Ergotamine
- Atc Codes:N02CA02
- CAS Codes:379-79-3#113-15-5
- PHARMGKB ID:379-79-3#113-15-5
Table of contents
- Brand Names
- Drug Combinations
- Chemistry
- Pharmacologic Category
- Mechanism of Action
- Therapeutic Use
- Pregnancy and Lactation Implications
- Contraindications
- Warnings and Precautions
- Adverse Reactions
- Toxicological Effects
- Caution and personalized dose adjustment in patients with the following genotypes
- Other genes that may be involved
- Substrate of
- Inhibits
- Drug Interactions
- Nutrition/Nutraceutical Interactions
- Dosage
- Pharmacokinetics and Pharmacodynamics
- Special Considerations
Brand Names
Europe
Germany: Ergo-Kranit Migräne; Hungary: Ergam; Italy: Ergota T, Ergotan IM; Luxembourg: Ergosanol Spezial N; Poland: Ergotaminum.
North America
USA: Ergomar.
Drug combinations
Ergotamine and Caffeine
Ergotamine and L-Lysine
Ergotamine, Atropine, and Phenobarbital
Ergotamine, Caffeine, and Dipyrone
Ergotamine, Caffeine, and Ibuprofen
Ergotamine, Caffeine, and Terapirol
Ergotamine, Clonixin, and Cyproheptadine
Ergotamine, Acetaminophen, Caffeine, and Chlorpheniramine
Ergotamine, Caffeine, Dipyrone, and Metoclopramide
Ergotamine, Caffeine, Chlorpheniramine, Dipyrone, and Metoclopramide
Chemistry
Ergotamine Tartrate: (C~33~H~35~N~5~O~5~)~2~ C~4~H~6~O~6~ Mw: 1313.41. Ergotaman-3′,6′,18-trione, 12′-hydroxy-2′-methyl-5′-(phenylmethyl)-, (5’α)-, [R-(R*,R*)]-2,3-dihydroxybutanedioate (2:1). CAS-379-79-3; CAS-113-15-5 (ergotamine).
Pharmacologic Category
Sympatholytic (Adrenergic Blocking) Agents; Non-selective α-Adrenergic Blocking Agents; Ergot Derivative. (ATC-Code: N02CA02).
Mechanism of action
α-Adrenergic blocking activity, direct stimulation of peripheral and cranial vascular smooth muscle, and serotonin antagonist activity. Mechanism by which ergotamine aborts vascular headaches is probably direct vasoconstriction of dilated carotid artery bed.
Therapeutic use
Prevention or abortion of vascular headaches (e.g. migraine, cluster headaches), when used alone or in fixed combination with caffeine. Amelioration of vasomotor symptoms (e.g. hot flushes, sweating, restlessness, insomnia) in menopausal women, when used in fixed combination with belladonna alkaloids and phenobarbital. Used for its autonomic effects in the treatment of various cardiovascular and GI disorders (when given in fixed combination with belladonna alkaloids and phenobarbital); has generally been replaced by more specific agents for these uses.
Pregnancy and lactiation implications
May cause prolonged constriction of uterine vessels and/or increased myometrial tone leading to reduced placental blood flow. This has contributed to fetal growth retardation in animals. Ergotamine is excreted in breast milk and may cause vomiting, diarrhea, weak pulse, and unstable blood pressure in the nursing infant.
Unlabeled use
Contraindications
Hypersensitivity to ergotamine or any component of the formulation. Peripheral vascular disease. Hepatic or renal disease. Coronary artery disease. Hypertension. Sepsis. Strong CYP3A4 inhibitors. Pregnancy.
Warnings and precautions
Ergot alkaloids have been associated with fibrotic valve thickening (e.g. aortic, mitral, tricuspid); usually associated with long-term, chronic use. Vasospasm or vasoconstriction can occur, possibly resulting in decreased cerebral blood flow, ECG changes, and hypertension. Sustained vasoconstriction may also lead to ischemic colitis, intermittent claudication, aggravation of angina, or precipitation of MI (avoid use in patients at risk or predisposed to vascular effects of ergot alkaloids). Ergot alkaloid use may result in ergotism (intense vasoconstriction) resulting in peripheral vascular ischemia and possible gangrene. Rare cases of pleural and/or retroperitoneal fibrosis reported with prolonged daily use. Possible serious and/or life-threatening cerebral and/or peripheral ischemia when administered concomitantly with potent CYP3A4 inhibitors (concomitant use contraindicated). Use with extreme caution or avoid use in the elderly (due to vasoconstrictive properties and cardiovascular adverse effects). Discontinuation after extended use may result in withdrawal symptoms (e.g. rebound headache).