ANZEMET dolasetron mesylate injection

Země: Spojené státy

Jazyk: angličtina

Zdroj: NLM (National Library of Medicine)

Aktivní složka:

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

Dostupné s:

sanofi-aventis U.S. LLC

INN (Mezinárodní Name):

dolasetron mesylate

Složení:

dolasetron mesylate 12.5 mg in 0.625 mL

Druh předpisu:

PRESCRIPTION DRUG

Stav Autorizace:

New Drug Application

Charakteristika produktu

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