Methylprednisolone

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Methylprednisolone
Systematic (IUPAC) name
(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
Identifiers
CAS number 83-43-2
ATC code D07AA01 D07AC14, D10AA02, H02AB04
PubChem 6741
DrugBank APRD00342
ChemSpider 6485
Chemical data
Formula C22H30O5 
Mol. mass 374.471 g/mol
Synonyms (6α, 11β)-11,17,21-trihydroxy-6-methyl-pregna-1,4-diene-3,20-dione
Pharmacokinetic data
Bioavailability  ?
Protein binding 78%
Metabolism liver primarily, kidney, tissues; CYP450: 3A4 substrate
Half life urine; Half-life: 18-26h (biological)
Excretion  ?
Therapeutic considerations
Pregnancy cat.

C

Legal status

POM(UK) -only(US)

Routes IV, IM, IV Infusion, oral

Methylprednisolone is a synthetic glucocorticoid drug. It is sold in the USA and Canada under the brand names Phocenta, Medrol, Solu-Medrol and Cadista.[1] It is also available as a generic drug.

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

Contents

[edit] 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 methlyprednisolone 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.

Methlyprednisolone is also prescribed for non-penetrating spinal cord injuries. It has been proven that a dose of 30 mg/kg IV followed by IV drip at 5.4 mg / kg / hr for 23 hours improves sensory and motor recovery if given within 8 hours of the injury.

It is also used for vestibular neuritis.[2]

[edit] Side effects

Methylprednisolone has serious side effects if taken long-term, including weight gain, glaucoma, osteoporosis and psychosis, especially when used at high dosage. The most serious side effect occurs after the adrenal glands cease natural production of cortisone, 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 dosage, including a pre-dosed "dose pack" detailing a specific number of pills to take at designated times over a few-day period.

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