Voglinorm-0.2/Voglinorm-0.3 Mechanism of Action

Pharmacology: Pharmacodynamics: Voglibose is an α-glucosidase inhibitor which reduces intestinal absorption of starch, dextrin and disaccharides by inhibiting the action of α-glucosidase in the intestinal brush border. Inhibition of this enzyme halts the decomposition of disaccharides into monosaccharide's and slows the digestion and absorption of carbohydrates; the postprandial rise in plasma glucose is blunted in both normal and diabetic subjects resulting in improvement of postprandial hyperglycemia and various disorders caused by hyperglycemia. α-glucosidase inhibitors do not stimulate insulin release and therefore do not result in hypoglycemia. These agents may be considered as monotherapy in elderly patients or in patients with predominantly postprandial hyperglycemia.
α-glucosidase inhibitors are typically used in combination with other oral antidiabetic agents and/or insulin. Voglibose should be administered at the start of a meal as it is poorly absorbed.
Pharmacokinetics: Absorption: Voglibose is poorly absorbed after oral dosing. Plasma concentrations after oral doses have usually been undetectable. After an 80 mg dose (substantially higher than the recommended dose), peak plasma levels of about 20 ng/mL were observed in 1-1.5 hrs. When voglibose tablets were repeatedly administered to healthy male adults (6 subjects) in a single dose of 0.2 mg, 3 times a day for 7 consecutive days, voglibose was not detected in plasma or urine. Similarly, when voglibose was administered to healthy male adults (10 subjects) as a single dose of 2 mg, voglibose was not detected in plasma or urine.
Distribution: After ingestion of voglibose (and other glucosidase inhibitors), the majority of active unchanged drug remains in the lumen of the gastrointestinal tract to exert its pharmacological activity.
Metabolism: Voglibose is metabolized by intestinal enzymes and by the microbial flora.
Elimination: Voglibose is excreted in the urine and feces.
In a study in which a single dose of 1 mg/kg of C14-Voglibose was administered to rats, the transfer of voglibose to the fetus and to mother's milk was observed, and the rates of excretion into urine and feces were about 5% and 98%, respectively.