Identification

Name
Ergotamine
Accession Number
DB00696  (APRD00677)
Type
Small Molecule
Groups
Approved
Description

A vasoconstrictor found in ergot of Central Europe. It is an alpha-1 selective adrenergic agonist and is commonly used in the treatment of migraine disorders. [PubChem]

Structure
Thumb
Synonyms
  • (5'alpha)-12'-hydroxy-2'-methyl-5'-(phenylmethyl)ergotoman-3',6',18-trione
  • 12'-Hydroxy-2'-methyl-5'alpha-(phenylmethyl)ergotaman-3',6',18-trione
  • Ergotamin
  • Ergotamina
  • Ergotamine
  • Ergotaminum
  • Gynergen
Product Ingredients
IngredientUNIICASInChI Key
Ergotamine TartrateMRU5XH3B48379-79-3CJMJLDQKTOJACI-BGQAIRJTSA-N
Product Images
Prescription Products
NameDosageStrengthRouteLabellerMarketing StartMarketing End
Ergomar Slt 2mgTablet2 mgSublingualAventis Pharma Ltd.1975-12-312003-07-22Canada
Generic Prescription Products
NameDosageStrengthRouteLabellerMarketing StartMarketing End
ErgomarTablet, orally disintegrating2 mg/1SublingualRosedale Therapeutics2012-08-31Not applicableUs
Ergomar SublingualTablet2 mg/1OralTer Sera Therapeutics, Llc2016-09-20Not applicableUs
International/Other Brands
Anervan (Recip) / Antimigraine (Ta Fong) / Enxak (Cazi) / Ergam (Gedeon Richter) / Ergo-Kranit (Krewel Meuselbach) / Gynaemine (Sriprasit Dispensary) / Wigrettes
Mixture Products
NameIngredientsDosageRouteLabellerMarketing StartMarketing End
Bellergal SpacetabsErgotamine Tartrate (0.6 mg) + Belladonna (0.2 mg) + Phenobarbital (40.0 mg)Tablet, extended releaseOralPaladin Labs Inc1959-01-01Not applicableCanada
Bellergal TabErgotamine (.3 mg) + Belladonna (.1 mg) + Phenobarbital (20 mg)TabletOralSandoz1951-12-311997-08-12Canada
CafergotErgotamine Tartrate (1 mg/1) + Caffeine (100 mg/1)TabletOralKaiser Foundations Hospitals2011-04-21Not applicableUs00781 5405 01 nlmimage10 4a132549
CafergotErgotamine Tartrate (1 mg/1) + Caffeine (100 mg/1)Tablet, film coatedOralSandoz1982-01-01Not applicableUs
Cafergot Pb SupErgotamine (2 mg) + Belladonna (0.25 mg) + Caffeine (100 mg) + Pentobarbital (60 mg)SuppositoryRectalNovartis1958-12-312003-01-15Canada
Cafergot Pb TabErgotamine (1 mg) + Belladonna (0.125 mg) + Caffeine (100 mg) + Pentobarbital Sodium (30 mg)TabletOralNovartis1951-12-311999-08-04Canada
Cafergot SupErgotamine Tartrate (2 mg) + Caffeine (100 mg)SuppositoryRectalNovartis1990-12-312006-11-13Canada
Cafergot TabErgotamine Tartrate (1 mg) + Caffeine (100 mg)TabletOralNovartis1951-12-312014-03-31Canada
Ergodryl CapErgotamine Tartrate (1 mg) + Caffeine citrate (100 mg) + Diphenhydramine hydrochloride (25 mg)CapsuleOralErfa Canada 2012 Inc1964-12-312013-07-09Canada
ErgotamineErgotamine Tartrate (1 mg/1) + Caffeine (100 mg/1)Tablet, film coatedOralWest Ward Pharmaceutical2004-09-17Not applicableUs
Categories
UNII
PR834Q503T
CAS number
113-15-5
Weight
Average: 581.6615
Monoisotopic: 581.263819255
Chemical Formula
C33H35N5O5
InChI Key
XCGSFFUVFURLIX-VFGNJEKYSA-N
InChI
InChI=1S/C33H35N5O5/c1-32(35-29(39)21-15-23-22-10-6-11-24-28(22)20(17-34-24)16-25(23)36(2)18-21)31(41)38-26(14-19-8-4-3-5-9-19)30(40)37-13-7-12-27(37)33(38,42)43-32/h3-6,8-11,15,17,21,25-27,34,42H,7,12-14,16,18H2,1-2H3,(H,35,39)/t21-,25-,26+,27+,32-,33+/m1/s1
IUPAC Name
(4R,7R)-N-[(1S,2S,4R,7S)-7-benzyl-2-hydroxy-4-methyl-5,8-dioxo-3-oxa-6,9-diazatricyclo[7.3.0.0²,⁶]dodecan-4-yl]-6-methyl-6,11-diazatetracyclo[7.6.1.0²,⁷.0¹²,¹⁶]hexadeca-1(16),2,9,12,14-pentaene-4-carboxamide
SMILES
[H][[email protected]@]12CCCN1C(=O)[[email protected]](CC1=CC=CC=C1)N1C(=O)[[email protected]](C)(NC(=O)[[email protected]]3CN(C)[[email protected]]4([H])CC5=CNC6=CC=CC(=C56)C4=C3)O[[email protected]@]21O

Pharmacology

Indication

For use as therapy to abort or prevent vascular headache, e.g., migraine, migraine variants, or so called "histaminic cephalalgia".

Structured Indications
Pharmacodynamics

Ergotamine is a vasoconstrictor and alpha adrenoreceptor antagonist. The pharmacological properties of ergotamine are extremely complex; some of its actions are unrelated to each other, and even mutually antagonistic. The drug has partial agonist and/or antagonist activity against tryptaminergic, dopaminergic and alpha adrenergic receptors depending upon their site, and it is a highly active uterine stimulant. It causes constriction of peripheral and cranial blood vessels and produces depression of central vasomotor centers. The pain of a migraine attack is believed to be due to greatly increased amplitude of pulsations in the cranial arteries, especially the meningeal branches of the external carotid artery. Ergotamine reduces extracranial blood flow, causes a decline in the amplitude of pulsation in the cranial arteries, and decreases hyperperfusion of the territory of the basilar artery. It does not reduce cerebral hemispheric blood flow.

Mechanism of action

Ergotamine acts on migraine by one of two proposed mechanisms: 1) activation of 5-HT1D receptors located on intracranial blood vessels, including those on arterio-venous anastomoses, leads to vasoconstriction, which correlates with the relief of migraine headache, and 2) activation of 5-HT1D receptors on sensory nerve endings of the trigeminal system results in the inhibition of pro-inflammatory neuropeptide release.

TargetActionsOrganism
A5-hydroxytryptamine receptor 1D
agonist
Human
A5-hydroxytryptamine receptor 1B
agonist
Human
A5-hydroxytryptamine receptor 2A
agonist
Human
UD(2) dopamine receptor
agonist
Human
AAlpha-1A adrenergic receptor
partial agonist
Human
AAlpha-1B adrenergic receptor
partial agonist
Human
AAlpha-1D adrenergic receptor
partial agonist
Human
UAlpha-2A adrenergic receptor
partial agonist
Human
UAlpha-2B adrenergic receptor
agonist
partial agonist
Human
USodium-dependent noradrenaline transporter
inhibitor
Human
UD(1) dopamine receptor
agonist
Human
U5-hydroxytryptamine receptor 1A
agonist
Human
U5-hydroxytryptamine receptor 1F
agonist
Human
U5-hydroxytryptamine receptor 2C
agonist
Human
U5-hydroxytryptamine receptor 2BNot AvailableHuman
Absorption

The bioavailability of sublingually administered ergotamine has not been determined.

Volume of distribution
Not Available
Protein binding
Not Available
Metabolism

Hepatic. Ergotamine is metabolized by the liver by largely undefined pathways, and 90% of the metabolites are excreted in the bile.

Route of elimination
Not Available
Half life

2 hours

Clearance
Not Available
Toxicity

Signs of overexposure include irritation, nausea, vomiting, headache, diarrhea, thirst, coldness of skin, pruritus, weak pulse, numbness, tingling of extremities, and confusion.

Affected organisms
  • Humans and other mammals
Pathways
Not Available
Pharmacogenomic Effects/ADRs
Not Available

Interactions

Drug Interactions
DrugInteractionDrug group
7,8-Dichloro-1,2,3,4-tetrahydroisoquinoline7,8-Dichloro-1,2,3,4-tetrahydroisoquinoline may increase the hypertensive activities of Ergotamine.Experimental
AbirateroneThe serum concentration of Ergotamine can be increased when it is combined with Abiraterone.Approved
AcebutololErgotamine may increase the atrioventricular blocking (AV block) activities of Acebutolol.Approved
AcetaminophenThe risk or severity of adverse effects can be increased when Ergotamine is combined with Acetaminophen.Approved
AcetazolamideThe risk or severity of adverse effects can be increased when Ergotamine is combined with Acetazolamide.Approved, Vet Approved
AfatinibThe serum concentration of Afatinib can be increased when it is combined with Ergotamine.Approved
AldesleukinThe risk or severity of adverse effects can be increased when Ergotamine is combined with Aldesleukin.Approved
AlfuzosinAlfuzosin may decrease the vasoconstricting activities of Ergotamine.Approved, Investigational
AlprazolamThe risk or severity of adverse effects can be increased when Ergotamine is combined with Alprazolam.Approved, Illicit, Investigational
AlprenololErgotamine may increase the atrioventricular blocking (AV block) activities of Alprenolol.Approved, Withdrawn
AmbroxolThe risk or severity of adverse effects can be increased when Ergotamine is combined with Ambroxol.Approved, Investigational
AmineptineAmineptine may decrease the antihypertensive activities of Ergotamine.Illicit, Withdrawn
AmiodaroneThe metabolism of Ergotamine can be decreased when combined with Amiodarone.Approved, Investigational
AmitriptylineAmitriptyline may decrease the antihypertensive activities of Ergotamine.Approved
AmlodipineThe risk or severity of adverse effects can be increased when Ergotamine is combined with Amlodipine.Approved
AmoxapineAmoxapine may increase the vasopressor activities of Ergotamine.Approved
AmphetamineAmphetamine may increase the hypertensive activities of Ergotamine.Approved, Illicit
AmprenavirThe risk or severity of adverse effects can be increased when Ergotamine is combined with Amprenavir.Approved
AnastrozoleThe risk or severity of adverse effects can be increased when Ergotamine is combined with Anastrozole.Approved, Investigational
AntipyrineThe risk or severity of adverse effects can be increased when Ergotamine is combined with Antipyrine.Approved
AprepitantThe serum concentration of Ergotamine can be increased when it is combined with Aprepitant.Approved, Investigational
ArotinololErgotamine may increase the atrioventricular blocking (AV block) activities of Arotinolol.Investigational
Arsenic trioxideThe risk or severity of adverse effects can be increased when Ergotamine is combined with Arsenic trioxide.Approved, Investigational
AstemizoleThe risk or severity of adverse effects can be increased when Ergotamine is combined with Astemizole.Approved, Withdrawn
AtazanavirThe metabolism of Ergotamine can be decreased when combined with Atazanavir.Approved, Investigational
AtenololErgotamine may increase the atrioventricular blocking (AV block) activities of Atenolol.Approved
AtomoxetineThe metabolism of Ergotamine can be decreased when combined with Atomoxetine.Approved
AtorvastatinThe risk or severity of adverse effects can be increased when Ergotamine is combined with Atorvastatin.Approved
AzelastineThe risk or severity of adverse effects can be increased when Ergotamine is combined with Azelastine.Approved
AzithromycinThe metabolism of Ergotamine can be decreased when combined with Azithromycin.Approved
BefunololErgotamine may increase the atrioventricular blocking (AV block) activities of Befunolol.Experimental
Benzylpenicilloyl PolylysineErgotamine may decrease effectiveness of Benzylpenicilloyl Polylysine as a diagnostic agent.Approved
BetamethasoneThe risk or severity of adverse effects can be increased when Ergotamine is combined with Betamethasone.Approved, Vet Approved
BetaxololErgotamine may increase the atrioventricular blocking (AV block) activities of Betaxolol.Approved
BevantololErgotamine may increase the atrioventricular blocking (AV block) activities of Bevantolol.Approved
BicalutamideThe risk or severity of adverse effects can be increased when Ergotamine is combined with Bicalutamide.Approved
BifonazoleThe risk or severity of adverse effects can be increased when Ergotamine is combined with Bifonazole.Approved, Investigational
BisoprololErgotamine may increase the atrioventricular blocking (AV block) activities of Bisoprolol.Approved
BoceprevirThe serum concentration of Ergotamine can be increased when it is combined with Boceprevir.Approved, Withdrawn
BopindololErgotamine may increase the atrioventricular blocking (AV block) activities of Bopindolol.Approved
BortezomibThe metabolism of Ergotamine can be decreased when combined with Bortezomib.Approved, Investigational
BosentanThe serum concentration of Ergotamine can be decreased when it is combined with Bosentan.Approved, Investigational
BosutinibThe serum concentration of Bosutinib can be increased when it is combined with Ergotamine.Approved
Brentuximab vedotinThe serum concentration of Brentuximab vedotin can be increased when it is combined with Ergotamine.Approved
BrofaromineBrofaromine may increase the hypertensive activities of Ergotamine.Experimental
BromocriptineThe risk or severity of adverse effects can be increased when Ergotamine is combined with Bromocriptine.Approved, Investigational
BucindololErgotamine may increase the atrioventricular blocking (AV block) activities of Bucindolol.Investigational
BufuralolErgotamine may increase the atrioventricular blocking (AV block) activities of Bufuralol.Experimental, Investigational
BunazosinBunazosin may decrease the vasoconstricting activities of Ergotamine.Investigational
BupranololErgotamine may increase the atrioventricular blocking (AV block) activities of Bupranolol.Approved
BuprenorphineThe risk or severity of adverse effects can be increased when Ergotamine is combined with Buprenorphine.Approved, Illicit, Investigational, Vet Approved
CabergolineThe risk or severity of adverse effects can be increased when Ergotamine is combined with Cabergoline.Approved
CaffeineThe metabolism of Ergotamine can be decreased when combined with Caffeine.Approved
CapsaicinThe risk or severity of adverse effects can be increased when Ergotamine is combined with Capsaicin.Approved
CarbamazepineThe metabolism of Ergotamine can be increased when combined with Carbamazepine.Approved, Investigational
Carboprost TromethamineThe risk or severity of adverse effects can be increased when Carboprost Tromethamine is combined with Ergotamine.Approved
CarteololErgotamine may increase the atrioventricular blocking (AV block) activities of Carteolol.Approved
CarvedilolErgotamine may increase the atrioventricular blocking (AV block) activities of Carvedilol.Approved, Investigational
CaspofunginThe risk or severity of adverse effects can be increased when Ergotamine is combined with Caspofungin.Approved
CeliprololErgotamine may increase the atrioventricular blocking (AV block) activities of Celiprolol.Approved, Investigational
CeritinibThe serum concentration of Ergotamine can be increased when it is combined with Ceritinib.Approved
CerivastatinThe serum concentration of Cerivastatin can be increased when it is combined with Ergotamine.Withdrawn
ChloramphenicolThe risk or severity of adverse effects can be increased when Ergotamine is combined with Chloramphenicol.Approved, Vet Approved
ChlorzoxazoneThe risk or severity of adverse effects can be increased when Ergotamine is combined with Chlorzoxazone.Approved
CilostazolThe risk or severity of adverse effects can be increased when Ergotamine is combined with Cilostazol.Approved
CiprofloxacinThe risk or severity of adverse effects can be increased when Ergotamine is combined with Ciprofloxacin.Approved, Investigational
CirazolineErgotamine may increase the hypertensive activities of Cirazoline.Experimental
CisaprideThe risk or severity of adverse effects can be increased when Ergotamine is combined with Cisapride.Approved, Investigational, Withdrawn
CitalopramThe metabolism of Ergotamine can be decreased when combined with Citalopram.Approved
ClarithromycinThe serum concentration of Ergotamine can be increased when it is combined with Clarithromycin.Approved
ClemastineThe metabolism of Ergotamine can be decreased when combined with Clemastine.Approved
ClindamycinThe risk or severity of adverse effects can be increased when Ergotamine is combined with Clindamycin.Approved, Vet Approved
ClofazimineThe risk or severity of adverse effects can be increased when Ergotamine is combined with Clofazimine.Approved, Investigational
ClomifeneThe risk or severity of adverse effects can be increased when Ergotamine is combined with Clomifene.Approved, Investigational
ClomipramineClomipramine may decrease the antihypertensive activities of Ergotamine.Approved, Vet Approved
CloranololErgotamine may increase the atrioventricular blocking (AV block) activities of Cloranolol.Experimental
ClotiazepamThe risk or severity of adverse effects can be increased when Ergotamine is combined with Clotiazepam.Approved, Illicit
ClotrimazoleThe metabolism of Ergotamine can be decreased when combined with Clotrimazole.Approved, Vet Approved
ClozapineThe risk or severity of adverse effects can be increased when Ergotamine is combined with Clozapine.Approved
CobicistatThe serum concentration of Ergotamine can be increased when it is combined with Cobicistat.Approved
CocaineThe risk or severity of adverse effects can be increased when Ergotamine is combined with Cocaine.Approved, Illicit
ColchicineThe serum concentration of Colchicine can be increased when it is combined with Ergotamine.Approved
ConivaptanThe serum concentration of Conivaptan can be increased when it is combined with Ergotamine.Approved, Investigational
Cortisone acetateThe risk or severity of adverse effects can be increased when Ergotamine is combined with Cortisone acetate.Approved
CrizotinibThe serum concentration of Ergotamine can be increased when it is combined with Crizotinib.Approved
CyclobenzaprineCyclobenzaprine may decrease the antihypertensive activities of Ergotamine.Approved
CyclophosphamideThe risk or severity of adverse effects can be increased when Ergotamine is combined with Cyclophosphamide.Approved, Investigational
CyclosporineThe metabolism of Ergotamine can be decreased when combined with Cyclosporine.Approved, Investigational, Vet Approved
Cyproterone acetateThe serum concentration of Ergotamine can be decreased when it is combined with Cyproterone acetate.Approved, Investigational
Dabigatran etexilateThe serum concentration of the active metabolites of Dabigatran etexilate can be increased when Dabigatran etexilate is used in combination with Ergotamine.Approved
DabrafenibThe serum concentration of Ergotamine can be decreased when it is combined with Dabrafenib.Approved
DalfopristinThe risk or severity of adverse effects can be increased when Ergotamine is combined with Dalfopristin.Approved
DanazolThe risk or severity of adverse effects can be increased when Ergotamine is combined with Danazol.Approved
DarunavirThe metabolism of Ergotamine can be decreased when combined with Darunavir.Approved
DasatinibThe serum concentration of Ergotamine can be increased when it is combined with Dasatinib.Approved, Investigational
DaunorubicinThe risk or severity of adverse effects can be increased when Ergotamine is combined with Daunorubicin.Approved
DeferasiroxThe serum concentration of Ergotamine can be decreased when it is combined with Deferasirox.Approved, Investigational
DelavirdineThe metabolism of Ergotamine can be decreased when combined with Delavirdine.Approved
DesipramineDesipramine may decrease the antihypertensive activities of Ergotamine.Approved
DexamethasoneThe risk or severity of adverse effects can be increased when Ergotamine is combined with Dexamethasone.Approved, Investigational, Vet Approved
DextropropoxypheneThe risk or severity of adverse effects can be increased when Ergotamine is combined with Dextropropoxyphene.Approved, Illicit, Investigational, Withdrawn
DiazepamThe risk or severity of adverse effects can be increased when Ergotamine is combined with Diazepam.Approved, Illicit, Vet Approved
DibenzepinDibenzepin may decrease the antihypertensive activities of Ergotamine.Experimental
DiethylstilbestrolThe risk or severity of adverse effects can be increased when Ergotamine is combined with Diethylstilbestrol.Approved, Investigational
DihydroergocornineThe risk or severity of adverse effects can be increased when Dihydroergocornine is combined with Ergotamine.Approved
DihydroergocristineThe risk or severity of adverse effects can be increased when Dihydroergocristine is combined with Ergotamine.Approved, Experimental
DihydroergocryptineThe risk or severity of adverse effects can be increased when Dihydroergocryptine is combined with Ergotamine.Experimental
DihydroergotamineThe metabolism of Ergotamine can be decreased when combined with Dihydroergotamine.Approved
DiltiazemThe metabolism of Ergotamine can be decreased when combined with Diltiazem.Approved
Dimethyl sulfoxideThe risk or severity of adverse effects can be increased when Ergotamine is combined with Dimethyl sulfoxide.Approved, Vet Approved
DocetaxelThe risk or severity of adverse effects can be increased when Ergotamine is combined with Docetaxel.Approved, Investigational
DosulepinDosulepin may decrease the antihypertensive activities of Ergotamine.Approved
DoxazosinDoxazosin may decrease the vasoconstricting activities of Ergotamine.Approved
DoxepinDoxepin may decrease the antihypertensive activities of Ergotamine.Approved
DoxorubicinThe serum concentration of Doxorubicin can be increased when it is combined with Ergotamine.Approved, Investigational
DoxorubicinThe risk or severity of adverse effects can be increased when Ergotamine is combined with Doxorubicin.Approved, Investigational
DoxycyclineThe metabolism of Ergotamine can be decreased when combined with Doxycycline.Approved, Investigational, Vet Approved
DronedaroneThe metabolism of Ergotamine can be decreased when combined with Dronedarone.Approved
DroxidopaErgotamine may increase the hypertensive activities of Droxidopa.Approved, Investigational
EconazoleThe risk or severity of adverse effects can be increased when Ergotamine is combined with Econazole.Approved
EdoxabanThe serum concentration of Edoxaban can be increased when it is combined with Ergotamine.Approved
EfavirenzThe risk or severity of adverse effects can be increased when Ergotamine is combined with Efavirenz.Approved, Investigational
ElbasvirThe risk or severity of adverse effects can be increased when Ergotamine is combined with Elbasvir.Approved
EnasidenibThe risk or severity of adverse effects can be increased when Ergotamine is combined with Enasidenib.Approved
EnzalutamideThe serum concentration of Ergotamine can be decreased when it is combined with Enzalutamide.Approved
EpanololErgotamine may increase the atrioventricular blocking (AV block) activities of Epanolol.Experimental
EpinephrineThe risk or severity of adverse effects can be increased when Ergotamine is combined with Epinephrine.Approved, Vet Approved
Ergoloid mesylateThe risk or severity of adverse effects can be increased when Ergotamine is combined with Ergoloid mesylate.Approved
ErgonovineThe risk or severity of adverse effects can be increased when Ergotamine is combined with Ergonovine.Approved
ErythromycinThe metabolism of Ergotamine can be decreased when combined with Erythromycin.Approved, Vet Approved
EsmirtazapineEsmirtazapine may decrease the antihypertensive activities of Ergotamine.Investigational
EsmololErgotamine may increase the atrioventricular blocking (AV block) activities of Esmolol.Approved
EthanolThe risk or severity of adverse effects can be increased when Ergotamine is combined with Ethanol.Approved
EtoposideThe risk or severity of adverse effects can be increased when Ergotamine is combined with Etoposide.Approved
EtoricoxibThe risk or severity of adverse effects can be increased when Ergotamine is combined with Etoricoxib.Approved, Investigational
EverolimusThe serum concentration of Everolimus can be increased when it is combined with Ergotamine.Approved
EzetimibeThe risk or severity of adverse effects can be increased when Ergotamine is combined with Ezetimibe.Approved
FelodipineThe risk or severity of adverse effects can be increased when Ergotamine is combined with Felodipine.Approved, Investigational
FentanylThe serum concentration of Fentanyl can be decreased when it is combined with Ergotamine.Approved, Illicit, Investigational, Vet Approved
FluconazoleThe metabolism of Ergotamine can be decreased when combined with Fluconazole.Approved
FluoxetineThe risk or severity of adverse effects can be increased when Ergotamine is combined with Fluoxetine.Approved, Vet Approved
Fluticasone propionateThe risk or severity of adverse effects can be increased when Ergotamine is combined with Fluticasone propionate.Approved
FluvastatinThe serum concentration of Fluvastatin can be increased when it is combined with Ergotamine.Approved
FluvoxamineThe metabolism of Ergotamine can be decreased when combined with Fluvoxamine.Approved, Investigational
FosamprenavirThe metabolism of Ergotamine can be decreased when combined with Fosamprenavir.Approved
FosaprepitantThe serum concentration of Ergotamine can be increased when it is combined with Fosaprepitant.Approved
FosphenytoinThe metabolism of Ergotamine can be increased when combined with Fosphenytoin.Approved
FurazolidoneFurazolidone may increase the hypertensive activities of Ergotamine.Approved, Investigational, Vet Approved
Fusidic AcidThe serum concentration of Ergotamine can be increased when it is combined with Fusidic Acid.Approved
GemfibrozilThe risk or severity of adverse effects can be increased when Ergotamine is combined with Gemfibrozil.Approved
GlyburideThe risk or severity of adverse effects can be increased when Ergotamine is combined with Glyburide.Approved
Glycerol PhenylbutyrateThe risk or severity of adverse effects can be increased when Ergotamine is combined with Glycerol Phenylbutyrate.Approved
HaloperidolThe risk or severity of adverse effects can be increased when Ergotamine is combined with Haloperidol.Approved
HarmalineHarmaline may increase the hypertensive activities of Ergotamine.Experimental
HistamineThe risk or severity of adverse effects can be increased when Ergotamine is combined with Histamine.Approved, Investigational
HyaluronidaseHyaluronidase may increase the vasoconstricting activities of Ergotamine.Approved, Investigational
HydralazineThe risk or severity of adverse effects can be increased when Ergotamine is combined with Hydralazine.Approved
HydrocortisoneThe risk or severity of adverse effects can be increased when Ergotamine is combined with Hydrocortisone.Approved, Vet Approved
IbrutinibThe serum concentration of Ibrutinib can be increased when it is combined with Ergotamine.Approved
IdelalisibThe metabolism of Ergotamine can be decreased when combined with Idelalisib.Approved
IfosfamideThe risk or severity of adverse effects can be increased when Ergotamine is combined with Ifosfamide.Approved
IloperidoneThe risk or severity of adverse effects can be increased when Ergotamine is combined with Iloperidone.Approved
ImatinibThe metabolism of Ergotamine can be decreased when combined with Imatinib.Approved
ImipramineImipramine may decrease the antihypertensive activities of Ergotamine.Approved
IndenololErgotamine may increase the atrioventricular blocking (AV block) activities of Indenolol.Withdrawn
IndinavirThe metabolism of Ergotamine can be decreased when combined with Indinavir.Approved
IndisulamThe risk or severity of adverse effects can be increased when Ergotamine is combined with Indisulam.Investigational
IndoraminIndoramin may decrease the vasoconstricting activities of Ergotamine.Withdrawn
IobenguaneThe therapeutic efficacy of Iobenguane can be decreased when used in combination with Ergotamine.Approved, Investigational
IprindoleIprindole may decrease the antihypertensive activities of Ergotamine.Experimental
IproniazidIproniazid may increase the hypertensive activities of Ergotamine.Withdrawn
IrbesartanThe risk or severity of adverse effects can be increased when Ergotamine is combined with Irbesartan.Approved, Investigational
IrinotecanThe risk or severity of adverse effects can be increased when Ergotamine is combined with Irinotecan.Approved, Investigational
IsavuconazoniumThe metabolism of Ergotamine can be decreased when combined with Isavuconazonium.Approved, Investigational
IsoniazidThe risk or severity of adverse effects can be increased when Ergotamine is combined with Isoniazid.Approved
IsradipineThe metabolism of Ergotamine can be decreased when combined with Isradipine.Approved
ItraconazoleThe serum concentration of Ergotamine can be increased when it is combined with Itraconazole.Approved, Investigational
IvacaftorThe serum concentration of Ergotamine can be increased when it is combined with Ivacaftor.Approved
JosamycinThe risk or severity of adverse effects can be increased when Ergotamine is combined with Josamycin.Approved, Investigational
KetazolamThe risk or severity of adverse effects can be increased when Ergotamine is combined with Ketazolam.Approved
KetoconazoleThe serum concentration of Ergotamine can be increased when it is combined with Ketoconazole.Approved, Investigational
LabetalolErgotamine may increase the atrioventricular blocking (AV block) activities of Labetalol.Approved
LandiololErgotamine may increase the atrioventricular blocking (AV block) activities of Landiolol.Investigational
LansoprazoleThe risk or severity of adverse effects can be increased when Ergotamine is combined with Lansoprazole.Approved, Investigational
LapatinibThe risk or severity of adverse effects can be increased when Ergotamine is combined with Lapatinib.Approved, Investigational
LedipasvirThe serum concentration of Ledipasvir can be increased when it is combined with Ergotamine.Approved
LercanidipineThe risk or severity of adverse effects can be increased when Ergotamine is combined with Lercanidipine.Approved, Investigational
LevofloxacinThe risk or severity of adverse effects can be increased when Ergotamine is combined with Levofloxacin.Approved, Investigational
LevosalbutamolThe risk or severity of adverse effects can be increased when Ergotamine is combined with Levosalbutamol.Approved
LidocaineThe metabolism of Ergotamine can be decreased when combined with Lidocaine.Approved, Vet Approved
LinagliptinThe risk or severity of adverse effects can be increased when Ergotamine is combined with Linagliptin.Approved
LisurideThe risk or severity of adverse effects can be increased when Lisuride is combined with Ergotamine.Approved, Investigational
LobeglitazoneThe metabolism of Ergotamine can be decreased when combined with Lobeglitazone.Approved, Investigational
LofepramineLofepramine may decrease the antihypertensive activities of Ergotamine.Experimental
LomitapideThe risk or severity of adverse effects can be increased when Ergotamine is combined with Lomitapide.Approved
LomustineThe risk or severity of adverse effects can be increased when Ergotamine is combined with Lomustine.Approved
LopinavirThe metabolism of Ergotamine can be decreased when combined with Lopinavir.Approved
LoratadineThe risk or severity of adverse effects can be increased when Ergotamine is combined with Loratadine.Approved
LorpiprazoleThe serum concentration of Ergotamine can be increased when it is combined with Lorpiprazole.Approved
LosartanThe risk or severity of adverse effects can be increased when Ergotamine is combined with Losartan.Approved
LovastatinThe metabolism of Ergotamine can be decreased when combined with Lovastatin.Approved, Investigational
LuliconazoleThe serum concentration of Ergotamine can be increased when it is combined with Luliconazole.Approved
LumacaftorThe metabolism of Ergotamine can be increased when combined with Lumacaftor.Approved
LurasidoneThe risk or severity of adverse effects can be increased when Ergotamine is combined with Lurasidone.Approved
Lysergic Acid DiethylamideThe risk or severity of adverse effects can be increased when Lysergic Acid Diethylamide is combined with Ergotamine.Illicit, Investigational, Withdrawn
ManidipineThe risk or severity of adverse effects can be increased when Ergotamine is combined with Manidipine.Approved, Investigational
MefloquineThe risk or severity of adverse effects can be increased when Ergotamine is combined with Mefloquine.Approved
MephentermineErgotamine may increase the hypertensive activities of Mephentermine.Approved
MepindololErgotamine may increase the atrioventricular blocking (AV block) activities of Mepindolol.Experimental
MequitazineThe risk or severity of adverse effects can be increased when Ergotamine is combined with Mequitazine.Approved
MetaraminolErgotamine may increase the hypertensive activities of Metaraminol.Approved, Investigational
MetergolineThe risk or severity of adverse effects can be increased when Metergoline is combined with Ergotamine.Experimental
MethadoneThe risk or severity of adverse effects can be increased when Ergotamine is combined with Methadone.Approved
MethazolamideThe risk or severity of adverse effects can be increased when Ergotamine is combined with Methazolamide.Approved
MethimazoleThe risk or severity of adverse effects can be increased when Ergotamine is combined with Methimazole.Approved
MethoxamineErgotamine may increase the hypertensive activities of Methoxamine.Approved, Investigational
MethylergometrineThe risk or severity of adverse effects can be increased when Ergotamine is combined with Methylergometrine.Approved
MethylprednisoloneThe risk or severity of adverse effects can be increased when Ergotamine is combined with Methylprednisolone.Approved, Vet Approved
MethysergideThe risk or severity of adverse effects can be increased when Methysergide is combined with Ergotamine.Approved
MetoprololErgotamine may increase the atrioventricular blocking (AV block) activities of Metoprolol.Approved, Investigational
MetronidazoleThe risk or severity of adverse effects can be increased when Ergotamine is combined with Metronidazole.Approved
MetyraponeThe risk or severity of adverse effects can be increased when Ergotamine is combined with Metyrapone.Approved
MevastatinThe serum concentration of Mevastatin can be increased when it is combined with Ergotamine.Experimental
MexiletineThe metabolism of Ergotamine can be decreased when combined with Mexiletine.Approved
MianserinThe therapeutic efficacy of Ergotamine can be decreased when used in combination with Mianserin.Approved, Investigational
MibefradilThe risk or severity of adverse effects can be increased when Ergotamine is combined with Mibefradil.Investigational, Withdrawn
MiconazoleThe risk or severity of adverse effects can be increased when Ergotamine is combined with Miconazole.Approved, Investigational, Vet Approved
MidazolamThe risk or severity of adverse effects can be increased when Ergotamine is combined with Midazolam.Approved, Illicit
MidodrineErgotamine may increase the hypertensive activities of Midodrine.Approved
MidostaurinThe metabolism of Ergotamine can be decreased when combined with Midostaurin.Approved
MifepristoneThe serum concentration of Ergotamine can be increased when it is combined with Mifepristone.Approved, Investigational
MinaprineMinaprine may increase the hypertensive activities of Ergotamine.Approved
MirtazapineMirtazapine may decrease the antihypertensive activities of Ergotamine.Approved
MitotaneThe serum concentration of Ergotamine can be decreased when it is combined with Mitotane.Approved
MitoxantroneThe risk or severity of adverse effects can be increased when Ergotamine is combined with Mitoxantrone.Approved, Investigational
ModafinilThe risk or severity of adverse effects can be increased when Ergotamine is combined with Modafinil.Approved, Investigational
NadololErgotamine may increase the atrioventricular blocking (AV block) activities of Nadolol.Approved
NaloxegolThe serum concentration of Naloxegol can be increased when it is combined with Ergotamine.Approved
NebivololErgotamine may increase the atrioventricular blocking (AV block) activities of Nebivolol.Approved, Investigational
NefazodoneThe metabolism of Ergotamine can be decreased when combined with Nefazodone.Approved, Withdrawn
NelfinavirThe metabolism of Ergotamine can be decreased when combined with Nelfinavir.Approved
NetupitantThe serum concentration of Ergotamine can be increased when it is combined with Netupitant.Approved
NevirapineThe metabolism of Ergotamine can be increased when combined with Nevirapine.Approved
NialamideNialamide may increase the hypertensive activities of Ergotamine.Withdrawn
NicardipineThe risk or severity of adverse effects can be increased when Ergotamine is combined with Nicardipine.Approved
NicergolineThe risk or severity of adverse effects can be increased when Nicergoline is combined with Ergotamine.Approved, Investigational
NicotinamideThe risk or severity of adverse effects can be increased when Ergotamine is combined with Nicotinamide.Approved
NifedipineThe risk or severity of adverse effects can be increased when Ergotamine is combined with Nifedipine.Approved
NilotinibThe metabolism of Ergotamine can be decreased when combined with Nilotinib.Approved, Investigational
NilvadipineThe risk or severity of adverse effects can be increased when Ergotamine is combined with Nilvadipine.Approved, Investigational
NintedanibThe serum concentration of Nintedanib can be increased when it is combined with Ergotamine.Approved
NisoldipineThe risk or severity of adverse effects can be increased when Ergotamine is combined with Nisoldipine.Approved
NitrendipineThe risk or severity of adverse effects can be increased when Ergotamine is combined with Nitrendipine.Approved, Investigational
Nitric OxideThe risk or severity of adverse effects can be increased when Ergotamine is combined with Nitric Oxide.Approved
NitroglycerinThe bioavailability of Ergotamine can be increased when combined with Nitroglycerin.Approved, Investigational
NorfloxacinThe risk or severity of adverse effects can be increased when Ergotamine is combined with Norfloxacin.Approved
NortriptylineNortriptyline may decrease the antihypertensive activities of Ergotamine.Approved
NoscapineThe risk or severity of adverse effects can be increased when Ergotamine is combined with Noscapine.Investigational
OlanzapineThe risk or severity of adverse effects can be increased when Ergotamine is combined with Olanzapine.Approved, Investigational
OlaparibThe metabolism of Ergotamine can be decreased when combined with Olaparib.Approved
OmeprazoleThe risk or severity of adverse effects can be increased when Ergotamine is combined with Omeprazole.Approved, Investigational, Vet Approved
OpipramolOpipramol may decrease the antihypertensive activities of Ergotamine.Investigational
OsimertinibThe serum concentration of Ergotamine can be increased when it is combined with Osimertinib.Approved
OxprenololErgotamine may increase the atrioventricular blocking (AV block) activities of Oxprenolol.Approved
OxybutyninThe risk or severity of adverse effects can be increased when Ergotamine is combined with Oxybutynin.Approved, Investigational
OxymetholoneThe risk or severity of adverse effects can be increased when Ergotamine is combined with Oxymetholone.Approved, Illicit
PaclitaxelThe risk or severity of adverse effects can be increased when Ergotamine is combined with Paclitaxel.Approved, Vet Approved
PalbociclibThe serum concentration of Ergotamine can be increased when it is combined with Palbociclib.Approved
ParamethasoneThe risk or severity of adverse effects can be increased when Ergotamine is combined with Paramethasone.Approved
PargylinePargyline may increase the hypertensive activities of Ergotamine.Approved
PazopanibThe serum concentration of Pazopanib can be increased when it is combined with Ergotamine.Approved
Peginterferon alfa-2bThe serum concentration of Ergotamine can be increased when it is combined with Peginterferon alfa-2b.Approved
PenbutololErgotamine may increase the atrioventricular blocking (AV block) activities of Penbutolol.Approved, Investigational
PentobarbitalThe metabolism of Ergotamine can be increased when combined with Pentobarbital.Approved, Vet Approved
PergolideThe risk or severity of adverse effects can be increased when Ergotamine is combined with Pergolide.Approved, Investigational, Vet Approved, Withdrawn
PhenelzineThe risk or severity of adverse effects can be increased when Ergotamine is combined with Phenelzine.Approved
PhenobarbitalThe metabolism of Ergotamine can be increased when combined with Phenobarbital.Approved
PhenylephrineErgotamine may increase the hypertensive activities of Phenylephrine.Approved
PhenytoinThe metabolism of Ergotamine can be increased when combined with Phenytoin.Approved, Vet Approved
PilocarpineThe risk or severity of adverse effects can be increased when Ergotamine is combined with Pilocarpine.Approved
PimozideThe risk or severity of adverse effects can be increased when Ergotamine is combined with Pimozide.Approved
PindololErgotamine may increase the atrioventricular blocking (AV block) activities of Pindolol.Approved
PiperaquineThe risk or severity of adverse effects can be increased when Ergotamine is combined with Piperaquine.Approved, Investigational
PirlindolePirlindole may increase the hypertensive activities of Ergotamine.Approved
PitavastatinThe serum concentration of Pitavastatin can be increased when it is combined with Ergotamine.Approved
Platelet Activating FactorErgotamine may increase the atrioventricular blocking (AV block) activities of Platelet Activating Factor.Experimental
PosaconazoleThe serum concentration of Ergotamine can be increased when it is combined with Posaconazole.Approved, Investigational, Vet Approved
PractololErgotamine may increase the atrioventricular blocking (AV block) activities of Practolol.Approved
PravastatinThe serum concentration of Pravastatin can be increased when it is combined with Ergotamine.Approved
PrazosinPrazosin may decrease the vasoconstricting activities of Ergotamine.Approved
PrednisoloneThe risk or severity of adverse effects can be increased when Ergotamine is combined with Prednisolone.Approved, Vet Approved
PrednisoneThe risk or severity of adverse effects can be increased when Ergotamine is combined with Prednisone.Approved, Vet Approved
PrimaquineThe risk or severity of adverse effects can be increased when Ergotamine is combined with Primaquine.Approved
PrimidoneThe metabolism of Ergotamine can be increased when combined with Primidone.Approved, Vet Approved
ProgesteroneThe risk or severity of adverse effects can be increased when Ergotamine is combined with Progesterone.Approved, Vet Approved
PropofolThe risk or severity of adverse effects can be increased when Ergotamine is combined with Propofol.Approved, Investigational, Vet Approved
PropranololErgotamine may increase the atrioventricular blocking (AV block) activities of Propranolol.Approved, Investigational
ProtriptylineProtriptyline may decrease the antihypertensive activities of Ergotamine.Approved
PrucaloprideThe serum concentration of Prucalopride can be increased when it is combined with Ergotamine.Approved
QuinidineThe risk or severity of adverse effects can be increased when Ergotamine is combined with Quinidine.Approved
QuinineThe risk or severity of adverse effects can be increased when Ergotamine is combined with Quinine.Approved
QuinupristinThe risk or severity of adverse effects can be increased when Ergotamine is combined with Quinupristin.Approved
RabeprazoleThe risk or severity of adverse effects can be increased when Ergotamine is combined with Rabeprazole.Approved, Investigational
RaloxifeneThe risk or severity of adverse effects can be increased when Ergotamine is combined with Raloxifene.Approved, Investigational
RanitidineThe risk or severity of adverse effects can be increased when Ergotamine is combined with Ranitidine.Approved
RanolazineThe serum concentration of Ranolazine can be increased when it is combined with Ergotamine.Approved, Investigational
RegorafenibThe risk or severity of adverse effects can be increased when Ergotamine is combined with Regorafenib.Approved
RepaglinideThe risk or severity of adverse effects can be increased when Ergotamine is combined with Repaglinide.Approved, Investigational
ResveratrolThe risk or severity of adverse effects can be increased when Ergotamine is combined with Resveratrol.Approved, Experimental, Investigational
RifabutinThe metabolism of Ergotamine can be increased when combined with Rifabutin.Approved
RifampicinThe metabolism of Ergotamine can be increased when combined with Rifampicin.Approved
RifapentineThe metabolism of Ergotamine can be increased when combined with Rifapentine.Approved
RifaximinThe serum concentration of Rifaximin can be increased when it is combined with Ergotamine.Approved, Investigational
RilpivirineThe serum concentration of Rilpivirine can be increased when it is combined with Ergotamine.Approved
RisperidoneThe risk or severity of adverse effects can be increased when Ergotamine is combined with Risperidone.Approved, Investigational
RitonavirThe risk or severity of adverse effects can be increased when Ergotamine is combined with Ritonavir.Approved, Investigational
RivastigmineThe risk or severity of adverse effects can be increased when Ergotamine is combined with Rivastigmine.Approved, Investigational
RolitetracyclineThe risk or severity of adverse effects can be increased when Ergotamine is combined with Rolitetracycline.Approved
RopiniroleThe metabolism of Ergotamine can be decreased when combined with Ropinirole.Approved, Investigational
RosuvastatinThe serum concentration of Rosuvastatin can be increased when it is combined with Ergotamine.Approved
RoxithromycinThe risk or severity of adverse effects can be increased when Ergotamine is combined with Roxithromycin.Approved, Investigational, Withdrawn
RucaparibThe metabolism of Ergotamine can be decreased when combined with Rucaparib.Approved, Investigational
RutinThe risk or severity of adverse effects can be increased when Ergotamine is combined with Rutin.Experimental, Investigational
SalbutamolThe risk or severity of adverse effects can be increased when Ergotamine is combined with Salbutamol.Approved, Vet Approved
SaquinavirThe metabolism of Ergotamine can be decreased when combined with Saquinavir.Approved, Investigational
SarilumabThe therapeutic efficacy of Ergotamine can be decreased when used in combination with Sarilumab.Approved
SertralineThe risk or severity of adverse effects can be increased when Ergotamine is combined with Sertraline.Approved
SildenafilThe metabolism of Ergotamine can be decreased when combined with Sildenafil.Approved, Investigational
SilodosinThe serum concentration of Silodosin can be increased when it is combined with Ergotamine.Approved
SiltuximabThe serum concentration of Ergotamine can be decreased when it is combined with Siltuximab.Approved
SimeprevirThe serum concentration of Ergotamine can be increased when it is combined with Simeprevir.Approved
SimvastatinThe serum concentration of Simvastatin can be increased when it is combined with Ergotamine.Approved
SirolimusThe risk or severity of adverse effects can be increased when Ergotamine is combined with Sirolimus.Approved, Investigational
SitaxentanThe risk or severity of adverse effects can be increased when Ergotamine is combined with Sitaxentan.Approved, Investigational, Withdrawn
SorafenibThe risk or severity of adverse effects can be increased when Ergotamine is combined with Sorafenib.Approved, Investigational
SotalolErgotamine may increase the atrioventricular blocking (AV block) activities of Sotalol.Approved
SpironolactoneSpironolactone may decrease the vasoconstricting activities of Ergotamine.Approved
St. John's WortThe serum concentration of Ergotamine can be decreased when it is combined with St. John's Wort.Approved, Investigational, Nutraceutical
StiripentolThe serum concentration of Ergotamine can be increased when it is combined with Stiripentol.Approved
SulfamethoxazoleThe risk or severity of adverse effects can be increased when Ergotamine is combined with Sulfamethoxazole.Approved
SulfanilamideThe risk or severity of adverse effects can be increased when Ergotamine is combined with Sulfanilamide.Approved
SulfinpyrazoneThe risk or severity of adverse effects can be increased when Ergotamine is combined with Sulfinpyrazone.Approved
SulfisoxazoleThe metabolism of Ergotamine can be decreased when combined with Sulfisoxazole.Approved, Vet Approved
TacrolimusThe risk or severity of adverse effects can be increased when Ergotamine is combined with Tacrolimus.Approved, Investigational
TadalafilThe risk or severity of adverse effects can be increased when Ergotamine is combined with Tadalafil.Approved, Investigational
TalinololErgotamine may increase the atrioventricular blocking (AV block) activities of Talinolol.Investigational
TamoxifenThe risk or severity of adverse effects can be increased when Ergotamine is combined with Tamoxifen.Approved
TamsulosinTamsulosin may decrease the vasoconstricting activities of Ergotamine.Approved, Investigational
TelaprevirThe serum concentration of Ergotamine can be increased when it is combined with Telaprevir.Approved, Withdrawn
TelithromycinThe metabolism of Ergotamine can be decreased when combined with Telithromycin.Approved
TemsirolimusThe risk or severity of adverse effects can be increased when Ergotamine is combined with Temsirolimus.Approved
TeniposideThe risk or severity of adverse effects can be increased when Ergotamine is combined with Teniposide.Approved
Tenofovir disoproxilThe metabolism of Ergotamine can be decreased when combined with Tenofovir disoproxil.Approved, Investigational
TerazosinTerazosin may decrease the vasoconstricting activities of Ergotamine.Approved
TerfenadineThe risk or severity of adverse effects can be increased when Ergotamine is combined with Terfenadine.Withdrawn
TergurideThe risk or severity of adverse effects can be increased when Terguride is combined with Ergotamine.Experimental
TeriflunomideThe serum concentration of Ergotamine can be decreased when it is combined with Teriflunomide.Approved
TertatololErgotamine may increase the atrioventricular blocking (AV block) activities of Tertatolol.Experimental
TesmilifeneThe risk or severity of adverse effects can be increased when Ergotamine is combined with Tesmilifene.Investigational
TestosteroneThe risk or severity of adverse effects can be increased when Ergotamine is combined with Testosterone.Approved, Investigational
Testosterone cypionateThe risk or severity of adverse effects can be increased when Ergotamine is combined with Testosterone cypionate.Approved
Testosterone enanthateThe risk or severity of adverse effects can be increased when Ergotamine is combined with Testosterone enanthate.Approved
Testosterone undecanoateThe risk or severity of adverse effects can be increased when Ergotamine is combined with Testosterone undecanoate.Approved, Investigational
TetracyclineThe risk or severity of adverse effects can be increased when Ergotamine is combined with Tetracycline.Approved, Vet Approved
TheophyllineThe metabolism of Ergotamine can be decreased when combined with Theophylline.Approved
ThiopentalThe risk or severity of adverse effects can be increased when Ergotamine is combined with Thiopental.Approved, Vet Approved
TianeptineTianeptine may decrease the antihypertensive activities of Ergotamine.Approved, Investigational
TicagrelorThe risk or severity of adverse effects can be increased when Ergotamine is combined with Ticagrelor.Approved
TiclopidineThe metabolism of Ergotamine can be decreased when combined with Ticlopidine.Approved
TimololErgotamine may increase the atrioventricular blocking (AV block) activities of Timolol.Approved
TioconazoleThe risk or severity of adverse effects can be increased when Ergotamine is combined with Tioconazole.Approved
TipranavirThe risk or severity of adverse effects can be increased when Ergotamine is combined with Tipranavir.Approved, Investigational
TocilizumabThe serum concentration of Ergotamine can be decreased when it is combined with Tocilizumab.Approved
TofisopamThe risk or severity of adverse effects can be increased when Ergotamine is combined with Tofisopam.Approved
ToloxatoneToloxatone may increase the hypertensive activities of Ergotamine.Approved
TolvaptanThe serum concentration of Tolvaptan can be increased when it is combined with Ergotamine.Approved
TopiroxostatThe risk or severity of adverse effects can be increased when Ergotamine is combined with Topiroxostat.Approved, Investigational
TopotecanThe serum concentration of Topotecan can be increased when it is combined with Ergotamine.Approved, Investigational
TramadolThe risk or severity of adverse effects can be increased when Ergotamine is combined with Tramadol.Approved, Investigational
Trans-2-PhenylcyclopropylamineTrans-2-Phenylcyclopropylamine may increase the hypertensive activities of Ergotamine.Experimental
TranylcypromineThe risk or severity of adverse effects can be increased when Ergotamine is combined with Tranylcypromine.Approved
TrimazosinTrimazosin may decrease the vasoconstricting activities of Ergotamine.Experimental
TrimipramineTrimipramine may decrease the antihypertensive activities of Ergotamine.Approved
TroglitazoneThe risk or severity of adverse effects can be increased when Ergotamine is combined with Troglitazone.Investigational, Withdrawn
TroleandomycinThe risk or severity of adverse effects can be increased when Ergotamine is combined with Troleandomycin.Approved
UrapidilUrapidil may decrease the vasoconstricting activities of Ergotamine.Investigational
Valproic AcidThe risk or severity of adverse effects can be increased when Ergotamine is combined with Valproic Acid.Approved, Investigational
VemurafenibThe serum concentration of Ergotamine can be increased when it is combined with Vemurafenib.Approved
VenlafaxineThe metabolism of Ergotamine can be decreased when combined with Venlafaxine.Approved
VerapamilThe metabolism of Ergotamine can be decreased when combined with Verapamil.Approved
VinblastineThe risk or severity of adverse effects can be increased when Ergotamine is combined with Vinblastine.Approved
VincristineThe excretion of Vincristine can be decreased when combined with Ergotamine.Approved, Investigational
VincristineThe risk or severity of adverse effects can be increased when Ergotamine is combined with Vincristine.Approved, Investigational
VinorelbineThe risk or severity of adverse effects can be increased when Ergotamine is combined with Vinorelbine.Approved, Investigational
VoriconazoleThe serum concentration of Ergotamine can be increased when it is combined with Voriconazole.Approved, Investigational
ZafirlukastThe risk or severity of adverse effects can be increased when Ergotamine is combined with Zafirlukast.Approved, Investigational
ZiprasidoneThe metabolism of Ergotamine can be decreased when combined with Ziprasidone.Approved
ZucapsaicinThe metabolism of Ergotamine can be decreased when combined with Zucapsaicin.Approved
Food Interactions
  • Caffeine increases absorption.
  • Take without regard to meals.

References

General References
  1. Tfelt-Hansen P, Saxena PR, Dahlof C, Pascual J, Lainez M, Henry P, Diener H, Schoenen J, Ferrari MD, Goadsby PJ: Ergotamine in the acute treatment of migraine: a review and European consensus. Brain. 2000 Jan;123 ( Pt 1):9-18. [PubMed:10611116]
  2. Schardl CL, Panaccione DG, Tudzynski P: Ergot alkaloids--biology and molecular biology. Alkaloids Chem Biol. 2006;63:45-86. [PubMed:17133714]
External Links
Human Metabolome Database
HMDB0014834
KEGG Compound
C07544
PubChem Compound
8223
PubChem Substance
46507632
ChemSpider
7930
BindingDB
50027065
ChEBI
64318
ChEMBL
CHEMBL442
Therapeutic Targets Database
DAP000141
PharmGKB
PA164747651
HET
ERM
RxList
RxList Drug Page
Drugs.com
Drugs.com Drug Page
PDRhealth
PDRhealth Drug Page
Wikipedia
Ergotamine
ATC Codes
N02CA52 — Ergotamine, combinations excl. psycholepticsN02CA72 — Ergotamine, combinations with psycholepticsN02CA02 — Ergotamine
AHFS Codes
  • 12:16.00 — Sympatholytic (Adrenergic Blocking) Agents
PDB Entries
4iar / 4ib4 / 4nc3 / 5tud
MSDS
Download (53.1 KB)

Clinical Trials

Clinical Trials
PhaseStatusPurposeConditionsCount
1CompletedNot AvailableAutonomic Failure / Idiopathic orthostatic hypotension1

Pharmacoeconomics

Manufacturers
  • 3m pharmaceuticals inc
  • Rosedale therapeutics
  • Parke davis div warner lambert co
  • Organon usa inc
Packagers
Dosage forms
FormRouteStrength
Tablet, extended releaseOral
TabletOral
CapsuleOral
Tablet, orally disintegratingSublingual2 mg/1
TabletSublingual2 mg
TabletOral2 mg/1
Tablet, film coatedOral
SuppositoryRectal
Prices
Unit descriptionCostUnit
Ergotamine tartrate powder224.35USD powder
Ergomar 2 mg tablet sl8.97USD tablet
Migergot suppository7.39USD suppository
Cafergot tablet1.89USD tablet
Ergotamine-caffeine tablet1.14USD tablet
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)213.5 dec °CPhysProp
water solubilitySlightNot Available
logP2Not Available
Predicted Properties
PropertyValueSource
Water Solubility0.223 mg/mLALOGPS
logP2.95ALOGPS
logP2.6ChemAxon
logS-3.4ALOGPS
pKa (Strongest Acidic)9.7ChemAxon
pKa (Strongest Basic)7.78ChemAxon
Physiological Charge1ChemAxon
Hydrogen Acceptor Count6ChemAxon
Hydrogen Donor Count3ChemAxon
Polar Surface Area118.21 Å2ChemAxon
Rotatable Bond Count4ChemAxon
Refractivity160.17 m3·mol-1ChemAxon
Polarizability61.69 Å3ChemAxon
Number of Rings8ChemAxon
Bioavailability1ChemAxon
Rule of FiveNoChemAxon
Ghose FilterNoChemAxon
Veber's RuleNoChemAxon
MDDR-like RuleNoChemAxon
Predicted ADMET features
PropertyValueProbability
Human Intestinal Absorption+0.9311
Blood Brain Barrier-0.9644
Caco-2 permeable-0.7317
P-glycoprotein substrateSubstrate0.8678
P-glycoprotein inhibitor IInhibitor0.7801
P-glycoprotein inhibitor IIInhibitor0.6032
Renal organic cation transporterNon-inhibitor0.8178
CYP450 2C9 substrateNon-substrate0.8205
CYP450 2D6 substrateNon-substrate0.9116
CYP450 3A4 substrateSubstrate0.7408
CYP450 1A2 substrateInhibitor0.9107
CYP450 2C9 inhibitorNon-inhibitor0.9071
CYP450 2D6 inhibitorNon-inhibitor0.923
CYP450 2C19 inhibitorNon-inhibitor0.8849
CYP450 3A4 inhibitorInhibitor0.7959
CYP450 inhibitory promiscuityLow CYP Inhibitory Promiscuity0.6759
Ames testNon AMES toxic0.9133
CarcinogenicityNon-carcinogens0.9604
BiodegradationNot ready biodegradable0.99
Rat acute toxicity2.9840 LD50, mol/kg Not applicable
hERG inhibition (predictor I)Weak inhibitor0.8701
hERG inhibition (predictor II)Non-inhibitor0.6708
ADMET data is predicted using admetSAR, a free tool for evaluating chemical ADMET properties. (23092397)

Spectra

Mass Spec (NIST)
Download (12 KB)
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

Taxonomy

Description
This compound belongs to the class of organic compounds known as ergotamines, dihydroergotamines, and derivatives. These are organic compounds containing an ergotamine moiety, which is structurally characterized by a benzyl substituent attached to the piperazine ring of the ergopeptine backbone.
Kingdom
Organic compounds
Super Class
Alkaloids and derivatives
Class
Ergoline and derivatives
Sub Class
Lysergic acids and derivatives
Direct Parent
Ergotamines, dihydroergotamines, and derivatives
Alternative Parents
Hybrid peptides / Dipeptides / Lysergamides / Indoloquinolines / Benzoquinolines / Quinoline-3-carboxamides / Pyrroloquinolines / N-acyl-alpha amino acids and derivatives / 3-alkylindoles / Isoindoles and derivatives
show 19 more
Substituents
Ergotamine / Hybrid peptide / Alpha-dipeptide / Lysergic acid amide / Indoloquinoline / Benzoquinoline / Quinoline-3-carboxamide / N-acyl-alpha amino acid or derivatives / Pyrroloquinoline / Quinoline
show 39 more
Molecular Framework
Aromatic heteropolycyclic compounds
External Descriptors
peptide ergot alkaloid (CHEBI:64318)

Targets

Kind
Protein
Organism
Human
Pharmacological action
Yes
Actions
Agonist
General Function
Serotonin receptor activity
Specific Function
G-protein coupled receptor for 5-hydroxytryptamine (serotonin). Also functions as a receptor for ergot alkaloid derivatives, various anxiolytic and antidepressant drugs and other psychoactive subst...
Gene Name
HTR1D
Uniprot ID
P28221
Uniprot Name
5-hydroxytryptamine receptor 1D
Molecular Weight
41906.38 Da
References
  1. Silberstein SD, McCrory DC: Ergotamine and dihydroergotamine: history, pharmacology, and efficacy. Headache. 2003 Feb;43(2):144-66. [PubMed:12558771]
  2. Lovenberg TW, Erlander MG, Baron BM, Racke M, Slone AL, Siegel BW, Craft CM, Burns JE, Danielson PE, Sutcliffe JG: Molecular cloning and functional expression of 5-HT1E-like rat and human 5-hydroxytryptamine receptor genes. Proc Natl Acad Sci U S A. 1993 Mar 15;90(6):2184-8. [PubMed:8384716]
  3. Hoyer D, Lery H, Waeber C, Bruinvels AT, Nozulak J, Palacios JM: "5-HT1R" or 5-HT1D sites? Evidence for 5-HT1D binding sites in rabbit brain. Naunyn Schmiedebergs Arch Pharmacol. 1992 Sep;346(3):249-54. [PubMed:1407010]
  4. Sanchez-Lopez A, Centurion D, Vazquez E, Arulmani U, Saxena PR, Villalon CM: Pharmacological profile of the 5-HT-induced inhibition of cardioaccelerator sympathetic outflow in pithed rats: correlation with 5-HT1 and putative 5-ht5A/5B receptors. Br J Pharmacol. 2003 Oct;140(4):725-35. Epub 2003 Sep 22. [PubMed:14504136]
  5. Deliganis AV, Peroutka SJ: 5-Hydroxtryptamine1D receptor agonism predicts antimigraine efficacy. Headache. 1991 Apr;31(4):228-31. [PubMed:1646776]
Kind
Protein
Organism
Human
Pharmacological action
Yes
Actions
Agonist
General Function
Serotonin receptor activity
Specific Function
G-protein coupled receptor for 5-hydroxytryptamine (serotonin). Also functions as a receptor for ergot alkaloid derivatives, various anxiolytic and antidepressant drugs and other psychoactive subst...
Gene Name
HTR1B
Uniprot ID
P28222
Uniprot Name
5-hydroxytryptamine receptor 1B
Molecular Weight
43567.535 Da
References
  1. Villalon CM, De Vries P, Rabelo G, Centurion D, Sanchez-Lopez A, Saxena P: Canine external carotid vasoconstriction to methysergide, ergotamine and dihydroergotamine: role of 5-HT1B/1D receptors and alpha2-adrenoceptors. Br J Pharmacol. 1999 Feb;126(3):585-94. [PubMed:10188968]
  2. Willems EW, Trion M, De Vries P, Heiligers JP, Villalon CM, Saxena PR: Pharmacological evidence that alpha1-and alpha2-adrenoceptors mediate vasoconstriction of carotid arteriovenous anastomoses in anaesthetized pigs. Br J Pharmacol. 1999 Jul;127(5):1263-71. [PubMed:10455274]
  3. Cohen ML, Schenck K: Contractile responses to sumatriptan and ergotamine in the rabbit saphenous vein: effect of selective 5-HT(1F) receptor agonists and PGF(2alpha). Br J Pharmacol. 2000 Oct;131(3):562-8. [PubMed:11015308]
  4. Valdivia LF, Centurion D, Arulmani U, Saxena PR, Villalon CM: 5-HT1B receptors, alpha2A/2C- and, to a lesser extent, alpha1-adrenoceptors mediate the external carotid vasoconstriction to ergotamine in vagosympathectomised dogs. Naunyn Schmiedebergs Arch Pharmacol. 2004 Jul;370(1):46-53. Epub 2004 Jun 29. [PubMed:15224175]
Kind
Protein
Organism
Human
Pharmacological action
Yes
Actions
Agonist
General Function
Virus receptor activity
Specific Function
G-protein coupled receptor for 5-hydroxytryptamine (serotonin). Also functions as a receptor for various drugs and psychoactive substances, including mescaline, psilocybin, 1-(2,5-dimethoxy-4-iodop...
Gene Name
HTR2A
Uniprot ID
P28223
Uniprot Name
5-hydroxytryptamine receptor 2A
Molecular Weight
52602.58 Da
References
  1. Bom AH, Heiligers JP, Saxena PR, Verdouw PD: Reduction of cephalic arteriovenous shunting by ergotamine is not mediated by 5-HT1-like or 5-HT2 receptors. Br J Pharmacol. 1989 Jun;97(2):383-90. [PubMed:2758221]
  2. Panconesi A, Anselmi B, Curradi C, Perfetto F, Piluso A, Franchi G: Comparison between venoconstrictor effects of sumatriptan and ergotamine in migraine patients. Headache. 1994 Apr;34(4):194-7. [PubMed:8014033]
  3. Chen X, Ji ZL, Chen YZ: TTD: Therapeutic Target Database. Nucleic Acids Res. 2002 Jan 1;30(1):412-5. [PubMed:11752352]
Kind
Protein
Organism
Human
Pharmacological action
Unknown
Actions
Agonist
General Function
Potassium channel regulator activity
Specific Function
Dopamine receptor whose activity is mediated by G proteins which inhibit adenylyl cyclase.
Gene Name
DRD2
Uniprot ID
P14416
Uniprot Name
D(2) dopamine receptor
Molecular Weight
50618.91 Da
References
  1. Verhoeff NP, Visser WH, Ferrari MD, Saxena PR, van Royen EA: Dopamine D2-receptor imaging with 123I-iodobenzamide SPECT in migraine patients abusing ergotamine: does ergotamine cross the blood brain barrier? Cephalalgia. 1993 Oct;13(5):325-9. [PubMed:8242725]
  2. Larson BT, Samford MD, Camden JM, Piper EL, Kerley MS, Paterson JA, Turner JT: Ergovaline binding and activation of D2 dopamine receptors in GH4ZR7 cells. J Anim Sci. 1995 May;73(5):1396-400. [PubMed:7665369]
Kind
Protein
Organism
Human
Pharmacological action
Yes
Actions
Partial agonist
General Function
Protein heterodimerization activity
Specific Function
This alpha-adrenergic receptor mediates its action by association with G proteins that activate a phosphatidylinositol-calcium second messenger system. Its effect is mediated by G(q) and G(11) prot...
Gene Name
ADRA1A
Uniprot ID
P35348
Uniprot Name
Alpha-1A adrenergic receptor
Molecular Weight
51486.005 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. Gornemann T, Jahnichen S, Schurad B, Latte KP, Horowski R, Tack J, Flieger M, Pertz HH: Pharmacological properties of a wide array of ergolines at functional alpha(1)-adrenoceptor subtypes. Naunyn Schmiedebergs Arch Pharmacol. 2008 Jan;376(5):321-30. Epub 2007 Dec 8. [PubMed:18066532]
Kind
Protein
Organism
Human
Pharmacological action
Yes
Actions
Partial agonist
General Function
Protein heterodimerization activity
Specific Function
This alpha-adrenergic receptor mediates its action by association with G proteins that activate a phosphatidylinositol-calcium second messenger system. Its effect is mediated by G(q) and G(11) prot...
Gene Name
ADRA1B
Uniprot ID
P35368
Uniprot Name
Alpha-1B adrenergic receptor
Molecular Weight
56835.375 Da
References
  1. Gornemann T, Jahnichen S, Schurad B, Latte KP, Horowski R, Tack J, Flieger M, Pertz HH: Pharmacological properties of a wide array of ergolines at functional alpha(1)-adrenoceptor subtypes. Naunyn Schmiedebergs Arch Pharmacol. 2008 Jan;376(5):321-30. Epub 2007 Dec 8. [PubMed:18066532]
Kind
Protein
Organism
Human
Pharmacological action
Yes
Actions
Partial agonist
General Function
Alpha1-adrenergic receptor activity
Specific Function
This alpha-adrenergic receptor mediates its effect through the influx of extracellular calcium.
Gene Name
ADRA1D
Uniprot ID
P25100
Uniprot Name
Alpha-1D adrenergic receptor
Molecular Weight
60462.205 Da
References
  1. Gornemann T, Jahnichen S, Schurad B, Latte KP, Horowski R, Tack J, Flieger M, Pertz HH: Pharmacological properties of a wide array of ergolines at functional alpha(1)-adrenoceptor subtypes. Naunyn Schmiedebergs Arch Pharmacol. 2008 Jan;376(5):321-30. Epub 2007 Dec 8. [PubMed:18066532]
Kind
Protein
Organism
Human
Pharmacological action
Unknown
Actions
Partial agonist
General Function
Thioesterase binding
Specific Function
Alpha-2 adrenergic receptors mediate the catecholamine-induced inhibition of adenylate cyclase through the action of G proteins. The rank order of potency for agonists of this receptor is oxymetazo...
Gene Name
ADRA2A
Uniprot ID
P08913
Uniprot Name
Alpha-2A adrenergic receptor
Molecular Weight
48956.275 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. Gornemann T, Jahnichen S, Schurad B, Latte KP, Horowski R, Tack J, Flieger M, Pertz HH: Pharmacological properties of a wide array of ergolines at functional alpha(1)-adrenoceptor subtypes. Naunyn Schmiedebergs Arch Pharmacol. 2008 Jan;376(5):321-30. Epub 2007 Dec 8. [PubMed:18066532]
Kind
Protein
Organism
Human
Pharmacological action
Unknown
Actions
Agonist
Partial agonist
General Function
Epinephrine binding
Specific Function
Alpha-2 adrenergic receptors mediate the catecholamine-induced inhibition of adenylate cyclase through the action of G proteins. The rank order of potency for agonists of this receptor is clonidine...
Gene Name
ADRA2B
Uniprot ID
P18089
Uniprot Name
Alpha-2B adrenergic receptor
Molecular Weight
49565.8 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]
Kind
Protein
Organism
Human
Pharmacological action
Unknown
Actions
Inhibitor
General Function
Norepinephrine:sodium symporter activity
Specific Function
Amine transporter. Terminates the action of noradrenaline by its high affinity sodium-dependent reuptake into presynaptic terminals.
Gene Name
SLC6A2
Uniprot ID
P23975
Uniprot Name
Sodium-dependent noradrenaline transporter
Molecular Weight
69331.42 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]
Kind
Protein group
Organism
Human
Pharmacological action
Unknown
Actions
Agonist
General Function
G-protein coupled amine receptor activity
Specific Function
Dopamine receptor whose activity is mediated by G proteins which activate adenylyl cyclase.

Components:
References
  1. Bigal ME, Tepper SJ: Ergotamine and dihydroergotamine: a review. Curr Pain Headache Rep. 2003 Feb;7(1):55-62. [PubMed:12525272]
Kind
Protein
Organism
Human
Pharmacological action
Unknown
Actions
Agonist
General Function
Serotonin receptor activity
Specific Function
G-protein coupled receptor for 5-hydroxytryptamine (serotonin). Also functions as a receptor for various drugs and psychoactive substances. Ligand binding causes a conformation change that triggers...
Gene Name
HTR1A
Uniprot ID
P08908
Uniprot Name
5-hydroxytryptamine receptor 1A
Molecular Weight
46106.335 Da
References
  1. Bigal ME, Tepper SJ: Ergotamine and dihydroergotamine: a review. Curr Pain Headache Rep. 2003 Feb;7(1):55-62. [PubMed:12525272]
Kind
Protein
Organism
Human
Pharmacological action
Unknown
Actions
Agonist
General Function
Serotonin receptor activity
Specific Function
G-protein coupled receptor for 5-hydroxytryptamine (serotonin). Also functions as a receptor for various alkaloids and psychoactive substances. Ligand binding causes a conformation change that trig...
Gene Name
HTR1F
Uniprot ID
P30939
Uniprot Name
5-hydroxytryptamine receptor 1F
Molecular Weight
41708.505 Da
References
  1. Bigal ME, Tepper SJ: Ergotamine and dihydroergotamine: a review. Curr Pain Headache Rep. 2003 Feb;7(1):55-62. [PubMed:12525272]
Kind
Protein
Organism
Human
Pharmacological action
Unknown
Actions
Agonist
General Function
Serotonin receptor activity
Specific Function
G-protein coupled receptor for 5-hydroxytryptamine (serotonin). Also functions as a receptor for various drugs and psychoactive substances, including ergot alkaloid derivatives, 1-2,5,-dimethoxy-4-...
Gene Name
HTR2C
Uniprot ID
P28335
Uniprot Name
5-hydroxytryptamine receptor 2C
Molecular Weight
51820.705 Da
References
  1. Bigal ME, Tepper SJ: Ergotamine and dihydroergotamine: a review. Curr Pain Headache Rep. 2003 Feb;7(1):55-62. [PubMed:12525272]
Kind
Protein
Organism
Human
Pharmacological action
Unknown
General Function
Serotonin receptor activity
Specific Function
G-protein coupled receptor for 5-hydroxytryptamine (serotonin). Also functions as a receptor for various ergot alkaloid derivatives and psychoactive substances. Ligand binding causes a conformation...
Gene Name
HTR2B
Uniprot ID
P41595
Uniprot Name
5-hydroxytryptamine receptor 2B
Molecular Weight
54297.41 Da
References
  1. Rothman RB, Baumann MH, Savage JE, Rauser L, McBride A, Hufeisen SJ, Roth BL: Evidence for possible involvement of 5-HT(2B) receptors in the cardiac valvulopathy associated with fenfluramine and other serotonergic medications. Circulation. 2000 Dec 5;102(23):2836-41. [PubMed:11104741]

Enzymes

Kind
Protein
Organism
Human
Pharmacological action
Unknown
Actions
Substrate
Inhibitor
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 react...
Gene Name
CYP3A4
Uniprot ID
P08684
Uniprot Name
Cytochrome P450 3A4
Molecular Weight
57342.67 Da
References
  1. Preissner S, Kroll K, Dunkel M, Senger C, Goldsobel G, Kuzman D, Guenther S, Winnenburg R, Schroeder M, Preissner R: SuperCYP: a comprehensive database on Cytochrome P450 enzymes including a tool for analysis of CYP-drug interactions. Nucleic Acids Res. 2010 Jan;38(Database issue):D237-43. doi: 10.1093/nar/gkp970. Epub 2009 Nov 24. [PubMed:19934256]
Kind
Protein
Organism
Human
Pharmacological action
Unknown
Actions
Substrate
General Function
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. 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
Uniprot Name
Multidrug resistance protein 1
Molecular Weight
141477.255 Da
References
  1. 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]
  2. Yasuda K, Lan LB, Sanglard D, Furuya K, Schuetz JD, Schuetz EG: Interaction of cytochrome P450 3A inhibitors with P-glycoprotein. J Pharmacol Exp Ther. 2002 Oct;303(1):323-32. [PubMed:12235267]

Drug created on June 13, 2005 07:24 / Updated on January 23, 2018 12:13