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Identification
NameErgotamine
Accession NumberDB00696  (APRD00677)
TypeSmall Molecule
GroupsApproved
DescriptionA 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
External Identifiers Not Available
Approved Prescription Products
NameDosageStrengthRouteLabellerMarketing StartMarketing End
Ergomar Slt 2mgTablet2 mgSublingualAventis Pharma Inc1975-12-312003-07-22Canada
Approved 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
Approved Over the Counter ProductsNot Available
Unapproved/Other Products Not Available
International Brands
NameCompany
AnervanRecip
AntimigraineTa Fong
EnxakCazi
ErgamGedeon Richter
Ergo-KranitKrewel Meuselbach
GynaemineSriprasit Dispensary
WigrettesNot Available
Brand mixtures
NameLabellerIngredients
CafergotKAISER FOUNDATION HOSPITALS
Cafergot SupNovartis Pharmaceuticals Canada Inc
Cafergot TabNovartis Pharmaceuticals Canada Inc
Ergodryl CapErfa Canada 2012 Inc
ErgotamineWest ward Pharmaceutical Corp
Ergotamine Tartrate and CaffeineKAISER FOUNDATION HOSPITALS
Gravergol CapsulesCan Med Pharma Inc.
Megral TabsGlaxo Wellcome Inc.
MigergotG&W Laboratories, Inc.
Salts
Name/CASStructureProperties
Ergotamine Tartrate
ThumbNot applicableDBSALT000979
Categories
UNIIPR834Q503T
CAS number113-15-5
WeightAverage: 581.6615
Monoisotopic: 581.263819255
Chemical FormulaC33H35N5O5
InChI KeyXCGSFFUVFURLIX-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][C@@]12CCCN1C(=O)[[email protected]](CC1=CC=CC=C1)N1C(=O)[C@](C)(NC(=O)[[email protected]]3CN(C)[C@]4([H])CC5=CNC6=CC=CC(=C56)C4=C3)O[C@@]21O
Pharmacology
IndicationFor use as therapy to abort or prevent vascular headache, e.g., migraine, migraine variants, or so called "histaminic cephalalgia".
Structured Indications
PharmacodynamicsErgotamine 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 actionErgotamine 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.
TargetKindPharmacological actionActionsOrganismUniProt ID
5-hydroxytryptamine receptor 1DProteinyes
agonist
HumanP28221 details
5-hydroxytryptamine receptor 1BProteinyes
agonist
HumanP28222 details
5-hydroxytryptamine receptor 2AProteinyes
agonist
HumanP28223 details
D(2) dopamine receptorProteinunknown
agonist
HumanP14416 details
Alpha-1A adrenergic receptorProteinyes
partial agonist
HumanP35348 details
Alpha-1B adrenergic receptorProteinyes
partial agonist
HumanP35368 details
Alpha-1D adrenergic receptorProteinyes
partial agonist
HumanP25100 details
Alpha-2A adrenergic receptorProteinunknown
partial agonist
HumanP08913 details
Alpha-2B adrenergic receptorProteinunknown
agonist
partial agonist
HumanP18089 details
Sodium-dependent noradrenaline transporterProteinunknown
inhibitor
HumanP23975 details
D(1) dopamine receptorProtein groupunknown
agonist
Humannot applicabledetails
5-hydroxytryptamine receptor 1AProteinunknown
agonist
HumanP08908 details
5-hydroxytryptamine receptor 1FProteinunknown
agonist
HumanP30939 details
5-hydroxytryptamine receptor 2CProteinunknown
agonist
HumanP28335 details
Related Articles
AbsorptionThe bioavailability of sublingually administered ergotamine has not been determined.
Volume of distributionNot Available
Protein bindingNot 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 eliminationNot Available
Half life2 hours
ClearanceNot Available
ToxicitySigns 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
PathwaysNot Available
SNP Mediated EffectsNot Available
SNP Mediated Adverse Drug ReactionsNot Available
Interactions
Drug Interactions
DrugInteractionDrug group
1,10-PhenanthrolineThe serum concentration of Ergotamine can be increased when it is combined with 1,10-Phenanthroline.Experimental
3,4-DichloroisocoumarinThe serum concentration of Ergotamine can be increased when it is combined with 3,4-Dichloroisocoumarin.Experimental
4-(2-AMINOETHYL)BENZENESULFONYL FLUORIDEThe serum concentration of Ergotamine can be increased when it is combined with 4-(2-AMINOETHYL)BENZENESULFONYL FLUORIDE.Experimental
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
AcepromazineThe risk or severity of adverse effects can be increased when Ergotamine is combined with Acepromazine.Approved, Vet Approved
AceprometazineThe risk or severity of adverse effects can be increased when Ergotamine is combined with Aceprometazine.Approved
AcetaminophenThe serum concentration of Acetaminophen can be increased when it is combined with Ergotamine.Approved
AcetophenazineThe risk or severity of adverse effects can be increased when Ergotamine is combined with Acetophenazine.Approved
Acetylsalicylic acidThe serum concentration of Acetylsalicylic acid can be increased when it is combined with Ergotamine.Approved, Vet Approved
AdrafinilErgotamine may increase the hypertensive activities of Adrafinil.Withdrawn
AfatinibThe serum concentration of Afatinib can be increased when it is combined with Ergotamine.Approved
AldosteroneThe serum concentration of Aldosterone can be increased when it is combined with Ergotamine.Experimental
AlfuzosinAlfuzosin may decrease the vasoconstricting activities of Ergotamine.Approved, Investigational
AlitretinoinThe serum concentration of Alitretinoin can be increased when it is combined with Ergotamine.Approved, Investigational
AlmotriptanErgotamine may increase the vasoconstricting activities of Almotriptan.Approved, Investigational
AlogliptinThe serum concentration of Ergotamine can be increased when it is combined with Alogliptin.Approved
Alpha-1-proteinase inhibitorThe serum concentration of Ergotamine can be increased when it is combined with Alpha-1-proteinase inhibitor.Approved
AlprenololErgotamine may increase the atrioventricular blocking (AV block) activities of Alprenolol.Approved, Withdrawn
AmbrisentanThe serum concentration of Ambrisentan can be increased when it is combined with Ergotamine.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
AmisulprideThe risk or severity of adverse effects can be increased when Ergotamine is combined with Amisulpride.Approved, Investigational
AmitrazErgotamine may increase the hypertensive activities of Amitraz.Vet Approved
AmitriptylineAmitriptyline may decrease the antihypertensive activities of Ergotamine.Approved
AmoxapineThe risk or severity of adverse effects can be increased when Amoxapine is combined with Ergotamine.Approved
AmperozideThe risk or severity of adverse effects can be increased when Ergotamine is combined with Amperozide.Experimental
AmprenavirThe serum concentration of Ergotamine can be increased when it is combined with Amprenavir.Approved
AnisodamineErgotamine may increase the hypertensive activities of Anisodamine.Investigational
Antithrombin III humanThe serum concentration of Ergotamine can be increased when it is combined with Antithrombin III human.Approved
Aop200704Ergotamine may increase the atrioventricular blocking (AV block) activities of Aop200704.Investigational
ApixabanThe serum concentration of Ergotamine can be increased when it is combined with Apixaban.Approved
ApomorphineErgotamine may increase the vasoconstricting activities of Apomorphine.Approved, Investigational
ApraclonidineErgotamine may increase the hypertensive activities of Apraclonidine.Approved
AprepitantThe serum concentration of Ergotamine can be increased when it is combined with Aprepitant.Approved, Investigational
AprotininThe serum concentration of Ergotamine can be increased when it is combined with Aprotinin.Approved, Withdrawn
ArbutamineErgotamine may increase the hypertensive activities of Arbutamine.Approved
ArformoterolErgotamine may increase the hypertensive activities of Arformoterol.Approved, Investigational
ArgatrobanThe serum concentration of Ergotamine can be increased when it is combined with Argatroban.Approved, Investigational
AripiprazoleThe risk or severity of adverse effects can be increased when Ergotamine is combined with Aripiprazole.Approved, Investigational
ArotinololErgotamine may increase the atrioventricular blocking (AV block) activities of Arotinolol.Approved
Arsenic trioxideThe serum concentration of Arsenic trioxide can be increased when it is combined with Ergotamine.Approved, Investigational
AsenapineThe risk or severity of adverse effects can be increased when Ergotamine is combined with Asenapine.Approved
AsunaprevirThe serum concentration of Ergotamine can be increased when it is combined with Asunaprevir.Approved, Investigational
AtazanavirThe serum concentration of Ergotamine can be increased when it is 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
AxitinibThe serum concentration of Axitinib can be increased when it is combined with Ergotamine.Approved, Investigational
AzaperoneThe risk or severity of adverse effects can be increased when Ergotamine is combined with Azaperone.Vet Approved
AzithromycinThe metabolism of Ergotamine can be decreased when combined with Azithromycin.Approved
BatimastatThe serum concentration of Ergotamine can be increased when it is combined with Batimastat.Experimental
BefunololErgotamine may increase the hypertensive activities of Befunolol.Experimental
BenazeprilThe serum concentration of Ergotamine can be increased when it is combined with Benazepril.Approved, Investigational
BenmoxinBenmoxin may increase the hypertensive activities of Ergotamine.Withdrawn
BenperidolThe risk or severity of adverse effects can be increased when Ergotamine is combined with Benperidol.Investigational
BenzamidineThe serum concentration of Ergotamine can be increased when it is combined with Benzamidine.Experimental
Benzylpenicilloyl PolylysineErgotamine may decrease effectiveness of Benzylpenicilloyl Polylysine as a diagnostic agent.Approved
BetamethasoneThe serum concentration of Betamethasone can be increased when it is combined with Ergotamine.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
BexaroteneThe serum concentration of Ergotamine can be decreased when it is combined with Bexarotene.Approved, Investigational
Bi201335The serum concentration of Ergotamine can be increased when it is combined with Bi201335.Investigational
BifeprunoxThe risk or severity of adverse effects can be increased when Ergotamine is combined with Bifeprunox.Investigational
BisoprololErgotamine may increase the atrioventricular blocking (AV block) activities of Bisoprolol.Approved
BitolterolErgotamine may increase the hypertensive activities of Bitolterol.Withdrawn
BivalirudinThe serum concentration of Ergotamine can be increased when it is combined with Bivalirudin.Approved, Investigational
BoceprevirThe serum concentration of Ergotamine can be increased when it is combined with Boceprevir.Approved
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
BrexpiprazoleThe risk or severity of adverse effects can be increased when Ergotamine is combined with Brexpiprazole.Approved
BrimonidineErgotamine may increase the hypertensive activities of Brimonidine.Approved
BromocriptineBromocriptine may increase the hypertensive activities of Ergotamine.Approved, Investigational
BromperidolThe risk or severity of adverse effects can be increased when Ergotamine is combined with Bromperidol.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
BupranololErgotamine may increase the atrioventricular blocking (AV block) activities of Bupranolol.Approved
BuspironeThe risk or severity of adverse effects can be increased when Buspirone is combined with Ergotamine.Approved, Investigational
CabazitaxelThe serum concentration of Cabazitaxel can be increased when it is combined with Ergotamine.Approved
CabergolineCabergoline may increase the hypertensive activities of Ergotamine.Approved
CaffeineThe serum concentration of Caffeine can be increased when it is combined with Ergotamine.Approved
CamptothecinThe serum concentration of Camptothecin can be increased when it is combined with Ergotamine.Experimental
CanagliflozinThe serum concentration of Canagliflozin can be increased when it is combined with Ergotamine.Approved
CandoxatrilThe serum concentration of Ergotamine can be increased when it is combined with Candoxatril.Experimental
CandoxatrilatThe serum concentration of Ergotamine can be increased when it is combined with Candoxatrilat.Experimental
CaptoprilThe serum concentration of Ergotamine can be increased when it is combined with Captopril.Approved
CarbamazepineThe metabolism of Ergotamine can be increased when combined with Carbamazepine.Approved, Investigational
CarbomycinThe serum concentration of Ergotamine can be increased when it is combined with Carbomycin.Vet Approved
Carboprost TromethamineThe risk or severity of adverse effects can be increased when Carboprost Tromethamine is combined with Ergotamine.Approved
CarfilzomibThe serum concentration of Carfilzomib can be increased when it is combined with Ergotamine.Approved
CariprazineThe risk or severity of adverse effects can be increased when Ergotamine is combined with Cariprazine.Approved
CaroxazoneCaroxazone may increase the hypertensive activities of Ergotamine.Withdrawn
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
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
ChlorpromazineThe serum concentration of Chlorpromazine can be increased when it is combined with Ergotamine.Approved, Vet Approved
ChlorprothixeneThe risk or severity of adverse effects can be increased when Ergotamine is combined with Chlorprothixene.Approved, Withdrawn
ChymostatinThe serum concentration of Ergotamine can be increased when it is combined with Chymostatin.Experimental
CilastatinThe serum concentration of Ergotamine can be increased when it is combined with Cilastatin.Approved
CilazaprilThe serum concentration of Ergotamine can be increased when it is combined with Cilazapril.Approved
CimetidineThe serum concentration of Cimetidine can be increased when it is combined with Ergotamine.Approved
CiprofloxacinThe serum concentration of Ciprofloxacin can be increased when it is combined with Ergotamine.Approved, Investigational
CirazolineErgotamine may increase the hypertensive activities of Cirazoline.Experimental
CisplatinThe serum concentration of Cisplatin can be increased when it is combined with Ergotamine.Approved
CitalopramThe risk or severity of adverse effects can be increased when Citalopram is combined with Ergotamine.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
ClenbuterolErgotamine may increase the hypertensive activities of Clenbuterol.Approved, Vet Approved
ClobazamThe serum concentration of Clobazam can be increased when it is combined with Ergotamine.Approved, Illicit
ClomifeneThe serum concentration of Clomifene can be increased when it is combined with Ergotamine.Approved, Investigational
ClomipramineClomipramine may decrease the antihypertensive activities of Ergotamine.Approved, Vet Approved
ClonidineErgotamine may increase the hypertensive activities of Clonidine.Approved
ClopidogrelThe serum concentration of Clopidogrel can be increased when it is combined with Ergotamine.Approved, Nutraceutical
ClotrimazoleThe metabolism of Ergotamine can be decreased when combined with Clotrimazole.Approved, Vet Approved
ClozapineThe serum concentration of Clozapine can be increased when it is combined with Ergotamine.Approved
CobicistatThe serum concentration of Ergotamine can be increased when it is combined with Cobicistat.Approved
CobimetinibThe serum concentration of Cobimetinib can be increased when it is combined with Ergotamine.Approved
ColchicineThe serum concentration of Colchicine can be increased when it is combined with Ergotamine.Approved
ConivaptanThe serum concentration of Ergotamine can be increased when it is combined with Conivaptan.Approved, Investigational
Conjugated Equine EstrogensThe serum concentration of Conjugated Equine Estrogens can be increased when it is combined with Ergotamine.Approved
CrizotinibThe serum concentration of Ergotamine can be increased when it is combined with Crizotinib.Approved
CyamemazineThe risk or severity of adverse effects can be increased when Ergotamine is combined with Cyamemazine.Approved
CyclobenzaprineCyclobenzaprine may decrease the antihypertensive activities of Ergotamine.Approved
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
DactinomycinThe serum concentration of Dactinomycin can be increased when it is combined with Ergotamine.Approved
DapagliflozinThe serum concentration of Dapagliflozin can be increased when it is combined with Ergotamine.Approved
DapiprazoleThe risk or severity of adverse effects can be increased when Ergotamine is combined with Dapiprazole.Approved
DapoxetineThe risk or severity of adverse effects can be increased when Dapoxetine is combined with Ergotamine.Investigational
DarunavirThe serum concentration of Ergotamine can be increased when it is combined with Darunavir.Approved
DasatinibThe serum concentration of Ergotamine can be increased when it is combined with Dasatinib.Approved, Investigational
DaunorubicinThe serum concentration of Daunorubicin can be increased when it is combined with Ergotamine.Approved
DebrisoquinThe serum concentration of Debrisoquin can be increased when it is combined with Ergotamine.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
DesvenlafaxineThe risk or severity of adverse effects can be increased when Ergotamine is combined with Desvenlafaxine.Approved
DetomidineErgotamine may increase the hypertensive activities of Detomidine.Vet Approved
DexamethasoneThe serum concentration of Ergotamine can be decreased when it is combined with Dexamethasone.Approved, Investigational, Vet Approved
DexmedetomidineErgotamine may increase the hypertensive activities of Dexmedetomidine.Approved, Vet Approved
DextromethorphanThe risk or severity of adverse effects can be increased when Dextromethorphan is combined with Ergotamine.Approved
DiazepamThe serum concentration of Diazepam can be increased when it is combined with Ergotamine.Approved, Illicit, Vet Approved
DiethylstilbestrolThe serum concentration of Diethylstilbestrol can be increased when it is combined with Ergotamine.Approved
DigitoxinThe serum concentration of Digitoxin can be increased when it is combined with Ergotamine.Approved
DigoxinThe serum concentration of Digoxin can be increased when it is combined with Ergotamine.Approved
DihydroergotamineDihydroergotamine may increase the hypertensive activities of Ergotamine.Approved
DihydrotestosteroneThe serum concentration of Dihydrotestosterone can be increased when it is combined with Ergotamine.Illicit
DiltiazemThe metabolism of Ergotamine can be decreased when combined with Diltiazem.Approved
DipivefrinErgotamine may increase the hypertensive activities of Dipivefrin.Approved
DipyridamoleThe serum concentration of Dipyridamole can be increased when it is combined with Ergotamine.Approved
DobutamineErgotamine may increase the hypertensive activities of Dobutamine.Approved
DocetaxelThe serum concentration of Docetaxel can be increased when it is combined with Ergotamine.Approved, Investigational
DolasetronDolasetron may increase the serotonergic activities of Ergotamine.Approved
DomperidoneThe serum concentration of Domperidone can be increased when it is combined with Ergotamine.Approved, Investigational, Vet Approved
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
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
DroperidolThe risk or severity of adverse effects can be increased when Ergotamine is combined with Droperidol.Approved, Vet Approved
DroxidopaErgotamine may increase the hypertensive activities of Droxidopa.Approved, Investigational
DuloxetineThe risk or severity of adverse effects can be increased when Duloxetine is combined with Ergotamine.Approved
EcabetThe serum concentration of Ergotamine can be increased when it is combined with Ecabet.Approved, Investigational
EcopipamThe risk or severity of adverse effects can be increased when Ergotamine is combined with Ecopipam.Investigational
EdoxabanThe serum concentration of Edoxaban can be increased when it is combined with Ergotamine.Approved
EfavirenzThe serum concentration of Ergotamine can be decreased when it is combined with Efavirenz.Approved, Investigational
ElafinThe serum concentration of Ergotamine can be increased when it is combined with Elafin.Investigational
EletriptanErgotamine may increase the vasoconstricting activities of Eletriptan.Approved, Investigational
EnalaprilThe serum concentration of Ergotamine can be increased when it is combined with Enalapril.Approved, Vet Approved
EnalaprilatThe serum concentration of Ergotamine can be increased when it is combined with Enalaprilat.Approved
EnalkirenThe serum concentration of Ergotamine can be increased when it is combined with Enalkiren.Experimental
EnzalutamideThe serum concentration of Ergotamine can be decreased when it is combined with Enzalutamide.Approved
EphedrineErgotamine may increase the hypertensive activities of Ephedrine.Approved
EpinastineThe serum concentration of Epinastine can be increased when it is combined with Ergotamine.Approved, Investigational
EpinephrineErgotamine may increase the hypertensive activities of Epinephrine.Approved, Vet Approved
Ergoloid mesylateErgoloid mesylate may increase the vasoconstricting activities of Ergotamine.Approved
ErgonovineErgonovine may increase the hypertensive activities of Ergotamine.Approved
ErlotinibThe serum concentration of Erlotinib can be increased when it is combined with Ergotamine.Approved, Investigational
ErythromycinThe serum concentration of Ergotamine can be increased when it is combined with Erythromycin.Approved, Vet Approved
EscitalopramThe risk or severity of adverse effects can be increased when Ergotamine is combined with Escitalopram.Approved, Investigational
Eslicarbazepine acetateThe serum concentration of Ergotamine can be decreased when it is combined with Eslicarbazepine acetate.Approved
EsmirtazapineEsmirtazapine may decrease the antihypertensive activities of Ergotamine.Investigational
EsmololErgotamine may increase the atrioventricular blocking (AV block) activities of Esmolol.Approved
EstradiolThe serum concentration of Estradiol can be increased when it is combined with Ergotamine.Approved, Investigational, Vet Approved
EstriolThe serum concentration of Estriol can be increased when it is combined with Ergotamine.Approved, Vet Approved
EstroneThe serum concentration of Estrone can be increased when it is combined with Ergotamine.Approved
Ethinyl EstradiolThe serum concentration of Ethinyl Estradiol can be increased when it is combined with Ergotamine.Approved
EtilefrineErgotamine may increase the hypertensive activities of Etilefrine.Withdrawn
EtoposideThe serum concentration of Etoposide can be increased when it is combined with Ergotamine.Approved
EtravirineThe serum concentration of Ergotamine can be decreased when it is combined with Etravirine.Approved
EverolimusThe serum concentration of Everolimus can be increased when it is combined with Ergotamine.Approved
EzetimibeThe serum concentration of Ezetimibe can be increased when it is combined with Ergotamine.Approved
FencamfamineThe risk or severity of adverse effects can be increased when Ergotamine is combined with Fencamfamine.Approved, Illicit, Withdrawn
FenoterolErgotamine may increase the hypertensive activities of Fenoterol.Approved
FentanylThe serum concentration of Fentanyl can be decreased when it is combined with Ergotamine.Approved, Illicit, Investigational, Vet Approved
FesoterodineThe serum concentration of Fesoterodine can be increased when it is combined with Ergotamine.Approved
FexofenadineThe serum concentration of Fexofenadine can be increased when it is combined with Ergotamine.Approved
FidaxomicinThe serum concentration of Fidaxomicin can be increased when it is combined with Ergotamine.Approved
FluconazoleThe metabolism of Ergotamine can be decreased when combined with Fluconazole.Approved
FluoxetineThe risk or severity of adverse effects can be increased when Fluoxetine is combined with Ergotamine.Approved, Vet Approved
FlupentixolThe risk or severity of adverse effects can be increased when Ergotamine is combined with Flupentixol.Approved, Withdrawn
FluphenazineThe risk or severity of adverse effects can be increased when Ergotamine is combined with Fluphenazine.Approved
FluspirileneThe risk or severity of adverse effects can be increased when Ergotamine is combined with Fluspirilene.Approved
Fluticasone furoateThe serum concentration of Fluticasone furoate can be increased when it is combined with Ergotamine.Approved
FluvoxamineThe metabolism of Ergotamine can be decreased when combined with Fluvoxamine.Approved, Investigational
FormoterolErgotamine may increase the hypertensive activities of Formoterol.Approved, Investigational
FosamprenavirThe serum concentration of Ergotamine can be increased when it is combined with Fosamprenavir.Approved
FosaprepitantThe serum concentration of Ergotamine can be increased when it is combined with Fosaprepitant.Approved
FosinoprilThe serum concentration of Ergotamine can be increased when it is combined with Fosinopril.Approved
FosphenytoinThe metabolism of Ergotamine can be increased when combined with Fosphenytoin.Approved
FrovatriptanErgotamine may increase the vasoconstricting activities of Frovatriptan.Approved, Investigational
FurazolidoneFurazolidone may increase the hypertensive activities of Ergotamine.Approved, Vet Approved
Fusidic AcidThe serum concentration of Ergotamine can be increased when it is combined with Fusidic Acid.Approved
GabexateThe serum concentration of Ergotamine can be increased when it is combined with Gabexate.Investigational
GefitinibThe serum concentration of Gefitinib can be increased when it is combined with Ergotamine.Approved, Investigational
GeldanamycinThe serum concentration of Ergotamine can be increased when it is combined with Geldanamycin.Experimental
GemcitabineThe serum concentration of Gemcitabine can be increased when it is combined with Ergotamine.Approved
GM6001The serum concentration of Ergotamine can be increased when it is combined with GM6001.Experimental
GranisetronGranisetron may increase the serotonergic activities of Ergotamine.Approved, Investigational
GrazoprevirThe serum concentration of Grazoprevir can be increased when it is combined with Ergotamine.Approved
GrepafloxacinThe serum concentration of Grepafloxacin can be increased when it is combined with Ergotamine.Withdrawn
GuanabenzErgotamine may increase the hypertensive activities of Guanabenz.Approved
GuanfacineErgotamine may increase the hypertensive activities of Guanfacine.Approved, Investigational
HaloperidolThe serum concentration of Haloperidol can be increased when it is combined with Ergotamine.Approved
HexoprenalineErgotamine may increase the hypertensive activities of Hexoprenaline.Approved, Withdrawn
HigenamineErgotamine may increase the hypertensive activities of Higenamine.Investigational
HirulogThe serum concentration of Ergotamine can be increased when it is combined with Hirulog.Experimental
HyaluronidaseHyaluronidase may increase the vasoconstricting activities of Ergotamine.Approved, Investigational
HydracarbazineHydracarbazine may increase the hypertensive activities of Ergotamine.Approved
HydrocortisoneThe serum concentration of Hydrocortisone can be increased when it is combined with Ergotamine.Approved, Vet Approved
IbuprofenThe serum concentration of Ibuprofen can be increased when it is combined with Ergotamine.Approved
IdelalisibThe serum concentration of Ergotamine can be increased when it is combined with Idelalisib.Approved
idraparinuxThe serum concentration of Ergotamine can be increased when it is combined with idraparinux.Investigational
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
ImidaprilThe serum concentration of Ergotamine can be increased when it is combined with Imidapril.Investigational
ImipramineImipramine may decrease the antihypertensive activities of Ergotamine.Approved
IndacaterolThe serum concentration of Indacaterol can be increased when it is combined with Ergotamine.Approved
IndenololErgotamine may increase the atrioventricular blocking (AV block) activities of Indenolol.Withdrawn
IndinavirThe serum concentration of Ergotamine can be increased when it is combined with Indinavir.Approved
IndomethacinThe serum concentration of Indomethacin can be increased when it is combined with Ergotamine.Approved, 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
IproclozideIproclozide may increase the hypertensive activities of Ergotamine.Withdrawn
IproniazidIproniazid may increase the hypertensive activities of Ergotamine.Withdrawn
IrinotecanThe serum concentration of Irinotecan can be increased when it is combined with Ergotamine.Approved, Investigational
IsavuconazoniumThe metabolism of Ergotamine can be decreased when combined with Isavuconazonium.Approved, Investigational
IsocarboxazidIsocarboxazid may increase the hypertensive activities of Ergotamine.Approved
IsoetarineErgotamine may increase the hypertensive activities of Isoetarine.Approved
IsoflurophateThe serum concentration of Ergotamine can be increased when it is combined with Isoflurophate.Approved, Withdrawn
IsoprenalineErgotamine may increase the hypertensive activities of Isoprenaline.Approved
IsoxsuprineErgotamine may increase the hypertensive activities of Isoxsuprine.Approved, Withdrawn
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
IvermectinThe serum concentration of Ivermectin can be increased when it is combined with Ergotamine.Approved, Vet Approved
IxazomibThe serum concentration of Ergotamine can be increased when it is combined with Ixazomib.Approved
JosamycinThe serum concentration of Ergotamine can be increased when it is combined with Josamycin.Approved
KetazolamThe serum concentration of Ketazolam can be increased when it is combined with Ergotamine.Approved
KetoconazoleThe serum concentration of Ergotamine can be increased when it is combined with Ketoconazole.Approved, Investigational
KetoconazoleThe metabolism of Ergotamine can be decreased when combined with Ketoconazole.Approved, Investigational
KitasamycinThe serum concentration of Ergotamine can be increased when it is combined with Kitasamycin.Experimental
LabetalolErgotamine may increase the atrioventricular blocking (AV block) activities of Labetalol.Approved
LamivudineThe serum concentration of Lamivudine can be increased when it is combined with Ergotamine.Approved, Investigational
LamotrigineThe serum concentration of Lamotrigine can be increased when it is combined with Ergotamine.Approved, Investigational
LansoprazoleThe serum concentration of Lansoprazole can be increased when it is combined with Ergotamine.Approved, Investigational
LedipasvirThe serum concentration of Ledipasvir can be increased when it is combined with Ergotamine.Approved
LenalidomideThe serum concentration of Lenalidomide can be increased when it is combined with Ergotamine.Approved
LenvatinibThe serum concentration of Lenvatinib can be increased when it is combined with Ergotamine.Approved
LepirudinThe serum concentration of Ergotamine can be increased when it is combined with Lepirudin.Approved
LevetiracetamThe serum concentration of Levetiracetam can be increased when it is combined with Ergotamine.Approved, Investigational
LevobunololLevobunolol may increase the vasoconstricting activities of Ergotamine.Approved
LevofloxacinThe serum concentration of Levofloxacin can be increased when it is combined with Ergotamine.Approved, Investigational
LevomilnacipranThe risk or severity of adverse effects can be increased when Ergotamine is combined with Levomilnacipran.Approved
LidocaineThe metabolism of Ergotamine can be decreased when combined with Lidocaine.Approved, Vet Approved
LinagliptinThe serum concentration of Ergotamine can be increased when it is combined with Linagliptin.Approved
LinezolidThe risk or severity of adverse effects can be increased when Linezolid is combined with Ergotamine.Approved, Investigational
LisinoprilThe serum concentration of Ergotamine can be increased when it is combined with Lisinopril.Approved, Investigational
LisurideErgotamine may increase the vasoconstricting activities of Lisuride.Approved
LithiumThe risk or severity of adverse effects can be increased when Ergotamine is combined with Lithium.Approved
LofexidineErgotamine may increase the hypertensive activities of Lofexidine.Approved, Investigational
LoperamideThe serum concentration of Loperamide can be increased when it is combined with Ergotamine.Approved
LopinavirThe serum concentration of Ergotamine can be increased when it is combined with Lopinavir.Approved
LorcaserinThe risk or severity of adverse effects can be increased when Lorcaserin is combined with Ergotamine.Approved
LosartanThe serum concentration of Losartan can be increased when it is combined with Ergotamine.Approved
LovastatinThe metabolism of Ergotamine can be decreased when combined with Lovastatin.Approved, Investigational
LoxapineThe risk or severity of adverse effects can be increased when Ergotamine is combined with Loxapine.Approved
Lu AA21004Ergotamine may increase the vasoconstricting activities of Lu AA21004.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
MannitolThe serum concentration of Mannitol can be increased when it is combined with Ergotamine.Approved, Investigational
MaprotilineThe risk or severity of adverse effects can be increased when Ergotamine is combined with Maprotiline.Approved
MebanazineMebanazine may increase the hypertensive activities of Ergotamine.Withdrawn
MedetomidineErgotamine may increase the hypertensive activities of Medetomidine.Vet Approved
MelperoneThe risk or severity of adverse effects can be increased when Ergotamine is combined with Melperone.Approved
MephentermineErgotamine may increase the hypertensive activities of Mephentermine.Approved
MesoridazineThe risk or severity of adverse effects can be increased when Ergotamine is combined with Mesoridazine.Approved
MetaraminolErgotamine may increase the hypertensive activities of Metaraminol.Approved, Investigational
MethadoneThe risk or severity of adverse effects can be increased when Methadone is combined with Ergotamine.Approved
MethotrexateThe serum concentration of Methotrexate can be increased when it is combined with Ergotamine.Approved
MethotrimeprazineThe risk or severity of adverse effects can be increased when Ergotamine is combined with Methotrimeprazine.Approved
MethoxamineErgotamine may increase the hypertensive activities of Methoxamine.Approved
MethyldopaErgotamine may increase the hypertensive activities of Methyldopa.Approved
Methylene blueMethylene blue may increase the hypertensive activities of Ergotamine.Investigational
MethylprednisoloneThe serum concentration of Methylprednisolone can be increased when it is combined with Ergotamine.Approved, Vet Approved
MetipranololMetipranolol may increase the vasoconstricting activities of Ergotamine.Approved
MetoclopramideThe risk or severity of adverse effects can be increased when Ergotamine is combined with Metoclopramide.Approved, Investigational
MetoprololErgotamine may increase the atrioventricular blocking (AV block) activities of Metoprolol.Approved, Investigational
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
MidazolamThe serum concentration of Midazolam can be increased when it is combined with Ergotamine.Approved, Illicit
MidodrineErgotamine may increase the hypertensive activities of Midodrine.Approved
MifepristoneThe serum concentration of Ergotamine can be increased when it is combined with Mifepristone.Approved, Investigational
MilnacipranThe risk or severity of adverse effects can be increased when Ergotamine is combined with Milnacipran.Approved
MinaprineMinaprine may increase the hypertensive activities of Ergotamine.Approved
MirabegronErgotamine may increase the hypertensive activities of Mirabegron.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 serum concentration of Mitoxantrone can be increased when it is combined with Ergotamine.Approved, Investigational
MoclobemideMoclobemide may increase the hypertensive activities of Ergotamine.Approved
ModafinilThe serum concentration of Ergotamine can be decreased when it is combined with Modafinil.Approved, Investigational
MoexiprilThe serum concentration of Ergotamine can be increased when it is combined with Moexipril.Approved
MolindoneThe risk or severity of adverse effects can be increased when Ergotamine is combined with Molindone.Approved
MorphineThe serum concentration of Morphine can be increased when it is combined with Ergotamine.Approved, Investigational
Mycophenolate mofetilThe serum concentration of Mycophenolate mofetil can be increased when it is combined with Ergotamine.Approved, Investigational
N-(3-Propylcarbamoyloxirane-2-Carbonyl)-Isoleucyl-ProlineThe serum concentration of Ergotamine can be increased when it is combined with N-(3-Propylcarbamoyloxirane-2-Carbonyl)-Isoleucyl-Proline.Experimental
NadololErgotamine may increase the atrioventricular blocking (AV block) activities of Nadolol.Approved
NafamostatThe serum concentration of Ergotamine can be increased when it is combined with Nafamostat.Investigational
NafcillinThe serum concentration of Ergotamine can be decreased when it is combined with Nafcillin.Approved
NaloxegolThe serum concentration of Naloxegol can be increased when it is combined with Ergotamine.Approved
NaloxoneThe serum concentration of Naloxone can be increased when it is combined with Ergotamine.Approved, Vet Approved
NaphazolineErgotamine may increase the hypertensive activities of Naphazoline.Approved
NaratriptanErgotamine may increase the vasoconstricting activities of Naratriptan.Approved, Investigational
NCX 4016The serum concentration of Ergotamine can be increased when it is combined with NCX 4016.Investigational
NebivololErgotamine may increase the hypertensive activities of Nebivolol.Approved, Investigational
NefazodoneThe metabolism of Ergotamine can be decreased when combined with Nefazodone.Approved, Withdrawn
NelfinavirThe serum concentration of Ergotamine can be increased when it is 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 serum concentration of Nicardipine can be increased when it is combined with Ergotamine.Approved
NifedipineThe serum concentration of Nifedipine can be increased when it is combined with Ergotamine.Approved
NilotinibThe metabolism of Ergotamine can be decreased when combined with Nilotinib.Approved, Investigational
NintedanibThe serum concentration of Nintedanib can be increased when it is combined with Ergotamine.Approved
NitroaspirinThe serum concentration of Ergotamine can be increased when it is combined with Nitroaspirin.Investigational
NitroglycerinErgotamine may decrease the vasodilatory activities of Nitroglycerin.Approved, Investigational
NizatidineThe serum concentration of Nizatidine can be increased when it is combined with Ergotamine.Approved
NorepinephrineErgotamine may increase the hypertensive activities of Norepinephrine.Approved
NortriptylineNortriptyline may decrease the antihypertensive activities of Ergotamine.Approved
NylidrinErgotamine may increase the hypertensive activities of Nylidrin.Approved
OctamoxinOctamoxin may increase the hypertensive activities of Ergotamine.Withdrawn
OlanzapineThe serum concentration of Olanzapine can be increased when it is combined with Ergotamine.Approved, Investigational
OlaparibThe metabolism of Ergotamine can be decreased when combined with Olaparib.Approved
OleandomycinThe serum concentration of Ergotamine can be increased when it is combined with Oleandomycin.Vet Approved
OlodaterolErgotamine may increase the hypertensive activities of Olodaterol.Approved
OmapatrilatThe serum concentration of Ergotamine can be increased when it is combined with Omapatrilat.Investigational
OmbitasvirThe serum concentration of Ombitasvir can be increased when it is combined with Ergotamine.Approved
OndansetronOndansetron may increase the serotonergic activities of Ergotamine.Approved
OpipramolOpipramol may decrease the antihypertensive activities of Ergotamine.Investigational
OrciprenalineErgotamine may increase the hypertensive activities of Orciprenaline.Approved
OsanetantThe risk or severity of adverse effects can be increased when Ergotamine is combined with Osanetant.Investigational
OsimertinibThe serum concentration of Ergotamine can be increased when it is combined with Osimertinib.Approved
OtamixabanThe serum concentration of Ergotamine can be increased when it is combined with Otamixaban.Investigational
OxprenololErgotamine may increase the atrioventricular blocking (AV block) activities of Oxprenolol.Approved
OxymetazolineErgotamine may increase the hypertensive activities of Oxymetazoline.Approved
PaclitaxelThe serum concentration of Paclitaxel can be increased when it is combined with Ergotamine.Approved, Vet Approved
PalbociclibThe serum concentration of Ergotamine can be increased when it is combined with Palbociclib.Approved
PaliperidoneThe risk or severity of adverse effects can be increased when Ergotamine is combined with Paliperidone.Approved
PalonosetronPalonosetron may increase the serotonergic activities of Ergotamine.Approved, Investigational
PanobinostatThe serum concentration of Panobinostat can be increased when it is combined with Ergotamine.Approved, Investigational
PargylinePargyline may increase the hypertensive activities of Ergotamine.Approved
ParoxetineThe risk or severity of adverse effects can be increased when Ergotamine is combined with Paroxetine.Approved, Investigational
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
PerazineThe risk or severity of adverse effects can be increased when Ergotamine is combined with Perazine.Investigational
PergolideErgotamine may increase the vasoconstricting activities of Pergolide.Approved, Vet Approved, Withdrawn
PerindoprilThe serum concentration of Ergotamine can be increased when it is combined with Perindopril.Approved
PerospironeThe risk or severity of adverse effects can be increased when Ergotamine is combined with Perospirone.Approved
PerphenazineThe risk or severity of adverse effects can be increased when Ergotamine is combined with Perphenazine.Approved
PethidineThe risk or severity of adverse effects can be increased when Pethidine is combined with Ergotamine.Approved
PhenelzinePhenelzine may increase the hypertensive activities of Ergotamine.Approved
PheniprazinePheniprazine may increase the hypertensive activities of Ergotamine.Withdrawn
PhenobarbitalThe metabolism of Ergotamine can be increased when combined with Phenobarbital.Approved
PhenoxypropazinePhenoxypropazine may increase the hypertensive activities of Ergotamine.Withdrawn
PhenylephrineErgotamine may increase the hypertensive activities of Phenylephrine.Approved
PhenylpropanolamineErgotamine may increase the hypertensive activities of Phenylpropanolamine.Approved, Vet Approved, Withdrawn
PhenytoinThe metabolism of Ergotamine can be increased when combined with Phenytoin.Approved, Vet Approved
PhosphoramidonThe serum concentration of Ergotamine can be increased when it is combined with Phosphoramidon.Experimental
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
PipamperoneThe risk or severity of adverse effects can be increased when Ergotamine is combined with Pipamperone.Approved
PipotiazineThe risk or severity of adverse effects can be increased when Ergotamine is combined with Pipotiazine.Approved
PirbuterolErgotamine may increase the hypertensive activities of Pirbuterol.Approved
PirlindolePirlindole may increase the hypertensive activities of Ergotamine.Approved
PitavastatinThe serum concentration of Pitavastatin can be increased when it is combined with Ergotamine.Approved
PivhydrazinePivhydrazine may increase the hypertensive activities of Ergotamine.Withdrawn
PomalidomideThe serum concentration of Pomalidomide can be increased when it is combined with Ergotamine.Approved
PonatinibThe serum concentration of Ponatinib can be increased when it is combined with Ergotamine.Approved
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
PrazosinThe serum concentration of Prazosin can be increased when it is combined with Ergotamine.Approved
PrednisoloneThe serum concentration of Prednisolone can be increased when it is combined with Ergotamine.Approved, Vet Approved
PrednisoneThe serum concentration of Prednisone can be increased when it is combined with Ergotamine.Approved, Vet Approved
PrimidoneThe metabolism of Ergotamine can be increased when combined with Primidone.Approved, Vet Approved
PrinomastatThe serum concentration of Ergotamine can be increased when it is combined with Prinomastat.Investigational
ProcarbazineThe risk or severity of adverse effects can be increased when Ergotamine is combined with Procarbazine.Approved
ProcaterolErgotamine may increase the hypertensive activities of Procaterol.Approved
ProchlorperazineThe risk or severity of adverse effects can be increased when Ergotamine is combined with Prochlorperazine.Approved, Vet Approved
ProgesteroneThe serum concentration of Progesterone can be increased when it is combined with Ergotamine.Approved, Vet Approved
PromazineThe risk or severity of adverse effects can be increased when Ergotamine is combined with Promazine.Approved, Vet Approved
PromethazineThe risk or severity of adverse effects can be increased when Ergotamine is combined with Promethazine.Approved
PropericiazineThe risk or severity of adverse effects can be increased when Ergotamine is combined with Propericiazine.Approved
PropranololErgotamine may increase the atrioventricular blocking (AV block) activities of Propranolol.Approved, Investigational
ProthipendylThe risk or severity of adverse effects can be increased when Ergotamine is combined with Prothipendyl.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
PRX-00023Ergotamine may increase the vasoconstricting activities of PRX-00023.Investigational
PseudoephedrineErgotamine may increase the hypertensive activities of Pseudoephedrine.Approved
QuetiapineThe serum concentration of Quetiapine can be increased when it is combined with Ergotamine.Approved
QuinaprilThe serum concentration of Ergotamine can be increased when it is combined with Quinapril.Approved, Investigational
QuinidineThe serum concentration of Quinidine can be increased when it is combined with Ergotamine.Approved
QuinineThe serum concentration of Quinine can be increased when it is combined with Ergotamine.Approved
RacecadotrilThe serum concentration of Ergotamine can be increased when it is combined with Racecadotril.Investigational
RacepinephrineErgotamine may increase the hypertensive activities of Racepinephrine.Approved
RacloprideThe risk or severity of adverse effects can be increased when Ergotamine is combined with Raclopride.Investigational
RactopamineErgotamine may increase the hypertensive activities of Ractopamine.Vet Approved
RamiprilThe serum concentration of Ergotamine can be increased when it is combined with Ramipril.Approved
RanitidineThe serum concentration of Ranitidine can be increased when it is combined with Ergotamine.Approved
RanolazineThe serum concentration of Ranolazine can be increased when it is combined with Ergotamine.Approved, Investigational
RasagilineRasagiline may increase the hypertensive activities of Ergotamine.Approved
RemikirenThe serum concentration of Ergotamine can be increased when it is combined with Remikiren.Approved
RemoxiprideThe risk or severity of adverse effects can be increased when Ergotamine is combined with Remoxipride.Approved, Withdrawn
ReserpineThe serum concentration of Reserpine can be increased when it is combined with Ergotamine.Approved
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
RilmenidineErgotamine may increase the hypertensive activities of Rilmenidine.Investigational
RisperidoneThe serum concentration of Risperidone can be increased when it is combined with Ergotamine.Approved, Investigational
RitanserinThe risk or severity of adverse effects can be increased when Ergotamine is combined with Ritanserin.Investigational
RitobegronErgotamine may increase the hypertensive activities of Ritobegron.Investigational
RitodrineErgotamine may increase the hypertensive activities of Ritodrine.Approved
RitonavirThe serum concentration of Ergotamine can be increased when it is combined with Ritonavir.Approved, Investigational
RivaroxabanThe serum concentration of Ergotamine can be increased when it is combined with Rivaroxaban.Approved
RizatriptanErgotamine may increase the vasoconstricting activities of Rizatriptan.Approved
RomidepsinThe serum concentration of Romidepsin can be increased when it is combined with Ergotamine.Approved, Investigational
RomifidineErgotamine may increase the hypertensive activities of Romifidine.Vet Approved
RopiniroleErgotamine may increase the vasoconstricting activities of Ropinirole.Approved, Investigational
RoxithromycinThe serum concentration of Ergotamine can be increased when it is combined with Roxithromycin.Approved, Withdrawn
SafrazineSafrazine may increase the hypertensive activities of Ergotamine.Withdrawn
SalbutamolErgotamine may increase the hypertensive activities of Salbutamol.Approved, Vet Approved
Salicylic acidThe serum concentration of Salicylic acid can be increased when it is combined with Ergotamine.Approved, Vet Approved
SalmeterolErgotamine may increase the hypertensive activities of Salmeterol.Approved
SaquinavirThe serum concentration of Ergotamine can be increased when it is combined with Saquinavir.Approved, Investigational
SaxagliptinThe serum concentration of Ergotamine can be increased when it is combined with Saxagliptin.Approved
SelegilineSelegiline may increase the hypertensive activities of Ergotamine.Approved, Investigational, Vet Approved
SelexipagThe serum concentration of Selexipag can be increased when it is combined with Ergotamine.Approved
SertindoleThe risk or severity of adverse effects can be increased when Ergotamine is combined with Sertindole.Approved, Withdrawn
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
SitagliptinThe serum concentration of Ergotamine can be increased when it is combined with Sitagliptin.Approved, Investigational
SofosbuvirThe serum concentration of Sofosbuvir can be increased when it is combined with Ergotamine.Approved
SolabegronErgotamine may increase the hypertensive activities of Solabegron.Investigational
SolithromycinThe serum concentration of Ergotamine can be increased when it is combined with Solithromycin.Investigational
SorafenibThe serum concentration of Sorafenib can be increased when it is combined with Ergotamine.Approved, Investigational
SotalolErgotamine may increase the atrioventricular blocking (AV block) activities of Sotalol.Approved
SparfloxacinThe serum concentration of Sparfloxacin can be increased when it is combined with Ergotamine.Approved
SphingosineThe serum concentration of Sphingosine can be increased when it is combined with Ergotamine.Experimental
SpiraprilThe serum concentration of Ergotamine can be increased when it is combined with Spirapril.Approved
SpironolactoneSpironolactone may decrease the vasoconstricting activities of Ergotamine.Approved
SR 58611Ergotamine may increase the hypertensive activities of SR 58611.Investigational
St. John's WortThe serum concentration of Ergotamine can be decreased when it is combined with St. John's Wort.Nutraceutical
StiripentolThe serum concentration of Ergotamine can be increased when it is combined with Stiripentol.Approved
SulfisoxazoleThe metabolism of Ergotamine can be decreased when combined with Sulfisoxazole.Approved, Vet Approved
SulpirideThe risk or severity of adverse effects can be increased when Ergotamine is combined with Sulpiride.Approved
SumatriptanErgotamine may increase the vasoconstricting activities of Sumatriptan.Approved, Investigational
SynephrineErgotamine may increase the hypertensive activities of Synephrine.Experimental
TacrolimusThe serum concentration of Tacrolimus can be increased when it is combined with Ergotamine.Approved, Investigational
TamoxifenThe serum concentration of Tamoxifen can be increased when it is combined with Ergotamine.Approved
TamsulosinTamsulosin may decrease the vasoconstricting activities of Ergotamine.Approved, Investigational
TapentadolThe risk or severity of adverse effects can be increased when Ergotamine is combined with Tapentadol.Approved
Taurocholic AcidThe serum concentration of Taurocholic Acid can be increased when it is combined with Ergotamine.Experimental
Technetium Tc-99m sestamibiThe serum concentration of Technetium Tc-99m sestamibi can be increased when it is combined with Ergotamine.Approved
Tedizolid PhosphateTedizolid Phosphate may increase the serotonergic activities of Ergotamine.Approved
TelaprevirThe serum concentration of Ergotamine can be increased when it is combined with Telaprevir.Approved
TelithromycinThe metabolism of Ergotamine can be decreased when combined with Telithromycin.Approved
TemocaprilThe serum concentration of Ergotamine can be increased when it is combined with Temocapril.Experimental, Investigational
TemsirolimusThe serum concentration of Temsirolimus can be increased when it is combined with Ergotamine.Approved
TenofovirThe metabolism of Ergotamine can be decreased when combined with Tenofovir.Approved, Investigational
TerazosinTerazosin may decrease the vasoconstricting activities of Ergotamine.Approved
TerbutalineErgotamine may increase the hypertensive activities of Terbutaline.Approved
TeriflunomideThe serum concentration of Ergotamine can be decreased when it is combined with Teriflunomide.Approved
TheophyllineThe metabolism of Ergotamine can be decreased when combined with Theophylline.Approved
ThioproperazineThe risk or severity of adverse effects can be increased when Ergotamine is combined with Thioproperazine.Approved
ThioridazineThe risk or severity of adverse effects can be increased when Ergotamine is combined with Thioridazine.Approved
ThiorphanThe serum concentration of Ergotamine can be increased when it is combined with Thiorphan.Experimental
ThiothixeneThe risk or severity of adverse effects can be increased when Ergotamine is combined with Thiothixene.Approved
TianeptineTianeptine may decrease the antihypertensive activities of Ergotamine.Approved
TiaprideThe risk or severity of adverse effects can be increased when Ergotamine is combined with Tiapride.Investigational
TicagrelorThe serum concentration of Ticagrelor can be increased when it is combined with Ergotamine.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
TipranavirThe serum concentration of Ergotamine can be increased when it is combined with Tipranavir.Approved, Investigational
TizanidineErgotamine may increase the hypertensive activities of Tizanidine.Approved
TocilizumabThe serum concentration of Ergotamine can be decreased when it is combined with Tocilizumab.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
TopotecanThe serum concentration of Topotecan can be increased when it is combined with Ergotamine.Approved, Investigational
ToremifeneThe serum concentration of Toremifene can be increased when it is combined with Ergotamine.Approved, Investigational
TramadolThe risk or severity of adverse effects can be increased when Tramadol is combined with Ergotamine.Approved, Investigational
TrandolaprilThe serum concentration of Ergotamine can be increased when it is combined with Trandolapril.Approved
Trans-2-PhenylcyclopropylamineTrans-2-Phenylcyclopropylamine may increase the hypertensive activities of Ergotamine.Experimental
TranylcypromineTranylcypromine may increase the hypertensive activities of Ergotamine.Approved
Trastuzumab emtansineThe serum concentration of Trastuzumab emtansine can be increased when it is combined with Ergotamine.Approved
TrazodoneThe risk or severity of adverse effects can be increased when Trazodone is combined with Ergotamine.Approved, Investigational
TrifluoperazineThe risk or severity of adverse effects can be increased when Ergotamine is combined with Trifluoperazine.Approved
TriflupromazineThe risk or severity of adverse effects can be increased when Ergotamine is combined with Triflupromazine.Approved, Vet Approved
TrimazosinTrimazosin may decrease the vasoconstricting activities of Ergotamine.Experimental
TrimipramineTrimipramine may decrease the antihypertensive activities of Ergotamine.Approved
TroleandomycinThe serum concentration of Ergotamine can be increased when it is combined with Troleandomycin.Approved
TropisetronTropisetron may increase the serotonergic activities of Ergotamine.Investigational
TulobuterolErgotamine may increase the hypertensive activities of Tulobuterol.Investigational
TylosinThe serum concentration of Ergotamine can be increased when it is combined with Tylosin.Vet Approved
UbenimexThe serum concentration of Ergotamine can be increased when it is combined with Ubenimex.Experimental
UlinastatinThe serum concentration of Ergotamine can be increased when it is combined with Ulinastatin.Investigational
UlipristalThe serum concentration of Ulipristal can be increased when it is combined with Ergotamine.Approved
UmeclidiniumThe serum concentration of Umeclidinium can be increased when it is combined with Ergotamine.Approved
VecuroniumThe serum concentration of Vecuronium can be increased when it is combined with Ergotamine.Approved
VemurafenibThe serum concentration of Ergotamine can be increased when it is combined with Vemurafenib.Approved
VenetoclaxThe serum concentration of Venetoclax can be increased when it is combined with Ergotamine.Approved
VenlafaxineThe risk or severity of adverse effects can be increased when Venlafaxine is combined with Ergotamine.Approved
VerapamilThe metabolism of Ergotamine can be decreased when combined with Verapamil.Approved
VilazodoneErgotamine may increase the vasoconstricting activities of Vilazodone.Approved
VildagliptinThe serum concentration of Ergotamine can be increased when it is combined with Vildagliptin.Approved, Investigational
VinblastineThe serum concentration of Vinblastine can be increased when it is combined with Ergotamine.Approved
VincristineThe serum concentration of Vincristine can be increased when it is combined with Ergotamine.Approved, Investigational
VismodegibThe serum concentration of Vismodegib can be increased when it is combined with Ergotamine.Approved
VoriconazoleThe serum concentration of Ergotamine can be increased when it is combined with Voriconazole.Approved, Investigational
VortioxetineErgotamine may increase the vasoconstricting activities of Vortioxetine.Approved
XimelagatranThe serum concentration of Ergotamine can be increased when it is combined with Ximelagatran.Approved, Investigational, Withdrawn
XylazineErgotamine may increase the hypertensive activities of Xylazine.Vet Approved
YM-178Ergotamine may increase the hypertensive activities of YM-178.Investigational
Ym150The serum concentration of Ergotamine can be increased when it is combined with Ym150.Investigational
ZidovudineThe serum concentration of Zidovudine can be increased when it is combined with Ergotamine.Approved
ZiprasidoneThe metabolism of Ergotamine can be decreased when combined with Ziprasidone.Approved
ZolmitriptanErgotamine may increase the vasoconstricting activities of Zolmitriptan.Approved, Investigational
ZotepineThe risk or severity of adverse effects can be increased when Ergotamine is combined with Zotepine.Approved
ZuclopenthixolThe risk or severity of adverse effects can be increased when Ergotamine is combined with Zuclopenthixol.Approved, Investigational
Food Interactions
  • Caffeine increases absorption.
  • Take without regard to meals.
References
Synthesis ReferenceNot Available
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
ATC CodesN02CA52N02CA72N02CA02
AHFS CodesNot Available
PDB EntriesNot Available
FDA labelNot Available
MSDSDownload (53.1 KB)
ADMET
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 )
Pharmacoeconomics
Manufacturers
  • 3m pharmaceuticals inc
  • Rosedale therapeutics
  • Parke davis div warner lambert co
  • Organon usa inc
Packagers
Dosage forms
FormRouteStrength
CapsuleOral
Tablet, orally disintegratingSublingual2 mg/1
TabletSublingual2 mg
TabletOral2 mg/1
Tablet, film coatedOral
TabletOral
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.
PatentsNot Available
Properties
StateSolid
Experimental Properties
PropertyValueSource
melting point213.5 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 FiveYesChemAxon
Ghose FilterYesChemAxon
Veber's RuleYesChemAxon
MDDR-like RuleYesChemAxon
Spectra
Mass Spec (NIST)Download (12 KB)
Spectra
Spectrum TypeDescriptionSplash Key
Predicted LC-MS/MSPredicted LC-MS/MS Spectrum - 10V, PositiveNot Available
Predicted LC-MS/MSPredicted LC-MS/MS Spectrum - 20V, PositiveNot Available
Predicted LC-MS/MSPredicted LC-MS/MS Spectrum - 40V, PositiveNot Available
Predicted LC-MS/MSPredicted LC-MS/MS Spectrum - 10V, NegativeNot Available
Predicted LC-MS/MSPredicted LC-MS/MS Spectrum - 20V, NegativeNot Available
Predicted LC-MS/MSPredicted LC-MS/MS Spectrum - 40V, NegativeNot Available
Taxonomy
DescriptionThis 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.
KingdomOrganic compounds
Super ClassAlkaloids and derivatives
ClassErgoline and derivatives
Sub ClassLysergic acids and derivatives
Direct ParentErgotamines, dihydroergotamines, and derivatives
Alternative Parents
Substituents
  • Ergotamine
  • Hybrid peptide
  • Lysergic acid amide
  • Indoloquinoline
  • Benzoquinoline
  • Quinoline-3-carboxamide
  • Pyrroloquinoline
  • N-acyl-alpha amino acid or derivatives
  • Quinoline
  • Isoindole or derivatives
  • Indole or derivatives
  • Indole
  • Aralkylamine
  • N-alkylpiperazine
  • Tetrahydropyridine
  • Benzenoid
  • Piperazine
  • Oxazolidinone
  • 1,4-diazinane
  • Monocyclic benzene moiety
  • Heteroaromatic compound
  • Tertiary carboxylic acid amide
  • Pyrrolidine
  • Pyrrole
  • Tertiary aliphatic amine
  • Tertiary amine
  • Secondary carboxylic acid amide
  • Orthocarboxylic acid derivative
  • Lactam
  • Carboxamide group
  • Oxacycle
  • Azacycle
  • Organoheterocyclic compound
  • Carboxylic acid derivative
  • Carboxylic acid amide
  • Alkanolamine
  • Hydrocarbon derivative
  • Organooxygen compound
  • Organonitrogen compound
  • Carbonyl group
  • Amine
  • Aromatic heteropolycyclic compound
Molecular FrameworkAromatic heteropolycyclic compounds
External Descriptors

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 substances. Ligand binding causes a conformation change that triggers signaling via guanine nucleotide-binding proteins (G proteins) and modulates the activity of down-stream effectors, such as adenylate c...
Gene Name:
HTR1D
Uniprot ID:
P28221
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 substances, such as lysergic acid diethylamide (LSD). Ligand binding causes a conformation change that triggers signaling via guanine nucleotide-binding proteins (G proteins) and modulates the activity of ...
Gene Name:
HTR1B
Uniprot ID:
P28222
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-iodophenyl)-2-aminopropane (DOI) and lysergic acid diethylamide (LSD). Ligand binding causes a conformation change that triggers signaling via guanine nucleotide-binding proteins (G proteins) and modulates...
Gene Name:
HTR2A
Uniprot ID:
P28223
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
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) proteins. Nuclear ADRA1A-ADRA1B heterooligomers regulate phenylephrine(PE)-stimulated ERK signaling in cardiac myocytes.
Gene Name:
ADRA1A
Uniprot ID:
P35348
Molecular Weight:
51486.005 Da
References
  1. 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) proteins. Nuclear ADRA1A-ADRA1B heterooligomers regulate phenylephrine (PE)-stimulated ERK signaling in cardiac myocytes.
Gene Name:
ADRA1B
Uniprot ID:
P35368
Molecular Weight:
56835.375 Da
References
  1. 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
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 oxymetazoline > clonidine > epinephrine > norepinephrine > phenylephrine > dopamine > p-synephrine > p-tyramine > serotonin = p-octopamine. For antagonists, the rank order is yohimbine > phentolamine = mianser...
Gene Name:
ADRA2A
Uniprot ID:
P08913
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
agonistpartial 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 > norepinephrine > epinephrine = oxymetazoline > dopamine > p-tyramine = phenylephrine > serotonin > p-synephrine / p-octopamine. For antagonists, the rank order is yohimbine > chlorpromazine > phent...
Gene Name:
ADRA2B
Uniprot ID:
P18089
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
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:
NameUniProt IDDetails
D(1A) dopamine receptorP21728 Details
D(1B) dopamine receptorP21918 Details
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 signaling via guanine nucleotide-binding proteins (G proteins) and modulates the activity of down-stream effectors, such as adenylate cyclase. Beta-arrestin family members inhibit signaling via G pro...
Gene Name:
HTR1A
Uniprot ID:
P08908
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 triggers signaling via guanine nucleotide-binding proteins (G proteins) and modulates the activity of down-stream effectors, such as adenylate cyclase. Signaling inhibits adenylate cyclase activity.
Gene Name:
HTR1F
Uniprot ID:
P30939
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-iodophenyl-2-aminopropane (DOI) and lysergic acid diethylamide (LSD). Ligand binding causes a conformation change that triggers signaling via guanine nucleotide-binding proteins (G proteins) and modul...
Gene Name:
HTR2C
Uniprot ID:
P28335
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 ]

Enzymes

Kind
Protein
Organism
Human
Pharmacological action
unknown
Actions
substrateinhibitor
General Function:
Vitamin d3 25-hydroxylase activity
Specific Function:
Cytochromes P450 are a group of heme-thiolate monooxygenases. In liver microsomes, this enzyme is involved in an NADPH-dependent electron transport pathway. It performs a variety of oxidation reactions (e.g. caffeine 8-oxidation, omeprazole sulphoxidation, midazolam 1'-hydroxylation and midazolam 4-hydroxylation) of structurally unrelated compounds, including steroids, fatty acids, and xenobiot...
Gene Name:
CYP3A4
Uniprot ID:
P08684
Molecular Weight:
57342.67 Da
References
  1. Preissner S, Kroll K, Dunkel M, Senger C, Goldsobel G, Kuzman D, Guenther S, Winnenburg R, Schroeder M, Preissner R: SuperCYP: a comprehensive database on Cytochrome P450 enzymes including a tool for analysis of CYP-drug interactions. Nucleic Acids Res. 2010 Jan;38(Database issue):D237-43. doi: 10.1093/nar/gkp970. Epub 2009 Nov 24. [PubMed:19934256 ]
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 unrelated compounds, including steroids, fatty acids, and xenobiotics. Most active in catalyzing 2-hydroxylation. Caffeine is metabolized primarily by cytochrome CYP1A2 in the liver through an initial N...
Gene Name:
CYP1A2
Uniprot ID:
P05177
Molecular Weight:
58293.76 Da
References
  1. Preissner S, Kroll K, Dunkel M, Senger C, Goldsobel G, Kuzman D, Guenther S, Winnenburg R, Schroeder M, Preissner R: SuperCYP: a comprehensive database on Cytochrome P450 enzymes including a tool for analysis of CYP-drug interactions. Nucleic Acids Res. 2010 Jan;38(Database issue):D237-43. doi: 10.1093/nar/gkp970. Epub 2009 Nov 24. [PubMed:19934256 ]

Transporters

Kind
Protein
Organism
Human
Pharmacological action
unknown
Actions
inhibitor
General Function:
Xenobiotic-transporting atpase activity
Specific Function:
Energy-dependent efflux pump responsible for decreased drug accumulation in multidrug-resistant cells.
Gene Name:
ABCB1
Uniprot ID:
P08183
Molecular Weight:
141477.255 Da
References
  1. 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 ]
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Drug created on June 13, 2005 07:24 / Updated on August 17, 2016 12:23