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:

Validus Pharmaceuticals LLC

INN (International Name):

DOLASETRON MESYLATE

Composition:

DOLASETRON MESYLATE 50 mg

Administration route:

ORAL

Prescription type:

PRESCRIPTION DRUG

Therapeutic indications:

ANZEMET Tablets are indicated for the prevention of nausea and vomiting associated with moderately emetogenic cancer chemotherapy, including initial and repeat courses in adults and children 2 years and older. ANZEMET Tablets are contraindicated in patients known to have hypersensitivity to the drug.

Product summary:

Store at 68° to 77°F (20° to 25°C) [See USP Controlled Room Temperature].  Protect from light.

Authorization status:

New Drug Application

Summary of Product characteristics

ANZEMET- DOLASETRON MESYLATE TABLET, FILM COATED
VALIDUS PHARMACEUTICALS LLC
----------
ANZEMET
ANZEMET
TABLETS
(DOLASETRON MESYLATE, USP)
RX ONLY
DESCRIPTION
ANZEMET (dolasetron mesylate, USP) is an antinauseant and antiemetic
agent.
Chemically, dolasetron mesylate is
(2α,6α,8α,9aß)-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:
croscarmellose sodium,
hypromellose, lactose, magnesium stearate, polyethylene glycol,
polysorbate 80,
pregelatinized starch, synthetic red iron oxide, and titanium dioxide.
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 reflex.
®
3
19
20
2
3
3
3
2
3
3
3
In healthy volunteers (N=64), dolasetron mesylate in single
intravenous doses up to
5 mg/kg