Peringatan Keamanan

In rats, the oral and intraperitoneal LD50 are 1295 mg/kg and 430 mg/kg, respectively.L26821

There is limited clinical experience with overdosage of pirfenidone. A maximum tolerated pirfenidone dose of 4005 mg per day was tolerated when the drug was administered as five 267 mg capsules three times daily to healthy adult volunteers over a 12-day dose escalation. Overdosage should be managed with supportive and symptomatic care, including monitoring of vital signs and observation of the clinical status of the patient.L26801

Pirfenidone

DB04951

small molecule approved investigational

Deskripsi

Pirfenidone is a synthetic pyridone drug.A251370 It is an antifibrotic agent with anti-inflammatory and antioxidant properties A251370 that is used to treat idiopathic pulmonary fibrosis (IPF),L26801 which is a chronic, progressive form of interstitial pneumonia.A251370 While its mechanism of action is not yet fully understood, pirfenidone is proposed to primarily regulate tumor necrosis factor (TNF) pathways and modulate cellular oxidation.A251365 The FDA first approved pirfenidone alongside nintedanib as one of the first drugs to treat IPF.A251165

Struktur Molekul 2D

Berat 185.2218
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 terminal half-life is approximately three hours in healthy subjects.[L26801]
Volume Distribusi Mean apparent oral volume of distribution is approximately 59 to 71 L.[L26801] Pirfenidone is not widely distributed to tissues.[A251365]
Klirens (Clearance) Following administration of a single dose of 801 mg in healthy older adults, the mean apparent oral clearance of pirfenidone was 13.8 L/h with food and 11.8 L/h without food.[A251365]

Absorpsi

After a single oral-dose administration of 801 mg pirfenidone (as three 267 mg capsules), the Tmax ranged from 30 minutes to four hours. Food affects the absorption and safety profile of pirfenidone: in one study, food increased Tmax; decreased Cmax and AUC by 49% and 16%, respectively; and decreased the incidence of pirfenidone-induced adverse reactions.L26801

Metabolisme

According to in vitro studies, about 70-80% of pirfenidone metabolism is mediated by CYP1A2, as well as some minor contributions from CYP2C9, 2C19, 2D6, and 2E1. Four metabolites have been detected after oral administration of pirfenidone. In vitro data suggest that metabolites are not expected to be pharmacologically active at observed metabolite concentrations. The exact metabolic pathways of pirfenidone have not been fully characterized;L26801 however, one of the pathways involve CYP1A2-mediated 5-hydroxylation and subsequent oxidation to form 5-carboxy pirfenidone.A251145 In humans, only pirfenidone and 5-carboxy pirfenidone are present in plasma in significant quantities. The mean metabolite-to-parent ratio ranged from approximately 0.6 to 0.7.L26801

Rute Eliminasi

Within 24 hours, approximately 80% of the pirfenidone dose is excreted mainly in the urine.A251365 About 99.6% of the recovered dose of pirfenidone was excreted as the 5-carboxy metabolite.L26801 About less than 1% of the dose was excreted as unchanged parent drug and less than 0.1% of the dose was excreted as other metabolites.A251365

Interaksi Makanan

2 Data
  • 1. Take at the same time every day.
  • 2. Take with food. Food decreased the rate and extent of absorption. Food reduces the incidence of drug-related adverse reactions.

Interaksi Obat

1069 Data
Denosumab The risk or severity of adverse effects can be increased when Denosumab is combined with Pirfenidone.
Peginterferon alfa-2a The risk or severity of adverse effects can be increased when Peginterferon alfa-2a is combined with Pirfenidone.
Interferon alfa-n1 The risk or severity of adverse effects can be increased when Interferon alfa-n1 is combined with Pirfenidone.
Interferon alfa-n3 The risk or severity of adverse effects can be increased when Interferon alfa-n3 is combined with Pirfenidone.
Interferon gamma-1b The risk or severity of adverse effects can be increased when Interferon gamma-1b is combined with Pirfenidone.
Interferon alfa-2a The risk or severity of adverse effects can be increased when Interferon alfa-2a is combined with Pirfenidone.
Aldesleukin The risk or severity of adverse effects can be increased when Aldesleukin is combined with Pirfenidone.
Gemtuzumab ozogamicin The risk or severity of adverse effects can be increased when Gemtuzumab ozogamicin is combined with Pirfenidone.
Pegaspargase The risk or severity of adverse effects can be increased when Pegaspargase is combined with Pirfenidone.
Interferon beta-1b The risk or severity of adverse effects can be increased when Interferon beta-1b is combined with Pirfenidone.
Interferon alfacon-1 The risk or severity of adverse effects can be increased when Interferon alfacon-1 is combined with Pirfenidone.
Rituximab The risk or severity of adverse effects can be increased when Rituximab is combined with Pirfenidone.
Basiliximab The risk or severity of adverse effects can be increased when Basiliximab is combined with Pirfenidone.
Muromonab The risk or severity of adverse effects can be increased when Muromonab is combined with Pirfenidone.
Ibritumomab tiuxetan The risk or severity of adverse effects can be increased when Ibritumomab tiuxetan is combined with Pirfenidone.
Tositumomab The risk or severity of adverse effects can be increased when Tositumomab is combined with Pirfenidone.
Alemtuzumab The risk or severity of adverse effects can be increased when Alemtuzumab is combined with Pirfenidone.
Alefacept The risk or severity of adverse effects can be increased when Alefacept is combined with Pirfenidone.
Efalizumab The risk or severity of adverse effects can be increased when Efalizumab is combined with Pirfenidone.
Antithymocyte immunoglobulin (rabbit) The risk or severity of adverse effects can be increased when Antithymocyte immunoglobulin (rabbit) is combined with Pirfenidone.
Interferon alfa-2b The risk or severity of adverse effects can be increased when Interferon alfa-2b is combined with Pirfenidone.
Daclizumab The risk or severity of adverse effects can be increased when Daclizumab is combined with Pirfenidone.
Phenylalanine The risk or severity of adverse effects can be increased when Phenylalanine is combined with Pirfenidone.
Flunisolide The risk or severity of adverse effects can be increased when Flunisolide is combined with Pirfenidone.
Cladribine Pirfenidone may increase the immunosuppressive activities of Cladribine.
Carmustine The risk or severity of adverse effects can be increased when Carmustine is combined with Pirfenidone.
Amsacrine The risk or severity of adverse effects can be increased when Amsacrine is combined with Pirfenidone.
Bleomycin The risk or severity of adverse effects can be increased when Bleomycin is combined with Pirfenidone.
Chlorambucil The risk or severity of adverse effects can be increased when Chlorambucil is combined with Pirfenidone.
Raltitrexed The risk or severity of adverse effects can be increased when Raltitrexed is combined with Pirfenidone.
Mitomycin The risk or severity of adverse effects can be increased when Mitomycin is combined with Pirfenidone.
Bexarotene The risk or severity of adverse effects can be increased when Bexarotene is combined with Pirfenidone.
Vindesine The risk or severity of adverse effects can be increased when Vindesine is combined with Pirfenidone.
Floxuridine The risk or severity of adverse effects can be increased when Floxuridine is combined with Pirfenidone.
Indomethacin The risk or severity of adverse effects can be increased when Indomethacin is combined with Pirfenidone.
Tioguanine The risk or severity of adverse effects can be increased when Tioguanine is combined with Pirfenidone.
Vinorelbine The risk or severity of adverse effects can be increased when Vinorelbine is combined with Pirfenidone.
Dexrazoxane The risk or severity of adverse effects can be increased when Dexrazoxane is combined with Pirfenidone.
Beclomethasone dipropionate The risk or severity of adverse effects can be increased when Beclomethasone dipropionate is combined with Pirfenidone.
Sorafenib The risk or severity of adverse effects can be increased when Sorafenib is combined with Pirfenidone.
Streptozocin The risk or severity of adverse effects can be increased when Streptozocin is combined with Pirfenidone.
Trifluridine The risk or severity of adverse effects can be increased when Trifluridine is combined with Pirfenidone.
Gemcitabine The risk or severity of adverse effects can be increased when Gemcitabine is combined with Pirfenidone.
Betamethasone The risk or severity of adverse effects can be increased when Betamethasone is combined with Pirfenidone.
Teniposide The risk or severity of adverse effects can be increased when Teniposide is combined with Pirfenidone.
Epirubicin The risk or severity of adverse effects can be increased when Epirubicin is combined with Pirfenidone.
Chloramphenicol The risk or severity of adverse effects can be increased when Chloramphenicol is combined with Pirfenidone.
Lenalidomide The risk or severity of adverse effects can be increased when Lenalidomide is combined with Pirfenidone.
Altretamine The risk or severity of adverse effects can be increased when Altretamine is combined with Pirfenidone.
Zidovudine The risk or severity of adverse effects can be increased when Zidovudine is combined with Pirfenidone.
Cisplatin The risk or severity of adverse effects can be increased when Cisplatin is combined with Pirfenidone.
Oxaliplatin The risk or severity of adverse effects can be increased when Oxaliplatin is combined with Pirfenidone.
Cyclophosphamide The risk or severity of adverse effects can be increased when Cyclophosphamide is combined with Pirfenidone.
Vincristine The risk or severity of adverse effects can be increased when Vincristine is combined with Pirfenidone.
Fluorouracil The risk or severity of adverse effects can be increased when Fluorouracil is combined with Pirfenidone.
Propylthiouracil The risk or severity of adverse effects can be increased when Propylthiouracil is combined with Pirfenidone.
Pentostatin The risk or severity of adverse effects can be increased when Pentostatin is combined with Pirfenidone.
Methotrexate The risk or severity of adverse effects can be increased when Methotrexate is combined with Pirfenidone.
Vinblastine The risk or severity of adverse effects can be increased when Vinblastine is combined with Pirfenidone.
Fluticasone propionate The risk or severity of adverse effects can be increased when Fluticasone propionate is combined with Pirfenidone.
Fluocinolone acetonide The risk or severity of adverse effects can be increased when Fluocinolone acetonide is combined with Pirfenidone.
Linezolid The risk or severity of adverse effects can be increased when Linezolid is combined with Pirfenidone.
Imatinib The serum concentration of Pirfenidone can be increased when it is combined with Imatinib.
Triamcinolone The risk or severity of adverse effects can be increased when Triamcinolone is combined with Pirfenidone.
Clofarabine The risk or severity of adverse effects can be increased when Clofarabine is combined with Pirfenidone.
Prednisone The risk or severity of adverse effects can be increased when Prednisone is combined with Pirfenidone.
Pemetrexed The risk or severity of adverse effects can be increased when Pemetrexed is combined with Pirfenidone.
Fludrocortisone The risk or severity of adverse effects can be increased when Fludrocortisone is combined with Pirfenidone.
Mycophenolate mofetil The risk or severity of adverse effects can be increased when Mycophenolate mofetil is combined with Pirfenidone.
Daunorubicin The risk or severity of adverse effects can be increased when Daunorubicin is combined with Pirfenidone.
Irinotecan The risk or severity of adverse effects can be increased when Irinotecan is combined with Pirfenidone.
Methimazole The risk or severity of adverse effects can be increased when Methimazole is combined with Pirfenidone.
Etoposide The risk or severity of adverse effects can be increased when Etoposide is combined with Pirfenidone.
Sulfasalazine The risk or severity of adverse effects can be increased when Sulfasalazine is combined with Pirfenidone.
Dacarbazine The risk or severity of adverse effects can be increased when Dacarbazine is combined with Pirfenidone.
Temozolomide The risk or severity of adverse effects can be increased when Temozolomide is combined with Pirfenidone.
Penicillamine The risk or severity of adverse effects can be increased when Penicillamine is combined with Pirfenidone.
Prednisolone The risk or severity of adverse effects can be increased when Prednisolone is combined with Pirfenidone.
Sirolimus The risk or severity of adverse effects can be increased when Sirolimus is combined with Pirfenidone.
Mechlorethamine The risk or severity of adverse effects can be increased when Mechlorethamine is combined with Pirfenidone.
Azacitidine The risk or severity of adverse effects can be increased when Azacitidine is combined with Pirfenidone.
Carboplatin The risk or severity of adverse effects can be increased when Carboplatin is combined with Pirfenidone.
Methylprednisolone The risk or severity of adverse effects can be increased when Methylprednisolone is combined with Pirfenidone.
Dactinomycin The risk or severity of adverse effects can be increased when Dactinomycin is combined with Pirfenidone.
Cytarabine The risk or severity of adverse effects can be increased when Cytarabine is combined with Pirfenidone.
Azathioprine The risk or severity of adverse effects can be increased when Azathioprine is combined with Pirfenidone.
Doxorubicin The risk or severity of adverse effects can be increased when Doxorubicin is combined with Pirfenidone.
Hydroxyurea The risk or severity of adverse effects can be increased when Hydroxyurea is combined with Pirfenidone.
Busulfan The risk or severity of adverse effects can be increased when Busulfan is combined with Pirfenidone.
Mycophenolic acid The risk or severity of adverse effects can be increased when Mycophenolic acid is combined with Pirfenidone.
Topotecan The risk or severity of adverse effects can be increased when Topotecan is combined with Pirfenidone.
Mercaptopurine The risk or severity of adverse effects can be increased when Mercaptopurine is combined with Pirfenidone.
Thalidomide The risk or severity of adverse effects can be increased when Thalidomide is combined with Pirfenidone.
Melphalan The risk or severity of adverse effects can be increased when Melphalan is combined with Pirfenidone.
Fludarabine The risk or severity of adverse effects can be increased when Fludarabine is combined with Pirfenidone.
Flucytosine The risk or severity of adverse effects can be increased when Flucytosine is combined with Pirfenidone.
Capecitabine The serum concentration of Pirfenidone can be increased when it is combined with Capecitabine.
Trilostane The risk or severity of adverse effects can be increased when Trilostane is combined with Pirfenidone.
Procarbazine The risk or severity of adverse effects can be increased when Procarbazine is combined with Pirfenidone.
Arsenic trioxide The risk or severity of adverse effects can be increased when Arsenic trioxide is combined with Pirfenidone.

Target Protein

Transforming growth factor beta-1 proprotein TGFB1

Referensi & Sumber

Artikel (PubMed)
  • PMID: 20050822
    Cho ME, Kopp JB: Pirfenidone: an anti-fibrotic therapy for progressive kidney disease. Expert Opin Investig Drugs. 2010 Feb;19(2):275-83. doi: 10.1517/13543780903501539.
  • PMID: 21740331
    Biernacka A, Dobaczewski M, Frangogiannis NG: TGF-beta signaling in fibrosis. Growth Factors. 2011 Oct;29(5):196-202. doi: 10.3109/08977194.2011.595714. Epub 2011 Jul 11.
  • PMID: 31967851
    Ruwanpura SM, Thomas BJ, Bardin PG: Pirfenidone: Molecular Mechanisms and Potential Clinical Applications in Lung Disease. Am J Respir Cell Mol Biol. 2020 Apr;62(4):413-422. doi: 10.1165/rcmb.2019-0328TR.
  • PMID: 32341751
    Ballester B, Milara J, Cortijo J: Pirfenidone anti-fibrotic effects are partially mediated by the inhibition of MUC1 bioactivation. Oncotarget. 2020 Apr 14;11(15):1306-1320. doi: 10.18632/oncotarget.27526. eCollection 2020 Apr 14.
  • PMID: 34779706
    Zhang Y, Sato R, Fukami T, Nakano M, Nakajima M: Pirfenidone 5-hydroxylation is mainly catalysed by CYP1A2 and partly catalysed by CYP2C19 and CYP2D6 in the human liver. Xenobiotica. 2021 Dec;51(12):1352-1359. doi: 10.1080/00498254.2021.2007553. Epub 2021 Nov 30.
  • PMID: 33465323
    Dempsey TM, Payne S, Sangaralingham L, Yao X, Shah ND, Limper AH: Adoption of the Antifibrotic Medications Pirfenidone and Nintedanib for Patients with Idiopathic Pulmonary Fibrosis. Ann Am Thorac Soc. 2021 Jul;18(7):1121-1128. doi: 10.1513/AnnalsATS.202007-901OC.
  • PMID: 26308723
    Aravena C, Labarca G, Venegas C, Arenas A, Rada G: Pirfenidone for Idiopathic Pulmonary Fibrosis: A Systematic Review and Meta-Analysis. PLoS One. 2015 Aug 26;10(8):e0136160. doi: 10.1371/journal.pone.0136160. eCollection 2015.
  • PMID: 25604027
    Kim ES, Keating GM: Pirfenidone: a review of its use in idiopathic pulmonary fibrosis. Drugs. 2015 Feb;75(2):219-30. doi: 10.1007/s40265-015-0350-9.

Contoh Produk & Brand

Produk: 124 • International brands: 0
Produk
  • Auro-pirfenidone
    Tablet • 267 mg • Oral • Canada • Generic • Approved
  • Auro-pirfenidone
    Tablet • 801 mg • Oral • Canada • Generic • Approved
  • Esbriet
    Tablet, film coated • 801 mg • Oral • EU • Approved
  • Esbriet
    Tablet, film coated • 267 mg • Oral • EU • Approved
  • Esbriet
    Tablet, film coated • 267 mg • Oral • EU • Approved
  • Esbriet
    Tablet, film coated • 267 mg • Oral • EU • Approved
  • Esbriet
    Tablet, film coated • 267 mg • Oral • EU • Approved
  • Esbriet
    Tablet, film coated • 267 mg • Oral • EU • Approved
Menampilkan 8 dari 124 produk.

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