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Methylprednisolone (Metpred 4/8/16)

Clinical data

Trade names Metpred
AHFS/Drugs.com monograph
Routes Oral

Pharmacokinetic data

Protein binding 78%
Metabolism liver primarily, kidney, tissues; CYP450: 3A4 substrate
Half-life urine; Half-life: 18-26h (biological)

Identifiers

CAS number 83-43-2
ATC code D07AA01 D07AC14,D10AA02, H02AB04
PubChem CID 6741
Drug Bank DB00959
ChemSpider 6485
UNII X4W7ZR7023
KEGG D00407
ChEBI CHEBI:6888
ChEMBL CHEMBL650
Synonyms (6α, 11β)-11,17,21-trihydroxy-6-methyl-pregna-1,4-diene-3,20-dione

Chemical data

Formula C22H30O5
Mol. mass 374.471 g/mol
SMILES[show]
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Methylprednisolone

Methylprednisolone is a synthetic glucocorticoid or corticosteroid drug. It is marketed in the USA and Canada under the brand names Medrol and Solu-Medrol. It is also available as a generic drug.

It is a variant of prednisolone, methylated at carbon 6 of the B ring.

Uses

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.

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.

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 dosage. The most serious side effect occurs after the adrenal glands cease natural production of cortical, which methylprednisolone will replace. Abrupt cessation of the drug after this occurs can result in a condition known as Addison an crisis, which can be fatal. To prevent this, the drug is usually prescribed with a tapering dosage, including a pre-dosed “dose pack” detailing a specific number of tablets to take at designated times over a several-day period. Pharmacists sometimes advise that this drug can 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.

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