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)
- Nateglinide (Starlix)
- Significantly weaker activity compared with Repaglinide
VI. Dosing
VIII. Adverse Effects
- Hypoglycemia (lower risk than Sulfonylureas)
IX. Efficacy
- Lowers HBA1C by 0.5 to 1%
- 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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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 |
| nateglinide (on 12/21/2022 at Medicaid.Gov Survey of pharmacy drug pricing) | ||
| NATEGLINIDE 120 MG TABLET | Generic | $0.30 each |
| NATEGLINIDE 60 MG TABLET | Generic | $0.27 each |
Ontology: Meglitinide (C0065880)
| Definition (NCI) | A benzamide belonging to the meglitinide class of antidiabetic agents with hypoglycemic activity. Meglitinide represents the basic structure of the meglitinide-type agents and is not used therapeutically. |
| Concepts | Pharmacologic Substance (T121) , Organic Chemical (T109) |
| MSH | C030516 |
| SnomedCT | 109075003, 372566000 |
| English | 4-(2-(5-chloro-2-methoxybenzamido)ethyl)benzoic acid, meglitinide, meglitinide [Chemical/Ingredient], meglitinides, Meglitinide, MEGLITINIDE, Meglitinide (product), Meglitinide (substance) |
| Spanish | meglitinida (producto), meglitinida (sustancia), meglitinida |
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 |
Ontology: nateglinide (C0903898)
| Definition (NCI) | A phenylalanine derivative of the meglitinide class of agents with hypoglycemic activity. Nateglinide, compared to repaglitinide, binds with a higher affinity to the SUR1 subunit and with a faster onset of action and a shorter duration of action. This agent is metabolized by the cytochrome P450 isoenzyme CYP2C9, and, to a lesser extent, by CYP3A4. The parent drug and metabolites are mainly excreted in the urine and its half-life is about 1.5 hours. |
| Concepts | Pharmacologic Substance (T121) , Amino Acid, Peptide, or Protein (T116) |
| MSH | C060142 |
| SnomedCT | 129496008, 134604002, 387070004 |
| LNC | LP64443-2, MTHU026435 |
| English | IPCCPA, N-((4-isopropylcyclohexyl)carbonyl)phenylalanine, nate-glinide, nateglinide (medication), NATEGLINIDE, nateglinide [Chemical/Ingredient], nateglinide, D-phenylalanine, N-((trans-4-(1-methylethyl)cyclohexyl)carbonyl)-, senaglinide, Nateglinide (product), Nateglinide (substance), Nateglinide |
| Spanish | nateglinida (concepto no activo), nateglinida (producto), nateglinida (sustancia), nateglinida |
Ontology: Starlix (C1323198)
| Concepts | Pharmacologic Substance (T121) , Organic Chemical (T109) |
| MSH | C060142 |
| English | starlix, Starlix, Novartis brand of nateglinide |
