Products
In many countries, drugs containing ergotamine are currently no longer on the market. The active ingredient was available in tablet form in combination with caffeine, among other products (Cafergot), but was withdrawn from the market in 2014. Products containing ergotamine were first launched in the 1920s (Gynergen).
Structure and properties
Ergotamine (C33H35N5O5, Mr = 581.7 g/mol) is an ergot alkaloid and a natural constituent of the sclerotium of . It is present in drugs as ergotamine tartrate, a white crystalline powder, or as colorless crystals. Ergotamine was first isolated in 1918 by Arthur Stoll at Sandoz in Basel.
Effects
Ergotamine (ATC N02CA52) has vasoconstrictive, uterine contractile, and emetic properties. The effects are due to binding to serotonin and dopamine receptors and to alpha-adrenoceptors. Caffeine added to the tablets increases the absorption of ergotamine and also has vasoconstrictor effects itself.
Indications
For the treatment of acute migraine attacks (classic migraine) with or without aura.
Dosage
According to the SmPC. The tablets are taken at the onset of the first signs of migraine. During use, it is necessary to observe the maximum daily dose, which should not be exceeded. Ergotamine should be administered only as needed, not on a regular basis, and not for migraine prophylaxis.
Contraindications
- Hypersensitivity
- Vascular disease
- Uncontrolled arterial hypertension
- Severe hepatic or renal dysfunction
- Sepsis
- State of shock
- Hemiplegic or basilar migraine
- Pregnancy, lactation
- Concurrent treatment with vasoconstrictive agents.
- Concurrent treatment with potent CYP3A inhibitors.
Full precautions can be found in the drug label.
Interactions
Ergotamine is metabolized by CYP3A. It should not be co-administered with potent CYP3A inhibitors because plasma concentrations may increase. Also contraindicated is combination with vasoconstrictor drugs.
Adverse effects
The most common potential adverse effects include dizziness, nausea, and vomiting. Occasional adverse effects include diarrhea, cyanosis, sensory disturbances such as tingling or numbness, visual disturbances, pain and weakness in the extremities, and peripheral vasoconstriction. An overdose results in intoxication, severe vasoconstriction, and is potentially life-threatening (ergotism).
