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Drugs reference index «Exenatide»


Pronunciation: (ex-EN-a-tide)Class: Antidiabetic agent, Incretin mimetic agent

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.

Special Populations

Renal Function Impairment

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.


Age does not influence pharmacokinetic properties of exenatide.


Gender does not influence the distribution and elimination of exenatide.


Race does not influence the pharmacokinetics of exenatide.

Indications and Usage

Adjunctive therapy to diet and exercise to improve glycemic control in patients with type 2 diabetes mellitus.


Standard considerations.

Dosage and Administration


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.

General Advice

  • Administer dose in thigh, abdomen, or upper arm.
  • Do not administer after a meal.
  • Administer the doses approximately 6 h or more apart.
  • Exenatide solution is clear and colorless. Do not use if solution is cloudy or discolored, or contains particulate matter.


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.

Drug Interactions


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.


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.


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 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.


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.

Laboratory Test Interactions

None well documented.

Adverse Reactions


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).

Lab Tests

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.

Renal Function

Not recommended for use in patients with ESRD or severe renal function impairment (CrCl less than 30 mL/min).

GI disease

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.

Renal effects

Altered renal function has been reported. Use with caution in patients with risk factors for development of dehydration or renal impairment.

Type 1 diabetics

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.

Patient Information

  • Advise patient that medication will be started at a low dose but may be increased as tolerated to a dose that will provide max benefit.
  • Caution patient not to change the dose unless advised by health care provider. Instruct patient not to change frequency of administration.
  • Advise patient or caregiver to read the Medication Guide and Pen User Manual before using the first time and with each refill.
  • Advise patient that pen needles are not included with the prefilled pen and must be purchased separately. Advise patient to have health care provider determine which needle length and gauge would be best.
  • Ensure patient or caregiver understands how to store prefilled syringe, perform the “New Pen Set-Up” before using the first time, prepare and administer the dose, and dispose of used equipment and supplies. Caution patient not to store prefilled pen with the needle attached because medication may leak from the pen or air bubbles may form in the cartridge.
  • Instruct patient to administer prescribed dose by subcutaneous injection into the thigh, abdomen, or upper arm at any time within the 60-min period before the morning and evening meals. Caution patient not to administer medication after a meal.
  • Advise patient that if a dose is missed, to skip that dose and take the next one as scheduled. Caution patient not to double the dose to catch up.
  • Caution patient taking a sulfonylurea that low blood sugar (hypoglycemia) can occur when exenatide is started. Advise patient that health care provider may reduce the dose of the sulfonylurea to prevent this from happening.
  • Advise patient that treatment with this medication may reduce appetite, food intake, and body weight, but that no changes in exenatide dosing will need to be made if this occurs.
  • Educate patient or caregiver regarding diabetes and management, including target ranges for blood sugar control. Instruct patients that medication is not a substitute for diet and exercise and that they should continue to follow prescribed regimens.
  • Educate patient or caregiver regarding potential long-term complications of diabetes and need for regular general physical and eye examinations.
  • Ensure patient or caregiver understands how to use home glucose monitor and understands the need for frequent (eg, pre- and post-meal and bedtime) monitoring and recording of blood sugar measurements. Advise patient to take blood sugar log to each visit with health care provider.
  • Educate patient regarding value of periodic A 1c testing to confirm level of glucose control.
  • Review symptoms of hypoglycemia (low blood sugar) and hyperglycemia (high blood sugar) and action if either occurs.
  • Advise patient to discuss with health care provider a plan for managing each of the following situations: dosing diabetes medications during intercurrent conditions (eg, infection, sick days, stress, trauma, vomiting); accidental administration of too little or too much exenatide; inadequate food intake or a skipped meal; travel across time zones; change in physical activity.
  • Advise patient to carry medical identification (eg, card, bracelet) noting that they are diabetic.
  • Instruct patient to notify health care provider if any of the following occur: bothersome GI adverse reactions; injection-site reactions; serious hypersensitivity reactions; continuous or severe high blood sugar readings; low blood sugar episodes with little or no warning
  • Instruct patients to immediately report persistent, severe abdominal pain, which may be accompanied by vomiting, to health care provider.
  • Advise patients to inform health care provider if they are pregnant or planning to become pregnant, or breast-feeding.
  • Advise patients to inform health care provider if they have severe kidney disease or bowel motility disorder.

Copyright © 2009 Wolters Kluwer Health.

  • Exenatide MedFacts Consumer Leaflet (Wolters Kluwer)
  • Exenatide Detailed Consumer Information (PDR)
  • exenatide Subcutaneous Advanced Consumer (Micromedex) - Includes Dosage Information
  • exenatide Concise Consumer Information (Cerner Multum)

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