Brands, Medical Use, Clinical Data
Drug Category
- Neuroprotective Agents
- Glucocorticoids
- Antiemetics
- Anti-inflammatory Agents
- Adrenergic Agents
Dosage Forms
Brands / Synonyms
; 6alpha-Methylprednisolone; A-Methapred; Artisone-Wyeth; Besonia; Cortalone; Delta-Cortef; Depo-Medrol; Dopomedrol; Esametone; Fernisolone-P; Firmacort; Lemod; M-Predrol; Medesone; Medixon; Medlone 21; Medrate; Medrol; Medrol Acetate; Medrol Adt Pak; Medrol Dosepak; Medrone; MEPRDL; Mesopren; Metastab; Methyleneprednisolone; Methylprednisolon; Methylprednisolone; Methylprednisolone Acetate; Methylprednisolone Sodium Succinate; Methylprednisolone, Pharma; Methylprednisolonum [Inn-Latin]; Meti-Derm; Metilbetasone; Metilprednisolona [Inn-Spanish]; Metilprednisolone [Dcit]; Metrisone; Metrocort; Metysolon; Moderin; Nirypan; Noretona; Predni N Tablinen; Prednisolone; Prelone; Promacortine; Reactenol; Sieropresol; Solomet; Solu-Medrol; Sterane; Summicort; Suprametil; Urbason; Urbasone; Wyacort
Indications
Adjunctive therapy for short-term administration in rheumatoid arthritis.
Pharmacology
Methylprednisolone and its derivatives, methylprednisolone sodium succinate and methylprednisolone acetate, are synthetic glucocorticoids used as antiinflammatory or immunosuppressive agents.
Mechanism of Action
Unbound glucocorticoids cross cell membranes and bind with high affinity to specific cytoplasmic receptors, modifying transcription and protein synthesis. By this mechanism, glucocorticoids can inhibit leukocyte infiltration at the site of inflammation, interfere with mediators of inflammatory response, and suppress humoral immune responses. The antiinflammatory actions of corticosteroids are thought to involve phospholipase A2 inhibitory proteins, lipocortins, which control the biosynthesis of potent mediators of inflammation such as prostaglandins and leukotrienes.
Absorption
Oral bioavailability 80-99%
Toxicity
LD50=2000 mg/kg (orally in rat)
Biotrnasformation / Drug Metabolism
Hepatic
Contraindications
Systemic fungal infections and known hypersensitivity to components.
Drug Interactions
The pharmacokinetic interactions listed below are potentially clinically important. Mutual inhibition of
metabolism occurs with concurrent use of cyclosporin and methylprednisolone; therefore, it is possible that adverse
events associated with the individual use of either drug may be more apt to occur. convulsions have been reported
with concurrent use of methylprednisolone and cyclosporin. Drugs that induce hepatic enzymes such as phenobarbital,
phenytoin, and rifampin may increase the clearance of methylprednisolone and may require increased in
methylprednisolone dose to achieve the desired response. Drugs such as troleandomycin and ketoconazole may inhibit
the metabolism of methylprednisolone and thus decrease its clearance. Therefore, the dose of methylprednisolone
should be titrated to avoid steroid toxicity.
Methylprednisolone may increase the clearance of chronic high dose aspirin. This could lead to decreased
salicylate serum levels or increase the risk of salicylate toxicity when methylprednisolone is withdrawn. Aspirin
should be used cautiously in conjunction with corticosteroids in patients suffering from hypoprothrombinemia.
The effect of methylprednisolone on oral anticoagulants is variable. There are reports of enhanced as well as
diminished effects of anticoagulant when given concurrently with corticosteroids. Therefore, coagulation indices
should be monitored to maintain the desired anticoagulant effect.
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