Peringatan Keamanan

Fluticasone propionate's use in specific populations has not been well studiedF4358. Fluticasone propionate is not carcinogenic, mutagenic, or clastogenic, nor did it affect fertility in animal studiesF4358FDA Label. Subcutaneous fluticasone propionate has been shown to produce teratogenic effects in rats though oral administration does notF4355FDA Label. Generally, there are no reported adverse effects with fluticasone in pregnancyA177127. Fluticasone propionate in human milk may cause growth suppression, effects on endogenous corticosteroid production, or other effectsF4355,A7488. Pediatric patients treated with fluticasone propionate ointment experienced adrenal suppressionF4355. Geriatric patients treated with fluticasone propionate did not show any difference in safety or efficacy compared to other patient groups, though older patients may be more sensitive to adverse effectsF4355. There is no difference in the clearance of fluticasone propionate across genders or raceFDA Label. Patients with hepatic impairment should be closely monitored due to the elimination mechanismFDA LabelA176918.

Fluticasone propionate

DB00588

small molecule approved

Deskripsi

Fluticasone propionate is a synthetic glucocorticoidF4355,F4358FDA Label. These drugs are available as inhalers, nasal, sprays, and topical treatments for various inflammatory indicationsF4355,F4358FDA Label. Fluticasone propionate was first approved in 1990L5962.

Struktur Molekul 2D

Berat 500.571
Wujud solid

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

Profil Farmakokinetik

Waktu Paruh (Half-Life) 7.8 hours for intravenous fluticasone propionate[F4358][FDA Label]. A study of 24 healthy Caucasian males shows a half life of 14.0 hours following intravenous administration and 10.8 hours following inhalation[A7490].
Volume Distribusi The volume of distribution of intravenous fluticasone propionate is 4.2L/kg[F4358][FDA Label]. A study of 24 healthy Caucasian males showed a volume of distribution at steady state of 577L following intravenous administration[A7490].
Klirens (Clearance) 1093mL/min for fluticasone propionate[F4358]. A study of 24 healthy Caucasian males showed a clearance of 63.9L/h following intravenous administration[A7490].

Absorpsi

Intranasal bioavailability of fluticasone propionate is <2%, and oral bioavailability is <1%F4358FDA Label. Intranasal exposure results in the majority of the dose being swallowedA177118. Topical absorption of fluticasone propionate is very low but can change depending on a number of factors including integrity of the skin and the presence of inflammation or diseaseF4355. A study of 24 healthy Caucasian males showed an inhaled bioavailability of 9.0%A7490.

Metabolisme

Fluticasone propionate is cleared from hepatic metabolism by cytochrome P450 3A4F4358,A177121FDA Label. Fluticasone propionate is hydrolysed at the FIVE-S-fluoromethyl carbothioate group, forming an inactive metaboliteF4355,A177118FDA Label.

Rute Eliminasi

Fluticasone propionate is mainly eliminated in the feces with <5% eliminated in the urineF4358,A176918FDA Label.

Interaksi Obat

1796 Data
Denosumab The risk or severity of adverse effects can be increased when Denosumab is combined with Fluticasone propionate.
Peginterferon alfa-2a The risk or severity of adverse effects can be increased when Peginterferon alfa-2a is combined with Fluticasone propionate.
Interferon alfa-n1 The risk or severity of adverse effects can be increased when Interferon alfa-n1 is combined with Fluticasone propionate.
Interferon alfa-n3 The risk or severity of adverse effects can be increased when Interferon alfa-n3 is combined with Fluticasone propionate.
Peginterferon alfa-2b The risk or severity of adverse effects can be increased when Peginterferon alfa-2b is combined with Fluticasone propionate.
Interferon gamma-1b The risk or severity of adverse effects can be increased when Interferon gamma-1b is combined with Fluticasone propionate.
Interferon alfa-2a The risk or severity of adverse effects can be increased when Interferon alfa-2a is combined with Fluticasone propionate.
Aldesleukin The therapeutic efficacy of Aldesleukin can be decreased when used in combination with Fluticasone propionate.
Gemtuzumab ozogamicin The risk or severity of adverse effects can be increased when Gemtuzumab ozogamicin is combined with Fluticasone propionate.
Pegaspargase The serum concentration of Fluticasone propionate 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 propionate.
Interferon alfacon-1 The risk or severity of adverse effects can be increased when Interferon alfacon-1 is combined with Fluticasone propionate.
Rituximab The risk or severity of adverse effects can be increased when Rituximab is combined with Fluticasone propionate.
Basiliximab The risk or severity of adverse effects can be increased when Basiliximab is combined with Fluticasone propionate.
Muromonab The risk or severity of adverse effects can be increased when Muromonab is combined with Fluticasone propionate.
Ibritumomab tiuxetan The risk or severity of adverse effects can be increased when Ibritumomab tiuxetan is combined with Fluticasone propionate.
Tositumomab The risk or severity of adverse effects can be increased when Tositumomab is combined with Fluticasone propionate.
Alemtuzumab The risk or severity of adverse effects can be increased when Alemtuzumab is combined with Fluticasone propionate.
Alefacept The risk or severity of adverse effects can be increased when Alefacept is combined with Fluticasone propionate.
Efalizumab The risk or severity of adverse effects can be increased when Efalizumab is combined with Fluticasone propionate.
Antithymocyte immunoglobulin (rabbit) The risk or severity of adverse effects can be increased when Antithymocyte immunoglobulin (rabbit) is combined with Fluticasone propionate.
Interferon alfa-2b The risk or severity of adverse effects can be increased when Interferon alfa-2b is combined with Fluticasone propionate.
Daclizumab The risk or severity of adverse effects can be increased when Daclizumab is combined with Fluticasone propionate.
Phenylalanine The risk or severity of adverse effects can be increased when Phenylalanine is combined with Fluticasone propionate.
Cladribine Fluticasone propionate may increase the immunosuppressive activities of Cladribine.
Carmustine The risk or severity of adverse effects can be increased when Carmustine is combined with Fluticasone propionate.
Amsacrine The risk or severity of adverse effects can be increased when Amsacrine is combined with Fluticasone propionate.
Bleomycin The risk or severity of adverse effects can be increased when Bleomycin is combined with Fluticasone propionate.
Chlorambucil The risk or severity of adverse effects can be increased when Chlorambucil is combined with Fluticasone propionate.
Raltitrexed The risk or severity of adverse effects can be increased when Raltitrexed is combined with Fluticasone propionate.
Mitomycin The risk or severity of adverse effects can be increased when Mitomycin is combined with Fluticasone propionate.
Bexarotene The risk or severity of adverse effects can be increased when Bexarotene is combined with Fluticasone propionate.
Floxuridine The risk or severity of adverse effects can be increased when Floxuridine is combined with Fluticasone propionate.
Tioguanine The risk or severity of adverse effects can be increased when Tioguanine is combined with Fluticasone propionate.
Dexrazoxane The risk or severity of adverse effects can be increased when Dexrazoxane is combined with Fluticasone propionate.
Streptozocin The risk or severity of adverse effects can be increased when Streptozocin is combined with Fluticasone propionate.
Trifluridine The risk or severity of adverse effects can be increased when Trifluridine is combined with Fluticasone propionate.
Gemcitabine The risk or severity of adverse effects can be increased when Gemcitabine is combined with Fluticasone propionate.
Epirubicin The risk or severity of adverse effects can be increased when Epirubicin is combined with Fluticasone propionate.
Chloramphenicol The risk or severity of adverse effects can be increased when Chloramphenicol is combined with Fluticasone propionate.
Lenalidomide The risk or severity of adverse effects can be increased when Lenalidomide is combined with Fluticasone propionate.
Altretamine The risk or severity of adverse effects can be increased when Altretamine is combined with Fluticasone propionate.
Zidovudine The risk or severity of adverse effects can be increased when Zidovudine is combined with Fluticasone propionate.
Oxaliplatin The risk or severity of adverse effects can be increased when Oxaliplatin is combined with Fluticasone propionate.
Propylthiouracil The risk or severity of adverse effects can be increased when Propylthiouracil is combined with Fluticasone propionate.
Pentostatin The risk or severity of adverse effects can be increased when Pentostatin is combined with Fluticasone propionate.
Linezolid The risk or severity of adverse effects can be increased when Fluticasone propionate is combined with Linezolid.
Clofarabine The risk or severity of adverse effects can be increased when Fluticasone propionate is combined with Clofarabine.
Pemetrexed The risk or severity of adverse effects can be increased when Fluticasone propionate is combined with Pemetrexed.
Mycophenolate mofetil The risk or severity of adverse effects can be increased when Fluticasone propionate is combined with Mycophenolate mofetil.
Tretinoin The metabolism of Tretinoin can be decreased when combined with Fluticasone propionate.
Dacarbazine The risk or severity of adverse effects can be increased when Fluticasone propionate is combined with Dacarbazine.
Temozolomide The risk or severity of adverse effects can be increased when Fluticasone propionate is combined with Temozolomide.
Penicillamine The risk or severity of adverse effects can be increased when Fluticasone propionate is combined with Penicillamine.
Azacitidine The risk or severity of adverse effects can be increased when Fluticasone propionate is combined with Azacitidine.
Carboplatin The risk or severity of adverse effects can be increased when Fluticasone propionate is combined with Carboplatin.
Dactinomycin The risk or severity of adverse effects can be increased when Fluticasone propionate is combined with Dactinomycin.
Azathioprine The risk or severity of adverse effects can be increased when Fluticasone propionate is combined with Azathioprine.
Hydroxyurea The risk or severity of adverse effects can be increased when Fluticasone propionate is combined with Hydroxyurea.
Mycophenolic acid The risk or severity of adverse effects can be increased when Fluticasone propionate is combined with Mycophenolic acid.
Topotecan The risk or severity of adverse effects can be increased when Fluticasone propionate is combined with Topotecan.
Mercaptopurine The risk or severity of adverse effects can be increased when Fluticasone propionate is combined with Mercaptopurine.
Melphalan The risk or severity of adverse effects can be increased when Fluticasone propionate is combined with Melphalan.
Fludarabine The risk or severity of adverse effects can be increased when Fluticasone propionate is combined with Fludarabine.
Flucytosine The risk or severity of adverse effects can be increased when Fluticasone propionate is combined with Flucytosine.
Capecitabine The risk or severity of adverse effects can be increased when Fluticasone propionate is combined with Capecitabine.
Procarbazine The risk or severity of adverse effects can be increased when Fluticasone propionate is combined with Procarbazine.
Arsenic trioxide The risk or severity of adverse effects can be increased when Fluticasone propionate is combined with Arsenic trioxide.
Idarubicin The risk or severity of adverse effects can be increased when Fluticasone propionate is combined with Idarubicin.
Estramustine The risk or severity of adverse effects can be increased when Fluticasone propionate is combined with Estramustine.
Mitoxantrone The risk or severity of adverse effects can be increased when Fluticasone propionate is combined with Mitoxantrone.
Lomustine The risk or severity of adverse effects can be increased when Fluticasone propionate is combined with Lomustine.
Eculizumab The risk or severity of adverse effects can be increased when Fluticasone propionate is combined with Eculizumab.
Decitabine The risk or severity of adverse effects can be increased when Fluticasone propionate is combined with Decitabine.
Nelarabine The risk or severity of adverse effects can be increased when Fluticasone propionate is combined with Nelarabine.
Stepronin The risk or severity of adverse effects can be increased when Fluticasone propionate is combined with Stepronin.
Hydroxychloroquine The risk or severity of adverse effects can be increased when Fluticasone propionate is combined with Hydroxychloroquine.
Castanospermine The risk or severity of adverse effects can be increased when Fluticasone propionate is combined with Castanospermine.
Vorinostat The risk or severity of adverse effects can be increased when Fluticasone propionate is combined with Vorinostat.
2-Methoxyethanol The risk or severity of adverse effects can be increased when Fluticasone propionate is combined with 2-Methoxyethanol.
Brequinar The risk or severity of adverse effects can be increased when Fluticasone propionate is combined with Brequinar.
Pirfenidone The risk or severity of adverse effects can be increased when Fluticasone propionate is combined with Pirfenidone.
Interferon alfa The risk or severity of adverse effects can be increased when Fluticasone propionate is combined with Interferon alfa.
Glatiramer The risk or severity of adverse effects can be increased when Fluticasone propionate is combined with Glatiramer.
Briakinumab The risk or severity of adverse effects can be increased when Fluticasone propionate is combined with Briakinumab.
Human interferon omega-1 The risk or severity of adverse effects can be increased when Fluticasone propionate is combined with Human interferon omega-1.
Mepolizumab The risk or severity of adverse effects can be increased when Fluticasone propionate is combined with Mepolizumab.
Abetimus The risk or severity of adverse effects can be increased when Fluticasone propionate is combined with Abetimus.
Belatacept The risk or severity of adverse effects can be increased when Fluticasone propionate is combined with Belatacept.
Bendamustine The risk or severity of adverse effects can be increased when Fluticasone propionate is combined with Bendamustine.
Pralatrexate The risk or severity of adverse effects can be increased when Fluticasone propionate is combined with Pralatrexate.
Wortmannin The risk or severity of adverse effects can be increased when Fluticasone propionate is combined with Wortmannin.
Eribulin The risk or severity of adverse effects can be increased when Fluticasone propionate is combined with Eribulin.
Belimumab The risk or severity of adverse effects can be increased when Fluticasone propionate is combined with Belimumab.
Teriflunomide The risk or severity of adverse effects can be increased when Fluticasone propionate is combined with Teriflunomide.
Carfilzomib The risk or severity of adverse effects can be increased when Fluticasone propionate is combined with Carfilzomib.
Dimethyl fumarate The risk or severity of adverse effects can be increased when Fluticasone propionate is combined with Dimethyl fumarate.
Obinutuzumab The risk or severity of adverse effects can be increased when Fluticasone propionate is combined with Obinutuzumab.
Vedolizumab The risk or severity of adverse effects can be increased when Fluticasone propionate is combined with Vedolizumab.
Blinatumomab The risk or severity of adverse effects can be increased when Fluticasone propionate is combined with Blinatumomab.

Target Protein

Glucocorticoid receptor NR3C1
Progesterone receptor PGR
Cytosolic phospholipase A2 PLA2G4A
Mineralocorticoid receptor NR3C2

Referensi & Sumber

Synthesis reference: Joseph Kaspi, Oded Arad, Michael Brand, Moty Shookrun, Simona Malka, Mohammed Alnabari, Shalom Hazan, Vlado Malesevic, "Synthesis and powder preparation of fluticasone propionate." U.S. Patent US20060009435, issued January 12, 2006.
Artikel (PubMed)
  • 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.
  • 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: 11589253
    Crim C, Pierre LN, Daley-Yates PT: A review of the pharmacology and pharmacokinetics of inhaled fluticasone propionate and mometasone furoate. Clin Ther. 2001 Sep;23(9):1339-54.
  • 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.

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Sekuens Gen/Protein (FASTA)

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