Repaglinide

Early Type II Diabetes Mellitus Oral Agent
1. Elevated postprandial Glucose
2. Consider if only used intermittently for pre-meal Hyperglycemia

Insulin secretogogue
Benzoic acid derived from Sulfonylureas
Directly stimulates pancreatic beta cells (Similar to Sulfonylureas)
1. Binds different sites from Sulfonylureas (Sulfonylurea Receptors 1, 1A and 1B)
2. Closes ATP sensitive K+ channels
3. Results in Insulin secretion
Effects
1. Predominately effects postprandial Glucose
2. Faster oral absorption and onset than Sulfonylureas
3. Shorter duration of binding and shorter effect than Sulfonylureas

General
1. Take only before meals, especially before the largest meal (and skip if Fasting)
Adults (not FDA approved in children)
1. Take 0.5 to 2 mg orally before meals, from 3 to 4 times daily
2. Titrate dose in 1 week intervals
3. Maximum 16 mg/day
4. Starting Dose
  1. A1C<8%: Start at 0.5 mg orally three times daily before meals
  2. A1C>8%: Start at 1 to 2 mg orally three times daily before meals
  3. CrCl 20 to 40 ml/min: Start at 0.5 mg orally three times daily before meals

Lowers HBA1C by 0.5 to 1%
Repaglinide is significantly stronger than Nateglinide (Starlix)
Advantages in comparison to Sulfonylureas
1. Low risk of Hypoglycemia (2.4%) than Sulfonylureas
2. Effect depends on Ambient Blood Glucose levels
3. No significant gastrointestinal side effects
4. Minimal weight gain
5. No lab monitoring required
6. No significant Drug Interactions
7. No Lactic Acidosis
8. No adjustments needed (other than per meal)
  1. No adjustment in Congestive Heart Failure
  2. No adjustment for age
  3. No adjustment in Renal Insufficiency
Disadvantages in comparison to Sulfonylureas
1. Two to three times as expensive as Sulfonylureas