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Incretin Mimetic
Aka: Incretin Mimetic, Byetta, Exenatide, Bydureon, Liraglutide, Victoza, GLP-1 Analog, Glucagon-Like Peptide 1, GLP-1
- See Also
- Sitagliptin (Januvia)
- Dipeptidyl Peptidase-4 Inhibitor (DPP-4 Inhibitor)
- Indications
- Type II Diabetes Mellitus
- Especially in Obesity
- May be used in combination with basal Insulin (e.g. Lantus)
- Insulin deficiency and Insulin Resistance
- Adjunct to Glucophage, Sulfonylureas, Glitazones
- Contraindications
- Type I Diabetes Mellitus
- Concurrent prandial Insulin (bolus Insulin)
- Basal Insulin (e.g. Lantus) may be used with Byetta
- Renal Failure: Creatinine Clearance <30 ml/min
- Mechanism
- Synthetic form of exendin-4
- Originally identified in Gila Monster Saliva
- Peptide with 39 amino acids
- Incretin Mimetic
- Incretin analogue that mimics endogenous hormone
- Incretin released from GI tract following meals
- Incretin effects
- Increases Glucose dependent Insulin secretion
- Delays gastric emptying
- Decreases food intake (improves satiety)
- Preparations
- Exenatide (Byetta)
- Glucagon-Like Peptide 1 (GLP-1) agonist derived from Gila monster Saliva
- Associated with weight loss and Nausea
- Exenatide Weekly (Bydureon)
- Injected once weekly
- More effective than Byetta and as effectiev as Victoza
- Less Nausea than Byetta or Victoza
- Requires reconstitution from powder before dose
- Liraglutide (Victoza)
- Single daily injection (as contrasted with twice daily Byetta)
- More potent than Byetta in lowering Hemoglobin A1C and similar efficacy to
- Adverse effects include Nausea (transient) and Headache
- Dosing: Byetta
- Initial
- Byetta 5 mcg SQ twice daily
- Give within 60 minutes of morning and evening meals
- Later, if Blood Sugars not optimized
- May increase to 10 mcg bid after 1 month
- Preparations: Prefilled pen holds 30 day supply
- 5 mcg/dose pen holds 1.2 ml of 250 mcg/ml
- 10 mcg/dose pen holds 2.4 ml of 250 mcg/ml
- Efficacy
- Lowers HBA1C 0.4 to 0.8% (at 5 and 10 mcg doses)
- Lowers weight by up to 4-10 pounds
- Cost
- Monthly: $340 per month
- Adverse effects: Byetta
- Nausea (44%) or Vomiting (13%)
- Less frequent with Bydureon
- Diarrhea (13%)
- Dizziness (9%)
- Headache (9%)
- Hypoglycemia
- With Sulfonylurea: 14.4% at 5 mcg, 35.7% at 10 mcg
- With Glucophage: 4.5% at 5 mcg, 5.3% at 10 mcg
- Pancreatitis
- Incidence may be as high as 1 in 50 on Byetta for two years
- Singh (2013) JAMA Intern Med 173(7):534-9
- Precautions
- Avoid using 2 Incretins (e.g. Byetta with Januvia) in combination (raises cost, risk of Pancreatitis without significant benefit)
- (2012) Presc Lett 19(8): 45
- References
- (2012) Presc Lett 19(3): 15
- Dungan (2005) Clin Diabetes 23: 56-62
- Ezzo (2006) Am Fam Physician 73
- Fineman (2003) Diabetes Care 26:2370-7
- Jones (2007) Am Fam Physician 75:1831-5
- Joy (2005) Ann Pharmacol 39:110-8