The biguanides consist of phenformin (5.121), buformin (5.122) and metformin
(5.123). Phenformin was discontinued in the USA because of its implication in causing lactic acidosis. The mechanism of action of these agents is still being elucidated,
but it probably involves direct stimulation of tissue glycolysis with reduced hepatic
gluconeogenesis and slowed glucose absorption from the gastrointestinal tract.
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MEDICINAL CHEMISTRY
(5.123). Phenformin was discontinued in the USA because of its implication in causing lactic acidosis. The mechanism of action of these agents is still being elucidated,
but it probably involves direct stimulation of tissue glycolysis with reduced hepatic
gluconeogenesis and slowed glucose absorption from the gastrointestinal tract.
368
MEDICINAL CHEMISTRY