- Early Type II Diabetes Mellitus Oral Agent
- Elevated postprandial Glucose
- Consider if only used intermittently for pre-meal Hyperglycemia
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Insulin secretogogue
- Benzoic acid derived from Sulfonylureas
- Directly stimulates pancreatic beta cells (Similar to Sulfonylureas)
- Binds different sites from Sulfonylureas (Sulfonylurea Receptors 1, 1A and 1B)
- Closes ATP sensitive K+ channels
- Results in Insulin secretion
- Effects
- Predominately effects postprandial Glucose
- Faster oral absorption and onset than Sulfonylureas
- Shorter duration of binding and shorter effect than Sulfonylureas
- Repaglinide (Prandin) tablets: 0.5 mg, 1 mg, 2 mg
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General
- Take only before meals, especially before the largest meal (and skip if Fasting)
- Adults (not FDA approved in children)
- Take 0.5 to 2 mg orally before meals, from 3 to 4 times daily
- Titrate dose in 1 week intervals
- Maximum 16 mg/day
- Starting Dose
- A1C<8%: Start at 0.5 mg orally three times daily before meals
- A1C>8%: Start at 1 to 2 mg orally three times daily before meals
- CrCl 20 to 40 ml/min: Start at 0.5 mg orally three times daily before meals
- Renal excretion
- Hepatic metabolism (CYP3A4, CYP2C9)
- Pregnancy Category C
- Unknown safety in Lactation
- Lowers HBA1C by 0.5 to 1%
- Repaglinide is significantly stronger than Nateglinide (Starlix)
- Advantages in comparison to Sulfonylureas
- Low risk of Hypoglycemia (2.4%) than Sulfonylureas
- Effect depends on Ambient Blood Glucose levels
- No significant gastrointestinal side effects
- Minimal weight gain
- No lab monitoring required
- No significant Drug Interactions
- No Lactic Acidosis
- No adjustments needed (other than per meal)
- No adjustment in Congestive Heart Failure
- No adjustment for age
- No adjustment in Renal Insufficiency
- Disadvantages in comparison to Sulfonylureas
- Two to three times as expensive as Sulfonylureas
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