FLUMAZENIL INJECTION SOLUTION

מדינה: קנדה

שפה: אנגלית

מקור: Health Canada

מרכיב פעיל:

FLUMAZENIL

זמין מ:

SANDOZ CANADA INCORPORATED

קוד ATC:

V03AB25

INN (שם בינלאומי):

FLUMAZENIL

כמות:

0.1MG

טופס פרצבטיות:

SOLUTION

הרכב:

FLUMAZENIL 0.1MG

מסלול נתינה (של תרופות):

INTRAVENOUS

יחידות באריזה:

5ML

סוג מרשם:

Ethical

איזור תרפויטי:

MISCELLANEOUS CENTRAL NERVOUS SYSTEM AGENTS

leaflet_short:

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

מצב אישור:

APPROVED

תאריך אישור:

2005-08-09

מאפייני מוצר

_Flumazenil Injection _
_ _
_Page 1 of 27 _
PRODUCT MONOGRAPH
FLUMAZENIL INJECTION
(flumazenil)
0.1 MG/ML
THERAPEUTIC CLASSIFICATION
BENZODIAZEPINE ANTAGONIST
Sandoz Canada Inc.
145, Jules-Léger
Date of Revision: May 31, 2011
Boucherville, QC, Canada
J4B 7K8
Control No: 145620
_Flumazenil Injection _
_ _
_Page 2 of 27 _
FLUMAZENIL INJECTION
(flumazenil)
0.1 MG/ML
THERAPEUTIC CLASSIFICATION
Benzodiazepine Antagonist
ACTION AND CLINICAL PHARMACOLOGY
Flumazenil Injection, 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 concentrat