CAFERGOT TAB TABLET

Țară: Canada

Limbă: engleză

Sursă: Health Canada

Ingredient activ:

ERGOTAMINE TARTRATE; CAFFEINE

Disponibil de la:

NOVARTIS PHARMACEUTICALS CANADA INC

Codul ATC:

N02CA52

INN (nume internaţional):

ERGOTAMINE, COMBINATIONS EXCL. PSYCHOLEPTICS

Dozare:

1MG; 100MG

Forma farmaceutică:

TABLET

Compoziție:

ERGOTAMINE TARTRATE 1MG; CAFFEINE 100MG

Calea de administrare:

ORAL

Unități în pachet:

100

Tip de prescriptie medicala:

Prescription

Zonă Terapeutică:

SYMPATHOLYTIC (ADRENERGIC BLOCKING) AGENTS

Rezumat produs:

Active ingredient group (AIG) number: 0203679002; AHFS:

Statutul autorizaţiei:

CANCELLED POST MARKET

Data de autorizare:

2014-03-31

Caracteristicilor produsului

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