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:

100MG

Pharmaceutical form:

TABLET

Composition:

DOLASETRON MESYLATE 100MG

Administration route:

ORAL

Units in package:

15

Prescription type:

Prescription

Therapeutic area:

5-HT3 RECEPTOR ANTAGONISTS

Product summary:

Active ingredient group (AIG) number: 0132936002; AHFS:

Authorization status:

CANCELLED POST MARKET

Authorization date:

2014-04-21

Summary of Product characteristics

PRODUCT MONOGRAPH
PR
ANZEMET
®
(DOLASETRON MESYLATE)
100 MG TABLET
ANTIEMETIC
(5-HT
3 RECEPTOR ANTAGONIST)
sanofi-aventis Canada Inc.
2150 St. Elzéar Blvd. West
Laval, Quebec H7L 4A8
Date of Revision:
July 5, 2012
SUBMISSION CONTROL NO.: 155815
s-a Version dated
Page 2 of 25
_ _
PRODUCT MONOGRAPH
PR
ANZEMET
®
(Dolasetron Mesylate)
100 mg Tablet
_ _
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 administration has little or no