Meglitinide / D-phenylalanine Analogues

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Chapter: Essential pharmacology : Insulin, Oral Hypoglycaemic Drugs and Glucagon

These are recently developed quick and short acting insulin releases.


MEGLITINIDE / D-PHENYLALANINE ANALOGUES

 

These are recently developed quick and short acting insulin releases.

 

Repaglinide

 

It is a meglitinide analogue oral hypoglycaemic designed to normalise mealtime glucose excursions. Though not a sulfonylurea, it acts in an analogous mannerby binding to sulfonylurea receptor as well as to other distinct receptors  closure of ATP dependent K+ channels  depolarisation  insulin release.

 

Repaglinide induces rapid onset shortlasting insulin release. It is administered before each major meal to control postprandial hyperglycaemia; the dose should be omitted if a meal is missed. Because of short lasting action it may have a lower risk of serious hypoglycaemia. Side effects are mild headache, dyspepsia, arthralgia and weight gain.

 

Repaglinide is indicated only in type 2 DM as an alternative to sulfonylureas, or to supplement metformin/longacting insulin. It should be avoided in liver disease.

 

Nateglinide

 

This D-phenylalanine derivative principally stimulates the 1st phase insulin secretion resulting in rapid onset and shorter duration of hypoglycaemic action than repaglinide. Ingested 10–20 min before meal, it limits postprandial hyperglycaemia in type 2 diabetics without producing late phase hypoglycaemia. There is little effect on fasting blood glucose level. Episodes of hypoglycaemia are less frequent than with sulfonylureas. Side effects are dizziness, nausea, flu like symptoms and joint pain. It is used in type 2 DM along with other antidiabetics, to control postprandial rise in blood glucose.

 

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