Methylprednisolone

Therapeutic Area:

,

Generic Name:

Methylprednisolone

Dosage Form:

Ampoule

Drug Dose

Therapeutic Indications:

Allergic States:

Control of severe or incapacitating allergic conditions intractable to adequate trials of conventional treatment in asthma, atopic dermatitis, contact dermatitis, drug hypersensitivity reactions, seasonal or perennial allergic rhinitis, serum sickness, transfusion reactions.
Dermatologic Diseases:

Bullous dermatitis herpetiformis, exfoliative erythroderma, mycosis fungoides, pemphigus, severe erythema multiforme (Stevens-Johnson syndrome).
Endocrine Disorders:

Primary or secondary adrenocortical insufficiency (hydrocortisone or cortisone is the drug of choice; synthetic analogs may be used in conjunction with mineralocorticoids where applicable; in infancy,
mineralocorticoid supplementation is of particular importance), congenital adrenal hyperplasia, hypercalcemia associated with cancer, nonsuppurative thyroiditis.
Gastrointestinal Diseases:

To tide the patient over a critical period of the disease in regional enteritis (systemic therapy) and ulcerative colitis.
Hematologic Disorders:

Acquired (autoimmune) hemolytic anemia, congenital (erythroid) hypoplastic anemia (Diamond Blackfan anemia), pure red cell aplasia, select cases of secondary thrombocytopenia.

Neoplastic Diseases:

For palliative management of leukemias and lymphomas.
Nervous System:

Acute exacerbations of multiple sclerosis; cerebral edema associated with primary or metastatic brain tumor or craniotomy.

Ophthalmic Diseases:

Sympathetic ophthalmia, temporal arteritis, uveitis and ocular inflammatory conditions unresponsive to topical corticosteroids.
Renal Diseases:

To induce diuresis or remission of proteinuria in idiopathic nephrotic syndrome, or that due to lupus erythematosus.
Respiratory Diseases:

Berylliosis, fulminating or disseminated pulmonary tuberculosis when used concurrently with appropriate antituberculous chemotherapy, idiopathic eosinophilic pneumonias, symptomatic sarcoidosis.

Rheumatic Disorders:

As adjunctive therapy for short-term administration (to tide the patient over an acute episode or exacerbation) in acute gouty arthritis; acute rheumatic carditis; ankylosing spondylitis; psoriatic arthritis; rheumatoid arthritis, including juvenile rheumatoid arthritis (selected cases may require low-dose
maintenance therapy). For the treatment of dermatomyositis, polymyositis, and systemic lupus erythematosus.

Mechanism of Action:

In a tissue-specific manner, corticosteroids regulate gene expression subsequent to binding specific intracellular receptors and translocation into the nucleus. Corticosteroids exert a wide array of physiologic effects including modulation of carbohydrate, protein, and lipid metabolism and maintenance of fluid and electrolyte homeostasis. Moreover cardiovascular, immunologic, musculoskeletal, endocrine, and neurologic physiology are influenced by corticosteroids. Decreases inflammation by suppression of migration of polymorphonuclear leukocytes and reversal of increased capillary permeability.

Method of Administration:

Evidence to support an optimal dose and duration are lacking for most indications; recommendations provided are general guidelines only and primarily based on expert opinion. In general, glucocorticoid dosing should be individualized and the minimum effective dose/duration should be used. For select indications with weight-based dosing, consider using ideal body weight in obese patients, especially with longer durations of therapy

Notes

It is contraindicated in patients with known hypersensitivity to the product and its constituents. Intramuscular corticosteroid preparations are contraindicated for idiopathic thrombocytopenic purpura.

Interactions:

Amphotericin B: Corticosteroids (Systemic) may enhance the hypokalemic effect of Amphotericin B. Risk C: Monitor therapy

Antidiabetic Agents: Hyperglycemia-Associated Agents may diminish the therapeutic effect of Antidiabetic Agents. Risk C: Monitor therapy

CYP3A4 Inducers (Moderate): May decrease the serum concentration of MethylPREDNISolone. Risk C: Monitor therapy

CYP3A4 Inducers (Strong): May decrease the serum concentration of MethylPREDNISolone. Management: Consider methylprednisolone dose increases in patients receiving strong CYP3A4 inducers and monitor closely for reduced steroid efficacy. Risk D: Consider therapy modification

CYP3A4 Inhibitors (Moderate): May increase the serum concentration of MethylPREDNISolone. Risk C: Monitor therapy

CYP3A4 Inhibitors (Strong): May increase the serum concentration of MethylPREDNISolone. Risk C: Monitor therapy

Deferasirox: Corticosteroids (Systemic) may enhance the adverse/toxic effect of Deferasirox. Specifically, the risk for GI ulceration/irritation or GI bleeding may be increased. Risk C: Monitor therapy

Pregnancy and Lactation:

Methylprednisolone crosses the placenta.

Methylprednisolone is present in breast milk.

Use with caution.

Warning and Precaution:

  • Adrenal suppression: May cause hypercortisolism or suppression of hypothalamic-pituitary-adrenal (HPA) axis, particularly in younger children or in patients receiving high doses for prolonged periods. HPA axis suppression may lead to adrenal crisis. Withdrawal and discontinuation of a corticosteroid should be done slowly and carefully. Particular care is required when patients are transferred from systemic corticosteroids to inhaled products due to possible adrenal insufficiency or withdrawal from steroids, including an increase in allergic symptoms. Adult patients receiving >20 mg per day of prednisone (or equivalent) may be most susceptible. Fatalities have occurred due to adrenal insufficiency in asthmatic patients during and after transfer from systemic corticosteroids to aerosol steroids; aerosol steroids do not provide the systemic steroid needed to treat patients having trauma, surgery, or infections.
  • Anaphylactoid reactions: Rare cases of anaphylactoid reactions have been observed in patients receiving corticosteroids.
  • Dermal changes: Avoid injection or leakage into the dermis; dermal and/or subdermal skin depression may occur at the site of injection. Avoid deltoid muscle injection; subcutaneous atrophy may occur.
  • Hepatic effects: High doses of methylprednisolone IV (usually doses of 1 g/day in adults) may induce a toxic form of acute hepatitis (rare); serious hepatic injury may occur, resulting in acute liver failure and death. Time to onset can be several weeks or longer; resolution has been observed after discontinuation of therapy. Discontinue methylprednisolone if toxic hepatitis occurs. Avoid use of high doses in patients with a history of methylprednisone-induced toxic hepatitis.
  • Immunosuppression: Prolonged use of corticosteroids may increase the incidence of secondary infection, cause activation of latent infections, mask acute infection (including fungal infections), prolong or exacerbate viral or parasitic infections, or limit response to killed or inactivated vaccines. Exposure to chickenpox or measles should be avoided; corticosteroids should not be used to treat ocular herpes simplex. Corticosteroids should not be used for cerebral malaria, fungal infections, or viral hepatitis. Close observation is required in patients with latent tuberculosis and/or TB reactivity; restrict use in active TB (only fulminating or disseminated TB in conjunction with antituberculosis treatment). Amebiasis should be ruled out in any patient with recent travel to tropic climates or unexplained diarrhea prior to initiation of corticosteroids. Use with extreme caution in patients with Strongyloides infections; hyperinfection, dissemination and fatalities have occurred.
  • Kaposi sarcoma: Prolonged treatment with corticosteroids has been associated with the development of Kaposi sarcoma (case reports); discontinuation may result in clinical improvement (Goedert 2002).
  • Myopathy: Acute myopathy has been reported with high dose corticosteroids, usually in patients with neuromuscular transmission disorders; may involve ocular and/or respiratory muscles; monitor creatine kinase; recovery may be delayed.
  • Psychiatric disturbances: Corticosteroid use may cause psychiatric disturbances, including euphoria, insomnia, mood swings, personality changes, severe depression, or psychotic manifestations. Preexisting psychiatric conditions may be exacerbated by corticosteroid use.
  • Septic arthritis: May occur as a complication to parenteral therapy; institute appropriate antimicrobial therapy as required.

Adverse Reactions:

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

Central nervous system: Arachnoiditis, depression, emotional lability, 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

Storage:

Store below 30ºC and protect from freezing.