MEPRON SUSPENSION

Country: Canada

Language: English

Source: Health Canada

Active ingredient:

ATOVAQUONE

Available from:

GLAXOSMITHKLINE INC

ATC code:

P01AX06

INN (International Name):

ATOVAQUONE

Dosage:

750MG

Pharmaceutical form:

SUSPENSION

Composition:

ATOVAQUONE 750MG

Administration route:

ORAL

Units in package:

210 ML

Prescription type:

Prescription

Therapeutic area:

MISCELLANEOUS ANTIPROTOZOALS

Product summary:

Active ingredient group (AIG) number: 0124073001; AHFS:

Authorization status:

APPROVED

Authorization date:

2001-08-07

Summary of Product characteristics

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_Page 1 of 38_
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PRODUCT MONOGRAPH
PR
MEPRON
®
Atovaquone Oral Suspension, USP
750 mg/5 mL
ANTIPROTOZOAL AGENT
GlaxoSmithKline Inc.
7333 Mississauga Road
Mississauga, Ontario
L5N 6L4
Date of Revision:
July 26, 2016
SUBMISSION CONTROL NO: 188021
_©_
_2016 GlaxoSmithKline Inc., All Rights Reserved. _
_MEPRON is a registered trademark of Glaxo Group Limited, used under
license by GlaxoSmithKline Inc. _
_ _
_ _
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_Page 2 of 38_
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PRODUCT MONOGRAPH
PR
MEPRON
®
Atovaquone Oral Suspension, USP
750 mg/5 mL
ANTIPROTOZOAL AGENT
CLINICAL PHARMACOLOGY
Atovaquone is a hydroxy-1,4-naphthoquinone, an analog of ubiquinone,
with anti-
pneumocystis activity. The mechanism of action against _Pneumocystis
carinii_ has not
been fully elucidated.
The pharmacokinetics of atovaquone have been studied in healthy
volunteers, HIV-
infected adults with varying stages and manifestations of HIV
infection and in
immunocompromised children. The half-life of atovaquone is long (2 to
3 days) due to
presumed enterohepatic cycling and eventual fecal elimination. There
is no evidence
that the drug is metabolized in man.
Atovaquone is a highly lipophilic compound with a low aqueous
solubility. It is
extensively bound to plasma proteins (>99.9%).
The bioavailability of atovaquone is highly dependent on formulation
and diet.
MEPRON
®
(atovaquone) Oral Suspension, which has now replaced MEPRON
®
(atovaquone) Tablets, has atovaquone particles significantly smaller
than those in the
tablet formulation, and provides an approximately two-fold increase in
atovaquone
bioavailability in the fasting or fed state compared to the tablet
formulation studied under
the same conditions. The bioavailability of MEPRON
®
(atovaquone) Oral Suspension
can be increased greatly when administered with meals. In healthy
volunteers, a
standard meal (23 g fat; 610 kCal) increased the bioavailability two
to three-fold following
750 mg single doses of atovaquone suspension. The mean area under the
atovaquone
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_Page 3 of 38_
plasma concentration-time curve (AUC)