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Glipizide (Monograph)

Drug class: Sulfonylureas

Medically reviewed by Drugs.com on May 10, 2025. Written by ASHP.

Introduction

Antidiabetic agent; sulfonylurea.1 2 3

Uses for Glipizide

Type 2 Diabetes Mellitus

Used as an adjunct to diet and exercise to improve glycemic control in adults with type 2 diabetes mellitus.1 2 3 19 27 50 51 52 53 54 55 56 57 58 59 60 95

Used as monotherapy and in combination with other antidiabetic agents (e.g., metformin, thiazolidinedione).127 153 156 157 166

Commercially available as a single entity preparation and in fixed combination with metformin.1 95 153

Guidelines from the American Diabetes Association (ADA) and other experts generally recommend that use of sulfonylureas for the treatment of type 2 diabetes mellitus be limited or discontinued due to increased risk of weight gain and hypoglycemia.708 709 Sulfonylureas may be considered in patients with access or cost barriers to other antidiabetic regimens.709 When used, these guidelines recommend the lowest possible dosage.708 When selecting a treatment regimen for type 2 diabetes mellitus, consider factors such as cardiovascular and renal comorbidities, drug efficacy and adverse effects, hypoglycemia risk, presence of overweight or obesity, cost, access, and patient preferences.708 709 Weight management should be included as a distinct treatment goal and other healthy lifestyle behaviors should also be considered.708 709

Not indicated for treatment of type 1 diabetes mellitus or diabetic ketoacidosis.1 95

Glipizide Dosage and Administration

General

Patient Monitoring

Dispensing and Administration Precautions

Administration

Oral Administration

Commercially available as single-entity tablets or in fixed combination with metformin hydrochloride.1 95 153

Immediate-release tablets: Usually administered initially as a single daily dose in the morning before breakfast; recommended to administer 30 minutes before meal to achieve maximum reduction in postprandial blood glucose concentration.1 11 32 Once-daily dosing at dosages up to 15—20 mg shown to provide adequate control of blood glucose throughout the day in most patients with usual meal patterns;1 2 39 40 41 42 43 44 however, some may have a more satisfactory response when administered as 2 or 3 divided doses.1 2 11 44 50 Dosages exceeding 15—20 mg daily should be administered in divided doses before meals of sufficient caloric content.1 2 59 When divided-dosing regimen employed in patients receiving more than 15 mg daily, doses and schedule of administration should be individualized according to patient's meal pattern and response.1 2 11 44 50 51 52 53 57 58 59 60 Dosages greater than 30 mg daily have been given safely in twice-daily dosing regimens for prolonged periods.1 When given concomitantly with colesevelam, administer glipizide at least 4 hours prior to colesevelam.1

Extended-release tablets: Administer once daily, generally with breakfast or first main meal of the day.95 Swallow whole and do not divide, chew, or crush.95 Patients receiving extended-release tablets may occasionally notice a tablet-like substance in their stools; this is normal since tablet containing drug is designed to remain intact and slowly release drug from a nonabsorbable shell during passage through GI tract.95 When given concomitantly with colesevelam, administer glipizide at least 4 hours prior to colesevelam.95

Fixed combination of glipizide and metformin hydrochloride: Should be taken once or twice daily with food.153 See full prescribing information for additional instructions for combination product.153

Dosage

Adults

Type 2 Diabetes Mellitus
Glipizide
Oral

Initially, 5 mg once daily.1 95

In patients predisposed to hypoglycemia (e.g., debilitated, malnourished, or geriatric patients; those with hepatic or renal impairment; patients taking other antidiabetic drugs), initial dosage of 2.5 mg daily recommended.1 27 71 95

Subsequent dosage should be adjusted according to patient's tolerance and therapeutic response.1 95

Immediate-release tablets: Adjust dosage in increments of 2.5—5 mg at intervals of at least several days.1 2 51 54 59 60 Dosages above 15 mg daily should be divided; total daily dosages above 30 mg have safely been given twice daily.1

Extended-release tablets: Patients receiving immediate-release tablets may be switched to extended-release tablets by giving nearest equivalent total daily dosage once daily.95

Transition period generally not required when transferring from other oral antidiabetic agents to immediate-release tablets.1 Patients being transferred from longer half-life sulfonylureas should be monitored for hypoglycemia during initial 1—2 weeks of transition period due to potential for overlapping drug effect.1

Maintenance dosage of glipizide varies considerably, ranging from 2.5—40 mg daily.1 2 7 27 39 40 41 42 43 44 50 51 52 53 54 56 57 58 59 60 Most patients require 5—25 mg daily as immediate-release tablets27 39 40 41 42 43 44 50 51 52 53 54 56 57 58 59 60 or 5—10 mg daily as extended release tablets, but some clinicians report higher dosages may be necessary.7 25 95 Maximum daily dosage is 40 mg daily as immediate-release tablets or 20 mg daily as extended-release tablets.1 95

Transitioning from Insulin Therapy

Patients maintained on insulin dosages ≤20 units daily: May transfer directly to usual recommended initial dosage of glipizide and administration of insulin may be abruptly discontinued.1 95

Patients requiring insulin dosages >20 units daily: Usual initial recommended dosage of glipizide should be started and insulin dosage reduced by 50%.1 95 Subsequently, insulin is withdrawn gradually and dosage of glipizide is adjusted at intervals of at least several days according to patient's tolerance and therapeutic response.1 95

During period of insulin withdrawal, patients should test urine at least 3 times daily for glucose and ketones, and should be instructed to report results to clinician so that appropriate adjustments can be made, if necessary.94 In some patients, especially those requiring greater than 40 units of insulin daily, manufacturer suggests it may be advisable to consider hospitalization during the transition from insulin to glipizide.1

Glipizide/Metformin Hydrochloride Fixed-combination Therapy
Oral

Initially, 2.5 mg of glipizide and 250 mg metformin hydrochloride once daily.153 In patients with more severe hyperglycemia (i.e., fasting plasma glucose 280—320 mg/dL), initial dosage of 2.5 mg of glipizide and 500 mg of metformin hydrochloride twice daily may be considered.153 Efficacy not established in patients with fasting plasma glucose concentrations exceeding 320 mg/dL.153

Increase dosage in increments of 1 tablet daily every 2 weeks until minimum effective dosage required to achieve adequate glycemic control or to a maximum daily dosage of 10 mg of glipizide and 2 g of metformin hydrochloride reached.153

Patients inadequately controlled with sulfonylurea or metformin monotherapy: Initially, 2.5 or 5 mg of glipizide and 500 mg of metformin hydrochloride twice daily with morning and evening meals.153 Initial dosage in fixed combination should not exceed daily dosage of glipizide or metformin hydrochloride already being taken to minimize risk of hypoglycemia.153 Dosage of fixed combination should be titrated upwards in increments not exceeding 5 mg of glipizide and 500 mg of metformin hydrochloride until adequate glycemic control or maximum daily dosage of 20 mg of glipizide and 2 g of metformin hydrochloride is reached.153

Patients currently receiving glipizide (or other sulfonylurea agent) and metformin (administered as separate tablets): Initially, 2.5 or 5 mg of glipizide and metformin 500 mg tablets; initial dosage of fixed-combination preparation should not exceed daily dosages of glipizide (or equivalent dosage of other sulfonylurea) and metformin hydrochloride currently being taken.153 When transferring from previous therapy to fixed combination preparation, decision to switch to nearest equivalent dosage or titrate dosage is based on clinical judgment.153 Hypoglycemia and hyperglycemia is possible in such patients and change in therapy should be undertaken with appropriate monitoring.153 Safety and efficacy of switching from combined therapy with separate preparations to the fixed-combination preparation have not been established in clinical studies.153

Special Populations

Hepatic Impairment

Glipizide Monotherapy

Immediate release: Initial dosage of 2.5 mg recommended; initial and maintenance dosage should be conservative to avoid hypoglycemic reactions.1

Extended release: Initial dosage of 2.5 mg recommended.95

Glipizide/Metformin Hydrochloride Fixed-combination Therapy

Avoid use in patients with clinical or laboratory evidence of hepatic disease.153

Renal Impairment

Glipizide Monotherapy

Immediate release: No specific population dosage recommendations at this time; initial and maintenance dosage should be conservative to avoid hypoglycemic reactions.1

Extended release: No specific population dosage recommendations at this time.95

Glipizide/Metformin Hydrochloride Fixed-combination Therapy

Do not initiate in patients with eGFR between 30—45 mL/minute per 1.73 m2.153

Contraindicated if eGFR is <30 mL/minute per 1.73 m2.153

If patient already taking and eGFR falls below 45 mL/minute per 1.73 m2, assess benefits and risks of continuing therapy.153 Discontinue if eGFR falls below 30 mL/minute per 1.73 m2.153

Geriatric Patients

Glipizide Monotherapy

Immediate release: Initial starting dosage of 2.5 mg recommended; dosage selection should be conservative, usually starting at low end of dosage range, reflecting greater frequency of decreased hepatic, renal, or cardiac function, and of concomitant disease or other drug therapy, to avoid hypoglycemic reactions.1

Extended release: Initial dosage of 2.5 mg recommended.95

Glipizide/Metformin Hydrochloride Fixed-combination Therapy

No specific population dosage recommendations at this time; do not titrate to maximum dosage to avoid risk of hypoglycemia.153 Initial and maintenance dosage selection should be conservative, usually starting at low end of dosage range, reflecting greater frequency of decreased renal function.153

Cautions for Glipizide

Contraindications

Warnings/Precautions

Increased Risk of Cardiovascular Mortality

Administration of oral hypoglycemic drugs reported to be associated with increased cardiovascular mortality as compared to treatment with diet alone or diet plus insulin.1 95

Warning based on study conducted by the University Group Diabetes Program (UGDP), which reported that administration of oral antidiabetic agents was associated with increased cardiovascular mortality compared to diet alone or diet and insulin.1 75 95 Results of the UGDP study exhaustively analyzed and there has been general disagreement in scientific and medical communities regarding study's validity and clinical importance.64 72 75 Results from the United Kingdom Prospective Diabetes (UKPD) study, a large, long-term (over 10 years) study in newly diagnosed type 2 diabetes did not confirm increase in cardiovascular events or mortality in group treated intensively with sulfonylureas, insulin, or combination therapy compared with less intensive conventional antidiabetic therapy.96 97 99 100

Although only one drug in the sulfonylurea class (tolbutamide) was included in the UGDP study, it is prudent from a safety standpoint to consider that this warning may also apply to other hypoglycemic drugs in this class, in view of their similarities in mode of action and chemical structure.1 95 Patients should be informed of potential risks and advantages of glipizide and of alternative therapies.1 95

Macrovascular Outcomes

Manufacturer states there are no clinical studies that conclusively establish macrovascular risk reduction with glipizide or any other antidiabetic drug.1 95

Renal and Hepatic Disease

Metabolism and excretion of glipizide may be slowed in patients with renal and/or hepatic impairment.1 If hypoglycemia occurs in such patients, it may be prolonged and appropriate management should be instituted.1

Hypoglycemia

All sulfonylurea drugs are capable of causing severe hypoglycemia.1 95 Hypoglycemia may occur in patients receiving glipizide alone or when used in combination with other antidiabetic agents; concomitant use with other antidiabetic agents increases risk of hypoglycemia.1 2 27 50 54 58 60 70 95 153

Ability to concentrate and react may be impaired as a result of hypoglycemia.95 Severe hypoglycemia can lead to unconsciousness or convulsions and may result in temporary or permanent impairment of brain function or death.95

Early warning signs of hypoglycemia may be different or less pronounced in patients with autonomic neuropathy, in geriatric patients, and in patients taking β-adrenergic blocking agents.95 These situations may result in severe hypoglycemia before the patient is aware of the hypoglycemia.95

Appropriate patient selection and careful attention to dosage are important to avoid glipizide-induced hypoglycemia.1 27 71 95 If hypoglycemia occurs during therapy with the drug, immediate reevaluation and adjustment of glipizide dosage and/or patient's meal pattern are necessary.1 2 27 A lower dosage of glipizide may be required to minimize risk of hypoglycemia when used concomitantly with other antidiabetic agents.95 Educate patients to recognize and manage hypoglycemia.95

Loss of Glycemic Control

When a patient stabilized on any antidiabetic regimen is exposed to stress (e.g., fever, trauma, infection, or surgery), loss of glycemic control may occur.1 At times, it may be necessary to discontinue glipizide and administer insulin.1

Effectiveness of any oral hypoglycemic drug in lowering blood glucose to a desirable level decreases in many patients over a period of time, which may be due to progression of severity of disease or diminished responsiveness to the drug.1

Hemolytic Anemia

Patients with glucose 6-phosphate dehydrogenase (G6PD) deficiency who receive sulfonylureas may develop hemolytic anemia.1 95 In patients with G6PD deficiency, a non-sulfonylurea antidiabetic agent should be considered.1

Hemolytic anemia also reported with glipizide during postmarketing experience in patients who did not have known G6PD deficiency.1 95

Gastrointestinal Obstruction

Obstructive symptoms in patients with known strictures reported in association with another drug with a non-dissolvable extended release formulation.95

Avoid use of extended-release glipizide tablets (Glucotrol XL) in patients with preexisting gastrointestinal narrowing (pathologic or iatrogenic).95

Use of Fixed Combinations

When glipizide is used in fixed combination with metformin, the cautions, precautions, and contraindications associated with metformin must be considered in addition to those associated with glipizide.153

Specific Populations

Pregnancy

Available data from a small number of published studies and postmarketing experience with extended-release glipizide tablets in pregnancy over decades have not identified any drug-associated risks for major birth defects, miscarriage, or adverse maternal outcomes.95

Poorly controlled diabetes mellitus in pregnancy carries risk to the mother and fetus; however, use of glipizide is generally not recommended and should be used only when clearly necessary (i.e., when insulin therapy is infeasible).1 2 65

Neonates born to women with gestational diabetes treated with sulfonylureas during pregnancy may be at increased risk for neonatal intensive care admission and may develop respiratory distress, hypoglycemia, or birth injury; they also may be large for gestational age.95 Prolonged, severe hypoglycemia lasting up to 4—10 days has been reported in some neonates born to women receiving sulfonylureas up to the time of delivery; this effect has been reported more frequently with use of agents having prolonged elimination half-lives.1 95 To minimize risk of neonatal hypoglycemia if glipizide is used during pregnancy, discontinue drug at least 2 weeks before expected delivery date.95 Neonates should be observed for symptoms of hypoglycemia and respiratory distress and managed accordingly.95

Lactation

Unknown whether glipizide is distributed into milk in humans; some sulfonylureas are distributed into human milk.1 No data on effects on milk production.95 Developmental and health benefits of breast-feeding should be considered along with mother's clinical need for glipizide and any potential adverse effects on the breast-fed child from glipizide or underlying maternal condition.95 If used during breast-feeding, infants should be monitored for signs of hypoglycemia (e.g., jitters, cyanosis, apnea, hypothermia, excessive sleepiness, poor feeding, seizures).95 If glipizide is discontinued and dietary management alone is inadequate for controlling blood glucose concentration, administration of insulin should be considered.1

Pediatric Use

Safety and efficacy not established.1 95

Geriatric Use

No overall differences in effectiveness or safety between younger and older patients, but greater sensitivity cannot be ruled out.1 95 Geriatric patients are particularly susceptible to hypoglycemic action of antidiabetic agents; hypoglycemia may be difficult to recognize in these patients.95 In general, dosage selection should be cautious, usually starting at the low end of dosage range, reflecting the greater frequency of decreased hepatic, renal, or cardiac function, and of concomitant disease or other drug therapy.1

Hepatic Impairment

No information regarding effects of hepatic impairment on glipizide disposition.95 As glipizide is highly protein bound and hepatic biotransformation is predominant route of elimination, pharmacokinetics and/or pharmacodynamics may be altered in hepatic impairment.95 If hypoglycemia occurs in such patients, it may be prolonged and appropriate management should be instituted.95

Renal Impairment

Pharmacokinetics not evaluated in patients with varying degrees of renal impairment.95 Limited data indicate that glipizide biotransformation products may remain in circulation for a longer time in subjects with renal impairment than seen in normal renal function.95

Common Adverse Effects

Most common adverse effects (>3%): Dizziness, diarrhea, nervousness, tremor, hypoglycemia, flatulence.95

Does Glipizide interact with my other drugs?

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Drug Interactions

Protein-bound Drugs

Because glipizide is highly protein bound, it theoretically could be displaced from binding sites by, or could displace from binding sites, other protein-bound drugs such as oral anticoagulants, hydantoins, salicylate and other NSAIAs, and sulfonamides.1 2 47 72 Protein binding of glipizide is nonionic; consequently, glipizide may be less likely to be displaced from binding sites by, or displace from binding sites, other highly protein-bound drugs whose protein binding is ionic in nature.46

Patients receiving highly protein-bound drugs should be observed for adverse effects when glipizide is initiated or discontinued and vice versa.1

Drugs That May Alter the Hypoglycemic Effect of Sulfonylureas

Several drugs may enhance the hypoglycemic effect of sulfonylurea antidiabetic agents, including glipizide.1 2 72 95 When these drugs are administered or discontinued in patients receiving glipizide, monitor closely for hypoglycemia or loss of glycemic control, respectively.1

Several drugs may decrease the hypoglycemic effect of sulfonylurea antidiabetic agents, including glipizide.1 72 95 When these drugs are administered or discontinued in patients receiving glipizide, monitor closely for loss of glycemic control or hypoglycemia, respectively.1 95

Specific Drugs

Drug

Interaction

Comments

β-adrenergic blocking agents

May impair glucose tolerance,62 72 increase frequency or severity of hypoglycemia,62 72 delay rate of recovery of blood glucose following drug-induced hypoglycemia,62 72 alter hemodynamic response to hypoglycemia,62 and possibly impair peripheral circulation62

May potentiate or weaken the hypoglycemic effect of glipizide95

Signs of hypoglycemia may be reduced or absent95

Increased frequency of monitoring may be required95

Use of a β1-selective adrenergic blocking agent may be preferred if concomitant therapy is necessary1 95

Alcohol

May potentiate or weaken the hypoglycemic effect of glipizide95

Disulfiram-like reactions have occurred very rarely1 58 85

Increased frequency of monitoring may be required95

Angiotensin-converting enzyme (ACE) inhibitors

May enhance the hypoglycemic effect of glipizide95

Observe closely for hypoglycemia or loss of glycemic control when administered or discontinued in patients receiving glipizide, respectively95

Angiotensin II receptor antagonists

May enhance the hypoglycemic effect of glipizide95

Observe closely for hypoglycemia or loss of glycemic control when administered or discontinued in patients receiving glipizide, respectively95

Atypical antipsychotic agents (e.g., clozapine, olanzapine)

May decrease the hypoglycemic effect of glipizide95

Observe closely for loss of glycemic control or hypoglycemia when administered or discontinued in patients taking glipizide, respectively95

Azole antifungals

May result in increased plasma concentrations of glipizide and/or hypoglycemia95

Fluconazole: Increases glipizide AUC by 57%95 165

Voriconazole: May enhance the hypoglycemic effect of glipizide95

Fluconazole, miconazole: Monitor closely for hypoglycemia1 95

Voriconazole: Observe closely for hypoglycemia or loss of glycemic control when administered or discontinued in patients receiving glipizide, respectively95

Calcium channel blocking agents

May decrease the hypoglycemic effect of glipizide95

Observe closely for loss of glycemic control or hypoglycemia when administered or discontinued in patients taking glipizide, respectively95

Chloramphenicol

May enhance the hypoglycemic effect of glipizide1 2 72 95

Observe closely for hypoglycemia or loss of glycemic control when administered or discontinued in patients receiving glipizide, respectively1 2 72 95

Cimetidine

Substantially increases AUC of glipizide83

May potentiate hypoglycemic effect of glipizide83

Monitor closely for signs and symptoms of hypoglycemia; dosage adjustment of glipizide may be necessary83

Clonidine

May either potentiate or weaken the hypoglycemic effect of glipizide95

Signs of hypoglycemia may be reduced or absent95

Increased frequency of monitoring may be required95

Colesevelam

Reduces AUC and peak plasma concentration of extended-release glipizide tablets by 12 and 13%, respectively, when used concomitantly1 95

Administer glipizide at least 4 hours prior to colesevelam1 95

Corticosteroids

May decrease the hypoglycemic effect of glipizide95

Observe closely for loss of glycemic control or hypoglycemia when administered or discontinued in patients taking glipizide, respectively95

Coumarins

May enhance the hypoglycemic effect of glipizide95

Observe closely for hypoglycemia or loss of glycemic control when administered or discontinued in patients receiving glipizide, respectively95

Danazol

May decrease the hypoglycemic effect of glipizide95

Observe closely for loss of glycemic control or hypoglycemia when administered or discontinued in patients taking glipizide, respectively95

Diazoxide

When glipizide administered to counter hyperglycemic effect of diazoxide in severely hypertensive patients with impairment in renal function, hypoglycemic reactions resulted87

Some clinicians recommend not to use these drugs concomitantly87

Diuretics

May decrease the hypoglycemic effect of glipizide1 72 95

Thiazide diuretics: May exacerbate diabetes mellitus, resulting in increased requirements of sulfonylurea antidiabetic agents, temporary loss of glycemic control, or secondary failure72

Observe closely for loss of glycemic control or hypoglycemia when administered or discontinued in patients taking glipizide, respectively1 72 95

Thiazide diuretics: Use concomitantly with caution72

Disopyramide

May enhance the hypoglycemic effect of glipizide95

Observe closely for hypoglycemia or loss of glycemic control when administered or discontinued in patients receiving glipizide, respectively95

Estrogens

May decrease the hypoglycemic effect of glipizide95

Observe closely for loss of glycemic control or hypoglycemia when administered or discontinued in patients taking glipizide, respectively95

Fibric acid derivatives

May enhance the hypoglycemic effect of glipizide95

Observe closely for hypoglycemia or loss of glycemic control when administered or discontinued in patients receiving glipizide, respectively95

Fluoxetine

May enhance the hypoglycemic effect of glipizide95

Observe closely for hypoglycemia or loss of glycemic control when administered or discontinued in patients receiving glipizide, respectively95

Glucagon

May decrease the hypoglycemic effect of glipizide95

Observe closely for loss of glycemic control or hypoglycemia when administered or discontinued in patients taking glipizide, respectively95

Guanethidine

Signs of hypoglycemia may be reduced or absent95

Increased frequency of monitoring may be required95

Histamine H2-receptor antagonists

May enhance the hypoglycemic effect of glipizide95

Observe closely for hypoglycemia or loss of glycemic control when administered or discontinued in patients receiving glipizide, respectively95

Hormonal contraceptives

May decrease the hypoglycemic effect of glipizide1 72

Observe closely for loss of glycemic control or hypoglycemia when administered or discontinued in patients taking glipizide, respectively1 72

Isoniazid

May decrease the hypoglycemic effect of glipizide1

Observe closely for loss of glycemic control or hypoglycemia when administered or discontinued in patients taking glipizide, respectively1

Monoamine oxidase (MAO) inhibitors

May enhance the hypoglycemic effect of glipizide1 2 72

Observe closely for hypoglycemia or loss of glycemic control when administered or discontinued in patients receiving glipizide, respectively1 2 72

Niacin

May decrease the hypoglycemic effect of glipizide1 72

Observe closely for loss of glycemic control or hypoglycemia when administered or discontinued in patients taking glipizide, respectively1 72

NSAIAs

May enhance the hypoglycemic effect of glipizide95

Observe closely for hypoglycemia or loss of glycemic control when administered or discontinued in patients receiving glipizide, respectively95

Pentoxifylline

May enhance the hypoglycemic effect of glipizide95

Observe closely for hypoglycemia or loss of glycemic control when administered or discontinued in patients receiving glipizide, respectively95

Phenothiazines

May decrease the hypoglycemic effect of glipizide1 72

Observe closely for loss of glycemic control or hypoglycemia when administered or discontinued in patients taking glipizide, respectively1 72

Phenytoin

May decrease the hypoglycemic effect of glipizide1

Observe closely for loss of glycemic control or hypoglycemia when administered or discontinued in patients taking glipizide, respectively1

Pramlintide

May enhance the hypoglycemic effect of glipizide95

Observe closely for hypoglycemia or loss of glycemic control when administered or discontinued in patients receiving glipizide, respectively95

Probenecid

May enhance the hypoglycemic effect of glipizide1 72 95

Observe closely for hypoglycemia or loss of glycemic control when administered or discontinued in patients receiving glipizide, respectively1 72 95

Progestogens

May decrease the hypoglycemic effect of glipizide95

Observe closely for loss of glycemic control or hypoglycemia when administered or discontinued in patients taking glipizide, respectively95

Protease inhibitors

May decrease the hypoglycemic effect of glipizide95

Observe closely for loss of glycemic control or hypoglycemia when administered or discontinued in patients taking glipizide, respectively95

Quinolones

May enhance the hypoglycemic effect of glipizide95

Observe closely for hypoglycemia or loss of glycemic control when administered or discontinued in patients receiving glipizide, respectively95

Reserpine

May potentiate or weaken the hypoglycemic effect of glipizide95

Signs of hypoglycemia may be reduced or absent95

Increased frequency of monitoring may be required95

Rifampin

May decrease the hypoglycemic effect of glipizide1 72

Observe closely for loss of glycemic control or hypoglycemia when administered or discontinued in patients taking glipizide, respectively1 72

Salicylates

May enhance the hypoglycemic effects of glipizide95

Observe closely for hypoglycemia or loss of glycemic control when administered or discontinued in patients receiving glipizide, respectively95

Somatostatin analogs (e.g., octreotide)

May enhance the hypoglycemic effects of glipizide95

Observe closely for hypoglycemia or loss of glycemic control when administered or discontinued in patients receiving glipizide, respectively95

Somatropin

May decrease the hypoglycemic effect of glipizide95

Observe closely for loss of glycemic control or hypoglycemia when administered or discontinued in patients taking glipizide, respectively95

Sulfonamide antibiotics

May enhance the hypoglycemic effect of glipizide95

Observe closely for hypoglycemia or loss of glycemic control when administered or discontinued in patients receiving glipizide, respectively1 95

Sympathomimetic agents (e.g., albuterol, epinephrine, terbutaline)

May decrease the hypoglycemic effect of glipizide1

Observe closely for loss of glycemic control or hypoglycemia when administered or discontinued in patients taking glipizide, respectively1

Thyroid hormones

May decrease the hypoglycemic effect of glipizide1 72 95

Observe closely for loss of glycemic control or hypoglycemia when administered or discontinued in patients taking glipizide, respectively95

Glipizide Pharmacokinetics

Absorption

Bioavailability

Rapidly and essentially completely absorbed from GI tract.1 30 31 32 33 34 35 36 37 38

Absolute oral bioavailability: 80—100%.30 31

Biphasic peak serum concentrations may occur, suggesting enterohepatic circulation.30 39

Onset

Peak plasma concentration: 1—3 hours (range: 1—6 hours).1 9 30 31 32 33 34 35 36 39

Onset of hypoglycemic action (fasting state): 15—30 minutes, maximal within 1—2 hours.32 33

Duration

Hypoglycemic action may persist for up to 24 hours.1 39 40 41 42 43 44

Food

Peak plasma concentration delayed 20—40 minutes when administered in fasting state compared to nonfasting state.1 32 33

Special Populations

Glipizide concentrations may be increased in renal or hepatic insufficiency.1

Distribution

Extent

Distributed into bile;30 34 37 very small amounts distributed into erythrocytes and saliva.30

Unknown if distributed into human milk.1

Plasma Protein Binding

92—99%;30 34 36 46 principally nonionic.46 47

Elimination

Metabolism

Almost completely metabolized in liver.1 30 34 35 36 37

Elimination Route

Excreted principally in the urine (60—90%) as unchanged drug and metabolites within 24—72 hours.30 34 35 36 37 Less than 10% excreted as unchanged drug.34 36

Also excreted in feces (5—20%),30 34 35 37 almost completely via biliary elimination.30 35 36 37

Half-life

Glipizide: 3—4.7 hours (range: 2—7.3 hours).9 30 31 32 33 34 35 38 39 48

Glipizide metabolites: 2—6 hours.37

Special Populations

Half-life of metabolites prolonged to greater than 20 hours in impaired renal function;37 however, glipizide metabolites largely considered inactive.37 49

Pharmacokinetics and/or pharmacodynamics may be altered in hepatic impairment.95

Renal excretion and terminal elimination half-life of metabolites substantially decreased and increased, respectively, in severe renal impairment.37

No differences in pharmacokinetics observed in geriatric patients compared with younger subjects.95

Stability

Storage

Oral

Tablets

Store at 20—25°C in a tight, light-resistant container.1

Tablets, extended release

Store at 20—25°C (excursions permitted to 15—30°C) protected from moisture and humidity.95

Actions

Advice to Patients

Additional Information

The American Society of Health-System Pharmacists, Inc. represents that the information provided in the accompanying monograph was formulated with a reasonable standard of care, and in conformity with professional standards in the field. Readers are advised that decisions regarding use of drugs are complex medical decisions requiring the independent, informed decision of an appropriate health care professional, and that the information contained in the monograph is provided for informational purposes only. The manufacturer’s labeling should be consulted for more detailed information. The American Society of Health-System Pharmacists, Inc. does not endorse or recommend the use of any drug. The information contained in the monograph is not a substitute for medical care.

Preparations

Excipients in commercially available drug preparations may have clinically important effects in some individuals; consult specific product labeling for details.

Please refer to the ASHP Drug Shortages Resource Center for information on shortages of one or more of these preparations.

* available from one or more manufacturer, distributor, and/or repackager by generic (nonproprietary) name

glipiZIDE

Routes

Dosage Forms

Strengths

Brand Names

Manufacturer

Oral

Tablets

5 mg*

glipiZIDE Tablets

10 mg*

glipiZIDE Tablets

Tablets, extended-release

2.5 mg*

glipiZIDE Tablets ER

Glucotrol XL

Pfizer

5 mg*

glipiZIDE Tablets ER

Glucotrol XL

Pfizer

10 mg*

glipiZIDE Tablets ER

Glucotrol XL

Pfizer

* available from one or more manufacturer, distributor, and/or repackager by generic (nonproprietary) name

glipiZIDE Combinations

Routes

Dosage Forms

Strengths

Brand Names

Manufacturer

Oral

Tablets, film-coated

2.5 mg with 250 mg Metformin Hydrochloride*

glipiZIDE with Metformin Hydrochloride Tablets

2.5 mg with 500 mg Metformin Hydrochloride*

glipiZIDE with Metformin Hydrochloride Tablets

5 mg with 500 mg Metformin Hydrochloride*

glipiZIDE with Metformin Hydrochloride Tablets

AHFS DI Essentials™. © Copyright 2025, Selected Revisions May 10, 2025. American Society of Health-System Pharmacists, Inc., 4500 East-West Highway, Suite 900, Bethesda, Maryland 20814.

References

Only references cited for selected revisions after 1984 are available electronically.

1. Apotex. Glipizide tablets prescribing information. Weston, FL; 2024 Sep.

2. Brogden RN, Heel RC, Pakes GE et al. Glipizide: a review of its pharmacological properties and therapeutic use. Drugs. 1979; 18:329-53. https://pubmed.ncbi.nlm.nih.gov/389600

3. Jackson JE, Bressler R. Clinical pharmacology of sulphonylurea hypoglycaemic agents: part 1. Drugs. 1981; 22:211-45. https://pubmed.ncbi.nlm.nih.gov/7021124

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