JAMP-FLUMAZENIL SOLUTION

Kraj: Kanada

Język: angielski

Źródło: Health Canada

Składnik aktywny:

FLUMAZENIL

Dostępny od:

JAMP PHARMA CORPORATION

Kod ATC:

V03AB25

INN (International Nazwa):

FLUMAZENIL

Dawkowanie:

0.1MG

Forma farmaceutyczna:

SOLUTION

Skład:

FLUMAZENIL 0.1MG

Droga podania:

INTRAVENOUS

Sztuk w opakowaniu:

5ML/10ML

Typ recepty:

Ethical

Dziedzina terapeutyczna:

MISCELLANEOUS CENTRAL NERVOUS SYSTEM AGENTS

Podsumowanie produktu:

Active ingredient group (AIG) number: 0122202001; AHFS:

Status autoryzacji:

APPROVED

Data autoryzacji:

2014-10-31

Charakterystyka produktu

_Page 1 of 28_
PRODUCT MONOGRAPH
JAMP-FLUMAZENIL
FLUMAZENIL INJECTION, USP
(Flumazenil)
0.1
MG/ML
THERAPEUTIC CLASSIFICATION
BENZODIAZEPINE ANTAGONIST
JAMP Pharma Corporation
1380-203 newton
Boucherville, Québec
J4B 5H2
Date of Preparation :
October 9, 2014
Submission Control No: 178046
_Page 2 of 28_
JAMP-Flumazenil
(flumazenil)
0.1 MG/ML
THERAPEUTIC CLASSIFICATION
Benzodiazepine Antagonist
ACTION AND CLINICAL PHARMACOLOGY
JAMP-Flumazenil, an imidazobenzodiazepine, is a benzodiazepine
antagonist which blocks the
central effects of agents that act via the benzodiazepine receptor, by
competitive inhibition. The
antagonism is specific, since in animal experiments the effects of
compounds which have no
affinity
for
the
benzodiazepine
receptor
(e.g.
barbiturates,
meprobamate,
ethanol,
GABA-
mimetics, and adenosine receptor agonists) were not affected by
flumazenil. Flumazenil does not
reverse the central effects of opioids.
Following the intravenous administration of radiolabelled flumazenil
to human volunteers, the
distribution of radioactivity corresponded closely to the distribution
of benzodiazepine receptors
as determined by positron emission tomography.
The hypnotic-sedative effects of benzodiazepines are rapidly reversed
by flumazenil. However, the
residual effects may reappear gradually within a few hours, depending
on the dose and plasma
concentration of flumazenil, the time elapsed since the benzodiazepine
agonist was given, and the
dose and elimination half-life of the previously administered
benzodiazepine agonist. Flumazenil
has
shown
some
weak
intrinsic
agonistic
(e.g.
anticonvulsant) activity
without
therapeutic
relevance.
PHARMACOKINETICS
In young male volunteers, the pharmacokinetics of intravenous
flumazenil were linear over a dose
range of 2-100 mg. Increasing doses of flumazenil were accompanied by
a corresponding increase
in the area under the plasma concentration-time curve (AUC: 37
ng/mL•hr at 2 mg and
1906
ng/mL•hr at 100 mg), and maximum plasma concentration (C
max
: 55 ng/mL at 2 mg and