Trade Names:Byetta- Injection, solution 5 mcg/dose- Injection, solution 10 mcg/dose
Glucagon-like peptide-1 agonist that enhances glucose-dependent insulin secretion, suppresses inappropriately elevated glucagon secretion, and slows gastric emptying.
Median peak plasma concentration achieved 2.1 h after subcutaneous administration. Similar exposure achieved with subcutaneous administration in abdomen, thigh, or upper arm.
Mean apparent Vd is 28.3 L.
Predominantly eliminated by glomerular filtration with subsequent proteolytic degradation. Mean Cl is 9.1 L/h. Mean terminal half life is 2.4 h. Concentrations are measurable for approximately 10 h postdose.
In patients with mild to moderate renal impairment, exposure was similar to that of patients with healthy renal function. Exposure increased by 3.37-fold in patients with ESRD receiving dialysis.Hepatic Function Impairment
No pharmacokinetic studies have been done; however, because exenatide is cleared primarily by the kidney, hepatic function impairment is not expected to affect blood levels.Elderly
Age does not influence pharmacokinetic properties of exenatide.Gender
Gender does not influence the distribution and elimination of exenatide.Race
Race does not influence the pharmacokinetics of exenatide.
Adjunctive therapy to diet and exercise to improve glycemic control in patients with type 2 diabetes mellitus.
Subcutaneous Initial dosage of 5 mcg twice daily at any time within the 60-min period before morning and evening meal. Increase dosage to 10 mcg twice daily after 1 mo if clinical response not adequate.
Store in refrigerator at 36° to 46°F. After first use, can be stored at a temperature not exceeding 77°F. Do not freeze. Protect from light. Discard 30 days after first use, even if some drug remains in the pen.
When coadministered, acetaminophen AUC and C max may be decreased and the T max increased. Give acetaminophen at least 1 h before or 4 h after exenatide injection.Digoxin
Coadministration of repeated doses of exenatide may decrease digoxin C max and delay the T max . Monitor the clinical response of the patient. If an interaction is suspected, adjust the digoxin dose as needed.Drugs that require rapid GI absorption (eg, antibiotics, oral contraceptives)
Because the extent and rate of absorption of these agents may be reduced by exenatide, instruct patients to take at least 1 h before exenatide injection.Food
Do not administer exenatide after a meal (administer exenatide within 60 min before the 2 main meals of the day, approximately 6 h or more apart).Hypoglycemic agents (eg, meglitinides [eg, repaglinide], sulfonylureas [glimepiride])
The risk of hypoglycemia may be increased. Closely monitor blood glucose concentrations when exenatide is started or stopped in patients receiving other hypoglycemic agents. Reinforce patient instructions for hypoglycemic management, especially in patients receiving a sulfonylurea.Lovastatin
Lovastatin AUC and C max may be decreased and the T max may be delayed when coadministered with exenatide. Monitor the clinical response of the patient. If an interaction is suspected, adjust the lovastatin dose as needed.Warfarin
Exenatide may lead to increased INR and possibly increased bleeding when coadministered with warfarin. Monitor PT more frequently after starting or changing the dose of exenatide. Once a stable PT is established, monitor PT at intervals usually recommended for patients taking warfarin.
None well documented.
Dizziness, feeling jittery, headache (9%); asthenia (4%); decreased appetite (1% to less than 2%); somnolence (postmarketing).
Hyperhidrosis (3%); generalized pruritus, macular or papular rash, urticaria (postmarketing).
Nausea (44%); diarrhea, vomiting (13%); dyspepsia (7%); gastroesophageal reflux disease (3%); abdominal distention, abdominal pain, acute pancreatitis, constipation, dysgeusia, eructation, flatulence, hemorrhagic and necrotizing pancreatitis sometimes resulting in death (postmarketing).
Kidney transplant and kidney transplant dysfunction, renal impairment, worsened chronic or acute renal failure (postmarketing).
Anaphylactic reactions, angioedema (postmarketing).
Increased serum creatinine (postmarketing).
Injection-site reaction (postmarketing).
Hypoglycemia (5%); dehydration (postmarketing).
Monitor glycemic response to exenatide. Monitor INR in patients also taking warfarin.
Category C .
Safety and efficacy not established.
Not recommended for use in patients with ESRD or severe renal function impairment (CrCl less than 30 mL/min).
Use commonly associated with GI adverse reactions. Not recommended for use in patients with severe GI disease.
Anti-exenatide antibodies may develop. No increase in rates or types of adverse reactions, but glycemic response may be attenuated in some patients with high titers.
Acute pancreatitis, including fatal and nonfatal hemorrhagic or necrotizing pancreatitis, has been reported. Discontinue treatment and do not resume if it develops.
Altered renal function has been reported. Use with caution in patients with risk factors for development of dehydration or renal impairment.
Not a substitute for insulin. Do not use in patients with type 1 diabetes or for treatment of diabetic ketoacidosis.
Rapid decline in blood glucose concentration; severe hypoglycemia; severe nausea and vomiting.
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