Negara: Kanada
Bahasa: Inggris
Sumber: Health Canada
ERGOTAMINE TARTRATE; CAFFEINE
NOVARTIS PHARMACEUTICALS CANADA INC
N02CA52
ERGOTAMINE, COMBINATIONS EXCL. PSYCHOLEPTICS
1MG; 100MG
TABLET
ERGOTAMINE TARTRATE 1MG; CAFFEINE 100MG
ORAL
100
Prescription
SYMPATHOLYTIC (ADRENERGIC BLOCKING) AGENTS
Active ingredient group (AIG) number: 0203679002; AHFS:
CANCELLED POST MARKET
2014-03-31
PRODUCT MONOGRAPH PR CAFERGOT* Ergotamine tartrate and Caffeine Tablets USP MIGRAINE THERAPY Novartis Pharmaceuticals Canada Inc. DATE OF REVISION: Dorval, Quebec November 26, 2012 H9S 1A9 CONTROL NUMBER: 159731 PR CAFERGOT* is a registered trademark. 2 NAME OF DRUG PR CAFERGOT* Ergotamine tartrate and Caffeine Tablets USP THERAPEUTIC CLASSIFICATION Migraine Therapy CLINICAL PHARMACOLOGY The mechanism of action of CAFERGOT* in relieving migraine is not completely understood. Ergotamine is a ligand at serotonergic 5-HT 1 receptors (5-HT 1A , 5-HT 1B , 5-HT 1D , and 5-HT 1F ), 5-HT 2 receptors, adrenergic receptors (α 1 and α 2 ), and dopaminergic receptors (D 1 and D 2 ). The addition of caffeine to ergotamine tartrate facilitates the absorption of ergotamine and may increase migraine pain relief effects. _ _ ERGOTAMINE Absorption Ergotamine is rapidly and incompletely (approximately 62% of the oral dose) absorbed by the gastro-intestinal tract. Peak plasma levels are reached about 1-2 hours after ingestion. The bioavailability of unchanged drug is about 2% when the drug is administered orally. It has been suggested that the therapeutic effects of the drug are partially due to active metabolites. Several ergotamine metabolites have biologic activity similar to that of the parent drug itself and are often present in concentrations several times that of the parent compound. Distribution Limited information is available about the tissue distribution of ergotamine in humans. Following oral or intravenous administration in rats, ergotamine was detected in high concentrations in the liver and lung and in lower concentrations in the kidney, heart, and brain. About 98% of the drug is protein bound. Studies based on an _in vitro _ model system using porcine 3 brain endothelial cells have shown that ergot alkaloids such as ergotamine are able to cross the blood-brain barrier reaching the central nervous system (CNS) in a high concentration. Metabolism Ergotamine is extensively metabolized in the liver and cleared from the Baca dokumen lengkapnya