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Clinical Pharmacology of Biguanides

  • Chapter
Oral Antidiabetics

Part of the book series: Handbook of Experimental Pharmacology ((HEP,volume 119))

Abstract

The biguanide drugs have been used to treat hyperglycaemia in non-insulin-dependent diabetes mellitus (NIDDM) for almost 40 years (Sterne 1969; Hermann 1979; Schäfer 1983; Bailey 1992). Repeated reports of phenformin-associated lactic acidosis led to the withdrawal of this biguanide in the United States in 1977 and in most other countries. Buformin shared the same fate, but metformin escaped withdrawal, even if the use became more restricted. At the same time the University Group Diabetes Program (UGDP) investigation created a discussion about potential cardiovascular morbidity and mortality of oral antidiabetic agents. Although the findings of the UGDP have been challenged and the conclusions criticized, the trial had a considerable impact on the prescription. After the withdrawal of phen-formin and buformin, clinical pharmacological research on biguanides has largely been confined to metformin (Hermann and Melander 1992, 1995). The intended pharmacodynamic action of metformin is to reduce elevated blood glucose levels. The therapeutic effect is dependent on the metabolic state of the subject and counterregulatory mechanisms. Metformin and other biguanides do not reduce blood glucose concentrations in non-diabetic subjects and do not normally lower the blood glucose below the normal levels in diabetics. Hence, metformin has been labelled an antihyperglycaemic drug (Bailey 1992) rather than a hypoglycaemic agent.

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Hermann, L.S. (1996). Clinical Pharmacology of Biguanides. In: Kuhlmann, J., Puls, W. (eds) Oral Antidiabetics. Handbook of Experimental Pharmacology, vol 119. Springer, Berlin, Heidelberg. https://doi.org/10.1007/978-3-662-09127-2_14

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