DIABETA
Clinical safety rating: caution
Comprehensive clinical and safety monograph for DIABETA (DIABETA).
Glyburide is a sulfonylurea that stimulates insulin secretion from pancreatic beta cells by blocking ATP-sensitive potassium channels, leading to cell depolarization and calcium influx.
| Metabolism | Hepatic metabolism primarily via CYP2C9 to inactive metabolites. |
| Excretion | Approximately 50% renal (unchanged drug and metabolites), 50% biliary/fecal. Renal elimination accounts for 50% of dose, with about 20% unchanged and 30% as metabolites. Biliary excretion of metabolites contributes to fecal elimination. |
| Half-life | Terminal elimination half-life is approximately 10–12 hours in healthy individuals. Clinically, this supports once-daily dosing; may be prolonged in renal impairment. |
| Protein binding | Approximately 90–95% bound to serum albumin. |
| Volume of Distribution | Volume of distribution is approximately 0.1–0.3 L/kg, indicating distribution primarily into extracellular fluid. |
| Bioavailability | Oral bioavailability is nearly 100% for immediate-release formulations; extended-release formulations have slightly lower bioavailability (approximately 90%). |
| Onset of Action | Oral: Reduction in blood glucose begins within 1 hour; peak effect at 2–4 hours. For extended-release formulations, onset may be delayed but clinically significant effect within 2–4 hours. |
| Duration of Action | Duration of action for immediate-release: up to 12–14 hours, supporting twice-daily dosing. Extended-release: approximately 24 hours, allowing once-daily administration. Note: long-term glucose control requires regular dosing. |
Initial: 2.5-5 mg orally once daily, titrating to max 20 mg/day in 1-2 divided doses. Maintenance: 5-10 mg/day.
| Dosage form | TABLET |
| Renal impairment | GFR 30-60 mL/min: reduce dose by 50%. GFR <30 mL/min: avoid use. |
| Liver impairment | Child-Pugh A: no adjustment. Child-Pugh B: reduce dose by 50%. Child-Pugh C: avoid use. |
| Pediatric use | Not recommended for pediatric patients due to lack of safety data. |
| Geriatric use | Initial: 1.25-2.5 mg orally once daily; titrate slowly to avoid hypoglycemia. |
| 1st trimester | Consult provider |
| 2nd trimester | Consult provider |
| 3rd trimester | Consult provider |
Clinical note
Comprehensive clinical and safety monograph for DIABETA (DIABETA).
| Breastfeeding | Excreted in breast milk in low levels. M/P ratio not reported. Potential for hypoglycemia in infant. American Academy of Pediatrics considers compatible with breastfeeding; however, monitor infant for hypoglycemia, especially if maternal dose >10 mg/day. |
| Teratogenic Risk | FDA Pregnancy Category C: First trimester - limited human data; animal studies show no evidence of teratogenicity. Second and third trimesters - may cause neonatal hypoglycemia, and increased perinatal mortality due to maternal glycemic control. Avoid use during pregnancy; insulin preferred. |
■ FDA Black Box Warning
Increased risk of cardiovascular mortality based on the University Group Diabetes Program (UGDP) study.
| Serious Effects |
["Type 1 diabetes mellitus","Diabetic ketoacidosis","Known hypersensitivity to glyburide or sulfonylureas","Severe renal or hepatic impairment"]
| Precautions | ["Hypoglycemia risk, especially in elderly, debilitated, or malnourished patients","Hepatic or renal impairment may increase hypoglycemia risk","May cause hemolytic anemia in glucose-6-phosphate dehydrogenase (G6PD) deficiency","Use with caution in patients with history of sulfonamide allergy"] |
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| Fetal Monitoring |
| Monitor maternal blood glucose and HbA1c. For fetus: ultrasound for growth and anatomy, nonstress test or biophysical profile in third trimester. Monitor neonate for hypoglycemia, hyperbilirubinemia, and polycythemia. |
| Fertility Effects | No significant impact on fertility reported in humans. Animal studies show no adverse effects on fertility at clinically relevant doses. Glycemic control may improve fertility in women with diabetes. |