pharmacopeia
GET
/api/v1/drug/glipizide
2D structure
N-[2-[4-(cyclohexylcarbamoylsulfamoyl)phenyl]ethyl]-5-methylpyrazine-2-carboxamide
SMILES CC1=CN=C(C=N1)C(=O)NCCC2=CC=C(C=C2)S(=O)(=O)NC(=O)NC3CCCCC3
InChIKey ZJJXGWJIGJFDTL-UHFFFAOYSA-N

Mechanism of action

Sourced from openFDA

The primary mode of action of glipizide in experimental animals appears to be the stimulation of insulin secretion from the beta cells of pancreatic islet tissue and is thus dependent on functioning beta cells in the pancreatic islets. In humans, glipizide appears to lower the blood glucose acutely by stimulating the release of insulin from the pancreas, an effect dependent upon functioning beta cells in the pancreatic islets.

Insulin Receptor

Indications

Sourced from openFDA
  • Glipizide Tablets USP are indicated as an adjunct to diet and exercise to improve glycemic control in adults with type 2 diabetes mellitus.ICD-10: E11.9

Contraindications

Sourced from openFDA
  • Glipizide is contraindicated in patients with: 1. Known hypersensitivity to the drug.contraindicated

Dosage & administration

Sourced from openFDA

There is no fixed dosage regimen for the management of diabetes mellitus with glipizide or any other hypoglycemic agent. In addition to the usual monitoring of urinary glucose, the patient’s blood glucose must also be monitored periodically to determine the minimum effective dose for the patient; to detect primary failure, i.e., inadequate lowering of blood glucose at the maximum recommended dose of medication; and to detect secondary failure, i.e., loss of an adequate blood-glucose-lowering response after an initial period of effectiveness. Glycosylated hemoglobin levels may also be of value in monitoring the patient’s response to therapy. Short-term administration of glipizide may be sufficient during periods of transient loss of control in patients usually controlled well on diet. In general, glipizide should be given approximately 30 minutes before a meal to achieve the greatest reduction in postprandial hyperglycemia. Initial Dose The recommended starting dose is 5 mg, given before breakfast. Geriatric patients or those with liver disease may be started on 2.5 mg. Titration Dosage adjustments should ordinarily be in increments of 2.5 to 5 mg, as determined by blood glucose response. At least several days should elapse between titration steps. If response to a single dose is not satisfactory, dividing that dose may prove effective. The maximum recommended once daily dose is 15 mg. Doses above 15 mg should ordinarily be divided and given before meals of adequate caloric content. The maximum recommended total daily dose is 40 mg.

Warnings & precautions

Sourced from openFDA

SPECIAL WARNING ON INCREASED RISK OF CARDIOVASCULAR MORTALITY The administration of oral hypoglycemic drugs has been reported to be associated with increased cardiovascular mortality as compared to treatment with diet alone or diet plus insulin. This warning is based on the study conducted by the University Group Diabetes Program (UGDP), a long-term prospective clinical trial designed to evaluate the effectiveness of glucose-lowering drugs in preventing or delaying vascular complications in patients with non-insulin-dependent diabetes. The study involved 823 patients who were randomly assigned to one of four treatment groups ( Diabetes , 19, supp. 2:747-830, 1970). UGDP reported that patients treated for 5 to 8 years with diet plus a fixed dose of tolbutamide (1.5 grams per day) had a rate of cardiovascular mortality approximately 2½ times that of patients treated with diet alone. A significant increase in total mortality was not observed, but the use of tolbutamide was discontinued based on the increase in cardiovascular mortality, thus limiting the opportunity for the study to show an increase in overall mortality. Despite controversy regarding the interpretation of these results, the findings of the UGDP study provide an adequate basis for this warning. The patient should be informed of the potential risks and advantages of glipizide and of alternative modes of therapy.

Adverse reactions

Sourced from openFDA

In U.S. and foreign controlled studies, the frequency of serious adverse reactions reported was very low. Of 702 patients, 11.8% reported adverse reactions and in only 1.5% was glipizide discontinued. Hypoglycemia See PRECAUTIONS and OVERDOSAGE sections. Gastrointestinal Gastrointestinal disturbances are the most common reactions. Gastrointestinal complaints were reported with the following approximate incidence: nausea and diarrhea, one in seventy; constipation and gastralgia, one in one hundred. They appear to be dose-related and may disappear on division or reduction of dosage. Cholestatic jaundice may occur rarely with sulfonylureas: glipizide should be discontinued if this occurs. Dermatologic Allergic skin reactions including erythema, morbilliform or maculopapular eruptions, urticaria, pruritus, and eczema have been reported in about one in seventy patients. These may be transient and may disappear despite continued use of glipizide; if skin reactions persist, the drug should be discontinued. Porphyria cutanea tarda and photosensitivity reactions have been reported with sulfonylureas. Hematologic Leukopenia, agranulocytosis, thrombocytopenia, hemolytic anemia (see PRECAUTIONS ), aplastic anemia, and pancytopenia have been reported with sulfonylureas. Metabolic Hepatic porphyria and disulfiram-like reactions have been reported with sulfonylureas. In the mouse, glipizide pretreatment did not cause an accumulation of acetaldehyde after ethanol administration.

Use in specific populations

Sourced from openFDA

Pregnancy Glipizide was found to be mildly fetotoxic in rat reproductive studies at all dose levels (5 to 50 mg/kg). This fetotoxicity has been similarly noted with other sulfonylureas, such as tolbutamide and tolazamide. The effect is perinatal and believed to be directly related to the pharmacologic (hypoglycemic) action of glipizide. In studies in rats and rabbits, no teratogenic effects were found. There are no adequate and well controlled studies in pregnant women. Glipizide should be used during pregnancy only if the potential benefit justifies the potential risk to the fetus. Because recent information suggests that abnormal blood glucose levels during pregnancy are associated with a higher incidence of congenital abnormalities, many experts recommend that insulin be used during pregnancy to maintain blood glucose levels as close to normal as possible. Nonteratogenic Effects Prolonged severe hypoglycemia (4 to 10 days) has been reported in neonates born to mothers who were receiving a sulfonylurea drug at the time of delivery. This has been reported more frequently with the use of agents with prolonged half-lives. If glipizide is used during pregnancy, it should be discontinued at least one month before the expected delivery date.

Pharmacokinetics

Sourced from openFDA
Metabolism
Gastrointestinal absorption of glipizide in man is uniform, rapid, and essentially complete. Peak plasma concentrations occur 1 to 3 hours after a single oral dose.

Overdosage

Sourced from openFDA

There is no well documented experience with glipizide overdosage. The acute oral toxicity was extremely low in all species tested (LD 50 greater than 4 g/kg). Overdosage of sulfonylureas, including glipizide, can produce hypoglycemia. Mild hypoglycemic symptoms without loss of consciousness or neurologic findings should be treated aggressively with oral glucose and adjustments in drug dosage and/or meal patterns. Close monitoring should continue until the physician is assured that the patient is out of danger. Severe hypoglycemic reactions with coma, seizure, or other neurological impairment occur infrequently, but constitute medical emergencies requiring immediate hospitalization. If hypoglycemic coma is diagnosed or suspected, the patient should be given a rapid intravenous injection of concentrated (50%) glucose solution. This should be followed by a continuous infusion of a more dilute (10%) glucose solution at a rate that will maintain the blood glucose at a level above 100 mg/dL. Patients should be closely monitored for a minimum of 24 to 48 hours since hypoglycemia may recur after apparent clinical recovery.

Approval history

Sourced from openFDA
  • Apr 26, 1994NDANDA020329Pfizer
  • Nov 28, 1994ANDAANDA074378Oxford Pharms
  • Feb 27, 1995ANDAANDA074223Watson Labs Teva
  • Aug 31, 1995ANDAANDA074497Ani Pharms
  • Jun 13, 2001ANDAANDA075795Apotex
  • Oct 28, 2005ANDAANDA077270Teva Pharms
  • Jun 23, 2010ANDAANDA078728Heritage
  • Jan 31, 2011ANDAANDA078905Zydus Pharms Usa Inc

FDA shortages

View JSON

Reference statistics from the openFDA drug-shortage dataset. For a live view, consult the FDA database directly. Not clinical guidance.

  • Glucatrol XL, Tablet, Extended Release, 10 mg tablets; bottle of 500 (NDC 0049-0178-08)To be discontinued
    Sponsor: Pfizer Inc.
    Updated

FAERS reports

View JSON
Reference statistics only. FAERS reports are voluntarily submitted and are not incidence rates, safety signals, or causal evidence. Counts reflect reporting volume — how often a reaction was reported, not how often it occurs. For decision-grade use, consult openFDA and the FAERS Public Dashboard directly.
60,124 total reports matchedLatest report Share = reports listing the reaction ÷ total matched reports. Rows can sum to >100% because a single report often lists multiple reactions.
  1. 1Blood Glucose Increased6,69711%
  2. 2Nausea4,4987.5%
  3. 3Drug Ineffective3,5355.9%
  4. 4Diarrhoea3,3265.5%
  5. 5Fatigue3,0285.0%
  6. 6Weight Decreased2,8254.7%
  7. 7Dizziness2,4634.1%
  8. 8Dyspnoea2,4254.0%
  9. 9Blood Glucose Decreased2,2383.7%
  10. 10Vomiting2,2153.7%
  11. 11Asthenia2,1243.5%
  12. 12Pain2,0833.5%
  13. 13Headache2,0553.4%
  14. 14Death2,0473.4%
  15. 15Decreased Appetite1,9963.3%

Literature

View JSON

Recent PubMed references pinned to Glipizide as a MeSH major topic. Citations link to pubmed.ncbi.nlm.nih.gov.

Clinical trials

View JSON

The 10 most recently updated of 49 ClinicalTrials.gov registrations naming Glipizide as an intervention. Registration is not evidence of efficacy or safety — reference crosswalk only.

Pharmacogenomics

View JSON

CPIC-curated drug–gene pairs for Glipizide. Levels describe the strength of curated evidence and guideline status — never a recommendation to test or to adjust therapy.

  • G6PDCPIC CFDA label: Actionable PGx
    G6PD

Structural analogs

View JSON

Ranked by 2D fingerprint (Tanimoto) similarity over PubChem structures. Structural proximity only — not a claim of therapeutic equivalence.

Frequently asked questions

How does Glipizide work?
The primary mode of action of glipizide in experimental animals appears to be the stimulation of insulin secretion from the beta cells of pancreatic islet tissue and is thus dependent on functioning beta cells in the pancreatic islets. In humans, glipizide appears to lower the blood glucose acutely by stimulating the release of insulin from the pancreas, an effect dependent upon functioning beta cells in the pancreatic islets.
What is Glipizide used for?
According to FDA labeling, Glipizide carries indications including: Glipizide Tablets USP are indicated as an adjunct to diet and exercise to improve glycemic control in adults with type 2 diabetes mellitus.. This is a reference summary of labeled uses, not medical advice or a treatment recommendation.
What class of drug is Glipizide?
Glipizide is classified as Sulfonylureas, Sulfonylurea, Insulin Receptor Agonists, Decreased Glycolysis, Increased Glucose Transport into Cells, Increased Insulin Secretion.
What are the brand names for Glipizide?
Glipizide is marketed under brand names including Glucotrol.
What are the contraindications for Glipizide?
Glipizide labeling lists contraindications including: Glipizide is contraindicated in patients with: 1. Known hypersensitivity to the drug.. Always consult the full prescribing information and a clinician.
Note. Data for glipizide is illustrative MVP content compiled from public sources. pharmacopeia is for educational and informational use only and is not a substitute for professional medical advice.

Search pharmacopeia

Search drugs, classes, and ingredients