Pharmacology: Metformin reduces elevated blood glucose levels, predominantly by improving hepatic and peripheral tissue sensitivity to insulin without affecting secretion of this hormone. It also increases glucose utilization and reduces glucose production. Metformin has potentially beneficial effects on serum lipid profiles. Reduced circulating levels of free fatty acids, triglycerides and LDL cholesterol and increased HDL cholesterol levels have been reported in particular.
Pharmacokinetics: Metformin has on oral bioavailability of 50-60%, and GI absorption is apparently complete within 6 hrs of ingestion. It is rapidly distributed and does not bind to plasma proteins. No metabolites have been identified. The drug undergoes renal excretion and has a plasma elimination t½ after oral administration of between 4 and 8.7 hrs. This is prolonged in patients with renal impairment and correlates with CrCl.
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