Peringatan Keamanan

The oral LD50 value in rats is > 10000 mg/kg.MSDS The intraperitoneal LD50 value in rats is reported to be 3950 mg/kg MSDS. Although glimepiride is reported to have fewer risks of hypoglycemia compared to other sulfonylureas such as glyburide, overdosage of glimepiride may result in severe hypoglycemia with coma, seizure, or other neurological impairment may occur. This can be treated with glucagon or intravenous glucose. Continued observation and additional carbohydrate intake may be necessary since hypoglycemia may recur after apparent clinical recovery.L10319

In a study of rats given doses of up to 5000 parts per million (ppm) in complete feed for 30 months, there were no signs of carcinogenesis. Meanwhile, the administration of glimepiride at a dose much higher than the maximum human recommended dose for 24 months in mice resulted in an increase in benign pancreatic adenoma formation in a dose-related manner, which was thought to be the result of chronic pancreatic stimulation.L10319 Glimepiride was non-mutagenic in in vitro and in vivo mutagenicity studies. In male and female rat studies, glimepiride was shown to have no effects on fertility.L10319

Glimepiride

DB00222

small molecule approved

Deskripsi

First introduced in 1995, glimepiride is a member of the second-generation sulfonylurea (SU) drug class used for the management of type 2 diabetes mellitus (T2DM) to improve glycemic control. Type 2 diabetes is a metabolic disorder with increasing prevalences worldwide; it is characterized by insulin resistance in accordance with progressive ? cell failure and long-term microvascular and macrovascular complications that lead to co-morbidities and mortalities. Sulfonylureas are one of the insulin secretagogues widely used for the management of type 2 diabetes to lower blood glucose levels. The main effect of SUs is thought to be effective when residual pancreatic ?-cells are present,A177715 as they work by stimulating the release of insulin from the pancreatic beta cells and they are also thought to exert extra-pancreatic effects, such as increasing the insulin-mediated peripheral glucose uptake.A177709

Glimepiride works by stimulating the secretion of insulin granules from pancreatic islet beta cells by blocking ATP-sensitive potassium channels (KATP channels) and causing depolarization of the beta cells. Compared to glipizide, another second SU drug, glimepiride has a longer duration of action. It is sometimes classified as a third-generation SU because it has larger substitutions than other second-generation SUs.A177703 Compared to other SUs, glimepiride was associated with a lower risk of developing hypoglycemia and weight gain in clinical trials A177709 as well as fewer cardiovascular effects than other SUs due to minimal effects on ischemic preconditioning of cardiac myocytes.A177703 It is effective in reducing fasting plasma glucose, postprandial glucose, and glycosylated hemoglobin levels and is considered to be a useful, cost-effective treatment option for managing type 2 diabetes mellitus.A177703 Glimepiride was approved by the Food and Drug Administration (FDA) in the United States in 1995 for the treatment of T2DM. It is commonly marketed under the brand name Amaryl as oral tablets and is typically administered once daily.

Struktur Molekul 2D

Berat 490.62
Wujud solid

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

Profil Farmakokinetik

Waktu Paruh (Half-Life) The elimination half-life of glimepiride is approximately 5 to 8 hours,[A177715] which can increase up to 9 hours following multiple doses.[A177709]
Volume Distribusi Following intravenous dosing in healthy subjects, the volume of distribution was 8.8 L (113 mL/kg).[L10319]
Klirens (Clearance) A single-dose, crossover, dose-proportionality (1, 2, 4, and 8 mg) study in normal subjects and from a single- and multiple-dose, parallel, dose proportionality (4 and 8 mg) study in patients with type 2 diabetes (T2D) were performed. In these studies, the total body clearance was 52.1 +/- 16.0 mL/min, 48.5 +/- 29.3 mL/min in patients with T2D given a single oral dose, and 52.7 +/- 40.3 mL/min in patients with T2D given multiple oral doses.[L10322] Following intravenous dosing in healthy subjects, the total body clearance was 47.8 mL/min.[L10319]

Absorpsi

Glimepiride is completely absorbed after oral administration within 1 hour of administration with a linear pharmacokinetics profile.A177703 Following administration of a single oral dose of glimepiride in healthy subjects and with multiple oral doses with type 2 diabetes, the peak plasma concentrations (Cmax) were reached after 2 to 3 hours post-dose.L10319 Accumulation does not occur after multiple doses.A177703 When glimepiride was given with meals, the time to reach Cmax was increased by 12% while the mean and AUC (area under the curve) were decreased by 8 to 9%, respectively.L10322 In a pharmacokinetic study of Japanese patients with T2DM, Cmax value in once-daily dose was higher than those in twice-daily doses.A177724 The absolute bioavailability of glimepiride is reported to be complete following oral administration.A177721

Metabolisme

Glimepiride is reported to undergo hepatic metabolism. Following either an intravenous or oral dose, glimepiride undergoes oxidative biotransformation mediated by CYP2C9 enzyme to form a major metabolite, cyclohexyl hydroxymethyl derivative (M1), that is pharmacologically active. M1 can be further metabolized to the inactive metabolite carboxyl derivative (M2) by one or several cytosolic enzymes. M1 retained approximately one third of the pharmacologic activity of its parent in an animal model, with a half-life of 3-6 hours.A177715 However, whether the glucose-lowering effect of M1 is clinically significant is not clear.

Rute Eliminasi

Following oral administration of glimepiride in healthy male subjects, approximately 60% of the total radioactivity was recovered in the urine in 7 days, with M1 and M2 accounting for 80-90% of the total radioactivity recovered in the urine. The ratio of M1 to M2 was approximately 3:2 in two subjects and 4:1 in one subject.L10319 Approximately 40% of the total radioactivity was recovered in feces where M1 and M2 accounted for about 70% of the radioactivity and a ratio of M1 to M2 being 1:3. No parent drug was recovered from urine or feces.L10319

Interaksi Makanan

2 Data
  • 1. Avoid alcohol. Acute and chronic alcohol intake may unpredictably affect the glucose-lowering action of glimepiride.
  • 2. Take with food. The manufacturer recommends administration with the first meal of the day.

Interaksi Obat

1073 Data
Pegvisomant The risk or severity of hypoglycemia can be increased when Pegvisomant is combined with Glimepiride.
Cyclosporine Cyclosporine may decrease the excretion rate of Glimepiride which could result in a higher serum level.
Erythromycin Erythromycin may decrease the excretion rate of Glimepiride which could result in a higher serum level.
Reserpine Reserpine may decrease the excretion rate of Glimepiride which could result in a higher serum level.
Bosentan Bosentan may decrease the excretion rate of Glimepiride which could result in a higher serum level.
Tipranavir Tipranavir may decrease the excretion rate of Glimepiride which could result in a higher serum level.
Glyburide Glyburide may decrease the excretion rate of Glimepiride which could result in a higher serum level.
Ketoconazole Ketoconazole may decrease the excretion rate of Glimepiride which could result in a higher serum level.
Ursodeoxycholic acid Ursodeoxycholic acid may decrease the excretion rate of Glimepiride which could result in a higher serum level.
Cholic Acid Cholic Acid may decrease the excretion rate of Glimepiride which could result in a higher serum level.
Fusidic acid Fusidic acid may decrease the excretion rate of Glimepiride which could result in a higher serum level.
Simeprevir Simeprevir may decrease the excretion rate of Glimepiride which could result in a higher serum level.
Lenvatinib Lenvatinib may decrease the excretion rate of Glimepiride which could result in a higher serum level.
Valinomycin Valinomycin may decrease the excretion rate of Glimepiride which could result in a higher serum level.
Olmesartan Olmesartan may decrease the excretion rate of Glimepiride which could result in a higher serum level.
Pralsetinib Pralsetinib may decrease the excretion rate of Glimepiride which could result in a higher serum level.
Carbocisteine The risk or severity of adverse effects can be increased when Glimepiride is combined with Carbocisteine.
Chloramphenicol The metabolism of Glimepiride can be decreased when combined with Chloramphenicol.
Cimetidine The serum concentration of Glimepiride can be increased when it is combined with Cimetidine.
Colesevelam Colesevelam can cause a decrease in the absorption of Glimepiride resulting in a reduced serum concentration and potentially a decrease in efficacy.
Fluconazole The serum concentration of Glimepiride can be increased when it is combined with Fluconazole.
Metreleptin Metreleptin may increase the hypoglycemic activities of Glimepiride.
Probenecid The protein binding of Glimepiride can be decreased when combined with Probenecid.
Ranitidine The serum concentration of Glimepiride can be increased when it is combined with Ranitidine.
Voriconazole The serum concentration of Glimepiride can be increased when it is combined with Voriconazole.
Clarithromycin The serum concentration of Glimepiride 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 Glimepiride.
Rifampin The serum concentration of Glimepiride can be decreased when it is combined with Rifampicin.
Moxifloxacin The therapeutic efficacy of Glimepiride can be increased when used in combination with Moxifloxacin.
Grepafloxacin The therapeutic efficacy of Glimepiride can be increased when used in combination with Grepafloxacin.
Enoxacin The therapeutic efficacy of Glimepiride can be increased when used in combination with Enoxacin.
Pefloxacin The therapeutic efficacy of Glimepiride can be increased when used in combination with Pefloxacin.
Ciprofloxacin The therapeutic efficacy of Glimepiride can be increased when used in combination with Ciprofloxacin.
Trovafloxacin The therapeutic efficacy of Glimepiride can be increased when used in combination with Trovafloxacin.
Nalidixic acid The therapeutic efficacy of Glimepiride can be increased when used in combination with Nalidixic acid.
Rosoxacin The therapeutic efficacy of Glimepiride can be increased when used in combination with Rosoxacin.
Cinoxacin The therapeutic efficacy of Glimepiride can be increased when used in combination with Cinoxacin.
Lomefloxacin The therapeutic efficacy of Glimepiride can be increased when used in combination with Lomefloxacin.
Gatifloxacin The therapeutic efficacy of Glimepiride can be increased when used in combination with Gatifloxacin.
Norfloxacin The therapeutic efficacy of Glimepiride can be increased when used in combination with Norfloxacin.
Levofloxacin The therapeutic efficacy of Glimepiride can be increased when used in combination with Levofloxacin.
Gemifloxacin The therapeutic efficacy of Glimepiride can be increased when used in combination with Gemifloxacin.
Ofloxacin The therapeutic efficacy of Glimepiride can be increased when used in combination with Ofloxacin.
Sparfloxacin The therapeutic efficacy of Glimepiride can be increased when used in combination with Sparfloxacin.
Temafloxacin The therapeutic efficacy of Glimepiride can be increased when used in combination with Temafloxacin.
Fleroxacin The therapeutic efficacy of Glimepiride can be increased when used in combination with Fleroxacin.
Technetium Tc-99m ciprofloxacin The therapeutic efficacy of Glimepiride can be increased when used in combination with Technetium Tc-99m ciprofloxacin.
Garenoxacin The therapeutic efficacy of Glimepiride can be increased when used in combination with Garenoxacin.
Nemonoxacin The therapeutic efficacy of Glimepiride can be increased when used in combination with Nemonoxacin.
Flumequine The therapeutic efficacy of Glimepiride can be increased when used in combination with Flumequine.
Enrofloxacin The therapeutic efficacy of Glimepiride can be increased when used in combination with Enrofloxacin.
Orbifloxacin The therapeutic efficacy of Glimepiride can be increased when used in combination with Orbifloxacin.
Sarafloxacin The therapeutic efficacy of Glimepiride can be increased when used in combination with Sarafloxacin.
Difloxacin The therapeutic efficacy of Glimepiride can be increased when used in combination with Difloxacin.
Pazufloxacin The therapeutic efficacy of Glimepiride can be increased when used in combination with Pazufloxacin.
Prulifloxacin The therapeutic efficacy of Glimepiride can be increased when used in combination with Prulifloxacin.
Delafloxacin The therapeutic efficacy of Glimepiride can be increased when used in combination with Delafloxacin.
Sitafloxacin The therapeutic efficacy of Glimepiride can be increased when used in combination with Sitafloxacin.
Oxolinic acid The therapeutic efficacy of Glimepiride can be increased when used in combination with Oxolinic acid.
Rufloxacin The therapeutic efficacy of Glimepiride can be increased when used in combination with Rufloxacin.
Pipemidic acid The therapeutic efficacy of Glimepiride can be increased when used in combination with Pipemidic acid.
Methyclothiazide The therapeutic efficacy of Glimepiride can be decreased when used in combination with Methyclothiazide.
Chlorthalidone The therapeutic efficacy of Glimepiride can be decreased when used in combination with Chlorthalidone.
Bendroflumethiazide The therapeutic efficacy of Glimepiride can be decreased when used in combination with Bendroflumethiazide.
Metolazone The therapeutic efficacy of Glimepiride can be decreased when used in combination with Metolazone.
Benzthiazide The therapeutic efficacy of Glimepiride can be decreased when used in combination with Benzthiazide.
Hydroflumethiazide The therapeutic efficacy of Glimepiride can be decreased when used in combination with Hydroflumethiazide.
Indapamide The therapeutic efficacy of Glimepiride can be decreased when used in combination with Indapamide.
Chlorothiazide The therapeutic efficacy of Glimepiride can be decreased when used in combination with Chlorothiazide.
Hydrochlorothiazide The therapeutic efficacy of Glimepiride can be decreased when used in combination with Hydrochlorothiazide.
Trichlormethiazide The therapeutic efficacy of Glimepiride can be decreased when used in combination with Trichlormethiazide.
Polythiazide The therapeutic efficacy of Glimepiride can be decreased when used in combination with Polythiazide.
Quinethazone The therapeutic efficacy of Glimepiride can be decreased when used in combination with Quinethazone.
Cyclopenthiazide The therapeutic efficacy of Glimepiride can be decreased when used in combination with Cyclopenthiazide.
Epitizide The therapeutic efficacy of Glimepiride can be decreased when used in combination with Epitizide.
Esmolol Esmolol may increase the hypoglycemic activities of Glimepiride.
Landiolol Landiolol may increase the hypoglycemic activities of Glimepiride.
Ethanol The risk or severity of adverse effects can be increased when Glimepiride is combined with Ethanol.
Amitriptyline Amitriptyline may decrease the hypoglycemic activities of Glimepiride.
Protriptyline Protriptyline may decrease the hypoglycemic activities of Glimepiride.
Imipramine Imipramine may decrease the hypoglycemic activities of Glimepiride.
Nortriptyline Nortriptyline may decrease the hypoglycemic activities of Glimepiride.
Amoxapine Amoxapine may decrease the hypoglycemic activities of Glimepiride.
Desipramine Desipramine may decrease the hypoglycemic activities of Glimepiride.
Clomipramine Clomipramine may decrease the hypoglycemic activities of Glimepiride.
Amineptine Amineptine may decrease the hypoglycemic activities of Glimepiride.
Dimetacrine Dimetacrine may decrease the hypoglycemic activities of Glimepiride.
Butriptyline Butriptyline may decrease the hypoglycemic activities of Glimepiride.
Dosulepin Dosulepin may decrease the hypoglycemic activities of Glimepiride.
Tianeptine Tianeptine may decrease the hypoglycemic activities of Glimepiride.
Oxaprotiline Oxaprotiline may decrease the hypoglycemic activities of Glimepiride.
Opipramol Opipramol may decrease the hypoglycemic activities of Glimepiride.
Amitriptylinoxide Amitriptylinoxide may decrease the hypoglycemic activities of Glimepiride.
Dibenzepin Dibenzepin may decrease the hypoglycemic activities of Glimepiride.
Quinupramine Quinupramine may decrease the hypoglycemic activities of Glimepiride.
Melitracen Melitracen may decrease the hypoglycemic activities of Glimepiride.
Lofepramine Lofepramine may decrease the hypoglycemic activities of Glimepiride.
Iprindole Iprindole may decrease the hypoglycemic activities of Glimepiride.
Imipramine oxide Imipramine oxide may decrease the hypoglycemic activities of Glimepiride.
Doxepin Doxepin may decrease the hypoglycemic activities of Glimepiride.

Target Protein

ATP-binding cassette sub-family C member 9 ABCC9
ATP-sensitive inward rectifier potassium channel 11 KCNJ11
ATP-sensitive inward rectifier potassium channel 1 KCNJ1
ATP-binding cassette sub-family C member 8 ABCC8

Referensi & Sumber

Synthesis reference: Suresh Kadam, Venkatasubramanian Tarur, Sanjay Naik, Sachin Gavhane, "Process for preparation of substantially pure glimepiride." U.S. Patent US20070082943, issued April 12, 2007.
Artikel (PubMed)
  • PMID: 23028231
    Basit A, Riaz M, Fawwad A: Glimepiride: evidence-based facts, trends, and observations (GIFTS). corrected. Vasc Health Risk Manag. 2012;8:463-72. doi: 10.2147/HIV.S33194. Epub 2012 Aug 15.
  • PMID: 12852703
    Massi-Benedetti M: Glimepiride in type 2 diabetes mellitus: a review of the worldwide therapeutic experience. Clin Ther. 2003 Mar;25(3):799-816.
  • 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: 12369756
    Badian M, Korn A, Lehr KH, Malerczyk V, Waldhausl W: Absolute bioavailability of glimepiride (Amaryl) after oral administration. Drug Metabol Drug Interact. 1994;11(4):331-9.
  • PMID: 17603225
    Matsuki M, Matsuda M, Kohara K, Shimoda M, Kanda Y, Tawaramoto K, Shigetoh M, Kawasaki F, Kotani K, Kaku K: Pharmacokinetics and pharmacodynamics of glimepiride in type 2 diabetic patients: compared effects of once- versus twice-daily dosing. Endocr J. 2007 Aug;54(4):571-6. Epub 2007 Jul 2.
  • PMID: 16249427
    Koster JC, Permutt MA, Nichols CG: Diabetes and insulin secretion: the ATP-sensitive K+ channel (K ATP) connection. Diabetes. 2005 Nov;54(11):3065-72.
  • PMID: 15978902
    Shi NQ, Ye B, Makielski JC: Function and distribution of the SUR isoforms and splice variants. J Mol Cell Cardiol. 2005 Jul;39(1):51-60. doi: 10.1016/j.yjmcc.2004.11.024. Epub 2005 Feb 5.

Contoh Produk & Brand

Produk: 358 • International brands: 2
Produk
  • Amaryl
    Tablet • 1 mg/1 • Oral • US • Approved
  • Amaryl
    Tablet • 2 mg/1 • Oral • US • Approved
  • Amaryl
    Tablet • 4 mg/1 • Oral • US • Approved
  • Amaryl
    Tablet • 1 mg/1 • Oral • US • Approved
  • Amaryl
    Tablet • 2 mg/1 • Oral • US • Approved
  • Amaryl
    Tablet • 4 mg/1 • Oral • US • Approved
  • Amaryl
    Tablet • 1 mg • Oral • Canada • Approved
  • Amaryl
    Tablet • 2 mg • Oral • Canada • Approved
Menampilkan 8 dari 358 produk.
International Brands
  • GLIMPID — Ranbaxy Laboratories
  • GLIMY — Dr.Reddy's Labs

Sekuens Gen/Protein (FASTA)

Sekuens dimuat saat dibutuhkan agar halaman tetap ringan.
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