Ergotamine/caffeine

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Ergotamine/caffeine
Combination of
Ergotamine	vasoconstrictor, neurotransmitter agonist and antagonist
Caffeine	vasoconstrictor, phosphodiesterase inhibitor
Clinical data
Trade names	Cafergot, Migergot, others
AHFS/Drugs.com	Multum Consumer Information
MedlinePlus	a601048
License data	US DailyMed: Ergotamine and caffeine
Pregnancy category	AU: C Contraindicated
Routes of administration	By mouth, rectal
ATC code	N02CA52 (WHO)
Legal status
Legal status	US: ℞-only^[1]^[2]
Identifiers
CAS Number	69063-86-1
KEGG	D07600

Ergotamine/caffeine, sold under the brand name Cafergot among others, is a fixed-dose combination medication used for the treatment of migraine. It contains ergotamine, as the tartrate, an alpha adrenergic blocking agent; and caffeine, a cranial vasoconstrictor.^[3]

Ergotamine/caffeine is available as a generic medication.

Medical uses

Ergotamine/caffeine is indicated as therapy to abort or prevent vascular headache.^[1]^[2]

Mechanism of action

Ergotamine binds to 5HT 1b/d receptors.^[4] This along with binding to other serotonergic and dopaminergic receptors is their presumed mechanism of action in treating migraine.^[4]^[5]

Adverse effects

Because the vasoconstrictive effects of ergotamine and caffeine are not selective for the brain, adverse effects due to systemic vasoconstriction can occur. Cold feet or hands, angina pectoris, myocardial infarction,^[6] or dizziness are some examples.

It has also been shown to be associated with mitral valve stenosis. ^[7]

References

^ ^a ^b "Cafergot- ergotamine tartrate and caffeine tablet, film coated". DailyMed. U.S. National Library of Medicine. Archived from the original on 16 January 2014.
^ ^a ^b "Migergot- ergotamine tartrate and caffeine suppository". DailyMed. 29 November 2022. Retrieved 18 May 2024.
^ Diener HC, Jansen JP, Reches A, Pascual J, Pitei D, Steiner TJ (2002). "Efficacy, tolerability and safety of oral eletriptan and ergotamine plus caffeine (Cafergot) in the acute treatment of migraine: a multicentre, randomised, double-blind, placebo-controlled comparison". European Neurology. 47 (2): 99–107. doi:10.1159/000047960. PMID 11844898. S2CID 72629130.
^ ^a ^b "Acute treatment of migraine in adults". UpToDate. Wolters Kluwer. 15 January 2018. Retrieved 27 March 2018.
^ Fanciullacci M, Granchi G, Sicuteri F (November 1976). "Ergotamine and methysergide as serotonin partial agonists in migraine". Headache. 16 (5): 226–231. doi:10.1111/j.1526-4610.1976.hed1605226.x. PMID 977328. S2CID 45861917.
^ Olesen J, Goadsby PJ, Ramadan NM, Tfelt-Hansen P, Michael K, Welch A, eds. (2006). The Headaches (3rd ed.). Lippincott Williams and Wilkins. p. 463. ISBN 978-0781754002.
^ Austin SM, el-Hayek A, Comianos M, Tamulonis DJ (October 1993). "Mitral valve disease associated with long-term ergotamine use". Southern Medical Journal. 86 (10): 1179–1181. doi:10.1097/00007611-199310000-00024. PMID 8211344.

Antimigraine preparations (N02C)

Triptans	Almotriptan Avitriptan Donitriptan Eletriptan Frovatriptan Naratriptan Rizatriptan Sumatriptan Zolmitriptan
Ditans	Alniditan^§ Lasmiditan

Others

CGRP-R antagonists

Others

Paracetamol^#
Amidrine

Prophylactic

Calcium channel blockers	Dotarizine Lomerizine Verapamil Flunarizine
Progestogens	Flumedroxone acetate
Sympatholytics	Beta blockers Propranolol^# Timolol Clonidine
Tricyclic antidepressants	Amitriptyline Nortriptyline Imipramine
Anticonvulsants	Carbamazepine Oxcarbazepine Topiramate Valproate
Anti-CGRP/CGRP-R mAbs	Eptinezumab Erenumab Fremanezumab Galcanezumab
CGRP-R antagonists	Atogepant Rimegepant

^#WHO-EM
^‡Withdrawn from market
Clinical trials:
- ^†Phase III
- ^§Never to phase III

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