Identification

Name
Flunarizine
Accession Number
DB04841
Type
Small Molecule
Groups
Approved
Description

Flunarizine is a selective calcium entry blocker with calmodulin binding properties and histamine H1 blocking activity. It is effective in the prophylaxis of migraine, occlusive peripheral vascular disease, vertigo of central and peripheral origin, and as an adjuvant in the therapy of epilepsy.

Structure
Thumb
Synonyms
  • 1-[bis(4-fluorophenyl)methyl]-4-[(2E)-3-phenylprop-2-en-1-yl]piperazine
  • Flunarizina
  • Flunarizinum
Product Ingredients
IngredientUNIICASInChI Key
Flunarizine dihydrochlorideC11102TO5330484-77-6RXKMOPXNWTYEHI-RDRKJGRWSA-N
Prescription Products
NameDosageStrengthRouteLabellerMarketing StartMarketing End
FlunarizineCapsule5 mgOralAa Pharma Inc2002-08-08Not applicableCanada
Sibelium Cap 5mgCapsule5 mgOralPharmascience Inc1990-12-312009-01-29Canada
Generic Prescription Products
NameDosageStrengthRouteLabellerMarketing StartMarketing End
Novo-flunarizine - Cap 5mgCapsule5 mgOralNovopharm Limited1998-04-302015-10-26Canada
International/Other Brands
Flugeral (Italfarmaco) / Fluxarten (GlaxoSmithKline) / Gradient (Polifarma) / Sibelium (Janssen) / Zinasen (AtralCipan)
Categories
UNII
R7PLA2DM0J
CAS number
52468-60-7
Weight
Average: 404.4948
Monoisotopic: 404.206405252
Chemical Formula
C26H26F2N2
InChI Key
SMANXXCATUTDDT-QPJJXVBHSA-N
InChI
InChI=1S/C26H26F2N2/c27-24-12-8-22(9-13-24)26(23-10-14-25(28)15-11-23)30-19-17-29(18-20-30)16-4-7-21-5-2-1-3-6-21/h1-15,26H,16-20H2/b7-4+
IUPAC Name
1-[bis(4-fluorophenyl)methyl]-4-[(2E)-3-phenylprop-2-en-1-yl]piperazine
SMILES
FC1=CC=C(C=C1)C(N1CCN(C\C=C\C2=CC=CC=C2)CC1)C1=CC=C(F)C=C1

Pharmacology

Indication

Used in the prophylaxis of migraine, occlusive peripheral vascular disease, vertigo of central and peripheral origin, and as an adjuvant in the therapy of epilepsy.

Structured Indications
Pharmacodynamics

Flunarizine is a selective calcium entry blocker with calmodulin binding properties and histamine H1 blocking activity.

Mechanism of action

Flunarizine inhibits the influx of extracellular calcium through myocardial and vascular membrane pores by physically plugging the channel. The decrease in intracellular calcium inhibits the contractile processes of smooth muscle cells, causing dilation of the coronary and systemic arteries, increased oxygen delivery to the myocardial tissue, decreased total peripheral resistance, decreased systemic blood pressure, and decreased afterload.

TargetActionsOrganism
AVoltage-dependent T-type calcium channel subunit alpha-1G
inhibitor
Human
AVoltage-dependent T-type calcium channel subunit alpha-1H
inhibitor
Human
AVoltage-dependent T-type calcium channel subunit alpha-1I
inhibitor
Human
UHistamine H1 receptor
antagonist
Human
UCalmodulinNot AvailableHuman
Absorption

85% following oral administration.

Volume of distribution
Not Available
Protein binding

99% bound to plasma proteins

Metabolism

Hepatic, to two metabolites via N-dealylation and hydroxylation.

Route of elimination
Not Available
Half life

18 days

Clearance
Not Available
Toxicity

-Flunarizine should be used with care in patients with depression or those being prescribed other agents, such as phenothiazines, concurrently, which may cause extrapyramidal side-effects. -Acute overdosage has been reported and the observed symptoms were sedation, agitation and tachycardia. -Treatment of acute overdosage consists of charcoal administration, induction of emesis or gastric lavage, and supportive measures. No specific antidote is known.

Affected organisms
  • Humans and other mammals
Pathways
PathwayCategory
Flunarizine H1-Antihistamine ActionDrug action
Pharmacogenomic Effects/ADRs
Not 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 Flunarizine.Experimental
2-mercaptobenzothiazoleThe risk or severity of adverse effects can be increased when 2-mercaptobenzothiazole is combined with Flunarizine.Vet Approved
2,5-Dimethoxy-4-ethylamphetamine2,5-Dimethoxy-4-ethylamphetamine may decrease the sedative activities of Flunarizine.Experimental, Illicit
2,5-Dimethoxy-4-ethylthioamphetamine2,5-Dimethoxy-4-ethylthioamphetamine may decrease the sedative activities of Flunarizine.Experimental
3,4-Methylenedioxyamphetamine3,4-Methylenedioxyamphetamine may decrease the sedative activities of Flunarizine.Experimental, Illicit
4-Bromo-2,5-dimethoxyamphetamine4-Bromo-2,5-dimethoxyamphetamine may decrease the sedative activities of Flunarizine.Experimental, Illicit
AbirateroneThe serum concentration of Flunarizine can be increased when it is combined with Abiraterone.Approved
AlfuzosinAlfuzosin may increase the hypotensive activities of Flunarizine.Approved, Investigational
AmiodaroneThe metabolism of Flunarizine can be decreased when combined with Amiodarone.Approved, Investigational
AmobarbitalThe metabolism of Flunarizine can be increased when combined with Amobarbital.Approved, Illicit
AmorolfineThe risk or severity of adverse effects can be increased when Amorolfine is combined with Flunarizine.Approved, Investigational
AmphetamineAmphetamine may decrease the sedative activities of Flunarizine.Approved, Illicit
Amphotericin BThe risk or severity of adverse effects can be increased when Amphotericin B is combined with Flunarizine.Approved, Investigational
AnidulafunginThe risk or severity of adverse effects can be increased when Anidulafungin is combined with Flunarizine.Approved, Investigational
AprepitantThe metabolism of Flunarizine can be increased when combined with Aprepitant.Approved, Investigational
ArotinololThe risk or severity of hypotension, conduction block, and bradycardia can be increased when Arotinolol is combined with Flunarizine.Investigational
ArtemetherThe risk or severity of adverse effects can be increased when Artemether is combined with Flunarizine.Approved
AtomoxetineThe metabolism of Flunarizine can be decreased when combined with Atomoxetine.Approved
AtorvastatinThe risk or severity of adverse effects can be increased when Flunarizine is combined with Atorvastatin.Approved
AtosibanThe risk or severity of adverse effects can be increased when Flunarizine is combined with Atosiban.Approved, Investigational
AzithromycinThe metabolism of Flunarizine can be decreased when combined with Azithromycin.Approved
Bafilomycin A1The risk or severity of adverse effects can be increased when Bafilomycin A1 is combined with Flunarizine.Experimental
BarbexacloneThe metabolism of Flunarizine can be increased when combined with Barbexaclone.Experimental
BarbitalThe metabolism of Flunarizine can be increased when combined with Barbital.Illicit
Benzoic AcidThe risk or severity of adverse effects can be increased when Benzoic Acid is combined with Flunarizine.Approved
BenzphetamineBenzphetamine may decrease the sedative activities of Flunarizine.Approved, Illicit
Benzylpenicilloyl PolylysineFlunarizine may decrease effectiveness of Benzylpenicilloyl Polylysine as a diagnostic agent.Approved
BetahistineThe therapeutic efficacy of Betahistine can be decreased when used in combination with Flunarizine.Approved
BetaxololThe metabolism of Flunarizine can be decreased when combined with Betaxolol.Approved
BifonazoleThe risk or severity of adverse effects can be increased when Bifonazole is combined with Flunarizine.Approved, Investigational
BortezomibThe metabolism of Flunarizine can be decreased when combined with Bortezomib.Approved, Investigational
Brefeldin AThe risk or severity of adverse effects can be increased when Brefeldin A is combined with Flunarizine.Experimental
BucindololBucindolol may increase the hypotensive activities of Flunarizine.Investigational
BunazosinBunazosin may increase the hypotensive activities of Flunarizine.Investigational
BupropionThe metabolism of Flunarizine can be decreased when combined with Bupropion.Approved
ButenafineThe risk or severity of adverse effects can be increased when Butenafine is combined with Flunarizine.Approved
ButoconazoleThe risk or severity of adverse effects can be increased when Butoconazole is combined with Flunarizine.Approved
CaffeineThe metabolism of Flunarizine can be decreased when combined with Caffeine.Approved
Calcium AcetateThe therapeutic efficacy of Flunarizine can be decreased when used in combination with Calcium Acetate.Approved
Calcium CarbonateThe therapeutic efficacy of Flunarizine can be decreased when used in combination with Calcium Carbonate.Approved
Calcium ChlorideThe therapeutic efficacy of Flunarizine can be decreased when used in combination with Calcium Chloride.Approved
Calcium CitrateThe therapeutic efficacy of Flunarizine can be decreased when used in combination with Calcium Citrate.Approved
Calcium glubionateThe therapeutic efficacy of Flunarizine can be decreased when used in combination with Calcium glubionate.Approved
Calcium GluceptateThe therapeutic efficacy of Flunarizine can be decreased when used in combination with Calcium Gluceptate.Approved
Calcium gluconateThe therapeutic efficacy of Flunarizine can be decreased when used in combination with Calcium gluconate.Approved, Vet Approved
Calcium lactateThe therapeutic efficacy of Flunarizine can be decreased when used in combination with Calcium lactate.Approved, Experimental, Investigational, Vet Approved
Calcium lactate gluconateThe therapeutic efficacy of Flunarizine can be decreased when used in combination with Calcium lactate gluconate.Experimental
Calcium levulinateThe therapeutic efficacy of Flunarizine can be decreased when used in combination with Calcium laevulate.Experimental
Calcium pangamateThe therapeutic efficacy of Flunarizine can be decreased when used in combination with Calcium pangamate.Experimental
Calcium PhosphateThe therapeutic efficacy of Flunarizine can be decreased when used in combination with Calcium Phosphate.Approved
CandicidinThe risk or severity of adverse effects can be increased when Candicidin is combined with Flunarizine.Withdrawn
CapecitabineThe metabolism of Flunarizine can be decreased when combined with Capecitabine.Approved, Investigational
Capric acidThe risk or severity of adverse effects can be increased when Capric acid is combined with Flunarizine.Experimental
CarbamazepineThe serum concentration of Flunarizine can be decreased when it is combined with Carbamazepine.Approved, Investigational
CarbomycinThe metabolism of Flunarizine can be decreased when combined with Carbomycin.Vet Approved
CarvedilolCarvedilol may increase the hypotensive activities of Flunarizine.Approved, Investigational
CaseinThe therapeutic efficacy of Flunarizine can be decreased when used in combination with Casein.Approved
CaspofunginThe risk or severity of adverse effects can be increased when Caspofungin is combined with Flunarizine.Approved
CelecoxibThe metabolism of Flunarizine can be decreased when combined with Celecoxib.Approved, Investigational
CeritinibThe serum concentration of Flunarizine can be increased when it is combined with Ceritinib.Approved
CerivastatinThe risk or severity of adverse effects can be increased when Flunarizine is combined with Cerivastatin.Withdrawn
CeruleninThe risk or severity of adverse effects can be increased when Cerulenin is combined with Flunarizine.Approved
ChloroquineThe metabolism of Flunarizine can be decreased when combined with Chloroquine.Approved, Vet Approved
ChloroxineThe risk or severity of adverse effects can be increased when Chloroxine is combined with Flunarizine.Approved
ChlorphentermineChlorphentermine may decrease the sedative activities of Flunarizine.Illicit, Withdrawn
ChlorpromazineThe metabolism of Flunarizine can be decreased when combined with Chlorpromazine.Approved, Vet Approved
CholecalciferolThe metabolism of Flunarizine can be decreased when combined with Cholecalciferol.Approved, Nutraceutical
CiclopiroxThe risk or severity of adverse effects can be increased when Ciclopirox is combined with Flunarizine.Approved, Investigational
CimetidineThe serum concentration of Flunarizine can be increased when it is combined with Cimetidine.Approved
CinacalcetThe metabolism of Flunarizine can be decreased when combined with Cinacalcet.Approved
CitalopramThe metabolism of Flunarizine can be decreased when combined with Citalopram.Approved
ClarithromycinThe metabolism of Flunarizine can be decreased when combined with Clarithromycin.Approved
ClemastineThe metabolism of Flunarizine can be decreased when combined with Clemastine.Approved
ClobazamThe metabolism of Flunarizine can be decreased when combined with Clobazam.Approved, Illicit
ClomipramineThe metabolism of Flunarizine can be decreased when combined with Clomipramine.Approved, Vet Approved
ClopidogrelThe therapeutic efficacy of Clopidogrel can be decreased when used in combination with Flunarizine.Approved
ClotrimazoleThe risk or severity of adverse effects can be increased when Clotrimazole is combined with Flunarizine.Approved, Vet Approved
ClozapineThe metabolism of Flunarizine can be decreased when combined with Clozapine.Approved
CobicistatThe serum concentration of Flunarizine can be increased when it is combined with Cobicistat.Approved
CocaineThe metabolism of Flunarizine can be decreased when combined with Cocaine.Approved, Illicit
CordycepinThe risk or severity of adverse effects can be increased when Cordycepin is combined with Flunarizine.Investigational
CrisaboroleThe metabolism of Flunarizine can be decreased when combined with Crisaborole.Approved, Investigational
CrizotinibThe metabolism of Flunarizine can be decreased when combined with Crizotinib.Approved
CyclosporineThe risk or severity of adverse effects can be increased when Cyclosporine is combined with Flunarizine.Approved, Investigational, Vet Approved
Cyproterone acetateThe serum concentration of Flunarizine can be decreased when it is combined with Cyproterone acetate.Approved, Investigational
DabrafenibThe serum concentration of Flunarizine can be decreased when it is combined with Dabrafenib.Approved
DapoxetineDapoxetine may increase the orthostatic hypotensive activities of Flunarizine.Investigational
DarifenacinThe metabolism of Flunarizine can be decreased when combined with Darifenacin.Approved, Investigational
DarunavirThe serum concentration of Flunarizine can be increased when it is combined with Darunavir.Approved
DeferasiroxThe serum concentration of Flunarizine can be increased when it is combined with Deferasirox.Approved, Investigational
DelavirdineThe metabolism of Flunarizine can be decreased when combined with Delavirdine.Approved
DesipramineThe metabolism of Flunarizine can be decreased when combined with Desipramine.Approved
DextroamphetamineDextroamphetamine may decrease the sedative activities of Flunarizine.Approved, Illicit
DichloropheneThe risk or severity of adverse effects can be increased when Dichlorophene is combined with Flunarizine.Vet Approved
DiethylpropionDiethylpropion may decrease the sedative activities of Flunarizine.Approved, Illicit
DiphenhydramineThe metabolism of Flunarizine can be decreased when combined with Diphenhydramine.Approved
DosulepinThe metabolism of Flunarizine can be decreased when combined with Dosulepin.Approved
DoxazosinDoxazosin may increase the hypotensive activities of Flunarizine.Approved
DoxofyllineThe serum concentration of Doxofylline can be decreased when it is combined with Flunarizine.Approved, Investigational
DoxorubicinThe metabolism of Flunarizine can be decreased when combined with Doxorubicin.Approved, Investigational
DronedaroneThe metabolism of Flunarizine can be decreased when combined with Dronedarone.Approved
DuloxetineThe metabolism of Flunarizine can be decreased when combined with Duloxetine.Approved
EconazoleThe risk or severity of adverse effects can be increased when Econazole is combined with Flunarizine.Approved
EfavirenzThe serum concentration of Flunarizine 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 Flunarizine.Approved
EliglustatThe metabolism of Flunarizine can be decreased when combined with Eliglustat.Approved
ErythromycinThe metabolism of Flunarizine can be decreased when combined with Erythromycin.Approved, Vet Approved
EtravirineThe metabolism of Flunarizine can be decreased when combined with Etravirine.Approved
FenticonazoleThe risk or severity of adverse effects can be increased when Fenticonazole is combined with Flunarizine.Experimental
FloxuridineThe metabolism of Flunarizine can be decreased when combined with Floxuridine.Approved
FluconazoleThe serum concentration of Flunarizine 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 Flunarizine.Approved
FluorouracilThe metabolism of Flunarizine can be decreased when combined with Fluorouracil.Approved
FluoxetineThe metabolism of Flunarizine can be decreased when combined with Fluoxetine.Approved, Vet Approved
FlutrimazoleThe risk or severity of adverse effects can be increased when Flutrimazole is combined with Flunarizine.Experimental
FluvastatinThe metabolism of Flunarizine can be decreased when combined with Fluvastatin.Approved
FluvoxamineThe metabolism of Flunarizine can be decreased when combined with Fluvoxamine.Approved, Investigational
FosphenytoinThe serum concentration of Flunarizine can be decreased when it is combined with Fosphenytoin.Approved
GemfibrozilThe metabolism of Flunarizine can be decreased when combined with Gemfibrozil.Approved
GepefrineGepefrine may decrease the sedative activities of Flunarizine.Experimental
GlyphosateThe risk or severity of adverse effects can be increased when Glyphosate is combined with Flunarizine.Experimental
GriseofulvinThe risk or severity of adverse effects can be increased when Griseofulvin is combined with Flunarizine.Approved, Vet Approved
HachimycinThe risk or severity of adverse effects can be increased when Hachimycin is combined with Flunarizine.Experimental
HaloperidolThe metabolism of Flunarizine can be decreased when combined with Haloperidol.Approved
HaloproginThe risk or severity of adverse effects can be increased when Haloprogin is combined with Flunarizine.Approved, Withdrawn
HexetidineThe risk or severity of adverse effects can be increased when Hexetidine is combined with Flunarizine.Approved, Investigational
HexobarbitalThe metabolism of Flunarizine can be increased when combined with Hexobarbital.Approved
HyaluronidaseThe therapeutic efficacy of Hyaluronidase can be decreased when used in combination with Flunarizine.Approved, Investigational
HydroxyamphetamineHydroxyamphetamine may decrease the sedative activities of Flunarizine.Approved
ImipramineThe metabolism of Flunarizine can be decreased when combined with Imipramine.Approved
IndinavirThe metabolism of Flunarizine can be decreased when combined with Indinavir.Approved
IndoraminIndoramin may increase the hypotensive activities of Flunarizine.Withdrawn
Iofetamine I-123Iofetamine I-123 may decrease the sedative activities of Flunarizine.Approved
IrbesartanThe metabolism of Flunarizine can be decreased when combined with Irbesartan.Approved, Investigational
IsoconazoleThe risk or severity of adverse effects can be increased when Isoconazole is combined with Flunarizine.Approved
IsoniazidThe metabolism of Flunarizine can be decreased when combined with Isoniazid.Approved
ItraconazoleThe risk or severity of adverse effects can be increased when Itraconazole is combined with Flunarizine.Approved, Investigational
JosamycinThe metabolism of Flunarizine can be decreased when combined with Josamycin.Approved, Investigational
KetoconazoleThe risk or severity of adverse effects can be increased when Ketoconazole is combined with Flunarizine.Approved, Investigational
KitasamycinThe metabolism of Flunarizine can be decreased when combined with Kitasamycin.Experimental
LabetalolLabetalol may increase the hypotensive activities of Flunarizine.Approved
LeflunomideThe metabolism of Flunarizine can be decreased when combined with Leflunomide.Approved, Investigational
LidocaineThe metabolism of Flunarizine can be decreased when combined with Lidocaine.Approved, Vet Approved
LisdexamfetamineLisdexamfetamine may decrease the sedative activities of Flunarizine.Approved, Investigational
LobeglitazoneThe metabolism of Flunarizine can be decreased when combined with Lobeglitazone.Approved, Investigational
LopinavirThe metabolism of Flunarizine can be decreased when combined with Lopinavir.Approved
LorcaserinThe metabolism of Flunarizine can be decreased when combined with Lorcaserin.Approved
LosartanThe metabolism of Flunarizine can be decreased when combined with Losartan.Approved
LovastatinThe metabolism of Flunarizine can be decreased when combined with Lovastatin.Approved, Investigational
LumacaftorThe serum concentration of Flunarizine can be decreased when it is combined with Lumacaftor.Approved
LumefantrineThe metabolism of Flunarizine can be decreased when combined with Lumefantrine.Approved
ManidipineThe metabolism of Flunarizine can be decreased when combined with Manidipine.Approved, Investigational
MefloquineThe therapeutic efficacy of Flunarizine can be decreased when used in combination with Mefloquine.Approved
MepartricinThe risk or severity of adverse effects can be increased when Mepartricin is combined with Flunarizine.Experimental
MephedroneMephedrone may decrease the sedative activities of Flunarizine.Investigational
MephentermineMephentermine may decrease the sedative activities of Flunarizine.Approved
MethadoneThe metabolism of Flunarizine can be decreased when combined with Methadone.Approved
MethamphetamineMethamphetamine may decrease the sedative activities of Flunarizine.Approved, Illicit
MethohexitalThe metabolism of Flunarizine can be increased when combined with Methohexital.Approved
MethotrimeprazineThe metabolism of Flunarizine can be decreased when combined with Methotrimeprazine.Approved
MethoxyphenamineMethoxyphenamine may decrease the sedative activities of Flunarizine.Experimental
MethylphenobarbitalThe metabolism of Flunarizine can be increased when combined with Methylphenobarbital.Approved
MetoprololThe metabolism of Flunarizine can be decreased when combined with Metoprolol.Approved, Investigational
MevastatinThe risk or severity of adverse effects can be increased when Mevastatin is combined with Flunarizine.Experimental
MexiletineThe metabolism of Flunarizine can be decreased when combined with Mexiletine.Approved
MianserinThe therapeutic efficacy of Flunarizine can be decreased when used in combination with Mianserin.Approved, Investigational
MicafunginThe risk or severity of adverse effects can be increased when Micafungin is combined with Flunarizine.Approved, Investigational
MiconazoleThe risk or severity of adverse effects can be increased when Miconazole is combined with Flunarizine.Approved, Investigational, Vet Approved
MidomafetamineMidomafetamine may decrease the sedative activities of Flunarizine.Experimental, Illicit, Investigational
MidostaurinThe metabolism of Flunarizine can be decreased when combined with Midostaurin.Approved
MifepristoneThe serum concentration of Flunarizine 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 Flunarizine.Approved
MirabegronThe metabolism of Flunarizine can be decreased when combined with Mirabegron.Approved
MMDAMMDA may decrease the sedative activities of Flunarizine.Experimental, Illicit
MonensinThe risk or severity of adverse effects can be increased when Monensin is combined with Flunarizine.Vet Approved
MyxothiazolThe risk or severity of adverse effects can be increased when Myxothiazol is combined with Flunarizine.Experimental
NafcillinThe metabolism of Flunarizine can be increased when combined with Nafcillin.Approved
NaftifineThe risk or severity of adverse effects can be increased when Naftifine is combined with Flunarizine.Approved
NatamycinThe risk or severity of adverse effects can be increased when Natamycin is combined with Flunarizine.Approved
NevirapineThe metabolism of Flunarizine can be increased when combined with Nevirapine.Approved
NicardipineThe metabolism of Flunarizine can be decreased when combined with Nicardipine.Approved
NicotineThe metabolism of Flunarizine can be decreased when combined with Nicotine.Approved
NifuratelThe risk or severity of adverse effects can be increased when Nifuratel is combined with Flunarizine.Experimental
Nikkomycin ZThe risk or severity of adverse effects can be increased when Nikkomycin Z is combined with Flunarizine.Investigational
NilotinibThe metabolism of Flunarizine can be decreased when combined with Nilotinib.Approved, Investigational
NitroprussideFlunarizine may increase the hypotensive activities of Nitroprusside.Approved
NitroxolineThe risk or severity of adverse effects can be increased when Nitroxoline is combined with Flunarizine.Approved
NystatinThe risk or severity of adverse effects can be increased when Nystatin is combined with Flunarizine.Approved, Vet Approved
OleandomycinThe metabolism of Flunarizine can be decreased when combined with Oleandomycin.Vet Approved
OmeprazoleThe metabolism of Flunarizine can be decreased when combined with Omeprazole.Approved, Investigational, Vet Approved
OmoconazoleThe risk or severity of adverse effects can be increased when Omoconazole is combined with Flunarizine.Experimental
OrlistatThe serum concentration of Flunarizine can be decreased when it is combined with Orlistat.Approved, Investigational
OsimertinibThe serum concentration of Flunarizine can be decreased when it is combined with Osimertinib.Approved
OxiconazoleThe risk or severity of adverse effects can be increased when Oxiconazole is combined with Flunarizine.Approved
PafuramidineThe risk or severity of adverse effects can be increased when Pafuramidine is combined with Flunarizine.Investigational
PanobinostatThe serum concentration of Flunarizine can be increased when it is combined with Panobinostat.Approved, Investigational
ParoxetineThe metabolism of Flunarizine can be decreased when combined with Paroxetine.Approved, Investigational
Peginterferon alfa-2bThe serum concentration of Flunarizine can be decreased when it is combined with Peginterferon alfa-2b.Approved
PentamidineThe risk or severity of adverse effects can be increased when Pentamidine is combined with Flunarizine.Approved
PentobarbitalThe metabolism of Flunarizine can be increased when combined with Pentobarbital.Approved, Vet Approved
PhenobarbitalThe metabolism of Flunarizine can be increased when combined with Phenobarbital.Approved
PhenterminePhentermine may decrease the sedative activities of Flunarizine.Approved, Illicit
PhenytoinThe serum concentration of Flunarizine can be decreased when it is combined with Phenytoin.Approved, Vet Approved
PitavastatinThe risk or severity of adverse effects can be increased when Flunarizine is combined with Pitavastatin.Approved
PosaconazoleThe risk or severity of adverse effects can be increased when Posaconazole is combined with Flunarizine.Approved, Investigational, Vet Approved
PravastatinThe risk or severity of adverse effects can be increased when Flunarizine is combined with Pravastatin.Approved
PrazosinPrazosin may increase the hypotensive activities of Flunarizine.Approved
PregabalinThe therapeutic efficacy of Flunarizine can be decreased when used in combination with Pregabalin.Approved, Illicit, Investigational
PrimidoneThe metabolism of Flunarizine can be increased when combined with Primidone.Approved, Vet Approved
PromazineThe metabolism of Flunarizine can be decreased when combined with Promazine.Approved, Vet Approved
PseudoephedrinePseudoephedrine may decrease the sedative activities of Flunarizine.Approved
PyrimethamineThe metabolism of Flunarizine can be decreased when combined with Pyrimethamine.Approved, Vet Approved
PyrrolnitrinThe risk or severity of adverse effects can be increased when Pyrrolnitrin is combined with Flunarizine.Experimental
QuazepamThe serum concentration of Flunarizine can be increased when it is combined with Quazepam.Approved, Illicit
QuinidineThe metabolism of Flunarizine can be decreased when combined with Quinidine.Approved
QuinineThe metabolism of Flunarizine can be decreased when combined with Quinine.Approved
RadicicolThe risk or severity of adverse effects can be increased when Radicicol is combined with Flunarizine.Experimental
RanolazineThe metabolism of Flunarizine can be decreased when combined with Ranolazine.Approved, Investigational
RifabutinThe serum concentration of Flunarizine can be decreased when it is combined with Rifabutin.Approved
RifampicinThe metabolism of Flunarizine can be increased when combined with Rifampicin.Approved
RifapentineThe metabolism of Flunarizine can be increased when combined with Rifapentine.Approved
RifaximinThe serum concentration of Flunarizine can be decreased when it is combined with Rifaximin.Approved, Investigational
RitobegronRitobegron may decrease the sedative activities of Flunarizine.Investigational
RitonavirThe metabolism of Flunarizine can be decreased when combined with Ritonavir.Approved, Investigational
RolapitantThe metabolism of Flunarizine can be decreased when combined with Rolapitant.Approved
RopiniroleThe metabolism of Flunarizine can be decreased when combined with Ropinirole.Approved, Investigational
RosuvastatinThe risk or severity of adverse effects can be increased when Flunarizine is combined with Rosuvastatin.Approved
RucaparibThe metabolism of Flunarizine can be decreased when combined with Rucaparib.Approved, Investigational
Salicylhydroxamic AcidThe risk or severity of adverse effects can be increased when Salicylhydroxamic Acid is combined with Flunarizine.Experimental
Salicylic acidThe risk or severity of adverse effects can be increased when Salicylic acid is combined with Flunarizine.Approved, Vet Approved
SecobarbitalThe metabolism of Flunarizine can be increased when combined with Secobarbital.Approved, Vet Approved
SertaconazoleThe risk or severity of adverse effects can be increased when Sertaconazole is combined with Flunarizine.Approved
SertralineThe metabolism of Flunarizine can be decreased when combined with Sertraline.Approved
SildenafilThe metabolism of Flunarizine can be decreased when combined with Sildenafil.Approved, Investigational
SilodosinSilodosin may increase the hypotensive activities of Flunarizine.Approved
SimeprevirThe metabolism of Flunarizine can be decreased when combined with Simeprevir.Approved
SimvastatinThe risk or severity of adverse effects can be increased when Flunarizine is combined with Simvastatin.Approved
SinefunginThe risk or severity of adverse effects can be increased when Sinefungin is combined with Flunarizine.Experimental
SirolimusThe risk or severity of adverse effects can be increased when Sirolimus is combined with Flunarizine.Approved, Investigational
SolithromycinThe metabolism of Flunarizine can be decreased when combined with Solithromycin.Investigational
SorafenibThe metabolism of Flunarizine can be decreased when combined with Sorafenib.Approved, Investigational
StiripentolThe metabolism of Flunarizine can be decreased when combined with Stiripentol.Approved
SulconazoleThe risk or severity of adverse effects can be increased when Sulconazole is combined with Flunarizine.Approved
SulfadiazineThe metabolism of Flunarizine can be decreased when combined with Sulfadiazine.Approved, Vet Approved
SulfamethoxazoleThe metabolism of Flunarizine can be decreased when combined with Sulfamethoxazole.Approved
SulfisoxazoleThe metabolism of Flunarizine can be decreased when combined with Sulfisoxazole.Approved, Vet Approved
TamsulosinTamsulosin may increase the hypotensive activities of Flunarizine.Approved, Investigational
TavaboroleThe risk or severity of adverse effects can be increased when Tavaborole is combined with Flunarizine.Approved
TelithromycinThe metabolism of Flunarizine can be decreased when combined with Telithromycin.Approved
Tenofovir disoproxilThe metabolism of Flunarizine can be decreased when combined with Tenofovir disoproxil.Approved, Investigational
TerazosinTerazosin may increase the hypotensive activities of Flunarizine.Approved
TerbinafineThe metabolism of Flunarizine can be decreased when combined with Terbinafine.Approved, Investigational, Vet Approved
TerconazoleThe risk or severity of adverse effects can be increased when Terconazole is combined with Flunarizine.Approved
TeriflunomideThe serum concentration of Flunarizine can be decreased when it is combined with Teriflunomide.Approved
TheophyllineThe metabolism of Flunarizine can be decreased when combined with Theophylline.Approved
ThiamylalThe metabolism of Flunarizine can be increased when combined with Thiamylal.Approved, Vet Approved
ThiopentalThe metabolism of Flunarizine can be increased when combined with Thiopental.Approved, Vet Approved
ThioridazineThe metabolism of Flunarizine can be decreased when combined with Thioridazine.Approved, Withdrawn
ThiotepaThe metabolism of Flunarizine can be decreased when combined with Thiotepa.Approved
ThymolThe risk or severity of adverse effects can be increased when Thymol is combined with Flunarizine.Approved
TicagrelorThe metabolism of Flunarizine can be decreased when combined with Ticagrelor.Approved
TiclopidineThe metabolism of Flunarizine can be decreased when combined with Ticlopidine.Approved
TioconazoleThe risk or severity of adverse effects can be increased when Tioconazole is combined with Flunarizine.Approved
TipranavirThe metabolism of Flunarizine can be decreased when combined with Tipranavir.Approved, Investigational
TolbutamideThe metabolism of Flunarizine can be decreased when combined with Tolbutamide.Approved
TolciclateThe risk or severity of adverse effects can be increased when Tolciclate is combined with Flunarizine.Experimental
TolnaftateThe risk or severity of adverse effects can be increased when Tolnaftate is combined with Flunarizine.Approved, Vet Approved
TopiroxostatThe metabolism of Flunarizine can be decreased when combined with Topiroxostat.Approved, Investigational
TranylcypromineThe metabolism of Flunarizine can be decreased when combined with Tranylcypromine.Approved
TrimazosinTrimazosin may increase the hypotensive activities of Flunarizine.Experimental
TrimethoprimThe metabolism of Flunarizine can be decreased when combined with Trimethoprim.Approved, Vet Approved
TrimetrexateThe risk or severity of adverse effects can be increased when Trimetrexate is combined with Flunarizine.Approved, Investigational
TylosinThe metabolism of Flunarizine can be decreased when combined with Tylosin.Vet Approved
UbidecarenoneThe risk or severity of adverse effects can be increased when Flunarizine is combined with Ubidecarenone.Approved, Investigational, Nutraceutical
UrapidilUrapidil may increase the hypotensive activities of Flunarizine.Investigational
Valproic AcidThe metabolism of Flunarizine can be decreased when combined with Valproic Acid.Approved, Investigational
ValsartanThe metabolism of Flunarizine can be decreased when combined with Valsartan.Approved, Investigational
VemurafenibThe serum concentration of Flunarizine can be increased when it is combined with Vemurafenib.Approved
VenlafaxineThe metabolism of Flunarizine can be decreased when combined with Venlafaxine.Approved
VoriconazoleThe risk or severity of adverse effects can be increased when Voriconazole is combined with Flunarizine.Approved, Investigational
ZafirlukastThe metabolism of Flunarizine can be decreased when combined with Zafirlukast.Approved, Investigational
ZiprasidoneThe metabolism of Flunarizine can be decreased when combined with Ziprasidone.Approved
ZucapsaicinThe metabolism of Flunarizine can be decreased when combined with Zucapsaicin.Approved
Food Interactions
  • Avoid alcohol.
  • Take without regard to meals.

References

Synthesis Reference

Matthew Peterson, Julius Remenar, Carlos Sanrame, "NOVEL FLUNARIZINE SALT FORMS AND METHODS OF MAKING AND USING THE SAME." U.S. Patent US20080200474, issued August 21, 2008.

US20080200474
General References
Not Available
External Links
Human Metabolome Database
HMDB0015589
KEGG Drug
D01303
PubChem Compound
941361
PubChem Substance
46507129
ChemSpider
819216
BindingDB
50017702
ChEBI
135652
ChEMBL
CHEMBL30008
Therapeutic Targets Database
DAP000142
PharmGKB
PA164776636
Drugs.com
Drugs.com Drug Page
Wikipedia
Flunarizine
ATC Codes
N07CA03 — Flunarizine
AHFS Codes
  • 28:32.92 — Antimigraine Agents, Miscellaneous
  • 04:04.16 — Piperazine Derivatives

Clinical Trials

Clinical Trials
PhaseStatusPurposeConditionsCount
1CompletedTreatmentHuman Volunteers / Migraines1
4CompletedTreatmentChronic Migraine1
4CompletedTreatmentSchizophrenic Disorders1
Not AvailableRecruitingTreatmentMigraines1

Pharmacoeconomics

Manufacturers
Not Available
Packagers
Not Available
Dosage forms
FormRouteStrength
CapsuleOral5 mg
Prices
Unit descriptionCostUnit
Apo-Flunarizine 5 mg Capsule0.75USD capsule
DrugBank does not sell nor buy drugs. Pricing information is supplied for informational purposes only.
Patents
Not Available

Properties

State
Solid
Experimental Properties
PropertyValueSource
melting point (°C)251.5Janssen, P.A.J.; U.S. Patent 3,773,939; November 20, 1973; assigned to Janssen Pharmaceutica N.V.
logP5.78BIOBYTE (1995)
Predicted Properties
PropertyValueSource
Water Solubility0.00168 mg/mLALOGPS
logP5.3ALOGPS
logP6.17ChemAxon
logS-5.4ALOGPS
pKa (Strongest Basic)7.6ChemAxon
Physiological Charge1ChemAxon
Hydrogen Acceptor Count2ChemAxon
Hydrogen Donor Count0ChemAxon
Polar Surface Area6.48 Å2ChemAxon
Rotatable Bond Count6ChemAxon
Refractivity120.3 m3·mol-1ChemAxon
Polarizability44.2 Å3ChemAxon
Number of Rings4ChemAxon
Bioavailability1ChemAxon
Rule of FiveNoChemAxon
Ghose FilterNoChemAxon
Veber's RuleYesChemAxon
MDDR-like RuleYesChemAxon
Predicted ADMET features
PropertyValueProbability
Human Intestinal Absorption+0.9574
Blood Brain Barrier+0.9789
Caco-2 permeable+0.5893
P-glycoprotein substrateSubstrate0.7209
P-glycoprotein inhibitor IInhibitor0.9266
P-glycoprotein inhibitor IINon-inhibitor0.6563
Renal organic cation transporterInhibitor0.7605
CYP450 2C9 substrateNon-substrate0.8855
CYP450 2D6 substrateSubstrate0.8918
CYP450 3A4 substrateNon-substrate0.7208
CYP450 1A2 substrateInhibitor0.9107
CYP450 2C9 inhibitorNon-inhibitor0.9229
CYP450 2D6 inhibitorInhibitor0.9323
CYP450 2C19 inhibitorNon-inhibitor0.9025
CYP450 3A4 inhibitorNon-inhibitor0.9034
CYP450 inhibitory promiscuityHigh CYP Inhibitory Promiscuity0.7304
Ames testNon AMES toxic0.8902
CarcinogenicityNon-carcinogens0.9422
BiodegradationNot ready biodegradable1.0
Rat acute toxicity2.3271 LD50, mol/kg Not applicable
hERG inhibition (predictor I)Strong inhibitor0.5261
hERG inhibition (predictor II)Inhibitor0.7549
ADMET data is predicted using admetSAR, a free tool for evaluating chemical ADMET properties. (23092397)

Spectra

Mass Spec (NIST)
Not Available
Spectra
SpectrumSpectrum TypeSplash Key
Predicted GC-MS Spectrum - GC-MSPredicted GC-MSNot Available
Predicted MS/MS Spectrum - 10V, Positive (Annotated)Predicted LC-MS/MSNot Available
Predicted MS/MS Spectrum - 20V, Positive (Annotated)Predicted LC-MS/MSNot Available
Predicted MS/MS Spectrum - 40V, Positive (Annotated)Predicted LC-MS/MSNot Available
Predicted MS/MS Spectrum - 10V, Negative (Annotated)Predicted LC-MS/MSNot Available
Predicted MS/MS Spectrum - 20V, Negative (Annotated)Predicted LC-MS/MSNot Available
Predicted MS/MS Spectrum - 40V, Negative (Annotated)Predicted LC-MS/MSNot Available
LC-MS/MS Spectrum - LC-ESI-ITFT , positiveLC-MS/MSsplash10-0udi-0090100000-cef5de63fdba54327f14

Taxonomy

Description
This compound belongs to the class of organic compounds known as diphenylmethanes. These are compounds containing a diphenylmethane moiety, which consists of a methane wherein two hydrogen atoms are replaced by two phenyl groups.
Kingdom
Organic compounds
Super Class
Benzenoids
Class
Benzene and substituted derivatives
Sub Class
Diphenylmethanes
Direct Parent
Diphenylmethanes
Alternative Parents
Styrenes / N-alkylpiperazines / Fluorobenzenes / Aralkylamines / Aryl fluorides / Trialkylamines / Azacyclic compounds / Organopnictogen compounds / Organofluorides / Hydrocarbon derivatives
Substituents
Diphenylmethane / Styrene / Fluorobenzene / Halobenzene / Aralkylamine / N-alkylpiperazine / Aryl fluoride / Aryl halide / 1,4-diazinane / Piperazine
Molecular Framework
Aromatic heteromonocyclic compounds
External Descriptors
Not 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, hor...
Gene Name
CACNA1G
Uniprot ID
O43497
Uniprot Name
Voltage-dependent T-type calcium channel subunit alpha-1G
Molecular Weight
262468.62 Da
References
  1. Overington JP, Al-Lazikani B, Hopkins AL: How many drug targets are there? Nat Rev Drug Discov. 2006 Dec;5(12):993-6. [PubMed:17139284]
  2. Imming P, Sinning C, Meyer A: Drugs, their targets and the nature and number of drug targets. Nat Rev Drug Discov. 2006 Oct;5(10):821-34. [PubMed:17016423]
  3. Uebele VN, Nuss CE, Fox SV, Garson SL, Cristescu R, Doran SM, Kraus RL, Santarelli VP, Li Y, Barrow JC, Yang ZQ, Schlegel KA, Rittle KE, Reger TS, Bednar RA, Lemaire W, Mullen FA, Ballard JE, Tang C, Dai G, McManus OB, Koblan KS, Renger JJ: Positive allosteric interaction of structurally diverse T-type calcium channel antagonists. Cell Biochem Biophys. 2009;55(2):81-93. doi: 10.1007/s12013-009-9057-4. Epub 2009 Jul 7. [PubMed:19582593]
  4. Santi CM, Cayabyab FS, Sutton KG, McRory JE, Mezeyova J, Hamming KS, Parker D, Stea A, Snutch TP: Differential inhibition of T-type calcium channels by neuroleptics. J Neurosci. 2002 Jan 15;22(2):396-403. [PubMed:11784784]
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, hor...
Gene Name
CACNA1H
Uniprot ID
O95180
Uniprot Name
Voltage-dependent T-type calcium channel subunit alpha-1H
Molecular Weight
259160.2 Da
References
  1. Overington JP, Al-Lazikani B, Hopkins AL: How many drug targets are there? Nat Rev Drug Discov. 2006 Dec;5(12):993-6. [PubMed:17139284]
  2. Imming P, Sinning C, Meyer A: Drugs, their targets and the nature and number of drug targets. Nat Rev Drug Discov. 2006 Oct;5(10):821-34. [PubMed:17016423]
  3. Chen X, Ji ZL, Chen YZ: TTD: Therapeutic Target Database. Nucleic Acids Res. 2002 Jan 1;30(1):412-5. [PubMed:11752352]
  4. Uebele VN, Nuss CE, Fox SV, Garson SL, Cristescu R, Doran SM, Kraus RL, Santarelli VP, Li Y, Barrow JC, Yang ZQ, Schlegel KA, Rittle KE, Reger TS, Bednar RA, Lemaire W, Mullen FA, Ballard JE, Tang C, Dai G, McManus OB, Koblan KS, Renger JJ: Positive allosteric interaction of structurally diverse T-type calcium channel antagonists. Cell Biochem Biophys. 2009;55(2):81-93. doi: 10.1007/s12013-009-9057-4. Epub 2009 Jul 7. [PubMed:19582593]
  5. Santi CM, Cayabyab FS, Sutton KG, McRory JE, Mezeyova J, Hamming KS, Parker D, Stea A, Snutch TP: Differential inhibition of T-type calcium channels by neuroleptics. J Neurosci. 2002 Jan 15;22(2):396-403. [PubMed:11784784]
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, hor...
Gene Name
CACNA1I
Uniprot ID
Q9P0X4
Uniprot Name
Voltage-dependent T-type calcium channel subunit alpha-1I
Molecular Weight
245100.8 Da
References
  1. Overington JP, Al-Lazikani B, Hopkins AL: How many drug targets are there? Nat Rev Drug Discov. 2006 Dec;5(12):993-6. [PubMed:17139284]
  2. Imming P, Sinning C, Meyer A: Drugs, their targets and the nature and number of drug targets. Nat Rev Drug Discov. 2006 Oct;5(10):821-34. [PubMed:17016423]
  3. Uebele VN, Nuss CE, Fox SV, Garson SL, Cristescu R, Doran SM, Kraus RL, Santarelli VP, Li Y, Barrow JC, Yang ZQ, Schlegel KA, Rittle KE, Reger TS, Bednar RA, Lemaire W, Mullen FA, Ballard JE, Tang C, Dai G, McManus OB, Koblan KS, Renger JJ: Positive allosteric interaction of structurally diverse T-type calcium channel antagonists. Cell Biochem Biophys. 2009;55(2):81-93. doi: 10.1007/s12013-009-9057-4. Epub 2009 Jul 7. [PubMed:19582593]
  4. Santi CM, Cayabyab FS, Sutton KG, McRory JE, Mezeyova J, Hamming KS, Parker D, Stea A, Snutch TP: Differential inhibition of T-type calcium channels by neuroleptics. J Neurosci. 2002 Jan 15;22(2):396-403. [PubMed:11784784]
Kind
Protein
Organism
Human
Pharmacological action
Unknown
Actions
Antagonist
General Function
Histamine receptor activity
Specific Function
In peripheral tissues, the H1 subclass of histamine receptors mediates the contraction of smooth muscles, increase in capillary permeability due to contraction of terminal venules, and catecholamin...
Gene Name
HRH1
Uniprot ID
P35367
Uniprot Name
Histamine H1 receptor
Molecular Weight
55783.61 Da
References
  1. Overington JP, Al-Lazikani B, Hopkins AL: How many drug targets are there? Nat Rev Drug Discov. 2006 Dec;5(12):993-6. [PubMed:17139284]
  2. Imming P, Sinning C, Meyer A: Drugs, their targets and the nature and number of drug targets. Nat Rev Drug Discov. 2006 Oct;5(10):821-34. [PubMed:17016423]
  3. Taylor JE, Defeudis FV: Interactions of verapamil, D 600, flunarizine and nifedipine with cerebral histamine-receptors. Neurochem Int. 1986;9(3):379-81. [PubMed:20493137]
Kind
Protein
Organism
Human
Pharmacological action
Unknown
General Function
Titin binding
Specific Function
Calmodulin mediates the control of a large number of enzymes, ion channels, aquaporins and other proteins by Ca(2+). Among the enzymes to be stimulated by the calmodulin-Ca(2+) complex are a number...
Gene Name
CALM1
Uniprot ID
P0DP23
Uniprot Name
Calmodulin
Molecular Weight
16837.47 Da
References
  1. Overington JP, Al-Lazikani B, Hopkins AL: How many drug targets are there? Nat Rev Drug Discov. 2006 Dec;5(12):993-6. [PubMed:17139284]
  2. Imming P, Sinning C, Meyer A: Drugs, their targets and the nature and number of drug targets. Nat Rev Drug Discov. 2006 Oct;5(10):821-34. [PubMed:17016423]

Enzymes

Kind
Protein
Organism
Human
Pharmacological action
Unknown
Actions
Substrate
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...
Gene Name
CYP2D6
Uniprot ID
P10635
Uniprot Name
Cytochrome P450 2D6
Molecular Weight
55768.94 Da
References
  1. Zhou SF, Zhou ZW, Yang LP, Cai JP: Substrates, inducers, inhibitors and structure-activity relationships of human Cytochrome P450 2C9 and implications in drug development. Curr Med Chem. 2009;16(27):3480-675. Epub 2009 Sep 1. [PubMed:19515014]
  2. Preissner S, Kroll K, Dunkel M, Senger C, Goldsobel G, Kuzman D, Guenther S, Winnenburg R, Schroeder M, Preissner R: SuperCYP: a comprehensive database on Cytochrome P450 enzymes including a tool for analysis of CYP-drug interactions. Nucleic Acids Res. 2010 Jan;38(Database issue):D237-43. doi: 10.1093/nar/gkp970. Epub 2009 Nov 24. [PubMed:19934256]
Kind
Protein
Organism
Human
Pharmacological action
Unknown
Actions
Substrate
General Function
Steroid hydroxylase activity
Specific Function
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 un...
Gene Name
CYP2B6
Uniprot ID
P20813
Uniprot Name
Cytochrome P450 2B6
Molecular Weight
56277.81 Da
References
  1. Zhou SF, Zhou ZW, Yang LP, Cai JP: Substrates, inducers, inhibitors and structure-activity relationships of human Cytochrome P450 2C9 and implications in drug development. Curr Med Chem. 2009;16(27):3480-675. Epub 2009 Sep 1. [PubMed:19515014]
Kind
Protein
Organism
Human
Pharmacological action
Unknown
Actions
Substrate
General Function
Steroid hydroxylase activity
Specific Function
Cytochromes P450 are a group of heme-thiolate monooxygenases. In liver microsomes, this enzyme is involved in an NADPH-dependent electron transport pathway. It oxidizes a variety of structurally un...
Gene Name
CYP2C9
Uniprot ID
P11712
Uniprot Name
Cytochrome P450 2C9
Molecular Weight
55627.365 Da
References
  1. Zhou SF, Zhou ZW, Yang LP, Cai JP: Substrates, inducers, inhibitors and structure-activity relationships of human Cytochrome P450 2C9 and implications in drug development. Curr Med Chem. 2009;16(27):3480-675. Epub 2009 Sep 1. [PubMed:19515014]
  2. 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
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 un...
Gene Name
CYP1A1
Uniprot ID
P04798
Uniprot Name
Cytochrome P450 1A1
Molecular Weight
58164.815 Da
References
  1. Zhou SF, Zhou ZW, Yang LP, Cai JP: Substrates, inducers, inhibitors and structure-activity relationships of human Cytochrome P450 2C9 and implications in drug development. Curr Med Chem. 2009;16(27):3480-675. Epub 2009 Sep 1. [PubMed:19515014]
  2. 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
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 un...
Gene Name
CYP1A2
Uniprot ID
P05177
Uniprot Name
Cytochrome P450 1A2
Molecular Weight
58293.76 Da
References
  1. Zhou SF, Zhou ZW, Yang LP, Cai JP: Substrates, inducers, inhibitors and structure-activity relationships of human Cytochrome P450 2C9 and implications in drug development. Curr Med Chem. 2009;16(27):3480-675. Epub 2009 Sep 1. [PubMed:19515014]
  2. Preissner S, Kroll K, Dunkel M, Senger C, Goldsobel G, Kuzman D, Guenther S, Winnenburg R, Schroeder M, Preissner R: SuperCYP: a comprehensive database on Cytochrome P450 enzymes including a tool for analysis of CYP-drug interactions. Nucleic Acids Res. 2010 Jan;38(Database issue):D237-43. doi: 10.1093/nar/gkp970. Epub 2009 Nov 24. [PubMed:19934256]
Kind
Protein
Organism
Human
Pharmacological action
Unknown
Actions
Substrate
General Function
Steroid hydroxylase activity
Specific Function
Exhibits a high coumarin 7-hydroxylase activity. Can act in the hydroxylation of the anti-cancer drugs cyclophosphamide and ifosphamide. Competent in the metabolic activation of aflatoxin B1. Const...
Gene Name
CYP2A6
Uniprot ID
P11509
Uniprot Name
Cytochrome P450 2A6
Molecular Weight
56501.005 Da
References
  1. Zhou SF, Zhou ZW, Yang LP, Cai JP: Substrates, inducers, inhibitors and structure-activity relationships of human Cytochrome P450 2C9 and implications in drug development. Curr Med Chem. 2009;16(27):3480-675. Epub 2009 Sep 1. [PubMed:19515014]
  2. 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]

Drug created on September 27, 2007 07:47 / Updated on January 19, 2018 10:57