Indications

Primary or secondary adrenocortical insufficiency, congenital adrenal hyperplasia, nonsuppurative thyroiditis, and cancer-related hypercalcemia are all examples of endocrine disorders.

Rheumatoid Arthritis is one of the most common rheumatic diseases. Ankylosing Spondylitis, Acute, and Subacute Bursitis, Osteoarthritis Synovitis, Acute nonspecific Tenosynovitis, Post-traumatic Osteoarthritis, Psoriatic Arthritis, Epicondylitis, Acute Gouty Arthritis

Acute Rheumatic Carditis, Systemic Lupus Erythematosus, and Systemic Dermatomyositis are all collagen diseases.

Bullous Dermatitis Herpetiformis, Severe Erythema Multiforme (Stevens-Johnson syndrome), Severe.

Seasonal or perennial allergic rhinitis, drug hypersensitivity reactions, serum sickness, contact dermatitis, bronchial asthma, and atopic dermatitis are all examples of allergies.

Allergic Corneal Ulcers, Herpes Zoster Ophthalmicus, Anterior Segment Inflammation, Sympathetic Ophthalmia, Keratitis, Optic Neuritis, Allergic Conjunctivitis, Chorioretinitis, Iriditis, and Iridocyclitis are all examples of ophthalmic diseases.

Symptomatic sarcoidosis, Loeffler’s syndrome that cannot be treated with other medications, berylliosis, and aspiration pneumonitis are all examples of respiratory diseases.

Pharmacology

Pharmacodynamic properties: Methylprednisolone is a powerful anti-inflammatory with the ability to suppress the immune system completely. Glucocorticoids bind to and activate intracellular glucocorticoid receptors, which then bind to promoter regions of DMA (which can either activate or repress transcription) and activate transcription factors, resulting in gene inactivation via histone deacetylation. The kidneys, fluid and electrolyte balance, lipid, protein, and carbohydrate metabolism, skeletal muscle, the cardiovascular system, the immunological system, the neurological system, and the endocrine system are all affected by methylprednisolone.

Pharmacokinetic properties: Methylprednisclone has a high absolute bioavailability (82–89%) after oral administration, is rapidly absorbed, and the maximum plasma concentration is reached between 1.5 and 2.3 hours after oral administration across dosages in normal healthy adults. Methylprednisolone is widely dispersed throughout the body, with a distribution volume of 41-61.5 liter. It is secreted in breast milk after crossing the Wood-Brain Barrier and the Placental Barrier. In humans, Methylprednisolone binds to about 77 percent of plasma proteins. In the liver, methylprednisolone is converted to inactive metabolites. Renal dosage does not necessitate any changes.

Dosage & Administration

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 dirtied 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 to control severe allergy end dermatitis following the guideline listed below to minimize the 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 stats, Corficoid 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 corticoid therapy is anticipated.
• In less severe disease processes in which corticoid 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.

Interaction

Methylprednisolone metabolism is inhibited by Erythromycin, Clarithromycin, Phenobarbital, Phenytoin, Rifampin, and Ketoconazole. Estrogens, such as those found in birth control pills, can boost the effectiveness of corticosteroids by up to 50%. Methylprednisolone metabolism is slowed by cyclosporin. Cyclosporin metabolism is slowed by Methylprednisolone. Methylprednisolone can make blood thinners work better or worse (e.g. Warfarin). The dose of Methylprednisolone may need to be reduced as a result of all of these interactions.

Contraindications

Systemic fungal infections arid known as hypersensitivity to components.

Side Effects

Short courses of Methylprednisolone are generally well tolerated, with only a few minor side effects. High doses of Methyiprednisoione taken over a long period of time can have predictable and sometimes dangerous adverse effects. To avoid adverse effects, the lowest effective doses of Methylprednisolone should be administered for the shortest duration possible. Dosing on different days can also assist to reduce adverse effects. Methylprednisolone and other corticosteroids have a wide spectrum of side effects, from minor irritations to severe body harm. Fluid retention, weight gain, high blood pressure, potassium loss, headache, muscle weakness, facial hair growth, glaucoma, cataracts, and peptic ulcers are all possible side effects.

Pregnancy & Lactation

Pregnancy category C. Dregs should be given only if the potential benefit justifies the potential risk te the foetus. Mefhyiprednisofone has not been adequately evaluated in nursing mothers.

Precautions & Warnings

Adrenocortical insufficiency can last for months after you stop taking hormone therapy, therefore if you have a stressful circumstance during that time, hormone therapy should be restarted. Salt and/or a mineralocorticoid should be given together because mineralocorticoid secretion may be inhibited. Corticosteroids have a stronger effect on hypothyroidism patients and those with cirrhosis. Because of the risk of corneal perforation, corticosteroids should be taken with caution in individuals with ocular herpes simplex. In hypoprothrombinemia, aspirin should be taken with caution when used with corticosteroids. Infants and children’s growth and development on a long-term basis.

Therapeutic Class

Glucocorticoids

Storage Conditions

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

Pharmaceutical Name

Ziska Pharmaceuticals Ltd.