Pharmacology · Antidiabetic Drugs (Oral Hypoglycemics, Insulins)

Repaglinide must be taken within 30 minutes before each main meal. Which pharmacokinetic property dictates this dosing schedule?

  • A Slow dissociation from albumin over several hours
  • B Irreversible binding to the sulfonylurea receptor
  • C Enteric coating requiring gastric acid for absorption
  • D Half-life of approximately 1 hour, giving a brief prandial insulin secretagogue effect
Correct answer: D. Half-life of approximately 1 hour, giving a brief prandial insulin secretagogue effect

Explanation

Repaglinide is a meglitinide with a very short half-life (about 1 hour). Taken preprandially, it boosts early-phase insulin secretion covering the meal and is gone before the next meal, so it is skipped if the meal is skipped. This limits between-meal hypoglycemia compared with sulfonylureas. Its binding to SUR1 is reversible and at a site distinct from sulfonylureas, absorption is not acid dependent, and protein binding is not rate limiting.

Reference: Katzung Basic and Clinical Pharmacology, 15th ed.

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