Methylprednisolone (3 brand names, 2 dosage forms, 2 routes)
Available dosage forms: TABLET, OINTMENT.
Routes of administration: ORAL, OPHTHALMIC.
Brand Names
- MEDROL
- METHYLPREDNISOLONE
- NEO-MEDROL
Indications and Usage
Methylprednisolone Tablets are indicated in the following conditions: 1. Endocrine Disorders Primary or secondary adrenocortical insufficiency (hydrocortisone or cortisone is the first choice; synthetic analogs may be used in conjunction with mineralocorticoids where applicable; in infancy mineralocorticoid supplementation is of particular importance). Congenital adrenal hyperplasia Nonsuppurative thyroiditis Hypercalcemia associated with cancer 2. Rheumatic Disorders As adjunctive therapy for short-term administration (to tide the patient over an acute episode or exacerbation) in: Rheumatoid arthritis, including juvenile rheumatoid arthritis (selected cases may require low-dose maintenance therapy) Ankylosing spondylitis Acute and subacute bursitis Synovitis of osteoarthritis Acute nonspecific tenosynovitis Post-traumatic osteoarthritis Psoriatic arthritis Epicondylitis Acute gouty arthritis 3. Collagen Diseases During an exacerbation or as maintenance therapy in selected cases of: Systemic lupus erythematosus Systemic dermatomyositis (polymyositis) Acute rheumatic carditis 4. Dermatologic Diseases Bullous dermatitis herpetiformis Severe erythema multiforme (Stevens-Johnson syndrome) Severe seborrheic dermatitis Exfoliative dermatitis Mycosis fungoides Pemphigus Severe psoriasis 5. Allergic States Control of severe or incapacitating allergic conditions intractable to adequate trials of conventional treatment: Seasonal or perennial allergic rhinitis Drug hypersensitivity reactions Serum sickness Contact dermatitis Bronchial asthma Atopic dermatitis 6. Ophthalmic Diseases Severe acute and chronic allergic and inflammatory processes involving the eye and its adnexa such as: Allergic corneal marginal ulcers Herpes zoster ophthalmicus Anterior segment inflammation Diffuse posterior uveitis and choroiditis Sympathetic ophthalmia Keratitis Optic neuritis Allergic conjunctivitis Chorioretinitis Iritis and iridocyclitis 7. Respiratory Diseases Symptomatic sarcoidosis Beryll
Dosage and Administration
The initial dosage of Methylprednisolone Tablets may vary from 4 mg to 48 mg of methylprednisolone per day depending on the specific disease entity being treated. In situations of less severity lower doses will generally suffice while in selected patients higher initial doses may be required. The initial dosage should be maintained or adjusted until a satisfactory response is noted. If after a reasonable period of time there is a lack of satisfactory clinical response, Methylprednisolone Tablets should be discontinued and the patient transferred to other appropriate therapy. IT SHOULD BE EMPHASIZED THAT DOSAGE REQUIREMENTS ARE VARIABLE AND MUST BE INDIVIDUALIZED ON THE BASIS OF THE DISEASE UNDER TREATMENT AND THE RESPONSE OF THE PATIENT.After a favorable response is noted, the proper maintenance dosage should be determined by decreasing the initial drug dosage in small decrements at appropriate time intervals until the lowest dosage which will maintain an adequate clinical response is reached. It should be kept in mind that constant monitoring is needed in regard to drug dosage. Included in the situations which may make dosage adjustments necessary are changes in clinical status secondary to remissions or exacerbations in the disease process, the patient’s individual drug responsiveness, and the effect of patient exposure to stressful situations not directly related to the disease entity under treatment; in this latter situation it may be necessary to increase the dosage of Methylprednisolone Tablets for a period of time consistent with the patient’s condition. If after long-term therapy the drug is to be stopped, it is recommended that it be withdrawn gradually rather than abruptly. Multiple Sclerosis:In treatment of acute exacerbations of multiple sclerosis daily doses of 200 mg of prednisolone for a week followed by 80 mg every other day for 1 month have been shown to be effective (4 mg of methylprednisolone is equivalent to 5 mg of prednisolone). ADT® (Alternate
Contraindications
Systemic fungal infections and known hypersensitivity to components.
Adverse Reactions
Fluid and Electrolyte Disturbances ▪ Sodium retention ▪ Congestive heart failure in susceptible patients ▪ Hypertension ▪ Fluid retention ▪ Potassium loss ▪ Hypokalemic alkalosis Musculoskeletal ▪ Muscle weakness ▪ Loss of muscle mass ▪ Steroid myopathy ▪ Osteoporosis ▪ Tendon rupture, particularly of the Achilles tendon ▪ Vertebral compression fractures ▪ Aseptic necrosis of femoral and humeral heads ▪ Pathologic fracture of long bones Gastrointestinal ▪ Peptic ulcer with possible perforation and hemorrhage ▪ Pancreatitis ▪ Abdominal distention ▪ Ulcerative esophagitis Increases in alanine transaminase (ALT, SGPT), aspartate transaminase (AST, SGOT), and alkaline phosphatase have been observed following corticosteroid treatment. These changes are usually small, not associated with any clinical syndrome and are reversible upon discontinuation. Dermatologic ▪ Impaired wound healing ▪ Petechiae and ecchymoses ▪ May suppress reactions to skin tests ▪ Thin fragile skin ▪ Facial erythema ▪ Increased sweating Neurological ▪ Increased intracranial pressure with papilledema (pseudo-tumor cerebri) usually after treatment ▪ Convulsions ▪ Vertigo ▪ Headache Endocrine ▪ Development of Cushingoid state ▪ Suppression of growth in children ▪ Secondary adrenocortical and pituitary unresponsiveness, particularly in times of stress, as in trauma, surgery or illness ▪ Menstrual irregularities ▪ Decreased carbohydrate tolerance ▪ Manifestations of latent diabetes mellitus ▪ Increased requirements of insulin or oral hypoglycemic agents in diabetics Ophthalmic ▪ Posterior subcapsular cataracts ▪ Increased intraocular pressure ▪ Glaucoma ▪ Exophthalmos Metabolic ▪ Negative nitrogen balance due to protein catabolism The following additional reactions have been reported following oral as well as parenteral therapy: Urticaria and other allergic, anaphylactic or hypersensitivity reactions.
Drug Interactions
The pharmacokinetic interactions listed below are potentially clinically important. Mutual inhibition of metabolism occurs with concurrent use of cyclosporin and methylprednisolone; therefore, it is possible that adverse events associated with the individual use of either drug may be more apt to occur. Convulsions have been reported with concurrent use of methylprednisolone and cyclosporin. Drugs that induce hepatic enzymes such as phenobarbital, phenytoin and rifampin may increase the clearance of methylprednisolone and may require increases in methylprednisolone dose to achieve the desired response. Drugs such as troleandomycin and ketoconazole may inhibit the metabolism of methylprednisolone and thus decrease its clearance. Therefore, the dose of methylprednisolone should be titrated to avoid steroid toxicity. Methylprednisolone may increase the clearance of chronic high dose aspirin. This could lead to decreased salicylate serum levels or increase the risk of salicylate toxicity when methylprednisolone is withdrawn. Aspirin should be used cautiously in conjunction with corticosteroids in patients suffering from hypoprothrombinemia. The effect of methylprednisolone on oral anticoagulants is variable. There are reports of enhanced as well as diminished effects of anticoagulant when given concurrently with corticosteroids. Therefore, coagulation indices should be monitored to maintain the desired anticoagulant effect.