Composition:
Each uncoated tablet contains: Metformin Hydrochloride BP 500mg.
List of Excipients:
- Microcrystalline Cellulose Powder
- Maize Starch
- Sodium Methyl Hydroxybenzoate
- Povidone K30
- Purified Water
- Purified Talc
- Colloidal Anhydrous Silica
- Magnesium Stearate
Pharmacodynamic Properties
Blood glucose lowering drugs. Biguanide oral hypoglycemic agents. Metformin is a biguanide with antihyperglycemic effects, lowering both basal and post-prandial plasma glucose. It does not stimulate insulin secretion and therefore does not produce hypoglycemia. Metformin may act via 3 mechanisms. (1) Reduction of hepatic glucose production by inhibiting gluconeogenesis and glycogenolysis. (ii) In muscle, by increasing insulin sensitivity, improving peripheral glucose uptake and utilization. (iii) and delay of intestinal glucose absorption.
Pediatric Data
Metformin tablets can be used in children from 10 years of age and adolescents. The usual starting dose is one tablet of 500 mg or 850 mg once daily, given during meals or after meals. After 10 to 15 days the dose should be adjusted on the basis of blood glucose measurements. The maximum recommended dose of metformin is 2 g daily, taken as 2 or 3 divided doses or as directed by physician.
Pharmacokinetic Properties
Absorption: After an oral dose of metformin, Tmax is reached in 2.5 hours.
Absolute bioavailability of a 500mg or 850mg metformin tablet is approximately
50-60% in healthy subjects. After an oral dose, the non-absorbed fraction
recovered in faces was 20-30%.
Distribution: Plasma protein binding is negligible. Metformin partitions into
erythrocytes. The blood peak is lower than the plasma peak and appears
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 L.
Metabolism
Metformin is excreted unchanged in urine. No metabolites have been identified in humans.
Elimination
Renal clearance of metformin is 400ml/n in, 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.
Therapeutic Indications
Treatment of type 2 diabetes mellitus particularly in overweight patients, when dietary management and exercise alone does not result in adequate glycemic control. In adults, metformin 850mg tablets may be used as monotherapy or in combination with other oral anti-diabetic agents, or with insulin. In children from 10 years of age and adolescents, Metformin tablets may be used as monotherapy or in combination with insulin. A reduction of diabetic complications has been shown in overweight type 2 diabetic patients treated with metformin as first-line therapy after diet failure.
Dosage and Administration
The usual starting dose is one tablet 2 or 3 times daily given during or after meals. After 10 to 15 days the dose should be adjusted on the basis of blood glucose measurements. The maximum recommended dose of metformin is 3g daily, taken as 3 divided doses or as directed by the physician.
Possible Side Effects
The most common side effects are nausea, vomiting, diarrhea, abdominal pain and loss of appetite which resolve spontaneously in most cases.
Drug and Food Interaction
Alcohol intoxication is associated with an increased risk of lactic acidosis, particularly in cases of fasting, malnutrition or hepatic impairment. Avoid consumption of alcohol and alcohol-containing medications. Some medicinal products can adversely affect renal function which may increase the risk of lactic acidosis, e.g. NSAIDs, including selective cyclooxygenase (COX) II inhibitors, ACE inhibitors, angiotensin II receptor antagonists and diuretics, especially loop diuretics. When starting or using such products in combinations with metformin, close monitoring of renal function is necessary. Glucocorticoids (systemic and local routes), beta-2-agonists and diuretics have intrinsic hyperglycemic activity. Inform the patient and perform more frequent blood glucose monitoring, especially at the beginning of the treatment. If necessary, adjust the dosage of the antidiabetic drug during therapy with the other drug and upon its discontinuation.
Contraindication
Hypersensitivity to metformin hydrochloride or to any of the Excipients listed. diabetic pre-coma. Acute conditions with the potential to alter renal function such as dehydration, severe infection, shock, intravascular administration of iodinated contrast agents. Acute or chronic disease which may cause tissue hypoxia such as respiratory failure, decompensated heart failure, recent myocardial infarction, shock. Hepatic insufficiency, acute alcohol intoxication, alcoholism. Any type of acute metabolic acidosis (such as lactic acidosis, diabetic ketoacidosis). Severe renal failure.
Warnings and Precautions for Use
Lactic acidosis, a very rare but serious metabolic complication, most often occurs at acute worsening of renal function or cardiorespiratory illness or sepsis. Metformin accumulation occurs at acute worsening of renal function and increases the risk of lactic acidosis. In case of dehydration (severe diarrhea or vomiting, fever or reduced fluid intake), metformin should be temporarily discontinued and contact with a health care professional is recommended. Medicinal products that can acutely impair renal function (such as antihypertensives, diuretics and NSAIDS) should be initiated with caution in metformin-treated patients. Other risk factors for lactic acidosis are inadequately controlled diabetes, ketosis, prolonged fasting, excessive alcohol intake, hepatic insufficiency and any condition associated with hypoxia, as well as concomitant use of medicinal products that may cause lactic acidosis.
Caution
Metformin monotherapy does not cause hypoglycemia and therefore has no effect on the ability to drive or to use machines. However, patients should be alerted to the risk of hypoglycemia when metformin is used in combination with other antidiabetic agents (sulfonylureas, insulin, repaglinide).
Pregnancy and Lactation
Uncontrolled diabetes during pregnancy (gestational or permanent) is associated with increased risk of congenital abnormalities and perinatal mortality. Metformin is excreted into human breast milk. No adverse effects were observed in breastfed newborns/infants.
Overdose
Hypoglycemia has not been seen with metformin doses up to 85g, although lactic acidosis has occurred in such circumstances. High overdose or concomitant risks of metformin may lead to lactic acidosis. Lactic acidosis is a medical emergency and must be treated in hospital. The most effective method to remove lactate and metformin is hemodialysis.
Storage Condition
Store below 30°C. Protect from light & moisture.
Manufactured by: OA&J Pharmaceuticals Ltd. Tema Heavy Indl. Area, GHANA.
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