Exenatide

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

Pharmacology

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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.

Pharmacokinetics

Absorption

Median peak plasma concentration achieved 2.1 h after subcutaneous administration. Similar exposure achieved with subcutaneous administration in abdomen, thigh, or arm.

Distribution

Mean apparent Vd is 28.3 L.

Elimination

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

Cl reduced to 0.9 L/h in patients with end-stage renal disease receiving dialysis. No dosage adjustment required in mild to moderate renal 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.

Indications and Usage

Adjunctive therapy to improve glycemic control in patients with type 2 diabetes mellitus who are taking metformin, a sulfonylurea, a thiazolidinedione, a combination of metformin and a sulfonylurea, or a combination of metformin and a thiazolidinedione, but who have not achieved adequate glycemic control.

Contraindications

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, discolored, or contains particulate matter.

Storage/Stability

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

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

Increased INR associated with bleeding has been reported.

Laboratory Test Interactions

None well documented.

Adverse Reactions

CNS

Dizziness, feeling jittery, headache (9%); asthenia, decreased appetite (1% to less than 5%); somnolence (postmarketing).

Dermatologic

Profuse sweating (1% to less than 5%); generalized pruritus, macular or popular rash, urticaria (postmarketing).

GI

Nausea (44%); diarrhea, vomiting (13%); dyspepsia (6%); gastroesophageal reflux disease (1% to less than 5%); abdominal distention, abdominal pain, acute pancreatitis, constipation, dysgeusia, eructation, flatulence (postmarketing).

Genitourinary

Acute renal failure (postmarketing).

Hypersensitivity

Anaphylactic reactions, angioedema (postmarketing).

Lab Tests

Increased serum creatinine (postmarketing).

Local

Injection-site reaction (postmarketing).

Metabolic-Nutritional

Dehydration (postmarketing).

Miscellaneous

Anti-exenatide antibodies, which usually diminish over time.

Precautions

Pregnancy

Category C .

Lactation

Undetermined.

Children

Safety and efficacy not established.

Renal Function

Not recommended for use in patients with end-stage renal disease 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.

Hypoglycemia

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

Immunogenicity

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.

Pancreatitis

Acute pancreatitis has been reported. Discontinue treatment and do not resume if it develops.

Type 1 diabetics

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

Overdosage

Symptoms

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 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; continuous or severe high blood sugar readings; low blood sugar episodes with few or no warning symptoms; severe, continuous, or frequent low blood sugar episodes.
• Instruct patients to report persistent, severe abdominal pain, which may be accompanied by vomiting, immediately to health care provider.
• Advise patients to inform health care provider if they are pregnant or planning to become pregnant, or breast-feeding, or if they have severe kidney disease or bowel motility disorder.

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