CAFERGOT SUP SUPPOSITORY

Country: Canada

Language: English

Source: Health Canada

Active ingredient:

ERGOTAMINE TARTRATE; CAFFEINE

Available from:

NOVARTIS PHARMACEUTICALS CANADA INC

ATC code:

N02CA52

INN (International Name):

ERGOTAMINE, COMBINATIONS EXCL. PSYCHOLEPTICS

Dosage:

2MG; 100MG

Pharmaceutical form:

SUPPOSITORY

Composition:

ERGOTAMINE TARTRATE 2MG; CAFFEINE 100MG

Administration route:

RECTAL

Units in package:

12

Prescription type:

Prescription

Therapeutic area:

SYMPATHOLYTIC (ADRENERGIC BLOCKING) AGENTS

Product summary:

Active ingredient group (AIG) number: 0203679001; AHFS:

Authorization status:

CANCELLED POST MARKET

Authorization date:

2006-11-13

Summary of Product characteristics

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