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Glucotrol (GLIPIZIDE)
Glucotrol works by binding to the sulfonylurea receptor 1, Kir6.2, to stimulate insulin release from pancreatic beta cells.
Glucotrol (Glyburide) is a sulfonylurea medication originally developed by Pfizer and currently owned by the same company. It targets the sulfonylurea receptor 1, Kir6.2, to stimulate insulin release from pancreatic beta cells. Glucotrol is used to treat type 2 diabetes mellitus and is available as a generic medication due to its off-patent status. The medication has a bioavailability of 95% and a half-life of 3.3 hours. As a result, it is widely available from multiple generic manufacturers.
At a glance
| Generic name | GLIPIZIDE |
|---|---|
| Sponsor | Pfizer |
| Drug class | Sulfonylurea [EPC] |
| Target | Sulfonylurea receptor 1, Kir6.2 |
| Modality | Small molecule |
| Therapeutic area | Metabolic |
| Phase | FDA-approved |
| First approval | 1984 |
Mechanism of action
Mechanism of Action:. 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. The mechanism by which glipizide lowers blood glucose during long-term administration has not been clearly established. In man, stimulation of insulin secretion by glipizide in response to meal is undoubtedly of major importance. Fasting insulin levels are not elevated even on long-term glipizide administration, but the postprandial insulin response continues to be enhanced after at least months of treatment. The insulinotropic response to meal occurs within 30 minutes after an oral dose of glipizide in diabetic patients, but elevated insulin
Approved indications
- Diabetes mellitus type 2
Common side effects
- Dizziness
- Diarrhea
- Nervousness
- Tremor
- Flatulence
- Hypoglycemia
- Abdominal pain
- Cholestatic and hepatocellular forms of liver injury
- Leukopenia
- Agranulocytosis
- Thrombocytopenia
- Hemolytic anemia
Drug interactions
- labetalol
- levofloxacin
- metoprolol
- nadolol
- norfloxacin
- ofloxacin
- penbutolol
- pindolol
- propranolol
- rifampicin
- sotalol
- sulfamethoxazole
Key clinical trials
- Pharmacokinetic Study of Single-Dose Modified Release Glipizide in Healthy Volunteers (PHASE1)
- A Study of Glipizide to Treat High Blood Sugar in People With Pancreatic Cancer (PHASE2)
- Comparative Effectiveness and Safety of Four Second Line Pharmacological Strategies in Type 2 Diabetes Study
- Comparison of Type 2 Diabetes Pharmacotherapy Regimens
- Role of KATP Channel Loss in Type 2 Diabetes (NA)
- A Study for Comparison of Canagliflozin Versus Alternative Antihyperglycemic Treatments on Risk of Heart Failure Hospitalization and Amputation for Participants With Type 2 Diabetes Mellitus and the Subpopulation With Established Cardiovascular Disease
- Study to Understand the Genetics of the Acute Response to Metformin and Glipizide in Humans (PHASE1)
- Comparative Analysis of Cost-effectiveness Between Sulfonylureas and DPP4 Inhibitors in Combination With Metformin in Treatment of Type 2 Diabetic Patients : A Retrospective, Observational Study.
Primary sources
Every claim on this page is sourced from regulatory or scientific primary sources. See our editorial policy for full methodology.
| Source | Used for |
|---|---|
| FDA label | Mechanism, indications, dosing, boxed warnings, drug interactions |
| ClinicalTrials.gov | Trial enrolment, design, endpoints, results |
Competitive intelligence
For the full competitive landscape — auto-detected comparators, recent regulatory actions across the set, upcoming PDUFA, patent timeline, sponsor landscape:
- Glucotrol CI brief — competitive landscape report
- Glucotrol updates RSS · CI watch RSS
- Pfizer portfolio CI