METHOPRAZINE TABLET

Country: Canada

Language: English

Source: Health Canada

Active ingredient:

METHOTRIMEPRAZINE (METHOTRIMEPRAZINE MALEATE)

Available from:

AA PHARMA INC

ATC code:

N05AA02

INN (International Name):

LEVOMEPROMAZINE

Dosage:

2MG

Pharmaceutical form:

TABLET

Composition:

METHOTRIMEPRAZINE (METHOTRIMEPRAZINE MALEATE) 2MG

Administration route:

ORAL

Units in package:

100

Prescription type:

Prescription

Therapeutic area:

PHENOTHIAZINES

Product summary:

Active ingredient group (AIG) number: 0134080005; AHFS:

Authorization status:

APPROVED

Authorization date:

2012-08-30

Summary of Product characteristics

PRESCRIBING INFORMATION
PR
METHOPRAZINE
METHOTRIMEPRAZINE MALEATE TABLETS
2 MG, 5 MG, 25 MG AND 50 MG
HOUSE STANDARD
NEUROLEPTIC
AA PHARMA INC.
DATE OF PREPARATION:
1165 CREDITSTONE ROAD, UNIT#1
AUGUST 31, 2012
VAUGHAN, ONTARIO
L4K 4N7
CONTROL NUMBER: 158247
PRESCRIBING INFORMATION
Pr
METHOPRAZINE
Methotrimeprazine Maleate Tablets
2 mg, 5 mg, 25 mg and 50 mg
THERAPEUTIC CLASSIFICATION
Neuroleptic
ACTIONS AND CLINICAL PHARMACOLOGY
Methotrimeprazine possesses antipsychotic, tranquilizing, anxiolytic,
sedative and analgesic properties and
it is also a potent potentiator of anesthetics.
Methotrimeprazine possesses strong sedative properties. It potentiates
ether and hexobarbital anesthesia as
well as morphine analgesia. It also exerts a potent anti-apomorphine
effect, a hypothermic action 3 times
more potent than that of chlorpromazine and strong antispasmodic and
anti-histaminic effects.
Methotrimeprazine is capable of reversing epinephrine-induced
hypertension but has practically no effect
against norepinephrine and acetylcholine. It readily protects rats
against traumatic shock and produces
deep local anesthesia following parasciatic injections.
Comparative Bioavailability
A comparative bioavailability study was performed using healthy human
volunteers. The rate and extent of
absorption of methotrimeprazine were measured and compared following a
single oral 25 mg dose of
METHOPRAZINE or Nozinan. The results from measured data are summarized
as follows:
Summary Table of the Comparative Bioavailability Data
Methotrimeprazine Tablets (Dose: 25 mg)
From Measured Data
Geometric Mean
Arithmetic Mean (CV%)
Ratio of
Geometric
Means (%)
Parameter
METHOPRAZINE
Nozinan®†
AUC
T
(ng

hr/mL)
AUC
I
(ng

hr/mL)
C
max
(ng/mL)
T
max
(h)*
t
1/2
(h)*
26.9
40.5 (87)
34.3
47.3 (82)
3.44
4.66 (76)
2.96 (26)
10.8 (49)
27.9
41.1 (80)
35.1
47.1 (73)
3.67
4.96 (73)
2.73 (33)
10.3 (49)
96.4
97.7
93.7
--
--
*
Arithmetic means only (CV%).
†
Nozinan® (Rhône-Poulenc Rorer Inc.) was purchased at a Canadian
retail pharmacy.
INDICATION