Methylprednisolone

Oral
Anti-inflammatory or immunosuppressive
Adult: Dosage is individualised according to the condition being treated and patient's response. Initially, 4-48 mg daily; higher initial doses of up to 100 mg daily or more may be used in acute severe conditions. Dosage recommendations may vary among countries and individual products (refer to specific product or local treatment guidelines).
Child: Dosage is individualised according to the condition being treated and patient's response. Use the lowest effective dose for the shortest possible duration. Treatment recommendations may vary among countries and individual products (refer to specific product or local treatment guidelines).

Intravenous
Anti-inflammatory or immunosuppressive
Adult: Dosage is individualised according to the condition being treated and patient's response. As methylprednisolone Na succinate: Initially, 10-500 mg daily via inj or infusion. Administer doses exceeding 250 mg over at least 30 minutes and doses up to 250 mg over at least 5 minutes. Dosage recommendations may vary among countries and individual products (refer to specific product or local treatment guidelines).
Child: For treatment of high dose indications (e.g. haematological, rheumatic, renal, and dermatological conditions): As methylprednisolone Na succinate: 30 mg/kg daily via inj or infusion. Max: 1,000 mg daily. Doses may be given once daily or on alternate days for up to 3 doses. Dosage recommendations may vary among countries and individual products (refer to specific product or local treatment guidelines).
Reconstitution: Methylprednisolone Na succinate inj: Reconstitute vial with provided diluent or bacteriostatic water. For IV infusion, dilute reconstituted solution with 5% dextrose in water, 0.9% NaCl, or 5% dextrose in 0.9% NaCl solution.
Incompatibility: Methylprednisolone Na succinate inj: Incompatible with allopurinol, doxapram hydrochloride, tigecycline, diltiazem hydrochloride, Ca gluconate, vecuronium bromide, rocuronium bromide, cisatracurium besilate, glycopyrrolate, propofol.

Intravenous
Graft rejection reactions
Adult: Following transplantation: As methylprednisolone Na succinate: 500-1,000 mg daily via infusion over at least 30 minutes; continue until the patient has stabilised, usually not beyond 48-72 hours. Dosage recommendations may vary among countries and individual products (refer to specific product or local treatment guidelines).
Child: Following transplantation: As methylprednisolone Na succinate: 10-20 mg/kg daily for up to 3 days. Max: 1,000 mg daily.
Reconstitution: Methylprednisolone Na succinate inj: Reconstitute vial with provided diluent or bacteriostatic water. For IV infusion, dilute reconstituted solution with 5% dextrose in water, 0.9% NaCl, or 5% dextrose in 0.9% NaCl solution.
Incompatibility: Methylprednisolone Na succinate inj: Incompatible with allopurinol, doxapram hydrochloride, tigecycline, diltiazem hydrochloride, Ca gluconate, vecuronium bromide, rocuronium bromide, cisatracurium besilate, glycopyrrolate, propofol.

Intravenous
Acute spinal cord injury
Adult: As methylprednisolone Na succinate: 30 mg/kg via bolus inj over 15 minutes, followed by a 45-minute pause and then give 5.4 mg/kg/hour via infusion. Duration of infusion varies, for treatment initiated within 3 hours of injury, infusion may be given over 23 hours; for treatment initiated within 3-8 hours of injury, may give infusion over 47 hours.
Reconstitution: Methylprednisolone Na succinate inj: Reconstitute vial with provided diluent or bacteriostatic water. For IV infusion, dilute reconstituted solution with 5% dextrose in water, 0.9% NaCl, or 5% dextrose in 0.9% NaCl solution.
Incompatibility: Methylprednisolone Na succinate inj: Incompatible with allopurinol, doxapram hydrochloride, tigecycline, diltiazem hydrochloride, Ca gluconate, vecuronium bromide, rocuronium bromide, cisatracurium besilate, glycopyrrolate, propofol.

Intravenous
Acute exacerbations in multiple sclerosis
Adult: As methylprednisolone Na succinate: 1,000 mg daily for 3-5 days via infusion over at least 30 minutes. Dosage recommendations may vary among countries and individual products (refer to specific product or local treatment guidelines).
Reconstitution: Methylprednisolone Na succinate inj: Reconstitute vial with provided diluent or bacteriostatic water. For IV infusion, dilute reconstituted solution with 5% dextrose in water, 0.9% NaCl, or 5% dextrose in 0.9% NaCl solution.
Incompatibility: Methylprednisolone Na succinate inj: Incompatible with allopurinol, doxapram hydrochloride, tigecycline, diltiazem hydrochloride, Ca gluconate, vecuronium bromide, rocuronium bromide, cisatracurium besilate, glycopyrrolate, propofol.

Intramuscular
Anti-inflammatory or immunosuppressive
Adult: Dosage is individualised according to the condition being treated and patient's response. As methylprednisolone Na succinate: Initially, 10-500 mg daily. As methylprednisolone acetate: 40-120 mg via deep inj into the gluteal muscle. Dosage recommendations may vary among countries and individual products (refer to specific product or local treatment guidelines).
Reconstitution: Methylprednisolone Na succinate inj: Reconstitute vial with provided diluent or bacteriostatic water.
Incompatibility: Methylprednisolone Na succinate inj: Incompatible with allopurinol, doxapram hydrochloride, tigecycline, diltiazem hydrochloride, Ca gluconate, vecuronium bromide, rocuronium bromide, cisatracurium besilate, glycopyrrolate, propofol.

Intra-articular
Osteoarthritis
Adult: Dosage is individualised according to the size of the joint and severity of the condition. As methylprednisolone acetate: 4-10 mg (small joints); 10-40 mg (medium joints); 20-80 mg (large joints). May be repeated every 1-5 weeks or more depending on patient's response.

Intra-articular
Rheumatoid arthritis
Adult: Dosage is individualised according to the size of the joint and severity of the condition. As methylprednisolone acetate: 4-10 mg (small joints); 10-40 mg (medium joints); 20-80 mg (large joints). May be repeated every 1-5 weeks or more depending on patient's response.

Intralesional
Keloid scar
Adult: As methylprednisolone acetate: 20-60 mg administered directly into the lesion. For large lesions, doses of 20-40 mg distributed by repeated inj may be necessary. Usually, 1-4 inj are employed.

Intralesional
Alopecia areata
Adult: As methylprednisolone acetate: 20-60 mg administered directly into the lesion. For large lesions, doses of 20-40 mg distributed by repeated inj may be necessary. Usually, 1-4 inj are employed.

Intralesional
Discoid lupus erythematosus
Adult: As methylprednisolone acetate: 20-60 mg administered directly into the lesion. For large lesions, doses of 20-40 mg distributed by repeated inj may be necessary. Usually, 1-4 inj are employed.

Intralesional
Lichen planus
Adult: For treatment of localised hypertrophic, infiltrated, inflammatory lesions: As methylprednisolone acetate: 20-60 mg administered directly into the lesion. For large lesions, doses of 20-40 mg distributed by repeated inj may be necessary. Usually, 1-4 inj are employed.

Intralesional
Lichen simplex chronicus
Adult: For treatment of localised hypertrophic, infiltrated, inflammatory lesions: As methylprednisolone acetate: 20-60 mg administered directly into the lesion. For large lesions, doses of 20-40 mg distributed by repeated inj may be necessary. Usually, 1-4 inj are employed.

Intralesional
Granuloma annulare
Adult: For treatment of localised hypertrophic, infiltrated, inflammatory lesions: As methylprednisolone acetate: 20-60 mg administered directly into the lesion. For large lesions, doses of 20-40 mg distributed by repeated inj may be necessary. Usually, 1-4 inj are employed.

Intralesional
Plaque psoriasis
Adult: For treatment of localised hypertrophic, infiltrated, inflammatory lesions: As methylprednisolone acetate: 20-60 mg administered directly into the lesion. For large lesions, doses of 20-40 mg distributed by repeated inj may be necessary. Usually, 1-4 inj are employed.

Intrabursal
Bursitis
Adult: For treatment of subdeltoid, prepatellar, or olecranon bursitis: As methylprednisolone acetate: 4-30 mg administered directly into the bursae. Repeat administration may not be needed in most cases. Dosage recommendations may vary among countries and individual products (refer to specific product or local treatment guidelines).

Topical/Cutaneous
Eczema
Adult: For endogenous eczema, contact eczema, degenerative eczema, dyshidrotic eczema, or atopic dermatitis: As methylprednisolone aceponate 0.1% cream or ointment: Apply thinly onto the affected area once daily for up to 12 weeks. Treatment recommendations may vary among countries and individual products (refer to specific product or local treatment guidelines).
Child: As methylprednisolone aceponate 0.1% cream or ointment: Apply thinly onto the affected area once daily for up to 4 weeks. Treatment recommendations may vary among countries and individual products (refer to specific product or local treatment guidelines).

Special Populations: Patient subjected to unusual stress (e.g. trauma, surgery): Higher doses may be required.

Should be taken with food.

Untreated systemic fungal infections; idiopathic thrombocytopenic purpura (IM inj). Administration of live or live, attenuated vaccines (in patients receiving immunosuppressive doses of corticosteroids). Parenteral inj: Administration via intrathecal route.

Patient with known or suspected parasitic infections (e.g. Strongyloides infestation), history of any drug allergy, thyroid disease, diabetes mellitus or family history of diabetes; existing or previous history of severe affective disorders; history of seizure disorder, myasthenia gravis, existing or family history of glaucoma, ocular herpes simplex; CHF, hypertension, acute MI, predisposition to thromboembolic disorders; peptic ulceration, fresh intestinal anastomoses, abscess or other pyogenic infections, diverticulitis, non-specific ulcerative colitis (if with possible impending perforation); latent TB and/or TB reactivity, osteoporosis, systemic sclerosis; suspected or confirmed phaeochromocytoma. Patient subjected to unusual stress. Avoid in patient with Cushing's disease; exposure to chickenpox or measles. Consider gradual withdrawal in patients who have repeated courses (particularly if given for >3 weeks), have taken a short course within a year of cessation of long-term therapy (months or years), may have reasons for adrenocortical insufficiency aside from exogenous corticosteroid therapy, are receiving doses >32 mg daily, or are repeatedly taking doses in the evening. Renal and hepatic impairment. Children. Pregnancy and lactation. Monitoring Parameters Monitor blood pressure, weight, intraocular pressure (if >6 months of use); growth and development (in children), BMD. Obtain electrolyte and blood glucose levels. Monitor for signs of infection, HPA axis suppression, and changes in mood or behaviour.

Significant: Immunosuppression, increased susceptibility to infection, mask signs of infection; Kaposi's sarcoma, adrenal cortical atrophy (prolonged use); hypercortisolism or suppression of hypothalamic-pituitary-adrenal (HPA) axis (particularly in younger children or in those receiving high doses for long periods), withdrawal syndrome, new-onset or exacerbate Cushing's syndrome; increased blood glucose, worsen pre-existing diabetes; psychiatric disturbances (e.g. severe depression, mood swings, insomnia); epidural lipomatosis (prolonged use at high doses), visual disturbance; posterior subcapsular cataracts and nuclear cataracts (prolonged use, particularly in children), exophthalmos, increased intraocular pressure which may result in glaucoma with possible optic nerve damage; dyslipidaemia, hypertension, thrombosis (including venous thromboembolism); acute pancreatitis, acute myopathy (high dose); growth retardation (children); Charcot-like arthropathies (particularly after repeated intra-articular inj), fluid retention, electrolyte disturbances, scleroderma renal crisis. Rarely, anaphylactic or anaphylactoid reactions, hepatobiliary disorders. Gastrointestinal disorders: Peptic ulcer. General disorders and administration site conditions: Impaired healing; application site burning or pruritus (topical). Musculoskeletal and connective tissue disorders: Muscle weakness. Skin and subcutaneous tissue disorders: Acne, skin atrophy.
Potentially Fatal: Phaeochromocytoma crisis, serious hepatic injury.

Decreased plasma concentration with CYP3A4 inducers (e.g. rifampicin, phenobarbital, phenytoin, primidone). May increase the risk of adverse events with other CYP3A4 substrates (e.g. tacrolimus, cyclophosphamide). Increased plasma concentration with CYP3A4 inhibitors (e.g. ketoconazole, troleandomycin, mibefradil, cimetidine). May increase the acetylation rate and clearance of isoniazid. Incidence of gastrointestinal bleeding and ulceration may be increased when used concomitantly with NSAIDs. May increase the clearance of high dose aspirin, which may result in decreased salicylate levels. Concomitant use of high dose methylprednisolone and anticholinergics (e.g. neuromuscular blocking agents) may cause acute myopathy. May antagonise the effects of neuromuscular blockers (e.g. pancuronium, vecuronium). Effects of anticholinesterases in myasthenia gravis may be reduced by methylprednisolone. May enhance the efficacy of coumarin anticoagulants. Increased risk of hypokalaemia with K-depleting agents (e.g. diuretics, amphotericin B). Adrenal suppression induced by aminoglutethimide may exacerbate the endocrine changes caused by prolonged methylprednisolone therapy. Ciclosporin may enhance the seizure-potentiating effect of methylprednisolone.
Potentially Fatal: May diminish the efficacy of live or live, attenuated vaccines.

Increased plasma concentration with grapefruit juice.

Reduced response to skin tests.

Methylprednisolone is a synthetic glucocorticoid and a methyl derivative of prednisolone, which has potent anti-inflammatory and immunosuppression properties. It acts mainly by regulating gene expression following binding to specific intracellular receptors and translocation into the nucleus. Additionally, it reduces inflammation by inhibiting the migration of polymorphonuclear leucocytes and reversing the increased capillary permeability.
Onset: As methylprednisolone Na succinate: Within 1 hour (IV). As methylprednisolone acetate: 1 week (intra-articular).
Duration: As methylprednisolone acetate: 1-5 weeks (intra-articular).
Absorption: Rapidly or well absorbed from the gastrointestinal tract. Absorbed from joints but more slowly after deep IM inj (as methylprednisolone acetate). Bioavailability: 82-89% (oral). Time to peak plasma concentration: Oral: 1.5-2.3 hours; IV: 0.8 hours (as methylprednisolone Na succinate).
Distribution: Widely distributed into tissues. Crosses the placenta and blood-brain barrier; enters breast milk (small amounts). Volume of distribution: As methylprednisolone Na succinate: 24 ± 6 L (IV). Plasma protein binding: Approx 77%, mainly to globulin.
Metabolism: Metabolised mainly in the liver by CYP3A4 isoenzyme and to a lesser extent in the kidney into inactive metabolites.
Excretion: Via urine (oral: 1.3%; IV: 9.2% as unchanged drug [as methylprednisolone Na succinate]). Elimination half-life: 1.8-5.2 hours.

Intra-articular: Methylprednisolone acetate inj: Store between 20-25°C. Storage recommendations may vary among individual products. Refer to detailed product guidelines. Intrabursal: Methylprednisolone acetate inj: Store between 20-25°C. Storage recommendations may vary among individual products. Refer to detailed product guidelines. Intralesional: Methylprednisolone acetate inj: Store between 20-25°C. Storage recommendations may vary among individual products. Refer to detailed product guidelines. Intramuscular: Methylprednisolone acetate inj: Store between 20-25°C. Methylprednisolone Na succinate inj: Store unreconstituted vials between 20-25°C. Protect from light. Once reconstituted, store solutions between 20-25°C and use within 48 hours of mixing. Storage recommendations may vary among individual products. Refer to detailed product guidelines. Intravenous: Methylprednisolone Na succinate inj: Store unreconstituted vials between 20-25°C. Protect from light. Once reconstituted, store solutions between 20-25°C and use within 48 hours of mixing. Storage recommendations may vary among individual products. Refer to detailed product guidelines. Oral: Tab: Store between 20-25°C. Storage recommendations may vary among individual products. Refer to detailed product guidelines. Topical/Cutaneous: Methylprednisolone aceponate cream or ointment: Store below 25°C. Storage recommendations may vary among individual products. Refer to detailed product guidelines.

Corticosteroid Hormones / Topical Corticosteroids

D07AA01 - methylprednisolone ; Belongs to the class of weak (group I) corticosteroids. Used in the treatment of dermatological diseases.
H02AB04 - methylprednisolone ; Belongs to the class of glucocorticoids. Used in systemic corticosteroid preparations.
D10AA02 - methylprednisolone ; Belongs to the class of topical corticosteroids used in the treatment of acne.