Ergotamine is an α-adrenergic blocker with a direct stimulating effect on the smooth muscle of peripheral and cranial blood vessels, it also depresses central vasomotor centers.

Caffeine is also a cranial vasoconstrictor.

Ergotamine Tartrate and caffeine are indicated as therapy to abort or prevent vascular headache; e.g., migraine, migraine variants or so-called “histaminic cephalalgia.”

Usual Adult Dose for Cluster Headache:

Oral, Sublingual: 2 mg ergotamine in fixed combination with caffeine given as quickly as possible after the first symptom of headache. Additional 1 mg doses can be given every 30 minutes until the headache has been aborted or until a total dose of 6 mg has been reached or 10 mg/week.

Rectal: 2 mg ergotamine in fixed combination with caffeine given as quickly as possible after the first symptom of headache. An additional 2 mg dose can be given 1 hour later if the first dose fails to abort the headache. The total dose should not exceed 4 mg/attack or 10 mg/week.

Usual Adult Dose for Migraine:

Oral, Sublingual: 2 mg ergotamine in fixed combination with caffeine given as quickly as possible after the first symptom of headache. Additional 1 mg doses can be given every 30 minutes until the headache has been aborted or until a total dose of 6 mg has been reached or 10 mg/week.

Rectal: 2 mg ergotamine in fixed combination with caffeine given as quickly as possible after the first symptom of headache. An additional 2 mg dose can be given 1 hour later if the first dose fails to abort the headache. The total dose should not exceed 4 mg/attack or 10 mg/week.

Not to be used with potent inhibitors of CYP3A4 and protease inhibitors. Hyperthyroidism, renal or hepatic impairment. Pre existing vascular disease including coronary disease, obliterative vascular disease, angina, claudication, peripheral ischaemia, Raynaud's syndrome and hypertension. Not to be used when there is sepsis. Pregnancy and lactation.

Increased BP, hypotension, rapid and weak pulse, palpitations, arrhythmias, precordial pain, coronary infarction, fibrotic thickening of the heart valves. Cerebral ischaemia and thrombosis, blurred vision, sleep disturbances, urinary retention, muscle cramps and joint pains.

GI symptoms such as nausea, vomiting, constipation, abdominal pain. Dysaesthesia, paraesthesia, formication, tremor, convulsions, headache, extrapyramidal effects. Anxiety, depression, confusion, hallucinations, psychomotor impairment.

Overdose Effects

Acute overdosage:

• Symptoms: Nausea, vomiting, diarrhoea, extreme thirst, coldness, weakness, tingling and itching of the skin, rapid and weak pulse, hypotension, shock, confusion, convulsions and unconsciousness. BP may be difficult to measure; may result in fatalities. Further symptoms of peripheral vasoconstriction or CV disturbances may occur but be delayed.
• Treatment includes using activated charcoal to reduce absorption. General supportive measures should be instituted. IV vasodilators such as sodium nitroprusside infusion may be required to relieve vasospasm. Peritoneal dialysis and forced diuresis may be used to remove ergotamine from the body.

Chronic overdosage:

• Symptoms: Peripheral ischaemia of the extremities, especially the feet and legs. Gangrene may develop in the toes and fingers. Anginal pain, tachycardia or bradycardia and BP fluctuations may occur. Excessive use may lead to pleural and peritoneal fibrosis. Rebound headache may occur and is a major withdrawal symptom following the development of ergotamine dependence.
• Treatment: IV vasodilators e.g. nitroprusside and nitroglycerin may be used to re-establish normal blood flow. Captopril may be used to reverse the effects of chronic overdosage with ergotamine.

Not to be taken regularly or used for migraine prophylaxis. Increased risk of arterial constriction and other symptoms of ergotism. Discontinue treatment when symptoms of arterial occlusion occur e.g. numbness and tingling of the extremities. Caution when used in patients with infective hepatitis, cardiac disease or anaemia. GI tract obstructive disease, glaucoma, prostatic hypertrophy or urinary retention may be worsened by cyclizine. May increase risk of retroperitoneal and/or pleuropulmonary fibrosis. Not recommended for use with other vasoconstrictors. Elderly.

Use in Special Populations

Pediatric Use: Safety and effectiveness in pediatric patients have not been established.

Renal Dose Adjustments: Contraindicated in patients with renal dysfunction

Liver Dose Adjustments: Contraindicated in patients with liver dysfunction

Pregnancy & Lactation

Pregnancy: Category X. This medicine should not be used during pregnancy as it may be harmful to the unborn baby.

Lactation: Significant amounts of this medicine may pass into breast milk. It should not be used by breastfeeding mothers as it may be harmful to the nursing infant.