DrugindexOnline^{2nd edition}

Pronouncation: (METH-ill-pred-NIH-suh-lone)
Class: Glucocorticoid

Trade Names:
Medrol
- Tablets 2 mg
- Tablets 4 mg
- Tablets 8 mg
- Tablets 16 mg
- Tablets 24 mg
- Tablets 32 mg

Depo-Medrol (Canada)
Methylprednisolone Sodium Succinate

Trade Names:
A-Methapred
- Powder for injection 125 mg per vial
- Powder for injection 500 mg per vial
- Powder for injection 1 g per vial

Trade Names:
Solu-Medrol
- Powder for injection 125 mg per vial
- Powder for injection 500 mg per vial
- Powder for injection 1 g per vial
- Powder for injection 2 g per vial

Methylprednisolone Acetate

Trade Names:
depMedalone 40
- Injection 40 mg/mL suspension

Trade Names:
depMedalone 80
- Injection 80 mg/mL suspension

Trade Names:
Depo-Medrol
- Injection 20 mg/mL suspension
- Injection 40 mg/mL suspension
- Injection 80 mg/mL suspension

Trade Names:
Duralone-40
- Injection 40 mg/mL suspension

Trade Names:
Duralone-80
- Injection 80 mg/mL suspension

Trade Names:
Medralone 40
- Injection 40 mg/mL suspension

Trade Names:
Medralone 80
- Injection 80 mg/mL suspension

Mechanism of Action

Pharmacology

Depresses formation, release and activity of endogenous mediators of inflammation including prostaglandins, kinins, histamine, liposomal enzymes and complement system. Modifies body's immune response.

Pharmacokinetics

Elimination

Plasma t _{1/ 2} is longer than 3.5 hr.

Onset

Onset is 6 to 48 hr (IM).

Peak

Times to peak effect are 4 to 8 days (IM) and 1 to 2 hr (oral).

Duration

Durations are 1.25 to 1.5 days (oral) and 1 to 4 wk (IM).

Indications and Usage

Replacement therapy in primary or secondary adrenal cortex insufficiency; adjunctive therapy for short-term administration in rheumatic disorders; exacerbation or maintenance therapy in collagen diseases; treatment of dermatologic diseases; control of allergic states or allergic and inflammatory ophthalmic processes; management of respiratory diseases; treatment of hematologic disorders; palliative management of neo-plastic diseases; management of cerebral edema associated with primary or metastatic brain tumor, craniotomy or head injury; induction of diuresis in edematous states (from nephrotic syndrome); management of critical exacerbations of GI diseases; management of acute exacerbations of multiple sclerosis; treatment of tuberculous meningitis; management of trichinosis with neurologic or myocardial involvement.

Intra-articular or soft tissue administration

Adjunctive therapy for short-term administration in synovitis of osteoarthritis, rheumatoid arthritis, bursitis, acute gouty arthritis, epicondylitis, acute nonspecific tenosynovitis and posttraumatic osteoarthritis.

Intralesional administration

Management of keloids; treatment of localized hypertrophic, infiltrated, inflammatory lesions of lichen planus, psoriatic plaques, granuloma annulare, lichen simplex chronicus; treatment of discoid lupus erythematosus, necrobiosis lipoidica diabeticorum, alopecia areata and cystic tumors of aponeurosis or tendon.

Unlabeled Uses

Reduction of mortality in severe alcoholic hepatitis; prevention of respiratory distress syndrome; treatment of septic shock; improvement of neurologic function in acute spinal cord injury.

Contraindications

Systemic fungal infections; idiopathic thrombocytopenic purpura (IM administration); administration of live virus vaccines; topical monotherapy in primary bacterial infections; topical use on face, groin or axilla; use in premature infants (sodium succinate salt).

Dosage and Administration

Methylprednisolone
Adults

PO 4 to 48 mg/day.

Methylprednisolone Sodium Succinate
Adults

IV/IM 10 to 40 mg administered over 1 to several min. In severe condition, 30 mg/kg infused over 30 min; may repeat q 4 to 6 hr for 48 to 72 hr.

Infants and Children

IV/IM Not less than 0.5 mg/kg/24 hr.

Methylprednisolone Acetate
Adults

IM 40 to 120 mg q wk for 1 to 4 wk. Intra-articular/intralesional 4 to 80 mg into joints or lesions.

General Advice

• Administer once-daily dose or alternate-day dosing in morning before 9 am.
• With intra-articular injection, inject into synovial space. Do not inject unstable joints.
• When treating conditions such as tendonitis or tenosynovitis, inject into tendon sheath rather than into substance of tendon.
• When treating conditions such as epicondylitis, outline area of greatest tenderness and infiltrate drug into area.
• When treating ganglia of tendon sheaths, inject drug directly into cyst.
• When treating dermatologic conditions, avoid injection of sufficient material to cause blanching, which may cause small slough.
• Do not inject into deltoid muscle. Administer IM injection deeply into gluteal muscle.
• Although methylprednisolone sodium succinate can be given both IM and IV, methylprednisolone acetate can only be administered IM; it cannot be administered IV.
• Do not use topically on face, groin, or axilla.

Storage/Stability

Store at room temperature (59° to 86°F).

Drug Interactions

Anticholinesterases

May antagonize anticholinesterase effects in myasthenia gravis.

Barbiturates

May decrease pharmacologic effect of methylprednisolone.

Hydantoins, rifampin

May increase clearance and decrease efficacy of methylprednisolone.

Ketoconazole

May decrease clearance of methylprednisolone.

Macrolide antibiotics

Significantly decreases methylprednisolone clearance; may need to decrease dose.

Salicylates

May reduce serum levels and efficacy of salicylates.

Laboratory Test Interactions

Drug may cause increased levels of urine glucose and serum cholesterol, decreased serum levels of potassium, T ₃ and T ₄ , decreased uptake of thyroid I ¹³¹ , false-negative result in nitroblue-tetrazolium test for systemic bacterial infection and suppression of skin-test reactions.

Adverse Reactions

Cardiovascular

Thromboembolism or fat embolism; thrombophlebitis; necrotizing angiitis; cardiac arrhythmias or ECG changes; syncopal episodes; hypertension; myocardial rupture; fatal arrest; circulatory collapse; CHF.

CNS

Convulsions; pseudotumor cerebri (increased intracranial pressure with papilledema); vertigo; headache; neuritis; paresthesias; psychosis.

Dermatologic

Impaired wound healing; thin, fragile skin; petechiae and ecchymoses; erythema; lupus erythematosus-like lesions; subcutaneous fat atrophy; striae; hirsutism; acneiform eruptions; allergic dermatitis; urticaria; angioneurotic edema; perineal irritation; hyperpigmentation or hypopigmentation; burning, itching, irritation, dryness, folliculitis, hypertrichosis, pruritus, perioral dermatitis, allergic contact dermatitis, stinging, cracking and tightening of skin, secondary infections, skin atrophy, miliaria, telangiectasia (topical).

EENT

Posterior subcapsular cataracts; increased intraocular pressure; glaucoma; exophthalmos.

GI

Pancreatitis; abdominal distention; ulcerative esophagitis; nausea; vomiting; increased appetite and weight gain; peptic ulcer with perforation and hemorrhage; bowel perforation.

Genitourinary

Increased or decreased motility and number of spermatozoa.

Hematologic

Leukocytosis.

Metabolic

Sodium and fluid retention; hypokalemia; hypokalemic alkalosis; metabolic alkalosis; hypocalcemia.

Miscellaneous

Musculoskeletal effects (eg, weakness, myopathy, muscle mass loss, osteoporosis, spontaneous fractures); endocrine abnormalities (eg, menstrual irregularities, cushingoid state, growth suppression in children, sweating, decreased carbohydrate tolerance, hyperglycemia, glycosuria, increased insulin or sulfonylurea requirements in diabetic patients, hirsutism); anaphylactoid or hypersensitivity reactions; aggravation or masking of infections; fatigue; insomnia; osteonecrosis, tendon rupture, infection, skin atrophy, postinjection flare, hypersensitivity, facial flushing (intra-articular administration). Topical application may produce adverse reactions seen with systemic use because of absorption.

Precautions

Pregnancy

Pregnancy category undetermined (systemic use); Category C (topical use).

Lactation

Excreted in breast milk.

Children

May be more susceptible to adverse effects from topical use. Benzyl alcohol/gasping syndrome may occur with use of methylprednisolone sodium succinate.

Elderly

May require lower doses.

Hypersensitivity

Reactions, including anaphylaxis, may occur rarely.

Tartrazine Sensitivity

May contain tartrazine, which may cause allergic-type reactions in susceptible individuals.

Adrenal suppression

Prolonged therapy may lead to hypothalamic-pituitary-adrenal suppression.

Hepatitis

Drug may be harmful in chronic active hepatitis positive for hepatitis B surface antigen.

Immunosuppression

Because drug causes immunosuppressed state, do not administer live virus vaccines during treatment.

Infections

May mask signs of infection. May decrease host-defense mechanisms to prevent dissemination of infection.

Ocular effects

Use drug systemically with caution in ocular herpes simplex because of risk of possible corneal perforation.

Peptic ulcer

Drug may contribute to peptic ulceration, especially in large doses.

Repository injections

Do not inject subcutaneously. Avoid injection into deltoid muscle and repeated intramuscular injection into same site.

Stress

Increased dosage of rapidly acting corticosteroid may be needed before, during and after stressful situations.

Overdosage

Symptoms

Cushingoid changes, moonface, central obesity, striae, hirsutism, acne, ecchymoses, hypertension, osteoporosis, myopathy, sexual dysfunction, diabetes mellitus, hyperlipidemia, peptic ulcer, increased susceptibility to infection, electrolyte and fluid imbalance.

Patient Information

• Instruct patient to take medication at same time each day and with food if taking orally.
• With cream or ointment application, instruct patient to soak area of skin before gently applying light film of medication, to increase absorption. Caution patient to wash hands before and after application.
• Encourage patient to eat low-sodium, low-fat foods.
• Advise patient to practice frequent, thorough handwashing to help to prevent infections.
• Advise patient on chronic steroid therapy to wear or carry identification (eg, Medi-Alert ) indicating condition and medication regimen.
• Inform patient of potential for mood swings.
• Warn patient regarding increasing appetite and consequent weight gain. Instruct patient to weigh self daily.
• Inform patient of moonface, which often occurs with this medication.
• Advise patient of acne and skin flushing, which are often associated with this medication. Instruct patient in proper skin care practices to help to prevent irritation and/or acne.
• Instruct patient to report the following symptoms to health care provider: swelling in feet and ankles, signs of infection (eg, fever, over-growth in mouth, vaginal yeast, wound not healing or with drainage), diarrhea, nausea, vomiting, weight loss, discolored or painful urine, vision changes, menstrual irregularity and fatigue.