Non-Sulfonylurea Insulin Secretagogues

Aka: Non-Sulfonylurea Insulin Secretagogues, Meglitinide, Repaglinide, Prandin, Nateglinide, Starlix

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II. Mechanism

  1. Insulin secretogogue

III. Indication

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

IV. Contraindications

  1. Hypersensitivity Reaction to sulfa

V. Category

  1. Insulin Secretagogue

VI. Mechanism

  1. Benzoic acid derivative
  2. Similar to Sulfonylurea
    1. Binds different sites from Sulfonylureas
    2. Closes ATP sensitive K+ channels
    3. Results in Insulin secretion
    4. Shorter duration of binding and shorter effect
  3. Predominately effects postprandial Glucose

VII. Advantages

  1. Low risk of Hypoglycemia (2.4%)
  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

VIII. Adverse Effects

  1. Hypoglycemia (lower risk of Sulfonylureas)

IX. Disadvantages

  1. Two to three times as expensive as Sulfonylureas

X. Agents

  1. Repaglinide (Prandin)
  2. Nateglinide (Starlix)
    1. Significantly weaker activity compared with Prandin

XI. References

  1. Luna (2001) Am Fam Physician 63(9):1747-56 [PubMed]
  2. Luna (1999) Prim Care 26:895-915 [PubMed]

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Cost: Medications

repaglinide (on 5/17/2017 at Medicaid.Gov Survey of pharmacy drug pricing)
REPAGLINIDE 0.5 MG TABLET Generic $0.25 each
REPAGLINIDE 1 MG TABLET Generic $0.24 each
REPAGLINIDE 2 MG TABLET Generic $0.23 each
nateglinide (on 5/17/2017 at Medicaid.Gov Survey of pharmacy drug pricing)
NATEGLINIDE 120 MG TABLET Generic $0.56 each
NATEGLINIDE 60 MG TABLET Generic $0.54 each
starlix (on 1/4/2017 at Medicaid.Gov Survey of pharmacy drug pricing)
STARLIX 120 MG TABLET Generic $0.56 each
FPNotebook does not benefit financially from showing this medication data or their pharmacy links. This information is provided only to help medical providers and their patients see relative costs. Insurance plans negotiate lower medication prices with suppliers. Prices shown here are out of pocket, non-negotiated rates. See Needy Meds for financial assistance information.

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
Derived from the NIH UMLS (Unified Medical Language System)

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
Derived from the NIH UMLS (Unified Medical Language System)

Ontology: Prandin (C0722725)

Concepts Pharmacologic Substance (T121) , Organic Chemical (T109)
MSH C072379
English Prandin, repaglinide (Prandin), prandin, Novo Nordisk brand 2 of repaglinide
Derived from the NIH UMLS (Unified Medical Language System)

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
Derived from the NIH UMLS (Unified Medical Language System)

Ontology: Starlix (C1323198)

Concepts Pharmacologic Substance (T121) , Organic Chemical (T109)
MSH C060142
English starlix, Starlix, Novartis brand of nateglinide
Derived from the NIH UMLS (Unified Medical Language System)

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