Mepron (Methylprednisolone)

Uses

Methyl Prednisolone Tablets are used for the following conditions:

Endocrine Disorders: Primary or secondary adrenocortical insufficiency, Congenital adrenal hyperplasia, Nonsuppurative thyroiditis, Hypercalcemia associated with cancer

Rheumatic Disorders: As adjunctive therapy for short-term administration (to tide the patient over an acute episode orexacerbation) 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

Collagen Diseases: During an exacerbation or as maintenance therapy in selected cases of: Systemic lupus erythematosus Systemic dermatomyositis (polymyositis), 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 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

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

Respiratory Diseases: Symptomatic sarcoidosis, Berylliosis, Loeffler’s syndrome not manageable by other means, Fulminating or disseminated pulmonary tuberculosis when used concurrently with appropriate antituberculous chemotherapy, Aspiration pneumonitis

Hematologic Disorders: Idiopathic thrombocytopenic purpura in adults, Secondary thrombocytopenia in adults, Acquired (autoimmune) hemolytic anemia, Erythroblastopenia (RBC anemia), Congenital (erythroid) hypoplastic anemia

Neoplastic Diseases: For palliative management of: Leukemias and lymphomas in adults, Acute leukemia of childhood

Edematous States: To induce a diuresis or remission of proteinuria in the nephrotic syndrome, without uremia, of the idiopathic type or that due to lupus erythematosus.

Gastrointestinal Diseases: To tide the patient over a critical period of the disease in: Ulcerative colitis, Regional enteritis

Nervous System: Acute exacerbations of multiple sclerosis

Mepron (Methylprednisolone) is also used to associated treatment for these conditions: Acne Rosacea, Acute Gouty Arthritis, Adrenal cortical hypofunctions, Adrenocortical Hyperfunction, Allergic corneal marginal ulcers, Alopecia Areata (AA), Ankylosing Spondylitis (AS), Anterior Segment Inflammation, Aponeurosis contusion, Arthritis, Aspiration Pneumonitis, Asthma, Atopic Dermatitis (AD), Berylliosis, Bronchial Asthma, Bullous dermatitis herpetiformis, Bursitis, Chorioretinitis, Choroiditis, Congenital Adrenal Hyperplasia (CAH), Congenital Hypoplastic Anemia, Corneal Inflammation, Cushing's Syndrome, Degenerative Joint Disease, Dermatitis exfoliative generalised, Dermatitis, Contact, Discoid Lupus Erythematosus (DLE), Drug hypersensitivity reaction, Edema, Edema of the cerebrum, Epicondylitis, Erythroblastopenia, Gouty Arthritis, Hypercalcemia, Idiopathic Thrombocytopenic Purpura, Inflammation, Inflammatory Reaction of the Cysts, Iridocyclitis, Iritis, Keloid Scars, Leukemia, Acute, Lichen Planus (LP), Lichen simplex chronicus, Loeffler's syndrome, Malignant Lymphomas, Multiple sclerosis exacerbation, Mycosis Fungoides (MF), Necrobiosis lipoidica diabeticorum, Nummular Eczema, Ocular Inflammation, Ophthalmia, Sympathetic, Optic Neuritis, Pemphigus, Perennial Allergic Rhinitis (PAR), Polymyositis, Post-traumatic Osteoarthritis, Psoriatic Arthritis, Psoriatic plaque, Pure Red Cell Aplasia, Regional Enteritis, Rheumatoid Arthritis, Rheumatoid Arthritis, Juvenile, Sarcoidosis, Seasonal Allergic Conjunctivitis, Seasonal Allergic Rhinitis, Seborrheic Dermatitis, Eczematous, Secondary thrombocytopenia, Serum Sickness, Severe Allergic Asthma, Severe Seborrheic Dermatitis, Stevens-Johnson Syndrome, Synovitis, Systemic Lupus Erythematosus (SLE), Temporal Arteritis, Tendonitis exacerbated, Transfusion Reactions, Trichinosis, Tuberculosis (TB), Tuberculosis Meningitis, Tumors Metastatic to Brain, Ulcerative Colitis, Uveitis, Acquired immune hemolytic anemia, Acute nonspecific tenosynovitis, Acute rheumatic carditis, Cystic tumors of aponeurosis, Cystic tumors of tendon, Idiopathic eosinophilic pneumonias, Inflammatory dermatoses of the scalp, Localized Hypertrophic, Inflammatory, Infiltrated granuloma annulare lesions, Non-suppurative Thyroiditis, Severe Psoriasis, Systemic Dermatomyositis, Varicella-zoster virus acute retinal necrosis

How Mepron (Methylprednisolone) works

The short term effects of corticosteroids are decreased vasodilation and permeability of capillaries, as well as decreased leukocyte migration to sites of inflammation. Corticosteroids binding to the glucocorticoid receptor mediates changes in gene expression that lead to multiple downstream effects over hours to days.

Glucocorticoids inhibit neutrophil apoptosis and demargination; they inhibit phospholipase A2, which decreases the formation of arachidonic acid derivatives; they inhibit NF-Kappa B and other inflammatory transcription factors; they promote anti-inflammatory genes like interleukin-10.

Lower doses of corticosteroids provide an anti-inflammatory effect, while higher doses are immunosuppressive. High doses of glucocorticoids for an extended period bind to the mineralocorticoid receptor, raising sodium levels and decreasing potassium levels.

Dosage

Mepron (Methylprednisolone) dosage

The initial dosage of Methyl Prednisolone Tablets may vary from 4 mg to 48 mg of Methyl Prednisolone 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, Methyl Prednisolone 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 Mepron (Methylprednisolone) 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).

Side Effects

Short courses of Mepron (Methylprednisolone) are usually well-tolerated with few, mild side effects. Long term, high doses of Mepron (Methylprednisolone) may produce predictable and potentially serious side effects. Whenever possible, the lowest effective doses of Mepron (Methylprednisolone) should be used for the shortest length of time to minimize side effects. Alternate day dosing also can help reduce side effects. Side effects of Mepron (Methylprednisolone) and other corticosteroids range from mild annoyances to serious irreversible body damage. Side effects include fluid retention, weight gain, high blood pressure, potassium loss, headache, muscle weakness, hair growth on the face, glaucoma, cataracts, peptic ulceration, growth retardation in children, convulsions and psychic disturbances including depression, euphoria, insomnia etc.

Toxicity

The oral LD₅₀ in rats is >4g/kg. The intraperitoneal LD₅₀ in mice is 2292mg/kg and in rats is 100mg/kg.

Data regarding acute overdoses of glucocorticoids are rare. Chronic high doses of glucocorticoids can lead to the development of cataract, glaucoma, hypertension, water retention, hyperlipidemia, peptic ulcer, pancreatitis, myopathy, osteoporosis, mood changes, psychosis, dermal atrophy, allergy, acne, hypertrichosis, immune suppression, decreased resistance to infection, moon face, hyperglycemia, hypocalcemia, hypophosphatemia, metabolic acidosis, growth suppression, and secondary adrenal insufficiency. Treat acute overdoses with symptomatic and supportive therapy, while chronic overdoses will require temporarily reduced dosages.

Precaution

Adrenocortical insufficiency may persist for months after discontinuation of therapy; therefore, in any situation of stress occurring during that period, hormone therapy should be reinstituted. Since mineralocorticoid secretion may be impaired, salt and/or a mineralocorticoid should be administered concurrently. There is an enhanced effect of corticosteroids on patients with hypothyroidism and in those with cirrhosis. Corticosteroids should be used cautiously in conjunction with corticosteroids in hypoprothombinemia. Growth and development of infants and children on prolonged corticosteroid therapy should be carefully observed.

Interaction

Erythromycin, Clarithromycin, Phenobarbital, Phenytoin, Rifampin and Ketoconazole inhibit the metabolism of Mepron (Methylprednisolone). Estrogens including birth control pills, can increase the effect of corticosteroids by 50 %. Cyclosporin reduces the metabolism of Mepron (Methylprednisolone) while Mepron (Methylprednisolone) reduces the metabolism of Cyclosporin. Mepron (Methylprednisolone) may increase or decrease the effect of blood thinners (e.g. Warfarin). For all these interactions, the dose of Mepron (Methylprednisolone) may need to be lowered.

Food Interaction

• Avoid alcohol.
• Take with food. Food reduces GI irritation.

[Moderate] MONITOR: Grapefruit juice may increase the plasma concentrations of orally administered drugs that are substrates of the CYP450 3A4 isoenzyme.

The proposed mechanism is inhibition of CYP450 3A4-mediated first-pass metabolism in the gut wall by certain compounds present in grapefruit.

Because grapefruit juice inhibits primarily intestinal rather than hepatic CYP450 3A4, the magnitude of interaction is greatest for those drugs that undergo significant presystemic metabolism by CYP450 3A4 (i.e., drugs with low oral bioavailability).

In general, the effect of grapefruit juice is concentration-, dose- and preparation-dependent, and can vary widely among brands.

Certain preparations of grapefruit juice (e.g., high dose, double strength) have sometimes demonstrated potent inhibition of CYP450 3A4, while other preparations (e.g., low dose, single strength) have typically demonstrated moderate inhibition.

Pharmacokinetic interactions involving grapefruit juice are also subject to a high degree of interpatient variability, thus the extent to which a given patient may be affected is difficult to predict.

MANAGEMENT: Patients who regularly consume grapefruit or grapefruit juice should be monitored for adverse effects and altered plasma concentrations of drugs that undergo significant presystemic metabolism by CYP450 3A4.

Grapefruit and grapefruit juice should be avoided if an interaction is suspected.

Orange juice is not expected to interact with these drugs.

Mepron (Methylprednisolone) Cholesterol interaction

[Moderate] Corticosteroids may elevate serum triglyceride and LDL cholesterol levels if used for longer than brief periods.

Patients with preexisting hyperlipidemia may require closer monitoring during prolonged corticosteroid therapy, and adjustments made accordingly in their lipid-lowering regimen.

Mepron (Methylprednisolone) Hypertension interaction

[Moderate] Corticosteroids may cause hypernatremia, hypokalemia, fluid retention, and elevation in blood pressure.

These mineralocorticoid effects are most significant with fludrocortisone, followed by hydrocortisone and cortisone, then by prednisone and prednisolone.

The remaining corticosteroids, betamethasone, dexamethasone, methylprednisolone, and triamcinolone, have little mineralocorticoid activities.

However, large doses of any corticosteroid can demonstrate these effects, particularly if given for longer than brief periods.

Therapy with corticosteroids should be administered cautiously in patients with preexisting fluid retention, hypertension, congestive heart failure, and

Dietary sodium restriction and potassium supplementation may be advisable.

Mepron (Methylprednisolone) Drug Interaction

Moderate: aspirinMinor: albuterol / ipratropium, albuterol, alprazolamUnknown: diphenhydramine, duloxetine, omega-3 polyunsaturated fatty acids, cyclobenzaprine, fluticasone nasal, escitalopram, pregabalin, guaifenesin, acetaminophen / hydrocodone, acetaminophen, montelukast, acetaminophen, cyanocobalamin, ascorbic acid, cholecalciferol, cetirizine

Mepron (Methylprednisolone) Disease Interaction

Major: GI perforation, infections, prematurity, PUD, vaccinationModerate: (+) tuberculin test, cirrhosis, depression/psychoses, diabetes, electrolyte imbalance, fluid retention, hyperadrenocorticalism, hyperlipidemia, hypothyroidism, liver disease, MI, myasthenia gravis, myopathy, ocular herpes simplex, ocular toxicities, osteoporosis, scleroderma, strongyloidiasis, thromboembolism

Volume of Distribution

The average volume of distribution of methylprednisolone is 1.38L/kg.

Elimination Route

Oral methylprednisolone has 89.9% the bioavailability of oral methylprednisolone acetate, while rectal methylprednisolone has 14.2% the bioavailability. Intravitreal methylprednisolone has a T_max of 2.5h. Approximately 1/10 of an oral or IV dose of methylprednisolone will reach the vitreous humor. Further data regarding the absorption of methylprednisolone are not readily available.

Half Life

Mepron (Methylprednisolone) has a half life of 2.3h.

Clearance

The average plasma clearance of methylprednisolone is 336mL/h/kg.

Elimination Route

Mepron (Methylprednisolone) and its metabolites have been collected in urine in humans. A study in dogs showed 25-31% elimination in urine and 44-52% elimination in feces.

Pregnancy & Breastfeeding use

Pregnancy category C. Either studies in animals have revealed adverse effects on the foetus (teratogenic or embryocidal or other) and there is no controlled studies in women and animals are not available. Drugs should be given only if the potential benefit justifies the potential risk to the fetus.

Lactation: Mepron (Methylprednisolone) has not been adequately evaluated in nursing mothers.

Contraindication

Systemic fungal infections and known hypersensitivity to components.

Acute Overdose

Report of acute toxicity and/or death following overdose of glucocorticoid are rare. No specific antidote is available; treatment is supportive and symptomatic. Serum electrolytes should be monitored.

Storage Condition

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

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