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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.
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.
Methylprednisolone is also prescribed for nonpenetrating spinal cord injuries. It has been shown 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 eight hours of the injury.It is also used for vestibular neuritis.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.Methylprednisolone may also be beneficial in the treatment of patients in cardiac arrest.
Mechanism of action
Prednisolone irreversibly binds with glucocorticoid receptors (GR) alpha and beta for which they have a high affinity. AlphaGR and BetaGR are found in virtually all tissues with variable numbers between 3000 and 10000 per cell, depending on the tissue involved. Prednisolone can activate and influence biochemical behaviour of most cells. The steroid/receptor complexes dimerise and interact with cellular DNA in the nucleus, binding to steroid-response elements and modifying gene transcription. They induce synthesis of some proteins, and inhibit synthesis of others.
Not all metabolic actions on genes are known. Most mediator proteins are enzymes, e.g., cAMP-dependent kinase
Anti-inflammatory and immunosuppressive actions:
Inhibition of gene transcription for COX-2, cytokines, cell adhesion molecules, and inducible NO synthase
Blockage of Vit D3-mediated induction of osteocalcin gene in osteoblasts
Modification of collegenase gene transcription
Increase synthesis annexin-1, important in negative feedback on hypothalamus and anterior pituitary gland
Regulation of gene suppression leads to systemic suppression of inflammation and immune response. This is of clinical usefulness but ultimately leads to gluconeogenesis, proteolysis and lipolysis. Gene transcription returns to normal after cessation, but sudden stoppage can cause Addison's disease. Osteoporosis is permanent.
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 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 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.