Methylprednisolone Acetate

Indications

Methylprednisolone Acetate is used for: Anti-inflammatory or immunosuppressive, Corticosteroid-responsive dermatoses, Chronic contact dermatitis, Seborrheic dermatitis, Asthmatic patients, Allergic rhinitis (hay fever), Rheumatoid arthritis, Multiple sclerosis, Systemic lupus erythematosus

Adult Dose

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 Anti-inflammatory or immunosuppressive Adult: As methylprednisolone acetate: 20-60 mg every 1-5 wk depending on patient's response. Corticosteroid-responsive dermatoses Adult: As methylprednisolone acetate: 20-60 mg is injected into the lesion; 1-4 inj may be given at intervals depending on the type of lesion and the duration of improvement from the initial inj. Intramuscular Administration for Systemic Effect Usual dosing range, 10-80 mg IM every 1-2 weeks; as temporary substitute for PO, given in daily IM dose equal to daily PO dose;for prolonged effect, given in weekly IM dose equal to 7 times daily PO dose; may not be given IV Adrenogenital syndrome a single intramuscular injection of 40 mg every two weeks may be adequate. For maintenance of patients with rheumatoid arthritis the weekly intramuscular dose will vary from 40 to 120 mg. Dermatologic lesions benefited by systemic corticoid therapy 40 to 120 mg of methylprednisolone acetate administered intramuscularly at weekly intervals for one to four weeks. Acute severe dermatitis due to poison ivy relief may result within 8 to 12 hours following intramuscular administration of a single dose of 80 to 120 mg. Chronic contact dermatitis repeated injections at 5 to 10 day intervals may be necessary. Seborrheic dermatitis a weekly dose of 80 mg may be adequate to control the condition. Asthmatic patients, Allergic rhinitis (hay fever) IM administration of 80 to 120 mg, relief may result within 6 to 48 hours and persist for several days to two weeks.

Child Dose

Renal Dose

Administration

Contra Indications

Methylprednisolone acetate is contraindicated in patients with known hypersensitivity to the product and its constituents. Intramuscular corticosteroid preparations are contraindicated for idiopathic thrombocytopenic purpura. Methylprednisolone acetate injectable suspension is contraindicated for intrathecal administration. Methylprednisolone acetate is contraindicated in systemic fungal infections, except when administered as an intra-articular injection for localized joint conditions

Precautions

Patient w/ heart failure, HTN, DM, GI disease (e.g. diverticulitis, intestinal anastomoses, peptic ulcer, ulcerative colitis), multiple sclerosis, myasthenia gravis, acute MI, cataracts, glaucoma, osteoporosis, history of seizure disorder, thyroid disease. Avoid abrupt withdrawal. Renal and hepatic impairment (including cirrhosis). Childn. Pregnancy and lactation. Monitoring Parameters Monitor BP, blood glucose, electrolytes, growth in childn. Lactation: Drug enters milk; use with caution

Pregnancy-Lactation

Pregnancy category: C Lactation: Drug enters milk; use with caution

Interactions

Loss of corticosteroid-induced adrenal suppression w/ aminoglutethimide. Risk of hypokalaemia w/ K-depleting agents (e.g. amphotericin B, diuretics). Decreased clearance w/ macrolide antibiotics. May decrease serum levels of isoniazid. Increased clearance w/ cholestyramine. Risk of convulsions w/ ciclosporin. Increased risk of arrhythmias w/ digitalis glycosides. Decreased metabolism w/ oestrogens, including OCs. Enhanced metabolism w/ CYP3A4 inducers (e.g. rifampicin, barbiturates). Increased plasma concentrations w/ CYP3A4 inhibitors (e.g. ketoconazole, erythromycin). Risk of GI effects w/ aspirin or other NSAIDs. May increase the anticoagulant effect of warfarin. May reduce the therapeutic effect of antidiabetics. Potentially Fatal: May diminish response to live or live, attenuated vaccines.

Adverse Effects

Side effects of Methylprednisolone Acetate : Allergic Reactions Allergic or hypersensitivity reactions, anaphylactoid reaction, anaphylaxis, angioedema. Cardiovascular Bradycardia, cardiac arrest, cardiac arrhythmias, cardiac enlargement, circulatory collapse, congestive heart failure, fat embolism, hypertension, hypertrophic cardiomyopthy in premature infants, myocardial rupture following recent mycocardial infarction , pulmonary edema, syncope, tachycardia, thromboembolism, thrombophlebitis, vasculitis. Dermatologic Acne, allergic dermatitis, cutaneous and subcutaneous atrophy, dry scaly skin, ecchymoses and petechiae, edema, erythema, hyperpigmentation, hypopigmentation, impaired wound healing, increase sweating, rash, sterile abscess, striae, suppressed reactions to skin tests, thin fragile skin, thinning scalp hair, urticaria. Endocrine Decreased carbohydrate and glucose tolerance, development of cushingoid state, glycosuria, hirsutism, hypertrichosis, increased requirements for insulin or oral hypoglycemic agents in diabetes, manifestations of latent diabetes mellitus, menstrual irregularities, secondary adrenocortical and pituitary unresponsiveness (particularly in times of stress, as in trauma, surgery, or illness), suppression of growth in pediatric patients. Fluid and Electrolyte Disturbances Congestive heart failure in susceptible patients, Fluid retention, hypokalemic alkalosis, potassium loss, sodium retention. Gastrointestinal Abdominal distention, bowel/bladder dysfunction (after intrathecal administration), elevation in serum liver enzymes levels (usually reversible upon discontinuation), hepatomegaly, increased appetite, nausea, pancreatitis, peptic ulcer with possible subsequent perforation and hemorrhage, perforation of the small and large intestine (particularly in patients with inflammatory bowel disease), ulcerative esophagitis. Musculoskeletal Aseptic necrosis of femoral and humeral heads, calcinosis (following intra-articular or intra-lesional use), Charcot-like arthropathy, loss of muscle mass, muscle weakness, osteoporosis, pathologic fracture of long bones, postinjection flare (following intra-articular use), steroid myopathy, tendon rupture, vertebral compression fractures. Neurologic/Psychiatric Convulsions, depression, emotional instability, euphoria, headache, increased intracranial pressure with papilledema (pseudotumor cerebri) usually following discontinuation of treatment, insomnia, mood swings, neuritis, neuropathy, paresthesia, personality changes, psychic disorders, vertigo. Ophthalmic Exophthalmoses, glaucoma, increased intraocular pressure, posterior subcapsular cataracts.

Mechanism of Action

Methylprednisolone is a synthetic corticosteroid with mainly glucocorticoid activity and minimal mineralocorticoid properties. It decreases inflammation by suppression of migration of polymorphonuclear leukocytes and reversal of increased capillary permeability.