Peringatan Keamanan

Diverse studies performed on tixocortol proved that this drug is non-toxic and non-immunosupressive. This low toxicity and abscence of immuno supression gave tixocortol the potential to be a lead for topical or local anti-inflammatory treatments.A31448 Nevertheless, toxicortol is a potent cutaneous sensitizer, causing a local allergy.A31436

Tixocortol

DB09091

small molecule approved withdrawn

Deskripsi

Tixocortol is a 21-thiol derivative of hydrocortisone classified as a class A corticosteroid. It is a synthetic steroid with topical anti-inflammatory properties without the systemic glucocorticoid and mineralocorticoid activities and toxicity.L1078

Struktur Molekul 2D

Berat 378.53
Wujud solid

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

Profil Farmakokinetik

Waktu Paruh (Half-Life) Tixocortol presents a shorter half-life than cortisol.[A31447]
Volume Distribusi Studies have shown that oral or intravenous administration of tixocortol presents a significantly larger volume of distribution compared to cortisol of 21.7 L/kg.[A31439]
Klirens (Clearance) Studies have shown that oral or intravenous administration of tixocortol presents a significantly larger clearance rate compared to cortisol of 33.3 L h/kg.[A31439]

Absorpsi

The absorption of tixocortol is the same as in other steroids including hydrocortisone.L1078 Oral administration of tixocortol presents a 10-20% bioavailability with a significantly lower plasma Cmax than cortisol. The fast metabolism, larger volume of distribution and low bioavailability donates tixocortol with the absence of systemic activity.A31439

Metabolisme

Tixocortol is rapidly modified within red blood cells and it is immediately metabolized by a first-pass liver metabolism.L1078 The metabolites of tixocortol are mainly represented by the formation of sulfo- and glucurono-conjugates which are later hydrolyzed from the conjugate forming neutral steroids. The metabolic transformations are the reduction of the 3-keto and delta 4 system, reduction of the C-20 carbonyl group, oxidation of the C-11 alcohol and cleavage of the side chain at C-17. The specific metabolic pathways of the C-21 thiol ester function were its transformation into methylthio, methylsulfonyl and methylsulfonyl derivatives and reductive cleavage of the C-21-S bond leading to 21-methyl structures. None of the metabolites have affinity for glucocorticoid receptors. This and the extensive metabolism explains the exclusive local activities of tixocortol.A31443

Rute Eliminasi

Tixocortol has a rapid elimination after continuous metabolism. Urine analysis of oral administration of tixocortol demonstrate a complete lack of unchanged drug.A31443

Interaksi Obat

1365 Data
Denosumab The risk or severity of adverse effects can be increased when Denosumab is combined with Tixocortol.
Etanercept The risk or severity of adverse effects can be increased when Etanercept is combined with Tixocortol.
Peginterferon alfa-2a The risk or severity of adverse effects can be increased when Peginterferon alfa-2a is combined with Tixocortol.
Interferon alfa-n1 The risk or severity of adverse effects can be increased when Interferon alfa-n1 is combined with Tixocortol.
Interferon alfa-n3 The risk or severity of adverse effects can be increased when Interferon alfa-n3 is combined with Tixocortol.
Peginterferon alfa-2b The risk or severity of adverse effects can be increased when Peginterferon alfa-2b is combined with Tixocortol.
Anakinra The risk or severity of adverse effects can be increased when Anakinra is combined with Tixocortol.
Interferon gamma-1b The risk or severity of adverse effects can be increased when Interferon gamma-1b is combined with Tixocortol.
Interferon alfa-2a The risk or severity of adverse effects can be increased when Interferon alfa-2a is combined with Tixocortol.
Aldesleukin The risk or severity of adverse effects can be increased when Aldesleukin is combined with Tixocortol.
Adalimumab The risk or severity of adverse effects can be increased when Adalimumab is combined with Tixocortol.
Gemtuzumab ozogamicin The risk or severity of adverse effects can be increased when Gemtuzumab ozogamicin is combined with Tixocortol.
Pegaspargase The risk or severity of adverse effects can be increased when Pegaspargase is combined with Tixocortol.
Infliximab The risk or severity of adverse effects can be increased when Infliximab is combined with Tixocortol.
Interferon beta-1b The risk or severity of adverse effects can be increased when Interferon beta-1b is combined with Tixocortol.
Interferon alfacon-1 The risk or severity of adverse effects can be increased when Interferon alfacon-1 is combined with Tixocortol.
Rituximab The risk or severity of adverse effects can be increased when Rituximab is combined with Tixocortol.
Basiliximab The risk or severity of adverse effects can be increased when Basiliximab is combined with Tixocortol.
Muromonab The risk or severity of adverse effects can be increased when Muromonab is combined with Tixocortol.
Ibritumomab tiuxetan The risk or severity of adverse effects can be increased when Ibritumomab tiuxetan is combined with Tixocortol.
Tositumomab The risk or severity of adverse effects can be increased when Tositumomab is combined with Tixocortol.
Alemtuzumab The risk or severity of adverse effects can be increased when Alemtuzumab is combined with Tixocortol.
Alefacept The risk or severity of adverse effects can be increased when Alefacept is combined with Tixocortol.
Efalizumab The risk or severity of adverse effects can be increased when Efalizumab is combined with Tixocortol.
Antithymocyte immunoglobulin (rabbit) The risk or severity of adverse effects can be increased when Antithymocyte immunoglobulin (rabbit) is combined with Tixocortol.
Interferon alfa-2b The risk or severity of adverse effects can be increased when Interferon alfa-2b is combined with Tixocortol.
Daclizumab The risk or severity of adverse effects can be increased when Daclizumab is combined with Tixocortol.
Phenylalanine The risk or severity of adverse effects can be increased when Phenylalanine is combined with Tixocortol.
Bortezomib The risk or severity of adverse effects can be increased when Bortezomib is combined with Tixocortol.
Cladribine Tixocortol may increase the immunosuppressive activities of Cladribine.
Carmustine The risk or severity of adverse effects can be increased when Carmustine is combined with Tixocortol.
Amsacrine The risk or severity of adverse effects can be increased when Amsacrine is combined with Tixocortol.
Bleomycin The risk or severity of adverse effects can be increased when Bleomycin is combined with Tixocortol.
Chlorambucil The risk or severity of adverse effects can be increased when Chlorambucil is combined with Tixocortol.
Raltitrexed The risk or severity of adverse effects can be increased when Raltitrexed is combined with Tixocortol.
Mitomycin The risk or severity of adverse effects can be increased when Mitomycin is combined with Tixocortol.
Bexarotene The risk or severity of adverse effects can be increased when Bexarotene is combined with Tixocortol.
Vindesine The risk or severity of adverse effects can be increased when Vindesine is combined with Tixocortol.
Floxuridine The risk or severity of adverse effects can be increased when Floxuridine is combined with Tixocortol.
Tioguanine The risk or severity of adverse effects can be increased when Tioguanine is combined with Tixocortol.
Vinorelbine The risk or severity of adverse effects can be increased when Vinorelbine is combined with Tixocortol.
Dexrazoxane The risk or severity of adverse effects can be increased when Dexrazoxane is combined with Tixocortol.
Sorafenib The risk or severity of adverse effects can be increased when Sorafenib is combined with Tixocortol.
Streptozocin The risk or severity of adverse effects can be increased when Streptozocin is combined with Tixocortol.
Trifluridine The risk or severity of adverse effects can be increased when Trifluridine is combined with Tixocortol.
Gemcitabine The risk or severity of adverse effects can be increased when Gemcitabine is combined with Tixocortol.
Teniposide The risk or severity of adverse effects can be increased when Teniposide is combined with Tixocortol.
Epirubicin The risk or severity of adverse effects can be increased when Epirubicin is combined with Tixocortol.
Chloramphenicol The risk or severity of adverse effects can be increased when Chloramphenicol is combined with Tixocortol.
Lenalidomide The risk or severity of adverse effects can be increased when Lenalidomide is combined with Tixocortol.
Altretamine The risk or severity of adverse effects can be increased when Altretamine is combined with Tixocortol.
Zidovudine The risk or severity of adverse effects can be increased when Zidovudine is combined with Tixocortol.
Oxaliplatin The risk or severity of adverse effects can be increased when Oxaliplatin is combined with Tixocortol.
Cyclophosphamide The risk or severity of adverse effects can be increased when Cyclophosphamide is combined with Tixocortol.
Vincristine The risk or severity of adverse effects can be increased when Vincristine is combined with Tixocortol.
Fluorouracil The risk or severity of adverse effects can be increased when Fluorouracil is combined with Tixocortol.
Propylthiouracil The risk or severity of adverse effects can be increased when Propylthiouracil is combined with Tixocortol.
Pentostatin The risk or severity of adverse effects can be increased when Pentostatin is combined with Tixocortol.
Methotrexate The risk or severity of adverse effects can be increased when Methotrexate is combined with Tixocortol.
Carbamazepine The risk or severity of adverse effects can be increased when Carbamazepine is combined with Tixocortol.
Vinblastine The risk or severity of adverse effects can be increased when Vinblastine is combined with Tixocortol.
Linezolid The risk or severity of adverse effects can be increased when Linezolid is combined with Tixocortol.
Imatinib The risk or severity of adverse effects can be increased when Imatinib is combined with Tixocortol.
Clofarabine The risk or severity of adverse effects can be increased when Clofarabine is combined with Tixocortol.
Pemetrexed The risk or severity of adverse effects can be increased when Pemetrexed is combined with Tixocortol.
Mycophenolate mofetil The risk or severity of adverse effects can be increased when Mycophenolate mofetil is combined with Tixocortol.
Daunorubicin The risk or severity of adverse effects can be increased when Daunorubicin is combined with Tixocortol.
Irinotecan The risk or severity of adverse effects can be increased when Irinotecan is combined with Tixocortol.
Methimazole The risk or severity of adverse effects can be increased when Methimazole is combined with Tixocortol.
Etoposide The risk or severity of adverse effects can be increased when Etoposide is combined with Tixocortol.
Dacarbazine The risk or severity of adverse effects can be increased when Dacarbazine is combined with Tixocortol.
Temozolomide The risk or severity of adverse effects can be increased when Temozolomide is combined with Tixocortol.
Penicillamine The risk or severity of adverse effects can be increased when Penicillamine is combined with Tixocortol.
Sirolimus The risk or severity of adverse effects can be increased when Sirolimus is combined with Tixocortol.
Azacitidine The risk or severity of adverse effects can be increased when Azacitidine is combined with Tixocortol.
Carboplatin The risk or severity of adverse effects can be increased when Carboplatin is combined with Tixocortol.
Dactinomycin The risk or severity of adverse effects can be increased when Dactinomycin is combined with Tixocortol.
Cytarabine The risk or severity of adverse effects can be increased when Cytarabine is combined with Tixocortol.
Azathioprine The risk or severity of adverse effects can be increased when Azathioprine is combined with Tixocortol.
Doxorubicin The risk or severity of adverse effects can be increased when Doxorubicin is combined with Tixocortol.
Hydroxyurea The risk or severity of adverse effects can be increased when Hydroxyurea is combined with Tixocortol.
Busulfan The risk or severity of adverse effects can be increased when Busulfan is combined with Tixocortol.
Mycophenolic acid The risk or severity of adverse effects can be increased when Mycophenolic acid is combined with Tixocortol.
Topotecan The risk or severity of adverse effects can be increased when Topotecan is combined with Tixocortol.
Mercaptopurine The risk or severity of adverse effects can be increased when Mercaptopurine is combined with Tixocortol.
Thalidomide The risk or severity of adverse effects can be increased when Thalidomide is combined with Tixocortol.
Melphalan The risk or severity of adverse effects can be increased when Melphalan is combined with Tixocortol.
Fludarabine The risk or severity of adverse effects can be increased when Fludarabine is combined with Tixocortol.
Flucytosine The risk or severity of adverse effects can be increased when Flucytosine is combined with Tixocortol.
Capecitabine The risk or severity of adverse effects can be increased when Capecitabine is combined with Tixocortol.
Procarbazine The risk or severity of adverse effects can be increased when Procarbazine is combined with Tixocortol.
Arsenic trioxide The risk or severity of adverse effects can be increased when Arsenic trioxide is combined with Tixocortol.
Idarubicin The risk or severity of adverse effects can be increased when Idarubicin is combined with Tixocortol.
Ifosfamide The risk or severity of adverse effects can be increased when Ifosfamide is combined with Tixocortol.
Estramustine The risk or severity of adverse effects can be increased when Estramustine is combined with Tixocortol.
Mitoxantrone The risk or severity of adverse effects can be increased when Mitoxantrone is combined with Tixocortol.
Lomustine The risk or severity of adverse effects can be increased when Lomustine is combined with Tixocortol.
Paclitaxel The risk or severity of adverse effects can be increased when Paclitaxel is combined with Tixocortol.
Docetaxel The risk or severity of adverse effects can be increased when Docetaxel is combined with Tixocortol.
Dasatinib The risk or severity of adverse effects can be increased when Dasatinib is combined with Tixocortol.

Target Protein

Glucocorticoid receptor NR3C1
Histone deacetylase 2 HDAC2

Referensi & Sumber

Artikel (PubMed)
  • PMID: 2043986
    Friedman BS, Metcalfe DD: Effects of tixocortol pivalate on gastrointestinal disease in systemic mastocytosis: a preliminary study. Clin Exp Allergy. 1991 Mar;21(2):183-8.
  • PMID: 8977714
    Rasanen L, Tuomi ML, Ylitalo L: Reactivity of tixocortol pivalate-positive patients in intradermal and oral provocation tests. Br J Dermatol. 1996 Dec;135(6):931-4.
  • PMID: 7700614
    Bircher AJ, Hirsbrunner P, Tschopp K, Wildermuth V: Allergic contact dermatitis from tixocortol pivalate in a nasal spray masquerading as infectious complication of sinusitis. ORL J Otorhinolaryngol Relat Spec. 1995 Jan-Feb;57(1):54-6.
  • PMID: 6492803
    Chanoine F, Junien JL: Comparative pharmacokinetic studies of tixocortol pivalate and cortisol in the rat. J Steroid Biochem. 1984 Oct;21(4):453-9.
  • PMID: 2893715
    Chanoine F, Grenot C, Sellier N, Barrett WE, Thompson RM, Fentiman AF, Nixon JR, Goyer R, Junien JL: Isolation and identification of major metabolites of tixocortol pivalate in human urine. Drug Metab Dispos. 1987 Nov-Dec;15(6):868-76.
  • PMID: 3500591
    Lelievre V, Bertin B, Chanoine F, Bure J, Junien JL: Correlation between binding activity, inhibition of lymphoblastic transformation and metabolism of tixocortol 21 pivalate in mouse thymocytes. Agents Actions. 1987 Aug;21(3-4):262-5.
  • PMID: 6784735
    Uphill PF: A comparison of the effects of tixocortol pivalate (JO 1016), beclomethasone dipropionate and hydrocortisone acetate on the activation of lymphocytes. Arzneimittelforschung. 1981;31(3):459-62.
Textbook
  • Rietschel R. and Fowler J. (2008). Fisher's contact dermatitis. BC Decker.
  • Rainsford K. and Velo G. (1989). New developments in antirheumatic therapy. Kluwer Academic Publishers.

Contoh Produk & Brand

Produk: 2 • International brands: 0
Produk
  • Rectovalone 250mg/100ml
    Suspension • 250 mg / 100 mL • Rectal • Canada • Approved
  • T.R.U.E. Test Thin-Layer Rapid Use Patch Test
    Kit • - • Cutaneous • US • Approved

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