagliptinThe serum concentration of Linagliptin can be increased when it is combined with Mibefradil.Approved
LisinoprilLisinopril may increase the hypotensive activities of Mibefradil.Approved, Investigational
LofexidineMibefradil may increase the hypotensive activities of Lofexidine.Approved, Investigational
LoperamideThe serum concentration of Loperamide can be increased when it is combined with Mibefradil.Approved
LopinavirThe metabolism of Mibefradil can be decreased when combined with Lopinavir.Approved
LosartanThe serum concentration of Losartan can be increased when it is combined with Mibefradil.Approved
LovastatinThe metabolism of Mibefradil can be decreased when combined with Lovastatin.Approved, Investigational
LuliconazoleThe serum concentration of Mibefradil can be increased when it is combined with Luliconazole.Approved
LumacaftorThe metabolism of Mibefradil can be increased when combined with Lumacaftor.Approved
MacitentanMibefradil may increase the hypotensive activities of Macitentan.Approved
Magnesium hydroxideThe risk or severity of adverse effects can be increased when Mibefradil is combined with Magnesium hydroxide.Approved
Magnesium oxideThe risk or severity of adverse effects can be increased when Mibefradil is combined with Magnesium oxide.Approved
Magnesium salicylateThe risk or severity of adverse effects can be increased when Mibefradil is combined with Magnesium salicylate.Approved
Magnesium SulfateThe risk or severity of adverse effects can be increased when Mibefradil is combined with Magnesium Sulfate.Approved, Vet Approved
ManidipineMibefradil may increase the hypotensive activities of Manidipine.Approved
MannitolThe serum concentration of Mannitol can be increased when it is combined with Mibefradil.Approved, Investigational
MebanazineMebanazine may increase the hypotensive activities of Mibefradil.Withdrawn
MecamylamineMecamylamine may increase the hypotensive activities of Mibefradil.Approved
MethohexitalThe metabolism of Mibefradil can be increased when combined with Methohexital.Approved
MethotrexateThe serum concentration of Methotrexate can be increased when it is combined with Mibefradil.Approved
MethyldopaMethyldopa may increase the hypotensive activities of Mibefradil.Approved
Methylene blueMethylene blue may increase the hypotensive activities of Mibefradil.Investigational
MethylphenidateMethylphenidate may decrease the antihypertensive activities of Mibefradil.Approved, Investigational
MethylphenobarbitalThe metabolism of Mibefradil can be increased when combined with Methylphenobarbital.Approved
MethylprednisoloneThe serum concentration of Methylprednisolone can be increased when it is combined with Mibefradil.Approved, Vet Approved
MetipranololMetipranolol may increase the hypotensive activities of Mibefradil.Approved
MetolazoneMetolazone may increase the hypotensive activities of Mibefradil.Approved
MetoprololThe serum concentration of Metoprolol can be increased when it is combined with Mibefradil.Approved, Investigational
MetyrosineMibefradil may increase the hypotensive activities of Metyrosine.Approved
MevastatinThe risk or severity of adverse effects can be increased when Mevastatin is combined with Mibefradil.Experimental
MicafunginThe risk or severity of adverse effects can be increased when Micafungin is combined with Mibefradil.Approved, Investigational
MiconazoleThe risk or severity of adverse effects can be increased when Miconazole is combined with Mibefradil.Approved, Investigational, Vet Approved
MidazolamThe serum concentration of Midazolam can be increased when it is combined with Mibefradil.Approved, Illicit
MifepristoneThe serum concentration of Mibefradil can be increased when it is combined with Mifepristone.Approved, Investigational
MiltefosineThe risk or severity of adverse effects can be increased when Miltefosine is combined with Mibefradil.Approved
MinaprineMinaprine may increase the hypotensive activities of Mibefradil.Approved
MinoxidilMinoxidil may increase the hypotensive activities of Mibefradil.Approved
MirabegronThe serum concentration of Mirabegron can be increased when it is combined with Mibefradil.Approved
MitotaneThe serum concentration of Mibefradil can be decreased when it is combined with Mitotane.Approved
MitoxantroneThe serum concentration of Mitoxantrone can be increased when it is combined with Mibefradil.Approved, Investigational
MivacuriumMibefradil may increase the neuromuscular blocking activities of Mivacurium.Approved
MoclobemideMoclobemide may increase the hypotensive activities of Mibefradil.Approved
ModafinilThe serum concentration of Mibefradil can be decreased when it is combined with Modafinil.Approved, Investigational
MoexiprilMoexipril may increase the hypotensive activities of Mibefradil.Approved
MolsidomineMolsidomine may increase the hypotensive activities of Mibefradil.Approved
MonensinThe risk or severity of adverse effects can be increased when Monensin is combined with Mibefradil.Vet Approved
MorphineThe serum concentration of Morphine can be increased when it is combined with Mibefradil.Approved, Investigational
MoxonidineMibefradil may increase the hypotensive activities of Moxonidine.Approved
Mycophenolate mofetilThe serum concentration of Mycophenolate mofetil can be increased when it is combined with Mibefradil.Approved, Investigational
MyxothiazolThe risk or severity of adverse effects can be increased when Myxothiazol is combined with Mibefradil.Experimental
NadololThe serum concentration of Nadolol can be increased when it is combined with Mibefradil.Approved
NafcillinThe metabolism of Mibefradil can be increased when combined with Nafcillin.Approved
NaftifineThe risk or severity of adverse effects can be increased when Naftifine is combined with Mibefradil.Approved
NaftopidilMibefradil may increase the hypotensive activities of Naftopidil.Investigational
NaloxegolThe serum concentration of Naloxegol can be increased when it is combined with Mibefradil.Approved
NaloxoneThe serum concentration of Naloxone can be increased when it is combined with Mibefradil.Approved, Vet Approved
NatamycinThe risk or severity of adverse effects can be increased when Natamycin is combined with Mibefradil.Approved
NebivololMibefradil may increase the hypotensive activities of Nebivolol.Approved, Investigational
NefazodoneThe metabolism of Mibefradil can be decreased when combined with Nefazodone.Approved, Withdrawn
NelfinavirThe metabolism of Mibefradil can be decreased when combined with Nelfinavir.Approved
NetupitantThe serum concentration of Mibefradil can be increased when it is combined with Netupitant.Approved
NevirapineThe metabolism of Mibefradil can be increased when combined with Nevirapine.Approved
NialamideNialamide may increase the hypotensive activities of Mibefradil.Withdrawn
NicardipineThe serum concentration of Nicardipine can be increased when it is combined with Mibefradil.Approved
NicorandilMibefradil may increase the hypotensive activities of Nicorandil.Approved
NifedipineThe serum concentration of Nifedipine can be increased when it is combined with Mibefradil.Approved
NiguldipineMibefradil may increase the hypotensive activities of Niguldipine.Experimental
NilotinibThe metabolism of Mibefradil can be decreased when combined with Nilotinib.Approved, Investigational
NilvadipineMibefradil may increase the hypotensive activities of Nilvadipine.Approved
NimodipineNimodipine may increase the hypotensive activities of Mibefradil.Approved
NintedanibThe serum concentration of Nintedanib can be increased when it is combined with Mibefradil.Approved
NisoldipineNisoldipine may increase the hypotensive activities of Mibefradil.Approved
NitrendipineNitrendipine may increase the hypotensive activities of Mibefradil.Approved
NitroprussideMibefradil may increase the hypotensive activities of Nitroprusside.Approved
NitroxolineThe risk or severity of adverse effects can be increased when Nitroxoline is combined with Mibefradil.Approved
NizatidineThe serum concentration of Nizatidine can be increased when it is combined with Mibefradil.Approved
NystatinThe risk or severity of adverse effects can be increased when Nystatin is combined with Mibefradil.Approved, Vet Approved
ObinutuzumabMibefradil may increase the hypotensive activities of Obinutuzumab.Approved
OctamoxinOctamoxin may increase the hypotensive activities of Mibefradil.Withdrawn
OlanzapineThe serum concentration of Olanzapine can be increased when it is combined with Mibefradil.Approved, Investigational
OlaparibThe metabolism of Mibefradil can be decreased when combined with Olaparib.Approved
OleandomycinThe metabolism of Mibefradil can be decreased when combined with Oleandomycin.Vet Approved
OlmesartanOlmesartan may increase the hypotensive activities of Mibefradil.Approved, Investigational
OmapatrilatOmapatrilat may increase the hypotensive activities of Mibefradil.Investigational
OmbitasvirThe serum concentration of Ombitasvir can be increased when it is combined with Mibefradil.Approved
OsimertinibThe serum concentration of Mibefradil can be increased when it is combined with Osimertinib.Approved
OxiconazoleThe risk or severity of adverse effects can be increased when Oxiconazole is combined with Mibefradil.Approved
OxprenololMibefradil may increase the hypotensive activities of Oxprenolol.Approved
PaclitaxelThe serum concentration of Paclitaxel can be increased when it is combined with Mibefradil.Approved, Vet Approved
pafuramidineThe risk or severity of adverse effects can be increased when pafuramidine is combined with Mibefradil.Investigational
PalbociclibThe serum concentration of Mibefradil can be increased when it is combined with Palbociclib.Approved
PanobinostatThe serum concentration of Panobinostat can be increased when it is combined with Mibefradil.Approved, Investigational
PargylinePargyline may increase the hypotensive activities of Mibefradil.Approved
PazopanibThe serum concentration of Pazopanib can be increased when it is combined with Mibefradil.Approved
PenbutololPenbutolol may increase the hypotensive activities of Mibefradil.Approved, Investigational
PentamidineThe risk or severity of adverse effects can be increased when Pentamidine is combined with Mibefradil.Approved
PentobarbitalThe metabolism of Mibefradil can be increased when combined with Pentobarbital.Approved, Vet Approved
PentoliniumPentolinium may increase the hypotensive activities of Mibefradil.Approved
PentoxifyllinePentoxifylline may increase the hypotensive activities of Mibefradil.Approved, Investigational
PerindoprilPerindopril may increase the hypotensive activities of Mibefradil.Approved
PhenelzinePhenelzine may increase the hypotensive activities of Mibefradil.Approved
PheniprazinePheniprazine may increase the hypotensive activities of Mibefradil.Withdrawn
PhenobarbitalThe metabolism of Mibefradil can be increased when combined with Phenobarbital.Approved
PhenoxybenzaminePhenoxybenzamine may increase the hypotensive activities of Mibefradil.Approved
PhenoxypropazinePhenoxypropazine may increase the hypotensive activities of Mibefradil.Withdrawn
PhentolaminePhentolamine may increase the hypotensive activities of Mibefradil.Approved
PhenytoinThe serum concentration of Phenytoin can be increased when it is combined with Mibefradil.Approved, Vet Approved
PinacidilMibefradil may increase the hypotensive activities of Pinacidil.Withdrawn
PindololPindolol may increase the hypotensive activities of Mibefradil.Approved
PirlindolePirlindole may increase the hypotensive activities of Mibefradil.Approved
PitavastatinThe serum concentration of Pitavastatin can be increased when it is combined with Mibefradil.Approved
PivhydrazinePivhydrazine may increase the hypotensive activities of Mibefradil.Withdrawn
PolythiazidePolythiazide may increase the hypotensive activities of Mibefradil.Approved
PomalidomideThe serum concentration of Pomalidomide can be increased when it is combined with Mibefradil.Approved
PonatinibThe serum concentration of Ponatinib can be increased when it is combined with Mibefradil.Approved
PosaconazoleThe metabolism of Mibefradil can be decreased when combined with Posaconazole.Approved, Investigational, Vet Approved
PravastatinThe serum concentration of Pravastatin can be increased when it is combined with Mibefradil.Approved
PrazosinThe serum concentration of Prazosin can be increased when it is combined with Mibefradil.Approved
PrednisoloneThe serum concentration of Prednisolone can be increased when it is combined with Mibefradil.Approved, Vet Approved
PrednisoneThe serum concentration of Prednisone can be increased when it is combined with Mibefradil.Approved, Vet Approved
PrimidoneThe metabolism of Mibefradil can be increased when combined with Primidone.Approved, Vet Approved
ProgesteroneThe serum concentration of Progesterone can be increased when it is combined with Mibefradil.Approved, Vet Approved
PropranololThe serum concentration of Propranolol can be increased when it is combined with Mibefradil.Approved, Investigational
PrucaloprideThe serum concentration of Prucalopride can be increased when it is combined with Mibefradil.Approved
QuetiapineThe serum concentration of Quetiapine can be increased when it is combined with Mibefradil.Approved
QuinaprilQuinapril may increase the hypotensive activities of Mibefradil.Approved, Investigational
QuinidineThe serum concentration of Quinidine can be increased when it is combined with Mibefradil.Approved
QuinineQuinine may increase the hypotensive activities of Mibefradil.Approved
RadicicolThe risk or severity of adverse effects can be increased when Radicicol is combined with Mibefradil.Experimental
RamiprilRamipril may increase the hypotensive activities of Mibefradil.Approved
RanitidineThe serum concentration of Ranitidine can be increased when it is combined with Mibefradil.Approved
RanolazineThe serum concentration of Ranolazine can be increased when it is combined with Mibefradil.Approved, Investigational
RapacuroniumMibefradil may increase the neuromuscular blocking activities of Rapacuronium.Withdrawn
RasagilineRasagiline may increase the hypotensive activities of Mibefradil.Approved
RemikirenRemikiren may increase the hypotensive activities of Mibefradil.Approved
RescinnamineMibefradil may increase the hypotensive activities of Rescinnamine.Approved
ReserpineThe serum concentration of Reserpine can be increased when it is combined with Mibefradil.Approved
RifabutinThe metabolism of Mibefradil can be increased when combined with Rifabutin.Approved
RifampicinThe metabolism of Mibefradil can be increased when combined with Rifampicin.Approved
RifapentineThe metabolism of Mibefradil can be increased when combined with Rifapentine.Approved
RifaximinThe serum concentration of Rifaximin can be increased when it is combined with Mibefradil.Approved, Investigational
RilmenidineMibefradil may increase the hypotensive activities of Rilmenidine.Investigational
RiociguatMibefradil may increase the hypotensive activities of Riociguat.Approved
RisperidoneThe serum concentration of Risperidone can be increased when it is combined with Mibefradil.Approved, Investigational
RitonavirThe metabolism of Mibefradil can be decreased when combined with Ritonavir.Approved, Investigational
RituximabMibefradil may increase the hypotensive activities of Rituximab.Approved
RivaroxabanThe serum concentration of Rivaroxaban can be increased when it is combined with Mibefradil.Approved
RomidepsinThe serum concentration of Romidepsin can be increased when it is combined with Mibefradil.Approved, Investigational
SafrazineSafrazine may increase the hypotensive activities of Mibefradil.Withdrawn
Salicylhydroxamic AcidThe risk or severity of adverse effects can be increased when Salicylhydroxamic Acid is combined with Mibefradil.Experimental
Salicylic acidThe risk or severity of adverse effects can be increased when Salicylic acid is combined with Mibefradil.Approved, Vet Approved
SaprisartanSaprisartan may increase the hypotensive activities of Mibefradil.Experimental
SaquinavirThe metabolism of Mibefradil can be decreased when combined with Saquinavir.Approved, Investigational
SecobarbitalThe metabolism of Mibefradil can be increased when combined with Secobarbital.Approved, Vet Approved
SelegilineSelegiline may increase the hypotensive activities of Mibefradil.Approved, Investigational, Vet Approved
SelexipagThe serum concentration of Selexipag can be increased when it is combined with Mibefradil.Approved
SertaconazoleThe risk or severity of adverse effects can be increased when Sertaconazole is combined with Mibefradil.Approved
SildenafilSildenafil may increase the antihypertensive activities of Mibefradil.Approved, Investigational
SilodosinThe serum concentration of Silodosin can be increased when it is combined with Mibefradil.Approved
SiltuximabThe serum concentration of Mibefradil can be decreased when it is combined with Siltuximab.Approved
SimeprevirThe serum concentration of Mibefradil can be increased when it is combined with Simeprevir.Approved
SinefunginThe risk or severity of adverse effects can be increased when Sinefungin is combined with Mibefradil.Experimental
SirolimusThe risk or severity of adverse effects can be increased when Sirolimus is combined with Mibefradil.Approved, Investigational
SitagliptinThe serum concentration of Sitagliptin can be increased when it is combined with Mibefradil.Approved, Investigational
SitaxentanMibefradil may increase the hypotensive activities of Sitaxentan.Approved, Investigational, Withdrawn
SofosbuvirThe serum concentration of Sofosbuvir can be increased when it is combined with Mibefradil.Approved
SolithromycinThe metabolism of Mibefradil can be decreased when combined with Solithromycin.Investigational
SorafenibThe serum concentration of Sorafenib can be increased when it is combined with Mibefradil.Approved, Investigational
SparfloxacinThe serum concentration of Sparfloxacin can be increased when it is combined with Mibefradil.Approved
SphingosineThe serum concentration of Sphingosine can be increased when it is combined with Mibefradil.Experimental
SpiraprilSpirapril may increase the hypotensive activities of Mibefradil.Approved
St. John's WortThe serum concentration of Mibefradil can be decreased when it is combined with St. John's Wort.Nutraceutical
StiripentolThe serum concentration of Mibefradil can be increased when it is combined with Stiripentol.Approved
SulconazoleThe risk or severity of adverse effects can be increased when Sulconazole is combined with Mibefradil.Approved
SulfisoxazoleThe metabolism of Mibefradil can be decreased when combined with Sulfisoxazole.Approved, Vet Approved
TacrolimusThe serum concentration of Tacrolimus can be increased when it is combined with Mibefradil.Approved, Investigational
TadalafilTadalafil may increase the antihypertensive activities of Mibefradil.Approved, Investigational
TamoxifenThe serum concentration of Tamoxifen can be increased when it is combined with Mibefradil.Approved
TamsulosinTamsulosin may increase the hypotensive activities of Mibefradil.Approved, Investigational
Taurocholic AcidThe serum concentration of Taurocholic Acid can be increased when it is combined with Mibefradil.Experimental
TavaboroleThe risk or severity of adverse effects can be increased when Tavaborole is combined with Mibefradil.Approved
Technetium Tc-99m sestamibiThe serum concentration of Technetium Tc-99m sestamibi can be increased when it is combined with Mibefradil.Approved
TelaprevirThe metabolism of Mibefradil can be decreased when combined with Telaprevir.Approved
TelithromycinThe metabolism of Mibefradil can be decreased when combined with Telithromycin.Approved
TelmisartanTelmisartan may increase the hypotensive activities of Mibefradil.Approved, Investigational
TemocaprilMibefradil may increase the hypotensive activities of Temocapril.Experimental, Investigational
TemsirolimusThe serum concentration of Temsirolimus can be increased when it is combined with Mibefradil.Approved
TerazosinTerazosin may increase the hypotensive activities of Mibefradil.Approved
TerbinafineThe risk or severity of adverse effects can be increased when Terbinafine is combined with Mibefradil.Approved, Investigational, Vet Approved
TerconazoleThe risk or severity of adverse effects can be increased when Terconazole is combined with Mibefradil.Approved
TerlipressinMibefradil may increase the hypotensive activities of Terlipressin.Approved, Investigational
ThiamylalThe metabolism of Mibefradil can be increased when combined with Thiamylal.Approved, Vet Approved
ThiopentalThe metabolism of Mibefradil can be increased when combined with Thiopental.Approved, Vet Approved
ThioridazineThe serum concentration of Thioridazine can be increased when it is combined with Mibefradil.Approved
ThymolThe risk or severity of adverse effects can be increased when Thymol is combined with Mibefradil.Approved
TiboloneMibefradil may increase the hypotensive activities of Tibolone.Approved
TicagrelorThe serum concentration of Ticagrelor can be increased when it is combined with Mibefradil.Approved
TiclopidineThe metabolism of Mibefradil can be decreased when combined with Ticlopidine.Approved
TicrynafenMibefradil may increase the hypotensive activities of Ticrynafen.Withdrawn
TimololThe serum concentration of Timolol can be increased when it is combined with Mibefradil.Approved
TioconazoleThe risk or severity of adverse effects can be increased when Tioconazole is combined with Mibefradil.Approved
TocilizumabThe serum concentration of Mibefradil can be decreased when it is combined with Tocilizumab.Approved
TolazolineTolazoline may increase the hypotensive activities of Mibefradil.Approved, Vet Approved
TolnaftateThe risk or severity of adverse effects can be increased when Tolnaftate is combined with Mibefradil.Approved, Vet Approved
ToloxatoneToloxatone may increase the hypotensive activities of Mibefradil.Approved
TolvaptanThe serum concentration of Tolvaptan can be increased when it is combined with Mibefradil.Approved
TopotecanThe serum concentration of Topotecan can be increased when it is combined with Mibefradil.Approved, Investigational
TorasemideTorasemide may increase the hypotensive activities of Mibefradil.Approved
ToremifeneThe serum concentration of Toremifene can be increased when it is combined with Mibefradil.Approved, Investigational
TrandolaprilTrandolapril may increase the hypotensive activities of Mibefradil.Approved
Trans-2-PhenylcyclopropylamineTrans-2-Phenylcyclopropylamine may increase the hypotensive activities of Mibefradil.Experimental
TranylcypromineTranylcypromine may increase the hypotensive activities of Mibefradil.Approved
Trastuzumab emtansineThe serum concentration of Trastuzumab emtansine can be increased when it is combined with Mibefradil.Approved
TravoprostTravoprost may increase the hypotensive activities of Mibefradil.Approved
TreprostinilTreprostinil may increase the hypotensive activities of Mibefradil.Approved, Investigational
TrichlormethiazideTrichlormethiazide may increase the hypotensive activities of Mibefradil.Approved, Vet Approved
TrimazosinMibefradil may increase the hypotensive activities of Trimazosin.Experimental
TrimethaphanTrimethaphan may increase the hypotensive activities of Mibefradil.Approved
TrimetrexateThe risk or severity of adverse effects can be increased when Trimetrexate is combined with Mibefradil.Approved, Investigational
TroleandomycinThe metabolism of Mibefradil can be decreased when combined with Troleandomycin.Approved
TylosinThe metabolism of Mibefradil can be decreased when combined with Tylosin.Vet Approved
UdenafilUdenafil may increase the antihypertensive activities of Mibefradil.Approved, Investigational
UlipristalThe serum concentration of Ulipristal can be increased when it is combined with Mibefradil.Approved
UmeclidiniumThe serum concentration of Umeclidinium can be increased when it is combined with Mibefradil.Approved
UnoprostoneMibefradil may increase the hypotensive activities of Unoprostone.Approved
ValsartanValsartan may increase the hypotensive activities of Mibefradil.Approved, Investigational
VardenafilVardenafil may increase the antihypertensive activities of Mibefradil.Approved
VecuroniumThe serum concentration of Vecuronium can be increased when it is combined with Mibefradil.Approved
VenetoclaxThe serum concentration of Venetoclax can be increased when it is combined with Mibefradil.Approved
VenlafaxineThe metabolism of Mibefradil can be decreased when combined with Venlafaxine.Approved
VerapamilThe metabolism of Mibefradil can be decreased when combined with Verapamil.Approved
VinblastineThe serum concentration of Vinblastine can be increased when it is combined with Mibefradil.Approved
VincristineThe serum concentration of Vincristine can be increased when it is combined with Mibefradil.Approved, Investigational
VinpocetineMibefradil may increase the hypotensive activities of Vinpocetine.Investigational
VismodegibThe serum concentration of Vismodegib can be increased when it is combined with Mibefradil.Approved
VoriconazoleThe metabolism of Mibefradil can be decreased when combined with Voriconazole.Approved, Investigational
XylometazolineMibefradil may increase the hypotensive activities of Xylometazoline.Approved
YohimbineYohimbine may decrease the antihypertensive activities of Mibefradil.Approved, Vet Approved
ZidovudineThe serum concentration of Zidovudine can be increased when it is combined with Mibefradil.Approved
ZiprasidoneThe metabolism of Mibefradil can be decreased when combined with Ziprasidone.Approved
Food InteractionsNot Available
References
Synthesis ReferenceNot Available
General ReferencesNot Available
External Links
ATC CodesC08CX01
AHFS CodesNot Available
PDB EntriesNot Available
FDA labelNot Available
MSDSNot Available
ADMET
Predicted ADMET features
PropertyValueProbability
Human Intestinal Absorption+0.9964
Blood Brain Barrier+0.5
Caco-2 permeable+0.5
P-glycoprotein substrateSubstrate0.9087
P-glycoprotein inhibitor IInhibitor0.8718
P-glycoprotein inhibitor IIInhibitor0.8388
Renal organic cation transporterNon-inhibitor0.549
CYP450 2C9 substrateNon-substrate0.8596
CYP450 2D6 substrateNon-substrate0.9116
CYP450 3A4 substrateSubstrate0.7408
CYP450 1A2 substrateInhibitor0.9107
CYP450 2C9 inhibitorNon-inhibitor0.907
CYP450 2D6 inhibitorInhibitor0.8932
CYP450 2C19 inhibitorNon-inhibitor0.9025
CYP450 3A4 inhibitorInhibitor0.796
CYP450 inhibitory promiscuityHigh CYP Inhibitory Promiscuity0.6921
Ames testNon AMES toxic0.6864
CarcinogenicityNon-carcinogens0.892
BiodegradationNot ready biodegradable1.0
Rat acute toxicity2.8610 LD50, mol/kg Not applicable
hERG inhibition (predictor I)Weak inhibitor0.9611
hERG inhibition (predictor II)Inhibitor0.7742
ADMET data is predicted using admetSAR, a free tool for evaluating chemical ADMET properties. (23092397 )
Pharmacoeconomics
ManufacturersNot Available
PackagersNot Available
Dosage formsNot Available
PricesNot Available
PatentsNot Available
Properties
StateSolid
Experimental Properties
PropertyValueSource
Caco2 permeability-4.87ADME Research, USCD
Predicted Properties
PropertyValueSource
Water Solubility0.00104 mg/mLALOGPS
logP5.34ALOGPS
logP5.16ChemAxon
logS-5.7ALOGPS
pKa (Strongest Acidic)12.54ChemAxon
pKa (Strongest Basic)9.82ChemAxon
Physiological Charge1ChemAxon
Hydrogen Acceptor Count4ChemAxon
Hydrogen Donor Count1ChemAxon
Polar Surface Area67.45 Å2ChemAxon
Rotatable Bond Count12ChemAxon
Refractivity139.73 m3·mol-1ChemAxon
Number of Rings4ChemAxon
Bioavailability0ChemAxon
Rule of FiveYesChemAxon
Ghose FilterYesChemAxon
Veber's RuleYesChemAxon
MDDR-like RuleYesChemAxon
Spectra
Mass Spec (NIST)Not Available
SpectraNot Available
Taxonomy
DescriptionThis compound belongs to the class of organic compounds known as tetralins. These are polycyclic aromatic compounds containing a tetralin moiety, which consists of a benzene fused to a cyclohexane.
KingdomOrganic compounds
Super ClassBenzenoids
ClassTetralins
Sub ClassNot Available
Direct ParentTetralins
Alternative Parents
Substituents
  • Tetralin
  • Benzimidazole
  • Aralkylamine
  • Fluorobenzene
  • Aryl halide
  • Aryl fluoride
  • Heteroaromatic compound
  • Imidazole
  • Azole
  • Tertiary aliphatic amine
  • Tertiary amine
  • Carboxylic acid ester
  • Azacycle
  • Organoheterocyclic compound
  • Monocarboxylic acid or derivatives
  • Ether
  • Dialkyl ether
  • Carboxylic acid derivative
  • Hydrocarbon derivative
  • Organooxygen compound
  • Organonitrogen compound
  • Organofluoride
  • Organohalogen compound
  • Carbonyl group
  • Amine
  • Aromatic heteropolycyclic compound
Molecular FrameworkAromatic heteropolycyclic compounds
External DescriptorsNot Available

Targets

Kind
Protein
Organism
Human
Pharmacological action
yes
Actions
inhibitor
General Function:
Scaffold protein binding
Specific Function:
Voltage-sensitive calcium channels (VSCC) mediate the entry of calcium ions into excitable cells and are also involved in a variety of calcium-dependent processes, including muscle contraction, hormone or neurotransmitter release, gene expression, cell motility, cell division and cell death. The isoform alpha-1G gives rise to T-type calcium currents. T-type calcium channels belong to the "low-v...
Gene Name:
CACNA1G
Uniprot ID:
O43497
Molecular Weight:
262468.62 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. Lee TS, Kaku T, Takebayashi S, Uchino T, Miyamoto S, Hadama T, Perez-Reyes E, Ono K: Actions of mibefradil, efonidipine and nifedipine block of recombinant T- and L-type Ca channels with distinct inhibitory mechanisms. Pharmacology. 2006;78(1):11-20. Epub 2006 Aug 7. [PubMed:16899990 ]
  3. Monteil A, Chemin J, Bourinet E, Mennessier G, Lory P, Nargeot J: Molecular and functional properties of the human alpha(1G) subunit that forms T-type calcium channels. J Biol Chem. 2000 Mar 3;275(9):6090-100. [PubMed:10692398 ]
  4. Massie BM: Mibefradil: a selective T-type calcium antagonist. Am J Cardiol. 1997 Nov 6;80(9A):23I-32I. [PubMed:9375939 ]
  5. Clozel JP, Ertel EA, Ertel SI: Discovery and main pharmacological properties of mibefradil (Ro 40-5967), the first selective T-type calcium channel blocker. J Hypertens Suppl. 1997 Dec;15(5):S17-25. [PubMed:9481612 ]
  6. McNulty MM, Hanck DA: State-dependent mibefradil block of Na+ channels. Mol Pharmacol. 2004 Dec;66(6):1652-61. [PubMed:15562257 ]
Kind
Protein
Organism
Human
Pharmacological action
yes
Actions
inhibitor
General Function:
Scaffold protein binding
Specific Function:
Voltage-sensitive calcium channels (VSCC) mediate the entry of calcium ions into excitable cells and are also involved in a variety of calcium-dependent processes, including muscle contraction, hormone or neurotransmitter release, gene expression, cell motility, cell division and cell death. The isoform alpha-1H gives rise to T-type calcium currents. T-type calcium channels belong to the "low-v...
Gene Name:
CACNA1H
Uniprot ID:
O95180
Molecular Weight:
259160.2 Da
References
  1. Brueggemann LI, Martin BL, Barakat J, Byron KL, Cribbs LL: Low voltage-activated calcium channels in vascular smooth muscle: T-type channels and AVP-stimulated calcium spiking. Am J Physiol Heart Circ Physiol. 2005 Feb;288(2):H923-35. Epub 2004 Oct 21. [PubMed:15498818 ]
  2. Coste B, Crest M, Delmas P: Pharmacological dissection and distribution of NaN/Nav1.9, T-type Ca2+ currents, and mechanically activated cation currents in different populations of DRG neurons. J Gen Physiol. 2007 Jan;129(1):57-77. [PubMed:17190903 ]
  3. Cribbs LL, Lee JH, Yang J, Satin J, Zhang Y, Daud A, Barclay J, Williamson MP, Fox M, Rees M, Perez-Reyes E: Cloning and characterization of alpha1H from human heart, a member of the T-type Ca2+ channel gene family. Circ Res. 1998 Jul 13;83(1):103-9. [PubMed:9670923 ]
  4. Lee TS, Kaku T, Takebayashi S, Uchino T, Miyamoto S, Hadama T, Perez-Reyes E, Ono K: Actions of mibefradil, efonidipine and nifedipine block of recombinant T- and L-type Ca channels with distinct inhibitory mechanisms. Pharmacology. 2006;78(1):11-20. Epub 2006 Aug 7. [PubMed:16899990 ]
  5. Perez-Reyes E: Paradoxical role of T-type calcium channels in coronary smooth muscle. Mol Interv. 2004 Feb;4(1):16-8. [PubMed:14993472 ]
  6. Massie BM: Mibefradil: a selective T-type calcium antagonist. Am J Cardiol. 1997 Nov 6;80(9A):23I-32I. [PubMed:9375939 ]
  7. Clozel JP, Ertel EA, Ertel SI: Discovery and main pharmacological properties of mibefradil (Ro 40-5967), the first selective T-type calcium channel blocker. J Hypertens Suppl. 1997 Dec;15(5):S17-25. [PubMed:9481612 ]
  8. McNulty MM, Hanck DA: State-dependent mibefradil block of Na+ channels. Mol Pharmacol. 2004 Dec;66(6):1652-61. [PubMed:15562257 ]
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. Moosmang S, Haider N, Bruderl B, Welling A, Hofmann F: Antihypertensive effects of the putative T-type calcium channel antagonist mibefradil are mediated by the L-type calcium channel Cav1.2. Circ Res. 2006 Jan 6;98(1):105-10. Epub 2005 Nov 23. [PubMed:16306443 ]
  2. Lee TS, Kaku T, Takebayashi S, Uchino T, Miyamoto S, Hadama T, Perez-Reyes E, Ono K: Actions of mibefradil, efonidipine and nifedipine block of recombinant T- and L-type Ca channels with distinct inhibitory mechanisms. Pharmacology. 2006;78(1):11-20. Epub 2006 Aug 7. [PubMed:16899990 ]
  3. Mocanu MM, Gadgil S, Yellon DM, Baxter GF: Mibefradil, a T-type and L-type calcium channel blocker, limits infarct size through a glibenclamide-sensitive mechanism. Cardiovasc Drugs Ther. 1999 Apr;13(2):115-22. [PubMed:10372226 ]
  4. Jimenez C, Bourinet E, Leuranguer V, Richard S, Snutch TP, Nargeot J: Determinants of voltage-dependent inactivation affect Mibefradil block of calcium channels. Neuropharmacology. 2000;39(1):1-10. [PubMed:10665814 ]
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. Mocanu MM, Gadgil S, Yellon DM, Baxter GF: Mibefradil, a T-type and L-type calcium channel blocker, limits infarct size through a glibenclamide-sensitive mechanism. Cardiovasc Drugs Ther. 1999 Apr;13(2):115-22. [PubMed:10372226 ]
  2. Jimenez C, Bourinet E, Leuranguer V, Richard S, Snutch TP, Nargeot J: Determinants of voltage-dependent inactivation affect Mibefradil block of calcium channels. Neuropharmacology. 2000;39(1):1-10. [PubMed:10665814 ]
  3. Lee TS, Kaku T, Takebayashi S, Uchino T, Miyamoto S, Hadama T, Perez-Reyes E, Ono K: Actions of mibefradil, efonidipine and nifedipine block of recombinant T- and L-type Ca channels with distinct inhibitory mechanisms. Pharmacology. 2006;78(1):11-20. Epub 2006 Aug 7. [PubMed:16899990 ]
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. Mocanu MM, Gadgil S, Yellon DM, Baxter GF: Mibefradil, a T-type and L-type calcium channel blocker, limits infarct size through a glibenclamide-sensitive mechanism. Cardiovasc Drugs Ther. 1999 Apr;13(2):115-22. [PubMed:10372226 ]
  2. Jimenez C, Bourinet E, Leuranguer V, Richard S, Snutch TP, Nargeot J: Determinants of voltage-dependent inactivation affect Mibefradil block of calcium channels. Neuropharmacology. 2000;39(1):1-10. [PubMed:10665814 ]
  3. Lee TS, Kaku T, Takebayashi S, Uchino T, Miyamoto S, Hadama T, Perez-Reyes E, Ono K: Actions of mibefradil, efonidipine and nifedipine block of recombinant T- and L-type Ca channels with distinct inhibitory mechanisms. Pharmacology. 2006;78(1):11-20. Epub 2006 Aug 7. [PubMed:16899990 ]
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. Isoform alpha-1I gives rise to T-type calcium currents. T-type calcium channels belong to the "low-volta...
Gene Name:
CACNA1I
Uniprot ID:
Q9P0X4
Molecular Weight:
245100.8 Da
References
  1. Massie BM: Mibefradil: a selective T-type calcium antagonist. Am J Cardiol. 1997 Nov 6;80(9A):23I-32I. [PubMed:9375939 ]
  2. Clozel JP, Ertel EA, Ertel SI: Discovery and main pharmacological properties of mibefradil (Ro 40-5967), the first selective T-type calcium channel blocker. J Hypertens Suppl. 1997 Dec;15(5):S17-25. [PubMed:9481612 ]
  3. McNulty MM, Hanck DA: State-dependent mibefradil block of Na+ channels. Mol Pharmacol. 2004 Dec;66(6):1652-61. [PubMed:15562257 ]
  4. Lee TS, Kaku T, Takebayashi S, Uchino T, Miyamoto S, Hadama T, Perez-Reyes E, Ono K: Actions of mibefradil, efonidipine and nifedipine block of recombinant T- and L-type Ca channels with distinct inhibitory mechanisms. Pharmacology. 2006;78(1):11-20. Epub 2006 Aug 7. [PubMed:16899990 ]
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. Mocanu MM, Gadgil S, Yellon DM, Baxter GF: Mibefradil, a T-type and L-type calcium channel blocker, limits infarct size through a glibenclamide-sensitive mechanism. Cardiovasc Drugs Ther. 1999 Apr;13(2):115-22. [PubMed:10372226 ]
  2. Jimenez C, Bourinet E, Leuranguer V, Richard S, Snutch TP, Nargeot J: Determinants of voltage-dependent inactivation affect Mibefradil block of calcium channels. Neuropharmacology. 2000;39(1):1-10. [PubMed:10665814 ]
  3. Lee TS, Kaku T, Takebayashi S, Uchino T, Miyamoto S, Hadama T, Perez-Reyes E, Ono K: Actions of mibefradil, efonidipine and nifedipine block of recombinant T- and L-type Ca channels with distinct inhibitory mechanisms. Pharmacology. 2006;78(1):11-20. Epub 2006 Aug 7. [PubMed:16899990 ]
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. Lee TS, Kaku T, Takebayashi S, Uchino T, Miyamoto S, Hadama T, Perez-Reyes E, Ono K: Actions of mibefradil, efonidipine and nifedipine block of recombinant T- and L-type Ca channels with distinct inhibitory mechanisms. Pharmacology. 2006;78(1):11-20. Epub 2006 Aug 7. [PubMed:16899990 ]
  2. Mocanu MM, Gadgil S, Yellon DM, Baxter GF: Mibefradil, a T-type and L-type calcium channel blocker, limits infarct size through a glibenclamide-sensitive mechanism. Cardiovasc Drugs Ther. 1999 Apr;13(2):115-22. [PubMed:10372226 ]
  3. Jimenez C, Bourinet E, Leuranguer V, Richard S, Snutch TP, Nargeot J: Determinants of voltage-dependent inactivation affect Mibefradil block of calcium channels. Neuropharmacology. 2000;39(1):1-10. [PubMed:10665814 ]
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. Lee TS, Kaku T, Takebayashi S, Uchino T, Miyamoto S, Hadama T, Perez-Reyes E, Ono K: Actions of mibefradil, efonidipine and nifedipine block of recombinant T- and L-type Ca channels with distinct inhibitory mechanisms. Pharmacology. 2006;78(1):11-20. Epub 2006 Aug 7. [PubMed:16899990 ]
  2. Mocanu MM, Gadgil S, Yellon DM, Baxter GF: Mibefradil, a T-type and L-type calcium channel blocker, limits infarct size through a glibenclamide-sensitive mechanism. Cardiovasc Drugs Ther. 1999 Apr;13(2):115-22. [PubMed:10372226 ]
  3. Jimenez C, Bourinet E, Leuranguer V, Richard S, Snutch TP, Nargeot J: Determinants of voltage-dependent inactivation affect Mibefradil block of calcium channels. Neuropharmacology. 2000;39(1):1-10. [PubMed:10665814 ]
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. Lee TS, Kaku T, Takebayashi S, Uchino T, Miyamoto S, Hadama T, Perez-Reyes E, Ono K: Actions of mibefradil, efonidipine and nifedipine block of recombinant T- and L-type Ca channels with distinct inhibitory mechanisms. Pharmacology. 2006;78(1):11-20. Epub 2006 Aug 7. [PubMed:16899990 ]
  2. Mocanu MM, Gadgil S, Yellon DM, Baxter GF: Mibefradil, a T-type and L-type calcium channel blocker, limits infarct size through a glibenclamide-sensitive mechanism. Cardiovasc Drugs Ther. 1999 Apr;13(2):115-22. [PubMed:10372226 ]
  3. Jimenez C, Bourinet E, Leuranguer V, Richard S, Snutch TP, Nargeot J: Determinants of voltage-dependent inactivation affect Mibefradil block of calcium channels. Neuropharmacology. 2000;39(1):1-10. [PubMed:10665814 ]
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. Lee TS, Kaku T, Takebayashi S, Uchino T, Miyamoto S, Hadama T, Perez-Reyes E, Ono K: Actions of mibefradil, efonidipine and nifedipine block of recombinant T- and L-type Ca channels with distinct inhibitory mechanisms. Pharmacology. 2006;78(1):11-20. Epub 2006 Aug 7. [PubMed:16899990 ]
  2. Mocanu MM, Gadgil S, Yellon DM, Baxter GF: Mibefradil, a T-type and L-type calcium channel blocker, limits infarct size through a glibenclamide-sensitive mechanism. Cardiovasc Drugs Ther. 1999 Apr;13(2):115-22. [PubMed:10372226 ]
  3. Jimenez C, Bourinet E, Leuranguer V, Richard S, Snutch TP, Nargeot J: Determinants of voltage-dependent inactivation affect Mibefradil block of calcium channels. Neuropharmacology. 2000;39(1):1-10. [PubMed:10665814 ]

Enzymes

Kind
Protein
Organism
Human
Pharmacological action
unknown
Actions
substrateinhibitor
General Function:
Vitamin d3 25-hydroxylase activity
Specific Function:
Cytochromes P450 are a group of heme-thiolate monooxygenases. In liver microsomes, this enzyme is involved in an NADPH-dependent electron transport pathway. It performs a variety of oxidation reactions (e.g. caffeine 8-oxidation, omeprazole sulphoxidation, midazolam 1'-hydroxylation and midazolam 4-hydroxylation) of structurally unrelated compounds, including steroids, fatty acids, and xenobiot...
Gene Name:
CYP3A4
Uniprot ID:
P08684
Molecular Weight:
57342.67 Da
References
  1. Preissner S, Kroll K, Dunkel M, Senger C, Goldsobel G, Kuzman D, Guenther S, Winnenburg R, Schroeder M, Preissner R: SuperCYP: a comprehensive database on Cytochrome P450 enzymes including a tool for analysis of CYP-drug interactions. Nucleic Acids Res. 2010 Jan;38(Database issue):D237-43. doi: 10.1093/nar/gkp970. Epub 2009 Nov 24. [PubMed:19934256 ]
  2. Drug Interactions: Cytochrome P450 Drug Interaction Table [Link]
Kind
Protein
Organism
Human
Pharmacological action
unknown
Actions
inhibitor
General Function:
Oxidoreductase activity, acting on paired donors, with incorporation or reduction of molecular oxygen, reduced flavin or flavoprotein as one donor, and incorporation of one atom of oxygen
Specific Function:
Cytochromes P450 are a group of heme-thiolate monooxygenases. In liver microsomes, this enzyme is involved in an NADPH-dependent electron transport pathway. It oxidizes a variety of structurally unrelated compounds, including steroids, fatty acids, and xenobiotics. Most active in catalyzing 2-hydroxylation. Caffeine is metabolized primarily by cytochrome CYP1A2 in the liver through an initial N...
Gene Name:
CYP1A2
Uniprot ID:
P05177
Molecular Weight:
58293.76 Da
References
  1. Preissner S, Kroll K, Dunkel M, Senger C, Goldsobel G, Kuzman D, Guenther S, Winnenburg R, Schroeder M, Preissner R: SuperCYP: a comprehensive database on Cytochrome P450 enzymes including a tool for analysis of CYP-drug interactions. Nucleic Acids Res. 2010 Jan;38(Database issue):D237-43. doi: 10.1093/nar/gkp970. Epub 2009 Nov 24. [PubMed:19934256 ]
  2. Drug Interactions: Cytochrome P450 Drug Interaction Table [Link]
Kind
Protein
Organism
Human
Pharmacological action
unknown
Actions
inhibitor
General Function:
Steroid hydroxylase activity
Specific Function:
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 ]
  2. Drug Interactions: Cytochrome P450 Drug Interaction Table [Link]
Kind
Protein
Organism
Human
Pharmacological action
unknown
Actions
inhibitor
General Function:
Oxygen binding
Specific Function:
Cytochromes P450 are a group of heme-thiolate monooxygenases. In liver microsomes, this enzyme is involved in an NADPH-dependent electron transport pathway. It oxidizes a variety of structurally unrelated compounds, including steroids, fatty acids, and xenobiotics.
Gene Name:
CYP3A5
Uniprot ID:
P20815
Molecular Weight:
57108.065 Da
References
  1. Preissner S, Kroll K, Dunkel M, Senger C, Goldsobel G, Kuzman D, Guenther S, Winnenburg R, Schroeder M, Preissner R: SuperCYP: a comprehensive database on Cytochrome P450 enzymes including a tool for analysis of CYP-drug interactions. Nucleic Acids Res. 2010 Jan;38(Database issue):D237-43. doi: 10.1093/nar/gkp970. Epub 2009 Nov 24. [PubMed:19934256 ]
  2. Drug Interactions: Cytochrome P450 Drug Interaction Table [Link]
Kind
Protein
Organism
Human
Pharmacological action
unknown
Actions
inhibitor
General Function:
Oxygen binding
Specific Function:
Cytochromes P450 are a group of heme-thiolate monooxygenases. In liver microsomes, this enzyme is involved in an NADPH-dependent electron transport pathway. It oxidizes a variety of structurally unrelated compounds, including steroids, fatty acids, and xenobiotics.
Gene Name:
CYP3A7
Uniprot ID:
P24462
Molecular Weight:
57525.03 Da
References
  1. Preissner S, Kroll K, Dunkel M, Senger C, Goldsobel G, Kuzman D, Guenther S, Winnenburg R, Schroeder M, Preissner R: SuperCYP: a comprehensive database on Cytochrome P450 enzymes including a tool for analysis of CYP-drug interactions. Nucleic Acids Res. 2010 Jan;38(Database issue):D237-43. doi: 10.1093/nar/gkp970. Epub 2009 Nov 24. [PubMed:19934256 ]
  2. Drug Interactions: Cytochrome P450 Drug Interaction Table [Link]
Kind
Protein
Organism
Human
Pharmacological action
unknown
Actions
inhibitor
General Function:
Steroid 11-beta-monooxygenase activity
Specific Function:
Has steroid 11-beta-hydroxylase activity. In addition to this activity, the 18 or 19-hydroxylation of steroids and the aromatization of androstendione to estrone have also been ascribed to cytochrome P450 XIB.
Gene Name:
CYP11B1
Uniprot ID:
P15538
Molecular Weight:
57572.44 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 11-beta-monooxygenase activity
Specific Function:
Preferentially catalyzes the conversion of 11-deoxycorticosterone to aldosterone via corticosterone and 18-hydroxycorticosterone.
Gene Name:
CYP11B2
Uniprot ID:
P19099
Molecular Weight:
57559.62 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:
Vitamin d 24-hydroxylase activity
Specific Function:
Cytochromes P450 are a group of heme-thiolate monooxygenases. In liver microsomes, this enzyme is involved in an NADPH-dependent electron transport pathway. It oxidizes a variety of structurally unrelated compounds, including steroids, fatty acids, and xenobiotics.
Gene Name:
CYP1A1
Uniprot ID:
P04798
Molecular Weight:
58164.815 Da
References
  1. Preissner S, Kroll K, Dunkel M, Senger C, Goldsobel G, Kuzman D, Guenther S, Winnenburg R, Schroeder M, Preissner R: SuperCYP: a comprehensive database on Cytochrome P450 enzymes including a tool for analysis of CYP-drug interactions. Nucleic Acids Res. 2010 Jan;38(Database issue):D237-43. doi: 10.1093/nar/gkp970. Epub 2009 Nov 24. [PubMed:19934256 ]

Transporters

Kind
Protein
Organism
Human
Pharmacological action
unknown
Actions
inhibitor
General Function:
Xenobiotic-transporting atpase activity
Specific Function:
Energy-dependent efflux pump responsible for decreased drug accumulation in multidrug-resistant cells.
Gene Name:
ABCB1
Uniprot ID:
P08183
Molecular Weight:
141477.255 Da
References
  1. Wandel C, Kim RB, Guengerich FP, Wood AJ: Mibefradil is a P-glycoprotein substrate and a potent inhibitor of both P-glycoprotein and CYP3A in vitro. Drug Metab Dispos. 2000 Aug;28(8):895-8. [PubMed:10901697 ]
  2. Ekins S, Kim RB, Leake BF, Dantzig AH, Schuetz EG, Lan LB, Yasuda K, Shepard RL, Winter MA, Schuetz JD, Wikel JH, Wrighton SA: Three-dimensional quantitative structure-activity relationships of inhibitors of P-glycoprotein. Mol Pharmacol. 2002 May;61(5):964-73. [PubMed:11961113 ]
  3. 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 ]
  4. Nagy H, Goda K, Fenyvesi F, Bacso Z, Szilasi M, Kappelmayer J, Lustyik G, Cianfriglia M, Szabo G Jr: Distinct groups of multidrug resistance modulating agents are distinguished by competition of P-glycoprotein-specific antibodies. Biochem Biophys Res Commun. 2004 Mar 19;315(4):942-9. [PubMed:14985103 ]
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Drug created on July 06, 2007 14:41 / Updated on August 17, 2016 12:23