PMS-PIMOZIDE TABLET

Country: Canada

Language: English

Source: Health Canada

Active ingredient:

PIMOZIDE

Available from:

PHARMASCIENCE INC

ATC code:

N05AG02

INN (International Name):

PIMOZIDE

Dosage:

10MG

Pharmaceutical form:

TABLET

Composition:

PIMOZIDE 10MG

Administration route:

ORAL

Units in package:

100

Prescription type:

Prescription

Therapeutic area:

MISCELLANEOUS ANTIPSYCHOTICS

Product summary:

Active ingredient group (AIG) number: 0109963002; AHFS:

Authorization status:

APPROVED

Authorization date:

1999-03-16

Summary of Product characteristics

PRODUCT MONOGRAPH
PR
PMS-PIMOZIDE
(Pimozide Tablets USP)
2 and 4 and 10 mg
ANTIPSYCHOTIC AGENT
PHARMASCIENCE INC.
DATE OF PREPARATION:
6111 Royalmount Avenue, Suite 100
August 14, 2002
Montreal, Quebec
H4P 2T4 DATE OF REVISION:
January 16, 2007
Control Number:
108528
1
PRODUCT MONOGRAPH
NAME OF DRUG
PR
PMS-PIMOZIDE
(Pimozide Tablets USP)
2 and 4 and 10 mg
THERAPEUTIC CLASSIFICATION
Antipsychotic Agent
ACTION AND CLINICAL PHARMACOLOGY
Pimozide is a diphenylbutylpiperidine derivative with neuroleptic
properties that has been found to
be useful in the management of chronic schizophrenic patients. It is
relatively non-sedating and can
be administered in a single daily dosage.
It is assumed that the basic mechanism of action of pimozide is
related to its action on central
aminergic receptors. It appears to have a selective ability to block
central dopaminergic receptors,
although it affects noradrenaline turnover at higher doses. The
extrapyramidal effects typical of
other neuroleptic agents are seen also with pimozide, but it appears
to have fewer autonomic effects.
As with other neuroleptics, endocrine effects and ECG changes have
also been reported with
pimozide.
Pharmacokinetics
More than 50% of a dose of pimozide is absorbed after oral
administration. Peak serum levels occur
generally six to eight hours (range: 4-12 hours) after dosing.
Pimozide appears to undergo
2
significant first-pass metabolism. Pimozide is extensively
metabolized, primarily by N-dealkylation
in the liver. Two major metabolites have been identified:
1-(4-piperidyl)-2-benzimidazolinone ana
4,4-bis(4-fluorphenyl)butyric acid. These metabolites have no
antipsychotic activity. Only a very
small fraction of pimozide is excreted unchanged in the urine. The
major route of elimination of the
metabolites is through the kidney.
The mean elimination half-life of pimozide in schizophrenic patients
was approximately 55 hours.
There was a more than ten-fold interindividual difference in the area
under the serum pimozide level
time curve and an equivalent