Peringatan Keamanan

The oral LD50 in rats is >4g/kg.L10824 The intraperitoneal LD50 in mice is 2292mg/kg and in rats is 100mg/kg.L10824

Data regarding acute overdoses of glucocorticoids are rare.L10785,L10788 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 Treat acute overdoses with symptomatic and supportive therapy, while chronic overdoses will require temporarily reduced dosages.A188405,L10788

Methylprednisolone

DB00959

small molecule approved vet_approved

Deskripsi

Methylprednisolone is a prednisolone derivative glucocorticoid with higher potency than prednisone.A188811 It was first described in the literature in the late 1950s.A188811,A188814

Methylprednisolone was granted FDA approval on 24 October 1957.L10785 In the outbreak of COVID-19, low dose methylprednisolone-based therapy was successful in treating COVID-19-associated pneumonia in one patient with long-term immunosuppression.A192813 The efficacy of methylprednisolone in novel coronavirus pneumonia is being investigated further in clinical trials.L12666

Struktur Molekul 2D

Berat 374.4706
Wujud solid

Peta Jejaring Molekuler
Legenda: ObatTargetGenEnzim(Panah → menunjukkan arah efek / relasi)TransporterCarrier

Profil Farmakokinetik

Waktu Paruh (Half-Life) Methylprednisolone has a half life of 2.3h.[A188757,A188802]
Volume Distribusi The average volume of distribution of methylprednisolone is 1.38L/kg.[A188757]
Klirens (Clearance) The average plasma clearance of methylprednisolone is 336mL/h/kg.[A188757]

Absorpsi

Oral methylprednisolone has 89.9% the bioavailability of oral methylprednisolone acetate, while rectal methylprednisolone has 14.2% the bioavailability.A188802 Intravitreal methylprednisolone has a Tmax of 2.5h.A188808 Approximately 1/10 of an oral or IV dose of methylprednisolone will reach the vitreous humor.A188808 Further data regarding the absorption of methylprednisolone are not readily available.L10785,L10788

Metabolisme

The metabolism of methylprednisolone is thought to be mostly mediated by 11beta-hydroxysteroid dehydrogenases and 20-ketosteroid reductases.A188757

Rute Eliminasi

Methylprednisolone and its metabolites have been collected in urine in humans.A188766 A study in dogs showed 25-31% elimination in urine and 44-52% elimination in feces.A188799

Interaksi Makanan

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

Interaksi Obat

1168 Data
Denosumab The risk or severity of adverse effects can be increased when Denosumab is combined with Methylprednisolone.
Peginterferon alfa-2a The risk or severity of adverse effects can be increased when Peginterferon alfa-2a is combined with Methylprednisolone.
Interferon alfa-n1 The risk or severity of adverse effects can be increased when Interferon alfa-n1 is combined with Methylprednisolone.
Interferon alfa-n3 The risk or severity of adverse effects can be increased when Interferon alfa-n3 is combined with Methylprednisolone.
Peginterferon alfa-2b The risk or severity of adverse effects can be increased when Peginterferon alfa-2b is combined with Methylprednisolone.
Interferon gamma-1b The risk or severity of adverse effects can be increased when Interferon gamma-1b is combined with Methylprednisolone.
Interferon alfa-2a The risk or severity of adverse effects can be increased when Interferon alfa-2a is combined with Methylprednisolone.
Aldesleukin The risk or severity of adverse effects can be increased when Aldesleukin is combined with Methylprednisolone.
Gemtuzumab ozogamicin The risk or severity of adverse effects can be increased when Gemtuzumab ozogamicin is combined with Methylprednisolone.
Pegaspargase The risk or severity of adverse effects can be increased when Pegaspargase is combined with Methylprednisolone.
Interferon beta-1b The risk or severity of adverse effects can be increased when Interferon beta-1b is combined with Methylprednisolone.
Interferon alfacon-1 The risk or severity of adverse effects can be increased when Interferon alfacon-1 is combined with Methylprednisolone.
Rituximab The risk or severity of adverse effects can be increased when Rituximab is combined with Methylprednisolone.
Basiliximab The risk or severity of adverse effects can be increased when Basiliximab is combined with Methylprednisolone.
Muromonab The risk or severity of adverse effects can be increased when Muromonab is combined with Methylprednisolone.
Ibritumomab tiuxetan The risk or severity of adverse effects can be increased when Ibritumomab tiuxetan is combined with Methylprednisolone.
Tositumomab The risk or severity of adverse effects can be increased when Tositumomab is combined with Methylprednisolone.
Alemtuzumab The risk or severity of adverse effects can be increased when Alemtuzumab is combined with Methylprednisolone.
Alefacept The risk or severity of adverse effects can be increased when Alefacept is combined with Methylprednisolone.
Efalizumab The risk or severity of adverse effects can be increased when Efalizumab is combined with Methylprednisolone.
Antithymocyte immunoglobulin (rabbit) The risk or severity of adverse effects can be increased when Antithymocyte immunoglobulin (rabbit) is combined with Methylprednisolone.
Interferon alfa-2b The risk or severity of adverse effects can be increased when Interferon alfa-2b is combined with Methylprednisolone.
Daclizumab The risk or severity of adverse effects can be increased when Daclizumab is combined with Methylprednisolone.
Phenylalanine The risk or severity of adverse effects can be increased when Phenylalanine is combined with Methylprednisolone.
Cladribine Methylprednisolone may increase the immunosuppressive activities of Cladribine.
Carmustine The risk or severity of adverse effects can be increased when Carmustine is combined with Methylprednisolone.
Amsacrine The risk or severity of adverse effects can be increased when Amsacrine is combined with Methylprednisolone.
Bleomycin The risk or severity of adverse effects can be increased when Bleomycin is combined with Methylprednisolone.
Chlorambucil The risk or severity of adverse effects can be increased when Chlorambucil is combined with Methylprednisolone.
Raltitrexed The risk or severity of adverse effects can be increased when Raltitrexed is combined with Methylprednisolone.
Mitomycin The risk or severity of adverse effects can be increased when Mitomycin is combined with Methylprednisolone.
Bexarotene The risk or severity of adverse effects can be increased when Bexarotene is combined with Methylprednisolone.
Floxuridine The risk or severity of adverse effects can be increased when Floxuridine is combined with Methylprednisolone.
Tioguanine The risk or severity of adverse effects can be increased when Tioguanine is combined with Methylprednisolone.
Dexrazoxane The risk or severity of adverse effects can be increased when Dexrazoxane is combined with Methylprednisolone.
Streptozocin The risk or severity of adverse effects can be increased when Streptozocin is combined with Methylprednisolone.
Trifluridine The risk or severity of adverse effects can be increased when Trifluridine is combined with Methylprednisolone.
Gemcitabine The risk or severity of adverse effects can be increased when Gemcitabine is combined with Methylprednisolone.
Epirubicin The risk or severity of adverse effects can be increased when Epirubicin is combined with Methylprednisolone.
Chloramphenicol The risk or severity of adverse effects can be increased when Chloramphenicol is combined with Methylprednisolone.
Lenalidomide The risk or severity of adverse effects can be increased when Lenalidomide is combined with Methylprednisolone.
Altretamine The risk or severity of adverse effects can be increased when Altretamine is combined with Methylprednisolone.
Zidovudine The risk or severity of adverse effects can be increased when Zidovudine is combined with Methylprednisolone.
Oxaliplatin The risk or severity of adverse effects can be increased when Oxaliplatin is combined with Methylprednisolone.
Fluorouracil The risk or severity of adverse effects can be increased when Fluorouracil is combined with Methylprednisolone.
Propylthiouracil The risk or severity of adverse effects can be increased when Propylthiouracil is combined with Methylprednisolone.
Pentostatin The risk or severity of adverse effects can be increased when Pentostatin is combined with Methylprednisolone.
Linezolid The risk or severity of adverse effects can be increased when Linezolid is combined with Methylprednisolone.
Clofarabine The risk or severity of adverse effects can be increased when Clofarabine is combined with Methylprednisolone.
Pemetrexed The risk or severity of adverse effects can be increased when Pemetrexed is combined with Methylprednisolone.
Mycophenolate mofetil The risk or severity of adverse effects can be increased when Mycophenolate mofetil is combined with Methylprednisolone.
Dacarbazine The risk or severity of adverse effects can be increased when Dacarbazine is combined with Methylprednisolone.
Temozolomide The risk or severity of adverse effects can be increased when Temozolomide is combined with Methylprednisolone.
Penicillamine The risk or severity of adverse effects can be increased when Penicillamine is combined with Methylprednisolone.
Azacitidine The risk or severity of adverse effects can be increased when Azacitidine is combined with Methylprednisolone.
Carboplatin The risk or severity of adverse effects can be increased when Carboplatin is combined with Methylprednisolone.
Dactinomycin The risk or severity of adverse effects can be increased when Methylprednisolone is combined with Dactinomycin.
Azathioprine The risk or severity of adverse effects can be increased when Methylprednisolone is combined with Azathioprine.
Hydroxyurea The risk or severity of adverse effects can be increased when Methylprednisolone is combined with Hydroxyurea.
Mycophenolic acid The risk or severity of adverse effects can be increased when Methylprednisolone is combined with Mycophenolic acid.
Topotecan The risk or severity of adverse effects can be increased when Methylprednisolone is combined with Topotecan.
Mercaptopurine The risk or severity of adverse effects can be increased when Methylprednisolone is combined with Mercaptopurine.
Thalidomide The risk or severity of adverse effects can be increased when Methylprednisolone is combined with Thalidomide.
Melphalan The risk or severity of adverse effects can be increased when Methylprednisolone is combined with Melphalan.
Fludarabine The risk or severity of adverse effects can be increased when Methylprednisolone is combined with Fludarabine.
Flucytosine The risk or severity of adverse effects can be increased when Methylprednisolone is combined with Flucytosine.
Capecitabine The risk or severity of adverse effects can be increased when Methylprednisolone is combined with Capecitabine.
Procarbazine The risk or severity of adverse effects can be increased when Methylprednisolone is combined with Procarbazine.
Arsenic trioxide The risk or severity of adverse effects can be increased when Methylprednisolone is combined with Arsenic trioxide.
Idarubicin The risk or severity of adverse effects can be increased when Methylprednisolone is combined with Idarubicin.
Estramustine The risk or severity of adverse effects can be increased when Methylprednisolone is combined with Estramustine.
Mitoxantrone The risk or severity of adverse effects can be increased when Methylprednisolone is combined with Mitoxantrone.
Lomustine The risk or severity of adverse effects can be increased when Methylprednisolone is combined with Lomustine.
Eculizumab The risk or severity of adverse effects can be increased when Methylprednisolone is combined with Eculizumab.
Decitabine The risk or severity of adverse effects can be increased when Methylprednisolone is combined with Decitabine.
Nelarabine The risk or severity of adverse effects can be increased when Methylprednisolone is combined with Nelarabine.
Stepronin The risk or severity of adverse effects can be increased when Methylprednisolone is combined with Stepronin.
Hydroxychloroquine The risk or severity of adverse effects can be increased when Methylprednisolone is combined with Hydroxychloroquine.
Castanospermine The risk or severity of adverse effects can be increased when Methylprednisolone is combined with Castanospermine.
Vorinostat The risk or severity of adverse effects can be increased when Methylprednisolone is combined with Vorinostat.
2-Methoxyethanol The risk or severity of adverse effects can be increased when Methylprednisolone is combined with 2-Methoxyethanol.
Brequinar The risk or severity of adverse effects can be increased when Methylprednisolone is combined with Brequinar.
Pirfenidone The risk or severity of adverse effects can be increased when Methylprednisolone is combined with Pirfenidone.
Interferon alfa The risk or severity of adverse effects can be increased when Methylprednisolone is combined with Interferon alfa.
Glatiramer The risk or severity of adverse effects can be increased when Methylprednisolone is combined with Glatiramer.
Briakinumab The risk or severity of adverse effects can be increased when Methylprednisolone is combined with Briakinumab.
Human interferon omega-1 The risk or severity of adverse effects can be increased when Methylprednisolone is combined with Human interferon omega-1.
Mepolizumab The risk or severity of adverse effects can be increased when Methylprednisolone is combined with Mepolizumab.
Abetimus The risk or severity of adverse effects can be increased when Methylprednisolone is combined with Abetimus.
Belatacept The risk or severity of adverse effects can be increased when Methylprednisolone is combined with Belatacept.
Bendamustine The risk or severity of adverse effects can be increased when Methylprednisolone is combined with Bendamustine.
Pralatrexate The risk or severity of adverse effects can be increased when Methylprednisolone is combined with Pralatrexate.
Wortmannin The risk or severity of adverse effects can be increased when Methylprednisolone is combined with Wortmannin.
Eribulin The risk or severity of adverse effects can be increased when Methylprednisolone is combined with Eribulin.
Belimumab The risk or severity of adverse effects can be increased when Methylprednisolone is combined with Belimumab.
Teriflunomide The risk or severity of adverse effects can be increased when Methylprednisolone is combined with Teriflunomide.
Carfilzomib The risk or severity of adverse effects can be increased when Methylprednisolone is combined with Carfilzomib.
Dimethyl fumarate The risk or severity of adverse effects can be increased when Methylprednisolone is combined with Dimethyl fumarate.
Obinutuzumab The risk or severity of adverse effects can be increased when Methylprednisolone is combined with Obinutuzumab.
Vedolizumab The risk or severity of adverse effects can be increased when Methylprednisolone is combined with Vedolizumab.

Target Protein

Glucocorticoid receptor NR3C1
Annexin A1 ANXA1

Referensi & Sumber

Synthesis reference: Klaus Annen, Karl Petzoldt, Henry Laurent, Rudolf Wiechert, Helmut Hofmeister, "Novel 6.alpha.-methylprednisolone derivatives, their preparation, and their use." U.S. Patent US4587236, issued March, 1973.
Artikel (PubMed)
  • PMID: 3732369
    Szefler SJ, Ebling WF, Georgitis JW, Jusko WJ: Methylprednisolone versus prednisolone pharmacokinetics in relation to dose in adults. Eur J Clin Pharmacol. 1986;30(3):323-9. doi: 10.1007/bf00541537.
  • PMID: 28435101
    Abboud R, Akil M, Charcosset C, Greige-Gerges H: Interaction of glucocorticoids and progesterone derivatives with human serum albumin. Chem Phys Lipids. 2017 Oct;207(Pt B):271-278. doi: 10.1016/j.chemphyslip.2017.04.007. Epub 2017 Apr 21.
  • PMID: 23792784
    Matabosch X, Pozo OJ, Monfort N, Perez-Mana C, Farre M, Marcos J, Segura J, Ventura R: Urinary profile of methylprednisolone and its metabolites after oral and topical administrations. J Steroid Biochem Mol Biol. 2013 Nov;138:214-21. doi: 10.1016/j.jsbmb.2013.05.019. Epub 2013 Jun 20.
  • PMID: 14294877
    BUHLER DR, THOMAS RC Jr, SCHLAGEL CA: ABSORPTION, METABOLISM AND EXCRETION OF 6-ALPHA-METHYL-PREDNISOLONE-3H,21-ACETATE FOLLOWING ORAL AND INTRAMUSCULAR ADMINISTRATIONS IN THE DOG. Endocrinology. 1965 May;76:852-64. doi: 10.1210/endo-76-5-852.
  • PMID: 30285357
    Yasir M, Sonthalia S: Corticosteroid Adverse Effects .
  • PMID: 455892
    Garg DC, Wagner JG, Sakmar E, Weidler DJ, Albert KS: Rectal and oral absorption of methylprednisolone acetate. Clin Pharmacol Ther. 1979 Aug;26(2):232-9. doi: 10.1002/cpt1979262232.
  • PMID: 11217929
    Behar-Cohen FF, Gauthier S, El Aouni A, Chapon P, Parel JM, Renard G, Chauvaud D: Methylprednisolone concentrations in the vitreous and the serum after pulse therapy. Retina. 2001;21(1):48-53. doi: 10.1097/00006982-200102000-00008.
  • 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.
Menampilkan 8 dari 11 artikel.

Contoh Produk & Brand

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    Injection, suspension • 40 mg/1mL • Intra-articular; Intralesional; Intramuscular; Soft tissue • US • Approved
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    Injection, suspension • 40 mg/1mL • Intralesional; Intramuscular; Intrasynovial; Soft tissue • US • Approved
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