Peringatan Keamanan

In rats, the oral LD50 is reported to be greater than 4000 mg/kg and the intraperitoneal LD50 is 1200 mg/kg. The lowest published toxic dose (TDLo) via oral route in child was 379 ?g/kg.MSDS

Symptoms of overdose in sulfonylureas, including glipizide, may be related to severe hypoglycemia and may include coma, seizure, or other neurological impairment. These are symptoms of severe hypoglycemia and require immediate treatment with glucagon or intravenous glucose and close monitoring for a minimum of 24 to 48 hours since hypoglycemia may recur after apparent clinical recovery. Mild hypoglycemic symptoms without loss of consciousness or neurologic findings should be treated with oral glucose.label

Glipizide

DB01067

small molecule approved investigational

Deskripsi

Glipizide is an oral hypoglycemic agent in the second-generation sulfonylurea drug class that is used to control blood sugar levels in patients with type 2 diabetes mellitus. It was first introduced in 1984 A179491 and is available in various countries including Canada and the U.S. According to the 2018 Clinical Practice Guidelines by Diabetes Canada, sulfonylurea drugs are considered a second-line glucose-lowering therapy following metformin.L6712 Because sulfonylureas require functional pancreatic beta cells for their therapeutic effectiveness, sulfonylureas are more commonly used for early-stage type 2 diabetes when there is no progressed pancreatic failure.T28 Compared to the first-generation sulfonylureas, such as tolbutamide and chlorpropamide, second-generation sulfonylureas contain a more non-polar side chain in their chemical structure, which enhances their hypoglycemic potency.A179488 Compared to other members of the sulfonylurea drug group, glipizide displays rapid absorption and onset of action with the shortest half-life and duration of action, reducing the risk for long-lasting hypoglycemia that is often observed with blood glucose-lowering agents.A179485 Glipizide was first approved by the FDA in 1994 and is available in extended-release tablets under the brand name Glucotrol®, as well as in combination with metformin under the brand name Metaglip®.

Struktur Molekul 2D

Berat 445.535
Wujud solid

Peta Jejaring Molekuler
Legenda: Obat • Target • Gen • Enzim • (Panah → menunjukkan arah efek / relasi) • Transporter • Carrier

Profil Farmakokinetik

Waktu Paruh (Half-Life) The mean terminal elimination half-life of glipizide ranged from 2 to 5 hours after single or multiple doses in patients with type 2 diabetes mellitus.[label]
Volume Distribusi The mean volume of distribution was approximately 10 L following administration of single intravenous doses in patients with type 2 diabetes mellitus.[label] In mice and rat studies, the presence of the drug and its metabolites was none to minimal in the fetus of pregnant female animals.[L6745] Other sulfonylurea drugs were shown to cross the placenta and enter breast milk [T28] thus the potential risk of glipizide in fetus or infants cannot be excluded.
Klirens (Clearance) The mean total body clearance of glipizide was approximately 3 L/hr following administration of single intravenous doses in patients with type 2 diabetes mellitus.[label]

Absorpsi

Gastrointestinal absorption of glipizide is uniform, rapid, and essentially complete.A179485 The absolute bioavailability of glipizide in patients with type 2 diabetes receiving a single oral dose was 100%. The maximum plasma concentrations are expected to be reached within 6 to 12 hours following initial dosing. The steady-state plasma concentrations of glipizide from extended-release oral formulations are maintained over the 24-hour dosing interval.label In healthy volunteers, the absorption of glipizide was delayed by the presence of food but the total absorption was unaffected.L6745

Metabolisme

Glipizide is subject to hepatic metabolism, in which its major metabolites are formed from aromatic hydroxylation. These major metabolites are glipizide are reported to be pharmacologically inactive. In contrast, an acetylaminoethyl benzine derivative is formed as a minor metabolite which accounts for less than 2% of the initial dose and is reported to have one-tenth to one-third as much hypoglycemic activity as the parent compound.label

Rute Eliminasi

Glipizide is mainly eliminated by hepatic biotransformation, where less than 10% of the initial dose of the drug can be detected in the urine and feces as unchanged glipizide. About 80% of the metabolites of glipizide is excreted in the urine while 10% is excreted in the feces.label

Farmakogenomik

1 Varian
CYP2C9 (rs1057910)

Patients with this genotype have reduced metabolism of glipizide.

Interaksi Makanan

2 Data
  • 1. Avoid excessive or chronic alcohol consumption. The risk of hypoglycemia is increased when alcohol is ingested.
  • 2. Take before a meal. Take 30-60 minutes before breakfast.

Interaksi Obat

1537 Data
Pegvisomant The risk or severity of hypoglycemia can be increased when Pegvisomant is combined with Glipizide.
Erythromycin Erythromycin may decrease the excretion rate of Glipizide which could result in a higher serum level.
Reserpine Reserpine may decrease the excretion rate of Glipizide which could result in a higher serum level.
Bosentan Bosentan may decrease the excretion rate of Glipizide which could result in a higher serum level.
Glyburide Glyburide may decrease the excretion rate of Glipizide which could result in a higher serum level.
Ursodeoxycholic acid Ursodeoxycholic acid may decrease the excretion rate of Glipizide which could result in a higher serum level.
Cholic Acid Cholic Acid may decrease the excretion rate of Glipizide which could result in a higher serum level.
Fusidic acid Fusidic acid may decrease the excretion rate of Glipizide which could result in a higher serum level.
Simeprevir Simeprevir may decrease the excretion rate of Glipizide which could result in a higher serum level.
Lenvatinib Lenvatinib may decrease the excretion rate of Glipizide which could result in a higher serum level.
Valinomycin Valinomycin may decrease the excretion rate of Glipizide which could result in a higher serum level.
Cyclosporine Cyclosporine may decrease the excretion rate of Glipizide which could result in a higher serum level.
Ketoconazole Ketoconazole may decrease the excretion rate of Glipizide which could result in a higher serum level.
Nifedipine Glipizide may decrease the excretion rate of Nifedipine which could result in a higher serum level.
Olmesartan Olmesartan may decrease the excretion rate of Glipizide which could result in a higher serum level.
Pralsetinib Pralsetinib may decrease the excretion rate of Glipizide which could result in a higher serum level.
Carbocisteine The risk or severity of adverse effects can be increased when Glipizide is combined with Carbocisteine.
Chloramphenicol The metabolism of Glipizide can be decreased when combined with Chloramphenicol.
Cimetidine The serum concentration of Glipizide can be increased when it is combined with Cimetidine.
Fluconazole The serum concentration of Glipizide can be increased when it is combined with Fluconazole.
Metreleptin Metreleptin may increase the hypoglycemic activities of Glipizide.
Probenecid The protein binding of Glipizide can be decreased when combined with Probenecid.
Ranitidine The serum concentration of Glipizide can be increased when it is combined with Ranitidine.
Voriconazole The serum concentration of Glipizide can be increased when it is combined with Voriconazole.
Zidovudine The metabolism of Glipizide can be increased when combined with Zidovudine.
Lamotrigine The metabolism of Glipizide can be increased when combined with Lamotrigine.
Testosterone propionate The metabolism of Glipizide can be increased when combined with Testosterone propionate.
Ritonavir The metabolism of Glipizide can be increased when combined with Ritonavir.
Efavirenz The metabolism of Glipizide can be increased when combined with Efavirenz.
Primidone The metabolism of Glipizide can be increased when combined with Primidone.
Tipranavir Tipranavir may decrease the excretion rate of Glipizide which could result in a higher serum level.
Nelfinavir The metabolism of Glipizide can be increased when combined with Nelfinavir.
Colesevelam The serum concentration of Glipizide can be decreased when it is combined with Colesevelam.
Clarithromycin The serum concentration of Glipizide can be increased when it is combined with Clarithromycin.
Lipoic acid The risk or severity of hypoglycemia can be increased when Lipoic acid is combined with Glipizide.
Rifampin The serum concentration of Glipizide can be decreased when it is combined with Rifampicin.
Moxifloxacin The therapeutic efficacy of Glipizide can be increased when used in combination with Moxifloxacin.
Grepafloxacin The therapeutic efficacy of Glipizide can be increased when used in combination with Grepafloxacin.
Enoxacin The therapeutic efficacy of Glipizide can be increased when used in combination with Enoxacin.
Pefloxacin The therapeutic efficacy of Glipizide can be increased when used in combination with Pefloxacin.
Ciprofloxacin The therapeutic efficacy of Glipizide can be increased when used in combination with Ciprofloxacin.
Trovafloxacin The therapeutic efficacy of Glipizide can be increased when used in combination with Trovafloxacin.
Nalidixic acid The therapeutic efficacy of Glipizide can be increased when used in combination with Nalidixic acid.
Rosoxacin The therapeutic efficacy of Glipizide can be increased when used in combination with Rosoxacin.
Cinoxacin The therapeutic efficacy of Glipizide can be increased when used in combination with Cinoxacin.
Lomefloxacin The therapeutic efficacy of Glipizide can be increased when used in combination with Lomefloxacin.
Gatifloxacin The therapeutic efficacy of Glipizide can be increased when used in combination with Gatifloxacin.
Norfloxacin The therapeutic efficacy of Glipizide can be increased when used in combination with Norfloxacin.
Levofloxacin The therapeutic efficacy of Glipizide can be increased when used in combination with Levofloxacin.
Gemifloxacin The therapeutic efficacy of Glipizide can be increased when used in combination with Gemifloxacin.
Ofloxacin The therapeutic efficacy of Glipizide can be increased when used in combination with Ofloxacin.
Sparfloxacin The therapeutic efficacy of Glipizide can be increased when used in combination with Sparfloxacin.
Temafloxacin The therapeutic efficacy of Glipizide can be increased when used in combination with Temafloxacin.
Fleroxacin The therapeutic efficacy of Glipizide can be increased when used in combination with Fleroxacin.
Technetium Tc-99m ciprofloxacin The therapeutic efficacy of Glipizide can be increased when used in combination with Technetium Tc-99m ciprofloxacin.
Garenoxacin The therapeutic efficacy of Glipizide can be increased when used in combination with Garenoxacin.
Nemonoxacin The therapeutic efficacy of Glipizide can be increased when used in combination with Nemonoxacin.
Flumequine The therapeutic efficacy of Glipizide can be increased when used in combination with Flumequine.
Enrofloxacin The therapeutic efficacy of Glipizide can be increased when used in combination with Enrofloxacin.
Orbifloxacin The therapeutic efficacy of Glipizide can be increased when used in combination with Orbifloxacin.
Sarafloxacin The therapeutic efficacy of Glipizide can be increased when used in combination with Sarafloxacin.
Difloxacin The therapeutic efficacy of Glipizide can be increased when used in combination with Difloxacin.
Pazufloxacin The therapeutic efficacy of Glipizide can be increased when used in combination with Pazufloxacin.
Prulifloxacin The therapeutic efficacy of Glipizide can be increased when used in combination with Prulifloxacin.
Delafloxacin The therapeutic efficacy of Glipizide can be increased when used in combination with Delafloxacin.
Sitafloxacin The therapeutic efficacy of Glipizide can be increased when used in combination with Sitafloxacin.
Oxolinic acid The therapeutic efficacy of Glipizide can be increased when used in combination with Oxolinic acid.
Rufloxacin The therapeutic efficacy of Glipizide can be increased when used in combination with Rufloxacin.
Pipemidic acid The therapeutic efficacy of Glipizide can be increased when used in combination with Pipemidic acid.
Methyclothiazide The therapeutic efficacy of Glipizide can be decreased when used in combination with Methyclothiazide.
Chlorthalidone The therapeutic efficacy of Glipizide can be decreased when used in combination with Chlorthalidone.
Bendroflumethiazide The therapeutic efficacy of Glipizide can be decreased when used in combination with Bendroflumethiazide.
Metolazone The therapeutic efficacy of Glipizide can be decreased when used in combination with Metolazone.
Benzthiazide The therapeutic efficacy of Glipizide can be decreased when used in combination with Benzthiazide.
Hydroflumethiazide The therapeutic efficacy of Glipizide can be decreased when used in combination with Hydroflumethiazide.
Indapamide The therapeutic efficacy of Glipizide can be decreased when used in combination with Indapamide.
Chlorothiazide The therapeutic efficacy of Glipizide can be decreased when used in combination with Chlorothiazide.
Hydrochlorothiazide The therapeutic efficacy of Glipizide can be decreased when used in combination with Hydrochlorothiazide.
Trichlormethiazide The therapeutic efficacy of Glipizide can be decreased when used in combination with Trichlormethiazide.
Polythiazide The therapeutic efficacy of Glipizide can be decreased when used in combination with Polythiazide.
Quinethazone The therapeutic efficacy of Glipizide can be decreased when used in combination with Quinethazone.
Cyclopenthiazide The therapeutic efficacy of Glipizide can be decreased when used in combination with Cyclopenthiazide.
Epitizide The therapeutic efficacy of Glipizide can be decreased when used in combination with Epitizide.
Esmolol Esmolol may increase the hypoglycemic activities of Glipizide.
Landiolol Landiolol may increase the hypoglycemic activities of Glipizide.
Ethanol The risk or severity of adverse effects can be increased when Glipizide is combined with Ethanol.
Protriptyline Protriptyline may decrease the hypoglycemic activities of Glipizide.
Amoxapine Amoxapine may decrease the hypoglycemic activities of Glipizide.
Amineptine Amineptine may decrease the hypoglycemic activities of Glipizide.
Butriptyline Butriptyline may decrease the hypoglycemic activities of Glipizide.
Dosulepin Dosulepin may decrease the hypoglycemic activities of Glipizide.
Oxaprotiline Oxaprotiline may decrease the hypoglycemic activities of Glipizide.
Opipramol Opipramol may decrease the hypoglycemic activities of Glipizide.
Amitriptylinoxide Amitriptylinoxide may decrease the hypoglycemic activities of Glipizide.
Dibenzepin Dibenzepin may decrease the hypoglycemic activities of Glipizide.
Quinupramine Quinupramine may decrease the hypoglycemic activities of Glipizide.
Melitracen Melitracen may decrease the hypoglycemic activities of Glipizide.
Lofepramine Lofepramine may decrease the hypoglycemic activities of Glipizide.
Iprindole Iprindole may decrease the hypoglycemic activities of Glipizide.
Imipramine oxide Imipramine oxide may decrease the hypoglycemic activities of Glipizide.

Target Protein

ATP-binding cassette sub-family C member 8 ABCC8
ATP-sensitive inward rectifier potassium channel 10 KCNJ10
Peroxisome proliferator-activated receptor gamma PPARG

Referensi & Sumber

Synthesis reference: Suresh Kumar Gidwani, Purushottam Singnurkar, Prashant Kumar Tewari, "Sustained release pharmaceutical composition containing glipizide and method for producing same." U.S. Patent US6270797, issued February, 2000.
Artikel (PubMed)
  • PMID: 6424440
    Melander A, Wahlin-Boll E: Clinical pharmacology of glipizide. Am J Med. 1983 Nov 30;75(5B):41-5.
  • PMID: 6781341
    Skillman TG, Feldman JM: The pharmacology of sulfonylureas. Am J Med. 1981 Feb;70(2):361-72.
  • PMID: 23882374
    Quianzon CC, Cheikh IE: History of current non-insulin medications for diabetes mellitus. J Community Hosp Intern Med Perspect. 2012 Oct 15;2(3). pii: 19081. doi: 10.3402/jchimp.v2i3.19081. Print 2012.
  • PMID: 26322096
    Sola D, Rossi L, Schianca GP, Maffioli P, Bigliocca M, Mella R, Corliano F, Fra GP, Bartoli E, Derosa G: Sulfonylureas and their use in clinical practice. Arch Med Sci. 2015 Aug 12;11(4):840-8. doi: 10.5114/aoms.2015.53304. Epub 2015 Aug 11.
  • PMID: 23071876
    Olokoba AB, Obateru OA, Olokoba LB: Type 2 diabetes mellitus: a review of current trends. Oman Med J. 2012 Jul;27(4):269-73. doi: 10.5001/omj.2012.68.
Textbook
  • ISBN: 978-0-7020-3471-8
    30. (2012). In Rang and Dale's Pharmacology (7th ed., pp. 380-381, 383). Edinburgh: Elsevier/Churchill Livingstone.

Contoh Produk & Brand

Produk: 521 • International brands: 27
Produk
  • Glipizide
    Tablet • 5 mg/1 • Oral • US • Generic • Approved
  • Glipizide
    Tablet • 5 mg/1 • Oral • US • Generic • Approved
  • Glipizide
    Tablet • 5 mg/1 • Oral • US • Generic • Approved
  • Glipizide
    Tablet • 10 mg/1 • Oral • US • Generic • Approved
  • Glipizide
    Tablet • 5 mg/1 • Oral • US • Generic • Approved
  • Glipizide
    Tablet • 5 mg/1 • Oral • US • Generic • Approved
  • Glipizide
    Tablet • 10 mg/1 • Oral • US • Generic • Approved
  • Glipizide
    Tablet, film coated, extended release • 2.5 mg/1 • Oral • US • Generic • Approved
Menampilkan 8 dari 521 produk.
International Brands
  • Aldiab
  • Digrin
  • Dipazide
  • Glibenese — Pfizer
  • Glibénèse — Dexo
  • Glibetin — Johnson
  • Glican
  • Glidiab
  • Glipid
  • Glipin — Swiss Pharm

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