Endocrinology Book

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Incretin MimeticAka: Byetta, Exenatide, Sitagliptin, Januvia, GLP-1 Analog, Glucagon-Like Peptide 1

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  1. Indications
    1. Type II Diabetes Mellitus
    2. Insulin deficiency and Insulin Resistance
      1. Adjunct to Glucophage, Sulfonylureas, Glitazones
  2. Contraindications
    1. Type I Diabetes Mellitus
    2. Concurrent Insulin use
    3. Renal Failure: Creatinine Clearance <30 ml/min
  3. Mechanism
    1. Synthetic form of exendin-4
      1. Originally identified in Gila Monster Saliva
      2. Peptide with 39 amino acids
    2. Incretin Mimetic
      1. Incretin analogue that mimics endogenous hormone
      2. Incretin released from GI tract following meals
    3. Incretin effects
      1. Increases glucose dependent Insulin secretion
      2. Delays gastric emptying
      3. Decreases food intake (improves satiety)
  4. Preparations
    1. Exenatide (Byetta)
      1. GLP-1 Agonist derived from Gila monster Saliva
      2. Associated with weight loss and Nausea
    2. Sitagliptin (Januvia)
      1. Blocks DPP-4 allowing 2-3x accumulation of GLP-1
      2. Differs from Byetta: Weight neutral, no Nausea
  5. Dosing: Byetta
    1. Initial
      1. Byetta 5 mcg SQ twice daily
      2. Give within 60 minutes of morning and evening meals
    2. Later, if blood sugars not optimized
      1. May increase to 10 mcg bid after 1 month
    3. Preparations: Prefilled pen holds 30 day supply
      1. 5 mcg/dose pen holds 1.2 ml of 250 mcg/ml
      2. 10 mcg/dose pen holds 2.4 ml of 250 mcg/ml
  6. Efficacy: Byetta
    1. Lowers HBA1C 0.4 to 0.8% (at 5 and 10 mcg doses)
    2. Lowers weight by up to 4-10 pounds
  7. Cost: Byetta
    1. Monthly: $200 per month
  8. Adverse effects: Byetta
    1. Nausea (44%) or Vomiting (13%)
    2. Diarrhea (13%)
    3. Dizziness (9%)
    4. Headache (9%)
    5. Hypoglycemia
      1. With Sulfonylurea: 14.4% at 5 mcg, 35.7% at 10 mcg
      2. With Glucophage: 4.5% at 5 mcg, 5.3% at 10 mcg
  9. References
    1. Dungan (2005) Clin Diabetes 23:56
    2. Ezzo (2006) Am Fam Physician :
    3. Fineman (2003) Diabetes Care 26:2370
    4. Jones (2007) Am Fam Physician 75:1831
    5. Joy (2005) Ann Pharmacol 39:110

exenatide (C0167117)

ConceptsAmino Acid, Peptide, or Protein (T116) , Pharmacologic Substance (T121)
EnglishEx4 peptide, exenatide, Exendin 4
Spanishexenatida
CreditsDerived from the NIH UMLS (Unified Medical Language System)


sitagliptin (C1565750)

ConceptsOrganic Chemical (T109) , Pharmacologic Substance (T121)
Englishsitagliptin
Spanishsitagliptina
CreditsDerived from the NIH UMLS (Unified Medical Language System)


Byetta (C1636686)

ConceptsAmino Acid, Peptide, or Protein (T116) , Pharmacologic Substance (T121)
EnglishByetta
CreditsDerived from the NIH UMLS (Unified Medical Language System)


Januvia (C1702177)

ConceptsOrganic Chemical (T109) , Pharmacologic Substance (T121)
EnglishJanuvia
CreditsDerived from the NIH UMLS (Unified Medical Language System)



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