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Author: Admin | 2025-04-28
Methylprednisolone acetate (Depo-Medrol) and methylprednisolone succinate (Solu-Medrol) are approved for intramuscular injection.[23][22] Depo-Medrol is additionally approved for intralesional, intra-articular, and soft tissue injections. Depo-Medrol is available as sterile aqueous solution in 20 mg/mL, 40 mg/mL, or 80 mg/mL strengths.[23] Solu-Medrol is the only derivative of methylprednisolone that is approved for intravenous infusion, as the sterile powder is soluble in water and can be mixed with a diluent. Strengths vary from 40 mg to 2 g.[22]Synthetic glucocorticoids are similar to endogenous steroids in metabolism but differ in affinity for glucocorticoid and mineralocorticoid receptors, affinity for protein-binding, rate of elimination, and metabolic products.[4]Oral methylprednisolone is readily absorbed from the gastrointestinal tract with a bioavailability of 89.9%.[38] In contrast to endogenous GCs, methylprednisolone does not bind to the glycoprotein transcortin (corticosteroid-binding globulin, CBG) but does have moderate protein binding to albumin.[32] Thus, the pharmacokinetics of methylprednisolone are linear and show no dose dependency.[32] Patients exhibiting low albumin concentrations are at risk for adverse effects during glucocorticoid therapy.[32] Oral methylprednisolone has a moderate distribution into tissue at 1.38L/kg.[39]Methylprednisolone is primarily eliminated by hepatic metabolism and renal excretion of metabolites; with renal excretion of unchanged methylprednisolone at only 1.3–9.2%.[39] Methylprednisolone can be interconverted with methylprednisone.[32] Hepatic metabolism is mediated by 11 beta-hydroxysteroid dehydrogenases (11[beta]-HSD) and 20-ketosteroid reductases.[39] Methylprednisolone undergoes renal excretion of hydrophilic inactive metabolites, including 20-carboxymelthylprednisolone and 6[beta]-hydroxy-20[alpha]-hydroxymethylprednisolone.[32]Physical properties[edit]Oral methylprednisolone (Medrol) and its derivatives are a white, odorless crystalline powder. Its solubility ranges from practically insoluble in water, very slightly soluble in ether, slightly soluble in acetone and chloroform to sparingly soluble in alcohol, dioxane, and methanol.[40] Methylprednisolone acetate suspension (Depo-Medrol) is a 6-methyl derivative of prednisolone that melts at 215 degrees Celsius with some decomposition.[23] Methylprednisolone sodium succinate (Solu-Medrol) is the sodium succinate ester of methylprednisolone. Contrary to the solubilities above, methylprednisolone sodium succinate is soluble in water and alcohol, slightly soluble in acetone and insoluble in chloroform[22]Depo-Medrol (methylprednisolone acetate) injectable suspensionMethylprednisolone, or 6α-methylprednisolone, also known as 11β,17,21-trihydroxy-6α-methylpregna-1,4-diene-3,20-dione, is a synthetic pregnane steroid and a derivative of hydrocortisone (11β,17α,21-trihydroxypregn-4-ene-3,20-dione) and prednisolone (11β,17α,21-trihydroxypregn-1,4-diene-3,20-dione).[41][42] A variety of methylprednisolone esters with differing characteristics exist and have been marketed for medical use.[41][42] They include methylprednisolone aceponate (Advantan), methylprednisolone acetate (Depo-Medrol), methylprednisolone succinate (Solu-Medrol), and methylprednisolone suleptanate (Medrosol, Promedrol).[41][42]Synthetic steroids are synthesized from cholic acid and sapogenins obtained from cattle and plants, respectively.[4]Synthesis of MethylprednisoloneMethylprednisolone was first synthesized and manufactured by The Upjohn Company (now Pfizer) and Food and Drug Administration (FDA) approved in the United States in October 1957.[10] The patent has expired, and generics are available. In 2022, it was the 153rd most commonly prescribed medication in the United States, with more than 3 million prescriptions.[11][12]Methylprednisolone has been a prescribed therapy amidst the COVID-19 pandemic, but there is no evidence it is either safe or effective for this purpose.[43][44]^ "Methylprednisolone Use During Pregnancy". Drugs.com. 20 August 2019. Retrieved 20 February 2020.^ "Product monograph brand safety updates". Health Canada. 7 July 2016. Retrieved 3 April 2024.^ "List of nationally authorised medicinal products: Active substance: methylprednisolone: Procedure no.
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