Methylprednisolone Sodium Succinate is indicated in the following conditions:

Endocrine disorders: Primary or secondary adrenocortical insufficiency, acute adrenocortical insufficiency, shock unresponsive to conventional therapy, congenital adrenal hyperplasia, nonsuppurative thyroiditis, hypercalcemia associated with cancer.

Rheumatic disorders: Rheumatoid arthritis including juvenile rheumatoid arthritis, acute and subacute bursitis, epicondylitis, acute nonspecific tenosynovitis, acute gouty arthritis, psoriatic arthritis, ankylosing spondylitis.

Collagen diseases: During exacerbation or maintenance therapy in selected cases of systemic lupus erythematosus, acute rheumatic carditis, systemic dermatomyositis (polymyositis).

Dermatological diseases: Pemphigus, severe erythema multiforme (Stevens-Johnson syndrome), exfoliative dermatitis, bullous dermatitis herpetiformis, severe seborrheic dermatitis, severe psoriasis, mycosis fungoides.

Allergic states: Bronchial asthma, contact dermatitis, atopic dermatitis, serum sickness, seasonal or perennial allergic rhinitis, drug hypersensitivity reactions, urticarial transfusion reactions, acute noninfectious laryngeal edema (epinephrine is first line), anaphylactic reactions.

Ophthalmic diseases: Severe acute and chronic allergic and inflammatory eye conditions such as herpes zoster ophthalmicus, iritis, iridocyclitis, chorioretinitis, posterior uveitis, choroiditis, optic neuritis, sympathetic ophthalmia, anterior segment inflammation, allergic conjunctivitis, allergic corneal ulcers, keratitis.

Gastrointestinal diseases: Ulcerative colitis, regional enteritis, Crohn’s disease during acute exacerbations.

Respiratory diseases: Symptomatic sarcoidosis, berylliosis, fulminating or disseminated pulmonary tuberculosis (with antitubercular therapy), Loeffler’s syndrome not manageable by other means, aspiration pneumonitis.

Hematologic disorders: Acquired autoimmune hemolytic anemia, idiopathic thrombocytopenic purpura in adults (IV only; IM contraindicated), erythroblastopenia, congenital hypoplastic anemia, secondary thrombocytopenia in adults.

Neoplastic diseases: Palliative management of leukemias and lymphomas in adults, acute leukemia of childhood.

Edematous states: To induce diuresis or remission of proteinuria in nephrotic syndrome without uremia, idiopathic type or lupus erythematosus-related.

Miscellaneous: Tuberculous meningitis with subarachnoid block or impending block (with antituberculosis chemotherapy), trichinosis with neurologic or myocardial involvement.

Methylprednisolone Sodium Succinate is a synthetic glucocorticoid used as replacement therapy in adrenocortical insufficiency and primarily for its potent anti-inflammatory and immunosuppressive effects across multiple organ systems. After intravenous administration, effects appear within one hour and persist for a variable duration. The drug is almost completely eliminated within 12 hours; therefore, if continuous high blood levels are required, dosing every 4–6 hours may be needed. It is also rapidly absorbed after intramuscular injection with similar elimination pattern. Its anti-inflammatory potency is approximately 5:4 compared to prednisolone. It has minimal mineralocorticoid activity and a lower tendency to cause sodium and water retention than prednisolone. It influences carbohydrate, protein, fat and purine metabolism, electrolyte and water balance, and affects cardiovascular, renal, skeletal muscle, nervous system, and other organ functions. It also suppresses immune responses.

Methylprednisolone may be administered by IM or IV or by IV infusion. To administer by IM or IV injection, prepare solution as direction for reconstitution. The desired dose may be administered intravenously over a period of several minutes. When high dose therapy is desired, the recommended dose of Methylprednisolone Sodium Succinate for Injection, USP is 30 mg/kg administered intravenously over at least 30 minutes. This dose may be repeated every 4 to 6 hours for 48 hours. In general, high-dose corticosteroid therapy should be continued only until the patient’s condition has stabilized usually not beyond 48 to 72 hours.

Although adverse effects associated with high dose short-term corticoid therapy are uncommon, peptic ulceration may occur. Prophylactic antacid therapy may be indicated.

In other indications, the initial dosage will vary from 10 to 40 mg of Methylprednisolone depending on the clinical problem being treated. The larger doses may be required for short-term management of severe, acute conditions. The initial dose usually should be given intravenously over a period of several minutes. Subsequent doses may be given intravenously or intramuscularly at intervals dictated by the patient’s response and clinical condition. Corticoid therapy is an adjunct to, and not a replacement for conventional therapy.

Dosage must be decreased or discontinued gradually when the drug has been administered for more than a few days. If a period of spontaneous remission occurs in a chronic condition, treatment should be discontinued. Routine laboratory studies, such as urinalysis, two-hour postprandial blood sugar, determination of blood pressure and body weight, and a chest X-ray should be made at regular intervals during prolonged therapy. Upper GI X-rays are desirable in patients with an ulcer history or significant dyspepsia.

In pediatric patients, the initial dose of Methylprednisolone may vary depending on the specific disease being treated. The initial dose is 0.11–1.6 mg/day in three or four divided doses. Dosage may be reduced for infants and children but should be governed more by the severity of the condition and response of the patient than by age or size but it should not be less than 0.5 mg per kg every 24 hours.

In the treatment of acute exacerbations of multiple sclerosis daily doses is 160 mg daily for 3 days.

Methylprednisolone Sodium Succinate powder for injection/infusion should be given as an intravenous infusion over at least 30 minutes.

• Aminoglutethimide may lead to a loss of corticosteroid-induced adrenal suppression.
• Amphotericin B injection and potassium-depleting agents—When corticosteroids are administered concomitantly with potassium-depleting agents (i.e., amphotericin B, diuretics), patients should be observed closely for the development of hypokalemia.
• Macrolide antibiotics have been reported to cause a significant decrease in corticosteroid clearance.
• Anticholinesterases—Concomitant use of anticholinesterase agents and corticosteroids may produce severe weakness in patients with myasthenia gravis. If possible, anticholinesterase agents should be withdrawn at least 24 hours before initiating corticosteroid therapy.
• Anticoagulants, oral—Coadministration of corticosteroids and warfarin usually results in inhibition of response to warfarin, although there have been some conflicting reports.
• Antidiabetics—Because corticosteroids may increase blood glucose concentrations, dosage adjustments of antidiabetic agents may be required.
• Antitubercular drugs—Serum concentrations of isoniazid may be decreased.
• Cholestyramine may increase the clearance of corticosteroids.
• Cyclosporine—Increased activity of both cyclosporine and corticosteroids may occur when used concurrently. Convulsions have been reported.
• Digitalis glycosides—Patients may be at increased risk of arrhythmias due to hypokalemia.
• Estrogens, including oral contraceptives—May decrease hepatic metabolism of corticosteroids, increasing their effect.
• Hepatic enzyme inhibitors—Drugs inhibiting cytochrome P450 3A4 may increase plasma corticosteroid concentrations.
• Ketoconazole may significantly decrease corticosteroid metabolism (up to 60%), increasing risk of side effects.
• NSAIDs—Concomitant use increases risk of gastrointestinal side effects.
• Skin tests—Corticosteroids may suppress skin test reactions.
• Vaccines—Prolonged corticosteroid therapy may reduce response to vaccines and toxoids.

Methylprednisolone Sodium Succinate sterile powder is contraindicated:

• In systemic fungal infections and in patients with known hypersensitivity to the product or its constituents.
• For intrathecal administration (severe adverse events reported).
• Intramuscular corticosteroid preparations are contraindicated in idiopathic thrombocytopenic purpura.

Fluid and electrolyte disturbances: Sodium retention, fluid retention, congestive heart failure in susceptible patients, potassium loss, hypokalemic alkalosis, hypertension.

Musculoskeletal: Muscle weakness, steroid myopathy, loss of muscle mass, severe arthralgia, vertebral compression fractures, avascular necrosis of femoral and humeral heads, pathologic fractures, osteoporosis.

Gastrointestinal: Peptic ulcer with perforation/hemorrhage, pancreatitis, abdominal distention, ulcerative esophagitis.

Dermatologic: Impaired wound healing, thin fragile skin, petechiae, ecchymoses, facial erythema, increased sweating, suppressed skin test reactions.

Neurological: Increased intracranial pressure with papilledema (pseudotumor cerebri), convulsions, vertigo, headache.

Endocrine: Cushingoid state, growth suppression in children, secondary adrenal and pituitary suppression, menstrual irregularities, glucose intolerance, latent diabetes activation, increased insulin/oral hypoglycemic requirement.

Ophthalmic: Posterior subcapsular cataracts, increased intraocular pressure, glaucoma, exophthalmos.

Others: Negative nitrogen balance due to protein catabolism.

Additional parenteral reactions: Hyperpigmentation or hypopigmentation, subcutaneous atrophy, sterile abscess, anaphylactic reaction (with or without circulatory collapse), cardiac arrest, bronchospasm, urticaria, nausea, vomiting, arrhythmias, hypo/hypertension.

Pregnancy: Corticosteroids are teratogenic in animals. No adequate human studies exist. Use only if benefit outweighs fetal risk. Infants should be monitored for adrenal suppression.

Lactation: Systemic corticosteroids pass into breast milk and may affect infant growth and adrenal function. A decision should be made to discontinue breastfeeding or the drug.

Methylprednisolone Sodium Succinate is heat sensitive and should not be autoclaved. Lowest effective dose should be used, and tapering should be gradual. Risk-benefit assessment is required for dose and duration. Chronic conditions may improve after discontinuation.

Pediatric Use: Adverse effects similar to adults. Monitor blood pressure, growth, intraocular pressure, infection, and metabolic effects. Growth velocity may decrease; use lowest effective dose.

Geriatric Use: Start at lower end of dose range due to reduced hepatic, renal, or cardiac function and comorbidities.

Acute overdose requires supportive and symptomatic treatment. In chronic overdose, dose reduction or alternate-day therapy may be used cautiously.

Glucocorticoids

Protect from light. Store at 20°–25°C. Prepared solution should also be stored at 20°–25°C and used within 48 hours.