Repaglinide Tablets

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Therapeutic Indication

Hypertension (High Blood Pressure)
Congestive Heart Failure
Post Myocardial Infarction
Diabetic Nephropathy
Cardiovascular Risk Reduction
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Repaglinide

Tablet

Repaglinide one of the first of a new class of oral antidiabetic agents is categorized as carbamoylmethyl benzoic acid derivative and designed to balance postprandial glucose excursions in type 2 diabetes mellitus patients. Repaglinide reduces blood glucose by stimulating pancreatic β-cells to release insulin same as sulphonylureas, but differs from these in its structure, binding profile, duration of action and mode of excretion.

Speciality Diabetology | Endocrinology | General Medicine
Tags Antidiabetic | Type 2 Diabetes | Insulin Secretagogue | Blood Sugar Control
Strength
  • .5 mg
  • 1 mg
  • 2 mg
Packing Size
  • 10 Tablets

Check all Tablet Range

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Mechanism

Repaglinide acts by inhibition of ATP-sensitive potassium channels present on a unique receptor site on the β-cell membrane which appears to be the sole mechanism and is responsible to stimulates insulin secretion. In vitro experiments imitates that, repaglinide differs from sulphonylureas as it does not stimulate insulin secretion in the absence of glucose, does not inhibit glucose-stimulated proinsulin biosynthesis in isolated rat β-cells model and is able to reduce the metabolic stress induced by 2,4-dinitrophenol.

Pharmacokinetics

  • Absorption: Rapidly absorbed after oral administration
  • Bioavailability: ~60%
  • Distribution: Highly protein bound (>98%)
  • Metabolism: Extensively metabolized in liver (CYP3A4 & CYP2C8)
  • Elimination: Excreted mainly via bile
  • Half-life: ~1 hour

Side Effects

  • Hypoglycemia
  • Weight gain
  • Dizziness
  • Headache
  • Gastrointestinal discomfort

Contraindication

  • Type 1 diabetes mellitus
  • Diabetic ketoacidosis
  • Severe hepatic impairment
  • Hypersensitivity to repaglinide

Interaction

  • Gemfibrozil (contraindicated – increases hypoglycemia risk)
  • Rifampicin (reduces effectiveness)
  • Azole antifungals (increase levels)
  • Beta blockers (mask hypoglycemia symptoms)

Warning and Precautions

  • Take before meals to avoid hypoglycemia
  • Monitor blood glucose regularly
  • Adjust dose in liver impairment
  • Avoid skipping meals after dosing