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All about: Exenatide

Big Image Pronouncation: (ex-EN-a-tide)
Class: Antidiabetic agent, Incretin mimetic agent

Trade Names:
- Subcutaneous injection 5 mcg/dose
- Subcutaneous injection 10 mcg/dose

Mechanism of Action


Incretin mimetic that mimics antihyperglycemic actions of incretins, including enhancing glucose-dependent insulin secretion, suppressing inappropriately elevated glucagon secretion, slowing gastric emptying, and reducing food intake.



Median peak plasma concentration achieved 2.1 h after subcutaneous administration. Similar exposure achieved with subcutaneous administration in abdomen, thigh, or 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 t ½ is 2.4 h. Concentrations are measurable for approximately 10 h postdose.

Special Populations

Renal Function Impairment

Cl reduced to 0.9 L/h in patient with end-stage renal disease receiving dialysis.

Indications and Usage

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 have not achieved adequate glycemic control.


Standard considerations.

Dosage and Administration


Subcutaneous Initial dose 5 mcg twice daily at any time within the 60-min period before morning and evening meal. Increase dose to 10 mcg twice daily after 1 mo if clinical response not adequate. Administer dose in thigh, abdomen, or upper arm. Exenatide solution is clear and colorless. Do not use if solution is cloudy, discolored, or contains particulate matter. Do not administer after a meal.


Store prefilled syringes in refrigerator (36° to 46°F). Protect from light and freezing. Do not use if exenatide has been frozen. Discard pen 30 days after first use, even if some drug remains in pen.

Drug Interactions

Drugs that require rapid GI absorption (eg, antibiotics, oral contraceptives)

Because extent and rate of absorption of these agents may be reduced by exenatide, take at least 1 h before exenatide injection.

Laboratory Test Interactions

None well documented.

Adverse Reactions


Dizziness, feeling of jitteriness, headache (at least 5%); asthenia, decreased appetite (less than 5%).


Perfuse sweating (less than 5%).


Diarrhea, dyspepsia, nausea, vomiting (at least 5%); gastroesophageal reflux disease (less than 5%).


Hypoglycemia (at least 5%).



Category C .




Safety and efficacy not established.

Renal Function

Not recommended for use in patients with end-stage renal disease or severe renal function impairment (Ccr less than 30 mL/min).

GI disease

Use commonly associated with GI side effects. Not recommended for use in patients with severe GI disease.


Incidence of hypoglycemia increases when used in combination with sulfonylurea. Consider reducing dose of sulfonylurea when adding exenatide.


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.

Type 1 diabetics

Not a substitute for insulin in insulin-requiring patients. Do not be used in patients with type 1 diabetes or for treatment of diabetic ketoacidosis.



Severe nausea and vomiting, rapid decline in blood glucose concentration; severe hypoglycemia.

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 patient information leaflet 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 patient that medication is not a substitute for diet and exercise and 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 1 C testing to confirm level of glucose control.
  • Review symptoms of hypoglycemia (low blood sugar) and hyperglycemia (high blood sugar) and action if either occur.
  • Advise patient to discuss with their 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: severe, continuous, or frequent low blood sugar episodes; low blood sugar episodes with few or no warning symptoms; continuous or severe high blood sugar readings; bothersome GI side effects; injection site reactions.

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