Exenatide Injection (Byetta™)
Manufacturer: Amylin Pharmaceuticals, Inc./Eli Lilly
Indication: Adjunctive therapy to improve glycemic control in patients with type-2 diabetes mellitus who are taking metformin, a sulfonylurea, or a combination of metformin and a sulfonylurea but who have not achieved adequate glycemic control.
Drug Class: This is the first in a new class of diabetes drugs called “incretin mimetics.” Exenatide is a synthetic version of exendin-4, a naturally occurring hormone in humans. The amino acid sequence of exenatide partially overlaps with that of the human incretin hormone glucagon-like peptide-1 (GLP-1), but its half-life is longer than that of native GLP-1. buy kamagra uk
Uniqueness of Drug: Exenatide binds to and activates the human GLP-1 receptor in vitro. Having many of the same glucoregulatory effects as GLP-1, exenatide mimics natural physiology for self-regulating glycemic control. By mimicking the mechanisms of this hormone, exenatide is a diabetes self-regulating drug that stays in the blood, working actively only when blood glucose concentrations are too high. In clinical trials, exenatide regulated glucose levels. Most patients in long-term exenatide clinical studies also experienced reductions in weight.
Precautions: Adverse drug events (ADEs) associated with exenatide are generally mild to moderate in intensity. In clinical trials, the most frequently reported ADE was nausea, which varied with the dose. With continued therapy, the frequency and severity of nausea decreased over time in most patients.
Patients receiving exenatide in combination with a sulfonyl-urea may be at a higher risk of hypoglycemia. To minimize this risk, practitioners might consider reducing the sulfonylurea dosage. When patients begin taking exenatide, health care providers should explain the symptoms, treatment, and conditions that tend to result in hypoglycemia, and they should review and reinforce the patient’s usual instructions for hypo-glycemia management.
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Patients should also be advised that treatment with exe-natide may lead to a reduction in appetite, food intake, or body weight and that there is no need to modify the dosing regimen because of these effects.
Contraindications: Exenatide is not a substitute for insulin. It is not indicated for patients with (1) type-1 diabetes or ketoacidosis, (2) end-stage renal disease, (3) a creatinine clearance of below 30 ml/minute, or (4) severe gastrointestinal disease, including gastroparesis.
The most common side effect is nausea. The safety and effectiveness of exenatide have not been established in children.
Dosage: Exenatide 5 mcg is administered subcutaneously twice daily within 60 minutes of the morning and evening meals.
Commentary: This agent mimics the action of GLP-1, which is secreted by the gastrointestinal tract to spearhead insulin production after a meal, when blood glucose levels are elevated. This is important, because other diabetes drugs stimulate insulin secretion even if levels are already low, leading to the risk of hypoglycemia. Exenatide is a synthetic version of a protein found in the saliva of the Gila monster that works in a manner similar to that of human GLP-1. Exenatide was administered in conjunction with the sulfonylureas; another common diabetes drug, metformin; or in combination with earlier treatments. Adding exenatide triggered a decline of approximately 1% in glycosylated hemoglobin (HbA1C), an important measurement of blood glucose averages. This activity is consistent with the reductions caused by other diabetes drugs.
Exenatide should be used with caution in patients receiving oral medications that require rapid gastrointestinal absorption.