FLUMAZENIL INJECTION, USP SOLUTION

Riik: Kanada

keel: inglise

Allikas: Health Canada

Toimeaine:

FLUMAZENIL

Saadav alates:

MYLAN PHARMACEUTICALS ULC

ATC kood:

V03AB25

INN (Rahvusvaheline Nimetus):

FLUMAZENIL

Annus:

0.1MG

Ravimvorm:

SOLUTION

Koostis:

FLUMAZENIL 0.1MG

Manustamisviis:

INTRAVENOUS

Ühikuid pakis:

5ML/10ML

Retsepti tüüp:

Ethical

Terapeutiline ala:

MISCELLANEOUS CENTRAL NERVOUS SYSTEM AGENTS

Toote kokkuvõte:

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

Volitamisolek:

CANCELLED PRE MARKET

Loa andmise kuupäev:

2022-02-28

Toote omadused

_Page 1 of 28_
PRODUCT MONOGRAPH
FLUMAZENIL INJECTION, USP
(Flumazenil)
0.1
MG/ML
THERAPEUTIC CLASSIFICATION
BENZODIAZEPINE ANTAGONIST
Mylan Pharmaceuticals ULC
85 Advance Road
Etobicoke, ON
M8Z 2S6
Date of Preparation :
August 15, 2014
Submission Control No: 171176
_Page 2 of 28_
FLUMAZENIL INJECTION USP
(flumazenil)
0.1 MG/ML
THERAPEUTIC CLASSIFICATION
Benzodiazepine Antagonist
ACTION AND CLINICAL PHARMACOLOGY
Flumazenil Injection, USP, 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
33