Peringatan Keamanan

The oral LD50 in female mice was 6.5g/kg and 794mg/kg via the intravenous route.L10701

Overdoses are not expected with otic formulations.L10698 Chronic high doses of glucocorticoids can lead to the development of cataract, glaucoma, hypertension, water retention, hyperlipidemia, peptic ulcer, pancreatitis, myopathy, osteoporosis, mood changes, psychosis, dermal atrophy, allergy, acne, hypertrichosis, immune suppression, decreased resistance to infection, moon face, hyperglycemia, hypocalcemia, hypophosphatemia, metabolic acidosis, growth suppression, and secondary adrenal insufficiency.A188405 Overdose may be treated by adjusting the dose or stopping the corticosteroid as well as initiating symptomatic and supportive treatment.A188405

Dexamethasone

DB01234

small molecule approved investigational vet_approved

Deskripsi

Dexamethasone, or MK-125, is a corticosteroid fluorinated at position 9 used to treat endocrine, rheumatic, collagen, dermatologic, allergic, ophthalmic, gastrointestinal, respiratory, hematologic, neoplastic, edematous, and other conditions.L10701 Developed in 1957, it is structurally similar to other corticosteroids like hydrocortisone and prednisolone.A188724

Dexamethasone was granted FDA approval on 30 October 1958.L10695 In a press release for the Randomized Evaluation of COVID-19 Therapy (RECOVERY) trial on 16 June 2020, dexamethasone was recommended for use in COVID-19 patients with severe respiratory symptoms. Dexamethasone reduced deaths by approximately one third in patients requiring ventilation and by one fifth in those requiring oxygen.L14318

Struktur Molekul 2D

Berat 392.4611
Wujud solid

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

Profil Farmakokinetik

Waktu Paruh (Half-Life) The mean terminal half life of a 20mg oral tablet is 4 hours.[L10710] A 1.5mg oral dose of dexamethasone has a half life of 6.6±4.3h, while a 3mg intramuscular dose has a half life of 4.2±1.2h.[A188718]
Volume Distribusi A 1.5mg oral dose of dexamethasone has a volume of distribution of 51.0L, while a 3mg intramuscular dose has a volume of distribution of 96.0L.[A188718]
Klirens (Clearance) A 20mg oral tablet has a clearance of 15.7L/h.[L10710] A 1.5mg oral dose of dexamethasone has a clearance of 15.6±4.9L/h while a 3.0mg intramuscular dose has a clearance of 9.9±1.4L/h.[A188718]

Absorpsi

Absorption via the intramuscular route is slower than via the intravenous route.L10701 A 3mg intramuscular dose reaches a Cmax of 34.6±6.0ng/mL with a Tmax of 2.0±1.2h and an AUC of 113±38ng\*h/mL.A188718 A 1.5mg oral dose reaches a Cmax of 13.9±6.8ng/mL with a Tmax of 2.0±0.5h and an AUC of 331±50ng\*h/mL.A188718 Oral dexamethasone is approximately 70-78% bioavailable in healthy subjects.A188721

Metabolisme

Dexamethasone is 6-hydroxylated by CYP3A4 to 6?- and 6?-hydroxydexamethasone.A187268 Dexamethasone is reversibly metabolized to 11-dehydrodexamethasone by corticosteroid 11-beta-dehydrogenase isozyme 2 and can also be converted back to dexamethasone by Corticosteroid 11-beta-dehydrogenase isozyme 1.A10059,A188556

Rute Eliminasi

Corticosteroids are generally eliminated predominantly in the urine.A187436 However, dexamethasone is <10% elminated in urine.L10710

Interaksi Makanan

2 Data
  • 1. Avoid alcohol.
  • 2. Take with food. Food reduces irritation.

Interaksi Obat

1720 Data
Denosumab The risk or severity of adverse effects can be increased when Denosumab is combined with Dexamethasone.
Peginterferon alfa-2a The risk or severity of adverse effects can be increased when Peginterferon alfa-2a is combined with Dexamethasone.
Interferon alfa-n1 The risk or severity of adverse effects can be increased when Interferon alfa-n1 is combined with Dexamethasone.
Interferon alfa-n3 The risk or severity of adverse effects can be increased when Interferon alfa-n3 is combined with Dexamethasone.
Peginterferon alfa-2b The risk or severity of adverse effects can be increased when Peginterferon alfa-2b is combined with Dexamethasone.
Interferon gamma-1b The risk or severity of adverse effects can be increased when Interferon gamma-1b is combined with Dexamethasone.
Interferon alfa-2a The risk or severity of adverse effects can be increased when Interferon alfa-2a is combined with Dexamethasone.
Aldesleukin The risk or severity of adverse effects can be increased when Aldesleukin is combined with Dexamethasone.
Gemtuzumab ozogamicin The risk or severity of adverse effects can be increased when Gemtuzumab ozogamicin is combined with Dexamethasone.
Interferon beta-1b The risk or severity of adverse effects can be increased when Interferon beta-1b is combined with Dexamethasone.
Interferon alfacon-1 The risk or severity of adverse effects can be increased when Interferon alfacon-1 is combined with Dexamethasone.
Rituximab The risk or severity of adverse effects can be increased when Rituximab is combined with Dexamethasone.
Basiliximab The risk or severity of adverse effects can be increased when Basiliximab is combined with Dexamethasone.
Muromonab The risk or severity of adverse effects can be increased when Muromonab is combined with Dexamethasone.
Ibritumomab tiuxetan The risk or severity of adverse effects can be increased when Ibritumomab tiuxetan is combined with Dexamethasone.
Tositumomab The risk or severity of adverse effects can be increased when Tositumomab is combined with Dexamethasone.
Alemtuzumab The risk or severity of adverse effects can be increased when Alemtuzumab is combined with Dexamethasone.
Alefacept The risk or severity of adverse effects can be increased when Alefacept is combined with Dexamethasone.
Efalizumab The risk or severity of adverse effects can be increased when Efalizumab is combined with Dexamethasone.
Antithymocyte immunoglobulin (rabbit) The risk or severity of adverse effects can be increased when Antithymocyte immunoglobulin (rabbit) is combined with Dexamethasone.
Interferon alfa-2b The risk or severity of adverse effects can be increased when Interferon alfa-2b is combined with Dexamethasone.
Daclizumab The risk or severity of adverse effects can be increased when Daclizumab is combined with Dexamethasone.
Phenylalanine The risk or severity of adverse effects can be increased when Phenylalanine is combined with Dexamethasone.
Cladribine The excretion of Cladribine can be decreased when combined with Dexamethasone.
Carmustine The risk or severity of adverse effects can be increased when Carmustine is combined with Dexamethasone.
Amsacrine The risk or severity of adverse effects can be increased when Amsacrine is combined with Dexamethasone.
Bleomycin The risk or severity of adverse effects can be increased when Bleomycin is combined with Dexamethasone.
Chlorambucil The risk or severity of adverse effects can be increased when Chlorambucil is combined with Dexamethasone.
Raltitrexed The risk or severity of adverse effects can be increased when Raltitrexed is combined with Dexamethasone.
Mitomycin The risk or severity of adverse effects can be increased when Mitomycin is combined with Dexamethasone.
Bexarotene The risk or severity of adverse effects can be increased when Bexarotene is combined with Dexamethasone.
Floxuridine The risk or severity of adverse effects can be increased when Floxuridine is combined with Dexamethasone.
Tioguanine The risk or severity of adverse effects can be increased when Tioguanine is combined with Dexamethasone.
Dexrazoxane The risk or severity of adverse effects can be increased when Dexrazoxane is combined with Dexamethasone.
Streptozocin The risk or severity of adverse effects can be increased when Streptozocin is combined with Dexamethasone.
Trifluridine The risk or severity of adverse effects can be increased when Trifluridine is combined with Dexamethasone.
Gemcitabine The risk or severity of adverse effects can be increased when Gemcitabine is combined with Dexamethasone.
Epirubicin The risk or severity of adverse effects can be increased when Epirubicin is combined with Dexamethasone.
Chloramphenicol The risk or severity of adverse effects can be increased when Chloramphenicol is combined with Dexamethasone.
Altretamine The risk or severity of adverse effects can be increased when Altretamine is combined with Dexamethasone.
Zidovudine The risk or severity of adverse effects can be increased when Zidovudine is combined with Dexamethasone.
Oxaliplatin The risk or severity of adverse effects can be increased when Oxaliplatin is combined with Dexamethasone.
Propylthiouracil The risk or severity of adverse effects can be increased when Propylthiouracil is combined with Dexamethasone.
Pentostatin The risk or severity of adverse effects can be increased when Pentostatin is combined with Dexamethasone.
Linezolid The risk or severity of adverse effects can be increased when Linezolid is combined with Dexamethasone.
Clofarabine The risk or severity of adverse effects can be increased when Clofarabine is combined with Dexamethasone.
Pemetrexed The risk or severity of adverse effects can be increased when Pemetrexed is combined with Dexamethasone.
Mycophenolate mofetil The risk or severity of adverse effects can be increased when Mycophenolate mofetil is combined with Dexamethasone.
Tretinoin The metabolism of Tretinoin can be increased when combined with Dexamethasone.
Dacarbazine The risk or severity of adverse effects can be increased when Dacarbazine is combined with Dexamethasone.
Temozolomide The risk or severity of adverse effects can be increased when Temozolomide is combined with Dexamethasone.
Penicillamine The risk or severity of adverse effects can be increased when Penicillamine is combined with Dexamethasone.
Azacitidine The risk or severity of adverse effects can be increased when Azacitidine is combined with Dexamethasone.
Carboplatin The risk or severity of adverse effects can be increased when Carboplatin is combined with Dexamethasone.
Dactinomycin The risk or severity of adverse effects can be increased when Dactinomycin is combined with Dexamethasone.
Azathioprine The risk or severity of adverse effects can be increased when Azathioprine is combined with Dexamethasone.
Hydroxyurea The risk or severity of adverse effects can be increased when Hydroxyurea is combined with Dexamethasone.
Mycophenolic acid The risk or severity of adverse effects can be increased when Mycophenolic acid is combined with Dexamethasone.
Mercaptopurine The risk or severity of adverse effects can be increased when Mercaptopurine is combined with Dexamethasone.
Melphalan The risk or severity of adverse effects can be increased when Melphalan is combined with Dexamethasone.
Fludarabine The risk or severity of adverse effects can be increased when Fludarabine is combined with Dexamethasone.
Flucytosine The risk or severity of adverse effects can be increased when Flucytosine is combined with Dexamethasone.
Capecitabine The risk or severity of adverse effects can be increased when Capecitabine is combined with Dexamethasone.
Procarbazine The risk or severity of adverse effects can be increased when Procarbazine is combined with Dexamethasone.
Arsenic trioxide The risk or severity of adverse effects can be increased when Arsenic trioxide is combined with Dexamethasone.
Idarubicin The risk or severity of adverse effects can be increased when Idarubicin is combined with Dexamethasone.
Estramustine The risk or severity of adverse effects can be increased when Estramustine is combined with Dexamethasone.
Mitoxantrone The risk or severity of adverse effects can be increased when Mitoxantrone is combined with Dexamethasone.
Lomustine The risk or severity of adverse effects can be increased when Lomustine is combined with Dexamethasone.
Eculizumab The risk or severity of adverse effects can be increased when Dexamethasone is combined with Eculizumab.
Decitabine The risk or severity of adverse effects can be increased when Dexamethasone is combined with Decitabine.
Nelarabine The risk or severity of adverse effects can be increased when Dexamethasone is combined with Nelarabine.
Stepronin The risk or severity of adverse effects can be increased when Dexamethasone is combined with Stepronin.
Hydroxychloroquine The risk or severity of adverse effects can be increased when Dexamethasone is combined with Hydroxychloroquine.
Castanospermine The risk or severity of adverse effects can be increased when Dexamethasone is combined with Castanospermine.
Vorinostat The risk or severity of adverse effects can be increased when Dexamethasone is combined with Vorinostat.
2-Methoxyethanol The risk or severity of adverse effects can be increased when Dexamethasone is combined with 2-Methoxyethanol.
Brequinar The risk or severity of adverse effects can be increased when Dexamethasone is combined with Brequinar.
Pirfenidone The risk or severity of adverse effects can be increased when Dexamethasone is combined with Pirfenidone.
Interferon alfa The risk or severity of adverse effects can be increased when Dexamethasone is combined with Interferon alfa.
Glatiramer The risk or severity of adverse effects can be increased when Dexamethasone is combined with Glatiramer.
Briakinumab The risk or severity of adverse effects can be increased when Dexamethasone is combined with Briakinumab.
Human interferon omega-1 The risk or severity of adverse effects can be increased when Dexamethasone is combined with Human interferon omega-1.
Mepolizumab The risk or severity of adverse effects can be increased when Dexamethasone is combined with Mepolizumab.
Abetimus The risk or severity of adverse effects can be increased when Dexamethasone is combined with Abetimus.
Belatacept The risk or severity of adverse effects can be increased when Dexamethasone is combined with Belatacept.
Bendamustine The risk or severity of adverse effects can be increased when Dexamethasone is combined with Bendamustine.
Pralatrexate The risk or severity of adverse effects can be increased when Dexamethasone is combined with Pralatrexate.
Wortmannin The risk or severity of adverse effects can be increased when Dexamethasone is combined with Wortmannin.
Eribulin The risk or severity of adverse effects can be increased when Dexamethasone is combined with Eribulin.
Belimumab The risk or severity of adverse effects can be increased when Dexamethasone is combined with Belimumab.
Teriflunomide The risk or severity of adverse effects can be increased when Dexamethasone is combined with Teriflunomide.
Carfilzomib The risk or severity of adverse effects can be increased when Dexamethasone is combined with Carfilzomib.
Dimethyl fumarate The risk or severity of adverse effects can be increased when Dexamethasone is combined with Dimethyl fumarate.
Obinutuzumab The risk or severity of adverse effects can be increased when Dexamethasone is combined with Obinutuzumab.
Vedolizumab The risk or severity of adverse effects can be increased when Dexamethasone is combined with Vedolizumab.
Blinatumomab The risk or severity of adverse effects can be increased when Dexamethasone is combined with Blinatumomab.
Dinutuximab The risk or severity of adverse effects can be increased when Dexamethasone is combined with Dinutuximab.
Vilanterol The risk or severity of adverse effects can be increased when Dexamethasone is combined with Vilanterol.
Peginterferon beta-1a The risk or severity of adverse effects can be increased when Dexamethasone is combined with Peginterferon beta-1a.

Target Protein

Glucocorticoid receptor NR3C1
Nuclear receptor subfamily 0 group B member 1 NR0B1
Annexin A1 ANXA1
Nitric oxide synthase, inducible NOS2
Nuclear receptor subfamily 1 group I member 2 NR1I2

Referensi & Sumber

Synthesis reference: Fried, J.; US. Patent 2,852.51 1; September 16, 1958; assigned to Olin Mathieson Chemical Corporation. Muller, G., Bardoneschi, R. and Jolly, J.; U.S. Patent 3,007,923; November 7, 1961; assigned to Les Laboratories Francais de Chimiotherapie, France.
Artikel (PubMed)
  • PMID: 9408089
    Tomlinson ES, Maggs JL, Park BK, Back DJ: Dexamethasone metabolism in vitro: species differences. J Steroid Biochem Mol Biol. 1997 Jul;62(4):345-52. doi: 10.1016/s0960-0760(97)00038-1.
  • PMID: 24347992
    Ciriaco M, Ventrice P, Russo G, Scicchitano M, Mazzitello G, Scicchitano F, Russo E: Corticosteroid-related central nervous system side effects. J Pharmacol Pharmacother. 2013 Dec;4(Suppl 1):S94-8. doi: 10.4103/0976-500X.120975.
  • PMID: 30285357
    Yasir M, Sonthalia S: Corticosteroid Adverse Effects .
  • PMID: 15634032
    Czock D, Keller F, Rasche FM, Haussler U: Pharmacokinetics and pharmacodynamics of systemically administered glucocorticoids. Clin Pharmacokinet. 2005;44(1):61-98. doi: 10.2165/00003088-200544010-00003.
  • PMID: 3709651
    Loew D, Schuster O, Graul EH: Dose-dependent pharmacokinetics of dexamethasone. Eur J Clin Pharmacol. 1986;30(2):225-30. doi: 10.1007/bf00614309.
  • PMID: 24400953
    Spoorenberg SM, Deneer VH, Grutters JC, Pulles AE, Voorn GP, Rijkers GT, Bos WJ, van de Garde EM: Pharmacokinetics of oral vs. intravenous dexamethasone in patients hospitalized with community-acquired pneumonia. Br J Clin Pharmacol. 2014 Jul;78(1):78-83. doi: 10.1111/bcp.12295.
  • PMID: 9141556
    Diederich S, Hanke B, Oelkers W, Bahr V: Metabolism of dexamethasone in the human kidney: nicotinamide adenine dinucleotide-dependent 11beta-reduction. J Clin Endocrinol Metab. 1997 May;82(5):1598-602.
  • PMID: 9618784
    Diederich S, Hanke B, Burkhardt P, Muller M, Schoneshofer M, Bahr V, Oelkers W: Metabolism of synthetic corticosteroids by 11 beta-hydroxysteroid-dehydrogenases in man. Steroids. 1998 May-Jun;63(5-6):271-7. doi: 10.1016/s0039-128x(98)00039-7.
Menampilkan 8 dari 10 artikel.

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