Peringatan Keamanan

DB08906 administered nasally may be associated with adrenal suppression or an increase in QTc interval though the association has not been well demonstrated in studiesF4361,A7488. DB08906 requires no dosage adjustment in renal impairment but must be used in caution in hepatic impairment due to the elimination mechanismsF4361,F4364. DB08906 is not associated with carcinogenicity, mutagenicity, or impairment of fertilityF4361. 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 milkF4361. Generally, there are no reported adverse effects with fluticasone in pregnancyA177127. Pediatric patients should be given the lowest possible dose and monitored for reduction in growth velocityF4361,A7488. There is insufficient evidence to determine whether geriatric patients respond differently to other patientsF4361. Systemic exposure may be 27-49% higher in Japanese, Korean, and Chinese patients compared to Caucasian patientsF4364. Caution should be exercised in these patients and the benefit and risk should be assessed before deciding on a treatmentF4361.

DB00588's use in specific populations has not been well studiedF4358. DB00588 is not carcinogenic, mutagenic, or clastogenic, nor did it affect fertility in animal studiesF4358FDA Label. Subcutaneous DB00588 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. DB00588 in human milk may cause growth suppression, effects on endogenous corticosteroid production, or other effectsF4355,A7488. Pediatric patients treated with DB00588 ointment experienced adrenal suppressionF4355. Geriatric patients treated with DB00588 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 DB00588 across genders or raceFDA Label. Patients with hepatic impairment should be closely monitored due to the elimination mechanismFDA LabelA176918.

Fluticasone

DB13867

small molecule approved experimental

Deskripsi

Fluticasone is a synthetic glucocorticoid available as 2 esters, DB08906 and DB00588F4355,F4358,F4361,F4364FDA Label. These drugs are available as inhalers, nasal, sprays, and topical treatments for various inflammatory indicationsF4355,F4358,F4361,F4364FDA Label. DB00588 was first approved in 1990L5962 and DB08906 was approved in 2007L5965.

Struktur Molekul 2D

Berat 444.51
Wujud solid

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

Profil Farmakokinetik

Waktu Paruh (Half-Life) 15.1 hours for intranasal [DB08906][F4361] and 24 hours for the inhaled formulation[F4364]. A study of 24 healthy Caucasian males showed a half life of 13.6 hours following intravenous administration and 17.3-23.9 hours followed inhalation[A7490]. 7.8 hours for intravenous [DB00588][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 608L at steady state for intravenous administration of [DB08906][F4361]. Other reports suggest the mean volume of distribution at steady state is 661L[F4364]. A study of 24 healthy Caucasian males showed a volume of distribution at steady state of 704L following intravenous administration[A7490]. The volume of distribution of intravenous [DB00588] 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) 57.8L/h for [DB08906][F4361]. A study of 24 healthy Caucasian males showed a clearance of 71.8L/h following intravenous administration[A7490]. 1093mL/min for [DB00588][F4358]. A study of 24 healthy Caucasian males showed a clearance of 63.9L/h following intravenous administration[A7490].

Absorpsi

Intranasal exposure of DB08906 results in patients swallowing a larger portion of the doseF4361,A177118. However, absorption is poor and metabolism is high, therefore there is negligible systemic exposure with a nasal bioavailability of 0.50% and oral bioavialability of 1.26%F4361,A7490. Inhaled bioavailability is 13.9%F4364. A study of 24 healthy Caucasian males showed an inhaled bioavailability of 6.3-18.4%A7490. Intranasal bioavailability of DB00588 is <2%, and oral bioavailability is <1%F4358FDA Label. Intranasal exposure results in the majority of the dose being swallowedA177118. Topical absorption of DB00588 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

DB08906 and DB00588 are cleared from hepatic metabolism by cytochrome P450 3A4F4361,F4364,F4358,A177121FDA Label. Both are hydrolysed at the FIVE-S-fluoromethyl carbothioate group, forming an inactive metaboliteF4361,F4355,A177118FDA Label.

Rute Eliminasi

DB08906 is eliminated ?90% in the feces and 1-2% in the urineF4361,F4364. DB00588 is mainly eliminated in the feces with <5% eliminated in the urineF4358,A176918FDA Label.

Interaksi Obat

1211 Data
Denosumab The risk or severity of adverse effects can be increased when Denosumab is combined with Fluticasone.
Peginterferon alfa-2a The risk or severity of adverse effects can be increased when Peginterferon alfa-2a is combined with Fluticasone.
Interferon alfa-n1 The risk or severity of adverse effects can be increased when Interferon alfa-n1 is combined with Fluticasone.
Interferon alfa-n3 The risk or severity of adverse effects can be increased when Interferon alfa-n3 is combined with Fluticasone.
Peginterferon alfa-2b The risk or severity of adverse effects can be increased when Peginterferon alfa-2b is combined with Fluticasone.
Interferon gamma-1b The risk or severity of adverse effects can be increased when Interferon gamma-1b is combined with Fluticasone.
Interferon alfa-2a The risk or severity of adverse effects can be increased when Interferon alfa-2a is combined with Fluticasone.
Gemtuzumab ozogamicin The risk or severity of adverse effects can be increased when Gemtuzumab ozogamicin is combined with Fluticasone.
Pegaspargase The serum concentration of Fluticasone 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.
Interferon alfacon-1 The risk or severity of adverse effects can be increased when Interferon alfacon-1 is combined with Fluticasone.
Rituximab The risk or severity of adverse effects can be increased when Rituximab is combined with Fluticasone.
Basiliximab The risk or severity of adverse effects can be increased when Basiliximab is combined with Fluticasone.
Muromonab The risk or severity of adverse effects can be increased when Muromonab is combined with Fluticasone.
Ibritumomab tiuxetan The risk or severity of adverse effects can be increased when Ibritumomab tiuxetan is combined with Fluticasone.
Tositumomab The risk or severity of adverse effects can be increased when Tositumomab is combined with Fluticasone.
Alemtuzumab The risk or severity of adverse effects can be increased when Alemtuzumab is combined with Fluticasone.
Alefacept The risk or severity of adverse effects can be increased when Alefacept is combined with Fluticasone.
Efalizumab The risk or severity of adverse effects can be increased when Efalizumab is combined with Fluticasone.
Antithymocyte immunoglobulin (rabbit) The risk or severity of adverse effects can be increased when Antithymocyte immunoglobulin (rabbit) is combined with Fluticasone.
Interferon alfa-2b The risk or severity of adverse effects can be increased when Interferon alfa-2b is combined with Fluticasone.
Daclizumab The risk or severity of adverse effects can be increased when Daclizumab is combined with Fluticasone.
Phenylalanine The risk or severity of adverse effects can be increased when Phenylalanine is combined with Fluticasone.
Cladribine Fluticasone may increase the immunosuppressive activities of Cladribine.
Carmustine The risk or severity of adverse effects can be increased when Carmustine is combined with Fluticasone.
Amsacrine The risk or severity of adverse effects can be increased when Amsacrine is combined with Fluticasone.
Bleomycin The risk or severity of adverse effects can be increased when Bleomycin is combined with Fluticasone.
Chlorambucil The risk or severity of adverse effects can be increased when Chlorambucil is combined with Fluticasone.
Raltitrexed The risk or severity of adverse effects can be increased when Raltitrexed is combined with Fluticasone.
Mitomycin The risk or severity of adverse effects can be increased when Mitomycin is combined with Fluticasone.
Bexarotene The risk or severity of adverse effects can be increased when Bexarotene is combined with Fluticasone.
Floxuridine The risk or severity of adverse effects can be increased when Floxuridine is combined with Fluticasone.
Tioguanine The risk or severity of adverse effects can be increased when Tioguanine is combined with Fluticasone.
Dexrazoxane The risk or severity of adverse effects can be increased when Dexrazoxane is combined with Fluticasone.
Streptozocin The risk or severity of adverse effects can be increased when Streptozocin is combined with Fluticasone.
Trifluridine The risk or severity of adverse effects can be increased when Trifluridine is combined with Fluticasone.
Gemcitabine The risk or severity of adverse effects can be increased when Gemcitabine is combined with Fluticasone.
Epirubicin The risk or severity of adverse effects can be increased when Epirubicin is combined with Fluticasone.
Chloramphenicol The risk or severity of adverse effects can be increased when Chloramphenicol is combined with Fluticasone.
Lenalidomide The risk or severity of adverse effects can be increased when Lenalidomide is combined with Fluticasone.
Altretamine The risk or severity of adverse effects can be increased when Altretamine is combined with Fluticasone.
Zidovudine The risk or severity of adverse effects can be increased when Zidovudine is combined with Fluticasone.
Oxaliplatin The risk or severity of adverse effects can be increased when Oxaliplatin is combined with Fluticasone.
Propylthiouracil The risk or severity of adverse effects can be increased when Propylthiouracil is combined with Fluticasone.
Pentostatin The risk or severity of adverse effects can be increased when Pentostatin is combined with Fluticasone.
Linezolid The risk or severity of adverse effects can be increased when Linezolid is combined with Fluticasone.
Clofarabine The risk or severity of adverse effects can be increased when Clofarabine is combined with Fluticasone.
Pemetrexed The risk or severity of adverse effects can be increased when Pemetrexed is combined with Fluticasone.
Mycophenolate mofetil The risk or severity of adverse effects can be increased when Mycophenolate mofetil is combined with Fluticasone.
Tretinoin The metabolism of Tretinoin can be decreased when combined with Fluticasone.
Methimazole The risk or severity of adverse effects can be increased when Methimazole is combined with Fluticasone.
Dacarbazine The risk or severity of adverse effects can be increased when Dacarbazine is combined with Fluticasone.
Temozolomide The risk or severity of adverse effects can be increased when Temozolomide is combined with Fluticasone.
Penicillamine The risk or severity of adverse effects can be increased when Penicillamine is combined with Fluticasone.
Azacitidine The risk or severity of adverse effects can be increased when Azacitidine is combined with Fluticasone.
Carboplatin The risk or severity of adverse effects can be increased when Carboplatin is combined with Fluticasone.
Dactinomycin The risk or severity of adverse effects can be increased when Dactinomycin is combined with Fluticasone.
Azathioprine The risk or severity of adverse effects can be increased when Azathioprine is combined with Fluticasone.
Hydroxyurea The risk or severity of adverse effects can be increased when Hydroxyurea is combined with Fluticasone.
Mycophenolic acid The risk or severity of adverse effects can be increased when Mycophenolic acid is combined with Fluticasone.
Topotecan The risk or severity of adverse effects can be increased when Topotecan is combined with Fluticasone.
Mercaptopurine The risk or severity of adverse effects can be increased when Mercaptopurine is combined with Fluticasone.
Thalidomide The risk or severity of adverse effects can be increased when Thalidomide is combined with Fluticasone.
Melphalan The risk or severity of adverse effects can be increased when Melphalan is combined with Fluticasone.
Fludarabine The risk or severity of adverse effects can be increased when Fludarabine is combined with Fluticasone.
Flucytosine The risk or severity of adverse effects can be increased when Flucytosine is combined with Fluticasone.
Capecitabine The risk or severity of adverse effects can be increased when Capecitabine is combined with Fluticasone.
Procarbazine The risk or severity of adverse effects can be increased when Procarbazine is combined with Fluticasone.
Arsenic trioxide The risk or severity of adverse effects can be increased when Arsenic trioxide is combined with Fluticasone.
Idarubicin The risk or severity of adverse effects can be increased when Idarubicin is combined with Fluticasone.
Estramustine The risk or severity of adverse effects can be increased when Estramustine is combined with Fluticasone.
Mitoxantrone The risk or severity of adverse effects can be increased when Mitoxantrone is combined with Fluticasone.
Lomustine The risk or severity of adverse effects can be increased when Lomustine is combined with Fluticasone.
Eculizumab The risk or severity of adverse effects can be increased when Eculizumab is combined with Fluticasone.
Decitabine The risk or severity of adverse effects can be increased when Decitabine is combined with Fluticasone.
Nelarabine The risk or severity of adverse effects can be increased when Nelarabine is combined with Fluticasone.
Stepronin The risk or severity of adverse effects can be increased when Stepronin is combined with Fluticasone.
Hydroxychloroquine The risk or severity of adverse effects can be increased when Hydroxychloroquine is combined with Fluticasone.
Castanospermine The risk or severity of adverse effects can be increased when Castanospermine is combined with Fluticasone.
Vorinostat The risk or severity of adverse effects can be increased when Vorinostat is combined with Fluticasone.
2-Methoxyethanol The risk or severity of adverse effects can be increased when 2-Methoxyethanol is combined with Fluticasone.
Brequinar The risk or severity of adverse effects can be increased when Brequinar is combined with Fluticasone.
Pirfenidone The risk or severity of adverse effects can be increased when Pirfenidone is combined with Fluticasone.
Interferon alfa The risk or severity of adverse effects can be increased when Interferon alfa is combined with Fluticasone.
Glatiramer The risk or severity of adverse effects can be increased when Glatiramer is combined with Fluticasone.
Briakinumab The risk or severity of adverse effects can be increased when Briakinumab is combined with Fluticasone.
Human interferon omega-1 The risk or severity of adverse effects can be increased when Human interferon omega-1 is combined with Fluticasone.
Mepolizumab The risk or severity of adverse effects can be increased when Mepolizumab is combined with Fluticasone.
Abetimus The risk or severity of adverse effects can be increased when Abetimus is combined with Fluticasone.
Belatacept The risk or severity of adverse effects can be increased when Belatacept is combined with Fluticasone.
Bendamustine The risk or severity of adverse effects can be increased when Bendamustine is combined with Fluticasone.
Pralatrexate The risk or severity of adverse effects can be increased when Pralatrexate is combined with Fluticasone.
Wortmannin The risk or severity of adverse effects can be increased when Wortmannin is combined with Fluticasone.
Eribulin The risk or severity of adverse effects can be increased when Eribulin is combined with Fluticasone.
Belimumab The risk or severity of adverse effects can be increased when Belimumab is combined with Fluticasone.
Teriflunomide The risk or severity of adverse effects can be increased when Teriflunomide is combined with Fluticasone.
Carfilzomib The risk or severity of adverse effects can be increased when Carfilzomib is combined with Fluticasone.
Dimethyl fumarate The risk or severity of adverse effects can be increased when Dimethyl fumarate is combined with Fluticasone.
Obinutuzumab The risk or severity of adverse effects can be increased when Obinutuzumab is combined with Fluticasone.
Vedolizumab The risk or severity of adverse effects can be increased when Vedolizumab is combined with Fluticasone.

Target Protein

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

Referensi & Sumber

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.
  • 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.

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