Peringatan Keamanan

The oral Lowest published toxic dose (TDLO) is 0.3 mg/kg in rats and 1 mg/kg in mice.L32808

There is limited information regarding overdose with vildagliptin. In one study, patients experienced muscle pain, mild and transient paresthesia, fever, edema, and a transient increase in lipase levels at a dose of 400 mg. At 600 mg, one subject experienced edema of the feet and hands and increases in creatine phosphokinase (CPK), aspartate aminotransferase (AST), C-reactive protein (CRP) and myoglobin levels. Supportive management is recommended in case of an overdose. There is no known antidote, and vildagliptin and its major metabolite cannot be removed via hemodialysis.L32803

Vildagliptin

DB04876

small molecule approved investigational

Deskripsi

Vildagliptin (LAF237) is an orally active antihyperglycemic agent that selectively inhibits the dipeptidyl peptidase-4 (DPP-4) enzyme. It is used to manage type II diabetes mellitus, where GLP-1 secretion and insulinotropic effects are impaired.A232488 By inhibiting DPP-4, vildagliptin prevents the degradation of glucagon-like peptide 1 (GLP-1) and glucose-dependent insulinotropic polypeptide (GIP), which are incretin hormones that promote insulin secretion and regulate blood glucose levels. Elevated levels of GLP-1 and GIP consequently results in improved glycemic control.L32803 In clinical trials, vildagliptin has a relatively low risk of hypoglycemia.A232488

Oral vildagliptin was approved by the European Medicines Agency in 2008 for the treatment of type II diabetes mellitus in adults as monotherapy or in combination with metformin, a sulfonylurea, or a thiazolidinedione in patients with inadequate glycemic control following monotherapy. It is marketed as Galvus.L32803 Vildagliptin is also available as Eucreas, a fixed-dose formulation with metformin for adults in who do not adequately glycemic control from monotherapy.L32813 Vildagliptin is currently under investigation in the US.

Struktur Molekul 2D

Berat 303.3993
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 elimination half-life following intravenous administration is approximately two hours. The elimination half-life after oral administration is approximately three hours.[L32803]
Volume Distribusi The mean volume of distribution of vildagliptin at steady-state after intravenous administration is 71 L, suggesting extravascular distribution.[L32803]
Klirens (Clearance) After intravenous administration to healthy subjects, the total plasma and renal clearance of vildagliptin were 41 and 13 L/h, respectively.[L32803]

Absorpsi

In a fasting state, vildagliptin is rapidly absorbed following oral administration. Peak plasma concentrations are observed at 1.7 hours following administration.L32803 Plasma concentrations of vildagliptin increase in an approximately dose-proportional manner.A232488 Food delays Tmax to 2.5 hours and decreases Cmax by 19%, but has no effects on the overall exposure to the drug (AUC). Absolute bioavailability of vildagliptin is 85%.L32803

Metabolisme

About 69% of orally administered vildagpliptin is eliminated via metabolism not mediated by cytochrome P450 enzymes. Based on the findings of a rat study, DPP-4 contributes partially to the hydrolysis of vildagliptin.L32803 Vildagliptin is metabolized to pharmacologically inactive cyano (57%) and amide (4%) hydrolysis products in the kidney.A232488 LAY 151 (M20.7) is a major inactive metabolite and a carboxylic acid that is formed via hydrolysis of the cyano moiety: it accounts for 57% of the dose.L32803 Other circulating metabolites reported are an N-glucuronide (M20.2), an N-amide hydrolysis product (M15.3), two oxidation products, M21.6 and M20.9.L32818

Rute Eliminasi

Vildagliptin is eliminated via metabolism. Following oral administration, approximately 85% of the radiolabelled vildagliptin dose was excreted in urine and about 15% of the dose was recovered in feces. Of the recovered dose in urine, about 23% accounted for the unchanged parent compound.L32803

Interaksi Makanan

1 Data
  • 1. Take with or without food. Food reduces Cmax and delays Tmax, but not in a clinically significant way.

Interaksi Obat

650 Data
Pegvisomant The risk or severity of hypoglycemia can be increased when Pegvisomant is combined with Vildagliptin.
Lipoic acid The risk or severity of hypoglycemia can be increased when Lipoic acid is combined with Vildagliptin.
Moxifloxacin The therapeutic efficacy of Vildagliptin can be increased when used in combination with Moxifloxacin.
Grepafloxacin The therapeutic efficacy of Vildagliptin can be increased when used in combination with Grepafloxacin.
Enoxacin The therapeutic efficacy of Vildagliptin can be increased when used in combination with Enoxacin.
Pefloxacin The therapeutic efficacy of Vildagliptin can be increased when used in combination with Pefloxacin.
Ciprofloxacin The therapeutic efficacy of Vildagliptin can be increased when used in combination with Ciprofloxacin.
Trovafloxacin The therapeutic efficacy of Vildagliptin can be increased when used in combination with Trovafloxacin.
Nalidixic acid The therapeutic efficacy of Vildagliptin can be increased when used in combination with Nalidixic acid.
Rosoxacin The therapeutic efficacy of Vildagliptin can be increased when used in combination with Rosoxacin.
Cinoxacin The therapeutic efficacy of Vildagliptin can be increased when used in combination with Cinoxacin.
Lomefloxacin The therapeutic efficacy of Vildagliptin can be increased when used in combination with Lomefloxacin.
Gatifloxacin The therapeutic efficacy of Vildagliptin can be increased when used in combination with Gatifloxacin.
Norfloxacin The therapeutic efficacy of Vildagliptin can be increased when used in combination with Norfloxacin.
Levofloxacin The therapeutic efficacy of Vildagliptin can be increased when used in combination with Levofloxacin.
Gemifloxacin The therapeutic efficacy of Vildagliptin can be increased when used in combination with Gemifloxacin.
Ofloxacin The therapeutic efficacy of Vildagliptin can be increased when used in combination with Ofloxacin.
Sparfloxacin The therapeutic efficacy of Vildagliptin can be increased when used in combination with Sparfloxacin.
Temafloxacin The therapeutic efficacy of Vildagliptin can be increased when used in combination with Temafloxacin.
Fleroxacin The therapeutic efficacy of Vildagliptin can be increased when used in combination with Fleroxacin.
Technetium Tc-99m ciprofloxacin The therapeutic efficacy of Vildagliptin can be increased when used in combination with Technetium Tc-99m ciprofloxacin.
Garenoxacin The therapeutic efficacy of Vildagliptin can be increased when used in combination with Garenoxacin.
Nemonoxacin The therapeutic efficacy of Vildagliptin can be increased when used in combination with Nemonoxacin.
Flumequine The therapeutic efficacy of Vildagliptin can be increased when used in combination with Flumequine.
Enrofloxacin The therapeutic efficacy of Vildagliptin can be increased when used in combination with Enrofloxacin.
Orbifloxacin The therapeutic efficacy of Vildagliptin can be increased when used in combination with Orbifloxacin.
Sarafloxacin The therapeutic efficacy of Vildagliptin can be increased when used in combination with Sarafloxacin.
Difloxacin The therapeutic efficacy of Vildagliptin can be increased when used in combination with Difloxacin.
Pazufloxacin The therapeutic efficacy of Vildagliptin can be increased when used in combination with Pazufloxacin.
Prulifloxacin The therapeutic efficacy of Vildagliptin can be increased when used in combination with Prulifloxacin.
Delafloxacin The therapeutic efficacy of Vildagliptin can be increased when used in combination with Delafloxacin.
Sitafloxacin The therapeutic efficacy of Vildagliptin can be increased when used in combination with Sitafloxacin.
Oxolinic acid The therapeutic efficacy of Vildagliptin can be increased when used in combination with Oxolinic acid.
Rufloxacin The therapeutic efficacy of Vildagliptin can be increased when used in combination with Rufloxacin.
Pipemidic acid The therapeutic efficacy of Vildagliptin can be increased when used in combination with Pipemidic acid.
Methyclothiazide The therapeutic efficacy of Vildagliptin can be decreased when used in combination with Methyclothiazide.
Chlorthalidone The therapeutic efficacy of Vildagliptin can be decreased when used in combination with Chlorthalidone.
Bendroflumethiazide The therapeutic efficacy of Vildagliptin can be decreased when used in combination with Bendroflumethiazide.
Metolazone The therapeutic efficacy of Vildagliptin can be decreased when used in combination with Metolazone.
Benzthiazide The therapeutic efficacy of Vildagliptin can be decreased when used in combination with Benzthiazide.
Hydroflumethiazide The therapeutic efficacy of Vildagliptin can be decreased when used in combination with Hydroflumethiazide.
Indapamide The therapeutic efficacy of Vildagliptin can be decreased when used in combination with Indapamide.
Chlorothiazide The therapeutic efficacy of Vildagliptin can be decreased when used in combination with Chlorothiazide.
Hydrochlorothiazide The therapeutic efficacy of Vildagliptin can be decreased when used in combination with Hydrochlorothiazide.
Trichlormethiazide The therapeutic efficacy of Vildagliptin can be decreased when used in combination with Trichlormethiazide.
Polythiazide The therapeutic efficacy of Vildagliptin can be decreased when used in combination with Polythiazide.
Quinethazone The therapeutic efficacy of Vildagliptin can be decreased when used in combination with Quinethazone.
Cyclopenthiazide The therapeutic efficacy of Vildagliptin can be decreased when used in combination with Cyclopenthiazide.
Epitizide The therapeutic efficacy of Vildagliptin can be decreased when used in combination with Epitizide.
Amitriptyline Amitriptyline may decrease the hypoglycemic activities of Vildagliptin.
Protriptyline Protriptyline may decrease the hypoglycemic activities of Vildagliptin.
Imipramine Imipramine may decrease the hypoglycemic activities of Vildagliptin.
Nortriptyline Nortriptyline may decrease the hypoglycemic activities of Vildagliptin.
Amoxapine Amoxapine may decrease the hypoglycemic activities of Vildagliptin.
Trimipramine Trimipramine may decrease the hypoglycemic activities of Vildagliptin.
Doxepin Doxepin may decrease the hypoglycemic activities of Vildagliptin.
Desipramine Desipramine may decrease the hypoglycemic activities of Vildagliptin.
Clomipramine Clomipramine may decrease the hypoglycemic activities of Vildagliptin.
Amineptine Amineptine may decrease the hypoglycemic activities of Vildagliptin.
Dimetacrine Dimetacrine may decrease the hypoglycemic activities of Vildagliptin.
Butriptyline Butriptyline may decrease the hypoglycemic activities of Vildagliptin.
Dosulepin Dosulepin may decrease the hypoglycemic activities of Vildagliptin.
Tianeptine Tianeptine may decrease the hypoglycemic activities of Vildagliptin.
Oxaprotiline Oxaprotiline may decrease the hypoglycemic activities of Vildagliptin.
Opipramol Opipramol may decrease the hypoglycemic activities of Vildagliptin.
Amitriptylinoxide Amitriptylinoxide may decrease the hypoglycemic activities of Vildagliptin.
Dibenzepin Dibenzepin may decrease the hypoglycemic activities of Vildagliptin.
Quinupramine Quinupramine may decrease the hypoglycemic activities of Vildagliptin.
Melitracen Melitracen may decrease the hypoglycemic activities of Vildagliptin.
Lofepramine Lofepramine may decrease the hypoglycemic activities of Vildagliptin.
Iprindole Iprindole may decrease the hypoglycemic activities of Vildagliptin.
Imipramine oxide Imipramine oxide may decrease the hypoglycemic activities of Vildagliptin.
Glimepiride Vildagliptin may increase the hypoglycemic activities of Glimepiride.
Acetohexamide Vildagliptin may increase the hypoglycemic activities of Acetohexamide.
Chlorpropamide Vildagliptin may increase the hypoglycemic activities of Chlorpropamide.
Tolazamide Vildagliptin may increase the hypoglycemic activities of Tolazamide.
Glyburide Vildagliptin may increase the hypoglycemic activities of Glyburide.
Glipizide Vildagliptin may increase the hypoglycemic activities of Glipizide.
Gliclazide Vildagliptin may increase the hypoglycemic activities of Gliclazide.
Tolbutamide Vildagliptin may increase the hypoglycemic activities of Tolbutamide.
Gliquidone Vildagliptin may increase the hypoglycemic activities of Gliquidone.
Glisoxepide Vildagliptin may increase the hypoglycemic activities of Glisoxepide.
Glibornuride Vildagliptin may increase the hypoglycemic activities of Glibornuride.
Carbutamide Vildagliptin may increase the hypoglycemic activities of Carbutamide.
Metahexamide Vildagliptin may increase the hypoglycemic activities of Metahexamide.
Dapagliflozin Dapagliflozin may increase the hypoglycemic activities of Vildagliptin.
Canagliflozin Canagliflozin may increase the hypoglycemic activities of Vildagliptin.
Leuprolide The therapeutic efficacy of Vildagliptin can be decreased when used in combination with Leuprolide.
Goserelin The therapeutic efficacy of Vildagliptin can be decreased when used in combination with Goserelin.
Nelfinavir The therapeutic efficacy of Vildagliptin can be decreased when used in combination with Nelfinavir.
Indinavir The therapeutic efficacy of Vildagliptin can be decreased when used in combination with Indinavir.
Ziprasidone The therapeutic efficacy of Vildagliptin can be decreased when used in combination with Ziprasidone.
Etonogestrel The therapeutic efficacy of Vildagliptin can be decreased when used in combination with Etonogestrel.
Desogestrel The therapeutic efficacy of Vildagliptin can be decreased when used in combination with Desogestrel.
Olanzapine The therapeutic efficacy of Vildagliptin can be decreased when used in combination with Olanzapine.
Megestrol acetate The therapeutic efficacy of Vildagliptin can be decreased when used in combination with Megestrol acetate.
Clozapine The therapeutic efficacy of Vildagliptin can be decreased when used in combination with Clozapine.
Levonorgestrel The therapeutic efficacy of Vildagliptin can be decreased when used in combination with Levonorgestrel.
Progesterone The therapeutic efficacy of Vildagliptin can be decreased when used in combination with Progesterone.
Chlorpromazine The therapeutic efficacy of Vildagliptin can be decreased when used in combination with Chlorpromazine.

Target Protein

Dipeptidyl peptidase 4 DPP4

Referensi & Sumber

Synthesis reference: Stephen Winter, Jordi Bosch, Jordi Puig Serrano, Jose Javier Soto, "PROCESS FOR PREPARING VILDAGLIPTIN." U.S. Patent US20080167479, issued July 10, 2008.
Artikel (PubMed)
  • PMID: 17244786
    Balas B, Baig MR, Watson C, Dunning BE, Ligueros-Saylan M, Wang Y, He YL, Darland C, Holst JJ, Deacon CF, Cusi K, Mari A, Foley JE, DeFronzo RA: The dipeptidyl peptidase IV inhibitor vildagliptin suppresses endogenous glucose production and enhances islet function after single-dose administration in type 2 diabetic patients. J Clin Endocrinol Metab. 2007 Apr;92(4):1249-55. Epub 2007 Jan 23.
  • PMID: 18973400
    Croxtall JD, Keam SJ: Vildagliptin: a review of its use in the management of type 2 diabetes mellitus. Drugs. 2008;68(16):2387-409. doi: 10.2165/0003495-200868160-00009.
  • PMID: 18054733
    Ahren B: DPP-4 inhibitors. Best Pract Res Clin Endocrinol Metab. 2007 Dec;21(4):517-33. doi: 10.1016/j.beem.2007.07.005.
  • PMID: 19337548
    Mathieu C, Degrande E: Vildagliptin: a new oral treatment for type 2 diabetes mellitus. Vasc Health Risk Manag. 2008;4(6):1349-60. doi: 10.2147/vhrm.s3005.
  • PMID: 22339447
    He YL: Clinical pharmacokinetics and pharmacodynamics of vildagliptin. Clin Pharmacokinet. 2012 Mar 1;51(3):147-62. doi: 10.2165/11598080-000000000-00000.

Contoh Produk & Brand

Produk: 201 • International brands: 1
Produk
  • Eucreas
    Tablet, film coated • - • Oral • EU • Approved
  • Eucreas
    Tablet, film coated • - • Oral • EU • Approved
  • Eucreas
    Tablet, film coated • - • Oral • EU • Approved
  • Eucreas
    Tablet, film coated • - • Oral • EU • Approved
  • Eucreas
    Tablet, film coated • - • Oral • EU • Approved
  • Eucreas
    Tablet, film coated • - • Oral • EU • Approved
  • Eucreas
    Tablet, film coated • - • Oral • EU • Approved
  • Eucreas
    Tablet, film coated • - • Oral • EU • Approved
Menampilkan 8 dari 201 produk.
International Brands
  • EQUA

Sekuens Gen/Protein (FASTA)

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