For Intramuscular Administration: When oral therapy is not feasible and the strength, dosage form, and route of administration of the drug reasonably lend the preparation to the treatment of the condition, the intramuscular use of Methylprednisolone acetate Sterile Aqueous Suspension is indicated as follows: 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. Miscellaneous: Trichinosis with neurologic or myocardial involvement, tuberculous meningitis with subarachnoid block or impending block when used concurrently with appropriate antituberculous chemotherapy. 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, andsystemic lupus erythematosus. For Intra-Articular Or Soft Tissue Administration: Methylprednisolone acetate is indicated as adjunctive therapy for short-term administration (to tide the patient over an acute episode or exacerbation) in acute gouty arthritis, acute and subacute bursitis, acute nonspecific tenosynovitis, epicondylitis, rheumatoid arthritis, synovitis of osteoarthritis. For Intralesional Administration: Methylprednisolone acetate is indicated for intralesional use in alopecia areata, discoid lupus erythematosus, keloids, localized hypertrophic, infiltrated, inflammatory lesions of granuloma annulare, lichen planus, lichen simplex chronicus (neurodermatitis), and psoriatic plaques, necrobiosis lipoidica diabeticorum. Methylprednisolone acetate acetate also may be useful in cystic tumors of an aponeurosis or tendon(ganglia).
Pharmacodynamic properties: Methylprednisolone Is a potent anti-inflammatory agent with the capacity to profoundly inhibit the immune system. Glucocorticoids primarily bind to and activate intracellular glucocorticoid receptors that being activated bind to promoter regions of DMA (which may activate or suppress transcription) and activate transcription factors that result in inactivation of genes through deacetylation of histones. Methylprednisolone influences the kidney and fluid & electrolyte balance, lipid,
protein, and carbohydrate metabolism, skeletal muscle, the cardiovascular system, the immune system, the nervous system, and the endocrine system.
Pharmacokinetic properties: The absolute bioavailability of Methylprednisclone is generally high (82% to 89%) following oral administration and rapidly absorbed and the maximum plasma concentration is achieved around 1.5 to 2.3 hours across doses following oral administration in normal healthy adults. Methylprednisolone is widely distributed into the tissues and its volume of distribution is 41-61.5 liter. It crosses the Wood-brain barrier and the placental barrier and is secreted in breast milk. The plasma protein binding of Methylprednisolone in humans is approximately 77%. Methylprednisolone is metabolized in the liver to inactive metabolites. No dosing adjustments are necessary for renal failure. Methylprednisolone is haemodializable.
Intra-articular- Anti-inflammatory or immunosuppressive Adult: As methylprednisolone acetate: 4-10 mg (small joints); 10-40 mg (medium joints); 20-80 mg (large joints). May be repeated every 1-5 wk depending on patient’s response. Intralesional- Corticosteroid-responsive dermatoses Adult: As methylprednisolone acetate: 20-60 mg; 1-4 inj may be given at intervals depending on the type of lesion and the duration of improvement from the initial inj. Intralesional- Anti-inflammatory or immunosuppressive Adult: As methylprednisolone acetate: 20-60 mg every 1-5 wk depending on patient’s response.
Erythromycin, Clarithromycin, Phenobarbital, Phenytoin, Rifampin and Ketoconazole inhibit the metabolism of Methylprednisolone. Estrogens, including With control pills, can increase the effect of corticosteroids by 50%. Cyclosporin reduces the metabolism of Methylprednisolone. while Methylprednisolone reduces the metabolism of Cyclosporin. Methylprednisolone may increase or decrease the effect of blood thinners (e.g. Warfarin). For all these Interactions, the dose of Methylprednisolone may need to be lowered.
Systemic fungal infections unless specific anti-infective therapy is employed; IM admin in idiopathic thrombocytopenic purpura. Intrathecal admin. Concurrent admin of live or live, attenuated vaccines (in patients receiving immunosuppressive doses).
Adrenal suppression, anaphylactoid reactions, immunosuppression, acute myopathy, Kaposi’s sarcoma, psychiatric disturbances (e.g. depression, euphoria, insomnia, mood swings, personality changes), increased susceptibility and severity of infections, impaired healing, HTN, Na and fluid retention, CV collapse (high dose), peptic ulcer, cataract subcapsular, skin atrophy, acne, muscular weakness, growth retardation, decreased blood K; dermal/subdermal skin depression at inj site. Topical: Itching, burning erythema, vesiculation; rarely, folliculitis, hypertrichosis, perioral dermatitis, skin discolouration, allergic skin reactions.
Category C: Either studies in animals have revealed adverse effects on the foetus (teratogenic or embryocidal or other) and there are no controlled studies in women or studies in women and animals are not available. Drugs should be given only if the potential benefit justifies the potential risk to the foetus.
Report of acute toxicity and/or death following an overdose of glucocorticoid ere rare. No specific antidote is available; treatment is supportive and symptomatic. Serum electrolytes should be monitored.
Store in a cool and dry place, away from light. Keep out of reach of children.
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