Details
Stereochemistry | ABSOLUTE |
Molecular Formula | C33H35N5O5 |
Molecular Weight | 581.6615 |
Optical Activity | UNSPECIFIED |
Defined Stereocenters | 6 / 6 |
E/Z Centers | 0 |
Charge | 0 |
SHOW SMILES / InChI
SMILES
[H][C@@]12CCCN1C(=O)[C@H](CC3=CC=CC=C3)N4C(=O)[C@](C)(NC(=O)[C@H]5CN(C)[C@]6([H])CC7=CNC8=C7C(=CC=C8)C6=C5)O[C@@]24O
InChI
InChIKey=XCGSFFUVFURLIX-VFGNJEKYSA-N
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
Molecular Formula | C33H35N5O5 |
Molecular Weight | 581.6615 |
Charge | 0 |
Count |
|
Stereochemistry | ABSOLUTE |
Additional Stereochemistry | No |
Defined Stereocenters | 6 / 6 |
E/Z Centers | 0 |
Optical Activity | UNSPECIFIED |
DescriptionSources: https://www.ncbi.nlm.nih.gov/pubmed/17149427
Sources: https://www.ncbi.nlm.nih.gov/pubmed/17149427
The isolation and naming of ergotamine by Stoll occurred in 1925 but the complete elucidation of structure was not achieved until 1951, with synthesis following some 10 years later. Current sources of ergotamine include the isolation from field ergot and fermentation broth, as well as synthesis via coupling of (+)-lysergic acid with the appropriate synthetic peptidic moiety. Ergotamine was introduced into world commerce in 1921, and is currently marketed as its water soluble tartrate salt.
Ergotamine is a partial agonist at various tryptaminergic receptors (including the serotonin receptor [5-HT2]) and at various α-adrenergic receptors in blood vessels and various smooth muscles. It is likely that the major activity of ergotamine and related alkaloids is one of agonism at the 5-HT1B/1D receptors, just as with the “triptan” antimigraine compounds. FDA-labeled indications for ergotamine tartrate are in the abortion or prevention of vascular headaches, such as migraine, migraine variant, cluster headache, and histaminic cephalalgia.
Originator
Sources: https://www.ncbi.nlm.nih.gov/pubmed/17149427
Curator's Comment: In 1918 Arthur Stoll patented the isolation of ergotamine tartrate, which was subsequently marketed by Sandoz in 1921.
Approval Year
Targets
Primary Target | Pharmacology | Condition | Potency |
---|---|---|---|
Target ID: CHEMBL214 Sources: https://www.ncbi.nlm.nih.gov/pubmed/8397171 |
0.34 nM [Ki] | ||
Target ID: CHEMBL1898 Sources: https://www.ncbi.nlm.nih.gov/pubmed/8397171 |
5.4 nM [Ki] | ||
Target ID: CHEMBL1983 Sources: https://www.ncbi.nlm.nih.gov/pubmed/8397171 |
0.4 nM [Ki] | ||
Target ID: CHEMBL2182 Sources: https://www.ncbi.nlm.nih.gov/pubmed/8397171 |
9.4 nM [Ki] | ||
Target ID: CHEMBL1833 Sources: https://www.ncbi.nlm.nih.gov/pubmed/11104741 |
3.0 nM [Ki] | ||
Target ID: CHEMBL2094251 |
|||
Target ID: CHEMBL2095158 Sources: https://www.ncbi.nlm.nih.gov/pubmed/2881518 |
Conditions
Condition | Modality | Targets | Highest Phase | Product |
---|---|---|---|---|
Primary | ERGOMAR Approved UseErgomar® is indicated as therapy to abort or prevent vascular headache, e.g., migraine, migraine variants or a so-called "histaminic cephalalgia". Launch Date4.1472E11 |
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Primary | CAFERGOT Approved UseTreatment of acute attacks of migraine with or without aura in adults. |
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Sources: http://www.horizonpharma.com/migergot/ |
Primary | MIGERGOT Approved UseMIGERGOT is indicated as therapy to abort or prevent vascular headache, e.g., migraine, migraine variants or so-called “histaminic cephalalgia.” Ergotamine tartrate and caffeine suppositories should only be used for migraine headaches as they are not effective for other types of headaches and they lack analgesic properties. Launch Date4.33987191E11 |
Cmax
Value | Dose | Co-administered | Analyte | Population |
---|---|---|---|---|
21.4 pg/mL EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/3732370/ |
2 mg single, oral dose: 2 mg route of administration: Oral experiment type: SINGLE co-administered: |
ERGOTAMINE plasma | Homo sapiens population: HEALTHY age: ADULT sex: FEMALE / MALE food status: FASTED |
|
454 pg/mL EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/3732370/ |
2 mg single, rectal dose: 2 mg route of administration: Rectal experiment type: SINGLE co-administered: |
ERGOTAMINE plasma | Homo sapiens population: HEALTHY age: ADULT sex: FEMALE / MALE food status: FASTED |
AUC
Value | Dose | Co-administered | Analyte | Population |
---|---|---|---|---|
4.38 ng × h/mL EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/3932078/ |
3.89 μg/kg bw single, intravenous dose: 3.89 μg/kg bw route of administration: Intravenous experiment type: SINGLE co-administered: |
ERGOTAMINE plasma | Homo sapiens population: HEALTHY age: ADULT sex: FEMALE / MALE food status: FED |
|
61 pg × h/mL EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/3732370/ |
2 mg single, oral dose: 2 mg route of administration: Oral experiment type: SINGLE co-administered: |
ERGOTAMINE plasma | Homo sapiens population: HEALTHY age: ADULT sex: FEMALE / MALE food status: FASTED |
|
1.36 ng × h/mL EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/3932078/ |
1.01 μg/kg bw single, intravenous dose: 1.01 μg/kg bw route of administration: Intravenous experiment type: SINGLE co-administered: |
ERGOTAMINE plasma | Homo sapiens population: HEALTHY age: ADULT sex: FEMALE / MALE food status: FED |
|
2.04 ng × h/mL EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/3932078/ |
1.94 μg/kg bw single, intravenous dose: 1.94 μg/kg bw route of administration: Intravenous experiment type: SINGLE co-administered: |
ERGOTAMINE plasma | Homo sapiens population: HEALTHY age: ADULT sex: FEMALE / MALE food status: FED |
|
1216 pg × h/mL EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/3732370/ |
2 mg single, rectal dose: 2 mg route of administration: Rectal experiment type: SINGLE co-administered: |
ERGOTAMINE plasma | Homo sapiens population: HEALTHY age: ADULT sex: FEMALE / MALE food status: FASTED |
T1/2
Value | Dose | Co-administered | Analyte | Population |
---|---|---|---|---|
2.15 h EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/3932078/ |
3.89 μg/kg bw single, intravenous dose: 3.89 μg/kg bw route of administration: Intravenous experiment type: SINGLE co-administered: |
ERGOTAMINE plasma | Homo sapiens population: HEALTHY age: ADULT sex: FEMALE / MALE food status: FED |
|
2.08 h EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/3932078/ |
1.01 μg/kg bw single, intravenous dose: 1.01 μg/kg bw route of administration: Intravenous experiment type: SINGLE co-administered: |
ERGOTAMINE plasma | Homo sapiens population: HEALTHY age: ADULT sex: FEMALE / MALE food status: FED |
|
2.13 h EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/3932078/ |
1.94 μg/kg bw single, intravenous dose: 1.94 μg/kg bw route of administration: Intravenous experiment type: SINGLE co-administered: |
ERGOTAMINE plasma | Homo sapiens population: HEALTHY age: ADULT sex: FEMALE / MALE food status: FED |
|
3.35 h EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/3732370/ |
2 mg single, rectal dose: 2 mg route of administration: Rectal experiment type: SINGLE co-administered: |
ERGOTAMINE plasma | Homo sapiens population: HEALTHY age: ADULT sex: FEMALE / MALE food status: FASTED |
Doses
Dose | Population | Adverse events |
---|---|---|
20 mg single, oral Overdose Dose: 20 mg Route: oral Route: single Dose: 20 mg Co-administed with:: caffeine, p.o(2000 mg, single) Sources: |
healthy, 21 n = 1 Health Status: healthy Age Group: 21 Sex: F Population Size: 1 Sources: |
Disc. AE: Nausea, Vomiting... AEs leading to discontinuation/dose reduction: Nausea Sources: Vomiting (severe) Dizziness Blood pressure decreased Peripheral vasoconstriction Paresthesia Cyanosis peripheral Angina |
2 mg single, oral Recommended Dose: 2 mg Route: oral Route: single Dose: 2 mg Co-administed with:: caffeine, p.o(200 mg, single) Sources: Page: p.319 |
unhealthy, 40+/-10 n = 289 Health Status: unhealthy Condition: Migraine Age Group: 40+/-10 Sex: M+F Population Size: 289 Sources: Page: p.319 |
Disc. AE: Depression, Vertigo... AEs leading to discontinuation/dose reduction: Depression Sources: Page: p.319Vertigo Blurred vision Arrhythmia Hypersensitivity Migraine aggravated Urticaria Dyspnoea Fatigue Tachycardia Vagal reaction Dizziness Tinnitus |
2 mg single, oral Recommended Dose: 2 mg Route: oral Route: single Dose: 2 mg Sources: Page: p.2 |
unhealthy n = 41 Health Status: unhealthy Condition: Migraine Sex: M+F Population Size: 41 Sources: Page: p.2 |
Disc. AE: Nausea, Lightheadedness... AEs leading to discontinuation/dose reduction: Nausea (2.4%) Sources: Page: p.2Lightheadedness (2.4%) |
AEs
AE | Significance | Dose | Population |
---|---|---|---|
Angina | Disc. AE | 20 mg single, oral Overdose Dose: 20 mg Route: oral Route: single Dose: 20 mg Co-administed with:: caffeine, p.o(2000 mg, single) Sources: |
healthy, 21 n = 1 Health Status: healthy Age Group: 21 Sex: F Population Size: 1 Sources: |
Blood pressure decreased | Disc. AE | 20 mg single, oral Overdose Dose: 20 mg Route: oral Route: single Dose: 20 mg Co-administed with:: caffeine, p.o(2000 mg, single) Sources: |
healthy, 21 n = 1 Health Status: healthy Age Group: 21 Sex: F Population Size: 1 Sources: |
Cyanosis peripheral | Disc. AE | 20 mg single, oral Overdose Dose: 20 mg Route: oral Route: single Dose: 20 mg Co-administed with:: caffeine, p.o(2000 mg, single) Sources: |
healthy, 21 n = 1 Health Status: healthy Age Group: 21 Sex: F Population Size: 1 Sources: |
Dizziness | Disc. AE | 20 mg single, oral Overdose Dose: 20 mg Route: oral Route: single Dose: 20 mg Co-administed with:: caffeine, p.o(2000 mg, single) Sources: |
healthy, 21 n = 1 Health Status: healthy Age Group: 21 Sex: F Population Size: 1 Sources: |
Nausea | Disc. AE | 20 mg single, oral Overdose Dose: 20 mg Route: oral Route: single Dose: 20 mg Co-administed with:: caffeine, p.o(2000 mg, single) Sources: |
healthy, 21 n = 1 Health Status: healthy Age Group: 21 Sex: F Population Size: 1 Sources: |
Paresthesia | Disc. AE | 20 mg single, oral Overdose Dose: 20 mg Route: oral Route: single Dose: 20 mg Co-administed with:: caffeine, p.o(2000 mg, single) Sources: |
healthy, 21 n = 1 Health Status: healthy Age Group: 21 Sex: F Population Size: 1 Sources: |
Peripheral vasoconstriction | Disc. AE | 20 mg single, oral Overdose Dose: 20 mg Route: oral Route: single Dose: 20 mg Co-administed with:: caffeine, p.o(2000 mg, single) Sources: |
healthy, 21 n = 1 Health Status: healthy Age Group: 21 Sex: F Population Size: 1 Sources: |
Vomiting | severe Disc. AE |
20 mg single, oral Overdose Dose: 20 mg Route: oral Route: single Dose: 20 mg Co-administed with:: caffeine, p.o(2000 mg, single) Sources: |
healthy, 21 n = 1 Health Status: healthy Age Group: 21 Sex: F Population Size: 1 Sources: |
Arrhythmia | Disc. AE | 2 mg single, oral Recommended Dose: 2 mg Route: oral Route: single Dose: 2 mg Co-administed with:: caffeine, p.o(200 mg, single) Sources: Page: p.319 |
unhealthy, 40+/-10 n = 289 Health Status: unhealthy Condition: Migraine Age Group: 40+/-10 Sex: M+F Population Size: 289 Sources: Page: p.319 |
Blurred vision | Disc. AE | 2 mg single, oral Recommended Dose: 2 mg Route: oral Route: single Dose: 2 mg Co-administed with:: caffeine, p.o(200 mg, single) Sources: Page: p.319 |
unhealthy, 40+/-10 n = 289 Health Status: unhealthy Condition: Migraine Age Group: 40+/-10 Sex: M+F Population Size: 289 Sources: Page: p.319 |
Depression | Disc. AE | 2 mg single, oral Recommended Dose: 2 mg Route: oral Route: single Dose: 2 mg Co-administed with:: caffeine, p.o(200 mg, single) Sources: Page: p.319 |
unhealthy, 40+/-10 n = 289 Health Status: unhealthy Condition: Migraine Age Group: 40+/-10 Sex: M+F Population Size: 289 Sources: Page: p.319 |
Dizziness | Disc. AE | 2 mg single, oral Recommended Dose: 2 mg Route: oral Route: single Dose: 2 mg Co-administed with:: caffeine, p.o(200 mg, single) Sources: Page: p.319 |
unhealthy, 40+/-10 n = 289 Health Status: unhealthy Condition: Migraine Age Group: 40+/-10 Sex: M+F Population Size: 289 Sources: Page: p.319 |
Dyspnoea | Disc. AE | 2 mg single, oral Recommended Dose: 2 mg Route: oral Route: single Dose: 2 mg Co-administed with:: caffeine, p.o(200 mg, single) Sources: Page: p.319 |
unhealthy, 40+/-10 n = 289 Health Status: unhealthy Condition: Migraine Age Group: 40+/-10 Sex: M+F Population Size: 289 Sources: Page: p.319 |
Fatigue | Disc. AE | 2 mg single, oral Recommended Dose: 2 mg Route: oral Route: single Dose: 2 mg Co-administed with:: caffeine, p.o(200 mg, single) Sources: Page: p.319 |
unhealthy, 40+/-10 n = 289 Health Status: unhealthy Condition: Migraine Age Group: 40+/-10 Sex: M+F Population Size: 289 Sources: Page: p.319 |
Hypersensitivity | Disc. AE | 2 mg single, oral Recommended Dose: 2 mg Route: oral Route: single Dose: 2 mg Co-administed with:: caffeine, p.o(200 mg, single) Sources: Page: p.319 |
unhealthy, 40+/-10 n = 289 Health Status: unhealthy Condition: Migraine Age Group: 40+/-10 Sex: M+F Population Size: 289 Sources: Page: p.319 |
Migraine aggravated | Disc. AE | 2 mg single, oral Recommended Dose: 2 mg Route: oral Route: single Dose: 2 mg Co-administed with:: caffeine, p.o(200 mg, single) Sources: Page: p.319 |
unhealthy, 40+/-10 n = 289 Health Status: unhealthy Condition: Migraine Age Group: 40+/-10 Sex: M+F Population Size: 289 Sources: Page: p.319 |
Tachycardia | Disc. AE | 2 mg single, oral Recommended Dose: 2 mg Route: oral Route: single Dose: 2 mg Co-administed with:: caffeine, p.o(200 mg, single) Sources: Page: p.319 |
unhealthy, 40+/-10 n = 289 Health Status: unhealthy Condition: Migraine Age Group: 40+/-10 Sex: M+F Population Size: 289 Sources: Page: p.319 |
Tinnitus | Disc. AE | 2 mg single, oral Recommended Dose: 2 mg Route: oral Route: single Dose: 2 mg Co-administed with:: caffeine, p.o(200 mg, single) Sources: Page: p.319 |
unhealthy, 40+/-10 n = 289 Health Status: unhealthy Condition: Migraine Age Group: 40+/-10 Sex: M+F Population Size: 289 Sources: Page: p.319 |
Urticaria | Disc. AE | 2 mg single, oral Recommended Dose: 2 mg Route: oral Route: single Dose: 2 mg Co-administed with:: caffeine, p.o(200 mg, single) Sources: Page: p.319 |
unhealthy, 40+/-10 n = 289 Health Status: unhealthy Condition: Migraine Age Group: 40+/-10 Sex: M+F Population Size: 289 Sources: Page: p.319 |
Vagal reaction | Disc. AE | 2 mg single, oral Recommended Dose: 2 mg Route: oral Route: single Dose: 2 mg Co-administed with:: caffeine, p.o(200 mg, single) Sources: Page: p.319 |
unhealthy, 40+/-10 n = 289 Health Status: unhealthy Condition: Migraine Age Group: 40+/-10 Sex: M+F Population Size: 289 Sources: Page: p.319 |
Vertigo | Disc. AE | 2 mg single, oral Recommended Dose: 2 mg Route: oral Route: single Dose: 2 mg Co-administed with:: caffeine, p.o(200 mg, single) Sources: Page: p.319 |
unhealthy, 40+/-10 n = 289 Health Status: unhealthy Condition: Migraine Age Group: 40+/-10 Sex: M+F Population Size: 289 Sources: Page: p.319 |
Lightheadedness | 2.4% Disc. AE |
2 mg single, oral Recommended Dose: 2 mg Route: oral Route: single Dose: 2 mg Sources: Page: p.2 |
unhealthy n = 41 Health Status: unhealthy Condition: Migraine Sex: M+F Population Size: 41 Sources: Page: p.2 |
Nausea | 2.4% Disc. AE |
2 mg single, oral Recommended Dose: 2 mg Route: oral Route: single Dose: 2 mg Sources: Page: p.2 |
unhealthy n = 41 Health Status: unhealthy Condition: Migraine Sex: M+F Population Size: 41 Sources: Page: p.2 |
Overview
CYP3A4 | CYP2C9 | CYP2D6 | hERG |
---|---|---|---|
OverviewOther
Other Inhibitor | Other Substrate | Other Inducer |
---|---|---|
Drug as perpetrator
Target | Modality | Activity | Metabolite | Clinical evidence |
---|---|---|---|---|
yes [Ki 13 uM] |
Drug as victim
Target | Modality | Activity | Metabolite | Clinical evidence |
---|---|---|---|---|
yes | yes (co-administration study) Comment: Coadministration of ergotamine with potent CYP 3A4 inhibitors (ritonavir, nelfinavir, indinavir, erythromycin, clarithromycin, and troleandomycin) has been associated with acute ergot toxicity (ergotism) characterized by vasospasm and ischemia of the extremities |
PubMed
Title | Date | PubMed |
---|---|---|
A case of multiple arterial thromboses after oral contraceptives and ergotamine. | 1967 Apr |
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[Severe generalized arteriospasm after a minimal therapeutic dose of ergotamine]. | 1972 Dec 14 |
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[Severe arterial spasms after the use of Ergotamine]. | 1972 Feb 8 |
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[Spasms of the main muscular arteries in the extremities following ingestion of ergotamine-containing drugs]. | 1973 Apr 20 |
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Arterial spasm associated with oral ergotamine therapy. | 1973 Dec |
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Ergotism. Unilateral brachial artery thrombosis secondary to ergotamine tartrate. | 1973 Jun |
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[Acute ischemia of the lower limbs due to ergotamine-induced arteriospasm]. | 1973 Nov 30 |
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[Chronic ergotamine poisoning after migraine treatment]. | 1974 |
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Ergotamine-induced venous thrombosis. | 1974 Apr |
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Ischaemic lateral popliteal nerve palsy due to ergot intoxication. | 1974 Dec |
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[Ergotamine as a cause of arterial insufficiency]. | 1974 Oct 10 |
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[Letter: Coronary spasm following ergotamine medication]. | 1975 Sep 5 |
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Peripheral vascular spasm due to ergotamine tartrate. | 1977 Dec |
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[Alarming course of drug-induced ergotism following prolonged use of ergotamine tartatare]. | 1977 Feb 18 |
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Myocardial ischaemia in migraine sufferers taking ergotamine. | 1978 Jan |
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[Bilateral vascular papillitis following ergotamin medication (author's transl)]. | 1978 Nov |
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Angina pectoris and sudden death in the absence of atherosclerosis following ergotamine therapy for migraine. | 1979 Jul |
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[Non-invasive method for recognition of coronary artery spasm: 201thallium sequential scintigraphy of the myocardium after ergotamine provocation (author's transl)]. | 1980 Apr 11 |
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Reversal of ergotamine-induced arteriospasm by mechanical intra-arterial dilatation. | 1980 Dec 13 |
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Acute myocardial infarction induced by ergotamine tartrate: possible role of coronary arterial spasm. | 1981 Jun |
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[A case report of acute myocardial infarction induced by ergotamine tartrate (author's transl)]. | 1981 Mar |
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Ergotamine abuse: results of ergotamine discontinuation, with special reference to the plasma concentrations. | 1982 Dec |
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Arterial complications of migraine treatment with methysergide and parenteral ergotamine. | 1982 Jul 24 |
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Myocardial infarction following administration of sublingual ergotamine. | 1982 Sep |
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[Myocardial infarct during ergotamine medication in a young man with normal coronary arteries]. | 1983 Apr 22 |
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[Ergotamine-induced spasm of the extremities with dorsalis pedis gangrene]. | 1983 Jun 10 |
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[Ergotism causing peripheral arterial occlusion in the hand]. | 1983 Mar |
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Screening for new compounds with antiherpes activity. | 1984 Oct |
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Reversible cerebral arteriopathy associated with the administration of ergot derivatives. | 1984 Sep |
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[Ergotism with cerebral complications. Case report and review of the literature]. | 1986 Apr 5 |
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Ergotamine-induced peripheral ischaemia reversed by oral thymoxamine hydrochloride. | 1986 Jan |
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Amelioration of ergotamine withdrawal symptoms with naproxen. | 1987 Mar |
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[Myocardial infarct caused by an ergotamine tartrate-troleandomycin combination]. | 1988 Sep-Oct |
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St. Anthony's fire: a medieval disease in modern times: case history. | 1989 Oct |
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[Generalized brain edema and cerebral infarct in ergotamine abuse: imaging by computerized tomography, magnetic resonance tomography and angiography]. | 1989 Sep |
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Mitral and aortic valve disease associated with ergotamine therapy for migraine. Report of two cases and review of literature. | 1990 Jan |
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Ergotamine headache mistaken for temporal arteritis. | 1990 Sep |
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Two members of a distinct subfamily of 5-hydroxytryptamine receptors differentially expressed in rat brain. | 1993 Apr 15 |
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[Daily chronic headache in patients with migraine induced by abuse of ergotamine-analgesics: response due to a protocol of outpatient treatment]. | 1993 Aug-Sep |
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Ergotamine-induced fetal stress: review of side effects of ergot alkaloids during pregnancy. | 1993 Sep |
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[Ergotamine-induced rectal lesions in asymptomatic patients]. | 1994 |
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Variant angina complicating ergot therapy of migraine. | 1994 Apr |
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Cloning and characterisation of the human 5-HT5A serotonin receptor. | 1994 Dec 5 |
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Ergot induced peripheral vascular insufficiency, non-interventional treatment. | 1994 Mar |
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Ergotamine-induced headache can be sustained by sumatriptan daily intake. | 1994 Oct |
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Prinzmetal-variant angina in a patient using zolmitriptan and citalopram. | 2010 Feb |
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Cytotoxicity and accumulation of ergot alkaloids in human primary cells. | 2011 Apr 11 |
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Structural features for functional selectivity at serotonin receptors. | 2013 May 3 |
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Structural basis for molecular recognition at serotonin receptors. | 2013 May 3 |
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FDA-approved drugs and other compounds tested as inhibitors of human glutathione transferase P1-1. | 2013 Sep 5 |
Patents
Sample Use Guides
MIGERGOT - ergotamine tartrate and caffeine rectal suppository.
One suppository at start of attack; second suppository after 1 hour, if needed for full relief. Two suppositories is the maximum dose for an individual attack.
Cafergot (Ergotamine tartrate 1 mg and Caffeine 100 mg Tablets)
First attack: The first time Cafergot is taken, an initial dose of 2 Cafergot tablets orally, is recommended. If relief is not obtained within half an hour, a further tablet should be administered; this may be repeated at half-hourly intervals, but the maximum daily dose of 6 tablets should not be exceeded. Subsequent attacks: If the pain persists, take 1 tablet every half an hour up to the maximum daily dose of 6 tablets. The maximum weekly dose is 10 tablets.
ERGOMAR SUBLINGUAL- ergotamine tartrate tablet
For best results, dosage should start at the first sign of an attack. Early Administration Gives Maximum Effectiveness. At the first sign of an attack or to relieve symptoms after onset of an attack, one 2 mg tablet is placed under the tongue. Another tablet should be taken at half-hour intervals thereafter, if necessary, but dosage must not exceed three tablets in any 24hour period. Total weekly dosage should not exceed five tablets (10 mg) in any one week. Ergomar® Sublingual Tablets should not be used for chronic daily administration.
Route of Administration:
Other
In Vitro Use Guide
Sources: https://www.ncbi.nlm.nih.gov/pubmed/3569604
The bovine anterior pituitary cells were implanted on culture tubes using D-valine minimal essential medium with serum to suppress the overgrowth of fibroblasts and then maintained in L-valine Dulbecco's modified Eagle medium. (3H)-Uridine uptake by these cells was suppressed by ergotamine at a concentration varing from 1-10 uM
Substance Class |
Chemical
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Record UNII |
PR834Q503T
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Validated (UNII)
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Classification Tree | Code System | Code | ||
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DEA NO. |
8676
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NDF-RT |
N0000007621
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NCI_THESAURUS |
C47794
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NDF-RT |
N0000007621
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WHO-ATC |
N02CA72
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WHO-VATC |
QN02CA52
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WHO-ATC |
N02CA02
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LIVERTOX |
363
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NDF-RT |
N0000175766
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WHO-ATC |
N02CA52
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WHO-VATC |
QN02CA02
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WHO-VATC |
QN02CA72
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1043
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113-15-5
Created by
admin on Wed Jul 05 22:31:22 UTC 2023 , Edited by admin on Wed Jul 05 22:31:22 UTC 2023
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C61751
Created by
admin on Wed Jul 05 22:31:22 UTC 2023 , Edited by admin on Wed Jul 05 22:31:22 UTC 2023
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SUB06598MIG
Created by
admin on Wed Jul 05 22:31:22 UTC 2023 , Edited by admin on Wed Jul 05 22:31:22 UTC 2023
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149
Created by
admin on Wed Jul 05 22:31:22 UTC 2023 , Edited by admin on Wed Jul 05 22:31:22 UTC 2023
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64318
Created by
admin on Wed Jul 05 22:31:22 UTC 2023 , Edited by admin on Wed Jul 05 22:31:22 UTC 2023
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DB00696
Created by
admin on Wed Jul 05 22:31:22 UTC 2023 , Edited by admin on Wed Jul 05 22:31:22 UTC 2023
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D004878
Created by
admin on Wed Jul 05 22:31:22 UTC 2023 , Edited by admin on Wed Jul 05 22:31:22 UTC 2023
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DTXSID9043774
Created by
admin on Wed Jul 05 22:31:22 UTC 2023 , Edited by admin on Wed Jul 05 22:31:22 UTC 2023
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PR834Q503T
Created by
admin on Wed Jul 05 22:31:22 UTC 2023 , Edited by admin on Wed Jul 05 22:31:22 UTC 2023
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Ergotamine
Created by
admin on Wed Jul 05 22:31:22 UTC 2023 , Edited by admin on Wed Jul 05 22:31:22 UTC 2023
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95090
Created by
admin on Wed Jul 05 22:31:22 UTC 2023 , Edited by admin on Wed Jul 05 22:31:22 UTC 2023
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PR834Q503T
Created by
admin on Wed Jul 05 22:31:22 UTC 2023 , Edited by admin on Wed Jul 05 22:31:22 UTC 2023
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4025
Created by
admin on Wed Jul 05 22:31:22 UTC 2023 , Edited by admin on Wed Jul 05 22:31:22 UTC 2023
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PRIMARY | RxNorm | ||
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100000084579
Created by
admin on Wed Jul 05 22:31:22 UTC 2023 , Edited by admin on Wed Jul 05 22:31:22 UTC 2023
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M4988
Created by
admin on Wed Jul 05 22:31:22 UTC 2023 , Edited by admin on Wed Jul 05 22:31:22 UTC 2023
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PRIMARY | Merck Index | ||
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8223
Created by
admin on Wed Jul 05 22:31:22 UTC 2023 , Edited by admin on Wed Jul 05 22:31:22 UTC 2023
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4076
Created by
admin on Wed Jul 05 22:31:22 UTC 2023 , Edited by admin on Wed Jul 05 22:31:22 UTC 2023
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ERGOTAMINE
Created by
admin on Wed Jul 05 22:31:22 UTC 2023 , Edited by admin on Wed Jul 05 22:31:22 UTC 2023
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204-023-9
Created by
admin on Wed Jul 05 22:31:22 UTC 2023 , Edited by admin on Wed Jul 05 22:31:22 UTC 2023
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CHEMBL442
Created by
admin on Wed Jul 05 22:31:22 UTC 2023 , Edited by admin on Wed Jul 05 22:31:22 UTC 2023
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PRIMARY |
Related Record | Type | Details | ||
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SALT/SOLVATE -> PARENT |
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SALT/SOLVATE -> PARENT |
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TARGET -> AGONIST |
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TARGET -> AGONIST |
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TARGET -> AGONIST |
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Related Record | Type | Details | ||
---|---|---|---|---|
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METABOLITE ACTIVE -> PARENT |
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Related Record | Type | Details | ||
---|---|---|---|---|
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PARENT -> IMPURITY |
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Related Record | Type | Details | ||
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ACTIVE MOIETY |
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