ergotamine

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Dose	Unit	Route
4	mg	Inhal.aerosol
4	mg	O
4	mg	P
4	mg	R
4	mg	SL
4	mg	O
4	mg	O

Property	Value	Reference
BDDCS (Biopharmaceutical Drug Disposition Classification System)	2	Bocci G, Oprea TI, Benet LZ
S (Water solubility)	0.00 mg/mL	Bocci G, Oprea TI, Benet LZ
MRTD (Maximum Recommended Therapeutic Daily Dose)	0.15 µM/kg/day	Contrera JF, Matthews EJ, Kruhlak NL, Benz RD
BA (Bioavailability)	2 %	Kim MT, Sedykh A, Chakravarti SK, Saiakhov RD, Zhu H
Vd (Volume of distribution)	3.60 L/kg	Lombardo F, Berellini G, Obach RS
CL (Clearance)	15 mL/min/kg	Lombardo F, Berellini G, Obach RS
fu (Fraction unbound in plasma)	0.02 %	Lombardo F, Berellini G, Obach RS
t_half (Half-life)	2.10 hours	Lombardo F, Berellini G, Obach RS

Property	Description	Value
kinase-safety-class	ACVR2B,AXL,BRAF,BTK,CAMK2D,CDK5,CDK9,EIF2AK3,ERBB2,GRK2,ITK,MAPK10,MAPK7,PDK1,PDK2,PDK4,PIK3CB,PRKDC,TEK	19
kinase-selectivity-class	AXL	1
pfas-class	PFAS structural alert (1 = True, 0 = False)	0

Source	Code	Description
ATC	N02CA02	NERVOUS SYSTEM ANALGESICS ANTIMIGRAINE PREPARATIONS Ergot alkaloids
ATC	N02CA52	NERVOUS SYSTEM ANALGESICS ANTIMIGRAINE PREPARATIONS Ergot alkaloids
ATC	N02CA72	NERVOUS SYSTEM ANALGESICS ANTIMIGRAINE PREPARATIONS Ergot alkaloids
FDA CS	M0007665	Ergotamines
MeSH PA	D000316	Adrenergic alpha-Agonists
MeSH PA	D000700	Analgesics
MeSH PA	D002317	Cardiovascular Agents
MeSH PA	D010120	Oxytocics
MeSH PA	D012102	Reproductive Control Agents
MeSH PA	D014662	Vasoconstrictor Agents
MeSH PA	D017366	Serotonin Receptor Agonists
MeSH PA	D018377	Neurotransmitter Agents
MeSH PA	D018490	Serotonin Agents
MeSH PA	D018663	Adrenergic Agents
MeSH PA	D018689	Sensory System Agents
MeSH PA	D018712	Analgesics, Non-Narcotic
MeSH PA	D058646	Adrenergic alpha-1 Receptor Agonists
FDA EPC	N0000175766	Ergotamine Derivative
CHEBI has role	CHEBI:25442	mycotoxin
CHEBI has role	CHEBI:35481	non-narcotic analgesic
CHEBI has role	CHEBI:35569	α-adrenergic agonist
CHEBI has role	CHEBI:35941	serotonergic agonist
CHEBI has role	CHEBI:36063	oxytocic
CHEBI has role	CHEBI:50514	vasoconstrictor agent

Disease	Relation	SNOMED_ID	DOID
Migraine	indication	37796009	DOID:6364
Vascular headache	indication	128187005
Cluster headache syndrome	indication	193031009
Cluster Headache Prevention	indication
Brain damage	contraindication	2470005
Necrotizing enterocolitis in fetus OR newborn	contraindication	2707005
Tachyarrhythmia	contraindication	6285003
Suicidal thoughts	contraindication	6471006
Urinary tract obstruction	contraindication	7163005	DOID:5200
Alcoholism	contraindication	7200002
Hyperammonemia	contraindication	9360008
Bacterial septicemia	contraindication	10001005	DOID:0040085
Peptic ulcer	contraindication	13200003	DOID:750
Chronic obstructive lung disease	contraindication	13645005	DOID:3083
Hepatic encephalopathy	contraindication	13920009	DOID:13413
Severe chronic ulcerative colitis	contraindication	14311001
Toxic megacolon	contraindication	28536002	DOID:1770
Atony of colon	contraindication	29479008
Vascular surgery procedure	contraindication	30904006
Hyperthyroidism	contraindication	34486009	DOID:7998
Depressive disorder	contraindication	35489007
Hypertensive disorder	contraindication	38341003	DOID:10763
Complete trisomy 21 syndrome	contraindication	41040004	DOID:14250
Hyperactive behavior	contraindication	44548000
Conduction disorder of the heart	contraindication	44808001
Achalasia of esophagus	contraindication	45564002	DOID:9164
Chronic heart failure	contraindication	48447003
Retroperitoneal fibrosis	contraindication	49120005
Fibrosis of lung	contraindication	51615001	DOID:3770
Paralytic ileus	contraindication	55525008	DOID:8442
Peptic reflux disease	contraindication	57643001
Acute nephropathy	contraindication	58574008
Hepatic failure	contraindication	59927004
Diarrhea	contraindication	62315008
Thrombophlebitis	contraindication	64156001	DOID:3875
Ulcerative colitis	contraindication	64766004	DOID:8577
Poisoning by phenobarbital	contraindication	64921004
Drug AND/OR toxin-induced diarrhea	contraindication	65979008
Substance abuse	contraindication	66214007
Agoraphobia	contraindication	70691001	DOID:593
Hepatic coma	contraindication	72836002	DOID:12550
Sleep apnea	contraindication	73430006	DOID:0050847
Spastic paralysis	contraindication	78403003
Disturbance of salivary secretion	contraindication	78948009
Hiatal hernia	contraindication	84089009	DOID:12642
Prinzmetal angina	contraindication	87343002
Kidney disease	contraindication	90708001	DOID:557
Myasthenia gravis	contraindication	91637004	DOID:437
Gastrointestinal obstruction	contraindication	126765001
Seizure disorder	contraindication	128613002
Autonomic dysreflexia	contraindication	129618003
Bleeding	contraindication	131148009
Obsessive-compulsive disorder	contraindication	191736004	DOID:10933
Insomnia	contraindication	193462001
Impaired renal function disorder	contraindication	197663003
Myocardial dysfunction	contraindication	233928007
Peripheral ischemia	contraindication	233958001
Disease of liver	contraindication	235856003	DOID:409
Bladder outflow obstruction	contraindication	236645006
Sepsis syndrome	contraindication	238150007
Pyloric obstruction	contraindication	244815007
Sleep automatism	contraindication	247962006
Raynaud's phenomenon	contraindication	266261006
Benign prostatic hyperplasia	contraindication	266569009
Dyspnea	contraindication	267036007
Retention of urine	contraindication	267064002
Anemia	contraindication	271737000	DOID:2355
Drowsy	contraindication	271782001
Cerebral ischemia	contraindication	287731003
Pregnancy, function	contraindication	289908002
Thrombocytopenic disorder	contraindication	302215000	DOID:1588
Neutropenic disorder	contraindication	303011007	DOID:1227
Panic disorder	contraindication	371631005	DOID:594
Angle-closure glaucoma	contraindication	392291006	DOID:13550
Cardiovascular event risk	contraindication	395112001
Gastric ulcer	contraindication	397825006	DOID:10808
Peripheral vascular disease	contraindication	400047006
Respiratory insufficiency	contraindication	409623005
Breastfeeding (mother)	contraindication	413712001
Chronic lung disease	contraindication	413839001
Disorder of coronary artery	contraindication	414024009
Myocardial ischemia	contraindication	414795007	DOID:3393
Myocardial infarction in recovery phase	contraindication	418044006
Porphyria	contraindication	418470004
Fibrosis of pleura	contraindication	442110002
Hypertensive urgency	contraindication	443482000
Acute exacerbation of asthma	contraindication	708038006
Severe Pruritus	contraindication
Ergot Alkaloid Toxicity	contraindication

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ergotamine 🐶 Veterinary Use | Indications/Contra | FAERs-F | FAERs-M | Orange Bk | PK/Tox | Related Drugs | BioActivity |

Description:

Drug dosage:

ADMET properties:

Predicted pharmacokinetic/toxicological properties (PK-AZ):

Approvals:

FDA Adverse Event Reporting System (Female)

FDA Adverse Event Reporting System (Male)

FDA Adverse Event Reporting System (Geriatric)

FDA Adverse Event Reporting System (Pediatric)

Pharmacologic Action:

Related Drugs by ATC class:

Drug Use | Suggest Off label Use Form| |View source of the data|

🐶 Veterinary Drug Use

🐶 Veterinary products

Acid dissociation constants calculated using MoKa v3.0.0

Orange Book patent data (new drug applications)

Orange Book exclusivity data (new drug applications)

Bioactivity Summary:

External reference:

Pharmaceutical products:

Target	Class	Pharos	UniProt	Action	Type	Activity value (-log[M])	Bioact source	MoA source
5-hydroxytryptamine receptor 1D	GPCR	P28221	5HT1D_HUMAN	AGONIST	Ki	9.10	CHEMBL	CHEMBL
Beta-1 adrenergic receptor	GPCR	P08588	ADRB1_HUMAN		Ki	5.62	DRUG MATRIX
Beta-2 adrenergic receptor	GPCR	P07550	ADRB2_HUMAN		Ki	5.72	DRUG MATRIX
D(1A) dopamine receptor	GPCR	P21728	DRD1_HUMAN		Ki	6.06	DRUG MATRIX
D(2) dopamine receptor	GPCR	P14416	DRD2_HUMAN		Ki	8.85	DRUG MATRIX
Alpha-2A adrenergic receptor	GPCR	P08913	ADA2A_HUMAN		Ki	9.10	DRUG MATRIX
Cytochrome P450 3A4	Enzyme	P08684	CP3A4_HUMAN		IC50	6	DRUG MATRIX
5-hydroxytryptamine receptor 1A	GPCR	P08908	5HT1A_HUMAN		Ki	9.35	DRUG MATRIX
5-hydroxytryptamine receptor 2A	GPCR	P28223	5HT2A_HUMAN	AGONIST	Ki	9	IUPHAR
5-hydroxytryptamine receptor 2B	GPCR	P41595	5HT2B_HUMAN	AGONIST	Ki	8.90	IUPHAR
5-hydroxytryptamine receptor 2C	GPCR	P28335	5HT2C_HUMAN	AGONIST	Ki	8.70	IUPHAR
5-hydroxytryptamine receptor 6	GPCR	P50406	5HT6R_HUMAN	AGONIST	Ki	8.60	IUPHAR
Alpha-1A adrenergic receptor	GPCR	P35348	ADA1A_HUMAN	AGONIST			WOMBAT-PK
Alpha-2B adrenergic receptor	GPCR	P18089	ADA2B_HUMAN		Ki	8.75	DRUG MATRIX
D(3) dopamine receptor	GPCR	P35462	DRD3_HUMAN		Ki	8.84	DRUG MATRIX
D(1B) dopamine receptor	GPCR	P21918	DRD5_HUMAN		Ki	6.77	PDSP
Muscarinic acetylcholine receptor M1	GPCR	P11229	ACM1_HUMAN		Ki	6.06	PDSP
Muscarinic acetylcholine receptor M2	GPCR	P08172	ACM2_HUMAN		Ki	6.04	PDSP
5-hydroxytryptamine receptor 1B	GPCR	P28222	5HT1B_HUMAN		Ki	8.68	CHEMBL
Alpha-2C adrenergic receptor	GPCR	P18825	ADA2C_HUMAN		Ki	8.74	DRUG MATRIX
Alpha-1D adrenergic receptor	GPCR	P25100	ADA1D_HUMAN		Ki	8.49	DRUG MATRIX
5-hydroxytryptamine receptor 5A	GPCR	P47898	5HT5A_HUMAN		Ki	7.85	CHEMBL
5-hydroxytryptamine receptor 1F	GPCR	P30939	5HT1F_HUMAN	AGONIST	Ki	6.80	IUPHAR
5-hydroxytryptamine receptor 1E	GPCR	P28566	5HT1E_HUMAN	AGONIST	Ki	6.30	IUPHAR
Tyrosine-protein kinase Lck	Kinase	P06239	LCK_HUMAN		IC50	5.19	DRUG MATRIX
Tyrosine-protein kinase Fyn	Kinase	P06241	FYN_HUMAN		IC50	5.50	DRUG MATRIX
Thromboxane-A synthase	Enzyme	P24557	THAS_HUMAN		IC50	5.51	DRUG MATRIX
5-hydroxytryptamine receptor 2A	GPCR		5HT2A_RAT	AGONIST	Ki	8	IUPHAR
5-hydroxytryptamine receptor 7	GPCR		5HT7R_MOUSE	ANTAGONIST	Ki	7.30	IUPHAR
5-hydroxytryptamine receptor 2C	GPCR		5HT2C_RAT	AGONIST	Ki	7.90	IUPHAR
5-hydroxytryptamine receptor 1B	GPCR		5HT1B_RAT		Ki	10.04	DRUG MATRIX
5-hydroxytryptamine receptor 4	GPCR		5HT4R_CAVPO		Ki	6.58	DRUG MATRIX
Alpha-1B adrenergic receptor	GPCR		ADA1B_RAT		Ki	8.34	DRUG MATRIX
Alpha-1A adrenergic receptor	GPCR		ADA1A_RAT		IC50	8.09	CHEMBL
Gastrin/cholecystokinin type B receptor	GPCR		GASR_MOUSE		IC50	4.77	CHEMBL
5-hydroxytryptamine receptor 6	GPCR		5HT6R_RAT	AGONIST	Ki	8.60	IUPHAR
Cholecystokinin A receptor	GPCR		CCKAR_MOUSE		IC50	4.47	CHEMBL
Adenylate cyclase	Enzyme		O32393_ARTPT		IC50	4.15	CHEMBL
5-hydroxytryptamine receptor 5A	GPCR		5HT5A_RAT	ANTAGONIST	Ki	8.20	IUPHAR
5-hydroxytryptamine receptor 5A	GPCR		5HT5A_MOUSE	ANTAGONIST	Ki	8.40	IUPHAR
5-hydroxytryptamine receptor 1A	GPCR		5HT1A_RAT		IC50	9.11	CHEMBL
5-hydroxytryptamine receptor 1F	GPCR		5HT1F_RAT	AGONIST	IC50	7.30	IUPHAR

ID	Source
4022407	VUID
N0000020412	NUI
D00679	KEGG_DRUG
379-79-3	SECONDARY_CAS_RN
4018515	VANDF
4022407	VANDF
C0014710	UMLSCUI
CHEBI:64318	CHEBI
ERM	PDB_CHEM_ID
CHEMBL442	ChEMBL_ID
CHEMBL2448612	ChEMBL_ID
D004878	MESH_DESCRIPTOR_UI
DB00696	DRUGBANK_ID
149	IUPHAR_LIGAND_ID
391	INN_ID
PR834Q503T	UNII
8223	PUBCHEM_CID
4025	RXNORM
44346	MMSL
4674	MMSL
d00222	MMSL
000678	NDDF
004526	NDDF
32647002	SNOMEDCT_US
395975005	SNOMEDCT_US
396046007	SNOMEDCT_US
639-81-6	SECONDARY_CAS_RN
PR834Q503T	INXIGHT DRUGS

Product	Category	Ingredients	NDC	Form	Quantity	Route	Marketing	Label
ERGOTAMINE	HUMAN PRESCRIPTION DRUG LABEL	2	0143-2120	TABLET, FILM COATED	1 mg	ORAL	ANDA	22 sections
MIGERGOT	HUMAN PRESCRIPTION DRUG LABEL	2	0713-0166	SUPPOSITORY	2 mg	RECTAL	ANDA	14 sections
ergotamine tartrate and caffeine	HUMAN PRESCRIPTION DRUG LABEL	2	24470-917	TABLET, FILM COATED	1 mg	ORAL	ANDA	24 sections
Cafergot	HUMAN PRESCRIPTION DRUG LABEL	2	73352-917	TABLET, FILM COATED	1 mg	ORAL	ANDA	24 sections
Migergot	HUMAN PRESCRIPTION DRUG LABEL	2	75987-090	SUPPOSITORY	2 mg	RECTAL	ANDA	22 sections
Ergomar Sublingual	HUMAN PRESCRIPTION DRUG LABEL	1	81279-104	TABLET	2 mg	ORAL	ANDA	25 sections

Dissociation level	Dissociation constant	Type (acidic/basic)
pKa1	11.58	acidic
pKa2	12.56	acidic
pKa3	13.71	acidic
pKa4	6.51	Basic