Pharmacology Of Methylprednisolone

Indication Adjunctive therapy for short-term administration in rheumatoid arthritis.
Pharmacodynamics 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%
Volume of distribution Not Available
Protein binding 78%
Metabolism Hepatic
Route of elimination Not Available
Half life 1-3 hours
Clearance Not Available
Toxicity LD50=2000 mg/kg (orally in rat)