GLUCOPHAGE XR 1000 mg TABLET

Country: South Africa

Language: English

Source: South African Health Products Regulatory Authority (SAHPRA)

Available from:

Merck (Pty) Ltd

Dosage:

See ingredients

Pharmaceutical form:

TABLET

Composition:

EACH TABLET CONTAINS METFORMIN HYDROCHLORIDE 1000,0 mg

Authorization status:

Registered

Authorization date:

2016-03-11

Summary of Product characteristics

Page 1 of 15
GLUCOPHAGE XR RANGE PACKAGE INSERT
SCHEDULING STATUS
S3
PROPRIETARY NAME (AND DOSAGE FORM)
GLUCOPHAGE XR 500 MG (prolonged release tablet)
GLUCOPHAGE XR 750 MG (prolonged release tablet)
GLUCOPHAGE XR 1000 MG (prolonged release tablet)
COMPOSITION
Each prolonged release Glucophage XR 500 mg tablet contains 500 mg
metformin
hydrochloride.
Each prolonged release Glucophage XR 750 mg tablet contains 750 mg
metformin
hydrochloride.
Each prolonged release Glucophage XR 1000 mg tablet contains 1000 mg
metformin
hydrochloride.
Inactive ingredients: magnesium stearate, sodium
carboxymethylcellulose; hydroxypropyl
methylcellulose.
PHARMACOLOGICAL CLASSIFICATION
A 21.2
Oral hypoglycaemics
PHARMACOLOGICAL ACTION
PHARMACODYNAMIC PROPERTIES_ _
Metformin
is
a
biguanide
with
anti-hyperglycaemic
effects,
lowering
both
basal
and
postprandial plasma glucose. It does not stimulate insulin secretion
and therefore does not
produce hypoglycaemia.
Metformin may act _via_ three mechanisms:
-
reduction of hepatic glucose production by inhibiting gluconeogenesis
and
glycogenolysis;
-
in muscle, by increasing glucose sensitivity, improving peripheral
glucose uptake and
utilisation; and
-
delay of intestinal glucose absorption.
Metformin stimulates intracellular glycogen synthesis by acting on
glycogen synthase.
Metformin increases the transport capacity of all types of membrane
glucose transporters.
PHARMACOKINETIC PROPERTIES
ABSORPTION
Following a single oral dose of Glucophage XR 500 mg peak plasma
levels (C
max
) are
achieved with a median value of 7 hours.
Page 2 of 15
Following a single oral dose of 1500 mg of Glucophage XR 750 mg, a
mean plasma
concentration of 1193 ng/ml is achieved after a median value of 5
hours (range of 4 to 12
hours).
Glucophage XR 750 mg was shown to be bioequivalent to Glucophage XR
500 mg, at a total
daily dose of 1500 mg, with respect to C
max
and AUC in healthy fed and fasted subjects.
Following a single oral administration in the fed state of one tablet
of Glucophage XR 1000
mg, a mean peak p