Peringatan Keamanan

The adverse effects associated with overdosage of montelukast include abdominal pain, somnolence, thirst, headache, vomiting, psychomotor hyperactivity, and less frequently, convulsion.L6301,L6304,L6307,L6310,L6325,L6328,L6331

The oral LD50 value determined for mice and rats is >5000 mg/kg.L6301,L6304,L6307,L6310,L6325,L6328,L6331

Montelukast has not been studied in pregnant women.L6301,L6304,L6307,L6310,L6325,L6328,L6331 Consequently, it should be used during pregnancy only if clearly needed.L6301,L6304,L6307,L6310,L6325,L6328,L6331

Additionally, as it is unknown whether montelukast is excreted into human breast milk, there is also caution regarding the use of the medication in nursing mothers.L6301,L6304,L6307,L6310,L6325,L6328,L6331

The plasma half-life of montelukast is somewhat prolonged in elderly patients, although no dosage adjustment is generally necessary.L6301,L6304,L6307,L6310,L6325,L6328,L6331

Montelukast

DB00471

small molecule approved

Deskripsi

Montelukast was first approved for clinical use by the US FDA in 1998 as Merck's brand name Singulair.L6301 The medication is a member of the leukotriene receptor antagonist (LTRA) category of drugs.L6301,L6304,L6307,L6310,L6325,L6328,L6331 Although capable of demonstrating effectiveness, the use of such LTRAs like montelukast is typically in addition to or complementary with the use of inhaled corticosteroids or other agents in asthma step therapy.A178645 Regardless, in 2008-2009, there were FDA-led investigations into the possibility of montelukast to elicit neuropsychiatric effects like agitation, hallucinations, suicidal behaviour, and others in individuals who used the medication.A178651 And although these kinds of effects are currently included in the official prescribing information for montelukast,L6301,L6304,L6307,L6310,L6325,L6328,L6331 the drug still sees extensive use worldwide via millions of prescriptions annually and has since become available as a generic and as a brand name product.

Struktur Molekul 2D

Berat 586.183
Wujud solid

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

Profil Farmakokinetik

Waktu Paruh (Half-Life) Studies have demonstrated that the mean plasma half-life of montelukast varies from 2.7 to 5.5 hours when observed in healthy young adults.[L6301,L6304,L6307,L6325,L6328,L6331]
Volume Distribusi The steady-state volume of distribution recorded for montelukast is an average between 8 to 11 litres.[L6301,L6304,L6307,L6325,L6328,L6331]
Klirens (Clearance) The plasma clearance documented for montelukast is an average of 45 mL/min when observed in healthy adults.[L6301,L6304,L6307,L6325,L6328,L6331]

Absorpsi

It has been observed that montelukast is quickly absorbed following administration by the oral route.L6301,L6304,L6307,L6310,L6325,L6328,L6331 The oral bioavailability documented for the drug is 64%.L6301,L6304,L6307,L6310,L6325,L6328,L6331 Furthermore, it seems that having a regular meal in the morning or even a high fat snack in the evening does not affect the absorption of montelukast.L6301,L6304,L6307,L6310,L6325,L6328,L6331

Metabolisme

It has been determined that montelukast is highly metabolized and typically so by the cytochrome P450 3A4, 2C8, and 2C9 isoenzymes.L6301,L6304,L6307,L6310,L6325,L6328,L6331 In particular, it seems that the CYP2C8 enzymes play a significant role in the metabolism of the drug.L6301,L6304,L6307,L6310,L6325,L6328,L6331 Nevertheless, at therapeutic doses, the plasma concentrations of montelukast metabolites are undetectable at steady state in adults and pediatric patients.L6301,L6304,L6307,L6310,L6325,L6328,L6331

Rute Eliminasi

It has been reported that montelukast and its metabolites are almost exclusively excreted in the bile and into the feces.L6301,L6304,L6307,L6310,L6325,L6328,L6331

Interaksi Makanan

1 Data
  • 1. Take with or without food. The absorption is unaffected by food.

Interaksi Obat

556 Data
Loxapine The therapeutic efficacy of Montelukast can be decreased when used in combination with Loxapine.
Mifepristone The serum concentration of Montelukast can be increased when it is combined with Mifepristone.
Fluvoxamine The metabolism of Montelukast can be decreased when combined with Fluvoxamine.
Troglitazone The metabolism of Montelukast can be decreased when combined with Troglitazone.
Fluoxetine The metabolism of Montelukast can be decreased when combined with Fluoxetine.
Nabilone The metabolism of Nabilone can be decreased when combined with Montelukast.
Imatinib The metabolism of Montelukast can be decreased when combined with Imatinib.
Felbamate The metabolism of Montelukast can be decreased when combined with Felbamate.
Sulfinpyrazone The metabolism of Montelukast can be decreased when combined with Sulfinpyrazone.
Iproniazid The metabolism of Montelukast can be decreased when combined with Iproniazid.
Abiraterone The metabolism of Montelukast can be decreased when combined with Abiraterone.
Medical Cannabis The metabolism of Montelukast can be decreased when combined with Medical Cannabis.
Valproic acid The metabolism of Montelukast can be decreased when combined with Valproic acid.
Quinidine The metabolism of Montelukast can be decreased when combined with Quinidine.
Fluconazole The metabolism of Montelukast can be decreased when combined with Fluconazole.
Floxuridine The metabolism of Montelukast can be decreased when combined with Floxuridine.
Nicardipine The metabolism of Montelukast can be decreased when combined with Nicardipine.
Miconazole The metabolism of Montelukast can be decreased when combined with Miconazole.
Gemfibrozil The metabolism of Montelukast can be decreased when combined with Gemfibrozil.
Sulfaphenazole The metabolism of Montelukast can be decreased when combined with Sulfaphenazole.
Secobarbital The metabolism of Montelukast can be increased when combined with Secobarbital.
Rifampin The metabolism of Montelukast can be increased when combined with Rifampicin.
Pentobarbital The metabolism of Montelukast can be increased when combined with Pentobarbital.
Teriflunomide The metabolism of Montelukast can be decreased when combined with Teriflunomide.
Bexarotene The metabolism of Montelukast can be decreased when combined with Bexarotene.
Levothyroxine The metabolism of Montelukast can be decreased when combined with Levothyroxine.
Oxybutynin The metabolism of Montelukast can be decreased when combined with Oxybutynin.
Lovastatin The risk or severity of myopathy, rhabdomyolysis, and myoglobinuria can be increased when Lovastatin is combined with Montelukast.
Diltiazem The metabolism of Montelukast can be decreased when combined with Diltiazem.
Quinine The metabolism of Montelukast can be decreased when combined with Quinine.
Irbesartan The metabolism of Montelukast can be decreased when combined with Irbesartan.
Pioglitazone The metabolism of Montelukast can be decreased when combined with Pioglitazone.
Salmeterol The metabolism of Montelukast can be decreased when combined with Salmeterol.
Mometasone furoate The metabolism of Montelukast can be decreased when combined with Mometasone furoate.
Clopidogrel The metabolism of Montelukast can be decreased when combined with Clopidogrel.
Candesartan cilexetil The metabolism of Montelukast can be decreased when combined with Candesartan cilexetil.
Fluticasone The metabolism of Montelukast can be decreased when combined with Fluticasone.
Fluticasone propionate The metabolism of Montelukast can be decreased when combined with Fluticasone propionate.
Felodipine The metabolism of Montelukast can be decreased when combined with Felodipine.
Tranylcypromine The metabolism of Montelukast can be decreased when combined with Tranylcypromine.
Letrozole The metabolism of Montelukast can be decreased when combined with Letrozole.
Pitolisant The serum concentration of Montelukast can be decreased when it is combined with Pitolisant.
Metreleptin The metabolism of Montelukast can be increased when combined with Metreleptin.
Leuprolide The risk or severity of myopathy, rhabdomyolysis, and myoglobinuria can be increased when Leuprolide is combined with Montelukast.
Somatotropin The risk or severity of myopathy, rhabdomyolysis, and myoglobinuria can be increased when Somatotropin is combined with Montelukast.
Daptomycin The risk or severity of myopathy, rhabdomyolysis, and myoglobinuria can be increased when Daptomycin is combined with Montelukast.
Pravastatin The risk or severity of myopathy, rhabdomyolysis, and myoglobinuria can be increased when Pravastatin is combined with Montelukast.
Baclofen The risk or severity of myopathy, rhabdomyolysis, and myoglobinuria can be increased when Baclofen is combined with Montelukast.
Cladribine The risk or severity of myopathy, rhabdomyolysis, and myoglobinuria can be increased when Cladribine is combined with Montelukast.
Pamidronic acid The risk or severity of myopathy, rhabdomyolysis, and myoglobinuria can be increased when Pamidronic acid is combined with Montelukast.
Mefloquine The risk or severity of myopathy, rhabdomyolysis, and myoglobinuria can be increased when Mefloquine is combined with Montelukast.
Tacrine The risk or severity of myopathy, rhabdomyolysis, and myoglobinuria can be increased when Tacrine is combined with Montelukast.
Carbimazole The risk or severity of myopathy, rhabdomyolysis, and myoglobinuria can be increased when Carbimazole is combined with Montelukast.
Cerivastatin The risk or severity of myopathy, rhabdomyolysis, and myoglobinuria can be increased when Cerivastatin is combined with Montelukast.
Trimethoprim The metabolism of Montelukast can be decreased when combined with Trimethoprim.
Betamethasone The risk or severity of myopathy, rhabdomyolysis, and myoglobinuria can be increased when Betamethasone is combined with Montelukast.
Zidovudine The risk or severity of myopathy, rhabdomyolysis, and myoglobinuria can be increased when Montelukast is combined with Zidovudine.
Cimetidine The risk or severity of myopathy, rhabdomyolysis, and myoglobinuria can be increased when Montelukast is combined with Cimetidine.
Lercanidipine The risk or severity of myopathy, rhabdomyolysis, and myoglobinuria can be increased when Montelukast is combined with Lercanidipine.
Ciprofloxacin The metabolism of Montelukast can be decreased when combined with Ciprofloxacin.
Vincristine The risk or severity of myopathy, rhabdomyolysis, and myoglobinuria can be increased when Montelukast is combined with Vincristine.
Propylthiouracil The risk or severity of myopathy, rhabdomyolysis, and myoglobinuria can be increased when Montelukast is combined with Propylthiouracil.
Methotrexate The risk or severity of myopathy, rhabdomyolysis, and myoglobinuria can be increased when Montelukast is combined with Methotrexate.
Enalapril The risk or severity of myopathy, rhabdomyolysis, and myoglobinuria can be increased when Montelukast is combined with Enalapril.
Nizatidine The risk or severity of myopathy, rhabdomyolysis, and myoglobinuria can be increased when Montelukast is combined with Nizatidine.
Ivermectin The risk or severity of myopathy, rhabdomyolysis, and myoglobinuria can be increased when Montelukast is combined with Ivermectin.
Chloroquine The risk or severity of myopathy, rhabdomyolysis, and myoglobinuria can be increased when Montelukast is combined with Chloroquine.
Triamcinolone The risk or severity of myopathy, rhabdomyolysis, and myoglobinuria can be increased when Montelukast is combined with Triamcinolone.
Niacin The risk or severity of myopathy, rhabdomyolysis, and myoglobinuria can be increased when Montelukast is combined with Niacin.
Alendronic acid The risk or severity of myopathy, rhabdomyolysis, and myoglobinuria can be increased when Montelukast is combined with Alendronic acid.
Clofibrate The risk or severity of myopathy, rhabdomyolysis, and myoglobinuria can be increased when Montelukast is combined with Clofibrate.
Stavudine The risk or severity of myopathy, rhabdomyolysis, and myoglobinuria can be increased when Montelukast is combined with Stavudine.
Nafarelin The risk or severity of myopathy, rhabdomyolysis, and myoglobinuria can be increased when Montelukast is combined with Nafarelin.
Amphotericin B The risk or severity of myopathy, rhabdomyolysis, and myoglobinuria can be increased when Montelukast is combined with Amphotericin B.
Mycophenolate mofetil The risk or severity of myopathy, rhabdomyolysis, and myoglobinuria can be increased when Montelukast is combined with Mycophenolate mofetil.
Lamivudine The risk or severity of myopathy, rhabdomyolysis, and myoglobinuria can be increased when Montelukast is combined with Lamivudine.
Ibandronate The risk or severity of myopathy, rhabdomyolysis, and myoglobinuria can be increased when Montelukast is combined with Ibandronate.
Propofol The risk or severity of myopathy, rhabdomyolysis, and myoglobinuria can be increased when Montelukast is combined with Propofol.
Terbinafine The risk or severity of myopathy, rhabdomyolysis, and myoglobinuria can be increased when Montelukast is combined with Terbinafine.
Penicillamine The risk or severity of myopathy, rhabdomyolysis, and myoglobinuria can be increased when Montelukast is combined with Penicillamine.
Ranitidine The risk or severity of myopathy, rhabdomyolysis, and myoglobinuria can be increased when Montelukast is combined with Ranitidine.
Eprosartan The risk or severity of myopathy, rhabdomyolysis, and myoglobinuria can be increased when Montelukast is combined with Eprosartan.
Risedronic acid The risk or severity of myopathy, rhabdomyolysis, and myoglobinuria can be increased when Montelukast is combined with Risedronic acid.
Bumetanide The risk or severity of myopathy, rhabdomyolysis, and myoglobinuria can be increased when Montelukast is combined with Bumetanide.
Ethanol The risk or severity of myopathy, rhabdomyolysis, and myoglobinuria can be increased when Montelukast is combined with Ethanol.
Isoniazid The metabolism of Montelukast can be decreased when combined with Isoniazid.
Methyldopa The risk or severity of myopathy, rhabdomyolysis, and myoglobinuria can be increased when Montelukast is combined with Methyldopa.
Isotretinoin The risk or severity of myopathy, rhabdomyolysis, and myoglobinuria can be increased when Montelukast is combined with Isotretinoin.
Cytarabine The risk or severity of myopathy, rhabdomyolysis, and myoglobinuria can be increased when Montelukast is combined with Cytarabine.
Ganciclovir The risk or severity of myopathy, rhabdomyolysis, and myoglobinuria can be increased when Montelukast is combined with Ganciclovir.
Sulfamethoxazole The risk or severity of myopathy, rhabdomyolysis, and myoglobinuria can be increased when Montelukast is combined with Sulfamethoxazole.
Minocycline The risk or severity of myopathy, rhabdomyolysis, and myoglobinuria can be increased when Montelukast is combined with Minocycline.
Procainamide The risk or severity of myopathy, rhabdomyolysis, and myoglobinuria can be increased when Montelukast is combined with Procainamide.
Fenofibrate The risk or severity of myopathy, rhabdomyolysis, and myoglobinuria can be increased when Montelukast is combined with Fenofibrate.
Norfloxacin The risk or severity of myopathy, rhabdomyolysis, and myoglobinuria can be increased when Montelukast is combined with Norfloxacin.
Fluvastatin The metabolism of Montelukast can be decreased when combined with Fluvastatin.
Leflunomide The metabolism of Montelukast can be decreased when combined with Leflunomide.
Rosuvastatin The risk or severity of myopathy, rhabdomyolysis, and myoglobinuria can be increased when Montelukast is combined with Rosuvastatin.
Ofloxacin The risk or severity of myopathy, rhabdomyolysis, and myoglobinuria can be increased when Montelukast is combined with Ofloxacin.
Procarbazine The risk or severity of myopathy, rhabdomyolysis, and myoglobinuria can be increased when Montelukast is combined with Procarbazine.

Target Protein

Cysteinyl leukotriene receptor 1 CYSLTR1
Polyunsaturated fatty acid 5-lipoxygenase ALOX5

Referensi & Sumber

Synthesis reference: Evgeny Shapiro, Ronit Yahalomi, Valerie Niddam-Hildesheim, Greta Sterimbaum, Kobi Chen, "Processes for preparing montelukast sodium." U.S. Patent US20050256156, issued November 17, 2005.
Artikel (PubMed)
  • PMID: 27637121
    Falk NP, Hughes SW, Rodgers BC: Medications for Chronic Asthma. Am Fam Physician. 2016 Sep 15;94(6):454-62.
  • PMID: 25920571
    Lu CY, Zhang F, Lakoma MD, Butler MG, Fung V, Larkin EK, Kharbanda EO, Vollmer WM, Lieu T, Soumerai SB, Chen Wu A: Asthma Treatments and Mental Health Visits After a Food and Drug Administration Label Change for Leukotriene Inhibitors. Clin Ther. 2015 Jun 1;37(6):1280-91. doi: 10.1016/j.clinthera.2015.03.027. Epub 2015 Apr 25.

Contoh Produk & Brand

Produk: 391 • International brands: 13
Produk
  • Accel-montelukast Sodium Tablets
    Tablet • 10 mg • Oral • Canada • Generic • Approved
  • Ach-montelukast
    Tablet • 10 mg • Oral • Canada • Generic • Approved
  • Ach-montelukast
    Tablet, chewable • 4 mg • Oral • Canada • Generic • Approved
  • Ach-montelukast
    Tablet, chewable • 5 mg • Oral • Canada • Generic • Approved
  • Ag-montelukast
    Tablet, chewable • 4 mg • Oral • Canada • Generic • Approved
  • Ag-montelukast
    Tablet, chewable • 5 mg • Oral • Canada • Generic • Approved
  • Ag-montelukast
    Tablet • 10 mg • Oral • Canada • Generic • Approved
  • Apo-montelukast
    Tablet • 10 mg • Oral • Canada • Generic • Approved
Menampilkan 8 dari 391 produk.
International Brands
  • Lukotas
  • Molly — Allenge
  • Monocast — Beximco
  • Monteflo
  • Montelo-10
  • Montene — Square
  • Respaire — Santa-Farma
  • Surfair — Sandoz
  • Telumantes — Actavis
  • Ventek — Searle

Sekuens Gen/Protein (FASTA)

Sekuens dimuat saat dibutuhkan agar halaman tetap ringan.
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