Methylprednisolone 21-acetate

Methylprednisolone acetate Repository injection 40 mg/mL 80 mg/mL 240 mg intramuscularly once 7.5 mg/kg intramuscularly once... 

A single intramuscular injection of a long-acting corticosteroid (e.g., methylprednisolone acetate) can be used as an alternative to the oral route if patients are unable to take oral therapy. If not contraindicated, low-dose colchicine can be used as adjunctive therapy to injectable corticosteroids to prevent rebound flare-ups. 

Intraarticular corticosteroid injections can provide relief, particularly when a joint effusion is present. Average doses for injection of large joints in adults are methylprednisolone acetate 20 to 40 mg or triamcinolone hexacetonide 10 to 20 mg. After aseptic aspiration of the effusion and corticosteroid injection, initial pain relief may occur within 24 to 72 hours, with peak relief occurring in about 1 week and lasting for 4 to 8 weeks. The patient should minimize joint activity and stress on the joint for several days after the injection. Therapy is generally limited to three or four injections per year because of the potential systemic effects of the drugs and because the need for more frequent injections indicates poor response to therapy. 

However, it is pertinent to mention here that certain steroids esterified at C-21 position, such as hydrocortisone acetate, methylprednisolone acetate are duly hydrolyzed in the alkaline medium to give rise to the corresponding free C-21 hydroxy steroids and hence, may also be assayed by adopting the same procedure. 

Methylprednisolone acetate - Not for IV use. As a temporary substitute for oral therapy, administer the total daily dose as a single IM injection. For prolonged effect, give a single weekly dose. 

Rheumatic Dz Adults. Intra-articular Hydrocortisone acetate 25-37.5 mg large joint, 10-25 mg small joint methylprednisolone acetate 20-80 mg large joint, 4-10 mg small joint. Intrabursal Hydrocortisone acetate 25-37.5 mg. Intraganglial Hydrocortisone acetate 25-37.5 mg. Tendon sheath Hydrocortisone acetate 5-12.5 mg. 

The mineralocorticosteroid activity of methyl-prednisolone is even less than that of prednisone/ prednisolone. It has a comparable duration of action. It is less suitable for substitution therapy in patients with adrenal hypofunctional states. Methyl-prednisolone sodium succinate is formulated for parental administration while methylprednisolone acetate is used for intra-articularly or peri-articularly injections. It can also be administered IM and then has prolonged systemic effects, lasting 1 weeks as the acetate is absorbed slowly from the site of injection. Oral absorption is rapid with peak effects within 1-2 hours. The duration of action is then about 1.5 days. 

Spinal cord injury IV Bolus 30 mg/kg over 15 min. Maintenance dose 5.4 mg/kg/hr over 23 hr, to be given within 45 min of bolus dose. IM (methylprednisolone acetate) 10-80 mg/day. Intra-artlcular, Intraleslonal 4-40 mg, up to 80 mg ql-5wk. 

Oral 2, 4, 8, 16, 24, 32 mg tablets Methylprednisolone acetate (generic, DepoMedrol)... 

Suspensions offer another dispersed platform for delivery of poorly water-soluble agents. As compared with solutions, suspensions afford higher loading. However, as with emulsions, the suspended particles must be stabilized with surfactants to prevent aggregation. A number of steroids have been available for years as suspensions for IM and intra-articular delivery. Examples include DEPO-MEDROL (Pfizer, Kalamazoo, Michigan, U.S.A.) Sterile Aqueous Suspension. The marketed product contains methylprednisolone acetate, a white, water-insoluble, crystalline... 

Mace S, Vadas P, Pruzanski W. Anaphylactic shock induced by intraarticular injection of methylprednisolone acetate. J Rheumatol 1997 24(6) 1191—4. 

An 11-year-old boy with iridocyclitis developed Cushing s syndrome, a posterior subcapsular cataract, and increased intraocular pressure in both eyes after the topical administration of prednisolone acetate 1 % eye-drops bilaterally for 6 months. The Cushing s syndrome was aggravated when periocular methylprednisolone acetate was started while bilateral posterior subtenon injections of 80 mg of suspension were continued every 6 weeks for 6 months. He had not used systemic glucocorticoids before. 

Contamination of catheters, with subsequent clinical infection, is a potential hazard of epidural analgesia. But not every suspected infection is what it seems aseptic meningitis has been described after an intradural injection of bupivacaine with methylprednisolone acetate (150). 

Methylprednisolone acetate (MPA) is a synthetic corticosteroid produced as the 6a-methyl derivative of prednisolone. Pharmacological studies of the esters of MPA show that it is rapidly converted to methylprednisolone, the active form. Reversible metabolism of methylpredniso/o to methyl-prednisoMC creates the inactive metabolite. The conversion from the prodrug to the active form of the drug is partially responsible for variations identified in the classification of the duration of MPA activity. High levels of the active product, methylprednisolone, have been identified in synovial fluid within 2 h of MPA injection. Despite the persistence of MPA levels for 5-39 days after injection, the active metabolite was only identifiable for 2-6 days (Auteflage et al 1986). 

Pelletier J, Mineau F, Raynauld J et al 1994 Intraarticular injections with methylprednisolone acetate reduce osteoarthritic lesions in parallel with chondrocyte stromelysin synthesis in experimental osteoarthritis. Arthritis and Rheumatism 37 414-423... 

Todhunter R J, Fubini S L, Wootton J A M et al 1996 Effect of methylprednisolone acetate on proteoglycan and collagen metabolism of articular cartilage explants. Journal of Rheumatology 23 1207-1213... 

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