Methsolon 8 mg is indicated in:

Endocrine Disorders: Primary or secondary adrenocortical insufficiency, congenital adrenal hyperplasia, nonsuppurative thyroiditis, hypercalcemia associated with cancer.

Rheumatic Disorders: Juvenile rheumatoid arthritis, ankylosing spondylitis, acute and subacute bursitis, synovitis of osteoarthritis, acute nonspecific tenosynovitis, post-traumatic osteoarthritis, psoriatic arthritis, epicondylitis, acute gouty arthritis.

Collagen Diseases: Systemic lupus erythematosus, systemic dermatomyositis, acute rheumatic carditis.

Dermatologic Diseases: Bullous dermatitis herpetiformis, severe erythema multiforme (Stevens-Johnson syndrome), severe seborrheic dermatitis, exfoliative dermatitis, mycosis fungoides, pemphigus, severe psoriasis.

Allergic Conditions: Seasonal or perennial allergic rhinitis, drug hypersensitivity reactions, serum sickness, contact dermatitis, bronchial asthma, atopic dermatitis.

Ophthalmic Diseases: Allergic corneal ulcers, herpes zoster ophthalmicus, anterior segment inflammation, sympathetic ophthalmia, keratitis, optic neuritis, allergic conjunctivitis, chorioretinitis, iritis, iridocyclitis.

Respiratory Diseases: Symptomatic sarcoidosis, Loeffler’s syndrome not manageable by other means, berylliosis, aspiration pneumonitis.

Hematological Disorders: Idiopathic thrombocytopenic purpura in adults, secondary thrombocytopenia in adults, acquired autoimmune hemolytic anemia, erythroblastopenia, congenital hypoplastic anemia.

Neoplastic Diseases: Palliative management of leukemias and lymphomas in adults, acute leukemia of childhood.

Edematous States: To induce diuresis or remission of proteinuria in nephrotic syndrome without uremia, idiopathic type or lupus erythematosus-related.

Gastrointestinal Diseases: Ulcerative colitis and regional enteritis during acute exacerbations.

CNS Disease: Acute exacerbations of multiple sclerosis.

Methylprednisolone is a potent anti-inflammatory steroid with greater anti-inflammatory activity than prednisolone and a lower tendency to cause sodium and water retention. Its relative potency compared to hydrocortisone is at least 4:1.

Pharmacodynamic properties: Methylprednisolone is a potent anti-inflammatory and immunosuppressive agent. It binds to intracellular glucocorticoid receptors, which regulate gene transcription by interacting with DNA promoter regions and transcription factors, leading to suppression of inflammatory gene expression through histone deacetylation. It affects kidney function, fluid and electrolyte balance, lipid, protein and carbohydrate metabolism, skeletal muscle, cardiovascular system, immune system, nervous system, and endocrine system.

Pharmacokinetic properties: Oral bioavailability is high (82–89%). Peak plasma concentration occurs within 1.5–2.3 hours after oral dosing. It is widely distributed (volume of distribution 41–61.5 L), crosses the blood-brain barrier, placenta, and is excreted in breast milk. Plasma protein binding is about 77%. It is metabolized in the liver to inactive metabolites. No dose adjustment is needed in renal failure and it is dialyzable.

Methylprednisolone

The usual range is 2–48 mg daily in divided doses, depending on the specific disease being treated.

As anti-inflammatory or immunosuppressive initial dosage: As anti-inflammatory or immunosuppressive, the initial dosage of Methylprednisolone tablets may vary from 4–48 mg 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 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.

As anti-inflammatory or immunosuppressive maintenance dosage: 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. 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 the treatment of acute exacerbations of multiple sclerosis, daily doses of 160 mg of Methylprednisolone for a week followed by 64 mg every other day for 1 month have been shown to be effective.

Methylprednisolone 4 mg tablet can be used to treat and control severe allergy and dermatitis following the guideline listed below to minimize steroid withdrawal syndromes:

• Day 1: 2 tablets before breakfast + 1 tablet after lunch + 1 tablet after dinner + 2 tablets at bedtime
• Day 2: 1 tablet before breakfast + 1 tablet after lunch + 1 tablet after dinner + 2 tablets at bedtime
• Day 3: 1 tablet before breakfast + 1 tablet after lunch + 1 tablet after dinner + 1 tablet at bedtime
• Day 4: 1 tablet before breakfast + 1 tablet after lunch + 1 tablet at bedtime
• Day 5: 1 tablet before breakfast + 1 tablet at bedtime
• Day 6: 1 tablet before breakfast

Alternate-day therapy (ADT): Alternate-day therapy is a corticosteroid dosing regimen in which twice the usual daily dose of corticoid is administered every other morning. The purpose of this mode of therapy is to provide the patient requiring long-term pharmacologic dose treatment with the beneficial effects of corticoids, while minimizing certain undesirable effects, including pituitary-adrenal suppression, Cushingoid state, corticosteroid withdrawal symptoms, and growth suppression in children.

The following should be kept in mind when considering alternate-day therapy:

• Basic principles and indications for corticosteroid therapy should be applied.
• Alternate-day therapy is a therapeutic technique primarily designed for patients in whom long-term pharmacologic corticosteroid therapy is anticipated.
• In less severe disease processes in which corticosteroid therapy is indicated, it may be possible to initiate treatment with alternate-day therapy. More severe disease states usually will require daily divided high dose therapy for initial control of the disease process. The initial suppressive dose level should be continued until a satisfactory clinical response is obtained, usually four to ten days in the case of many allergic and collagen diseases.

Systemic fungal infections and known hypersensitivity to any component of the formulation.

Short-term courses of methylprednisolone are usually well tolerated with mild side effects. Long-term or high-dose therapy may cause serious and sometimes irreversible adverse effects. The lowest effective dose for the shortest duration is recommended. Alternate-day dosing may reduce side effects. Side effects include fluid retention, weight gain, hypertension, potassium loss, headache, muscle weakness, facial hair growth, glaucoma, cataracts, peptic ulcer, growth retardation in children, convulsions, and psychiatric effects such as depression, euphoria, and insomnia. Prolonged use may suppress adrenal function. Abrupt withdrawal may cause corticosteroid insufficiency with nausea, vomiting, and shock; therefore, dose should be tapered gradually. Gradual tapering also reduces disease flare risk.

Pregnancy Category C. The drug should be used only if the potential benefit justifies the potential risk to the fetus. Methylprednisolone has not been adequately evaluated in nursing mothers.

Adrenocortical insufficiency may persist for months after stopping therapy; hormone therapy may be needed during stress. Mineralocorticoid deficiency may require salt or mineralocorticoid supplementation. Increased corticosteroid effect may occur in hypothyroidism and cirrhosis. Use cautiously in ocular herpes simplex due to risk of corneal perforation. Aspirin should be used cautiously with corticosteroids in hypoprothrombinemia. Growth and development of children on long-term therapy should be monitored.

Acute toxicity or death from glucocorticoid overdose is rare. No specific antidote is available; treatment is supportive and symptomatic. Serum electrolytes should be monitored.

Glucocorticoids

Store in a cool and dry place, away from light. Keep out of reach of children.