Methylprednisolone succinate and acetate

Methylprednisolone Succinate and Acetate (Solu-Medrol, DepO Medrol) [Steroid] Uses Tx inflammation d/t anaphylaxis and asthma suspected SCI Action Adrenal corticost oid Dose Adul. Anaphylaxis/ status asthmaticus 125-250 mg IV/EM Suspected SCI Load w/ 30 mg/kg then inf... 

The prodrug approach described above also can be used to alter the solubility characteristics, which, in turn, can increase the flexibility in formulating dosage forms. The solubility of methylprcdnisolonc can be altered from essentially water-insoluble methylpredni.solone acetate to slightly water-insoluble methylprednisolone to water-soluble meth-ylprednisolone. sodium succinate. The water-soluble sodium hemisuccinate salt is used in oral, intravenous, and intramuscular dosage forms. Methylprednisolone itself is normally found in tablels. The acetate ester is found in topical ointments and sterile aqueous suspensions for intramuscular injection. Both the succinate and acetate esters are hydrolyzed to the active methylprednisolone by the patient s own systemic hydrolytic enzymes (esterases). 

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. 

Anaphylactic shock has been described after intranasal hydrocortisone acetate, intramuscular methylprednisolone (SEDA-21, 419) (251), intravenous methylprednisolone (SEDA-22, 448) (252), intramuscular dexamethasone (SEDA-22, 448) (253), and intra-articular methylprednisolone (SEDA-22, 449) (254). A life-threatening anaphylac-tic-like reaction to intravenous hydrocortisone has been described in patients with asthma (255). Acute laryngeal obstruction has been described for the first time after the intravenous administration of hydrocortisone (SEDA-22, 449) (256). There is some reason to believe that sodium succinate esters are more likely to cause hypersensitivity reactions (SEDA-17, 449), but unconjugated glucocorticoids can definitely produce allergy in some cases (SEDA-16, 452). 

---