Glyburide (Diabeta / Micronase)
Second-generation sulfonylurea — the most potent and longest-acting in its class — that stimulates insulin secretion by blocking pancreatic beta-cell K-ATP channels (SUR1). Longer half-life (10 h) and active metabolites confer higher hypoglycemia risk than glipizide or glimepiride. Metabolized by CYP2C9 and CYP3A4; contraindicated in severe renal impairment.
Projected serum levels — 5 mg, once daily
Maintenance schedule: 5 mg once daily (oral).
Loading schedule: 6.3 mg on day 1, then 5 mg once daily — reaching therapeutic levels sooner.
Modeled steady state after ~1 days: peak ≈ 4.7 mg, trough ≈ 1.2 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
- 10 h
- Common dose
- 5 mg
- Suggested maximum
- 20 mg/day
- Reference dose range
- 1.3–20 mg (single dose)
- Suggested cadence
- once daily
- Validated against
- 5 mg oral — Cmax 0.25 mg/L at 3.5 h
Documented interactions
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danger
Carbamazepine (Tegretol) + Glyburide (Diabeta / Micronase)
Carbamazepine (Tegretol) inducer of CYP3A4 predicted to change Glyburide (Diabeta / Micronase) AUC by ~0.36x
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danger
Efavirenz (Sustiva) + Glyburide (Diabeta / Micronase)
Efavirenz (Sustiva) inducer of CYP3A4 predicted to change Glyburide (Diabeta / Micronase) AUC by ~0.24x
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danger
Levothyroxine (Synthroid) + Glyburide (Diabeta / Micronase)
Glyburide (Diabeta / Micronase) may displace Levothyroxine (Synthroid) from plasma protein binding sites, transiently raising free drug concentration. This drug has a narrow therapeutic index; free…
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danger
Rifampin + Glyburide (Diabeta / Micronase)
Rifampin inducer of CYP3A4 predicted to change Glyburide (Diabeta / Micronase) AUC by ~0.24x
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danger
St. John's Wort (Hypericum perforatum) + Glyburide (Diabeta / Micronase)
St. John's Wort (Hypericum perforatum) inducer of CYP3A4 predicted to change Glyburide (Diabeta / Micronase) AUC by ~0.43x
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danger
Tacrolimus (Prograf) + Glyburide (Diabeta / Micronase)
Glyburide (Diabeta / Micronase) may displace Tacrolimus (Prograf) from plasma protein binding sites, transiently raising free drug concentration. This drug has a narrow therapeutic index; free…
Serum checks 214 modeled interaction pairings for glyburide (diabeta / micronase) across your whole stack — absorption conflicts, enzyme inhibition, and nutrient depletion included.
Research behind this entry
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Effects of a fixed combination of perindopril and indapamide on macrovascular and microvascular outcomes in patients with type 2 diabetes mellitus (the ADVANCE trial): a randomised controlled trial
Landmark RCT of 11,140 type 2 diabetes patients, many on glyburide/gliclazide background therapy, showing intensive glucose control reduced nephropathy by 21% and strengthened the evidence for sulfonylurea-based…
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Effect of intensive blood-glucose control with metformin on complications in overweight patients with type 2 diabetes (UKPDS 34)
Companion to UKPDS 33, this trial of 1,704 overweight patients found metformin reduced all-cause mortality and stroke compared to sulfonylureas (including glyburide) or insulin, establishing metformin as preferred…
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Sulfonylurea inadequacy: efficacy of addition of insulin over 6 years in patients with type 2 diabetes mellitus in the UKPDS 57
UKPDS analysis of 826 patients on sulfonylurea monotherapy (primarily glyburide) demonstrating progressive beta-cell decline — 53% required insulin addition by 6 years, illustrating the natural history of type 2…
3 published studies referenced in the app, each with a plain-language summary.