Byetta (exenatide)
Last reviewed · Source: First Databank (FDB) drug data
Overview
Exenatide, a synthetic, human glucagon-like peptide-1 (GLP-1) receptor agonist (incretin mimetic), is an antidiabetic agent.
Exenatide, a synthetic analog of a naturally occurring peptide isolated from the saliva of Heloderma suspectum (Gila monster), is a glucagon-like peptide-1 (GLP-1) mimetic (incretin mimetic). Exenatide has 53% amino acid similarity to human GLP-1 and is structurally and pharmacologically unrelated to insulin, sulfonylureas, meglitinides, biguanides, thiazolidinediones, and alpha-glucosidase inhibitors. Several antihyperglycemic actions of exenatide similar to the effects of human GLP-1 are involved in the lowering of fasting and postprandial glucose concentrations in patients with type 2 diabetes mellitus.
The drug improves pancreatic beta-cell function by increasing glucose-dependent insulin synthesis, secretion, and acute beta-cell responsiveness (i.e., first phase insulin response). In contrast to sulfonylureas, stimulation of insulin secretion by exenatide subsides as blood glucose concentrations following a meal decrease and approach euglycemia. Exenatide inhibits inappropriately high glucagon secretion during episodes of hyperglycemia (e.g., after a meal) in patients with type 2 diabetes mellitus but does not impair the normal glucagon response to hypoglycemia.
In addition, exenatide slows gastric emptying, which reduces the rate of glucose absorption from a meal, reduces food intake, and is associated with weight loss; the drug also may reduce appetite and promote early satiety. Exenatide does not appear to be associated with clinically important prolongation of the QT interval (corrected for rate using Bazett's formula (QTc)).
Extended-release exenatide consists of exenatide incorporated in an extended-release microsphere formulation containing the 50:50 poly(D,L-lactide-co-glycolide) polymer along with sucrose. Each dose of extended-release exenatide contains 37.2 mg of the polymer and 0.8 mg of sucrose. Following a single dose of exenatide given as the extended-release formulation, the drug is released from the microspheres over approximately 10 weeks.
Exenatide plasma concentration peaks around week 2 and week 6-7 after administration of the extended-release formulation, representing an initial surface-bound release and then a more gradual release of the drug from microspheres. Steady-state plasma concentrations of the drug are reached at approximately 6-7 weeks with once-weekly (every 7 days) administration. Plasma exenatide concentrations generally fall to undetectable levels approximately 10 weeks after discontinuance of dosing.
USES: Exenatide is used with a proper diet and exercise program to control high blood sugar. It is used by people with type 2 diabetes. Controlling high blood sugar helps prevent kidney damage, blindness, nerve problems, loss of limbs, and sexual function problems.
Proper control of diabetes may also lessen your risk of a heart attack or stroke. Exenatide is a diabetes drug that is similar to a natural hormone in your body (incretin). It works by increasing insulin release (especially after a meal) and decreasing the amount of sugar your liver makes.
It also slows down food digestion in your stomach, decreases the amount of sugar absorbed from food, and may help decrease your appetite.
Generic name: exenatide
Pronunciation: (ex-EN-a-tide)
Reference product & biosimilars
No reference, biosimilar or interchangeable associated with this drug.
Today’s intelligence on Byetta
Indications
The following indications are listed for Byetta:
- Type 2 Diabetes Mellitus
Also known as: Adult Onset Diabetes, Adult Onset Diabetes Mellitus, Adult Onset Dm, Diabetes Mellitus Type 2, Diabetes Mellitus Type Ii, Ketosis-Resistant Diabetes Mellitus, Ketosis-Resistant Dm, Maturity Onset Diabetes, Maturity Onset Diabetes Mellitus, Non-Insulin Dependent Diabetes Mellitus, Non-Insulin-Dependent Diabetes Mellitus, Type Ii Diabetes Mellitus.
Dosing
No dosing information is available for this tab.
No dosing information is available for this tab.
No dosing information is available for this tab.
No dosing information is available for this tab.
Drug interactions
There is no enhanced messaging for this drug.
There are no contraindication interactions for this drug.
There are no severe interactions for this drug.
There are no moderate interactions for this drug.
Contraindications
Known hypersensitivity to exenatide or any ingredient in the formulation.
History of drug-induced immune-mediated thrombocytopenia from exenatide products.
Extended-release exenatide is contraindicated in patients with a personal or family history of medullary thyroid carcinoma (MTC) and in patients with multiple endocrine neoplasia syndrome type 2 (MEN 2).
There are no contraindication contraindications for this drug.
There are no severe contraindications for this drug.
There are no moderate contraindications for this drug.
Adverse reactions
The most common adverse effects (>=5%) in clinical trials of exenatide injection were nausea, hypoglycemia, vomiting,diarrhea, feeling jittery, dizziness, headache, dyspepsia,constipation, andasthenia. Nausea usually decreased over time.
The most common adverse effects (>=5%) in clinical trials of extended-release exanatide were injection-site nodule and nausea.
There are no severe adverse reactions for this drug.
There are no less severe adverse reactions for this drug.
Precautions
No enhanced messaging available.
Safety and efficacy of immediate-release exenatide have not been established in patients. Safety and efficacy of extended-release exenatide have not been established in pediatric patients <10 years of age. Use of extended-release exenatide in pediatric patients >=10 years of age is supported by a 24-week placebo-controlled trial witha previous formulation of extended-release exenatide and a 28-week open-label uncontrolled extension in 82 pediatric patients >=10 years of age with type 2 diabetes, a pediatricpharmacokinetic study, and studies in adults with type 2 diabetes mellitus.
Data are lacking on the use of exenatide or extended-release exenatide in pregnant women. In animal reproduction studies in rats, exenatide or extended-release exenatide use during pregnancy was associated with reduced fetal growth and skeletal ossification deficits. In animal reproduction studies in mice, exenatide use was associated with an increased number of neonatal deaths. Exenatide or extended-release exenatide should be used during pregnancy only if the potential benefit justifies the potential risk to the fetus.
Exenatide is distributed into milk in mice. It is not known whether exenatide is distributed into human milk. The benefits of breast-feeding and the importance of exenatide or extended-release exenatide to the woman should be considered along with any potential adverse effects on the breast-fed infant from the drug or from the underlying maternal condition.
Careful dosage selection is recommended in geriatric patients due to possible age-related decrease in renal function and concomitant disease and drug therapy; however, dosage requirements generally are similar in geriatric patients and younger adults. Caution should be used when initiating extended-release exenatide in geriatric patients.
No substantial differences in safety and efficacy nor in pharmacokinetics have been observed in geriatric patients relative to younger adults. Because geriatric patients are more likely to have decreased renal function, caution should be used when initiating therapy with the drug in such patients.
ICD codes
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Formulary status
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Last reviewed · Source: First Databank (FDB) drug data
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