Peringatan Keamanan

LD50=100-250 mg/kg (acute oral toxicity)

Leflunomide

DB01097

small molecule approved investigational

Deskripsi

Leflunomide is a pyrimidine synthesis inhibitor belonging to the DMARD (disease-modifying antirheumatic drug) class of drugs, which are chemically and pharmacologically very heterogeneous. Leflunomide was approved by FDA and in many other countries (e.g., Canada, Europe) in 1999.

Struktur Molekul 2D

Berat 270.2073
Wujud solid

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

Profil Farmakokinetik

Waktu Paruh (Half-Life) 2 weeks
Volume Distribusi * 0.13 L/kg
Klirens (Clearance) -

Absorpsi

Well absorbed, peak plasma concentrations appear 6-12 hours after dosing

Metabolisme

Primarily hepatic. Leflunomide is converted to its active form following oral intake.

Rute Eliminasi

The active metabolite is eliminated by further metabolism and subsequent renal excretion as well as by direct biliary excretion. In a 28 day study of drug elimination (n=3) using a single dose of radiolabeled compound, approximately 43% of the total radioactivity was eliminated in the urine and 48% was eliminated in the feces. It is not known whether leflunomide is excreted in human milk. Many drugs are excreted in human milk, and there is a potential for serious adverse reactions in nursing infants from leflunomide.

Farmakogenomik

1 Varian
CYP1A2 (rs762551)

The presence of this genotype in CYP1A2 may be associated with an increased risk of drug-related toxicity from leflunomide therapy.

Interaksi Makanan

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

Interaksi Obat

904 Data
Denosumab The risk or severity of adverse effects can be increased when Denosumab is combined with Leflunomide.
Natalizumab The risk or severity of immunosuppression can be increased when Leflunomide is combined with Natalizumab.
Pimecrolimus The risk or severity of adverse effects can be increased when Pimecrolimus is combined with Leflunomide.
Roflumilast Roflumilast may increase the immunosuppressive activities of Leflunomide.
Sipuleucel-T The therapeutic efficacy of Sipuleucel-T can be decreased when used in combination with Leflunomide.
Deferasirox The serum concentration of Leflunomide can be increased when it is combined with Deferasirox.
Metoclopramide The serum concentration of Metoclopramide can be decreased when it is combined with Leflunomide.
Efavirenz The serum concentration of Efavirenz can be decreased when it is combined with Leflunomide.
Tamoxifen The serum concentration of Tamoxifen can be decreased when it is combined with Leflunomide.
Azelastine The serum concentration of Azelastine can be decreased when it is combined with Leflunomide.
Mefenamic acid The serum concentration of Mefenamic acid can be decreased when it is combined with Leflunomide.
Flecainide The serum concentration of Flecainide can be decreased when it is combined with Leflunomide.
Fluvoxamine The serum concentration of Fluvoxamine can be decreased when it is combined with Leflunomide.
Betaxolol The serum concentration of Betaxolol can be decreased when it is combined with Leflunomide.
Caffeine The serum concentration of Caffeine can be decreased when it is combined with Leflunomide.
Anagrelide The serum concentration of Anagrelide can be decreased when it is combined with Leflunomide.
Ropinirole The serum concentration of Ropinirole can be decreased when it is combined with Leflunomide.
Theophylline The serum concentration of Theophylline can be decreased when it is combined with Leflunomide.
Disopyramide The serum concentration of Disopyramide can be decreased when it is combined with Leflunomide.
Lidocaine The serum concentration of Lidocaine can be decreased when it is combined with Leflunomide.
Conjugated estrogens The serum concentration of Conjugated estrogens can be decreased when it is combined with Leflunomide.
Ropivacaine The serum concentration of Ropivacaine can be decreased when it is combined with Leflunomide.
Zolmitriptan The serum concentration of Zolmitriptan can be decreased when it is combined with Leflunomide.
Acetaminophen The serum concentration of Acetaminophen can be decreased when it is combined with Leflunomide.
Amitriptyline The serum concentration of Amitriptyline can be decreased when it is combined with Leflunomide.
Olanzapine The serum concentration of Olanzapine can be decreased when it is combined with Leflunomide.
Chlorzoxazone The serum concentration of Chlorzoxazone can be decreased when it is combined with Leflunomide.
Clozapine The serum concentration of Clozapine can be decreased when it is combined with Leflunomide.
Grepafloxacin The serum concentration of Grepafloxacin can be decreased when it is combined with Leflunomide.
Mirtazapine The serum concentration of Mirtazapine can be decreased when it is combined with Leflunomide.
Mexiletine The serum concentration of Mexiletine can be decreased when it is combined with Leflunomide.
Tacrine The serum concentration of Tacrine can be decreased when it is combined with Leflunomide.
Triamterene The serum concentration of Triamterene can be decreased when it is combined with Leflunomide.
Promazine The serum concentration of Promazine can be decreased when it is combined with Leflunomide.
Zolpidem The serum concentration of Zolpidem can be decreased when it is combined with Leflunomide.
Entecavir The serum concentration of Entecavir can be decreased when it is combined with Leflunomide.
Imipramine The serum concentration of Imipramine can be decreased when it is combined with Leflunomide.
Nabumetone The serum concentration of Nabumetone can be decreased when it is combined with Leflunomide.
Quinine The serum concentration of Quinine can be decreased when it is combined with Leflunomide.
Fluoxetine The serum concentration of Fluoxetine can be decreased when it is combined with Leflunomide.
Chlorpromazine The serum concentration of Chlorpromazine can be decreased when it is combined with Leflunomide.
Flutamide The serum concentration of Flutamide can be decreased when it is combined with Leflunomide.
Haloperidol The serum concentration of Haloperidol can be decreased when it is combined with Leflunomide.
Albendazole The serum concentration of Albendazole can be decreased when it is combined with Leflunomide.
Erlotinib The serum concentration of Erlotinib can be decreased when it is combined with Leflunomide.
Mephenytoin The serum concentration of Mephenytoin can be decreased when it is combined with Leflunomide.
Rofecoxib The serum concentration of Rofecoxib can be decreased when it is combined with Leflunomide.
Cinnarizine The serum concentration of Cinnarizine can be decreased when it is combined with Leflunomide.
Propranolol The serum concentration of Propranolol can be decreased when it is combined with Leflunomide.
Clonidine The serum concentration of Clonidine can be decreased when it is combined with Leflunomide.
Diclofenac The serum concentration of Diclofenac can be decreased when it is combined with Leflunomide.
Guanabenz The serum concentration of Guanabenz can be decreased when it is combined with Leflunomide.
Verapamil The serum concentration of Verapamil can be decreased when it is combined with Leflunomide.
Warfarin The serum concentration of Warfarin can be decreased when it is combined with Leflunomide.
Tizanidine The serum concentration of Tizanidine can be decreased when it is combined with Leflunomide.
Thiabendazole The serum concentration of Thiabendazole can be decreased when it is combined with Leflunomide.
Riluzole The serum concentration of Riluzole can be decreased when it is combined with Leflunomide.
Zileuton The serum concentration of Zileuton can be decreased when it is combined with Leflunomide.
Clopidogrel The serum concentration of Clopidogrel can be decreased when it is combined with Leflunomide.
Estradiol The serum concentration of Estradiol can be decreased when it is combined with Leflunomide.
Acyclovir The serum concentration of Acyclovir can be decreased when it is combined with Leflunomide.
Naproxen The serum concentration of Naproxen can be decreased when it is combined with Leflunomide.
Pentoxifylline The serum concentration of Pentoxifylline can be decreased when it is combined with Leflunomide.
Trifluoperazine The serum concentration of Trifluoperazine can be decreased when it is combined with Leflunomide.
Perphenazine The serum concentration of Perphenazine can be decreased when it is combined with Leflunomide.
Terbinafine The serum concentration of Terbinafine can be decreased when it is combined with Leflunomide.
Ranitidine The serum concentration of Ranitidine can be decreased when it is combined with Leflunomide.
Ethanol The serum concentration of Ethanol can be decreased when it is combined with Leflunomide.
Cyclobenzaprine The serum concentration of Cyclobenzaprine can be decreased when it is combined with Leflunomide.
Maprotiline The serum concentration of Maprotiline can be decreased when it is combined with Leflunomide.
Alosetron The serum concentration of Alosetron can be decreased when it is combined with Leflunomide.
Lomefloxacin The serum concentration of Lomefloxacin can be decreased when it is combined with Leflunomide.
Ramelteon The serum concentration of Ramelteon can be decreased when it is combined with Leflunomide.
Frovatriptan The serum concentration of Frovatriptan can be decreased when it is combined with Leflunomide.
Levobupivacaine The serum concentration of Levobupivacaine can be decreased when it is combined with Leflunomide.
Cinacalcet The serum concentration of Cinacalcet can be decreased when it is combined with Leflunomide.
Selegiline The serum concentration of Selegiline can be decreased when it is combined with Leflunomide.
Tocainide The serum concentration of Tocainide can be decreased when it is combined with Leflunomide.
Praziquantel The serum concentration of Praziquantel can be decreased when it is combined with Leflunomide.
Melatonin The serum concentration of Melatonin can be decreased when it is combined with Leflunomide.
Primaquine The serum concentration of Primaquine can be decreased when it is combined with Leflunomide.
Hesperetin The serum concentration of Hesperetin can be decreased when it is combined with Leflunomide.
Pimozide The serum concentration of Pimozide can be decreased when it is combined with Leflunomide.
Nifedipine The serum concentration of Nifedipine can be decreased when it is combined with Leflunomide.
Carvedilol The serum concentration of Carvedilol can be decreased when it is combined with Leflunomide.
Doxepin The serum concentration of Doxepin can be decreased when it is combined with Leflunomide.
Cilostazol The serum concentration of Cilostazol can be decreased when it is combined with Leflunomide.
Propafenone The serum concentration of Propafenone can be decreased when it is combined with Leflunomide.
Domperidone The serum concentration of Domperidone can be decreased when it is combined with Leflunomide.
Dexfenfluramine The serum concentration of Dexfenfluramine can be decreased when it is combined with Leflunomide.
Aminophylline The serum concentration of Aminophylline can be decreased when it is combined with Leflunomide.
Clomipramine The serum concentration of Clomipramine can be decreased when it is combined with Leflunomide.
Oxtriphylline The serum concentration of Oxtriphylline can be decreased when it is combined with Leflunomide.
Rasagiline The serum concentration of Rasagiline can be decreased when it is combined with Leflunomide.
Temafloxacin The serum concentration of Temafloxacin can be decreased when it is combined with Leflunomide.
Theobromine The serum concentration of Theobromine can be decreased when it is combined with Leflunomide.
Acenocoumarol The serum concentration of Acenocoumarol can be decreased when it is combined with Leflunomide.
Aminophenazone The serum concentration of Aminophenazone can be decreased when it is combined with Leflunomide.
Antipyrine The serum concentration of Antipyrine can be decreased when it is combined with Leflunomide.
Fenethylline The serum concentration of Fenethylline can be decreased when it is combined with Leflunomide.

Target Protein

Dihydroorotate dehydrogenase (quinone), mitochondrial DHODH
Dihydroorotate dehydrogenase (quinone), mitochondrial
Aryl hydrocarbon receptor AHR
Protein-tyrosine kinase 2-beta PTK2B

Referensi & Sumber

Synthesis reference: Ilya Avrutov, "Novel processes for making- and a new crystalline form of- leflunomide." U.S. Patent US20010031878, issued October 18, 2001.
Artikel (PubMed)
  • PMID: 10890256
    Goldenberg MM: Leflunomide, a novel immunomodulator for the treatment of active rheumatoid arthritis. Clin Ther. 1999 Nov;21(11):1837-52; discussion 1821.
  • PMID: 15189743
    Li EK, Tam LS, Tomlinson B: Leflunomide in the treatment of rheumatoid arthritis. Clin Ther. 2004 Apr;26(4):447-59.
  • PMID: 12003373
    Sanders S, Harisdangkul V: Leflunomide for the treatment of rheumatoid arthritis and autoimmunity. Am J Med Sci. 2002 Apr;323(4):190-3.
  • PMID: 11053058
    Breedveld FC, Dayer JM: Leflunomide: mode of action in the treatment of rheumatoid arthritis. Ann Rheum Dis. 2000 Nov;59(11):841-9.
  • PMID: 1060033
    Reitzik M, Lownie JF: Familial polyostotic fibrous dysplasia. Oral Surg Oral Med Oral Pathol. 1975 Dec;40(6):769-74.
  • PMID: 10878294
    Herrmann ML, Schleyerbach R, Kirschbaum BJ: Leflunomide: an immunomodulatory drug for the treatment of rheumatoid arthritis and other autoimmune diseases. Immunopharmacology. 2000 May;47(2-3):273-89.
  • PMID: 10878295
    Schattenkirchner M: The use of leflunomide in the treatment of rheumatoid arthritis: an experimental and clinical review. Immunopharmacology. 2000 May;47(2-3):291-8.
  • PMID: 9666414
    Fox RI: Mechanism of action of leflunomide in rheumatoid arthritis. J Rheumatol Suppl. 1998 Jul;53:20-6.

Contoh Produk & Brand

Produk: 154 • International brands: 0
Produk
  • Accel-leflunomide
    Tablet • 10 mg • Oral • Canada • Generic • Approved
  • Accel-leflunomide
    Tablet • 20 mg • Oral • Canada • Generic • Approved
  • Apo-leflunomide
    Tablet • 10 mg • Oral • Canada • Generic • Approved
  • Apo-leflunomide
    Tablet • 20 mg • Oral • Canada • Generic • Approved
  • Arava
    Tablet, film coated • 10 mg/1 • Oral • US • Approved
  • Arava
    Tablet, film coated • 10 mg/1 • Oral • US • Approved
  • Arava
    Tablet, film coated • 20 mg/1 • Oral • US • Approved
  • Arava
    Tablet, film coated • 100 mg/1 • Oral • US • Approved
Menampilkan 8 dari 154 produk.

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