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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.
Methylprednisolone succinate, sold under the brand name Solu-Medrol among others, is a synthetic glucocorticoid corticosteroid and a corticosteroid ester—specifically the C21 succinate ester of methylprednisolone—which is used by intravenous administration.
[1] [4] [5] Methylprednisolone acetate was previously suspended with polyethylene glycol but is no longer formulated with this excipient due to concerns about possible toxicity. [6] [8] Depo methylprednisolone acetate is a depot injection and is absorbed slowly with a duration of weeks to months with a single intramuscular injection. [5]
Prednisolone has a relatively short half-life, ranging 2–4 hours. It also has a large therapeutic window, considering the dosage required to produce a therapeutic effect is a few times higher than what the body naturally produces. [14] Prednisolone is 70–90% plasma protein bound, it binds to proteins such as albumin. [14]
[6] [7] [8] Applying once daily is enough as it is as effective as twice or more daily application. [9] To prevent tachyphylaxis, a topical steroid is often prescribed to be used on a week on, week off routine. Some recommend using the topical steroid for 3 consecutive days on, followed by 4 consecutive days off. [10]
Prednisone is a prodrug and must be converted to prednisolone by the liver before it becomes active. [6] [7] Prednisolone then binds to glucocorticoid receptors, activating them and triggering changes in gene expression. [4] Prednisone was patented in 1954 and approved for medical use in the United States in 1955.
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Δ 7-Prednisolone 21-acetate; Alclometasone dipropionate; Amcinonide (triamcinolone acetate cyclopentanonide); Chloroprednisone acetate; Ciclometasone (a corticosteroid 21-[4-[(acetylamino)methyl]cyclohexyl]carboxylate ester)
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