Peringatan Keamanan

Oral LD50 value in mice, rats and dogs is reported to be > 5000 mg/kg.L49091

There have been no reports of significant overdose with dexlansoprazole. Multiple doses of 120 mg and a single dose of 300 mg did not result in death or other severe adverse events; however, serious adverse events of hypertension have been reported in association with twice daily doses of 60 mg. Nonserious adverse reactions observed with twice daily doses of 60 mg include hot flashes, contusion, oropharyngeal pain, and weight loss. Dexlansoprazole is not expected to be removed from the circulation by hemodialysis. In the event of over-exposure, treatment should be symptomatic and supportive.L48827

Dexlansoprazole

DB05351

small molecule approved investigational

Deskripsi

Dexlansoprazole is a new-generation proton pump inhibitor (PPI) used for the management of symptoms associated with gastroesophageal reflux disease (GERD) and erosive esophagitis. Dexlansoprazole is the R-enantiomer of DB00448, which is composed of a racemic mixture of the R- and S-enantiomers. Compared to the older generation of PPIs (which includes DB00213, DB00338, and DB00448),A178084 dexlansoprazole has a unique pharmacokinetic profile due to its delayed-release and dual-delivery release system: This aims to address some limitations of the older-generation PPIs, such as short plasma half-life and the need for meal-associated dosing.A19566, A19568, A178084, A174244 Dexlansoprazole inhibits the final step in gastric acid production by blocking the (H+, K+)-ATPase enzyme.L48827

Struktur Molekul 2D

Berat 369.36
Wujud solid

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

Profil Farmakokinetik

Waktu Paruh (Half-Life) Dexlansoprazole is eliminated with a half-life of approximately one to two hours.[A19573, L48827]
Volume Distribusi The apparent volume of distribution (Vz/F) after multiple doses in symptomatic GERD patients was 40 L.[L48827]
Klirens (Clearance) Apparent clearance (CL/F) in healthy subjects was 11.4 to 11.6 L/hour, respectively, after five days of 30 or 60 mg once daily administration.[L48827]

Absorpsi

The dual delayed-release formulation of dexlansoprazole results in a plasma concentration-time profile with two distinct peaks; the first peak occurs one to two hours after administration, followed by a second peak within four to five hours. About 25% of the dose is released at the pH level of 5.5 in the proximal duodenum, while the other 75% is released in the distal small intestine at the pH level of 6.75.A19567, L48827 After oral administration of dexlansoprazole 30 or 60 mg to healthy subjects and symptomatic GERD patients, mean Cmax and AUC values of dexlansoprazole increased approximately dose-proportionally. Following administration of 30 mg in healthy adults, the mean (%CV) Cmax and AUC were 658 (40%) ng/mL and 3275 (47%) ng x h/mL, respectively. At a dose of 60 mg, the mean (%CV) Cmax and AUC were 1397 (51%) ng/mL and 6529 (60%) ng x h/mL, respectively. In healthy subjects, food increased Cmax by 12 to 55% and AUC by 9 to 37%. The effect of food on Tmax varied, as both an increase and a decrease was observed.L48827

Metabolisme

Dexlansoprazole is extensively metabolized in the liver. It undergoes oxidation and reduction, followed by subsequent sulfation, glucuronidation, and glutathione conjugation to form inactive metabolites. Oxidative metabolites are formed from CYP2C19-mediated hydroxylation and CYP3A4-mediated oxidation to the sulfone.A19575, L48827 CYP2C19 is a polymorphic liver enzyme which exhibits three phenotypes in the metabolism of CYP2C19 substrates: extensive metabolizers (*1/*1), intermediate metabolizers (*1/mutant) and poor metabolizers (mutant/mutant). Dexlansoprazole is the major circulating component in plasma regardless of CYP2C19 metabolizer status. In CYP2C19 intermediate and extensive metabolizers, the major plasma metabolites are 5-hydroxy dexlansoprazole and its glucuronide conjugate, while in CYP2C19 poor metabolizers dexlansoprazole sulfone is the major plasma metabolite.L48827

Rute Eliminasi

Dexlansoprazole does not appear to be eliminated unchanged in the urine.A19573, L48827 Following the administration of 14C dexlansoprazole to six healthy male subjects, approximately 50.7% (standard deviation (SD): 9.0%) of the administered radioactivity was excreted in urine and 47.6% (SD: 7.3%) in the feces.L48827

Interaksi Makanan

2 Data
  • 1. Avoid St. John's Wort. It may induce the CYP3A4 metabolism of dexlansoprazole, possibly leading to reduced efficacy.
  • 2. Take with or without food. Dexlansoprazole's dual delayed release formulation allows it to be taken without regard to food in contrast to other PPIs.

Interaksi Obat

338 Data
Dabrafenib The serum concentration of Dexlansoprazole can be decreased when it is combined with Dabrafenib.
Amphetamine Dexlansoprazole can cause an increase in the absorption of Amphetamine resulting in an increased serum concentration and potentially a worsening of adverse effects.
Atazanavir Dexlansoprazole can cause a decrease in the absorption of Atazanavir resulting in a reduced serum concentration and potentially a decrease in efficacy.
Bosutinib Dexlansoprazole can cause a decrease in the absorption of Bosutinib resulting in a reduced serum concentration and potentially a decrease in efficacy.
Cefditoren The serum concentration of Cefditoren can be decreased when it is combined with Dexlansoprazole.
Dabigatran etexilate Dexlansoprazole can cause a decrease in the absorption of Dabigatran etexilate resulting in a reduced serum concentration and potentially a decrease in efficacy.
Dasatinib Dexlansoprazole can cause a decrease in the absorption of Dasatinib resulting in a reduced serum concentration and potentially a decrease in efficacy.
Delavirdine Dexlansoprazole can cause a decrease in the absorption of Delavirdine resulting in a reduced serum concentration and potentially a decrease in efficacy.
Dextroamphetamine Dexlansoprazole can cause an increase in the absorption of Dextroamphetamine resulting in an increased serum concentration and potentially a worsening of adverse effects.
Erlotinib Dexlansoprazole can cause a decrease in the absorption of Erlotinib resulting in a reduced serum concentration and potentially a decrease in efficacy.
Fluconazole The metabolism of Dexlansoprazole can be decreased when combined with Fluconazole.
Gefitinib Dexlansoprazole can cause a decrease in the absorption of Gefitinib resulting in a reduced serum concentration and potentially a decrease in efficacy.
Indinavir Dexlansoprazole can cause a decrease in the absorption of Indinavir resulting in a reduced serum concentration and potentially a decrease in efficacy.
Itraconazole Dexlansoprazole can cause a decrease in the absorption of Itraconazole resulting in a reduced serum concentration and potentially a decrease in efficacy.
Ledipasvir Dexlansoprazole can cause a decrease in the absorption of Ledipasvir resulting in a reduced serum concentration and potentially a decrease in efficacy.
Methotrexate The excretion of Methotrexate can be decreased when combined with Dexlansoprazole.
Methylphenidate Dexlansoprazole can cause an increase in the absorption of Methylphenidate resulting in an increased serum concentration and potentially a worsening of adverse effects.
Dexmethylphenidate Dexlansoprazole can cause an increase in the absorption of Dexmethylphenidate resulting in an increased serum concentration and potentially a worsening of adverse effects.
Nelfinavir The serum concentration of Nelfinavir can be decreased when it is combined with Dexlansoprazole.
Nilotinib The serum concentration of Nilotinib can be decreased when it is combined with Dexlansoprazole.
Pazopanib Dexlansoprazole can cause a decrease in the absorption of Pazopanib resulting in a reduced serum concentration and potentially a decrease in efficacy.
Posaconazole Dexlansoprazole can cause a decrease in the absorption of Posaconazole resulting in a reduced serum concentration and potentially a decrease in efficacy.
Raltegravir Dexlansoprazole can cause an increase in the absorption of Raltegravir resulting in an increased serum concentration and potentially a worsening of adverse effects.
Rilpivirine The serum concentration of Rilpivirine can be decreased when it is combined with Dexlansoprazole.
Riociguat Dexlansoprazole can cause a decrease in the absorption of Riociguat resulting in a reduced serum concentration and potentially a decrease in efficacy.
Risedronic acid Dexlansoprazole can cause an increase in the absorption of Risedronic acid resulting in an increased serum concentration and potentially a worsening of adverse effects.
Saquinavir The metabolism of Dexlansoprazole can be decreased when combined with Saquinavir.
Voriconazole The metabolism of Dexlansoprazole can be decreased when combined with Voriconazole.
Luliconazole The serum concentration of Dexlansoprazole can be increased when it is combined with Luliconazole.
Levothyroxine Dexlansoprazole can cause a decrease in the absorption of Levothyroxine resulting in a reduced serum concentration and potentially a decrease in efficacy.
Clopidogrel The serum concentration of the active metabolites of Clopidogrel can be reduced when Clopidogrel is used in combination with Dexlansoprazole resulting in a loss in efficacy.
Bisacodyl The therapeutic efficacy of Bisacodyl can be decreased when used in combination with Dexlansoprazole.
Captopril Dexlansoprazole can cause a decrease in the absorption of Captopril resulting in a reduced serum concentration and potentially a decrease in efficacy.
Cefuroxime The serum concentration of Cefuroxime can be decreased when it is combined with Dexlansoprazole.
Rifampin The metabolism of Dexlansoprazole can be increased when combined with Rifampicin.
Memantine Dexlansoprazole may decrease the excretion rate of Memantine which could result in a higher serum level.
Sulpiride The therapeutic efficacy of Sulpiride can be increased when used in combination with Dexlansoprazole.
Mesalazine Dexlansoprazole can cause a decrease in the absorption of Mesalazine resulting in a reduced serum concentration and potentially a decrease in efficacy.
Mycophenolic acid Dexlansoprazole can cause a decrease in the absorption of Mycophenolic acid resulting in a reduced serum concentration and potentially a decrease in efficacy.
Mycophenolate mofetil Dexlansoprazole can cause a decrease in the absorption of Mycophenolate mofetil resulting in a reduced serum concentration and potentially a decrease in efficacy.
Tolevamer The therapeutic efficacy of Tolevamer can be decreased when used in combination with Dexlansoprazole.
Alendronic acid The therapeutic efficacy of Alendronic acid can be decreased when used in combination with Dexlansoprazole.
Ibandronate The therapeutic efficacy of Ibandronate can be decreased when used in combination with Dexlansoprazole.
Clodronic acid The therapeutic efficacy of Clodronic acid can be decreased when used in combination with Dexlansoprazole.
Etidronic acid The therapeutic efficacy of Etidronic acid can be decreased when used in combination with Dexlansoprazole.
Tiludronic acid The therapeutic efficacy of Tiludronic acid can be decreased when used in combination with Dexlansoprazole.
Incadronic acid The therapeutic efficacy of Incadronic acid can be decreased when used in combination with Dexlansoprazole.
Cysteamine The bioavailability of Cysteamine can be decreased when combined with Dexlansoprazole.
Ketoconazole Dexlansoprazole can cause a decrease in the absorption of Ketoconazole resulting in a reduced serum concentration and potentially a decrease in efficacy.
Lumacaftor The metabolism of Dexlansoprazole can be increased when combined with Lumacaftor.
Tacrolimus The metabolism of Tacrolimus can be decreased when combined with Dexlansoprazole.
Methenamine The therapeutic efficacy of Methenamine can be decreased when used in combination with Dexlansoprazole.
Fluvoxamine The metabolism of Dexlansoprazole can be decreased when combined with Fluvoxamine.
Ticlopidine The metabolism of Dexlansoprazole can be decreased when combined with Ticlopidine.
Chloramphenicol The metabolism of Dexlansoprazole can be decreased when combined with Chloramphenicol.
Lansoprazole The metabolism of Dexlansoprazole can be decreased when combined with Lansoprazole.
Fluoxetine The metabolism of Dexlansoprazole can be decreased when combined with Fluoxetine.
Zafirlukast The metabolism of Dexlansoprazole can be decreased when combined with Zafirlukast.
Isoniazid The metabolism of Dexlansoprazole can be decreased when combined with Isoniazid.
Miconazole The metabolism of Dexlansoprazole can be decreased when combined with Miconazole.
Gemfibrozil The metabolism of Dexlansoprazole can be decreased when combined with Gemfibrozil.
Imipramine The metabolism of Dexlansoprazole can be decreased when combined with Imipramine.
Clomipramine The metabolism of Dexlansoprazole can be decreased when combined with Clomipramine.
Eslicarbazepine acetate The metabolism of Dexlansoprazole can be decreased when combined with Eslicarbazepine acetate.
Prussian blue Dexlansoprazole can cause a decrease in the absorption of Prussian blue resulting in a reduced serum concentration and potentially a decrease in efficacy.
Iron sucrose Dexlansoprazole can cause a decrease in the absorption of Iron sucrose resulting in a reduced serum concentration and potentially a decrease in efficacy.
Ferric ammonium citrate Dexlansoprazole can cause a decrease in the absorption of Ferric ammonium citrate resulting in a reduced serum concentration and potentially a decrease in efficacy.
Ferumoxsil Dexlansoprazole can cause a decrease in the absorption of Ferumoxsil resulting in a reduced serum concentration and potentially a decrease in efficacy.
Ferumoxides Dexlansoprazole can cause a decrease in the absorption of Ferumoxides resulting in a reduced serum concentration and potentially a decrease in efficacy.
Ferric sulfate Dexlansoprazole can cause a decrease in the absorption of Ferric sulfate resulting in a reduced serum concentration and potentially a decrease in efficacy.
Ferrous bisglycinate Dexlansoprazole can cause a decrease in the absorption of Ferrous bisglycinate resulting in a reduced serum concentration and potentially a decrease in efficacy.
Gleptoferron Dexlansoprazole can cause a decrease in the absorption of Gleptoferron resulting in a reduced serum concentration and potentially a decrease in efficacy.
Perflubutane Dexlansoprazole can cause a decrease in the absorption of Perflubutane resulting in a reduced serum concentration and potentially a decrease in efficacy.
Sodium feredetate Dexlansoprazole can cause a decrease in the absorption of Sodium feredetate resulting in a reduced serum concentration and potentially a decrease in efficacy.
Ferric hydroxide Dexlansoprazole can cause a decrease in the absorption of Ferric hydroxide resulting in a reduced serum concentration and potentially a decrease in efficacy.
Ferric cation Dexlansoprazole can cause a decrease in the absorption of Ferric cation resulting in a reduced serum concentration and potentially a decrease in efficacy.
Ferrous gluconate Dexlansoprazole can cause a decrease in the absorption of Ferrous gluconate resulting in a reduced serum concentration and potentially a decrease in efficacy.
Ferrous succinate Dexlansoprazole can cause a decrease in the absorption of Ferrous succinate resulting in a reduced serum concentration and potentially a decrease in efficacy.
Ferrous fumarate Dexlansoprazole can cause a decrease in the absorption of Ferrous fumarate resulting in a reduced serum concentration and potentially a decrease in efficacy.
Tetraferric tricitrate decahydrate Dexlansoprazole can cause a decrease in the absorption of Tetraferric tricitrate decahydrate resulting in a reduced serum concentration and potentially a decrease in efficacy.
Ferric oxyhydroxide Dexlansoprazole can cause a decrease in the absorption of Ferric oxyhydroxide resulting in a reduced serum concentration and potentially a decrease in efficacy.
Iron Dextran Dexlansoprazole can cause a decrease in the absorption of Iron Dextran resulting in a reduced serum concentration and potentially a decrease in efficacy.
Iron Dexlansoprazole can cause a decrease in the absorption of Iron resulting in a reduced serum concentration and potentially a decrease in efficacy.
Ferric pyrophosphate Dexlansoprazole can cause a decrease in the absorption of Ferric pyrophosphate resulting in a reduced serum concentration and potentially a decrease in efficacy.
Ferric maltol Dexlansoprazole can cause a decrease in the absorption of Ferric maltol resulting in a reduced serum concentration and potentially a decrease in efficacy.
Iron polymaltose Dexlansoprazole can cause a decrease in the absorption of Iron polymaltose resulting in a reduced serum concentration and potentially a decrease in efficacy.
Apalutamide The metabolism of Dexlansoprazole can be increased when combined with Apalutamide.
Pitolisant The serum concentration of Dexlansoprazole can be decreased when it is combined with Pitolisant.
Metreleptin The metabolism of Dexlansoprazole can be increased when combined with Metreleptin.
Bortezomib The metabolism of Dexlansoprazole can be decreased when combined with Bortezomib.
Pantoprazole The metabolism of Dexlansoprazole can be decreased when combined with Pantoprazole.
Olanzapine The metabolism of Dexlansoprazole can be decreased when combined with Olanzapine.
Omeprazole The metabolism of Dexlansoprazole can be decreased when combined with Omeprazole.
Nilutamide The metabolism of Dexlansoprazole can be decreased when combined with Nilutamide.
Esomeprazole The metabolism of Dexlansoprazole can be decreased when combined with Esomeprazole.
Ethanol The metabolism of Dexlansoprazole can be decreased when combined with Ethanol.
Zonisamide The metabolism of Dexlansoprazole can be decreased when combined with Zonisamide.
Etoricoxib The metabolism of Dexlansoprazole can be decreased when combined with Etoricoxib.
Oritavancin The metabolism of Dexlansoprazole can be decreased when combined with Oritavancin.
Methadone The metabolism of Dexlansoprazole can be decreased when combined with Methadone.

Target Protein

Potassium-transporting ATPase alpha chain 1 ATP4A
Potassium-transporting ATPase subunit beta ATP4B
N(G),N(G)-dimethylarginine dimethylaminohydrolase 1 DDAH1

Referensi & Sumber

Artikel (PubMed)
  • PMID: 21780890
    Behm BW, Peura DA: Dexlansoprazole MR for the management of gastroesophageal reflux disease. Expert Rev Gastroenterol Hepatol. 2011 Aug;5(4):439-45. doi: 10.1586/egh.11.37.
  • PMID: 26759624
    Skrzydlo-Radomanska B, Radwan P: Dexlansoprazole - a new-generation proton pump inhibitor. Prz Gastroenterol. 2015;10(4):191-6. doi: 10.5114/pg.2015.56109. Epub 2015 Dec 16.
  • PMID: 26586949
    Frye JW, Peura DA: Managing gastroesophageal reflux disease - comparative efficacy and outcomes of dexlansoprazole MR. Ther Clin Risk Manag. 2015 Oct 30;11:1649-56. doi: 10.2147/TCRM.S66680. eCollection 2015.
  • PMID: 21694835
    Wittbrodt ET, Baum C, Peura DA: Delayed release dexlansoprazole in the treatment of GERD and erosive esophagitis. Clin Exp Gastroenterol. 2009;2:117-28. Epub 2009 Nov 17.
  • PMID: 22455762
    Grabowski B, Lee RD: Absorption, distribution, metabolism and excretion of 14Cdexlansoprazole in healthy male subjects. Clin Drug Investig. 2012 May 1;32(5):319-32. doi: 10.2165/11630930-000000000-00000.
  • PMID: 11430506
    Tytgat GN: Shortcomings of the first-generation proton pump inhibitors. Eur J Gastroenterol Hepatol. 2001 May;13 Suppl 1:S29-33.
  • PMID: 29658189
    Haastrup PF, Thompson W, Sondergaard J, Jarbol DE: Side Effects of Long-Term Proton Pump Inhibitor Use: A Review. Basic Clin Pharmacol Toxicol. 2018 Aug;123(2):114-121. doi: 10.1111/bcpt.13023. Epub 2018 May 24.
  • PMID: 19362552
    Reimer C, Sondergaard B, Hilsted L, Bytzer P: Proton-pump inhibitor therapy induces acid-related symptoms in healthy volunteers after withdrawal of therapy. Gastroenterology. 2009 Jul;137(1):80-7, 87.e1. doi: 10.1053/j.gastro.2009.03.058. Epub 2009 Apr 10.
Menampilkan 8 dari 9 artikel.

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