Cyclizine, Ergotamine and Caffeine

Antimigraine Preparations · Ergot alkaloid/Piperazine derivative/Xanthine

Indications

Acute migraine attack.

Dosage

Adults: Should be taken as soon as possible after the first warning of an attack of migraine and repeated if necessary at the prescribed intervals. The usual initial dose is one tab. Additional dose of one tab may then be required at half- hourly intervals. Not more than 4 tablets should be taken in any one attack. Not more than 6 tablets (12 mg ergotamine) should be given in any one wk. Children: Not recommended.

Adverse Effects

Rebound headache, peripheral ischaemia, abdominal pain, drowsiness, dry mouth, GI upset, dizziness, arterial insufficiency, cold extremities (discontinue), retroperitoneal, pleuropulmonary and cardiac valve fibrosis.

Risk Factor (Pregnancy/Lactation)

Pregnancy: Contraindicated in pregnancy. Lactation: Contraindicated or not recommended. Contraindications: Sepsis, coronary, peripheral or occlusive vascular disease, severe hypertension, angina, claudication, Raynaud's syndrome, impaired hepatic or renal function. Hyperthyroidism, porphyria. Precautions: Elderly. Anaemia, prostatic hypertrophy, urinary retention, infective hepatitis, cardiac disease, GI obstruction, glaucoma.

Interactions

Erythromycin, beta-blockers, CNS depressants, CYP3A4 inhibitors, grapefruit juice, alcohol, antiarrhythmics, ciprofloxacin, tetracyclines, phenytoin, antimuscarinics, methysergide, other 5HT1 agonists, diazepam, disulfiram, lithium, nicotine, nitrates, oestrogens, progestogens, sympathomimetics, theophylline, vasoconstrictors.

Advice to Patient

Discontinue medication immediately if there is numbness and tingling of extremities.

Pharmacokinetics

CYCLIZINE: Onset: Within 2 hrs. Duration: 4 hrs. Absorption: Absorbed from GI tract. Metabolism: Hepatic. Half-life elimination: 20 hrs. Time to peak, plasma: Approx. 2 hrs. Excretion: Urine (<1% of total oral dose). ERGOTAMINE: Absorption: Incompletely absorbed from GI tract. Metabolism: Hepatic. Bioavailability: Oral: 1-5%. Half-life elimination: Biphasic. Initial: 2 hrs. Terminal: 21 hrs. Time to peak, plasma: Oral: 1-2 hrs. Excretion: Faeces (mainly). Urine (4%). CAFFEINE: Metabolism: Hepatic. Half-life elimination: Neonates: 72-96 hrs. Children >9 mths and Adults: 5 hrs. Time to peak, serum: Oral: Within 30 mins-2 hrs. Excretion: Neonates =1 mth: 86% excreted unchanged in urine. Infants >1 mth and Adults: In urine, as metabolites.

Compiled by Healify Pharmacy from published drug references. How we compile it →

Always consult a pharmacist or doctor.