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Glipizide

GLUCOTROL

What it isSulfonylurea that blocks beta-cell KATP channels; type 2 diabetes.

Why this oneShorter action and inactive metabolites make it the preferred sulfonylurea when age or kidney disease makes glyburide unsafe.

What limits itHypoglycemia and weight gain limit it; missed meals increase risk. It fails as beta-cell reserve declines.

FDA-approved for

FDA label

FDA dosingPopulationStartTargetMax
Type 2 diabetes mellitus (adjunct to diet; IR tablets)Adults5 mg QD, ~30 min before breakfast (geriatric or liver disease: 2.5 mg QD)Minimum effective dose per blood glucose response; if single-dose response unsatisfactory, divide the dose15 mg QD as single dose; 40 mg/day total (divide doses >15 mg/day before meals)

Titration At least several days between titration steps (increments of 2.5–5 mg)

Renal Conservative initial and maintenance dosing to avoid hypoglycemia

Hepatic Start 2.5 mg QD; conservative initial/maintenance dosing (hypoglycemia may be prolonged)

No fixed regimen — dose to minimum effective by blood glucose monitoring; conservative dosing in elderly, debilitated/malnourished, renal or hepatic impairment

Instructions

Contraindications

Cautions

Adverse reactions

Pregnancy No drug-associated major-defect signal in decades of use, but sulfonylureas cross the placenta — neonatal hypoglycemia reported; discontinue ≥2 wk before expected delivery (from ER label)

Lactation Undetectable in human milk in one small assay-limited study; monitor breastfed infants for hypoglycemia (from ER label)

NO BOXED WARNINGS

Principal riskHypoglycemia, prolonged in renal impairment

Cost, est. cash$5–$150/month

Generic entry1994

Classes and tags

Clinical profile

Therapeutic safety burden2 / 4
Overdose danger4 / 4
Weight-gain liability2 / 4
Sedation liability0 / 4
QT / Torsades0 / 4
Direct muscarinic antagonism0 / 4
Embryofetal risk0 / 4

Legacy pregnancy categoryMultiple / indication-, trimester- or formulation-dependent

Defining liabilitySevere hypoglycemia can occur, especially with excess dosing, poor intake or interacting drugs.

Mechanism of action: Glipizide ballicule

Glipizide ballicule: receptor binding, kinetics and half-life diagram

Open Glipizide in the interactive console ↗

Memory aids: mascots and interaction avatars

Glipizide GLUCOTROL mascot mnemonic cartoon
“Clip a side for glucose control”
Glipizide CYP2C9 substrate avatar
CYP2C9 substrate

Open Glipizide in the interactive console ↗