ANZEMET dolasetron mesylate injection

国: アメリカ合衆国

言語: 英語

ソース: NLM (National Library of Medicine)

有効成分:

dolasetron mesylate (UNII: U3C8E5BWKR) (dolasetron - UNII:82WI2L7Q6E)

から入手可能:

sanofi-aventis U.S. LLC

INN（国際名）:

dolasetron mesylate

構図:

dolasetron mesylate 12.5 mg in 0.625 mL

処方タイプ:

PRESCRIPTION DRUG

認証ステータス:

New Drug Application

製品の特徴

ANZEMET- DOLASETRON MESYLATE INJECTION
SANOFI-AVENTIS U.S. LLC
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ANZEMET INJECTION
(DOLASETRON MESYLATE)
DESCRIPTION
ANZEMET (dolasetron mesylate) is an antinauseant and antiemetic agent.
Chemically, dolasetron
mesylate is
(2α,6α,8α,9aβ)-octahydro-3-oxo-2,6-methano-2_H_-quinolizin-8-yl-1_H_-indole-3-carboxylate
monomethanesulfonate, monohydrate. It is a highly specific and
selective serotonin subtype 3 (5-HT )
receptor antagonist both in vitro and in vivo. Dolasetron mesylate has
the following structural formula:
The empirical formula is C
H N O • CH SO H • H O, with a molecular weight of 438.50.
Approximately 74% of dolasetron mesylate monohydrate is dolasetron
base.
Dolasetron mesylate monohydrate is a white to off-white powder that is
freely soluble in water and
propylene glycol, slightly soluble in ethanol, and slightly soluble in
normal saline.
ANZEMET Injection is a clear, colorless, nonpyrogenic, sterile
solution for intravenous administration.
Each milliliter of ANZEMET Injection contains 20 mg of dolasetron
mesylate and 38.2 mg mannitol,
USP, with an acetate buffer in water for injection. The pH of the
resulting solution is 3.2 to 3.8.
ANZEMET Injection multidose vials contain a clear, colorless,
nonpyrogenic, sterile solution for
intravenous administration. Each ANZEMET multidose vial contains 25 mL
(500 mg) dolasetron
mesylate. Each milliliter contains 20 mg dolasetron mesylate, 29 mg
mannitol, USP, and 5 mg phenol,
USP, with an acetate buffer in water for injection. The pH of the
resulting solution is 3.2 to 3.7.
CLINICAL PHARMACOLOGY
Dolasetron mesylate and its active metabolite, hydrodolasetron (MDL
74,156), are selective serotonin
5-HT receptor antagonists not shown to have activity at other known
serotonin receptors and with low
affinity for dopamine receptors. The serotonin 5-HT receptors are
located on the nerve terminals of
the vagus in the periphery and centrally in the chemoreceptor trigger
zone of the area postrema.
In healthy volunteers (N=64), dolasetron mesylate in single