Peringatan Keamanan

No dosage adjustment is necessary based on race, age, weight, sex, renal impairment, or hepatic impairmentA37050.

Studies of efficacy and safety in pediatric populations were not included in the original drug approvalL9557 but recent clinical trials show linagliptin to be well tolerated in patients 10 to 18 years oldA176960.

Animal studies showed an increased risk of lymphoma in female rats at over 200 times the clinical doseL9557. Aside from this effect, linagliptin was not shown to be mutagenic, clastogenic, or have an effect on fertilityL9557.

Linagliptin

DB08882

small molecule approved

Deskripsi

Linagliptin is a DPP-4 inhibitor developed by Boehringer Ingelheim for the treatment of type II diabetes L9557. Linagliptin differs from other DPP-4 inhibitors in that it has a non-linear pharmacokinetic profile, is not primarily eliminated by the renal system, and obeys concentration dependant protein bindingA37050. Linagliptin was approved by the FDA on May 2, 2011L9557.

Struktur Molekul 2D

Berat 472.5422
Wujud solid

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

Profil Farmakokinetik

Waktu Paruh (Half-Life) The terminal half life of linagliptin is 155 hours[A176948].
Volume Distribusi A single intravenous dose of 5mg results in a volume of distribution of 1110L[A37050]. However an intravenous infusion of 0.5-10mg results in a volume of distribution of 380-1540L[A37050].
Klirens (Clearance) Total clearance of linagliptin is 374mL/min[A176948].

Absorpsi

Oral bioavailability of linagliptin is 30%A37050.

Metabolisme

An oral dose of linagliptin is excreted primarily in the fecesA176948. 90% of an oral dose is excreted unchanged in the urine and fecesA176948,A37050. The predominant metabolite in the plasma is CD1790 and the predominant metabolite recovered after excretion was M489(1)A176948. Other metabolites are produced through oxidation, oxidative degradation, N-acetylation, glucuronidation, and cysteine adduct formationA176948. Other metabolites have been identified through mass spectrometry though no structures were determinedA176948. Metabolism of linagliptin is mediated by cytochrome P450 3A4, aldo-keto reductases, and carbonyl reductasesA176948.

Rute Eliminasi

84.7% of linagliptin is eliminated in the feces and 5.4% is eliminated in the urineA176948,A37050.

Interaksi Makanan

2 Data
  • 1. Avoid excessive or chronic alcohol consumption. Chronic or binge drinking can increase the risk of serious side effects.
  • 2. Take with or without food. High fat meals reduce the maximum concentration and increase the AUC, but not to a clinically significant extent.

Interaksi Obat

1430 Data
Pegvisomant The risk or severity of hypoglycemia can be increased when Pegvisomant is combined with Linagliptin.
Afatinib The serum concentration of Afatinib can be increased when it is combined with Linagliptin.
Bosutinib The serum concentration of Bosutinib can be increased when it is combined with Linagliptin.
Brentuximab vedotin The serum concentration of Brentuximab vedotin can be increased when it is combined with Linagliptin.
Edoxaban The serum concentration of Edoxaban can be increased when it is combined with Linagliptin.
Ledipasvir The serum concentration of Ledipasvir can be increased when it is combined with Linagliptin.
Naloxegol The serum concentration of Naloxegol can be increased when it is combined with Linagliptin.
Pazopanib The serum concentration of Pazopanib can be increased when it is combined with Linagliptin.
Prucalopride The serum concentration of Prucalopride can be increased when it is combined with Linagliptin.
Ranolazine The serum concentration of Ranolazine can be increased when it is combined with Linagliptin.
Silodosin The excretion of Silodosin can be decreased when combined with Linagliptin.
Topotecan The serum concentration of Topotecan can be increased when it is combined with Linagliptin.
Phenytoin The metabolism of Linagliptin can be increased when combined with Phenytoin.
Fosphenytoin The metabolism of Linagliptin can be increased when combined with Fosphenytoin.
Brexpiprazole The metabolism of Brexpiprazole can be decreased when combined with Linagliptin.
Eliglustat The metabolism of Eliglustat can be decreased when combined with Linagliptin.
Everolimus The metabolism of Everolimus can be decreased when combined with Linagliptin.
Flibanserin The metabolism of Flibanserin can be decreased when combined with Linagliptin.
Ibrutinib The metabolism of Ibrutinib can be decreased when combined with Linagliptin.
Ivabradine The metabolism of Ivabradine can be decreased when combined with Linagliptin.
Ivacaftor The metabolism of Ivacaftor can be decreased when combined with Linagliptin.
Lurasidone The metabolism of Lurasidone can be decreased when combined with Linagliptin.
Olaparib The metabolism of Olaparib can be decreased when combined with Linagliptin.
Sonidegib The metabolism of Sonidegib can be decreased when combined with Linagliptin.
Avanafil The metabolism of Avanafil can be decreased when combined with Linagliptin.
Eplerenone The metabolism of Eplerenone can be decreased when combined with Linagliptin.
Rifaximin The serum concentration of Rifaximin can be increased when it is combined with Linagliptin.
Cilostazol The metabolism of Cilostazol can be decreased when combined with Linagliptin.
Colchicine The serum concentration of Colchicine can be increased when it is combined with Linagliptin.
Fentanyl The metabolism of Fentanyl can be decreased when combined with Linagliptin.
Iloperidone The metabolism of Iloperidone can be decreased when combined with Linagliptin.
Retapamulin The metabolism of Retapamulin can be decreased when combined with Linagliptin.
Tofacitinib The metabolism of Tofacitinib can be decreased when combined with Linagliptin.
Vardenafil The metabolism of Vardenafil can be decreased when combined with Linagliptin.
Eszopiclone The metabolism of Eszopiclone can be decreased when combined with Linagliptin.
Zopiclone The metabolism of Zopiclone can be decreased when combined with Linagliptin.
Lovastatin The metabolism of Lovastatin can be decreased when combined with Linagliptin.
Trazodone The serum concentration of Linagliptin can be decreased when it is combined with Trazodone.
Mifepristone The serum concentration of Linagliptin can be decreased when it is combined with Mifepristone.
Rifampin The serum concentration of Linagliptin can be decreased when it is combined with Rifampicin.
St. John's Wort The serum concentration of Linagliptin can be decreased when it is combined with St. John's Wort.
Etravirine The metabolism of Linagliptin can be increased when combined with Etravirine.
Prednisolone phosphate The serum concentration of Linagliptin can be decreased when it is combined with Prednisolone phosphate.
Tipranavir The serum concentration of Linagliptin can be decreased when it is combined with Tipranavir.
Dexamethasone acetate The serum concentration of Linagliptin can be decreased when it is combined with Dexamethasone acetate.
Bupropion The excretion of Linagliptin can be decreased when combined with Bupropion.
Alfuzosin The metabolism of Alfuzosin can be decreased when combined with Linagliptin.
Alprazolam The metabolism of Alprazolam can be decreased when combined with Linagliptin.
Warfarin The serum concentration of Warfarin can be increased when it is combined with Linagliptin.
Acenocoumarol The serum concentration of Acenocoumarol can be increased when it is combined with Linagliptin.
(R)-warfarin The serum concentration of (R)-warfarin can be increased when it is combined with Linagliptin.
R,S-Warfarin alcohol The serum concentration of R,S-Warfarin alcohol can be increased when it is combined with Linagliptin.
S,R-Warfarin alcohol The serum concentration of S,R-Warfarin alcohol can be increased when it is combined with Linagliptin.
(S)-Warfarin The serum concentration of (S)-Warfarin can be increased when it is combined with Linagliptin.
Midazolam The serum concentration of Midazolam can be increased when it is combined with Linagliptin.
Tacrolimus The serum concentration of Tacrolimus can be increased when it is combined with Linagliptin.
Atorvastatin The metabolism of Atorvastatin can be decreased when combined with Linagliptin.
Lipoic acid The risk or severity of hypoglycemia can be increased when Lipoic acid is combined with Linagliptin.
Moxifloxacin The therapeutic efficacy of Linagliptin can be increased when used in combination with Moxifloxacin.
Enoxacin The therapeutic efficacy of Linagliptin can be increased when used in combination with Enoxacin.
Pefloxacin The therapeutic efficacy of Linagliptin can be increased when used in combination with Pefloxacin.
Ciprofloxacin The therapeutic efficacy of Linagliptin can be increased when used in combination with Ciprofloxacin.
Trovafloxacin The therapeutic efficacy of Linagliptin can be increased when used in combination with Trovafloxacin.
Nalidixic acid The therapeutic efficacy of Linagliptin can be increased when used in combination with Nalidixic acid.
Rosoxacin The therapeutic efficacy of Linagliptin can be increased when used in combination with Rosoxacin.
Cinoxacin The therapeutic efficacy of Linagliptin can be increased when used in combination with Cinoxacin.
Lomefloxacin The therapeutic efficacy of Linagliptin can be increased when used in combination with Lomefloxacin.
Gatifloxacin The therapeutic efficacy of Linagliptin can be increased when used in combination with Gatifloxacin.
Norfloxacin The therapeutic efficacy of Linagliptin can be increased when used in combination with Norfloxacin.
Gemifloxacin The therapeutic efficacy of Linagliptin can be increased when used in combination with Gemifloxacin.
Ofloxacin The therapeutic efficacy of Linagliptin can be increased when used in combination with Ofloxacin.
Sparfloxacin The therapeutic efficacy of Linagliptin can be increased when used in combination with Sparfloxacin.
Temafloxacin The therapeutic efficacy of Linagliptin can be increased when used in combination with Temafloxacin.
Fleroxacin The therapeutic efficacy of Linagliptin can be increased when used in combination with Fleroxacin.
Technetium Tc-99m ciprofloxacin The therapeutic efficacy of Linagliptin can be increased when used in combination with Technetium Tc-99m ciprofloxacin.
Garenoxacin The therapeutic efficacy of Linagliptin can be increased when used in combination with Garenoxacin.
Nemonoxacin The therapeutic efficacy of Linagliptin can be increased when used in combination with Nemonoxacin.
Flumequine The therapeutic efficacy of Linagliptin can be increased when used in combination with Flumequine.
Enrofloxacin The therapeutic efficacy of Linagliptin can be increased when used in combination with Enrofloxacin.
Orbifloxacin The therapeutic efficacy of Linagliptin can be increased when used in combination with Orbifloxacin.
Sarafloxacin The therapeutic efficacy of Linagliptin can be increased when used in combination with Sarafloxacin.
Difloxacin The therapeutic efficacy of Linagliptin can be increased when used in combination with Difloxacin.
Pazufloxacin The therapeutic efficacy of Linagliptin can be increased when used in combination with Pazufloxacin.
Prulifloxacin The therapeutic efficacy of Linagliptin can be increased when used in combination with Prulifloxacin.
Delafloxacin The therapeutic efficacy of Linagliptin can be increased when used in combination with Delafloxacin.
Sitafloxacin The therapeutic efficacy of Linagliptin can be increased when used in combination with Sitafloxacin.
Oxolinic acid The therapeutic efficacy of Linagliptin can be increased when used in combination with Oxolinic acid.
Rufloxacin The therapeutic efficacy of Linagliptin can be increased when used in combination with Rufloxacin.
Pipemidic acid The therapeutic efficacy of Linagliptin can be increased when used in combination with Pipemidic acid.
Levofloxacin The therapeutic efficacy of Linagliptin can be increased when used in combination with Levofloxacin.
Grepafloxacin The therapeutic efficacy of Linagliptin can be increased when used in combination with Grepafloxacin.
Methyclothiazide The therapeutic efficacy of Linagliptin can be decreased when used in combination with Methyclothiazide.
Chlorthalidone The therapeutic efficacy of Linagliptin can be decreased when used in combination with Chlorthalidone.
Bendroflumethiazide The therapeutic efficacy of Linagliptin can be decreased when used in combination with Bendroflumethiazide.
Metolazone The therapeutic efficacy of Linagliptin can be decreased when used in combination with Metolazone.
Benzthiazide The therapeutic efficacy of Linagliptin can be decreased when used in combination with Benzthiazide.
Hydroflumethiazide The therapeutic efficacy of Linagliptin can be decreased when used in combination with Hydroflumethiazide.
Indapamide The therapeutic efficacy of Linagliptin can be decreased when used in combination with Indapamide.
Chlorothiazide The therapeutic efficacy of Linagliptin can be decreased when used in combination with Chlorothiazide.
Hydrochlorothiazide The therapeutic efficacy of Linagliptin can be decreased when used in combination with Hydrochlorothiazide.

Target Protein

Dipeptidyl peptidase 4 DPP4

Referensi & Sumber

Synthesis reference: Pietro ALLEGRINI, Emanuele ATTOLINO, Marco ARTICO, "PROCESS FOR THE PREPARATION OF LINAGLIPTIN." U.S. Patent US20120165525, issued June 28, 2012.
Artikel (PubMed)
  • PMID: 22149370
    Forst T, Pfutzner A: Linagliptin, a dipeptidyl peptidase-4 inhibitor with a unique pharmacological profile, and efficacy in a broad range of patients with type 2 diabetes. Expert Opin Pharmacother. 2012 Jan;13(1):101-10. doi: 10.1517/14656566.2012.642863.
  • PMID: 20086031
    Blech S, Ludwig-Schwellinger E, Grafe-Mody EU, Withopf B, Wagner K: The metabolism and disposition of the oral dipeptidyl peptidase-4 inhibitor, linagliptin, in humans. Drug Metab Dispos. 2010 Apr;38(4):667-78. doi: 10.1124/dmd.109.031476. Epub 2010 Jan 19.
  • PMID: 22568694
    Graefe-Mody U, Retlich S, Friedrich C: Clinical pharmacokinetics and pharmacodynamics of linagliptin. Clin Pharmacokinet. 2012 Jul 1;51(7):411-27. doi: 10.2165/11630900-000000000-00000.
  • PMID: 29171139
    Tamborlane WV, Laffel LM, Weill J, Gordat M, Neubacher D, Retlich S, Hettema W, Hoesl CE, Kaspers S, Marquard J: Randomized, double-blind, placebo-controlled dose-finding study of the dipeptidyl peptidase-4 inhibitor linagliptin in pediatric patients with type 2 diabetes. Pediatr Diabetes. 2018 Jun;19(4):640-648. doi: 10.1111/pedi.12616. Epub 2017 Nov 24.

Contoh Produk & Brand

Produk: 92 • International brands: 1
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International Brands
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Sekuens Gen/Protein (FASTA)

Sekuens dimuat saat dibutuhkan agar halaman tetap ringan.
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