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Thread: Biguanides

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    Question Biguanides

    vt is the prime mechanism of action othese hypoglycemics?

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    Quote Originally Posted by rupu View Post
    vt is the prime mechanism of action othese hypoglycemics?
    Biguanides

    Mechanism of Action:


    Decrease hepatic glucose production (glycogenolysis/gluconeogenesis), decrease carbohydrate absorption in the gut, increase central and peripheral insulin sensitivity.

    The exact mechanism of action remains unknown. However metformin has no direct stimulatory effect on insulin release. Metformin has been shown to increase insulin binding to its receptor both in vitro and in vivo. In rat adipocytes, metrormin increases insulin-induced translocation of glucose transport proteins from an intracellular pool to plasma membrane.

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    Rightly said a4assasins !! Here is some additional information:

    A biguanide differs from the sulfonylureas in not stimulating insulin secretion. The risk of hypoglycemia is less than with sulfonylurea agents. Metformin may be used alone or in combination with the sulfonylureas. Metformin acts primarily by decreasing hepatic glucose output, largely by inhibiting gluconeogenesis. A very important property is its ability to reduce hyperlipidemia (LDL and VLDL cholesterol concentrations fall and HDL cholesterol rises). The patient often loses weight. Metformin is considered by some experts as the drug of choice in newly diagnosed Type II diabetics. Metformin is well absorbed orally, is not bound to serum proteins and is not metabolized. Excretion is via the urine. Adverse effects are largely gastrointestinal. Rarely, potentially fatal lactic acidosis has occurred. [Note: Phenformin, a previous biguanide hypoglycemic agent, was withdrawn for this reason.] Long term use may interfere with B12 absorption. The drug is contraindicated in renal and hepatic insufficiency.

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