methylprednisolone (systemic)
Medrol, Meprolone

methylprednisolone acetate
depMedalone 40, depMedalone 80, Depoject-40, Depoject-80, Depo-Medrol, Depopred-40, Depopred-80, Duralone-40, Duralone-80, Medralone, Methacort 40, Methylcotolone, Predacorten, Rep-Pred 40, Rep-Pred 80

methylprednisolone sodium succinate
A-Methapred, Solu-Medrol

Available forms
Available by prescription only
methylprednisolone
Tablets: 2 mg, 4 mg, 8 mg, 16 mg, 24 mg, 32 mg
methylprednisolone acetate
Injection: 20 mg/ml, 40 mg/ml, 80 mg/ml suspension
methylprednisolone sodium succinate
Injection: 40 mg, 125 mg, 500 mg, 1,000 mg, 2,000 mg/ vial

Indications and dosages
 Multiple sclerosis. methylprednisolone (systemic) Adults: 200 mg P.O. daily for 1 week, followed by 80 mg every other day for 1 month.
 Inflammation.
methylprednisolone
Adults: 2 to 60 mg P.O. daily in four divided doses, depending on disease being treated.
Children: 0.117 to 1.66 mg/kg daily or 3.3 to 50 mg/m² P.O. daily in three to four divided doses.
methylprednisolone acetate
Adults: 10 to 80 mg I.M. daily; or 4 to 80 mg into joints and soft tissue, p.r.n., q 1 to 5 weeks; or 20 to 60 mg intralesionally.
methylprednisolone sodium succinate
Adults: 10 to 250 mg I.M. or I.V. q 4 hours.
Children: 0.03 to 0.2 mg/kg or 1 to 6.25 mg/m² I.M. or I.V. daily in 1 or 2 divided doses.
 Shock. methylprednisolone sodium succinate. Adults: 100 to 250 mg I.V. at 2- to 6-hour intervals or 30 mg/kg I.V. initially and repeat q 4 to 6 hours, p.r.n. Or, after original I.V. push dose, 30 mg/kg I.V. infusion q 12 hours for 24 to 48 hours.
 Severe lupus nephritis ◇. Adults: 1 g I.V. over 1 hour for 3 days. Therapy is then continued orally at 0.5 mg/kg daily.
Children: 30 mg/kg I.V. every other day for six doses.
 Treatment or minimization of motor and sensory defects caused by acute spinal cord injury ◇. Adults: Initially, 30 mg/kg I.V. over 15 minutes followed in 45 minutes by I.V. infusion of 5.4 mg/kg/hour for 23 hours.
 Adjunct to moderate-severe Pneumocystis carinii pneumonia ◇. Adults and children older than age 13: 30 mg I.V. b.i.d. for 5 days; 30 mg I.V. daily for for 5 days; 15 mg I.V. daily for 11 days (or until completion of anti-infective regimen).

Pharmacodynamics
Anti-inflammatory action: Methylprednisolone suppresses the immune system by reducing activity and volume of the lymphatic system, thus producing lymphocytopenia (primarily of T lymphocytes), decreasing immunoglobulin and complement levels, decreasing passage of immune complexes through basement membranes, and possibly by depressing reactivity of tissue to antigen-antibody interactions.
 Drug is an intermediate-acting glucocorticoid. It has essentially no mineralocorticoid activity but is a potent glucocorticoid, with five times the potency of an equal weight of hydrocortisone. It’s used primarily as an anti-inflammatory and immunosuppressant.

Pharmacokinetics
Absorption: Absorbed readily after oral administration.
Distribution: Distributed rapidly to muscle, liver, skin, intestines, and kidneys. Adrenocorticoids are distributed into breast milk and through the placenta.
Metabolism: Metabolized in the liver to inactive glucuronide and sulfate metabolites.
Excretion: Inactive metabolites and small amounts of unmetabolized drug are excreted by the kidneys. Insignificant quantities of drug are excreted in feces. Biological half-life of methylprednisolone is 18 to 36 hours.

Contraindications and precautions
Contraindicated in patients allergic to any component of the formulation, in those with systemic fungal infections, and in premature infants (acetate and succinate).
  Use cautiously in patients with renal disease, GI ulceration, hypertension, osteoporosis, diabetes mellitus, hypothyroidism, cirrhosis, diverticulitis, nonspecific ulcerative colitis, recent intestinal anastomoses, thromboembolic disorders, seizures, myasthenia gravis, heart failure, tuberculosis, emotional instability, ocular herpes simplex, and psychotic tendencies.

Interactions
Drug-drug. Amphotericin B, diuretic therapy: May enhance hypokalemia. Monitor serum potassium level.
Antacids, cholestyramine, colestipol: Decreases corticosteroid effect. Separate administration times.
Anticholinesterase: Causes profound weakness. Use together cautiously.
Barbiturates, phenytoin, rifampin: May decrease corticosteroid effects because of increased hepatic metabolism. Monitor patient for potential dosage adjustment.
Cyclosporine: May increase cyclosporine levels. Use together cautiously.
Estrogens: Reduces metabolism of corticosteroids. Dosage adjustment may be needed.
Insulin, oral antidiabetics: Increases risk of hyperglycemia. Dosage adjustment may be needed.
Isoniazid, salicylates: Increases metabolism. Dosage adjustment of isoniazid or salicylates may be needed.
Oral anticoagulants: Decreases effectiveness. Monitor PT and INR.
Ulcerogenic drugs such as NSAIDs: Increases risk of GI ulceration. Use together cautiously.
Vaccines: Decreases effectiveness of vaccines. Vaccine shouldn’t be administered during corticosteroid therapy.

Adverse reactions
CNS: euphoria, insomnia, psychotic behavior, pseudotumor cerebri, vertigo, headache, paresthesia, seizures.
CV: heart failure, hypertension, edema, arrhythmias, thrombophlebitis, thromboembolism, fatal arrest or circulatory collapse (following rapid administration of large I.V. doses).
EENT: cataracts, glaucoma.
GI: peptic ulceration, GI irritation, increased appetite, pancreatitis, nausea, vomiting.
GU: menstrual irregularities.
Metabolic: hypokalemia, hyperglycemia, hypocalcemia, carbohydrate intolerance, growth suppression in children, cushingoid state (moonface, buffalo hump, central obesity).
Musculoskeletal: muscle weakness, osteoporosis.
Skin: delayed wound healing, acne, various skin eruptions, hirsutism.
Other: susceptibility to infections, acute adrenal insufficiency that may occur with increased stress (infection, surgery, or trauma) or abrupt withdrawal after long-term therapy.

Effects on lab test results
• May increase glucose and cholesterol levels. May decrease potassium and calcium levels.

Overdose and treatment
Acute ingestion, even in massive doses, is rarely a clinical problem. Toxic signs and symptoms rarely occur if drug is used for less than 3 weeks, even at large doses. However, chronic use causes adverse physiologic effects, including suppression of the hypothalamus-pituitary-adrenal axis, cushingoid appearance, muscle weakness, and osteoporosis.
 Gradually taper dosage. Treat patient symptomatically.

Special considerations
• Most adverse reactions to corticosteroids are dose- or duration-dependent.
• Methylprednisolone may be administered orally. Methylprednisolone sodium succinate may be administered by I.M. or I.V. injection or by I.V. infusion, usually at 4- to 6-hour intervals.
• Methylprednisolone acetate suspension may be administered by intra-articular, intramuscular, intrasynovial, intrabursal, intralesional, or soft tissue injection. It has a slow onset but a long duration of action.
• Determine whether patient is sensitive to other corticosteroids.
• Most adverse reactions to corticosteroids are dose- or duration-dependent.
• For better results and less toxicity, give a once-daily dose in the morning.
• Give oral dose with food when possible. Critically ill patients may need concomitant antacid or H₂-receptor antagonist therapy.
• Salt forms aren’t interchangeable.
 ALERT Don’t give Solu-Medrol intrathecally because severe adverse reactions have been reported.
• Give I.M. injection deep into gluteal muscle. Avoid S.C. injection because atrophy and sterile abscesses may occur.
• Dermal atrophy may occur with large doses of acetate salt. Use several small injections rather than a single large dose, and rotate injection sites.
• Don’t use acetate if immediate onset of action is needed.
• Discard reconstituted solution after 48 hours.
• Always adjust to lowest effective dose.
• Gradually reduce dosage after long-term therapy.
• Unless contraindicated, give low-sodium diet that’s high in potassium and protein. Administer potassium supplements as needed.
 ALERT Don’t confuse Solu-Medrol with Solu-Cortef (hydrocortisone sodium succinate) or methylprednisolone with medroxyprogesterone.
 ALERT Use only methylprednisolone sodium succinate for I.V. route; never use acetate form. Reconstitute according to manufacturer’s directions using supplied diluent, or use bacteriostatic water for injection with benzyl alcohol.
• When administering as direct injection, inject diluted drug into vein or free-flowing compatible I.V. solution over at least 1 minute. For shock, give massive doses over at least 10 minutes to prevent arrhythmias and circulatory collapse. When administering as an intermittent or continuous infusion, dilute solution according to manufacturer’s instructions, and give over prescribed duration. If used for continuous infusion, change solution every 24 hours.
• Monitor patient’s weight, blood pressure, serum electrolyte levels, and sleep patterns. Euphoria may initially interfere with sleep, but patients typically adjust to therapy in 1 to 3 weeks.
• Monitor patient for cushingoid effects, including moonface, buffalo hump, central obesity, thinning hair, hypertension, and increased susceptibility to infection.
• Drug may mask or worsen infections, including latent amebiasis.
• Watch for depression or psychotic episodes, especially in high-dose therapy.
• Diabetic patient may need increased insulin; monitor blood glucose level.
• Watch for an enhanced response to drug in patients with hypothyroidism or cirrhosis.
• Watch for allergic reaction to tartrazine in patients with sensitivity to aspirin.
Pediatric patients
• Long-term use of adrenocorticoids in children and adolescents may delay growth and maturation.
Geriatric patients
• Compare the risks and benefits of corticosteroid use; lower doses are recommended. Elderly patients may be more susceptible to osteoporosis with prolonged use.
• Monitor blood pressure and blood glucose and electrolyte levels at least every 6 months.

Patient education
• Tell patient not to stop drug abruptly or without medical consent.
• Instruct patient to take oral form of drug with food.
• Teach patient early signs of adrenal insufficiency: fatigue, muscle weakness, joint pain, fever, anorexia, nausea, dyspnea, dizziness, and fainting.
• Tell patient to carry a card identifying need for supplemental systemic steroids during stress. Medication, dose, and name of prescriber should appear on card.
• Teach patient on long-term therapy to report sudden weight gain or swelling.
• Tell patient on long-term therapy to call about the need for vitamin D or calcium supplement, or a physical exercise program.
• Warn patient to avoid exposure to infections (such as chickenpox or measles) and to report if such exposure occurs.

Reactions may be common, uncommon, life-threatening, or COMMON AND LIFE THREATENING.
◆ Canada only
◇ Unlabeled clinical use