ANZEMET TABLET

Country: Canada

Language: English

Source: Health Canada

Active ingredient:

DOLASETRON MESYLATE

Available from:

SANOFI-AVENTIS CANADA INC

ATC code:

A04AA04

INN (International Name):

DOLASETRON

Dosage:

50MG

Pharmaceutical form:

TABLET

Composition:

DOLASETRON MESYLATE 50MG

Administration route:

ORAL

Units in package:

15

Prescription type:

Prescription

Therapeutic area:

5-HT3 RECEPTOR ANTAGONISTS

Product summary:

Active ingredient group (AIG) number: 0132936001; AHFS:

Authorization status:

CANCELLED POST MARKET

Authorization date:

2010-01-01

Summary of Product characteristics

PRODUCT MONOGRAPH
PR
ANZEMET
®
(DOLASETRON MESYLATE)
50 AND 100 MG TABLETS
ANTIEMETIC
(5-HT
3 RECEPTOR ANTAGONIST)
sanofi-aventis Canada Inc.
2150 St. Elzéar Blvd. West
Laval, Quebec H7L 4A8
Date of Revision:
August 03, 2011
Submission Control No.: 147004
s-a Version 4.0 dated
Page 2 of 25
_ _
PRODUCT MONOGRAPH
PR
ANZEMET
®
(Dolasetron Mesylate)
50 and 100 mg Tablets
Antiemetic
(5-HT
3
receptor antagonist)
ACTION AND CLINICAL PHARMACOLOGY
Dolasetron and its active metabolite, hydrodolasetron (MDL 74156), are
selective 5-HT
3
receptor antagonists shown not to have activity at other known
serotonin receptors and with
low affinity for dopamine receptors. The serotonin 5-HT
3
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 serotonin then activates the 5-HT
3
receptors located on vagal afferents to initiate the
vomiting reflex.
In healthy volunteers (N=4), dolasetron mesylate in single intravenous
doses up to 5 mg/kg
produced no effect on pupil size or meaningful changes in EEG
tracings. Results from
neuropsychiatric
tests
revealed
that
dolasetron
mesylate
does
not
alter
mood
or
concentration. Multiple daily doses of dolasetron have no effect on
colonic transit in
humans. Dolasetron has no effect on plasma prolactin concentrations.
EFFECTS ON ELECTROCARDIOGRAM
Acute, reversible, ECG changes (PR and QTc; QRS widening), caused by
dolasetron, have
been
observed
in
controlled
clinical
trials.
Dolasetron
appears
to
prolong
both
depolarization and repolarization time. The magnitude and frequency of
the ECG changes
increased with dose (related to the peak plasma concentration of
hydrodolasetron but not
the parent compound). These ECG changes usually returned to baseline
within 6 to 8
hours, but in some patients have lasted 24 h or longer. Dolasetron
mesylate administrati