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Methylprednisolone

Methylprednisolone
Clinical data
Trade namesMedrol, others
Other names6α-Methylprednisolone; 11β,17,21-trihydroxy-6α-methyl-δ1-progesterone; 11β,17,21-Trihydroxy-6α-methylpregna-1,4-diene-3,20-dione
AHFS/Drugs.comMonograph
MedlinePlusa682795
License data
Pregnancy
category
Routes of
administration		By mouth, intramuscular, intra-articular, intravenous
ATC code
Legal status
Legal status
Pharmacokinetic data
Protein binding78%
MetabolismLiver primarily, kidney, tissues; CYP3A4
Elimination half-life1.8–2.6 hours
ExcretionUrine
Identifiers
  • (1S,2R,8S,10S,11S,14R,15S,17S)-14,17-dihydroxy-14-(2-hydroxyacetyl)-2,8,15-trimethyltetracyclo[8.7.0.02,7.011,15]heptadeca-3,6-dien-5-one
CAS Number
PubChem CID
IUPHAR/BPS
DrugBank
ChemSpider
UNII
KEGG
ChEBI
ChEMBL
CompTox Dashboard (EPA)
ECHA InfoCard100.001.343 Edit this at Wikidata
Chemical and physical data
FormulaC22H30O5
Molar mass374.477 g·mol−1
3D model (JSmol)
Melting point228 to 237 °C (442 to 459 °F)
Solubility in water1.20x10+2
  • O=C\1\C=C/[C@]4(/C(=C/1)[C@@H](C)C[C@@H]2[C@@H]4[C@@H](O)C[C@@]3([C@@](O)(C(=O)CO)CC[C@@H]23)C)C
  • InChI=1S/C22H30O5/c1-12-8-14-15-5-7-22(27,18(26)11-23)21(15,3)10-17(25)19(14)20(2)6-4-13(24)9-16(12)20/h4,6,9,12,14-15,17,19,23,25,27H,5,7-8,10-11H2,1-3H3/t12-,14-,15-,17-,19+,20-,21-,22-/m0/s1 checkY
  • Key:VHRSUDSXCMQTMA-PJHHCJLFSA-N checkY
  (verify)

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 concomitantly at high doses during acute flares. Methylprednisolone and its derivatives can be administered orally or parenterally.[7]

Regardless of 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, and skin atrophy.[9]

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.[10] In 2021, it was the 168th most commonly prescribed medication in the United States, with more than 3 million prescriptions.[11][12] Methylprednisolone is also on the World Health Organization's List of Essential Medicines for its effects against lymphoid leukemia.[13]

  1. ^ "Methylprednisolone Use During Pregnancy". Drugs.com. 20 August 2019. Retrieved 20 February 2020.
  2. ^ "Product monograph brand safety updates". Health Canada. 7 July 2016. Retrieved 3 April 2024.
  3. ^ "List of nationally authorised medicinal products : Active substance: methylprednisolone : Procedure no. PSUSA/00002026/202011" (PDF). European Medicines Agency (EMA). Retrieved 12 March 2022.
  4. ^ 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.
  5. ^ 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.
  6. ^ 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.
  7. ^ Ocejo A, Correa R (2020). "Methylprednisolone". StatPearls. Treasure Island (FL): StatPearls Publishing. PMID 31335060. Retrieved 10 November 2020.
  8. ^ 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.
  9. ^ 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.
  10. ^ "Drugs@FDA: FDA-Approved Drugs". U.S. Food and Drug Administration (FDA). Retrieved 5 December 2020.
  11. ^ "The Top 300 of 2021". ClinCalc. Archived from the original on 15 January 2024. Retrieved 14 January 2024.
  12. ^ "Methylprednisolone - Drug Usage Statistics". ClinCalc. Retrieved 14 January 2024.
  13. ^ World Health Organization (2021). World Health Organization model list of essential medicines: 22nd list 2021. Geneva: World Health Organization. WHO/MHP/HPS/EML/2021.02. License: CC BY-NC-SA 3.0 IGO.
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