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Chapter: Modern Pharmacology with Clinical Applications: Insulin and Oral Drugs for Diabetes Mellitus

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Meglitinides - Oral Agents For Treating Diabetes Mellitus

Though structurally unrelated to sulfonylureas, the meglitinide class of hypoglycemic drugs bind to the same KATP channel as do the sulfonylureas, but it is un-clear whether they bind to the same SUR1 subunit within the KATP complex.

Meglitinides

 

Though structurally unrelated to sulfonylureas, the meglitinide class of hypoglycemic drugs bind to the same KATP channel as do the sulfonylureas, but it is un-clear whether they bind to the same SUR1 subunit within the KATP complex. As a class, the meglitinides are incapable of stimulating insulin secretion in nutrient-starved β-cells, but in the presence of glucose, they demonstrate hypoglycemic effects by augmenting the release of insulin. Consequently, meglitinides seem rel-atively unlikely to cause fasting hypoglycemia.

 

Repaglinide (Prandin), a member of the meglitinide class, is approved for monotherapy or in combination with metformin. Repaglinide is taken before each meal, three times a day, and is rapidly absorbed; it is metabo-lized by the liver and has a half life of an hour. Insulin levels transiently rise postprandially after repaglinide administration but generally return to baseline by the next meal. Although repaglinide does not appear to of-fer any advantage over the sulfonylureas, it may be helpful in patients with a known allergy to sulfa drugs. Hypoglycemia is the most common side effect.

 

Nateglinide (Starlix), a newer drug in the meglitinide class, is a phenylalanine derivative that also works by binding to a specific site on the K+ –ATP–sensitive chan-nel on the surface of β-cells. Nateglinide binds with a higher affinity than does repaglinide and has a faster onset of action and a shorter duration of action. Like repaglinide, it is approved for both monotherapy and in combination with metformin. Nateglinide is taken three times a day before meals and achieves peak plasma levels within an hour. Nateglinide administra-tion results in plasma insulin levels that peak within 2 hours; they return to baseline by 4 hours. Nateglinide is metabolized by the liver and excreted by the kidney. The main side effect of nateglinide is hypoglycemia, though its effects on fasting insulin levels is not sub-stantially reduced.

 

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