Peringatan Keamanan

There are no data regarding overdosage with orally administered roflumilast. Phase I studies in which roflumilast was administered at single doses up to 5000 mcg showed an increase in the incidence of headache, gastrointestinal disorders, dizziness, palpitations, lightheadedness, clamminess, and arterial hypotension.L37564 In the event of an overdose, administer support medical care as soon as possible. Hemodialysis is unlikely to be of benefit given the extensive protein binding of roflumilast.L37564

Roflumilast

DB01656

small molecule approved

Deskripsi

Roflumilast is a highly selective phosphodiesterase-4 (PDE4) inhibitor.A251385 PDE4 is a major cyclic-3',5?-adenosinemonophosphate (cyclic AMP, cAMP)-metabolizing enzyme L37564 expressed on nearly all immune and pro-inflammatory cells, in addition to structural cells like those of the smooth muscle or epithelium.A251385 The resultant increase in intracellular cAMP induced by roflumilast's inhibition of PDE4 is thought to mediate its disease-modifying effects, although its precise mechanism of action has yet to be elucidated.L37564,A251385

The oral formulation of roflumilast is indicated to manage chronic obstructive pulmonary disease.L46546 It was first approved by the EMA in July 2010, and by the FDA in January 2018.L37564 Roflumilast topical cream is indicated to treat plaque psoriasis. The cream formulation was first approved by the FDA in July 2022 L42580 and by Health Canada in April 2023.L46541 On December 15, 2023, the FDA approved a new topical foam formulation of roflumilast for the treatment of seborrheic dermatitis in patients aged 9 years and older.L49281

Struktur Molekul 2D

Berat 403.207
Wujud solid

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

Profil Farmakokinetik

Waktu Paruh (Half-Life) Following oral administration, the plasma half-lives of roflumilast and roflumilast N-oxide are 17 hours and 30 hours, respectively.[L37564]
Volume Distribusi Following a single oral dose of 500 mcg, the volume of distribution of roflumilast is approximately 2.9 L/kg.[L37564]
Klirens (Clearance) Plasma clearance of roflumilast following short-term intravenous infusion is approximately 9.6 L/h.[L37564]

Absorpsi

After a 500mcg dose, the bioavailability of roflumilast is about 80%.L37564 In the fasted state, maximum plasma concentrations are reached in 0.5 to 2 hours, while in the fed state, Cmax is reduced by 40%, Tmax is increased by one hour, and total absorption is unchanged.L37564 Applied topically, the mean systemic exposure for roflumilast and its N-oxide metabolite in adults was 72.7 ± 53.1 and 628 ± 648 h?ng/mL, respectively.L42580 The mean systemic exposure for roflumilast and its N-oxide metabolite in adolescents was 25.1 ± 24.0 and 140 ± 179 h?ng/mL, respectively.L42580

Metabolisme

Roflumilast is metabolized to roflumilast N-oxide, the active metabolite of roflumilast in humans, by CYP3A4 and CYP1A2.L37564 The N-oxide metabolite is less potent than its parent drug in regards to PDE4 inhibition, but its plasma AUC is approximately 10-fold greater.L37564

Rute Eliminasi

Roflumilast is excreted 70% in the urine as roflumilast N-oxide.A38469

Interaksi Makanan

1 Data
  • 1. Take with or without food. Administering roflumilast with a high-fat meal reduced and delayed the Cmax and Tmax, respectively, but did not impact the AUC of roflumilast or its active metabolite (roflumilast N‐oxide).

Interaksi Obat

1446 Data
Peginterferon alfa-2a The serum concentration of Roflumilast can be increased when it is combined with Peginterferon alfa-2a.
Interferon alfa-n1 The serum concentration of Roflumilast can be increased when it is combined with Interferon alfa-n1.
Interferon alfa-n3 The serum concentration of Roflumilast can be increased when it is combined with Interferon alfa-n3.
Peginterferon alfa-2b The serum concentration of Roflumilast can be increased when it is combined with Peginterferon alfa-2b.
Interferon gamma-1b The serum concentration of Roflumilast can be increased when it is combined with Interferon gamma-1b.
Interferon alfa-2a The serum concentration of Roflumilast can be increased when it is combined with Interferon alfa-2a.
Aldesleukin The serum concentration of Roflumilast can be increased when it is combined with Aldesleukin.
Gemtuzumab ozogamicin Roflumilast may increase the immunosuppressive activities of Gemtuzumab ozogamicin.
Pegaspargase Roflumilast may increase the immunosuppressive activities of Pegaspargase.
Interferon beta-1b The serum concentration of Roflumilast can be increased when it is combined with Interferon beta-1b.
Interferon alfacon-1 The serum concentration of Roflumilast can be increased when it is combined with Interferon alfacon-1.
Trastuzumab Roflumilast may increase the immunosuppressive activities of Trastuzumab.
Rituximab Roflumilast may increase the immunosuppressive activities of Rituximab.
Basiliximab Roflumilast may increase the immunosuppressive activities of Basiliximab.
Muromonab Roflumilast may increase the immunosuppressive activities of Muromonab.
Ibritumomab tiuxetan Roflumilast may increase the immunosuppressive activities of Ibritumomab tiuxetan.
Tositumomab Roflumilast may increase the immunosuppressive activities of Tositumomab.
Alemtuzumab Roflumilast may increase the immunosuppressive activities of Alemtuzumab.
Cyclosporine The serum concentration of Roflumilast can be increased when it is combined with Cyclosporine.
Alefacept Roflumilast may increase the immunosuppressive activities of Alefacept.
Efalizumab Roflumilast may increase the immunosuppressive activities of Efalizumab.
Antithymocyte immunoglobulin (rabbit) Roflumilast may increase the immunosuppressive activities of Antithymocyte immunoglobulin (rabbit).
Interferon alfa-2b The serum concentration of Roflumilast can be increased when it is combined with Interferon alfa-2b.
Natalizumab Roflumilast may increase the immunosuppressive activities of Natalizumab.
Daclizumab Roflumilast may increase the immunosuppressive activities of Daclizumab.
Phenylalanine Roflumilast may increase the immunosuppressive activities of Phenylalanine.
Flunisolide Roflumilast may increase the immunosuppressive activities of Flunisolide.
Bortezomib Roflumilast may increase the immunosuppressive activities of Bortezomib.
Cladribine Roflumilast may increase the immunosuppressive activities of Cladribine.
Carmustine Roflumilast may increase the immunosuppressive activities of Carmustine.
Amsacrine Roflumilast may increase the immunosuppressive activities of Amsacrine.
Bleomycin Roflumilast may increase the immunosuppressive activities of Bleomycin.
Chlorambucil Roflumilast may increase the immunosuppressive activities of Chlorambucil.
Raltitrexed Roflumilast may increase the immunosuppressive activities of Raltitrexed.
Mitomycin Roflumilast may increase the immunosuppressive activities of Mitomycin.
Bexarotene Roflumilast may increase the immunosuppressive activities of Bexarotene.
Vindesine Roflumilast may increase the immunosuppressive activities of Vindesine.
Floxuridine Roflumilast may increase the immunosuppressive activities of Floxuridine.
Indomethacin Roflumilast may increase the immunosuppressive activities of Indomethacin.
Tioguanine Roflumilast may increase the immunosuppressive activities of Tioguanine.
Vinorelbine Roflumilast may increase the immunosuppressive activities of Vinorelbine.
Dexrazoxane Roflumilast may increase the immunosuppressive activities of Dexrazoxane.
Beclomethasone dipropionate Roflumilast may increase the immunosuppressive activities of Beclomethasone dipropionate.
Sorafenib The serum concentration of Roflumilast can be increased when it is combined with Sorafenib.
Streptozocin Roflumilast may increase the immunosuppressive activities of Streptozocin.
Trifluridine Roflumilast may increase the immunosuppressive activities of Trifluridine.
Gemcitabine Roflumilast may increase the immunosuppressive activities of Gemcitabine.
Betamethasone Roflumilast may increase the immunosuppressive activities of Betamethasone.
Teniposide The serum concentration of Roflumilast can be increased when it is combined with Teniposide.
Epirubicin Roflumilast may increase the immunosuppressive activities of Epirubicin.
Chloramphenicol The serum concentration of Roflumilast can be increased when it is combined with Chloramphenicol.
Lenalidomide Roflumilast may increase the immunosuppressive activities of Lenalidomide.
Altretamine Roflumilast may increase the immunosuppressive activities of Altretamine.
Zidovudine Roflumilast may increase the immunosuppressive activities of Zidovudine.
Cisplatin Roflumilast may increase the immunosuppressive activities of Cisplatin.
Oxaliplatin Roflumilast may increase the immunosuppressive activities of Oxaliplatin.
Cyclophosphamide Roflumilast may increase the immunosuppressive activities of Cyclophosphamide.
Vincristine Roflumilast may increase the immunosuppressive activities of Vincristine.
Fluorouracil Roflumilast may increase the immunosuppressive activities of Fluorouracil.
Propylthiouracil Roflumilast may increase the immunosuppressive activities of Propylthiouracil.
Pentostatin Roflumilast may increase the immunosuppressive activities of Pentostatin.
Methotrexate Roflumilast may increase the immunosuppressive activities of Methotrexate.
Carbamazepine The serum concentration of Roflumilast can be increased when it is combined with Carbamazepine.
Vinblastine The serum concentration of Roflumilast can be increased when it is combined with Vinblastine.
Fluticasone propionate The serum concentration of Roflumilast can be increased when it is combined with Fluticasone propionate.
Fluocinolone acetonide Roflumilast may increase the immunosuppressive activities of Fluocinolone acetonide.
Linezolid Roflumilast may increase the immunosuppressive activities of Linezolid.
Imatinib The serum concentration of Roflumilast can be increased when it is combined with Imatinib.
Triamcinolone Roflumilast may increase the immunosuppressive activities of Triamcinolone.
Clofarabine Roflumilast may increase the immunosuppressive activities of Clofarabine.
Prednisone Roflumilast may increase the immunosuppressive activities of Prednisone.
Pemetrexed Roflumilast may increase the immunosuppressive activities of Pemetrexed.
Fludrocortisone Roflumilast may increase the immunosuppressive activities of Fludrocortisone.
Mycophenolate mofetil Roflumilast may increase the immunosuppressive activities of Mycophenolate mofetil.
Daunorubicin The serum concentration of Roflumilast can be increased when it is combined with Daunorubicin.
Hydrocortisone Roflumilast may increase the immunosuppressive activities of Hydrocortisone.
Irinotecan Roflumilast may increase the immunosuppressive activities of Irinotecan.
Methimazole The serum concentration of Roflumilast can be increased when it is combined with Methimazole.
Etoposide The serum concentration of Roflumilast can be increased when it is combined with Etoposide.
Sulfasalazine Roflumilast may increase the immunosuppressive activities of Sulfasalazine.
Dacarbazine Roflumilast may increase the immunosuppressive activities of Dacarbazine.
Temozolomide Roflumilast may increase the immunosuppressive activities of Temozolomide.
Penicillamine Roflumilast may increase the immunosuppressive activities of Penicillamine.
Prednisolone Roflumilast may increase the immunosuppressive activities of Prednisolone.
Tacrolimus The serum concentration of Roflumilast can be increased when it is combined with Tacrolimus.
Sirolimus Roflumilast may increase the immunosuppressive activities of Sirolimus.
Mechlorethamine Roflumilast may increase the immunosuppressive activities of Mechlorethamine.
Azacitidine Roflumilast may increase the immunosuppressive activities of Azacitidine.
Carboplatin Roflumilast may increase the immunosuppressive activities of Carboplatin.
Methylprednisolone Roflumilast may increase the immunosuppressive activities of Methylprednisolone.
Dactinomycin Roflumilast may increase the immunosuppressive activities of Dactinomycin.
Cytarabine Roflumilast may increase the immunosuppressive activities of Cytarabine.
Azathioprine Roflumilast may increase the immunosuppressive activities of Azathioprine.
Doxorubicin The serum concentration of Roflumilast can be increased when it is combined with Doxorubicin.
Hydroxyurea Roflumilast may increase the immunosuppressive activities of Hydroxyurea.
Busulfan Roflumilast may increase the immunosuppressive activities of Busulfan.
Mycophenolic acid Roflumilast may increase the immunosuppressive activities of Mycophenolic acid.
Topotecan The serum concentration of Roflumilast can be increased when it is combined with Topotecan.
Mercaptopurine Roflumilast may increase the immunosuppressive activities of Mercaptopurine.
Thalidomide Roflumilast may increase the immunosuppressive activities of Thalidomide.

Target Protein

cAMP-specific 3',5'-cyclic phosphodiesterase 4 (PDE4) PDE4A

Referensi & Sumber

Synthesis reference: ???, ???, ???, ???, ???, ??, ??, & ???. (2015, March 25). Method for synthesizing roflumilast. CN103012256B.
Artikel (PubMed)
  • PMID: 17699872
    Meyers JA, Taverna J, Chaves J, Makkinje A, Lerner A: Phosphodiesterase 4 inhibitors augment levels of glucocorticoid receptor in B cell chronic lymphocytic leukemia but not in normal circulating hematopoietic cells. Clin Cancer Res. 2007 Aug 15;13(16):4920-7.
  • PMID: 17704822
    Sanz MJ, Cortijo J, Taha MA, Cerda-Nicolas M, Schatton E, Burgbacher B, Klar J, Tenor H, Schudt C, Issekutz AC, Hatzelmann A, Morcillo EJ: Roflumilast inhibits leukocyte-endothelial cell interactions, expression of adhesion molecules and microvascular permeability. Br J Pharmacol. 2007 Oct;152(4):481-92. Epub 2007 Aug 20.
  • PMID: 17726343
    Barone FC, Barton ME, White RF, Legos JJ, Kikkawa H, Shimamura M, Kuratani K, Kinoshita M: Inhibition of phosphodiesterase type 4 decreases stress-induced defecation in rats and mice. Pharmacology. 2008;81(1):11-7. Epub 2007 Aug 28.
  • PMID: 21563134
    Chong J, Poole P, Leung B, Black PN: Phosphodiesterase 4 inhibitors for chronic obstructive pulmonary disease. Cochrane Database Syst Rev. 2011 May 11;(5):CD002309. doi: 10.1002/14651858.CD002309.pub3.
  • PMID: 17573446
    Grootendorst DC, Gauw SA, Verhoosel RM, Sterk PJ, Hospers JJ, Bredenbroker D, Bethke TD, Hiemstra PS, Rabe KF: Reduction in sputum neutrophil and eosinophil numbers by the PDE4 inhibitor roflumilast in patients with COPD. Thorax. 2007 Dec;62(12):1081-7. Epub 2007 Jun 15.
  • PMID: 23280750
    Thappali SR, Varanasi KV, Veeraraghavan S, Vakkalanka SK, Mukkanti K: Simultaneous quantitation of IC87114, roflumilast and its active metabolite roflumilast N-oxide in plasma by LC-MS/MS: application for a pharmacokinetic study. J Mass Spectrom. 2012 Dec;47(12):1612-9. doi: 10.1002/jms.3103.
  • PMID: 20689641
    Giembycz MA, Field SK: Roflumilast: first phosphodiesterase 4 inhibitor approved for treatment of COPD. Drug Des Devel Ther. 2010 Jul 21;4:147-58. doi: 10.2147/dddt.s7667.
  • PMID: 22605906
    Baye J: Roflumilast (daliresp): a novel phosphodiesterase-4 inhibitor for the treatment of severe chronic obstructive pulmonary disease. P T. 2012 Mar;37(3):149-61.

Contoh Produk & Brand

Produk: 43 • International brands: 0
Produk
  • Daliresp
    Tablet, film coated • 500 μg • Oral • EU
  • Daliresp
    Tablet, film coated • 500 μg • Oral • EU
  • Daliresp
    Tablet, film coated • 500 μg • Oral • EU
  • Daliresp
    Tablet • 500 ug/1 • Oral • US • Approved
  • Daliresp
    Tablet • 500 ug/1 • Oral • US • Approved
  • Daliresp
    Tablet • 250 ug/1 • Oral • US • Approved
  • Daliresp
    Tablet • 500 ug/1 • Oral • US • Approved
  • Daxas
    Tablet • 250 ?g • Oral • EU • Approved
Menampilkan 8 dari 43 produk.

Sekuens Gen/Protein (FASTA)

Sekuens dimuat saat dibutuhkan agar halaman tetap ringan.
© 2025 Digital Pharmacy Research - Universitas Esa Unggul