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caffeine/ergotamine (Cafergot, Ercaf, Wigraine)

Indication: prevention or treatment of vascular headaches. Contraindications: 1) peripheral vascular disease 2) hepatic or renal disease 3) hypertension 4) peptic ulcer disease 5) sepsis 6) avoid use during pregnancy pregnancy-category X safety in lactation - Dosage: 1 mg ergotamine + 100 mg caffeine. - 2 tabs PO at onset, then 1 every 30 min - up to 6 tabs/24 hours Suppositories: (2 mg ergotamine + 100 mg caffeine). - up to 2/attack. Pharmacokinetics: 1) absorption increases with caffeine co-administration 2) metabolized by the liver 3) metabolites eliminated in the bile Adverse effects: 1) common (> 10%) - localized edema - numbness & paresthesias of fingers & toes - drowsiness - dizziness - dry mouth - diarrhea - nausea/vomiting 2) less common (1-10%) - angina, tachycardia, bradycardia, claudication, weakness 3) other - arterial spasm - vasoconstriction - rebound headache may occur with sudden withdrawal Drug interactions: 1) propranolol in combination may result in severe vasoconstriction 2) erythromycin & clarithromycin in combination may result in ergot toxicity Mechanism of action: 1) direct stimulation of vascular smooth muscle to vasoconstrict peripheral & cerebral vessels 2) antagonizes serotonin activity 3) caffeine is an adjunct agent also with vasoconstrictive actions on cerebral vessels

Interactions

drug interactions

General

antimigraine combination

Database Correlations

PUBCHEM cid=125740

References

  1. The Pharmacological Basis of Therapeutics, 9th ed. Gilman et al, eds. Permagon Press/McGraw Hill, 1996
  2. Drug Information & Medication Formulary, Veterans Affairs, Central California Health Care System, 1st ed., Ravnan et al eds, 1998
  3. Kaiser Permanente Northern California Regional Drug Formulary, 1998

Components

caffeine (NoDoz, Vivarin) ergotamine (Ergostat)