Land: Canada
Språk: engelsk
Kilde: Health Canada
ERGOTAMINE TARTRATE; CAFFEINE
NOVARTIS PHARMACEUTICALS CANADA INC
N02CA52
ERGOTAMINE, COMBINATIONS EXCL. PSYCHOLEPTICS
2MG; 100MG
SUPPOSITORY
ERGOTAMINE TARTRATE 2MG; CAFFEINE 100MG
RECTAL
12
Prescription
SYMPATHOLYTIC (ADRENERGIC BLOCKING) AGENTS
Active ingredient group (AIG) number: 0203679001; AHFS:
CANCELLED POST MARKET
2006-11-13
PRESCRIBING INFORMATION PR CAFERGOT ® * (Ergotamine tartrate and Caffeine) Tablets USP and Suppositories USP MIGRAINE THERAPY Novartis Pharmaceuticals Canada Inc. DATE OF REVISION: Dorval, Quebec January 10, 2007 H9S 1A9 Pr CAFERGOT* is a registered trademark. Control number: 104759 1 NAME OF DRUG PR CAFERGOT ® * Ergotamine tartrate and Caffeine Tablets USP and Suppositories USP THERAPEUTIC CLASSIFICATION Migraine Therapy CLINICAL PHARMACOLOGY The mechanism of action of Cafergot in relieving migraine is not completely understood. Ergotamine is an agonist at serotoninergic 5-HT1 receptors (5-HT 1A , 5-HT 1B , 5-HT 1D , and 5-HT 1F ), 5-HT 2 receptors, adrenergic receptors, and dopaminergic D 2 receptors. At higher doses, ergotamine is an alpha adrenergic blocking agent with a direct stimulating effect on the smooth muscle of peripheral and cranial blood vessels. In comparison to dihydrogenated ergotamine, the adrenergic blocking actions of ergotamine tartrate are less pronounced and vasoconstriction actions are greater. The addition of caffeine to ergotamine tartrate facilitates the absorption of ergotamine when administered orally or rectally and increases migraine pain relief effects. Ergotamine is rapidly and incompletely (approximately 62% of the oral dose) absorbed by the gastro-intestinal tract. Peak plasma levels are reached about 2 hours after ingestion. Ergotamine is extensively metabolized in the liver. The bioavailability of unchanged drug is about 2% when the drug is administered orally and 5% when it is administered by the rectal route. It has been suggested that the therapeutic effects of the drug are partially due to active metabolites. Protein 2 bindings amounts to 98%. Parent drug and metabolites are mainly excreted with the bile. Their elimination from plasma is biphasic with a half-life of 2.7 hours and 21 hours respectively. Caffeine is rapidly and almost completely absorbed; it is to a large extent metabolized. The metabolites are mainly excreted in the urine. Plasma elimination half-life is Les hele dokumentet