TEMAZEPAM capsule

Land: USA

Språk: engelsk

Kilde: NLM (National Library of Medicine)

Aktiv ingrediens:

TEMAZEPAM (UNII: CHB1QD2QSS) (TEMAZEPAM - UNII:CHB1QD2QSS)

Tilgjengelig fra:

KAISER FOUNDATION HOSPITALS

INN (International Name):

TEMAZEPAM

Sammensetning:

TEMAZEPAM 7.5 mg

Resept typen:

PRESCRIPTION DRUG

Autorisasjon status:

New Drug Application

Preparatomtale

TEMAZEPAM- TEMAZEPAM CAPSULE
KAISER FOUNDATION HOSPITALS
----------
TEMAZEPAM CAPSULES USP
CIV
RX ONLY
DESCRIPTION
Temazepam Capsules USP are benzodiazepine hypnotic agents. The
chemical name is 7-chloro-1,3-
dihydro-3-hydroxy-1-methyl-5-phenyl-2_H_-1,4-benzodiazepin-2-one, and
the structural formula is:
Temazepam is a white, crystalline substance, very slightly soluble in
water and sparingly soluble in
alcohol USP.
Temazepam capsules USP, 7.5 mg are for oral administration.
_7.5 MG CAPSULES_
_Active Ingredient:_ temazepam USP
_Inactive Ingredients:_ FD&C Blue #1, FD&C Red #3, gelatin, lactose,
magnesium stearate, red iron oxide,
titanium dioxide.
_May also include:_ n-butyl alcohol, iron oxide red, shellac, shellac
glaze, SD-35A alcohol.
CLINICAL PHARMACOLOGY
PHARMACOKINETICS
In a single and multiple dose absorption, distribution, metabolism,
and excretion (ADME) study, using
H labeled drug, Restoril was well absorbed and found to have minimal
(8%) first pass metabolism.
There were no active metabolites formed and the only significant
metabolite present in blood was the
O-conjugate. The unchanged drug was 96% bound to plasma proteins. The
blood level decline of the
parent drug was biphasic with the short half-life ranging from 0.4 to
0.6 hours and the terminal half-life
from 3.5 to 18.4 hours (mean 8.8 hours), depending on the study
population and method of determination.
Metabolites were formed with a half-life of 10 hours and excreted with
a half-life of approximately 2
hours. Thus, formation of the major metabolite is the rate limiting
step in the biodisposition of
temazepam. There is no accumulation of metabolites. A
dose-proportional relationship has been
3
established for the area under the plasma concentration/time curve
over the 15 to 30 mg dose range.
Temazepam was completely metabolized through conjugation prior to
excretion; 80% to 90% of the
dose appeared in the urine. The major metabolite was the O-conjugate
of temazepam (90%); the O-
conjugate of N-desmethyl temazepam was a minor metabolite (7%).
B