Drug reference

Exenatide

GLP-1 Receptor Agonist · Antidiabetic

Also known as Bydureon

GLP-1 Receptor AgonistAntidiabetic

CDSCO approved

EXCRETION

—

not curated

INTERACTIONS

2 major

SEVERE in our sources

PREGNANCY

FDA category + note

Top interactionssee all 4 →

BexaroteneSevereDatabaseDDInter
GatifloxacinSevereDatabaseDDInter

Mechanism

Binds to, and activates, the GLP-1 (glucagon-like peptide-1) receptor to increase insulin secretion, suppresses glucagon secretion, and slows gastric emptying.

Indications

Type 2 diabetes mellitus in combination with metformin or a sulfonylurea, or both, or with pioglitazone, or with both metformin and pioglitazone, in patients who have not achieved adequate glycaemic control with these drugs alone or in combinationType 2 diabetes mellitus in combination with basal insulin alone or with metformin or pioglitazone (or both)Mitigate antipsychotic-induced weight gainMonotherapy for type 2 diabetesAdjunctive therapy for type 2 diabetes (with metformin, sulfonylurea, or thiazolidinedione)Adjunctive therapy for type 2 diabetes (with basal insulin)type 2 diabetes mellitus (add-on to metformin/SU or combination, or pioglitazone in poorly controlled patients)

Dosing

Adult: Immediate-release (subcutaneous injection): Initially 5 micrograms twice daily for at least 1 month, then increased if necessary up to 10 micrograms twice daily. Dose to be taken within 1 hour before 2 main meals (at least 6 hours apart). Modified-release (subcutaneous injection): 2 mg once weekly.
Max dose: Immediate-release: 10 micrograms twice daily. Modified-release: 2 mg once weekly.

Pharmacokinetics

Peak effect

2 h

Duration

Effect of modified-release exenatide injection (Bydureon) may persist for 10 weeks after discontinuation.

Half-life

2-3 h

Bioavailability

SC: ∼100%

Protein binding

—

Excretion

Primarily by glomerular filtration, with tubular proteolysis

Contraindications

Serious and life-threatening cases of diabetic ketoacidosis have been reported in patients with type 2 diabetes mellitus when concomitant insulin was rapidly reduced or discontinued.

Side effects

Common

NauseaVomitingnausea (~50% recipients, tolerance develops)

Serious

Diabetic ketoacidosis (when concomitant insulin was rapidly reduced or discontinued)
Gallbladder disease (increased risk)
Pancreatitis (possible association)
Medullary carcinoma of the thyroid (contraindication)