Exenatide

Exenatide Brand Names- Bydureon | Bydureon BCise | Byetta

What is Exenatide

Exenatide is a subcutaneously administered 39-amino acid glucagon-like peptide-1 agonist (GLP-1 RA) isolated from the salivary gland venom of the lizard Heloderma suspectum (Gila monster).

Exenatide was the first agent FDA-approved in the incretin mimetics class. Incretins are endogenous compounds, such as glucagon-like peptide-1 (GLP-1), that improve glycemic control once released into the circulation via the gut.

Exenatide mimics the enhancement of glucose-dependent insulin secretion and other antihyperglycemic actions of the incretins; exenatide has 53% amino acid similarity to mammalian GLP-1 and has a 3,000-fold greater potency for glucose lowering in vivo.

Exenatide is used to improve glycemic control in adult patients with type 2 diabetes mellitus (DM) who have not achieved adequate glycemic control on other medications.

The exenatide immediate-release injections are given twice daily with meals and can be used with other antidiabetic medications, including basal insulin. Use with short- or rapid-acting prandial insulin has not been studied and is not recommended.

Extended-release exenatide has been used once-weekly as monotherapy and may be used as part of combination therapy; use with prandial insulin has not been studied.

Several clinical trials have demonstrated the effectiveness of exenatide with other oral antidiabetic agents.

Exenatide injections significantly reduce hemoglobin A1C levels by a mean of 1.6% as monotherapy and a larger number of patients achieve their target A1C with its use when used as add-on therapy relative to placebo. Also, modest weight reductions occur.

As with other agents in the class, exenatide extended-release injections are not recommended as first-line therapy for patients who have inadequate glycemic control on diet and exercise because of the boxed warning regarding rodent C-cell tumor findings and the uncertain relevance to humans.

Metformin is first-line in the treatment of type 2 DM. Additional therapy with a GLP-1 RA that has proven cardiovascular (CV) benefit should be considered in patients with indicators of high-risk or established CV disease, independent of baseline A1C or individualized A1C target.

Among the GLP-1 RAs, evidence of CV benefit is strongest for liraglutide, favorable for semaglutide, and less certain for exenatide; there is no evidence of CV benefit with lixisenatide. GLP-1 RAs have high glucose-lowering efficacy, but with variation within the drug class.

Evidence suggests that the effect may be greatest for semaglutide once weekly, followed by dulaglutide and liraglutide, closely followed by exenatide once weekly, and then exenatide twice daily and lixisenatide.

GLP-1 RAs improve CV outcomes, as well as secondary outcomes such as heart failure (HF) and progression of renal disease, in patients with established CV disease or chronic kidney disease (CKD); this makes them an alternative treatment option in patients with indicators of high-risk or established heart failure HF or CKD who cannot tolerate a sodium-glucose cotransporter 2 inhibitor (SGLT2i). For patients requiring an injectable medication, GLP-1 RAs are preferred to insulin due to similar or even better efficacy in A1C reduction, lower risk of hypoglycemia, and reductions in body weight

Indications

• type 2 diabetes mellitus

For the treatment of type 2 diabetes mellitus in combination with diet and exercise

Side Effects

1. abdominal pain
2. alopecia
3. anaphylactoid reactions
4. angioedema
5. anorexia
6. antibody formation
7. asthenia
8. bleeding
9. cholecystitis
10. cholelithiasis
11. constipation
12. diarrhea
13. dizziness
14. drowsiness
15. dysgeusia
16. dyspepsia
17. eructation
18. fatigue
19. flatulence
20. gastroesophageal reflux
21. headache
22. hyperhidrosis
23. hypoglycemia
24. injection site reaction
25. maculopapular rash
26. nausea
27. new primary malignancy
28. pancreatitis
29. pruritus
30. renal failure (unspecified)
31. restlessness
32. sinus tachycardia
33. skin necrosis
34. thrombocytopenia
35. urticaria
36. vomiting
37. weight loss

Monitoring Parameters

• blood glucose
• glycosylated hemoglobin A1c (HbA1c)
• serum creatinine

Contraindications

• breast-feeding
• burns
• children
• cholelithiasis
• Crohn’s disease
• dehydration
• diabetic ketoacidosis
• dialysis
• fever
• gallbladder disease
• gastroparesis
• geriatric
• GI disease
• hypoglycemia
• hypovolemia
• infants
• infection
• inflammatory bowel disease
• kidney transplant
• medullary thyroid carcinoma (MTC)
• multiple endocrine neoplasia syndrome type 2 (MEN 2)
• pancreatitis
• pregnancy
• renal failure
• renal impairment
• surgery
• thrombocytopenia
• thyroid C-cell tumors
• thyroid cancer
• thyroid disease
• tobacco smoking
• trauma
• type 1 diabetes mellitus
• ulcerative colitis

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