Peringatan Keamanan

The oral LD50 in rats is >3200mg/kg, in mice is >1500mg/kg, in rabbits is >10,000mg/kg, and in guinea pigs is >1500mg/kg.L8135

Patients experiencing an overdose may present with hypoglycemia.L8123 Mild hypoglycemia should be treated with oral glucose and adjustments to drug doses or meal schedules.L8123 Severe hypoglycemia may present with coma, seizure, and neurological impairment.L8123 This should be treated immediately in hospital with intravenous glucose and monitoring for 24-48 hours.L8123

Glyburide

DB01016

small molecule approved

Deskripsi

Glyburide is a second generation sulfonylurea used to treat patients with diabetes mellitus type II.L8123 It is typically given to patients who cannot be managed with the standard first line therapy, metformin.L8123 Glyburide stimulates insulin secretion through the closure of ATP-sensitive potassium channels on beta cells, raising intracellular potassium and calcium ion concentrations.A183617

Glyburide was granted FDA approval on 1 May 1984.L8117 A formulation with metformin was granted FDA approval on on 31 July 2000.L8120

Struktur Molekul 2D

Berat 494.004
Wujud solid

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

Profil Farmakokinetik

Waktu Paruh (Half-Life) Elderly patients have a terminal elimination half life of 4.0-13.4h, while younger patients have a terminal elimination half life of 4.0-13.9h.[A183554]
Volume Distribusi Elderly patients have a volume of distribution of 19.3-52.6L, while younger patients have a volume of distribution of 21.5-49.3L.[A183554]
Klirens (Clearance) Elderly patients have a clearance of 2.70-3.55L/h, while younger patients have a clearance of 2.47-4.11L/h.[A183554]

Absorpsi

Elderly patients taking glyburide reached a Cmax of 211-315ng/mL with a Tmax of 0.9-1.0h, while younger patients reached a Cmax of 144-302ng/mL with a Tmax of 1.3-3.0h.A183554 Patients taking glyburide have and AUC of 348ng*h/mL.A183593

Metabolisme

Glyburide is metabolized mainly by CYP3A4, followed by CYP2C9, CYP2C19, CYP3A7, and CYP3A5.A183560,A183569 These enzymes metabolize glyburide to 4-trans-hydroxycyclohexyl glyburide (M1), 4-cis-hydroxycyclohexyl glyburide (M2a), 3-cis-hydroxycyclohexyl glyburide (M2b), 3-trans-hydroxycyclohexyl glyburide (M3), 2-trans-hydroxycyclohexyl glyburide (M4), and ethylhydroxycyclohexyl glyburide (M5).A183569 The M1 and M2b metabolites are considered active, along with the parent molecule.A183569

Rute Eliminasi

Unlike other sulfonylureas, glyburide is 50% excreted in the urine and 50% in the feces.L8123 Glyburide is mainly excreted as the metabolite 4-trans-hydroxyglyburide.L8123

Interaksi Makanan

2 Data
  • 1. Avoid alcohol. Alcohol increases the risk of hypoglycemia.
  • 2. Take before a meal. Take 30-60 minutes before breakfast.

Interaksi Obat

1412 Data
Pegvisomant The risk or severity of hypoglycemia can be increased when Pegvisomant is combined with Glyburide.
Glycochenodeoxycholic Acid Glyburide may decrease the excretion rate of Glycochenodeoxycholic Acid which could result in a higher serum level.
Pravastatin Glyburide may decrease the excretion rate of Pravastatin which could result in a higher serum level.
Glimepiride Glyburide may decrease the excretion rate of Glimepiride which could result in a higher serum level.
Isradipine Glyburide may decrease the excretion rate of Isradipine which could result in a higher serum level.
Olmesartan Olmesartan may decrease the excretion rate of Glyburide which could result in a higher serum level.
Flucloxacillin Glyburide may decrease the excretion rate of Flucloxacillin which could result in a higher serum level.
Indomethacin Glyburide may decrease the excretion rate of Indomethacin which could result in a higher serum level.
Cerivastatin Glyburide may decrease the excretion rate of Cerivastatin which could result in a higher serum level.
Loratadine Glyburide may decrease the excretion rate of Loratadine which could result in a higher serum level.
Atropine Glyburide may decrease the excretion rate of Atropine which could result in a higher serum level.
Diclofenac Glyburide may decrease the excretion rate of Diclofenac which could result in a higher serum level.
Losartan The metabolism of Losartan can be decreased when combined with Glyburide.
Fluorescein Glyburide may decrease the excretion rate of Fluorescein which could result in a higher serum level.
Nitrofurantoin Glyburide may decrease the excretion rate of Nitrofurantoin which could result in a higher serum level.
Naproxen Glyburide may decrease the excretion rate of Naproxen which could result in a higher serum level.
Disulfiram Glyburide may decrease the excretion rate of Disulfiram which could result in a higher serum level.
Cefaclor Glyburide may decrease the excretion rate of Cefaclor which could result in a higher serum level.
Tinidazole Glyburide may decrease the excretion rate of Tinidazole which could result in a higher serum level.
Repaglinide Glyburide may decrease the excretion rate of Repaglinide which could result in a higher serum level.
Telmisartan Glyburide may decrease the excretion rate of Telmisartan which could result in a higher serum level.
Ezetimibe Glyburide may decrease the excretion rate of Ezetimibe which could result in a higher serum level.
Dipyridamole Glyburide may decrease the excretion rate of Dipyridamole which could result in a higher serum level.
Sulfamethoxazole Glyburide may decrease the excretion rate of Sulfamethoxazole which could result in a higher serum level.
Fenofibrate Glyburide may decrease the excretion rate of Fenofibrate which could result in a higher serum level.
Nitrendipine Glyburide may decrease the excretion rate of Nitrendipine which could result in a higher serum level.
Glipizide Glyburide may decrease the excretion rate of Glipizide which could result in a higher serum level.
Rosuvastatin Glyburide may decrease the excretion rate of Rosuvastatin which could result in a higher serum level.
Sulfinpyrazone Glyburide may decrease the excretion rate of Sulfinpyrazone which could result in a higher serum level.
Ofloxacin Glyburide may decrease the excretion rate of Ofloxacin which could result in a higher serum level.
Taurocholic acid Glyburide may decrease the excretion rate of Taurocholic acid which could result in a higher serum level.
Prasterone sulfate Glyburide may decrease the excretion rate of Prasterone sulfate which could result in a higher serum level.
Indocyanine green acid form Glyburide may decrease the excretion rate of Indocyanine green acid form which could result in a higher serum level.
Benzbromarone Glyburide may decrease the excretion rate of Benzbromarone which could result in a higher serum level.
Pilsicainide Glyburide may decrease the excretion rate of Pilsicainide which could result in a higher serum level.
Dihydroergocristine Glyburide may decrease the excretion rate of Dihydroergocristine which could result in a higher serum level.
Glycyrrhizic acid Glyburide may decrease the excretion rate of Glycyrrhizic acid which could result in a higher serum level.
Nifedipine Glyburide may decrease the excretion rate of Nifedipine which could result in a higher serum level.
Ranolazine Glyburide may decrease the excretion rate of Ranolazine which could result in a higher serum level.
Pralsetinib Pralsetinib may decrease the excretion rate of Glyburide which could result in a higher serum level.
Belantamab mafodotin Glyburide may decrease the excretion rate of Belantamab mafodotin which could result in a higher serum level.
Cyclosporine The therapeutic efficacy of Glyburide can be decreased when used in combination with Cyclosporine.
Lomitapide The metabolism of Lomitapide can be decreased when combined with Glyburide.
Dabrafenib The serum concentration of Glyburide can be decreased when it is combined with Dabrafenib.
Eliglustat The metabolism of Eliglustat can be decreased when combined with Glyburide.
Ibrutinib The metabolism of Ibrutinib can be decreased when combined with Glyburide.
Luliconazole The serum concentration of Glyburide can be increased when it is combined with Luliconazole.
Cilostazol The metabolism of Cilostazol can be decreased when combined with Glyburide.
Colchicine The metabolism of Colchicine can be decreased when combined with Glyburide.
Fentanyl The metabolism of Glyburide can be decreased when combined with Fentanyl.
Iloperidone The metabolism of Iloperidone can be decreased when combined with Glyburide.
Retapamulin The metabolism of Retapamulin can be decreased when combined with Glyburide.
Tofacitinib The metabolism of Tofacitinib can be decreased when combined with Glyburide.
Vardenafil The metabolism of Vardenafil can be decreased when combined with Glyburide.
Eszopiclone The metabolism of Eszopiclone can be decreased when combined with Glyburide.
Zopiclone The metabolism of Zopiclone can be decreased when combined with Glyburide.
Carbocisteine The risk or severity of adverse effects can be increased when Glyburide is combined with Carbocisteine.
Chloramphenicol The metabolism of Glyburide can be decreased when combined with Chloramphenicol.
Cimetidine The serum concentration of Glyburide can be increased when it is combined with Cimetidine.
Fluconazole The serum concentration of Glyburide can be increased when it is combined with Fluconazole.
Metreleptin Metreleptin may increase the hypoglycemic activities of Glyburide.
Probenecid The protein binding of Glyburide can be decreased when combined with Probenecid.
Ranitidine The serum concentration of Glyburide can be increased when it is combined with Ranitidine.
Voriconazole The serum concentration of Glyburide can be increased when it is combined with Voriconazole.
Lovastatin The metabolism of Lovastatin can be decreased when combined with Glyburide.
Alfuzosin The metabolism of Alfuzosin can be decreased when combined with Glyburide.
Alprazolam The metabolism of Alprazolam can be decreased when combined with Glyburide.
Bosentan Glyburide may increase the hepatotoxic activities of Bosentan.
Warfarin The serum concentration of Warfarin can be increased when it is combined with Glyburide.
Acenocoumarol The serum concentration of Acenocoumarol can be increased when it is combined with Glyburide.
(R)-warfarin The serum concentration of (R)-warfarin can be increased when it is combined with Glyburide.
R,S-Warfarin alcohol The serum concentration of R,S-Warfarin alcohol can be increased when it is combined with Glyburide.
S,R-Warfarin alcohol The serum concentration of S,R-Warfarin alcohol can be increased when it is combined with Glyburide.
(S)-Warfarin The serum concentration of (S)-Warfarin can be increased when it is combined with Glyburide.
Midazolam The serum concentration of Midazolam can be increased when it is combined with Glyburide.
Tacrolimus The serum concentration of Tacrolimus can be increased when it is combined with Glyburide.
Colesevelam The serum concentration of Glyburide can be decreased when it is combined with Colesevelam.
Clarithromycin The serum concentration of Glyburide can be increased when it is combined with Clarithromycin.
Atorvastatin The metabolism of Atorvastatin can be decreased when combined with Glyburide.
Lipoic acid The risk or severity of hypoglycemia can be increased when Lipoic acid is combined with Glyburide.
Rifampin The serum concentration of Glyburide can be decreased when it is combined with Rifampicin.
Moxifloxacin The therapeutic efficacy of Glyburide can be increased when used in combination with Moxifloxacin.
Grepafloxacin The therapeutic efficacy of Glyburide can be increased when used in combination with Grepafloxacin.
Enoxacin The therapeutic efficacy of Glyburide can be increased when used in combination with Enoxacin.
Pefloxacin The therapeutic efficacy of Glyburide can be increased when used in combination with Pefloxacin.
Trovafloxacin The therapeutic efficacy of Glyburide can be increased when used in combination with Trovafloxacin.
Nalidixic acid The therapeutic efficacy of Glyburide can be increased when used in combination with Nalidixic acid.
Rosoxacin The therapeutic efficacy of Glyburide can be increased when used in combination with Rosoxacin.
Cinoxacin The therapeutic efficacy of Glyburide can be increased when used in combination with Cinoxacin.
Lomefloxacin The therapeutic efficacy of Glyburide can be increased when used in combination with Lomefloxacin.
Gatifloxacin The therapeutic efficacy of Glyburide can be increased when used in combination with Gatifloxacin.
Norfloxacin The therapeutic efficacy of Glyburide can be increased when used in combination with Norfloxacin.
Levofloxacin The therapeutic efficacy of Glyburide can be increased when used in combination with Levofloxacin.
Gemifloxacin The therapeutic efficacy of Glyburide can be increased when used in combination with Gemifloxacin.
Sparfloxacin The therapeutic efficacy of Glyburide can be increased when used in combination with Sparfloxacin.
Temafloxacin The therapeutic efficacy of Glyburide can be increased when used in combination with Temafloxacin.
Fleroxacin The therapeutic efficacy of Glyburide can be increased when used in combination with Fleroxacin.
Technetium Tc-99m ciprofloxacin The therapeutic efficacy of Glyburide can be increased when used in combination with Technetium Tc-99m ciprofloxacin.
Garenoxacin The therapeutic efficacy of Glyburide can be increased when used in combination with Garenoxacin.
Nemonoxacin The therapeutic efficacy of Glyburide can be increased when used in combination with Nemonoxacin.

Target Protein

ATP-binding cassette sub-family C member 8 ABCC8
Sulfonylurea receptor 1, Kir6.2 ABCC8
ATP-binding cassette sub-family C member 9 ABCC9
Bile salt export pump ABCB11
Phospholipid-transporting ATPase ABCA1 ABCA1
Mitochondrial ATP-sensitive potassium channel KCNJ11
Carnitine O-palmitoyltransferase 1, liver isoform CPT1A
Cystic fibrosis transmembrane conductance regulator CFTR
Transient receptor potential cation channel subfamily M member 4 TRPM4

Referensi & Sumber

Synthesis reference: Suresh Gidwani, "Solid oral dosage form of metformin and glyburide and the method of preparation thereof." U.S. Patent US20040175421, issued September 09, 2004.
Artikel (PubMed)
  • PMID: 8740326
    Jaber LA, Antal EJ, Welshman IR: Pharmacokinetics and pharmacodynamics of glyburide in young and elderly patients with non-insulin-dependent diabetes mellitus. Ann Pharmacother. 1996 May;30(5):472-5. doi: 10.1177/106002809603000507.
  • PMID: 17011523
    Ravindran S, Zharikova OL, Hill RA, Nanovskaya TN, Hankins GD, Ahmed MS: Identification of glyburide metabolites formed by hepatic and placental microsomes of humans and baboons. Biochem Pharmacol. 2006 Dec 15;72(12):1730-7. doi: 10.1016/j.bcp.2006.08.024. Epub 2006 Aug 30.
  • PMID: 25450675
    Shuster DL, Risler LJ, Prasad B, Calamia JC, Voellinger JL, Kelly EJ, Unadkat JD, Hebert MF, Shen DD, Thummel KE, Mao Q: Identification of CYP3A7 for glyburide metabolism in human fetal livers. Biochem Pharmacol. 2014 Dec 15;92(4):690-700. doi: 10.1016/j.bcp.2014.09.025. Epub 2014 Oct 22.
  • PMID: 7560255
    Olsen KM, Kearns GL, Kemp SF: Glyburide protein binding and the effect of albumin glycation in children, young adults, and older adults with diabetes. J Clin Pharmacol. 1995 Jul;35(7):739-45.
  • PMID: 29772022
    Proks P, Kramer H, Haythorne E, Ashcroft FM: Binding of sulphonylureas to plasma proteins - A KATP channel perspective. PLoS One. 2018 May 17;13(5):e0197634. doi: 10.1371/journal.pone.0197634. eCollection 2018.
  • PMID: 21084763
    Graefe-Mody U, Rose P, Ring A, Zander K, Iovino M, Woerle HJ: Assessment of the pharmacokinetic interaction between the novel DPP-4 inhibitor linagliptin and a sulfonylurea, glyburide, in healthy subjects. Drug Metab Pharmacokinet. 2011;26(2):123-9. Epub 2010 Nov 12.
  • PMID: 12819907
    Gribble FM, Reimann F: Sulphonylurea action revisited: the post-cloning era. Diabetologia. 2003 Jul;46(7):875-91. doi: 10.1007/s00125-003-1143-3. Epub 2003 Jun 18.
  • PMID: 3966729
    Kreisberg RA: The second-generation sulfonylureas: change or progress? Ann Intern Med. 1985 Jan;102(1):125-6. doi: 10.7326/0003-4819-102-1-125.
Menampilkan 8 dari 9 artikel.

Contoh Produk & Brand

Produk: 409 • International brands: 4
Produk
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  • Amglidia
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  • Apo Glyburide Tab 2.5mg
    Tablet • 2.5 mg • Oral • Canada • Generic • Approved
  • Apo Glyburide Tab 5mg
    Tablet • 5 mg • Oral • Canada • Generic • Approved
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International Brands
  • Daonil
  • Delmide
  • Novo-Glyburide — Novopharm
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