ANZEMET dolasetron mesylate tablet film coated

Country: United States

Language: English

Source: NLM (National Library of Medicine)

Active ingredient:

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

Available from:

sanofi-aventis U.S. LLC

INN (International Name):

dolasetron mesylate

Composition:

dolasetron mesylate 50 mg

Prescription type:

PRESCRIPTION DRUG

Authorization status:

New Drug Application

Summary of Product characteristics

ANZEMET- DOLASETRON MESYLATE TABLET, FILM COATED
SANOFI-AVENTIS U.S. LLC
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ANZEMET TABLETS
(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.
Each ANZEMET Tablet for oral administration contains dolasetron
mesylate (as the monohydrate) and
also contains the inactive ingredients: carnauba wax, croscarmellose
sodium, hypromellose, lactose,
magnesium stearate, polyethylene glycol, polysorbate 80,
pregelatinized starch, synthetic red iron
oxide, titanium dioxide, and white wax. The tablets are printed with
black ink, which contains lecithin,
pharmaceutical glaze, propylene glycol, and synthetic black iron
oxide.
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. It is
thought that chemotherapeutic agents produce nausea and vomiting by
releasing serotonin from the
enterochromaffin cells of the small intestine, and that the released
serotonin then activates 5-HT
receptors located on vagal efferents to initiate the vomiting re