Pharmacology :
Metformin is an oral antihyperglycemic drug used in the management of type 2 diabetes mellitus. Metformin improves glucose tolerance, lowering both basal and postprandial plasma glucose, decrease hepatic glucose production, decrease intestinal absorption of glucose, improves insulin sensitivity. metformin does not cause hypoglycemia and hyperinsulinemia. In clinal studies, Metformin lower mean fasting serum tryglicerides, total cholesterol and LDL cholesterol level and had no adverse affects on other lipid levels. Metformin chemical name is N,N-dimethylimidodicarbonimidic diamide.
Pharmacokinetics :
Metformin has an oral bioavailability of 50–60% under fasting conditions, steady state plasma concentrations of Metformin are reached within 24 to 48 hours and are generally <1 mcg/mL. Following oral administration, approximately 90% of the absorbed drug is eliminated via the renal route within the first 24 hours, with a plasma elimination half-life of approximately 6.2 hours. In blood, the elimination half-life is approximately 17.6 hours, suggesting that the erythrocyte mass may be a compartment of distribution.
Indications:
Hyperglycemia: As monotherapy, as an adjunct to diet to lower blood glucose in patients with type 2 diabetes mellitus whose hyperglycemia cannot be satisfactorily managed to diet alone. Metformin may be used concomitantly with a sulfonylurea when diet and metformin or a sulfonylurea alone do not result in adequate glycemic control.
Special Populations :
Patients with Type 2 Diabetes
In the presence of normal renal function, there are no differences between single- or multiple-dose pharmacokinetics of Metformin between patients with type 2 diabetes and normal subjects, nor is there any accumulation of Metformin in either group at usual clinical doses.
Gender
Metformin pharmacokinetic parameters did not differ significantly between normal subjects and patients with type 2 diabetes when analyzed according to gender.
Contraindications:
Diabetic coma, ketoacidosis, serious kidney dysfunction, chronic liver disease, cardiac failure, myocardial infarction, alcoholism hypoxemia.
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