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Methylprednisolone

Pronunciation

Pronunciation: METH-il-pred-NIS-oh-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 Acetate

Depo-Medrol
- Injection, suspension 20 mg/mL
- Injection, suspension 40 mg/mL
- Injection, suspension 80 mg/mL

Methylprednisolone Sodium Succinate

A-Methapred
- Injection, powder for solution 125 mg per vial
- Injection, powder for solution 500 mg per vial
- Injection, powder for solution 1 g per vial

Solu-Medrol
- Injection, powder for solution 125 mg per vial
- Injection, powder for solution 500 mg per vial
- Injection, powder for solution 1 g per vial
- Injection, powder for solution 2 g per vial

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.

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Pharmacokinetics

Metabolism

The metabolism generally parallels hydrocortisone, which is metabolized in the liver.

Elimination

Plasma half-life is 78 to 188 min. Approximately 1% is excreted in the urine daily.

Onset

Onset is 6 to 48 h (IM).

Peak

Times to peak effect are 4 to 8 days (IM) and 1 to 2 h (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; treatment of congenital adrenal hyperplasia, hypercalcemia associated with cancer, and/or nonsuppurative thyroiditis; 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 neoplastic 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; 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, except when administered as an intra-articular injection for localized joint conditions; idiopathic thrombocytopenic purpura (IM administration); administration of live virus vaccines; topical monotherapy in primary bacterial infections; intrathecal administration; 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 Acetate
Adults IM Acute severe dermatitis due to poison ivy

80 to 120 mg single dose; relief may result within 8 to 12 h.

Adrenogenital syndrome

40 mg single dose every 2 wk.

Allergic rhinitis

80 to 120 mg; relief may result within 6 h, persisting for several days to 3 wk.

Asthma

80 to 120 mg; relief may result within 6 to 48 h and persist for several days to 2 wk.

Chronic contact dermatitis

Repeated injections at 5- to 10-day intervals may be necessary.

Dermatologic lesions

40 to 120 mg at weekly intervals for 1 to 4 wk.

Multiple sclerosis

160 mg daily for 1 wk followed by 64 mg every other day for 1 mo.

Rheumatoid arthritis

40 to 120 mg weekly.

Seborrheic dermatitis

80 mg weekly.

Intra-articular Large joint (knees, ankles, shoulders)

20 to 80 mg.

Medium joint (elbows, wrists)

10 to 40 mg.

Small joint (metacarpophalangeal, interphalangeal, sternoclavicular, acromioclavicular)

4 to 10 mg.

Tendinous or bursal structures

4 to 30 mg.

In recurrent or chronic cases, injections may be repeated at intervals ranging from 1 to 5 or more wk, depending upon the degree of relief obtained from the initial injection.

Intralesional

20 to 60 mg injected into the lesion. It may be necessary to distribute doses ranging from 20 to 40 mg by repeated local injections in the case of large lesions. One to four injections are usually employed; the intervals between injections vary with the type of lesion being treated and the duration of improvement produced by the initial injection.

Children

IM 0.11 to 1.6 mg/kg/day initially. After a favorable response is noted, the proper maintenance dose should be determined by decreasing the initial dosage in small increments at appropriate time intervals until the lowest dosage that will maintain an adequate clinical response is reached.

Methylprednisolone Sodium Succinate
Adults

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

Infants and Children

IV/IM Not less than 0.5 mg/kg per 24 h.

General Advice

  • Administer once-daily dose or alternate-day dosing in the morning before 9 AM.
  • Do not mix or dilute with other solutions.
  • 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 IM or 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 59° to 86°F. These products may be sensitive to heat. Do not autoclave when it is desirable to sterilize the outside of the vial.

Drug Interactions

Aminoglutethimide

Aminoglutethimide may lead to loss of methylprednisolone-induced adrenal suppression.

Amphotericin B

The risk of hypokalemia may be increased. Closely monitor patients for hypokalemia.

Anticholinesterases

May antagonize anticholinesterase effects in myasthenia gravis. If possible, withhold anticholinesterase agents at least 24 h before starting methylprednisolone therapy.

Antidiabetic agents (eg, sulfonylureas [eg, glyburide])

Methylprednisolone may increase blood glucose levels. Closely monitor blood glucose and adjust the antidiabetic dose as needed.

Aprepitant

Methylprednisolone plasma concentrations may be elevated, increasing the pharmacologic effects and risk of adverse reactions. Monitor the response of the patient. Methylprednisolone dosage adjustments may be needed when starting or stopping aprepitant.

Aspirin, NSAIDs (eg, ibuprofen)

The risk of GI adverse effects may be increased. Closely monitor patients for these reactions.

Azole antifungal agents (eg, ketoconazole), diltiazem, macrolide antibiotics (eg, erythromycin), nefazodone

Methylprednisolone plasma concentrations may be elevated, increasing the pharmacologic effects and risk of adverse reactions. The methylprednisolone dosage requirements may be decreased. Methylprednisolone dosage adjustments may be needed when one of these agents is started or stopped.

Barbiturates, carbamazepine, methimazole, rifamycins (eg, rifampin)

May decrease methylprednisolone plasma concentrations and pharmacologic effect. Monitor the response of the patient and adjust the methylprednisolone dose as needed when one of these agents is started or stopped.

Cholestyramine

Methylprednisolone Cl may be increased, decreasing the pharmacologic effects. Monitor the clinical response of the patient. The dose of methylprednisolone may need to be increased.

Cyclosporine

The pharmacologic effects and risk of adverse reactions of both drugs may be increased. Monitor the patient for adverse reactions (eg, increased serum creatinine, Cushingoid symptoms). If an interaction is suspected, consider decreasing the dose of one or both drugs.

CYP3A4 inducers (eg, phenytoin)

Methylprednisolone plasma concentrations may be reduced, decreasing the pharmacologic effects. The methylprednisolone dosage requirements may be increased.

CYP3A4 inhibitors (eg, macrolide antibiotics [eg, erythromycin])

Methylprednisolone plasma concentrations may be elevated, increasing the pharmacologic effects and risk of adverse reactions. The methylprednisolone dosage requirements may be decreased.

Digoxin

The risk of arrhythmias due to hypokalemia may be increased. Closely monitor serum potassium and for signs of digitalis toxicity.

Hormonal contraceptives

Methylprednisolone metabolism may be decreased, increasing methylprednisolone plasma concentrations, therapeutic effects, and risk of adverse reactions. Monitor the patient. If an interaction is suspected, it may be necessary to decrease the methylprednisolone dose when starting hormonal contraceptives.

Hydantoins (eg, phenytoin)

Methylprednisolone and phenytoin plasma concentrations may be reduced, decreasing the effects of both agents. Monitor the clinical response of the patient and adjust the dose of both drugs as needed.

Interleukin-2

The pharmacologic effects of interleukin-2 may be decreased. Toxic, as well as therapeutic, effects of interleukin-2 may be decreased. Avoid coadministration of these agents.

Isoniazid

Isoniazid plasma concentrations may be reduced, decreasing the pharmacologic effects. It may be necessary to adjust the isoniazid dose when starting or stopping methylprednisolone.

Loop diuretics (eg, furosemide), thiazide diuretics (eg, chlorothiazide)

The risk of hypokalemia may be increased. Closely monitor patients for hypokalemia.

Mifepristone

Administration of mifepristone and misoprostol for the termination of pregnancy is contraindicated in patients receiving long-term corticosteroid therapy.

Neuromuscular blocking agents (eg, pancuronium)

The risk of acute myopathy may be increased, which may involve ocular and respiratory muscles and may result in quadriparesis. Monitor creatine kinase. Improvement or recovery may take weeks to years after discontinuing methylprednisolone.

Quinolone antibiotics (eg, ciprofloxacin)

The risk of tendon rupture may be increased by coadministration of quinolone antibiotics and methylprednisolone, especially in patients 60 years of age and older. Instruct patients to contact their health care provider if they develop tendon-related pain or swelling, or weakness or inability to use 1 of their joints. Discontinue the quinolone and use a nonquinolone antibiotic if further antimicrobial treatment is necessary.

Salicylates

Salicylate plasma concentrations may be reduced, decreasing the pharmacologic effects. Monitor salicylate concentrations when starting or stopping methylprednisolone and adjust the salicylate dose as needed.

Skin tests

Methylprednisolone may suppress skin test reactions.

Tacrolimus

Tacrolimus plasma concentrations may be increased or decreased. If methylprednisolone must be coadministered, additional monitoring of tacrolimus plasma concentrations and renal function is indicated when starting or stopping methylprednisolone. Adjust the tacrolimus dose as needed.

Vaccines

Administration of live or live, attenuated vaccines is contraindicated in patients receiving immunosuppressive doses of corticosteroids. Killed or inactivated vaccines may be administered, but the response cannot be predicted. Immunization procedures may be undertaken in patients receiving corticosteroid replacement therapy (eg, Addison disease). Defer routine administration of vaccines or toxoids until methylprednisolone therapy is discontinued.

Warfarin

The anticoagulant effects of warfarin may be increased or decreased. Monitor coagulation parameters and adjust the warfarin dose as needed when starting or stopping methylprednisolone.

Adverse Reactions

Cardiovascular

Bradycardia, cardiac arrest, cardiac arrhythmias or ECG changes, cardiac enlargement, CHF, circulatory collapse, fatal arrest, hypertension, myocardial rupture, necrotizing angiitis, syncopal episodes, thromboembolism or fat embolism, thrombophlebitis, vasculitis.

CNS

Convulsions, depression, emotional instability, euphoria, fatigue, headache, insomnia, malaise, mood swings, neuritis, neuropathy, paresthesias, personality changes, pseudotumor cerebri (increased intracranial pressure with papilledema), psychosis, vertigo.

Dermatologic

Acneiform eruptions; allergic dermatitis; angioneurotic edema; cutaneous and subcutaneous atrophy; dry, scaly, thin, fragile skin; erythema; hirsutism; hyperpigmentation or hypopigmentation; hypertrichosis; impaired wound healing; increased sweating; lupus erythematosus–like lesions; perineal irritation; petechiae and ecchymoses; rash; striae; sterile abscess; suppressed reactions to skin tests; thinning scalp hair; urticaria; allergic contact dermatitis, burning, cracking and tightening of skin, dryness, folliculitis, hypertrichosis, irritation, itching, miliaria, perioral dermatitis, pruritus, secondary infections, skin atrophy, stinging .

EENT

Exophthalmos, glaucoma, increased IOP, posterior subcapsular cataracts.

GI

Abdominal distention; abdominal fat deposits; bowel dysfunction; bowel, small, and/or large intestine perforation; elevation in serum liver enzymes; hepatomegaly; hiccups; increased appetite and weight gain; nausea; pancreatitis; peptic ulcer with perforation and hemorrhage; ulcerative esophagitis; vomiting.

Genitourinary

Bladder dysfunction, glycosuria, increased or decreased motility and number of spermatozoa, menstrual irregularities.

Hematologic

Leukocytosis.

Metabolic

Cushingoid state, decreased carbohydrate or glucose tolerance, edema, growth suppression in children, hyperglycemia, hypocalcemia, hypokalemia, hypokalemic alkalosis, insulin or sulfonylurea requirements in diabetic patients, manifestation of latent diabetes, metabolic alkalosis, negative nitrogen balance, sodium and fluid retention.

Musculoskeletal

Aseptic necrosis of femoral and humeral heads, calcinosis, Charcot-like arthropathy, muscle mass loss, myopathy, osteonecrosis, osteoporosis, spontaneous fractures, steroid myopathy, tendon rupture, weakness.

Miscellaneous

Aggravation or masking of infections; allergic, anaphylactoid, or hypersensitivity reactions; anaphylaxis; angioedema; decreased resistance to infection; infection; injection-site reactions; moon face; postinjection flare.

Precautions

Monitor

Monitor patients for hypothalamic-pituitary-adrenal (HPA) axis suppression, Cushing syndrome, and hyperglycemia in patients on long-term therapy. Monitor IOP if therapy is continued for more than 6 wk. Monitor linear growth in children.


Pregnancy

Category C .

Lactation

Excreted in breast milk.

Children

May be more susceptible to adverse effects from topical use. Products that contain benzyl alcohol are contraindicated in premature infants.

Elderly

May require lower doses.

Hypersensitivity

Reactions, including anaphylaxis, may occur rarely.

Renal Function

Use with caution.

Special Risk Patients

Use with caution in patients with CHF, hypertension, recent MI, active or latent peptic ulcer, fresh intestinal anastomoses, nonspecific ulcerative colitis.

Tartrazine Sensitivity

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

Adrenal suppression

Prolonged therapy may lead to HPA suppression.

Benzyl alcohol

Some of these products may contain benzyl alcohol, which has been reported to be associated with a fatal gasping syndrome in premature infants.

Bone effects

May lead to inhibitions of bone growth in children and the development of osteoporosis at any age.

Brain injury

Do not use high doses of systemic corticosteroids for the treatment for traumatic brain injury.

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. Do not use in cerebral malaria.

Kaposi sarcoma

May occur, most often for chronic conditions.

Myopathy

Acute myopathy has been observed with the use of high doses of corticosteroids, most often occurring in patients with disorders of neuromuscular transmission (eg, myasthenia gravis), or in patients receiving concomitant therapy with neuromuscular blocking drugs (eg, pancuronium). This acute myopathy is generalized, may involve ocular and respiratory muscles, and may result in quadriparesis. Elevations of creatine kinase may occur. Clinical improvement or recovery after stopping corticosteroids may require weeks to years.

Ocular effects

May produce posterior subcapsular cataracts or glaucoma with possible damage to the optic nerves, and may enhance the establishment of secondary ocular infections due to bacteria, fungi, or viruses. Not recommended in the treatment of optic neuritis. Use drug systemically with caution in ocular herpes simplex because of risk of possible corneal perforation; do not use in active ocular herpes simplex.

Peptic ulcer

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

Psychiatric effects

Psychic derangements may appear when corticosteroids are used, ranging from euphoria, insomnia, mood swings, personality changes, and severe depression to frank psychotic manifestations. Existing emotional instability or psychotic tendencies may be aggravated by corticosteroids.

Repository injections

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

Stress

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

Overdosage

Symptoms

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

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 long-term steroid therapy to wear or carry identification (eg, card, bracelet) 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: diarrhea, discolored or painful urine, fatigue, menstrual irregularity, nausea, signs of infection (eg, fever, overgrowth in mouth, vaginal yeast, wound not healing or with drainage), swelling in feet and ankles, vision changes, vomiting, and weight loss.

Copyright © 2009 Wolters Kluwer Health.

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