Methylprednisolone

Methylprednisolone, a corticosteroid, is similar to a natural hormone produced by your adrenal glands. It is often used to replace this chemical when your body does not make enough of it. It relieves inflammation (swelling, heat, redness, and pain) and is used to treat certain forms of arthritis; skin, blood, kidney, eye, thyroid, and intestinal disorders (e.g., colitis); severe allergies; and asthma. Methylprednisolone is also used to treat certain types of cancer.

This medication is sometimes prescribed for other uses; ask your doctor or pharmacist for more information.

• Medrol^®

In patients on corticosteroid therapy subjected to unusual stress, increased dosage of rapidly acting corticosteroids before, during, and after the stressful situation is indicated.

Corticosteroids may mask some signs of infection, and new infections may appear during their use. Infections with any pathogen including viral, bacterial, fungal, protozoan or helminthic infections, in any location of the body, may be associated with the use of corticosteroids alone or in combination with other immunosuppressive agents that affect cellular immunity, humoral immunity, or neutrophil function.1

These infections may be mild, but can be severe and at times fatal. With increasing doses of corticosteroids, the rate of occurrence of infectious complications increases.2 There may be decreased resistance and inability to localize infec-tion when corticosteroids are used.

Prolonged use of corticosteroids may produce posterior subcapsular cataracts, glaucoma with possible damage to the optic nerves, and may enhance the establishment of secondary ocular infections due to fungi or viruses.

Usage in pregnancy: Since adequate human reproduction studies have not been done with corticosteroids, the use of these drugs in pregnancy, nursing mothers or women of child-bearing potential requires that the possible benefits of the drug be weighed against the potential hazards to the mother and embryo or fetus. Infants born of mothers who have received substantial doses of corticosteroids during pregnancy, should be carefully observed for signs of hypoadrenalism.

Average and large doses of hydrocortisone or cortisone can cause elevation of blood pressure, salt and water retention, and increased excretion of potassium. These effects are less likely to occur with the synthetic derivatives except when used in large doses. Dietary salt restriction and potassium supplementation may be necessary. All corticosteroids increase calcium excretion.

Administration of live or live, attenuated vaccines is contraindicated in patients receiving immunosuppressive doses of corticosteroids. Killed or inactivated vaccines may be administered to patients receiving immunosuppressive doses of corticosteroids; however, the response to such vaccines may be diminished. Indicated immunization procedures may be undertaken in patients receiving nonimmunosuppressive doses of corticosteroids.

The use of MEDROL (methylprednisolone) Tablets in active tuberculosis should be restricted to those cases of fulminating or disseminated tuberculosis in which the corticosteroid is used for the management of the disease in conjunction with an appropriate antituberculous regimen.

If corticosteroids are indicated in patients with latent tuberculosis or tuberculin reactivity, close observation is necessary as reactivation of the disease may occur. During prolonged corticosteroid therapy, these patients should receive chemoprophylaxis.

Persons who are on drugs which suppress the immune system are more susceptible to infections than healthy individuals. Chicken pox and measles, for example, can have a more serious or even fatal course in non-immune children or adults on corticosteroids. In such children or adults who have not had these diseases particular care should be taken to avoid exposure. How the dose, route and duration of corticosteroid administration affects the risk of developing a disseminated infection is not known. The contribution of the underlying disease and/or prior corticosteroid treatment to the risk is also not known. If exposed, to chicken pox, prophylaxis with varicella zoster immune globulin (VZIG) may be indicated. If exposed to measles, prophylaxis with pooled intramuscular immunoglobulin (IG) may be indicated. (See the respective package inserts for complete VZIG and IG prescribing information.) If chicken pox develops, treatment with antiviral agents may be considered. Similarly, corticosteroids should be used with great care in patients with known or suspected Strongyloides (threadworm) infestation. In such patients, corticosteroid-induced immunosuppression may lead to Strongyloides hyperinfection and dissemination with widespread larval migration, often accompanied by severe enterocolitis and potentially fatal gram-negative septicemia.

Before taking methylprednisolone, tell your doctor about all of your medical conditions. Especially tell your doctor if you:

• are allergic to methylprednisolone, aspirin (Ecotrin), or any ingredient within this medication product
• have a history of liver, kidney, intestinal, or heart disease
• have diabetes, an underactive thyroid gland, high blood pressure, or mental illness
• have myasthenia gravis (disease of weak muscles), osteoporosis, seizures, or ulcers
• have or have had tuberculosis or any other type of ongoing infection
• have a history of ulcers (holes in the stomach)
• have a history of alcohol use or abuse
• have are or about to receive a vaccine, especially a live one such as the nasal influenza, MMR, or varicella vaccines
• are pregnant or breastfeeding

Tell your doctor about all the medicines you take including prescription and non-prescription medicines, vitamins, and herbal supplements.

Treatment of a wide variety of diseases and conditions principally for glucocorticoid effects as an anti-inflammatory and immunosuppressant agent and for its effects on blood and lymphatic systems in the palliative treatment of various diseases.c d

Usually, inadequate alone for adrenocortical insufficiency because of minimal mineralocorticoid activity.c

Adrenocortical Insufficiency

Corticosteroids are administered in physiologic dosages to replace deficient endogenous hormones in patients with adrenocortical insufficiency.a c

Because production of both mineralocorticoids and glucocorticoids is deficient in adrenocortical insufficiency, hydrocortisone or cortisone (in conjunction with liberal salt intake) usually is the corticosteroid of choice for replacement therapy.a c d m

If methylprednisolone is used, must also administer a mineralocorticoid (fludrocortisone), particularly in infants.a c d

In suspected or known adrenal insufficiency, parenteral therapy may be used preoperatively or during serious trauma, illness, or shock unresponsive to conventional therapy.d e m

In shock unresponsive to conventional therapy, IV therapy in conjunction with other therapy for shock is essential; hydrocortisone is preferred, but a synthetic glucocorticoid like methylprednisolone can be substituted.c e

Adrenogenital Syndrome

Lifelong glucocorticoid treatment of congenital adrenogenital syndrome.a c

In salt-losing forms, cortisone or hydrocortisone is preferred in conjunction with liberal salt intake; a mineralocorticoid may be necessary in conjunction through at least 5–7 years of age.c

A glucocorticoid, usually alone, for long-term therapy after early childhood.c

In hypertensive forms, a “short-acting” glucocorticoid with minimal mineralocorticoid activity (e.g., methylprednisolone, prednisone) is preferred;c avoid long-acting glucocorticoids (e.g., dexamethasone) because of tendency toward overdosage and growth retardation.c

Hypercalcemia

Treatment of hypercalcemia associated with malignancy.a c d m

Usually ameliorates hypercalcemia associated with bone involvement in multiple myeloma.c

Most effective long-term treatment for hypercalcemia associated with breast cancer in postmenopausal women.c

Efficacy varies in other malignancies.c

Treatment of hypercalcemia associated with sarcoidosis†.c

Treatment of hypercalcemia associated with vitamin D intoxication†.c

Not effective for hypercalcemia caused by hyperparathyroidism†.c

Thyroiditis

Treatment of granulomatous (subacute, nonsuppurative) thyroiditis.a c d m

Anti-inflammatory actions relieves fever, acute thyroid pain, and swelling.c

May reduce orbital edema in endocrine exophthalmos (thyroid ophthalmopathy).c

Usually reserved for palliative therapy in severely ill patients unresponsive to salicylates and thyroid hormones.c

Rheumatic Disorders and Collagen Diseases

Short-term palliative treatment of acute episodes or exacerbations and systemic complications of rheumatic disorders (e.g., rheumatoid arthritis, juvenile arthritis, psoriatic arthritis, acute gouty arthritis, posttraumatic osteoarthritis, synovitis of osteoarthritis, epicondylitis, acute nonspecific tenosynovitis, ankylosing spondylitis, Reiter syndrome†, rheumatic fever† [especially with carditis]) and collagen diseases (e.g., acute rheumatic carditis, systemic lupus erythematosus, dermatomyositis† [polymyositis], polyarteritis nodosa†, vasculitis†) refractory to more conservative measures.a c d l m

Relieves inflammation and suppresses symptoms but not disease progression.c

Rarely indicated as maintenance therapy.c

May be used as maintenance therapy (e.g., in rheumatoid arthritis, acute gouty arthritis, systemic lupus erythematosus, acute rheumatic carditis) as part of a total treatment program in selected patients when more conservative therapies have proven ineffective.a b c d

Glucocorticoid withdrawal is extremely difficult if used for maintenance; relapse and recurrence usually occur with drug discontinuance.c

Local injection can provide dramatic relief initially for articular manifestations of rheumatic disorders (e.g., rheumatoid arthritis) that involve only a few persistently inflamed joints or for inflammation of tendons or bursae;c inflammation tends to recur and sometimes is more intense after drug cessation.c

Local injection used for the management of cystic tumors of an aponeurosis or tendon (ganglia).d

Local injection can prevent invalidism by facilitating movement of joints that might otherwise become immobile.c

Controls acute manifestations of rheumatic carditis more rapidly than salicylates and may be life-saving; cannot prevent valvular damage and no better than salicylates for long-term treatment.c

Adjunctively for severe systemic complications of Wegener’s granulomatosis†, but cytotoxic therapy is the treatment of choice.c

Primary treatment to control symptoms and prevent severe, often life-threatening complications in patients with dermatomyositis† and polymyositis†, polyarteritis nodosa†, relapsing polychondritis†, polymyalgia rheumatica† and giant-cell (temporal) arteritis†, or mixed connective tissue disease syndrome†.a c High dosage may be required for acute situations; after a response has been obtained, drug must often be continued for long periods at low dosage.c

Polymyositis† associated with malignancy and childhood dermatomyositis may not respond well.c

Rarely indicated in psoriatic arthritis, diffuse scleroderma† (progressive systemic sclerosis), acute and subacute bursitis, or osteoarthritis†; risks outweigh benefits.a c d m

In osteoarthritis†, intra-articular injections may be beneficial but should be limited in number as joint damage may occur.c d

Dermatologic Diseases

Treatment of pemphigus and pemphigoid†, bullous dermatitis herpetiformis, severe erythema multiforme (Stevens-Johnson syndrome), exfoliative dermatitis, uncontrollable eczema†, cutaneous sarcoidosis†, mycosis fungoides, lichen planus, lichen simplex chronicus (neurodermatitis), severe psoriasis, and severe seborrheic dermatitis.a c d e

Usually reserved for acute exacerbations unresponsive to conservative therapy.c

Early initiation of systemic glucocorticoid therapy may be life-saving in pemphigus vulgaris and pemphigoid†, and high or massive doses may be required.c

For control of severe or incapacitating allergic conditions (e.g., contact dermatitis, atopic dermatitis) intractable to adequate trials of conventional treatment.a d e f m

Chronic skin disorders seldom an indication for systemic glucocorticoids.c

Intralesional or sublesional injections occasionally indicated for localized chronic skin disorders, keloids, psoriatic plaques, alopecia areata, discoid lupus erythematosus, necrobiosis lipoidica diabeticorum, granuloma annulared m unresponsive to topical therapy.c

Rarely indicated for psoriasis†;c if used, exacerbation may occur when the drug is withdrawn or dosage is decreased.c

Rarely indicated systemically for alopecia (areata, totalis, or universalis).c May stimulate hair growth, but hair loss returns when the drug is discontinued.c

Allergic Conditions

For control of severe or incapacitating allergic conditions intractable to adequate trials of conventional treatment and control of acute manifestations, including anaphylactic and anaphylactoid reactions†, angioedema†, acute noninfectious laryngeal edema, serum sickness, allergic symptoms of trichinosis†, asthma, urticarial transfusion reactions, drug hypersensitivity reactions, and severe seasonal or perennial rhinitis.a c d e f m

Systemic therapy usually reserved for acute conditions and severe exacerbations.c

For acute conditions, usually used in high dosage and with other therapies (e.g., antihistamines, sympathomimetics).c

Reserve prolonged treatment of chronic allergic conditions for disabling conditions unresponsive to more conservative therapy and when risks of long-term glucocorticoid therapy are justified.c

Ocular Disorders

To suppress a variety of allergic and nonpyogenic ocular inflammations.c

To reduce scarring in ocular injuries†.c

For the treatment of severe acute and chronic allergic and inflammatory processes involving the eye and adnexa (e.g., allergic conjunctivitis, keratitis, allergic corneal marginal ulcers, herpes zoster ophthalmicus, iritis and iridocyclitis, chorioretinitis, diffuse posterior uveitis and choroiditis, anterior segment inflammation, optic neuritis, sympathetic ophthalmia, temporal arteritis).a c d e f m

Acute optic neuritis optimally treated with initial high-dose IV therapy followed by chronic oral therapy. Assists in recovery of vision and slows progression to clinically definite multiple sclerosis.

Less severe allergic and inflammatory allergic conditions of the eye are treated with topical (to the eye) corticosteroids.g

Topically applied glucocorticoids appear to be as effective as systemic steroids for the treatment of most anterior ocular inflammations.c

Systemically in stubborn cases of anterior segment eye disease and when deeper ocular structures are involved.c

Asthma

Adjunctively for moderate to severe exacerbations of asthma and for maintenance in persistent asthma.c g

Systemically (oral or IV) for treatment of moderate to severe acute exacerbations of asthma (oral prednisone usually preferred); speeds resolution of airflow obstruction and reduces rate of relapse.g

Because onset of effects is delayed, do not use alone for emergency treatment.c

Early systemic glucocorticoid therapy particularly important for asthma exacerbations in infants and children.g

In hospital management of an acute asthma exacerbation, may give systemic adjunctive glucocorticoids if response to oral inhalation therapy is not immediate, if oral corticosteroids were used as self-medication prior to hospitalization, or if the episode is severe.c

For severe persistent asthma once initial control is achieved, high dosages of inhaled corticosteroids are preferable to oral glucocorticoids for maintenance because inhaled corticosteroids have fewer systemic effects.

Maintenance therapy with low doses of an orally inhaled corticosteroid is preferred treatment for adults and children with mild persistent asthmac (i.e., patients with daytime symptoms of asthma more than twice weekly but less than once daily, and nocturnal symptoms of asthma more than twice per month).b

Orally as an adjunct to other therapy to speed resolution of all but the mildest exacerbations of asthma when response to a short-acting inhaled β2-agonist is not prompt or sustained after 1 hour or in those who have a history of severe exacerbations.c

Oral glucocorticoids with minimal mineralocorticoid activity and relatively short half-life (e.g., prednisone, prednisolone, methylprednisolone) are preferred.

COPD

For severe exacerbations of COPD†, a short (e.g., 1–2 weeks) course of oral glucocorticoids can be added to existing therapy.

Effects in stable COPD are much less dramatic than in asthma, and role of glucocorticoids in the management of stable COPD is limited to very specific indications.

Croup

Adjunctive treatment of croup† in pediatric patients.g

Decreases edema in laryngeal mucosa.g

Reduces need for hospitalization, shorter duration of hospitalization, and reduces need for subsequent interventions (e.g., epinephrine).g

Sarcoidosis

Management of symptomatic sarcoidosis.a c d e f m

Systemic glucocorticoids are indicated for hypercalcemia; ocular, CNS, glandular, myocardial, or severe pulmonary involvement; or severe skin lesions unresponsive to intralesional injections of glucocorticoids.c

Advanced Pulmonary and Extrapulmonary Tuberculosis

Systemically as adjunctive therapy with effective antimycobacterial agents (e.g., streptomycin, isoniazid) to suppress manifestations related to the host’s inflammatory response to the bacillus (Mycobacterium tuberculosis) and ameliorate complications in severe pulmonary or extrapulmonary tuberculosis.a m

Adjunctive glucocorticoid therapy may enhance short-term resolution of disease manifestations (e.g., clinical and radiographic abnormalities) in advanced pulmonary tuberculosis and also may reduce mortality associated with certain forms of extrapulmonary disease (e.g., meningitis, pericarditis).

Systemic adjunctive glucocorticoids may reduce sequelae (e.g., intellectual impairment) and/or improve survival in moderate to severe tuberculous meningitis; used in the treatment of tuberculous meningitis with subarachnoid block or impending block concurrently with appropriate antituberculous chemotherapy.a d e f m

Systemic adjunctive glucocorticoid therapy rapidly reduces the size of pericardial effusions and the need for drainage procedures and decreases mortality (probably through control of hemodynamically threatening effusion) in acute tuberculous pericarditis.

Hastens the resolution of pain, dyspnea, and fever associated with tuberculous pleurisy.c

Lipid Pneumonitis

Promotes the breakdown or dissolution of pulmonary lesions and eliminates sputum lipids in lipid pneumonitis.c

Pneumocystis jiroveci Pneumonia

Systemic adjunctive glucocorticoids decrease the likelihood of deterioration of oxygenation, respiratory failure, and/or death in moderate to severe Pneumocystis jiroveci (formerly Pneumocystis carinii) pneumonia in AIDS†.

Prevents early deterioration in oxygenation associated with antipneumocystis therapy; initiate adjunctive glucocorticoid therapy as early as possible in moderate to severe pneumocystis pneumonia.

Not known whether patients with mild pneumocystis pneumonia (arterial oxygen pressure >70 mm Hg or arterial-alveolar gradient <35 mm Hg on room air) will have clinically important benefit with adjunctive glucocorticoid therapy.

Oral prednisone or parenteral methylprednisolone generally is preferred.

Loeffler’s Syndrome

Symptomatic relief of acute manifestations of symptomatic Loeffler’s syndrome not manageable by other means.a f

Berylliosis

Symptomatic relief of acute manifestations of berylliosis.a d f m

Aspiration Pneumonitis

Symptomatic relief of acute manifestations of aspiration pneumonitis.a d f

Anthrax

Adjunct to anti-infective therapy in the treatment of anthrax† in an attempt to ameliorate toxin-mediated effects associated with Bacillus anthracis infections.

For cutaneous anthrax† if there are signs of systemic involvement or extensive edema involving the neck and thoracic region, anthrax meningitis†, and inhalational anthrax† that occurs as the result of exposure to anthrax spores in the context of biologic warfare or bioterrorism if extensive edema, respiratory compromise, or meningitis is present.

Hematologic Disorders

Management of acquired (autoimmune) hemolytic anemia, pure red cell aplasia, idiopathic thrombocytopenic purpura (ITP), secondary thrombocytopenia, erythroblastopenia, or congenital (erythroid) hypoplastic anemia.a d e f m

High or even massive dosages decrease bleeding tendencies and normalize blood counts; does not affect the course or duration of hematologic disorders.c

Glucocorticoids, immune globulin IV (IGIV), or splenectomy are first-line therapies for moderate to severe ITP, depending on the extent of bleeding involved.

May not affect or prevent renal complications in Henoch-Schoenlein purpura.c

Insufficient evidence of effectiveness in aplastic anemia in children, but widely used.c

Shock

Although IV glucocorticoids may be life-saving in shock secondary to adrenocortical insufficiency (see Adrenocortical Insufficiency under Uses), the value of the drugs in the treatment of shock resulting from other causes† is controversial.c

Management of shock should be based on specific treatment of the primary cause and secondary abnormalities, and glucocorticoids, if used, should be regarded only as adjunctive supportive treatment.c

Value in adjunctive treatment of septic shock† is particularly controversial. Conflicting evidence regarding effects of high-dose regimens on morbidity and mortality in septic shock. In a clinical study, methylprednisolone was ineffective in the treatment of sepsis syndrome and septic shock, and may increase the risk of mortality in certain patients (i.e., patients with increased Scr or those who develop secondary infections after treatment).e

Pericarditis

To reduce the pain, fever, and inflammation of pericarditis†, including that associated with MI.c

Glucocorticoids can provide effective symptomatic relief, but aspirin considered the treatment of choice for post-MI pericarditis because of greater evidence establishing benefit.

Important to distinguish between pain caused by pericarditis and that caused by ischemia since management will differ.

Consider possibility that cardiac rupture may account for recurrent pain since use of glucocorticoids may be a risk factor in its development.

Glucocorticoids may cause thinning of developing scar and myocardial rupture.

Management of tuberculous pericarditis. (See Advanced Pulmonary and Extrapulmonary Tuberculosis under Uses.)

GI Diseases

Short-term palliative therapy for acute exacerbations and systemic complications of ulcerative colitis, regional enteritis (Crohn’s disease), and celiac disease†.a c d e f m

Do not use if a probability of impending perforation, abscess, or other pyogenic infection.e

Rarely indicated for maintenance therapy in chronic GI diseases (e.g., ulcerative colitis, celiac disease) since does not prevent relapses and may produce severe adverse reactions with long-term administration.c

Occasionally, low dosages, in conjunction with other supportive therapy, may be useful for disease unresponsive to the usual therapy indicated for chronic conditions.c

Management of mildly to moderately active and moderately to severely active Crohn’s disease .

Parenteral glucocorticoids recommended for patients with severe fulminant Crohn’s disease. Once patients respond to parenteral therapy, they should gradually be switched to an equivalent regimen of an oral glucocorticoid.

Some experts state that glucocorticoids should not be used for the management of mildly to moderately active Crohn’s disease because of the high incidence of adverse effects and their use should be reserved for patients with moderately to severely active disease.

Glucocorticoids should not be used for maintenance therapy of chronic GI diseases (e.g., ulcerative colitis, Crohn’s disease) because they usually do not prevent relapses and the drugs may produce severe adverse effects with long-term administration.a c

Glucocorticoids have been used in the management of moderately to severely active Crohn’s disease and in mild esophageal or gastroduodenal Crohn’s disease in pediatric patients.

Neoplastic Diseases

Alone or as a component of various chemotherapeutic regimens in the palliative treatment of neoplastic diseases of the lymphatic system (e.g., leukemias and lymphomas in adults and acute leukemias in children).a d e f m

Treatment of breast cancer†; glucocorticoids alone not as effective as other agents (e.g., cytotoxic agents, hormones, antiestrogens) and should be reserved for unresponsive disease.c

Glucocorticoids alone or as a component of various combination chemotherapeutic regimens for palliative treatment of advanced, symptomatic (i.e., painful) hormone-refractory prostate cancer†.

Cancer Chemotherapy-induced Nausea and Vomiting

Prevention of nausea and vomiting associated with emetogenic cancer chemotherapy†.

Cerebral Edema

To decrease cerebral edema associated with brain tumors and neurosurgery.c d m

Cerebral edema associated with pseudotumor cerebri may also benefit, but efficacy of glucocorticoids is controversial and remains to be established.c

Edema resulting from brain abscesses is less responsive than that resulting from brain tumors.c

Pharmacologic management of cerebral edema is not a substitute for careful neurosurgical evaluation and definitive management such as neurosurgery or other specific therapy.c d f

Head Injury

Efficacy of glucocorticoid therapy is not established in patients with head injury; such therapy can be detrimental and is associated with a substantial increase in risk of death. Use to improve outcome or reduce intracranial pressure not recommended in patients with head injury.

Cerebral Malaria

Glucocorticoids are not effective and can have detrimental effects in the management of cerebral malaria caused by Plasmodium falciparum; no longer recommended for this condition.c

Acute Spinal Cord Injury

Some evidence indicates that large IV doses of glucocorticoids (i.e., methylprednisolone) can improve motor and sensory function in patients with acute spinal cord injury† when treatment is initiated promptly following injury (within 8 hours). It is not known whether improvement in neurologic function with such therapy will routinely lead to specific improvements in disability.

Low Back Pain

Has been used epidurally† (alone or combined with a local anesthetic and/or an opiate analgesic) for symptomatic relief of low back pain†.

Although use remains controversial and convincing evidence of efficacy is lacking, most experts consider such therapy an option for short-term relief of acute, subacute, or chronic radicular pain in patients with low back pain and radiculopathy associated with disk disease or herniation or spinal stenosis when more conservative therapies (e.g., rest, analgesics, physical therapy) fail and as a means of potentially avoiding surgery. (See Nervous System Effects under Cautions.)

Limited evidence suggests that therapeutic facet joint† and intradiscal glucocorticoid injections† are minimally effective or ineffective in the treatment of low back pain, although facet joint injections may be useful in some patients with facet arthropathy. Inclusion of a glucocorticoid in trigger point injections does not appear to be beneficial.

Sacroiliac joint injections performed using fluoroscopic guidance may provide temporary pain relief in some patients when the principal source of spinal pain is the sacroiliac joint.

Oral glucocorticoids† have been used; however, they do not appear to be effective and evidence supporting such use is lacking.

Bacterial Meningitis

Limited data in animals suggest that dexamethasone may be superior to methylprednisolone in reversing certain CSF abnormalities (e.g., intracranial hypertension, elevated lactate concentrations) associated with bacterial meningitis, and experience is insufficient to allow recommendation of glucocorticoids other than dexamethasone for adjunctive therapy in bacterial meningitis†.

Short-term IV adjunctive therapy with dexamethasone is preferred.

Multiple Sclerosis

Glucocorticoids are drugs of choice for the management of acute relapses of multiple sclerosis†a d m and have replaced corticotropin as the therapy of choice because of a more rapid onset of action, more consistent effects, and fewer adverse effects.

Anti-inflammatory and immunomodulating effects accelerate neurologic recovery by restoring the blood-brain barrier, reducing edema, and possibly improving axonal conduction.

Shortens the duration of relapse and accelerates recovery; remains to be established whether the overall degree of recovery improves or the long-term course is altered.

Myasthenia Gravis

Management of myasthenia gravis†, usually when there is an inadequate response to anticholinesterase therapy.

Parenterally for the treatment of myasthenic crisis.

Organ Transplants

In massive dosage, used concomitantly with other immunosuppressive drugs to prevent rejection of transplanted organs†.c

Incidence of secondary infections is high with immunosuppressive drugs; limit to clinicians experienced in their use.c

Trichinosis

Treatment of trichinosis with neurologic or myocardial involvement.a d e f

Nephrotic Syndrome and Lupus Nephritis

Treatment of idiopathic nephrotic syndrome without uremia.a d e f

Can induce diuresis and remission of proteinuria in nephrotic syndromea c d e f m secondary to lupus erythematosus or primary renal disease, especially when there is minimal renal histologic change.b d m

Treatment of lupus nephritis.a d e

Carpal Tunnel Syndrome

Local injection of glucocorticoids (e.g., methylprednisolone, betamethasone) into the tissue near the carpal tunnel has been used in a limited number of patients to relieve symptoms (e.g., pain, edema, sensory deficit) of carpal tunnel syndrome†.

Absorption

Bioavailability

Absorption from IM injection of methylprednisolone sodium succinate is rapid.b

Systemic absorption of methylprednisolone acetate occurs slowly following intra-articular, intrabursal, intrasynovial, intradermal, or soft tissue injection; c d m Absorption from intra-articular injection sites is usually very slow and continues for about 7 days.b

Onset

Following IM administration (80–120 mg) in patients with severe poison ivy, relief onset within 8–12 hours.d

Following oral administration in patients with asthma, effects may not be evident for several hours.

Duration

The duration of anti-inflammatory activity of methylprednisolone approximately equals the duration of HPA-axis suppression, about 1.25–1.5 days for a single 40-mg oral dose.c

Distribution

Extent

Most glucocorticoids are removed rapidly from the blood and distributed to muscles, liver, skin, intestines, and kidneys.c

Glucocorticoids appear in breast milk and the placenta.c

Elimination

Metabolism

Metabolized in most tissues, but mainly in the liver, to inactive compounds.c

Half-life

Approximately 2.5–3.5 hours following oral administration of methylprednisolone or IV or IM administration of methylprednisolone sodium succinate.h

Special Populations

The metabolic clearance of corticosteroids may be decreased in patients with hypothyroidism and increased in those with hyperthyroidism.d m

IV (succinate): Within 1 hour; Intra-articular (IV acetate): 1 week

Time to Peak

Oral: 2.1 ± 0.7 hours (Czock 2005)

IV (succinate): 0.8 hours (Czock 2005)

Hypersensitivity to methylprednisolone or any component of the formulation; systemic fungal infection (except intra-articular injection for localized joint conditions); intrathecal administration; live or attenuated virus vaccines (with immunosuppressive doses of corticosteroids); use in premature infants (formulations containing benzyl alcohol preservative only); immune thrombocytopenia (formerly known as idiopathic thrombocytopenic purpura) (IM administration only)

Canadian labeling: Additional contraindications (not in US labeling):

Methylprednisolone tablets: Herpes simplex of the eye, vaccinia and varicella (except for short-term or emergency therapy)

Methylprednisolone acetate injection: Epidural or intravascular administration; intra-articular injections in unstable joints; herpes simplex of the eye, vaccinia and varicella (except for short-term or emergency therapy)

Methylprednisolone sodium succinate: Hypersensitivity to cow's milk or its components or other dairy products which may contain trace amounts of milk ingredients; epidural administration; herpes simplex of the eye, vaccinia and varicella, arrested tuberculosis, acute psychoses, Cushing syndrome, peptic ulcer, markedly elevated serum creatinine (except for short-term or emergency therapy)

Documentation of allergenic cross-reactivity for corticosteroids is limited. However, because of similarities in chemical structure and/or pharmacologic actions, the possibility of cross-sensitivity cannot be ruled out with certainty.

The lowest possible dose should be used to control the condition; when dose reduction is possible, the dose should be reduced gradually. Only sodium succinate salt may be given IV.

Allergic conditions: Oral: Tapered-dosage schedule (eg, dose-pack containing 21 x 4 mg tablets):

Day 1: 24 mg on day 1 administered as 8 mg (2 tablets) before breakfast, 4 mg (1 tablet) after lunch, 4 mg (1 tablet) after supper, and 8 mg (2 tablets) at bedtime OR 24 mg (6 tablets) as a single dose or divided into 2 or 3 doses upon initiation (regardless of time of day)

Day 2: 20 mg on day 2 administered as 4 mg (1 tablet) before breakfast, 4 mg (1 tablet) after lunch, 4 mg (1 tablet) after supper, and 8 mg (2 tablets) at bedtime

Day 3: 16 mg on day 3 administered as 4 mg (1 tablet) before breakfast, 4 mg (1 tablet) after lunch, 4 mg (1 tablet) after supper, and 4 mg (1 tablet) at bedtime

Day 4: 12 mg on day 4 administered as 4 mg (1 tablet) before breakfast, 4 mg (1 tablet) after lunch, and 4 mg (1 tablet) at bedtime

Day 5: 8 mg on day 5 administered as 4 mg (1 tablet) before breakfast and 4 mg (1 tablet) at bedtime

Day 6: 4 mg on day 6 administered as 4 mg (1 tablet) before breakfast

Anti-inflammatory or immunosuppressive: Note: Initial dosage depends upon condition being treated; adjust subsequent doses based on patient response.

Oral: 4 to 48 mg/day in 1 to 4 divided doses initially, followed by gradual reduction in dosage to the lowest possible level consistent with maintaining an adequate clinical response.

IM (succinate): 10 to 40 mg/day initially

IM (acetate): 4 to 120 mg single dose; repeated injections may be necessary for recurrent or chronic conditions.

IV (succinate): 10 to 40 mg over a period of several minutes and repeated IV or IM at intervals depending on clinical response; when high dosages are needed, administer 30 mg/kg over a period ≥30 minutes and may be repeated every 4 to 6 hours for 48 hours.

Intralesional (acetate): 20 to 60 mg; for large lesions, it may be necessary to distribute doses ranging from 20 to 40 mg by repeated local injections; 1 to 4 injections are usually employed with intervals between injections varying with the type of lesion being treated and clinical response.

Soft tissue (acetate): 4 to 30 mg; repeated injections may be necessary for recurrent or chronic conditions.

Arthritis: Intra-articular (acetate): Administer every 1 to 5 weeks.

Large joints (eg, knee, ankle, shoulder): 20 to 80 mg

Medium joints (eg, elbow, wrist): 10 to 40 mg

Small joints (eg, metacarpophalangeal, interphalangeal, sternoclavicular, acromioclavicular): 4 to 10 mg

Asthma, exacerbations:

Acute, short-course “burst” (NAEPP 2007):

Oral: 40 to 60 mg/day in divided doses once or twice daily for 3 to 10 days; Note: Burst should be continued until symptoms resolve and peak expiratory flow is at least 80% of personal best; usually requires 3 to 10 days of treatment; longer treatment may be required.

IM (acetate): 240 mg as a one-time dose; Note: This may be given in place of short-course “burst” of oral steroids in patients who are vomiting or if compliance is a problem.

Hospital/emergency medical care doses: Oral, IV: 40 to 80 mg/day in divided doses once or twice daily until peak expiratory flow is 70% of predicted or personal best.

Asthma, long-term (maintenance) (NAEPP 2007): Oral: 7.5 to 60 mg once daily in the morning or every other day as needed for asthma control

Multiple sclerosis, acute exacerbation:

Note: Treatment guidelines recommend high-dose IV methylprednisolone succinate or oral methylprednisolone for acute exacerbations of multiple sclerosis (AAN [Scott 2011]); NICE 2014).

Manufacturer’s labeling: Oral, IV (succinate only), IM (acetate or succinate): 160 mg daily for 1 week, followed by 64 mg every other day for 1 month.

Off-label dosing:

Oral: 500 mg daily for 5 days (NICE 2014).

IV (succinate only): 1,000 mg daily for 3 to 7 days (AAN [Scott 2011]; NICE 2014).

Bronchiolitis obliterans syndrome, prevention (off-label use): IV (sodium succinate): 1000 mg daily for 3 days. Note: Many centers use 10 to 15 mg/kg/day for smaller patients (Meyer 2014).

Cadaveric organ recovery (hormonal resuscitation) (off-label use): IV (sodium succinate): 15 mg/kg or 2,000 mg bolus administered to the brain-dead donor who is hemodynamically unstable requiring significant vasopressor support; give concomitantly with vasopressin, levothyroxine or liothyronine (preferred), dextrose (if bolus dose insulin used), and regular insulin (bolus dose or continuous infusion). If continuous infusion insulin is employed, maintain blood glucose 120 to 180 mg/dL (Rosendale 2003a; Rosendale 2003b; Rosengard 2002; Salim 2007; Zaroff 2002).

Cardiac transplant: Acute cellular rejection (treatment) or antibody-mediated rejection (treatment) (off-label use): IV (sodium succinate): 250 to 1,000 mg daily for 3 days (AHA [Colvin 2015]; ISHLT [Costanzo 2010]).

COPD exacerbation (off-label use): Note: Dose, frequency, and duration of therapy not established. GOLD guidelines recommend the use of oral prednisone; however, methylprednisolone may be used as an alternative (GOLD [Decramer 2014]). No comparative studies exist to examine safety and efficacy between low-, medium-, or high-dose regimens. While several clinical trials have examined the use of methylprednisolone in this setting, these trials included low numbers of patients, employed vastly different regimens, and/or examined different clinical outcomes (Albert 1980; Alía 2011; Niewoehner 1999; Sayiner 2001; Shortall 2002; Vrondracek 2006; Willaert 2002). Current dosing strategies are empiric and have not been established by clinical trials. Based on expert opinion, commonly used regimens ranging from 60 to 125 mg IV administered 1 to 4 times daily followed by oral therapy (eg, prednisone 40 mg once daily) for a total of 5 to 14 days of therapy may be employed; the shorter duration (ie, 5 days) may be preferred (Leuppi 2013); however, comparative prospective data does not exist. IV administration with a higher dose (eg, ≥60 mg) may be preferred for those patients with impending or actual acute respiratory failure; outcome trials not available for this approach.

Dermatomyositis/polymyositis (off-label dosing): IV (succinate): 1,000 mg daily for 3 to 5 days for severe muscle weakness, followed by conversion to oral prednisone (Drake 1996)

Gout, acute (off-label dosing): IV (succinate), IM: Initial: 0.5 to 2 mg/kg; may be repeated as clinically indicated (ACR guidelines [Khanna 2012])

Lupus nephritis (off-label dosing): High-dose “pulse” therapy: IV (succinate): 0.5 to 1 g/day for 3 days (Ponticelli 2010)

Pneumocystis pneumonia in AIDS patients (off-label use): IV (succinate): 30 mg twice daily on days 1 to 5, then 30 mg once daily on days 6 to 10, then 15 mg once daily on days 11 to 21 (CDC 2009a).

Spinal cord injury, acute (off-label use): IV (succinate): 30 mg/kg over 15 minutes followed in 45 minutes by a continuous infusion of 5.4 mg/kg/hour for 23 hours; Note: Due to insufficient evidence of clinical efficacy (ie, preserving or improving spinal cord function), the routine use of methylprednisolone in the treatment of acute spinal cord injury is no longer recommended. If used in this setting, methylprednisolone should not be initiated >8 hours after the injury; not effective in penetrating trauma (eg, gunshot) (Consortium for Spinal Cord Medicine 2008).

Frequency not defined:

Cardiovascular: Bradycardia, cardiac arrest, cardiac arrhythmia, cardiac failure, cardiomegaly, circulatory shock, congestive heart failure, edema, embolism (fat), hypertension, hypertrophic cardiomyopathy (in neonates), myocardial rupture (post MI), syncope, tachycardia, thromboembolism, thrombophlebitis, vasculitis

Central nervous system: Arachnoiditis, depression, emotionallability, euphoria, headache, increased intracranial pressure, insomnia, malaise, meningitis, myasthenia, neuritis, neuropathy, paraplegia, paresthesia, personality changes, psychic disorders, pseudotumor cerebri (usually following discontinuation), seizure, sensory disturbance, vertigo

Dermatologic: Acne vulgaris, allergic dermatitis, alopecia, atrophic striae, diaphoresis, ecchymoses, epidermal thinning, erythema, exfoliation of skin, facial erythema, hyperpigmentation, hypertrichosis, hypopigmentation, skin atrophy, skin rash, suppression of skin test reaction, thinning hair, urticaria, xeroderma

Endocrine & metabolic: Adrenal suppression, calcinosis, cushingoid state, Cushing syndrome, decreased glucose tolerance, diabetes mellitus, fluid retention, glycosuria, growth suppression (children), hirsutism, HPA-axis suppression, hyperglycemia, hyperlipidemia, hypokalemia, hypokalemic alkalosis, insulin resistance (increased requirements for insulin or oral hypoglycemic agents in diabetes), menstrual disease, moon face, negative nitrogen balance, protein catabolism, sodium retention, weight gain

Gastrointestinal: Abdominal distention, bladder dysfunction (after intrathecal administration, including bowel dysfunction), carbohydrate intolerance (increased), gastrointestinal hemorrhage, gastrointestinal perforation, hiccups, increased appetite, intestinal perforation (of both of the small and large intestines; especially in patients with inflammatory bowel disease), nausea, pancreatitis, peptic ulcer, spermatozoa disorder (decreased motility and number of spermatozoa), ulcerative esophagitis

Hematologic: Leukocytosis (transient), malignant neoplasm (secondary), petechia

Hepatic: Hepatomegaly, increased liver enzymes, increased serum transaminases

Hypersensitivity: Anaphylactoid reaction, anaphylaxis, angioedema, hypersensitivity reaction

Infection: Increased susceptibility to infection, infection (ophthalmic), sterile abscess

Local: Injection site infection

Neuromuscular & skeletal: Amyotrophy, arthropathy, aseptic necrosis of femoral head, aseptic necrosis of humoral head, bone fracture, Charcot-like arthropathy, lipotrophy, osteoporosis, rupture of tendon, steroid myopathy, vertebral compression fracture

Ophthalmic: Blindness, exophthalmoses, glaucoma, increased intraocular pressure, ophthalmic inflammation (ophthalmic), subcapsular posterior cataract, visual impairment

Respiratory: Pulmonary edema, rhinitis

Miscellaneous: Anaphylactoid reaction, anaphylaxis, angioedema, hypersensitivity reactions, tissue sloughing (residue or slough at injection site), wound healing impairment

<1%, postmarketing, and/or case reports: Venous thrombosis (Johannesdottir 2013)

• Discuss specific use of drug and side effects with patient as it relates to treatment. HCAHPS: During this hospital stay, were you given any medicine that you had not taken before? Before giving you any new medicine, how often did hospital staff tell you what the medicine was for? How often did hospital staff describe possible side effects in a way you could understand?)

• Patient may experience nausea, vomiting, insomnia, agitation, or sweating a lot. Have patient report immediately to prescriber signs of infection, signs of high blood sugar (confusion, feeling sleepy, more thirst, hunger, passing urine more often, flushing, fast breathing, or breath that smells like fruit), signs of low potassium (muscle pain or weakness, muscle cramps, or an abnormal heartbeat), signs of Cushing’s disease (weight gain in upper back or stomach; moon face; severe headache; or slow healing), signs of adrenal gland problems (severe nausea, vomiting, severe dizziness, passing out, muscle weakness, severe fatigue, mood changes, lack of appetite, or weight loss), signs of pancreatitis (severe abdominal pain, severe back pain, severe nausea, or vomiting), signs of skin changes (pimples, stretch marks, slow healing, or hair growth), severe loss of strength and energy; irritability; tremors; tachycardia; confusion; dizziness; shortness of breath; excessive weight gain; swelling of arms or legs; angina; menstrual irregularities; bone pain; joint pain; vision changes; behavioral changes; depression; seizures; burning or numbness feeling; bruising; bleeding; severe abdominal pain; vomiting blood; or black, tarry, or bloody stools (HCAHPS).

• Educate patient about signs of a significant reaction (eg, wheezing; chest tightness; fever; itching; bad cough; blue skin color; seizures; or swelling of face, lips, tongue, or throat). Note: This is not a comprehensive list of all side effects. Patient should consult prescriber for additional questions.

Intended Use and Disclaimer: Should not be printed and given to patients. This information is intended to serve as a concise initial reference for healthcare professionals to use when discussing medications with a patient. You must ultimately rely on your own discretion, experience and judgment in diagnosing, treating and advising patients.