Drug intelligence / Profile preview

ergotamine + caffeine

Development stage
Approved
Lead developer
Sandoz
Modality
Small Molecules
Administration
Oral, Rectal
01

Overview

Ergotamine + caffeine is a fixed-dose combination drug used to treat or prevent vascular headaches, including migraine and cluster headaches. Ergotamine is an ergot alkaloid that acts as an alpha-adrenergic blocker with direct stimulatory effects on the smooth muscle of peripheral and cranial blood vessels, leading to vasoconstriction. It also exhibits serotonin antagonism. Caffeine enhances the vasoconstrictive effect of ergotamine and increases its absorption without requiring higher doses of ergotamine itself. The combination works by narrowing dilated blood vessels in the head that are believed to cause headache pain[1][3][4][5][6]. This medication is available as oral tablets (typically 1 mg ergotamine/100 mg caffeine per tablet) or rectal suppositories (2 mg ergotamine/100 mg caffeine per suppository)[7][8]. Brand name Cafergot has been discontinued in many markets but generic versions remain available[1][7].

Brand names
CafergotMigergot
Other names
caffeine and ergotamineergotamine/caffeine
02

Targets

ADORA2A (Adenosine A₂A Receptor)HTR1B (5-Hydroxytryptamine Receptor 1B)HTR1D (5-hydroxytryptamine receptor 1D)ADORA1 (Adenosine receptor A1 subtype)ADRA1A (α1A)PDE (Phosphodiesterase family)CYP1A2 (Cytochrome P450 1A2)

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