Medically reviewed by Drugs.com. Last updated on Sep 24, 2020.
(ex EN a tide)
- AC 2993
Excipient information presented when available (limited, particularly for generics); consult specific product labeling. [DSC] = Discontinued product
Bydureon BCise: 2 mg/0.85 mL (0.85 mL)
Pen-injector, Subcutaneous [preservative free]:
Bydureon: 2 mg (1 ea)
Solution Pen-injector, Subcutaneous:
Byetta 10 MCG Pen: 10 mcg/0.04 mL (2.4 mL) [contains metacresol]
Byetta 5 MCG Pen: 5 mcg/0.02 mL (1.2 mL) [contains metacresol]
Suspension Reconstituted ER, Subcutaneous:
Bydureon: 2 mg (1 ea [DSC])
Brand Names: U.S.
- Bydureon BCise
- Byetta 10 MCG Pen
- Byetta 5 MCG Pen
- Antidiabetic Agent, Glucagon-Like Peptide-1 (GLP-1) Receptor Agonist
Exenatide is an analog of the hormone incretin (glucagon-like peptide 1 or GLP-1) which increases glucose-dependent insulin secretion, decreases inappropriate glucagon secretion, increases B-cell growth/replication, slows gastric emptying, and decreases food intake. Exenatide administration results in decreases in hemoglobin A1c by approximately 0.5% to 1% (immediate release) or 1.5% to 1.9% (extended release).
Vd: 28.3 L
Minimal systemic metabolism; proteolytic degradation may occur following glomerular filtration
Urine (majority of dose)
Time to Peak
Immediate release (daily) formulation: 2.1 hours
Extended release (weekly) formulation: Single dose: Initial period of release of surface-bound exenatide is followed by a gradual release from microspheres with peaks at week 2 and week 6 to 7 respectively; with once-weekly dosing steady state is achieved at 6 to 7 weeks (Bydureon) and 10 weeks (Bydureon BCise).
Immediate release (daily) formulation: 2.4 hours
Extended release (weekly) formulation: ~2 weeks
Special Populations: Renal Function Impairment
In patients with mild to moderate renal impairment, exposure to exenatide was increased compared with patients with normal renal function.
Use: Labeled Indications
Diabetes mellitus, type 2, treatment: As an adjunct to diet and exercise to improve glycemic control in adults with type 2 diabetes mellitus.
Prior serious hypersensitivity to exenatide or any component of the formulation; history of or family history of medullary thyroid carcinoma (exenatide ER only); patients with multiple endocrine neoplasia syndrome type 2 (exenatide ER only); history of drug-induced immune-mediated thrombocytopenia.
Canadian labeling: Additional contraindications (not in US labeling):
Bydureon: End-stage renal disease (ESRD) or severe renal impairment (CrCl <30 mL/minute) including dialysis patients.
Byetta: Diabetic ketoacidosis, diabetic coma/precoma or type 1 diabetes mellitus; ESRD or severe renal impairment (CrCl <30 mL/minute) including dialysis patients.
Note: Due to lack of additive glycemic benefit, avoid concomitant use with a dipeptidyl peptidase-4 inhibitor (ADA/EASD [Davies 2018]). May require a dose reduction of insulin and/or insulin secretagogues to avoid hypoglycemia.
Diabetes mellitus, type 2, treatment:
Note: May be used as an adjunctive agent or alternative monotherapy for patients who fail initial therapy with lifestyle intervention and metformin or who cannot take metformin. May be preferred when weight loss is desired and/or in patients with an HbA1c relatively far from goal (eg, HbA1c 9% to 10%) and type 1 diabetes is not likely; use has not been associated with improved or worsened cardiovascular outcomes (ADA 2020; Holman 2017; Wexler 2020).
Immediate release: Initial: 5 mcg twice daily within 60 minutes prior to morning and evening meals (or before the 2 main meals of the day, ≥6 hours apart); may increase to 10 mcg twice daily after 1 month if needed to achieve glycemic goals.
Missed dose: Missed dose should be skipped; resume at the next scheduled dose.
Extended release: 2 mg once weekly without regard to meals. If changing the day of administration is necessary, allow at least 3 days between 2 doses.
Missed dose: Missed dose should be administered as soon as possible if the next scheduled dose is due in ≥3 days; resume usual schedule thereafter. If there are <3 days until next scheduled dose, omit the missed dose and resume administration at the next scheduled weekly dose.
Conversion from immediate release to extended release:Initiate weekly administration of exenatide extended release the day after discontinuing exenatide immediate release. Note: May experience increased blood glucose levels for ~2 to 4 weeks after conversion. Pretreatment with exenatide immediate release is not required when initiating exenatide extended release.
Dosage adjustment for concomitant therapy: Significant drug interactions exist, requiring dose/frequency adjustment or avoidance. Consult drug interactions database for more information.
Refer to adult dosing.
Bydureon: Reconstitute vial/pen using provided diluent; use immediately.
SubQ: Administer via SubQ injection in the upper arm, thigh, or abdomen; rotate injection sites. If using concomitantly with insulin, administer as separate injections (do not mix); may inject in the same body region as insulin, but not adjacent to one another. Do not inject IV or IM.
Immediate release: Use only if clear, colorless, and free of particulate matter. Administer within 60 minutes prior to morning and evening meal (or prior to the 2 main meals of the day, approximately ≥6 hours apart). Set up each new pen before the first use by priming it. See pen user manual for further details. Dial the dose into the dose window before each administration.
ER: May administer without regard to meals or time of day.
Bydureon single-dose tray: Administer immediately after reconstitution in diluent, the mixture should be white to off-white and cloudy. Do not substitute needles or any other components provided with the single-dose tray.
Bydureon Pen: Allow pen to come to room temperature (wait at least 15 minutes after removal from refrigerator) prior to administration. Hold pen by the end with the orange label and tap firmly against palm of hand to mix (may need to tap up to 80 times or more to thoroughly mix); suspension should appear opaque and white to off-white and evenly mixed. Administer immediately after mixing. To ensure full dose is delivered, after insertion of needle press injection button until it clicks and hold for 10 seconds.
Bydureon BCise autoinjector: Allow autoinjector to come to room temperature (wait at least 15 minutes after removal from refrigerator) prior to administration. Shake autoinjector vigorously for at least 15 seconds; suspension should appear opaque and white to off-white and evenly mixed. Administer immediately after mixing. To ensure full dose is delivered, press autoinjector against skin until it clicks and hold for 15 seconds.
Bydureon single-dose tray or pen: Store under refrigeration at 2°C to 8°C (36°F to 46°F); vials/pens may be stored at ≤25°C (≤77°F) for up to 4 weeks. Do not freeze (discard if freezing occurs). Protect from light.
Bydureon BCise autoinjector: Store under refrigeration at 2°C to 8°C (36°F to 46°F); if necessary, may store at ≤30°C (≤86°F) for up to 4 weeks. Protect from light. Must be stored flat.
Byetta: Prior to initial use, store under refrigeration at 2°C to 8°C (36°F to 46°F); after initial use, may store at ≤25°C (≤77°F). Do not freeze (discard if freezing occurs). Protect from light. Pen should be discarded 30 days after initial use.
Alpha-Lipoic Acid: May enhance the hypoglycemic effect of Antidiabetic Agents. Monitor therapy
Androgens: May enhance the hypoglycemic effect of Agents with Blood Glucose Lowering Effects. Monitor therapy
Direct Acting Antiviral Agents (HCV): May enhance the hypoglycemic effect of Antidiabetic Agents. Monitor therapy
Estrogen Derivatives (Contraceptive): Exenatide may decrease the serum concentration of Estrogen Derivatives (Contraceptive). Management: Administer oral contraceptives at least one hour prior to exenatide. Consider therapy modification
Guanethidine: May enhance the hypoglycemic effect of Antidiabetic Agents. Monitor therapy
Hyperglycemia-Associated Agents: May diminish the therapeutic effect of Antidiabetic Agents. Monitor therapy
Hypoglycemia-Associated Agents: Antidiabetic Agents may enhance the hypoglycemic effect of Hypoglycemia-Associated Agents. Monitor therapy
Insulins: Glucagon-Like Peptide-1 Agonists may enhance the hypoglycemic effect of Insulins. Management: Consider insulin dose reductions when used in combination with glucagon-like peptide-1 agonists. Consider therapy modification
Maitake: May enhance the hypoglycemic effect of Agents with Blood Glucose Lowering Effects. Monitor therapy
Monoamine Oxidase Inhibitors: May enhance the hypoglycemic effect of Agents with Blood Glucose Lowering Effects. Monitor therapy
Pegvisomant: May enhance the hypoglycemic effect of Agents with Blood Glucose Lowering Effects. Monitor therapy
Progestins (Oral Contraceptive): Exenatide may decrease the serum concentration of Progestins (Oral Contraceptive). Management: Administer oral contraceptives at least one hour prior to exenatide. Consider therapy modification
Prothionamide: May enhance the hypoglycemic effect of Agents with Blood Glucose Lowering Effects. Monitor therapy
Quinolones: May enhance the hypoglycemic effect of Agents with Blood Glucose Lowering Effects. Quinolones may diminish the therapeutic effect of Agents with Blood Glucose Lowering Effects. Specifically, if an agent is being used to treat diabetes, loss of blood sugar control may occur with quinolone use. Monitor therapy
Ritodrine: May diminish the therapeutic effect of Antidiabetic Agents. Monitor therapy
Salicylates: May enhance the hypoglycemic effect of Agents with Blood Glucose Lowering Effects. Monitor therapy
Selective Serotonin Reuptake Inhibitors: May enhance the hypoglycemic effect of Agents with Blood Glucose Lowering Effects. Monitor therapy
Sincalide: Drugs that Affect Gallbladder Function may diminish the therapeutic effect of Sincalide. Management: Consider discontinuing drugs that may affect gallbladder motility prior to the use of sincalide to stimulate gallbladder contraction. Consider therapy modification
Sulfonylureas: Glucagon-Like Peptide-1 Agonists may enhance the hypoglycemic effect of Sulfonylureas. Management: Consider sulfonylurea dose reductions when used in combination with glucagon-like peptide-1 agonists. Consider therapy modification
Thiazide and Thiazide-Like Diuretics: May diminish the therapeutic effect of Antidiabetic Agents. Monitor therapy
Vitamin K Antagonists (eg, warfarin): Exenatide may enhance the anticoagulant effect of Vitamin K Antagonists. Monitor therapy
The following adverse drug reactions and incidences are derived from product labeling unless otherwise specified.
Incidence rates are for the extended release formulation unless otherwise noted.
Gastrointestinal: Nausea (extended release: 8% to 11%; immediate release: 8%), diarrhea (extended release: 4% to 11%; immediate release: ≥1% to 2%)
Immunologic: Immunogenicity (20%, injection site reaction)
Local: Injection site reaction (17%), injection site nodule (11%)
1% to 10%:
Central nervous system: Headache (4% to 8%), dizziness (extended release: 3%; immediate release: ≥1% to 2%)
Dermatologic: Injection site pruritus (3%)
Endocrine & metabolic: Hypoglycemia (4% to 5%), severe hypoglycemia (≤2%)
Gastrointestinal: Constipation (2% to 9%), dyspepsia (extended release: 7%; immediate release: 3%), vomiting (immediate release: 4%, extended release: 3%), decreased appetite (immediate release: ≥1% to <2%)
Immunologic: Antibody development (extended release: 6%; immediate release: 1%; associated with glycemic response)
Local: Erythema at injection site (2% to 5%)
Frequency not defined: Cardiovascular: Increased heart rate (Robinson 2013)
<1%, postmarketing, and/or case reports (all formulations): Abdominal distention, abdominal pain, abscess at injection site, acute pancreatitis, acute renal failure, alopecia, anaphylaxis, angioedema, cellulitis at injection site, drowsiness, dysgeusia, eructation, exacerbation of renal failure, flatulence, hemorrhagic pancreatitis, hypersensitivity reaction, increased serum creatinine, kidney transplant dysfunction, macular eruption, necrotizing pancreatitis, papular rash, prolongation P-R Interval on ECG (Linnebjerg 2011), pruritus, renal function abnormality, renal insufficiency, tissue necrosis at injection site, urticaria
ALERT: U.S. Boxed WarningRisk of thyroid C-cell tumors (Bydureon):
Exenatide extended release (ER) causes an increased incidence in thyroid C-cell tumors at clinically relevant exposures in rats compared with controls. It is unknown whether exenatide causes thyroid C-cell tumors, including medullary thyroid carcinoma (MTC), in humans as the human relevance of exenatide-ER-induced rodent thyroid C-cell tumors has not been determined.
Exenatide ER is contraindicated in patients with a personal or family history of MTC and in patients with multiple endocrine neoplasia syndrome type 2 (MEN 2). Counsel patients regarding the potential risk for MTC with the use of exenatide ER and inform them of symptoms of thyroid tumors (eg, mass in the neck, dysphagia, dyspnea, persistent hoarseness). Routine monitoring of serum calcitonin or using thyroid ultrasound is of uncertain value for detection of MTC in patients treated with exenatide ER.
Concerns related to adverse effects:
• Hypersensitivity: Serious hypersensitivity reactions (eg, anaphylaxis, angioedema) have been reported; discontinue therapy in the event of a hypersensitivity reaction. Serious injection-site reactions (eg, abscess, cellulitis, necrosis), with or without subcutaneous nodules have been reported with use. Isolated cases required surgical intervention.
• Gallbladder disease: Cases of cholelithiasis and cholecystitis have been reported; gallbladder studies and further clinical assessment are indicated if cholelithiasis is suspected.
• GI symptoms: Most common reactions are GI related; these symptoms may be dose-related and may decrease in frequency/severity with gradual titration and continued use.
• Pancreatitis: Cases of acute pancreatitis (including hemorrhagic and necrotizing with some fatalities) have been reported; monitor for signs and symptoms of pancreatitis (eg, persistent severe abdominal pain that may radiate to the back, and that may or may not be accompanied by vomiting). Prior to initiating therapy, consider other factors associated with pancreatitis that may be present (eg, hypertriglyceridemia, ethanol abuse, cholelithiasis); it is unknown if exenatide increases the risk for pancreatitis in these patients. If pancreatitis is suspected, discontinue use. Do not resume unless an alternative etiology of pancreatitis is confirmed. Consider alternative antidiabetic therapy in patients with a history of pancreatitis.
• Renal effects: Cases of acute renal failure and chronic renal failure exacerbation, including severe cases requiring hemodialysis or kidney transplantation, have been reported. May cause nausea/vomiting/diarrhea with transient hypovolemia that can worsen renal function. Renal dysfunction was usually reversible with appropriate corrective measures, including discontinuation of exenatide. Risk may be increased in patients receiving concomitant medications affecting renal function and/or hydration status.
• Thrombocytopenia: Serious bleeding (may be fatal) from drug-induced immune-mediated thrombocytopenia has been reported. Discontinue use and do not reinitiate therapy if drug-induced thrombocytopenia is suspected; thrombocytopenia may persist for ~10 weeks after discontinuation of therapy.
• Thyroid tumors: Bydureon: [US Boxed Warning] Thyroid C-cell tumors have developed in animal studies with exenatide ER; it is not known if exenatide ER causes thyroid C-cell tumor, including medullary thyroid carcinoma (MTC) in humans. Patients should be counseled on the potential risk of MTC with the use of exenatide and informed of symptoms of thyroid tumors (eg, neck mass, dysphagia, dyspnea, persistent hoarseness). Use of exenatide ER is contraindicated in patients with a personal or a family history of medullary thyroid cancer and in patients with multiple endocrine neoplasia syndrome type 2 (MEN2). Consultation with an endocrinologist is recommended in patients who develop elevated calcitonin concentrations or have thyroid nodules detected during imaging studies or physical exam; routine monitoring of serum calcitonin or using thyroid ultrasound for early detection of MTC is of unknown value. Cases of MTC in humans have been reported with the GLP-1 agonist, liraglutide.
• Bariatric surgery:
- Dehydration: Evaluate, correct, and maintain postsurgical fluid requirements and volume status prior to initiating therapy, and closely monitor the patient for the duration of therapy; acute and chronic kidney failure exacerbation may occur. A majority of cases occurred in patients with nausea, vomiting, diarrhea, and/or dehydration. Nausea is common and fluid intake may be more difficult after gastric bypass, sleeve gastrectomy, and gastric band (Mechanick 2013).
- Excessive glucagon-like peptide-1 exposure: Closely monitor for efficacy and assess for signs and symptoms of pancreatitis if therapy is initiated after surgery; gastric bypass and sleeve gastrectomy (but not gastric band) significantly increase endogenous postprandial glucagon-like peptide-1 (GLP-1) concentrations (Korner 2009; Peterli 2012). Administration of exogenous GLP-1 agonists may be redundant to surgery effects.
• GI disease: Not recommended to be used in patients with gastroparesis or severe GI disease due to frequent GI adverse effects associated with use.
• Renal impairment: Use is not recommended in patients with a CrCl <30 mL/minute (exenatide) or <45 mL/minute (exenatide ER) or end-stage renal disease (ESRD). If used in renal transplant patients, monitor for hypovolemia.
Dosage form specific issues:
• Injection-site reactions: Bydureon: Serious injection-site reactions (eg, abscess, cellulitis, necrosis), with or without subcutaneous nodules, have been reported.
• Multiple dose injection pens: According to the CDC, pen-shaped injection devices should never be used for more than one person (even when the needle is changed) because of the risk of infection. The injection device should be clearly labeled with individual patient information to ensure that the correct pen is used (CDC 2012).
• Appropriate use: Not for use in patients with type 1 diabetes mellitus or diabetic ketoacidosis.
• Duplicate therapy: Avoid concurrent use of extended-release (weekly) and immediate-release (daily) exenatide formulations.
Serum glucose, HbA1c (at least twice yearly in patients who have stable glycemic control and are meeting treatment goals; quarterly in patients not meeting treatment goals or with therapy change [ADA 2020]), renal function, volume status, weight, triglycerides, signs/symptoms of pancreatitis, signs/symptoms of gallbladder disease.
Based on in vitro data, exenatide has a low potential to cross the placenta (Hiles 2003).
Poorly controlled diabetes during pregnancy can be associated with an increased risk of adverse maternal and fetal outcomes, including diabetic ketoacidosis, preeclampsia, spontaneous abortion, preterm delivery, delivery complications, major birth defects, stillbirth, and macrosomia. To prevent adverse outcomes, prior to conception and throughout pregnancy, maternal blood glucose and HbA1c should be kept as close to target goals as possible but without causing significant hypoglycemia (ADA 2020; Blumer 2013).
Agents other than exenatide are currently recommended to treat diabetes mellitus in pregnancy (ADA 2020).
What is this drug used for?
• It is used to lower blood sugar in patients with high blood sugar (diabetes).
All drugs may cause side effects. However, many people have no side effects or only have minor side effects. Call your doctor or get medical help if any of these side effects or any other side effects bother you or do not go away:
• Injection site bump or itching
• Loss of strength and energy
WARNING/CAUTION: Even though it may be rare, some people may have very bad and sometimes deadly side effects when taking a drug. Tell your doctor or get medical help right away if you have any of the following signs or symptoms that may be related to a very bad side effect:
• Kidney problems like unable to pass urine, blood in the urine, change in amount of urine passed, or weight gain
• Gallstones like pain in the upper right abdominal area, right shoulder area, or between the shoulder blades; yellow skin or eyes; or fever with chills
• Thyroid cancer like new lump or swelling in the neck, pain in the front of the neck, persistent cough, persistent change in voice like hoarseness, or trouble swallowing or breathing
• Pancreatitis like severe abdominal pain, severe back pain, severe nausea, or vomiting
• Low blood sugar like dizziness, headache, fatigue, feeling weak, shaking, fast heartbeat, confusion, increased hunger, or sweating
• Passing out
• Severe injection site pain, swelling, hardness, blisters, dark scab, lumps, open wound, or severe skin irritation
• Signs of an allergic reaction, like rash; hives; itching; red, swollen, blistered, or peeling skin with or without fever; wheezing; tightness in the chest or throat; trouble breathing, swallowing, or talking; unusual hoarseness; or swelling of the mouth, face, lips, tongue, or throat.
Note: This is not a comprehensive list of all side effects. Talk to your doctor if you have questions.
Consumer Information Use and Disclaimer: This information should not be used to decide whether or not to take this medicine or any other medicine. Only the healthcare provider has the knowledge and training to decide which medicines are right for a specific patient. This information does not endorse any medicine as safe, effective, or approved for treating any patient or health condition. This is only a limited summary of general information about the medicine's uses from the patient education leaflet and is not intended to be comprehensive. This limited summary does NOT include all information available about the possible uses, directions, warnings, precautions, interactions, adverse effects, or risks that may apply to this medicine. This information is not intended to provide medical advice, diagnosis or treatment and does not replace information you receive from the healthcare provider. For a more detailed summary of information about the risks and benefits of using this medicine, please speak with your healthcare provider and review the entire patient education leaflet.
Always consult your healthcare provider to ensure the information displayed on this page applies to your personal circumstances.
More about exenatide
- Side Effects
- During Pregnancy or Breastfeeding
- Dosage Information
- Drug Interactions
- 376 Reviews
- Drug class: incretin mimetics
- FDA Alerts (2)