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Glucophage XR

NAME OF THE MEDICINAL PRODUCT
Glucophage XR 750mg extended release tablet

QUALITATIVE AND QUANTITATIVE COMPOSITION
One extended release tablet contains 750 mg metformin hydrochloride corresponding to 585 mg metformin base. For a full list of excipients, see List of excipients.

PHARMACEUTICAL FORM
Extended release tablet
White to off-white capsule-shaped, biconvex tablet, debossed on one side with '750' and on the other side with 'Merck'.

CLINICAL PARTICULARS
Treatment of type 2 diabetes mellitus in adults, when dietary management and exercise alone does not result in adequate glycaemic control. Glucophage XR may be used as monotherapy or in combination with other oral antidiabetic agents, or with insulin.

A reduction of diabetic complications has been shown in overweight type 2 diabetic patients treated with immediate release metformin as first-line therapy after diet failure (see Pharmacodynamic properties).

Posology and method of administration
Monotherapy and combination with other oral antidiabetic agents:
The usual starting dose of Glucophage XR 750mg is one tablet daily given with the evening meal.
After 10 to 15 days the dose should be adjusted on the basis of blood glucose measurements. A slow increase of dose may improve gastro-intestinal tolerability. The maximum recommended dose is 2 tablets once daily with the evening meal.
In patients already treated with metformin tablets, the starting dose of Glucophage XR should be equivalent to the daily dose of metformin immediate release tablets.
If transfer from another oral antidiabetic agent is intended: discontinue the other agent and initiate Glucophage XR at the dose indicated above.

Combination with insulin:
Metformin and insulin may be used in combination therapy to achieve better blood glucose control. The usual starting dose of Glucophage XR is one tablet once daily with the evening meal, while insulin dosage is adjusted on the basis of blood glucose measurements.

Elderly: due to the potential for decreased renal function in elderly subjects, the metformin dosage should be adjusted based on renal function. Regular assessment of renal function is necessary (see Special warnings and special precautions for use).
Children: In the absence of available data, Glucophage XR should not be used in children.

Contraindications
Hypersensitivity to metformin or to any of the excipients.
Diabetic ketoacidosis, diabetic pre-coma.
Renal failure or renal dysfunction (creatinine clearance < 60 ml/min).
Acute conditions with the potential to alter renal function such as:
- Dehydration,
- severe infection,
- shock,
Acute or chronic disease which may cause tissue hypoxia such as:
- cardiac or respiratory failure,
- recent myocardial infarction,
- shock
Hepatic insufficiency, acute alcohol intoxication, alcoholism

Special warnings and precautions for use
Lactic acidosis:
Lactic acidosis is a rare, but serious (high mortality in the absence of prompt treatment), metabolic complication that can occur due to metformin accumulation. Reported cases of lactic acidosis in patients on metformin have occurred primarily in diabetic patients with significant renal failure. The incidence of lactic acidosis can and should be reduced by assessing also other associated risk factors such as
poorly controlled diabetes, ketosis, prolonged fasting, excessive alcohol intake, hepatic insufficiency and any condition associated with hypoxia.

Diagnosis:
The risk of lactic acidosis must be considered in the event of non-specific signs such as muscle cramps with digestive disorders as abdominal pain and severe asthenia.

a significant reduction of the absolute risk of any diabetes-related complication in the metformin group (29.8 events/ 1000 patient-years) versus diet alone (43.3 events/ 1000 patient-years), p=0.0023, and versus the combined sulphonylurea and insulin monotherapy groups (40.1 events/ 1000 patient-years), p=0.0034.
a significant reduction of the absolute risk of diabetes-related mortality: metformin 7.5 events/1000 patient-years, diet alone 12.7 events/ 1000 patient-years, p=0.017;
a significant reduction of the absolute risk of overall mortality: metformin 13.5 events/ 1000 patient-years versus diet alone 20.6 events/1000 patient-years (p=0.011), and versus the combined sulphonylurea and insulin monotherapy groups 18.9 events/ 1000 patient-
years (p=0.021);
a significant reduction in the absolute risk of myocardial infarction: metformin 11 events/ 1000 patient-years, diet alone 18 events/ 1000 patient-years (p=0.01)
For metformin used as second-line therapy, in combination with a sulphonylurea, benefit regarding clinical outcome has not been shown.

In type 1 diabetes, the combination of metformin and insulin has been used in selected patients, but the clinical benefit of this combination has not been formally established.

Pharmacokinetic properties
Absorption
Following a single oral administration of 1500 mg of Glucophage XR 750 mg, a mean peak plasma concentration of 1193 ng/ml is achieved with a median value of 5 hours and a range of 4 to 12 hours.

Glucophage XR 750 mg was shown to be bioequivalent to Glucophage XR 500 mg at a 1500 mg dose with respect to Cmax and AUC in healthy fed and fasted subjects.

The bioequivalent product shows the following properties:
At steady state, similar to the immediate release formulation, Cmax and AUC are not proportionally increased to the administered dose. The AUC after a single oral administration of 2000 mg of metformin extended release tablets is similar to that observed after administration of 1000 mg of metformin immediate release tablets b.i.d.

Intrasubject variability of Cmax and AUC of metformin extended release tablets is comparable to that observed with metformin immediate release tablets.

When the extended release tablet is administered in fasting conditions the AUC is decreased by 30% (both Cmax and Tmax are unaffected).

Metformin absorption from the extended release formulation is not altered by meal composition.

No accumulation is observed after repeated administration
of up to 2000 mg of metformin extended release tablets.

Distribution
Plasma protein binding is negligible. Metformin partitions into erythrocytes. The blood peak is lower than the plasma peak and appears at approximately the same time. The red blood cells most likely represent a secondary compartment of distribution. The mean volume of distribution (Vd) ranged between 63-276 I.

Metabolism
Metformin is excreted unchanged in the urine. No metabolites have been identified in humans.

Elimination
Renal clearance of metformin is > 400 ml/min, indicating that metformin is eliminated by glomerular filtration and tubular secretion. Following an oral dose, the apparent terminal elimination half-life is approximately 6.5 hours. When renal function is impaired, renal clearance is decreased in proportion to that of creatinine and thus the elimination half-life is prolonged, leading to increased levels of metformin in plasma.

Preclinical safety data
Preclinical data reveal no special hazard for humans based on conventional studies on safety pharmacology, repeated dose toxicity, genotoxicity, carcinogenic potential, toxicity reproduction.

PHARMACEUTICAL PARTICULARS
List of Excipients
Magnesium stearate
Carmellose sodium
Hypromellose.

Incompatibilities
None

Shelf life
3 years

Special precautions for storage
Protect from moisture, freezing and excessive heat.
Store below 30C

Nature and contents of container
30 and 60 tablets in blister strips.
Not all pack sizes may be marketed.

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