II. Indications
- Early Type II Diabetes Mellitus Oral Agent
- Elevated postprandial Glucose
- Consider if only used intermittently for pre-meal Hyperglycemia
III. Contraindications
- Sulfa Hypersensitivity
- Chronic Kidney Disease Stage 5 (eGFR <15 ml/min)
IV. Mechanism
- 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
V. Medications
- Repaglinide (Prandin) tablets: 0.5 mg, 1 mg, 2 mg
VI. Dosing
-
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
VIII. Adverse Effects
- Hypoglycemia (lower risk than Sulfonylureas)
IX. Safety
- Pregnancy Category C
- Unknown safety in Lactation
X. Efficacy
- 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
XI. Resources
Images: Related links to external sites (from Bing)
Related Studies
repaglinide (on 12/21/2022 at Medicaid.Gov Survey of pharmacy drug pricing) | ||
REPAGLINIDE 0.5 MG TABLET | Generic | $0.11 each |
REPAGLINIDE 1 MG TABLET | Generic | $0.12 each |
REPAGLINIDE 2 MG TABLET | Generic | $0.13 each |
Ontology: repaglinide (C0246689)
Definition (NCI) | A nonsulfonylurea insulin secretagogue belonging to the melgitinide class with hypoglycemic activity. Repaglinide is rapidly absorbed and has a rapid onset and short duration of action. This agent is metabolized in the liver by CYP2C8 and CYP3A4 and its metabolites are excreted in the bile. Repaglinide has a half-life of one hour. |
Concepts | Pharmacologic Substance (T121) , Organic Chemical (T109) |
MSH | C072379 |
SnomedCT | 109074004, 386964000 |
LNC | LP34567-5, MTHU017515 |
English | repaglinide, (+)-2-Ethoxy-alpha-(((S)-alpha-isobutyl-o-piperidinobenzyl)carbamoyl)-p-toluic Acid, Benzoic Acid, 2-ethoxy-4-(2-((3-methyl-1-(2-(1-piperidinyl)phenyl)butyl)amino)-2-oxoethyl)-,(S)-, repa-glinide, repaglinide (medication), REPAGLINIDE, repaglinide [Chemical/Ingredient], (S)-2-ethoxy-4-(2-((3-methyl-1-(2-(1-piperidinyl)-phenyl)butyl)amino)-2-oxoethyl)-benzoic acid, Repaglinide, Repaglinide (product), Repaglinide (substance) |
Japanese | レパグリニド |
Spanish | repaglinida (producto), repaglinida (sustancia), repaglinida |
Ontology: Prandin (C0722725)
Concepts | Pharmacologic Substance (T121) , Organic Chemical (T109) |
MSH | C072379 |
English | Prandin, repaglinide (Prandin), prandin, Novo Nordisk brand 2 of repaglinide |