mL/minute following single oral dose of 0.5-1.5 g. Metformin is removed by hemodialysis at a rate of approximay 170 ml/min under good hemodynamic conditions.
The volume of distribution following IV administration is 63-276 L, likely due to less binding in the GI tract and/or different methods used to determine volume of distribution. 654 L for metformin 850 mg administered as a single dose.
Metformin is not metabolized.
In 2012, a combination tablet of linagliptin plus metformin hydrochloride was marketed under the name Jentadueto for use in patients when treatment with both linagliptin and metformin is appropriate. Metformin is the only oral antihyperglycemic agent that is not associated with weight gain. Metformin should be avoided in those with severely compromised renal function (creatinine clearance < 30 ml/min), acute/decompensated heart failure, severe liver disease and for 48 hours after the use of iodinated contrast dyes due to the risk of lactic acidosis. When used alone, metformin does not cause hypoglycemia; however, it may potentiate the hypoglycemic effects of sulfonylureas and insulin. Metformin may also have a positive effect on lipid levels. It improves glycemic control by decreasing hepatic glucose production, decreasing glucose absorption and increasing insulin-mediated glucose uptake. Metformin is a biguanide antihyperglycemic agent used for treating non-insulin-dependent diabetes mellitus ( NIDDM ). Lower doses should be used in the elderly and those with decreased renal function. Metformin may induce weight loss and is the drug of choice for obese NIDDM patients. Metformin decreases fasting plasma glucose, postprandial blood glucose and glycosolated hemoglobin (HbA1c) levels, which are reflective of the last 8-10 weeks of glucose control. Dose titration and/or use of smaller divided doses may decrease side effects. Its main side effects are dyspepsia, nausea and diarrhea.
Kind: protein Organism: Human Pharmacological action: yes Actions: inducer Kind: protein Organism: Human Pharmacological action: unknown Actions: substrate inhibitor Kind: protein Organism: Human Pharmacological action: unknown Actions: substrate inhibitor Kind: protein Organism: Human Pharmacological action: unknown Actions: substrate Kind: protein Organism: Human Pharmacological action: unknown Actions: inhibitor Kind: protein Organism: Human Pharmacological action: unknown Actions: substrate. Patent US5955106, issued October, 1991. Jorn Moeckel, Rolf-Dieter Gabel, Heinrich Woog, “Pharmaceutical preparation containing metformin and a process for producing it.” U.S.
Metformin mechanism of action