Peringatan Keamanan

Fluticasone furoate administered nasally may be associated with adrenal suppression or an increase in QTc interval though the association has not been well demonstrated in studies.L40838,L44456,L46481,A7488 Fluticasone furoate requires no dosage adjustment in renal impairment but must be used with caution in hepatic impairment due to the elimination mechanisms.L40838,L44456,L46481 Fluticasone furoate is not associated with carcinogenicity, mutagenicity, or impairment of fertility.L40838,L44456,L46481 There are no well-controlled studies in pregnancy or lactation though animal studies have shown teratogenicity and hypoadrenalism in the offspring of treated mothers and other corticosteroids are known to be excreted in breast milkFDA Label. Generally, there are no reported adverse effects with fluticasone in pregnancy.A177127 Pediatric patients should be given the lowest possible dose and monitored for a reduction in growth velocity.L40838,L44456,L46481,A7488 There is insufficient evidence to determine whether geriatric patients respond differently to other patients.L40838,L44456,L46481 Systemic exposure may be 27-49% higher in Japanese, Korean, and Chinese patients compared to Caucasian patients.L40838,L44456,L46481 Caution should be exercised in these patients and the benefit and risk should be assessed before deciding on a treatment.L40838,L44456,L46481

Fluticasone furoate

DB08906

small molecule approved

Deskripsi

Fluticasone furoate is a synthetic glucocorticoid available as an inhaler and nasal spray for various inflammatory indicationsFDA LabelF4364. Fluticasone furoate was first approved in 2007L5965.

Struktur Molekul 2D

Berat 538.576
Wujud solid

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

Profil Farmakokinetik

Waktu Paruh (Half-Life) Following repeat-dose inhaled administration, the plasma elimination phase half-life averaged 24 hours.[L40838,L44456,L46481] A study of 24 healthy Caucasian males showed a half-life of 13.6 hours following intravenous administration and 17.3-23.9 hours following inhalation.[A7490]
Volume Distribusi Following intravenous administration to healthy subjects, the mean volume of distribution at steady state was 661 L.[L40838,L44456,L46481] A study of 24 healthy Caucasian males showed a volume of distribution at steady state of 704L following intravenous administration.[A7490]
Klirens (Clearance) Following intravenous administration to healthy subjects, fluticasone furoate was cleared from systemic circulation principally by hepatic metabolism via CYP3A4 with a total plasma clearance of 65.4 L/hr.[L46606] A study of 24 healthy Caucasian males also showed a clearance of 71.8L/h following intravenous administration.[A7490]

Absorpsi

Fluticasone furoate plasma levels may not predict therapeutic effect. Peak plasma concentrations are reached within 0.5 to 1 hour. Absolute bioavailability of fluticasone furoate when administrated by inhalation was 13.9%, primarily due to absorption of the inhaled portion of the dose delivered to the lung. Oral bioavailability from the swallowed portion of the dose is low (approximately 1.3%) due to extensive first-pass metabolism. Systemic exposure (AUC) in subjects with asthma was 26% lower than observed in healthy subjects.L40838 Following repeat dosing of inhaled fluticasone furoate, steady state was achieved within 6 days with up to 2.6-fold accumulation.L44456 Intranasal exposure of fluticasone furoate also results in patients swallowing a larger portion of the dose.A177118

Metabolisme

Fluticasone furoate is cleared from systemic circulation principally by hepatic metabolism via CYP3A4 to metabolites with significantly reduced corticosteroid activity. There was no in vivo evidence for cleavage of the furoate moiety resulting in the formation of fluticasone.L40838,L44456,L46481,A177121 Fluticasone furoate is also hydrolyzed at the FIVE-S-fluoromethyl carbothioate group, forming an inactive metabolite.A177118

Rute Eliminasi

Following intravenous dosing with radiolabeled fluticasone furoate, mass balance showed 90% of radiolabel in the feces and 2% in the urine. Following oral dosing, radiolabel recovered in feces was 101% of the total dose, and that in urine was approximately 1% of the total dose.L44456

Interaksi Obat

1231 Data
Denosumab The risk or severity of adverse effects can be increased when Denosumab is combined with Fluticasone furoate.
Peginterferon alfa-2a The risk or severity of adverse effects can be increased when Peginterferon alfa-2a is combined with Fluticasone furoate.
Interferon alfa-n1 The risk or severity of adverse effects can be increased when Interferon alfa-n1 is combined with Fluticasone furoate.
Interferon alfa-n3 The risk or severity of adverse effects can be increased when Interferon alfa-n3 is combined with Fluticasone furoate.
Peginterferon alfa-2b The risk or severity of adverse effects can be increased when Peginterferon alfa-2b is combined with Fluticasone furoate.
Interferon gamma-1b The risk or severity of adverse effects can be increased when Interferon gamma-1b is combined with Fluticasone furoate.
Interferon alfa-2a The risk or severity of adverse effects can be increased when Interferon alfa-2a is combined with Fluticasone furoate.
Gemtuzumab ozogamicin The risk or severity of adverse effects can be increased when Gemtuzumab ozogamicin is combined with Fluticasone furoate.
Pegaspargase The serum concentration of Fluticasone furoate can be increased when it is combined with Pegaspargase.
Interferon beta-1b The risk or severity of adverse effects can be increased when Interferon beta-1b is combined with Fluticasone furoate.
Interferon alfacon-1 The risk or severity of adverse effects can be increased when Interferon alfacon-1 is combined with Fluticasone furoate.
Rituximab The risk or severity of adverse effects can be increased when Rituximab is combined with Fluticasone furoate.
Basiliximab The risk or severity of adverse effects can be increased when Basiliximab is combined with Fluticasone furoate.
Muromonab The risk or severity of adverse effects can be increased when Muromonab is combined with Fluticasone furoate.
Ibritumomab tiuxetan The risk or severity of adverse effects can be increased when Ibritumomab tiuxetan is combined with Fluticasone furoate.
Tositumomab The risk or severity of adverse effects can be increased when Tositumomab is combined with Fluticasone furoate.
Alemtuzumab The risk or severity of adverse effects can be increased when Alemtuzumab is combined with Fluticasone furoate.
Alefacept The risk or severity of adverse effects can be increased when Alefacept is combined with Fluticasone furoate.
Efalizumab The risk or severity of adverse effects can be increased when Efalizumab is combined with Fluticasone furoate.
Antithymocyte immunoglobulin (rabbit) The risk or severity of adverse effects can be increased when Antithymocyte immunoglobulin (rabbit) is combined with Fluticasone furoate.
Interferon alfa-2b The risk or severity of adverse effects can be increased when Interferon alfa-2b is combined with Fluticasone furoate.
Daclizumab The risk or severity of adverse effects can be increased when Daclizumab is combined with Fluticasone furoate.
Phenylalanine The risk or severity of adverse effects can be increased when Phenylalanine is combined with Fluticasone furoate.
Cladribine Fluticasone furoate may increase the immunosuppressive activities of Cladribine.
Carmustine The risk or severity of adverse effects can be increased when Carmustine is combined with Fluticasone furoate.
Amsacrine The risk or severity of adverse effects can be increased when Amsacrine is combined with Fluticasone furoate.
Bleomycin The risk or severity of adverse effects can be increased when Bleomycin is combined with Fluticasone furoate.
Chlorambucil The risk or severity of adverse effects can be increased when Chlorambucil is combined with Fluticasone furoate.
Raltitrexed The risk or severity of adverse effects can be increased when Raltitrexed is combined with Fluticasone furoate.
Mitomycin The risk or severity of adverse effects can be increased when Mitomycin is combined with Fluticasone furoate.
Bexarotene The risk or severity of adverse effects can be increased when Bexarotene is combined with Fluticasone furoate.
Floxuridine The risk or severity of adverse effects can be increased when Floxuridine is combined with Fluticasone furoate.
Tioguanine The risk or severity of adverse effects can be increased when Tioguanine is combined with Fluticasone furoate.
Dexrazoxane The risk or severity of adverse effects can be increased when Dexrazoxane is combined with Fluticasone furoate.
Streptozocin The risk or severity of adverse effects can be increased when Streptozocin is combined with Fluticasone furoate.
Trifluridine The risk or severity of adverse effects can be increased when Trifluridine is combined with Fluticasone furoate.
Gemcitabine The risk or severity of adverse effects can be increased when Gemcitabine is combined with Fluticasone furoate.
Epirubicin The risk or severity of adverse effects can be increased when Epirubicin is combined with Fluticasone furoate.
Chloramphenicol The serum concentration of Fluticasone furoate can be increased when it is combined with Chloramphenicol.
Lenalidomide The risk or severity of adverse effects can be increased when Lenalidomide is combined with Fluticasone furoate.
Altretamine The risk or severity of adverse effects can be increased when Altretamine is combined with Fluticasone furoate.
Zidovudine The risk or severity of adverse effects can be increased when Zidovudine is combined with Fluticasone furoate.
Oxaliplatin The risk or severity of adverse effects can be increased when Oxaliplatin is combined with Fluticasone furoate.
Propylthiouracil The risk or severity of adverse effects can be increased when Propylthiouracil is combined with Fluticasone furoate.
Pentostatin The risk or severity of adverse effects can be increased when Pentostatin is combined with Fluticasone furoate.
Linezolid The risk or severity of adverse effects can be increased when Linezolid is combined with Fluticasone furoate.
Clofarabine The risk or severity of adverse effects can be increased when Clofarabine is combined with Fluticasone furoate.
Pemetrexed The risk or severity of adverse effects can be increased when Pemetrexed is combined with Fluticasone furoate.
Mycophenolate mofetil The risk or severity of adverse effects can be increased when Mycophenolate mofetil is combined with Fluticasone furoate.
Tretinoin The metabolism of Fluticasone furoate can be decreased when combined with Tretinoin.
Dacarbazine The risk or severity of adverse effects can be increased when Dacarbazine is combined with Fluticasone furoate.
Temozolomide The risk or severity of adverse effects can be increased when Temozolomide is combined with Fluticasone furoate.
Penicillamine The risk or severity of adverse effects can be increased when Penicillamine is combined with Fluticasone furoate.
Azacitidine The risk or severity of adverse effects can be increased when Azacitidine is combined with Fluticasone furoate.
Carboplatin The risk or severity of adverse effects can be increased when Carboplatin is combined with Fluticasone furoate.
Dactinomycin The risk or severity of adverse effects can be increased when Dactinomycin is combined with Fluticasone furoate.
Azathioprine The risk or severity of adverse effects can be increased when Azathioprine is combined with Fluticasone furoate.
Hydroxyurea The risk or severity of adverse effects can be increased when Hydroxyurea is combined with Fluticasone furoate.
Mycophenolic acid The risk or severity of adverse effects can be increased when Mycophenolic acid is combined with Fluticasone furoate.
Topotecan The serum concentration of Fluticasone furoate can be increased when it is combined with Topotecan.
Mercaptopurine The risk or severity of adverse effects can be increased when Mercaptopurine is combined with Fluticasone furoate.
Thalidomide The risk or severity of adverse effects can be increased when Thalidomide is combined with Fluticasone furoate.
Melphalan The risk or severity of adverse effects can be increased when Melphalan is combined with Fluticasone furoate.
Fludarabine The risk or severity of adverse effects can be increased when Fludarabine is combined with Fluticasone furoate.
Flucytosine The risk or severity of adverse effects can be increased when Flucytosine is combined with Fluticasone furoate.
Capecitabine The risk or severity of adverse effects can be increased when Capecitabine is combined with Fluticasone furoate.
Procarbazine The risk or severity of adverse effects can be increased when Procarbazine is combined with Fluticasone furoate.
Arsenic trioxide The risk or severity of adverse effects can be increased when Arsenic trioxide is combined with Fluticasone furoate.
Idarubicin The risk or severity of adverse effects can be increased when Idarubicin is combined with Fluticasone furoate.
Estramustine The risk or severity of adverse effects can be increased when Estramustine is combined with Fluticasone furoate.
Mitoxantrone The risk or severity of adverse effects can be increased when Mitoxantrone is combined with Fluticasone furoate.
Lomustine The risk or severity of adverse effects can be increased when Lomustine is combined with Fluticasone furoate.
Eculizumab The risk or severity of adverse effects can be increased when Eculizumab is combined with Fluticasone furoate.
Decitabine The risk or severity of adverse effects can be increased when Decitabine is combined with Fluticasone furoate.
Nelarabine The risk or severity of adverse effects can be increased when Nelarabine is combined with Fluticasone furoate.
Stepronin The risk or severity of adverse effects can be increased when Stepronin is combined with Fluticasone furoate.
Hydroxychloroquine The risk or severity of adverse effects can be increased when Hydroxychloroquine is combined with Fluticasone furoate.
Castanospermine The risk or severity of adverse effects can be increased when Castanospermine is combined with Fluticasone furoate.
Vorinostat The risk or severity of adverse effects can be increased when Vorinostat is combined with Fluticasone furoate.
2-Methoxyethanol The risk or severity of adverse effects can be increased when 2-Methoxyethanol is combined with Fluticasone furoate.
Brequinar The risk or severity of adverse effects can be increased when Brequinar is combined with Fluticasone furoate.
Pirfenidone The risk or severity of adverse effects can be increased when Pirfenidone is combined with Fluticasone furoate.
Interferon alfa The risk or severity of adverse effects can be increased when Interferon alfa is combined with Fluticasone furoate.
Glatiramer The risk or severity of adverse effects can be increased when Glatiramer is combined with Fluticasone furoate.
Briakinumab The risk or severity of adverse effects can be increased when Briakinumab is combined with Fluticasone furoate.
Human interferon omega-1 The risk or severity of adverse effects can be increased when Human interferon omega-1 is combined with Fluticasone furoate.
Mepolizumab The risk or severity of adverse effects can be increased when Mepolizumab is combined with Fluticasone furoate.
Abetimus The risk or severity of adverse effects can be increased when Abetimus is combined with Fluticasone furoate.
Belatacept The risk or severity of adverse effects can be increased when Belatacept is combined with Fluticasone furoate.
Bendamustine The risk or severity of adverse effects can be increased when Bendamustine is combined with Fluticasone furoate.
Pralatrexate The risk or severity of adverse effects can be increased when Pralatrexate is combined with Fluticasone furoate.
Wortmannin The risk or severity of adverse effects can be increased when Wortmannin is combined with Fluticasone furoate.
Eribulin The risk or severity of adverse effects can be increased when Eribulin is combined with Fluticasone furoate.
Belimumab The risk or severity of adverse effects can be increased when Belimumab is combined with Fluticasone furoate.
Teriflunomide The risk or severity of adverse effects can be increased when Teriflunomide is combined with Fluticasone furoate.
Carfilzomib The risk or severity of adverse effects can be increased when Carfilzomib is combined with Fluticasone furoate.
Dimethyl fumarate The risk or severity of adverse effects can be increased when Fluticasone furoate is combined with Dimethyl fumarate.
Obinutuzumab The risk or severity of adverse effects can be increased when Fluticasone furoate is combined with Obinutuzumab.
Vedolizumab The risk or severity of adverse effects can be increased when Fluticasone furoate is combined with Vedolizumab.
Blinatumomab The risk or severity of adverse effects can be increased when Fluticasone furoate is combined with Blinatumomab.

Target Protein

Glucocorticoid receptor NR3C1
Progesterone receptor PGR
Mineralocorticoid receptor NR3C2

Referensi & Sumber

Synthesis reference: Adrienne KOVACSNE-MEZEI, Roman Gabriel, Alexandr Jegorov, "POLYMORPHS OF FLUTICASONE FUROATE AND PROCESSES FOR PREPARATION THEREOF." U.S. Patent US20100240629, issued September 23, 2010.
Artikel (PubMed)
  • PMID: 2287791
    Phillipps GH: Structure-activity relationships of topically active steroids: the selection of fluticasone propionate. Respir Med. 1990 Nov;84 Suppl A:19-23.
  • PMID: 2287792
    Harding SM: The human pharmacology of fluticasone propionate. Respir Med. 1990 Nov;84 Suppl A:25-9.
  • PMID: 18047814
    Choi JS, Han JY, Kim MY, Velazquez-Armenta EY, Nava-Ocampo AA: Pregnancy outcomes in women using inhaled fluticasone during pregnancy: a case series. Allergol Immunopathol (Madr). 2007 Nov-Dec;35(6):239-42.
  • PMID: 28587510
    Spadijer Mirkovic C, Peric A, Vukomanovic Durdevic B, Vojvodic D: Effects of Fluticasone Furoate Nasal Spray on Parameters of Eosinophilic Inflammation in Patients With Nasal Polyposis and Perennial Allergic Rhinitis. Ann Otol Rhinol Laryngol. 2017 Aug;126(8):573-580. doi: 10.1177/0003489417713505. Epub 2017 Jun 6.
  • PMID: 23184737
    Allen A, Bareille PJ, Rousell VM: Fluticasone furoate, a novel inhaled corticosteroid, demonstrates prolonged lung absorption kinetics in man compared with inhaled fluticasone propionate. Clin Pharmacokinet. 2013 Jan;52(1):37-42. doi: 10.1007/s40262-012-0021-x.
  • PMID: 23578031
    Allen A, Schenkenberger I, Trivedi R, Cole J, Hicks W, Gul N, Jacques L: Inhaled fluticasone furoate/vilanterol does not affect hypothalamic-pituitary-adrenal axis function in adolescent and adult asthma: randomised, double-blind, placebo-controlled study. Clin Respir J. 2013 Oct;7(4):397-406. doi: 10.1111/crj.12026. Epub 2013 Jun 5.

Contoh Produk & Brand

Produk: 57 • International brands: 1
Produk
  • Alisade
    Spray, suspension • 27.5 micrograms/spray • Intrasinal • EU
  • Alisade
    Spray, suspension • 27.5 micrograms/spray • Intrasinal • EU
  • Alisade
    Spray, suspension • 27.5 micrograms/spray • Intrasinal • EU
  • Arnuity Ellipta
    Powder • 50 ug/1 • Respiratory (inhalation) • US • Approved
  • Arnuity Ellipta
    Powder • 100 ug/1 • Respiratory (inhalation) • US • Approved
  • Arnuity Ellipta
    Powder • 200 ug/1 • Respiratory (inhalation) • US • Approved
  • Arnuity Ellipta
    Powder • 100 mcg / act • Respiratory (inhalation) • Canada • Approved
  • Arnuity Ellipta
    Powder • 200 mcg / act • Respiratory (inhalation) • Canada • Approved
Menampilkan 8 dari 57 produk.
International Brands
  • Veramyst

Sekuens Gen/Protein (FASTA)

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