GLIPIZIDE
Clinical safety rating: safe
Animal studies have demonstrated safety
Stimulates insulin secretion from pancreatic beta cells by binding to ATP-sensitive potassium channels, leading to membrane depolarization and calcium influx.
| Metabolism | Hepatic metabolism primarily via CYP2C9 to inactive metabolites |
| Excretion | Renal (80% as metabolites, 3-5% unchanged); biliary/fecal (20%) |
| Half-life | 2-4 hours (terminal); prolonged in renal impairment |
| Protein binding | 98-99% bound (primarily albumin) |
| Volume of Distribution | 0.11 L/kg (low, consistent with minimal extravascular distribution) |
| Bioavailability | Oral: 80-100% (well absorbed) |
| Onset of Action | Oral: 15-30 minutes (fasting); 30-60 minutes (postprandial) |
| Duration of Action | 12-24 hours (dose-dependent; shorter with lower doses, up to 24 h with maximum dose) |
Initial dose 5 mg orally once daily, titrated to 10-15 mg once daily; maximum 20 mg once daily. Divide into twice-daily dosing if >15 mg/day is required.
| Dosage form | TABLET |
| Renal impairment | eGFR ≥50 mL/min: no adjustment; eGFR 30-49 mL/min: start at 2.5 mg once daily, maximum 10 mg daily; eGFR <30 mL/min: contraindicated. |
| Liver impairment | Child-Pugh A: no adjustment; Child-Pugh B: start at 2.5 mg once daily, monitor closely; Child-Pugh C: avoid use. |
| Pediatric use | Not FDA-approved for pediatric use. Limited data: initial 2.5-5 mg once daily, titrate based on glycemic response; maximum 20 mg/day. |
| Geriatric use | Start at 2.5 mg once daily due to increased risk of hypoglycemia; titrate slowly; avoid using long-acting sulfonylureas; consider shorter-acting agents. |
| 1st trimester | Consult provider |
| 2nd trimester | Consult provider |
| 3rd trimester | Consult provider |
Clinical note
Drugs that increase hypoglycemia risk (eg beta-blockers) Can cause hypoglycemia.
| Breastfeeding | Glipizide is excreted in breast milk in low amounts. M/P ratio is approximately 0.4. Limited data suggest no adverse effects in infants, but theoretical risk of neonatal hypoglycemia. Caution advised; monitor infant for signs of hypoglycemia. |
| Teratogenic Risk | Glipizide is FDA pregnancy category C. First trimester: Limited human data; animal studies show no major teratogenicity but some fetal toxicity at high doses. Second and third trimesters: Sulfonylureas may cause neonatal hypoglycemia and macrosomia; risk of perinatal mortality may be increased. Avoid use during pregnancy; insulin is preferred. |
■ FDA Black Box Warning
None
| Common Effects | Hypoglycemia |
| Serious Effects |
["Type 1 diabetes mellitus","Diabetic ketoacidosis","Hypersensitivity to glipizide or sulfonylureas"]
| Precautions | ["Hypoglycemia","Hemolytic anemia in G6PD deficiency","Hepatic impairment","Renal impairment"] |
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| Fetal Monitoring | Monitor maternal blood glucose levels regularly. Fetal monitoring: ultrasound for fetal growth and amniotic fluid volume; nonstress test or biophysical profile in third trimester if indicated. Neonatal monitoring: observe for hypoglycemia, especially if glipizide used near term. |
| Fertility Effects | No known direct effects on fertility. Improved glycemic control may restore fertility in women with diabetes-related menstrual irregularities. |