BYDUREON
Clinical safety rating: caution
Comprehensive clinical and safety monograph for BYDUREON (BYDUREON).
Glucagon-like peptide-1 (GLP-1) receptor agonist; increases insulin secretion, decreases glucagon secretion, slows gastric emptying, and promotes satiety.
| Metabolism | Degraded by proteolytic enzymes to amino acids and small peptides; not primarily metabolized by CYP450 enzymes. |
| Excretion | Excreted primarily via renal proteolytic degradation; intact exenatide is eliminated renally. Renal clearance accounts for approximately 80% of total clearance; fecal elimination is negligible (<5%). |
| Half-life | Terminal elimination half-life is approximately 2.4 hours after subcutaneous administration for immediate-release exenatide; however, BYDUREON (extended-release) exhibits a prolonged half-life of approximately 2 weeks (mean range 14-20 days) due to encapsulation in microspheres. |
| Protein binding | Extensively bound to plasma proteins (>99%), primarily to albumin. |
| Volume of Distribution | Volume of distribution is approximately 28 L (0.4 L/kg for a 70 kg individual), indicating distribution into total body water, consistent with limited tissue penetration. |
| Bioavailability | Subcutaneous: Bioavailability is approximately 30% for the extended-release formulation, with dose-proportional exposure at steady-state. |
| Onset of Action | Subcutaneous: Therapeutic concentrations achieved within 2 weeks of initial dose; steady-state reached at 6-7 weeks. No immediate clinical effect as drug release is sustained. |
| Duration of Action | Duration of action is 1 week for glycemic control after a single subcutaneous injection of BYDUREON (extended-release formulation). Clinical effect persists over the week-long dosing interval. |
2 mg subcutaneously once every 7 days (weekly).
| Dosage form | FOR SUSPENSION, EXTENDED RELEASE |
| Renal impairment | No dose adjustment required for GFR ≥30 mL/min. Not recommended for GFR <30 mL/min or end-stage renal disease. |
| Liver impairment | No dose adjustment required for mild to moderate hepatic impairment (Child-Pugh class A or B). Not studied in severe hepatic impairment (Child-Pugh class C). |
| Pediatric use | Safety and efficacy not established in pediatric patients. |
| Geriatric use | No specific dose adjustment required; consider renal function due to age-related decline. |
| 1st trimester | Consult provider |
| 2nd trimester | Consult provider |
| 3rd trimester | Consult provider |
Clinical note
Comprehensive clinical and safety monograph for BYDUREON (BYDUREON).
| Breastfeeding | Unknown if excreted in human milk. M/P ratio not determined. Risk to infant cannot be excluded. Consider alternative therapies or discontinue breastfeeding. |
| Teratogenic Risk | Animal studies show fetal harm (reduced fetal weight, skeletal ossification delays) at systemic exposures similar to human. Human data insufficient. Risk cannot be excluded. Avoid in pregnancy, especially 2nd and 3rd trimesters. |
| Fetal Monitoring |
■ FDA Black Box Warning
Risk of thyroid C-cell tumors; contraindicated in patients with a personal or family history of medullary thyroid carcinoma or Multiple Endocrine Neoplasia syndrome type 2.
| Serious Effects |
["Personal or family history of medullary thyroid carcinoma","Multiple Endocrine Neoplasia syndrome type 2","Hypersensitivity to exenatide or any product components"]
| Precautions | ["Pancreatitis: discontinue if suspected","Hypoglycemia with concomitant use of insulin or sulfonylureas","Renal impairment: acute renal failure reported","Severe gastrointestinal disease: may worsen","Hypersensitivity reactions: angioedema, anaphylaxis","Diabetic retinopathy complications: monitor in patients with history"] |
| Food/Dietary | No specific food restrictions; however, BYDUREON delays gastric emptying, which may reduce the rate of absorption of oral medications. Administer oral medications requiring rapid absorption (e.g., antibiotics, acetaminophen) at least 1 hour before or 4 hours after injection. |
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| Monitor blood glucose, HbA1c, and fetal growth via ultrasound. Watch for maternal hypoglycemia or glycemic fluctuations. |
| Fertility Effects | No human studies on fertility. Animal studies show no impairment of fertility at high doses. |
| Clinical Pearls | BYDUREON (exenatide once weekly) is a GLP-1 receptor agonist for type 2 diabetes. Administer as a subcutaneous injection every 7 days. Do not adjust dose based on glucose; titrate only as per renal function (contraindicated if eGFR <30 mL/min/1.73m2). Risk of acute pancreatitis; monitor for unexplained abdominal pain. May cause weight loss and delay gastric emptying, potentially affecting absorption of oral medications. Avoid in patients with severe gastrointestinal disease (e.g., gastroparesis). |
| Patient Advice | Inject BYDUREON once every 7 days on the same day each week, at any time of day, with or without meals. · Store the single-dose tray in the refrigerator between 36°F to 46°F (2°C to 8°C) until use; do not freeze. · Rotate injection sites (abdomen, thigh, or upper arm) to reduce lipodystrophy. · Do not share pens or needles. Recap needle after use and dispose in a sharps container. · Seek immediate medical attention if you experience severe abdominal pain, nausea, or vomiting (signs of pancreatitis). · If you miss a dose, take it as soon as remembered, provided at least 3 days remain before the next scheduled dose; then resume weekly schedule. |