Methylprednisolone

Methylprednisolone
Clinical data
Trade names Medrol, Meprolone, others
AHFS/Drugs.com Monograph
MedlinePlus a682795
License data
Pregnancy
category
  • AU: A
  • US: C (Risk not ruled out)
Routes of
administration		 IV, IM, by mouth
ATC code
Legal status
Legal status
Pharmacokinetic data
Protein binding 78%
Metabolism liver primarily, kidney, tissues; CYP450: 3A4 substrate
Biological half-life urine; Half-life: 18-26h (biological)
Identifiers
Synonyms (6α, 11β)-11,17,21-trihydroxy-6-methyl-pregna-1,4-diene-3,20-dione
CAS Number
PubChem CID
IUPHAR/BPS
DrugBank
ChemSpider
UNII
KEGG
ChEBI
ChEMBL
ECHA InfoCard 100.001.343
Chemical and physical data
Formula C22H30O5
Molar mass 374.471 g/mol
3D model (JSmol)
  (verify)

Methylprednisolone, sold under the brand names Depo-Medrol and Solu-Medrol among others, is a corticosteroid medication used to suppress the immune system and decrease inflammation. Conditions in which it is used include skin diseases, rheumatic disorders, allergies, asthma, croup, COPD, certain cancers, multiple sclerosis, and as add-on therapy for tuberculosis. It is given by mouth or by injection into a vein, or muscle.[1]

Serious side effects may include mental health problems and an increased risk of infection. Common side effects with long-term use include osteoporosis, cataracts, weakness, easy bruising, and yeast infections.[1] Short-term use around the time of delivery is safe for the baby; however, long-term use during pregnancy may result in harm.[2] Methylprednisolone is in the glucocorticoid family of medication.[1]

Methylprednisolone was approved for medical use in 1955.[3] It is on the World Health Organization's List of Essential Medicines, the most effective and safe medicines needed in a health system.[4] Methylprednisolone is available as a generic medication.[1] The wholesale cost in the developing world is about 3.81 to 9.35 USD per 500 mg vial.[5] In the United States a course of treatment typically costs less than 25 USD.[6]

Medical uses

Some 4-mg methylprednisolone tablets by Sandoz
Depo-Medrol (methylprednisolone acetate) injectable suspension

Like most adrenocortical steroids, methylprednisolone is typically used for its anti-inflammatory effects. However, glucocorticoids have a wide range of effects, including changes to metabolism and immune responses. The list of medical conditions for which methylprednisolone is prescribed is rather long, and is similar to other corticosteroids such as prednisolone. Common uses include arthritis therapy and short-term treatment of bronchial inflammation or acute bronchitis due to various respiratory diseases. It is used both in the treatment of acute periods and long-term management of autoimmune diseases, most notably systemic lupus erythematosus. It is also used as a treatment for multiple sclerosis.

Another potential use of methylprednisolone is for vestibular neuritis.[7]

After egg retrieval for a cycle of in vitro fertilization, methylprednisolone may be prescribed to prevent the body from rejecting the embryos being transferred, up to the time of implantation.[8][9]

Side effects

Long-term use of methylprednisolone, as with all corticosteroids, can be associated with hyperglycemia, decreased resistance to infection, swelling of face, weight gain, congestive cardiac insufficiency, fluid and sodium retention, edema, hypertension, increased eye pressure, glaucoma, osteoporosis, and psychosis, especially when used at high doses.[10][11] The most serious side effect occurs after the adrenal glands cease natural production of cortisol, which methylprednisolone will replace. Abrupt cessation of the drug after this occurs can result in a condition known as Addisonian crisis, which can be fatal. To prevent this, the drug is usually prescribed with a tapering dose, including a predosed "dose pack" detailing a specific number of tablets to take at designated times over a several-day period. Pharmacists sometimes advise that this drug may cause sleeplessness and "down" moods.

Individuals on methylprednisolone therapy should assiduously avoid exposure to measles and chicken pox, as contracting these viral infections while on high-dose corticosteroids can result in a potentially fatal viral course. Any accidental exposure to these viral infections by individuals uncertain of their immunity to chicken pox or measles should be reported immediately, as prophylactic immunoglobulin therapy may be administered. Additionally, the administration of live, attenuated vaccines is contraindicated for individuals taking immunosuppressive doses of methylprednisolone. The exception to this rule is patients receiving complete corticosteroid replacement therapy, e.g., for Addison's disease, who may follow standard immunization protocols.

Mechanism of action

Unbound glucocorticoids cross cell membranes and bind with high affinity to specific cytoplasmic receptors, modifying transcription and protein synthesis. By this mechanism, glucocorticoids can inhibit leukocyte infiltration at the site of inflammation, interfere with mediators of inflammatory response, and suppress humoral immune responses. The anti-inflammatory actions of corticosteroids are thought to involve phospholipase A2 inhibitory proteins, lipocortins, which control the biosynthesis of potent mediators of inflammation such as prostaglandins and leukotrienes.

See also

References

  1. 1 2 3 4 "Methylprednisolone". The American Society of Health-System Pharmacists. Retrieved 8 December 2016.
  2. ↑ "Methylprednisolone Use During Pregnancy | Drugs.com". www.drugs.com. Retrieved 22 December 2016.
  3. ↑ Fischer, Janos; Ganellin, C. Robin (2006). Analogue-based Drug Discovery. John Wiley & Sons. p. 486. ISBN 9783527607495.
  4. ↑ "WHO Model List of Essential Medicines (19th List)" (PDF). World Health Organization. April 2015. Retrieved 8 December 2016.
  5. ↑ "Methylprednisolone". International Drug Price Indicator Guide. Retrieved 8 December 2016.
  6. ↑ Hamilton, Richart (2015). Tarascon Pocket Pharmacopoeia 2015 Deluxe Lab-Coat Edition. Jones & Bartlett Learning. p. 202. ISBN 9781284057560.
  7. ↑ Strupp M, Zingler VC, Arbusow V, Niklas D, Maag KP, Dieterich M, Bense S, Theil D, Jahn K, Brandt T (July 2004). "Methylprednisolone, valacyclovir, or the combination for vestibular neuritis" (PDF). N. Engl. J. Med. 351 (4): 354–61. PMID 15269315. doi:10.1056/NEJMoa033280.
  8. ↑ "Medications Commonly Used During the IVF Cycle". Continuum Reproductive Center. Retrieved 14 June 2013.
  9. ↑ "In Vitro Fertilization (IVF)". Reproductive Medicine Associates of Michigan. Retrieved 14 June 2013.
  10. ↑ "SOLU-MEDROL (methylprednisolone sodium succinate) injection, powder, for solution". National Institutes of Health. Retrieved 24 August 2012.
  11. ↑ "Medrol (Methylprednisolone - Tablets by Pfizer)". Sfatul Medicului. Retrieved 14 April 2013.
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