Methylprednisolone
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| Trade names | Medrol, others |
| Other names | 6α-Methylprednisolone; 11β,17,21-trihydroxy-6α-methyl-δ1-progesterone; 11β,17,21-Trihydroxy-6α-methylpregna-1,4-diene-3,20-dione |
| AHFS/Drugs.com | Monograph |
| MedlinePlus | a682795 |
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| Routes of administration | By mouth, intramuscular, intra-articular, intravenous |
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| Pharmacokinetic data | |
| Protein binding | 78% |
| Metabolism | Liver primarily, kidney, tissues; CYP3A4 |
| Elimination half-life | 1.8–2.6 hours |
| Excretion | Urine |
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| ECHA InfoCard | 100.001.343 |
| Chemical and physical data | |
| Formula | C22H30O5 |
| Molar mass | 374.477 g·mol−1 |
| 3D model (JSmol) | |
| Melting point | 228 to 237 °C (442 to 459 °F) |
| Solubility in water | 1.20x10+2 |
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Methylprednisolone (Depo-Medrol, Medrol, Solu-Medrol) is a synthetic glucocorticoid, primarily prescribed for its anti-inflammatory and immunosuppressive effects.[4][5][6] It is either used at low doses for chronic illnesses or used at high doses during acute flares. Methylprednisolone and its derivatives can be administered orally or parenterally.[7]
Regardless of the route of administration, methylprednisolone integrates systemically as exhibited by its effectiveness to quickly reduce inflammation during acute flares.[8] It is associated with many adverse reactions that require tapering off the drug as soon as the disease is under control.[9] Serious side effects include iatrogenic Cushing's syndrome, hypertension, osteoporosis, diabetes, infection, psychosis, and skin atrophy.[9][10]
Chemically, methylprednisolone is a synthetic pregnane steroid hormone derived from hydrocortisone and prednisolone. It belongs to a class of synthetic glucocorticoids and more generally, corticosteroids. It acts as a mineralocorticoid and glucocorticoid receptor agonist. In comparison to other exogenous glucocorticoids, methylprednisolone has a higher affinity to glucocorticoid receptors than to mineralocorticoid receptors.
Glucocorticoid's name was derived after the discovery of their involvement in regulating carbohydrate metabolism.[9] The cellular functions of glucocorticoids, such as methylprednisolone, are now understood to regulate homeostasis, metabolism, development, cognition, and inflammation.[9] They play a critical role in adapting and responding to environmental, physical, and emotional stress.[9]
Methylprednisolone was first synthesized and manufactured by The Upjohn Company (now Viatris) and FDA approved in the United States in October 1957.[11] In 2022, it was the 153rd most commonly prescribed medication in the United States, with more than 3 million prescriptions.[12][13] It is on the World Health Organization's List of Essential Medicines.[14]
- ^ "Methylprednisolone Use During Pregnancy". Drugs.com. 20 August 2019. Retrieved 20 February 2020.
- ^ "Product monograph brand safety updates". Health Canada. 7 July 2016. Retrieved 3 April 2024.
- ^ "List of nationally authorised medicinal products: Active substance: methylprednisolone: Procedure no. PSUSA/00002026/202011" (PDF). European Medicines Agency (EMA). Retrieved 12 March 2022.
- ^ Katzung BG, Masters SB, Trevor AJ (2012). Basic & clinical pharmacology (12th ed.). New York: McGraw-Hill Medical. ISBN 978-0-07-176401-8. OCLC 761378641.
- ^ Timmermans S, Souffriau J, Libert C (2019). "A General Introduction to Glucocorticoid Biology". Frontiers in Immunology. 10: 1545. doi:10.3389/fimmu.2019.01545. PMC 6621919. PMID 31333672.
- ^ Xavier AM, Anunciato AK, Rosenstock TR, Glezer I (2016). "Gene Expression Control by Glucocorticoid Receptors during Innate Immune Responses". Frontiers in Endocrinology. 7: 31. doi:10.3389/fendo.2016.00031. PMC 4835445. PMID 27148162.
- ^ Ocejo A, Correa R (2020). "Methylprednisolone". StatPearls. Treasure Island (FL): StatPearls Publishing. PMID 31335060. Retrieved 10 November 2020.
- ^ Habib GS (July 2009). "Systemic effects of intra-articular corticosteroids". Clinical Rheumatology. 28 (7): 749–56. doi:10.1007/s10067-009-1135-x. PMID 19252817. S2CID 5645348.
- ^ a b c d e Paragliola RM, Papi G, Pontecorvi A, Corsello SM (October 2017). "Treatment with Synthetic Glucocorticoids and the Hypothalamus-Pituitary-Adrenal Axis". International Journal of Molecular Sciences. 18 (10): 2201. doi:10.3390/ijms18102201. PMC 5666882. PMID 29053578.
- ^ Cite error: The named reference
Pfizer and Upjohn Company LLC_2019was invoked but never defined (see the help page). - ^ "Drugs@FDA: FDA-Approved Drugs". U.S. Food and Drug Administration (FDA). Archived from the original on 30 April 2017. Retrieved 5 December 2020.
- ^ "The Top 300 of 2022". ClinCalc. Archived from the original on 30 August 2024. Retrieved 30 August 2024.
- ^ "Methylprednisolone Drug Usage Statistics, United States, 2013 - 2022". ClinCalc. Retrieved 30 August 2024.
- ^ World Health Organization (2023). The selection and use of essential medicines 2023: web annex A: World Health Organization model list of essential medicines: 23rd list (2023). Geneva: World Health Organization. hdl:10665/371090. WHO/MHP/HPS/EML/2023.02.