Glipizide (Glucotrol)
Second-generation sulfonylurea that stimulates insulin secretion from pancreatic beta cells by binding the SUR1 subunit of K-ATP channels, causing depolarization, Ca2+ influx, and insulin exocytosis. Metabolized primarily by CYP2C9; short half-life of 2-4 hours requires multiple daily dosing or extended-release GITS formulation. Hypoglycemia risk especially with renal impairment, elderly patients, or missed meals.
Projected serum levels — 5 mg, once daily
Maintenance schedule: 5 mg once daily (oral).
Modeled steady state after ~1 days: peak ≈ 3.0 mg, trough ≈ 0.025 mg body load. Population-based estimate over 15 days for a 5 mg dose at a 70 kg reference body mass — the interactive app scales curves to your doses, timing, and body mass.
Key facts
- Category
- Sulfonylurea
- Route modeled
- Oral
- Model confidence
- inferred
- Half-life
- 3 h
- Common dose
- 5 mg
- Suggested maximum
- 40 mg/day
- Reference dose range
- 2.5–40 mg (single dose)
- Suggested cadence
- once daily
- Validated against
- 5 mg oral — Cmax 0.40 mg/L at 2 h
Documented interactions
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danger
Carbamazepine (Tegretol) + Glipizide (Glucotrol)
Carbamazepine (Tegretol) inducer of CYP2C9 predicted to change Glipizide (Glucotrol) AUC by ~0.44x
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danger
CBD (Cannabidiol) + Glipizide (Glucotrol)
CBD (Cannabidiol) reversible_inhibitor of CYP2C9 predicted to change Glipizide (Glucotrol) AUC by ~2.47x
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danger
Efavirenz (Sustiva) + Glipizide (Glucotrol)
Efavirenz (Sustiva) inducer of CYP3A4 predicted to change Glipizide (Glucotrol) AUC by ~0.49x
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danger
Fluconazole + Glipizide (Glucotrol)
Fluconazole reversible_inhibitor of CYP2C9 predicted to change Glipizide (Glucotrol) AUC by ~2.47x
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danger
Fluvoxamine (Luvox) + Glipizide (Glucotrol)
Fluvoxamine (Luvox) reversible_inhibitor of CYP2C9 predicted to change Glipizide (Glucotrol) AUC by ~2.47x
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danger
Levothyroxine (Synthroid) + Glipizide (Glucotrol)
Glipizide (Glucotrol) may displace Levothyroxine (Synthroid) from plasma protein binding sites, transiently raising free drug concentration. This drug has a narrow therapeutic index; free…
Serum checks 208 modeled interaction pairings for glipizide (glucotrol) across your whole stack — absorption conflicts, enzyme inhibition, and nutrient depletion included.
Research behind this entry
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Intensive blood-glucose control with sulphonylureas or insulin compared with conventional treatment and risk of complications in patients with type 2 diabetes (UKPDS 33)
Landmark RCT of 3,867 patients showing intensive glucose control with sulfonylureas (including glipizide) or insulin reduced microvascular complications by 25% versus conventional treatment, establishing sulfonylureas…
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10-year follow-up of intensive glucose control in type 2 diabetes (UKPDS 80)
Post-trial follow-up demonstrating the glycemic legacy effect — early intensive glucose control with sulfonylureas/insulin continued to reduce myocardial infarction (15% RRR, p=0.014) and all-cause mortality (13% RRR,…
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A randomized trial comparing glipizide GITS with glyburide in type 2 diabetes
Comparative study demonstrating glipizide GITS (once-daily extended release) had lower hypoglycemia rates than glyburide while providing equivalent glycemic control, supporting the use of shorter-acting sulfonylureas in…
3 published studies referenced in the app, each with a plain-language summary.