Ergotamine Tartrate / Caffeine

What it is and how it works

Ergotamine is an ergot alkaloid acting as a partial agonist at 5-HT1B/1D, alpha-adrenergic and dopamine receptors, causing constriction of dilated cranial blood vessels and inhibition of trigeminal neurotransmission. Caffeine enhances the absorption of ergotamine and contributes vasoconstrictor effects.

Indications

Treatment of acute migraine attacks (with or without aura) and cluster headache, generally in patients who do not respond to analgesics or triptans; not for prophylaxis.

Dosage and administration (summary)

Oral (ergotamine 1 mg / caffeine 100 mg): 1–2 tablets at the onset of the attack, then 1 tablet every 30 minutes if needed, up to a maximum of 6 tablets per attack and 10 tablets per week; courses should not be repeated within 4 days.

Contraindications

Peripheral vascular disease, coronary heart disease, uncontrolled hypertension, Raynaud’s syndrome, severe hepatic or renal impairment, sepsis, hemiplegic or basilar migraine, porphyria; concomitant potent CYP3A4 inhibitors (macrolides, HIV protease inhibitors, azole antifungals) or triptans; pregnancy and breast-feeding.

Warnings and precautions

Overuse may cause ergotism (severe peripheral vasoconstriction, gangrene), medication-overuse headache and dependence; do not exceed recommended doses. Fibrotic reactions (pleural, retroperitoneal) have been reported with long-term use. Nausea and vomiting are common; triptans should not be given within 24 hours of ergotamine.

Pregnancy

Contraindicated in pregnancy because of its oxytocic and vasoconstrictor effects.

Storage and supply

Store below 25 °C, protected from light and moisture.

Source: reference summary prepared from the EU SmPC/EPAR, BNF and WHO Model Formulary. The approved product information in Iran governs.