Methylprednisolone is a synthetic corticosteroid with anti-inflammatory and immunomodulating properties. Methylprednisolone binds to and activates specific nuclear receptors, resulting in altered gene expression and inhibition of proinflammatory cytokine production. This agent also decreases the number of circulating lymphocytes, induces cell differentiation, and stimulates apoptosis in sensitive tumor cell populations.
Methylprednisolone and its derivatives, methylprednisolone sodium succinate and methylprednisolone acetate, are synthetic glucocorticoids used as anti-inflammatory or immunosuppressive agents. They are synthetic (man-made) corticosteroids. Corticosteroids are naturally-occurring chemicals produced by the adrenal glands located adjacent to the kidneys.
Mechanism of Action of Methylprednisolone
Unbound glucocorticoids cross cell membranes and bind with high affinity to specific cytoplasmic receptors, modifying transcription and protein synthesis. By this mechanism, glucocorticoids can inhibit leukocyte infiltration at the site of inflammation, interfere with mediators of inflammatory response, and suppress humoral immune responses. The antiinflammatory actions of corticosteroids are thought to involve phospholipase A2 inhibitory proteins, lipocortins, which control the biosynthesis of potent mediators of inflammation such as prostaglandins and leukotrienes.
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Glucocorticoids are capable of suppressing the inflammatory process through numerous pathways. They interact with specific intracellular receptor proteins in target tissues to alter the expression of corticosteroid-responsive genes. Glucocorticoid-specific receptors in the cell cytoplasm bind with steroid ligands to form hormone-receptor complexes that eventually translocate to the cell nucleus. There these complexes bind to specific DNA sequences and alter their expression. The complexes may induce the transcription of mRNA leading to synthesis of new proteins. Such proteins include lipocortin, a protein known to inhibit PLA2a and thereby block the synthesis of prostaglandins, leukotrienes, and PAF. Glucocorticoids also inhibit the production of other mediators including AA metabolites such as COX, cytokines, the interleukins, adhesion molecules, and enzymes such as collagenase.
Indications of Methylprednisolone
- Adjunctive therapy for short-term administration in rheumatoid arthritis.
- Inflammatory Conditions
- Adrenogenital Syndrome
- Allergic Rhinitis
- Osteoarthritis
- Asthma
- Atopic Dermatitis
- Dermatologic Lesion
- Gout
- Immunosuppression
- Neuralgia
- Plaque Psoriasis
- Psoriasis
- Transverse Myelitis
- Acne Rosacea
- Acute Gouty Arthritis
- Adrenal cortical hypofunctions
- Adrenocortical Hyperfunction
- Ankylosing Spondylitis
- Anterior Segment Inflammation
- Aspiration Pneumonitis
- Asthma Bronchial
- Atopic Dermatitis (AD)
- Bullous dermatitis herpetiformis
- Congenital Adrenal Hyperplasia (CAH)
- Congenital Hypoplastic Anemia
- Conjunctivitis, Seasonal Allergic
- Corneal Inflammation
- Cushing’s Syndrome
- Dermatitis, Contact
- Drug hypersensitivity reaction
- Epicondylitis
- Erythroblastopenia
- Hypercalcemia
- Idiopathic Thrombocytopenic Purpura (ITP)
- Inflammatory Reaction
- Iridocyclitis
- Leukaemia,
- Loeffler’s syndrome
- Malignant Lymphomas
- Mycosis Fungoides (MF)
- Ophthalmia, Sympathetic
- Perennial Allergic Rhinitis
- Post-traumatic Osteoarthritis
- Sarcoidosis
- Seasonal Allergic Rhinitis
- Secondary thrombocytopenia
- Serum Sickness
- Severe Seborrheic Dermatitis
- Stevens-Johnson Syndrome
- Synovitis
- Systemic Lupus Erythematosus (SLE)
- Trichinosis
- Tuberculosis
- Tuberculosis Meningitis
- Ulcerative Colitis (UC)
- Uveitis
- Acquired immune hemolytic anemia
- Acute nonspecific tenosynovitis
- Acute rheumatic carditis
- Diffuse posterior uveitis
- Exfoliative erythroderma
- Non-suppurative Thyroiditis
- Severe Psoriasis
- Varicella-zoster virus acute retinal necrosis
Therapeutic Indications
- Methylprednisolone and its derivatives are used principally as anti-inflammatory or immunosuppressant agents. Because methylprednisolone has only minimal mineralocorticoid properties, the drug is inadequate alone for the management of adrenocortical insufficiency. If methylprednisolone is used in the treatment of this condition, concomitant therapy with a mineralocorticoid is also required.
- In adults and adolescents older than 13 years of age with acquired immunodeficiency syndrome (AIDS) who require parenteral glucocorticoid therapy as an adjunct to anti-infective treatment of moderate to severe Pneumocystis carinii pneumonia, an iv methylprednisolone regimen currently is recommended. Such adjunctive glucocorticoid therapy preferably should be initiated within 24-72 hr of initial antipneumocystis therapy. However, it should be recognized that this recommendation is based on limited data and may not represent the optimum dosage and schedule. Therefore, clinicians should consult published protocols and the most current clinical guidelines. Shorter courses of glucocorticoid therapy would be desirable, but rebound deterioration in pulmonary function has occurred in some patients following discontinuance of glucocorticoid therapy, and some clinicians discourage the use of shorter treatment courses. In life-threatening shock, massive iv doses of methylprednisolone as the sodium succinate have been recommended. High dose therapy should be continued only until the patient’s condition has stabilized and usually should not be continued beyond 48-72 hr.
- When used to treat motor and/or sensory deficits and potentially minimize disability in patients with acute spinal cord injury, an initial dose given by rapid iv injection over 15 minutes, followed in 45 min by iv infusion … for 23 hr (total dose administered over 24 hr), has been recommended. Other glucocorticoids and other methylprednisolone dosage regimens have not been shown to be effective in humans to date, and glucocorticoid therapy should be initiated as early as possible after spinal cord injury since appreciable benefit has been observed only when methylprednisolone therapy was initiated within 8 hr of injury.
- In the successful management of severe lupus nephritis, methylprednisolone as the sodium succinate has been administered by so-called “pulse” therapy “Pulse” therapy with methylprednisolone sodium succinate has been followed by long-term oral prednisone or prednisolone therapy. Methylprednisolone sodium succinate
- Fifty-six cases of De Quervain’s tenosynovitis (in 55 patients) were treated with a long-acting corticosteroid, methylprednisolone acetate, and followed prospectively over a 4 yr period. Approximately 90% of these patients were effectively managed either with a single injection (58%) or with multiple injections (33%) of this compound. Seventeen patients experienced recurrence a mean of 11.9 months after the initial injection
- Methylprednisolone is in the treatment of trichinosis with neurological or myocardial involvement
- Methylprednisolone is indicated concurrently with other immunosuppressants such as azathioprine or cyclosporine to reduce the risk of rejection of transplanted organs.
- Indicated as adjunctive therapy during an acute episode or exacerbation /of rheumatic disorders. Local injections are preferred when only a few joints or areas are involved, ankylosing spondylitis, acute gouty arthritis, psoriatic arthritis, rheumatoid arthritis (including juvenile arthritis), post-traumatic osteoarthritis, polymyalgia rheumatica, synovitis of osteoarthritis,
- Indicated for treatment of oral lesions unresponsive to topical therapy. The presence of an oral herpetic lesion must be ruled out prior to initiation of.
- Indicated in the treatment of severe acute or chronic allergic and inflammatory ophthalmic conditions: chorioretinitis, diffuse posterior choroiditis, allergic conjunctivitis (not controlled topically), herpes zoster ophthalmicus, anterior segment inflammation, iridocyclitis, iritis, keratitis (not associated with herpes simplex or fungal infection), optic neuritis, sympathetic ophthalmia, corneal marginal allergic ulcers, and diffuse posterior uveitis.
- Methylprednisolone is indicated for the treatment of severe cases of myasthenia gravis not controlled by antimyasthenic agents alone. Glucocorticoid therapy may be more effective following thymectomy and in patients having disease onset after 40 years of age. Long-term therapy may be required.
- Methylprednisolone is indicated to induce diuresis or remission of proteinuria in idiopathic nephrotic syndrome (without uremia) and to improve renal function in patients with lupus erythematosus. In idiopathic nephrotic syndrome, long-term therapy may be required to prevent frequent relapses.
- Indicated during an acute episode or exacerbation (of nonrheumatic inflammatory disorders). Local injections are preferred when only a few joints or areas are involved: acute or subacute bursitis, epicondylitis, and acute nonspecific tenosynovitis.
- Indicated for the treatment of hematologic disorders: acquired hemolytic anemia (autoimmune), congenital hypoplastic anemia (erythroid), red blood cell anemia (erythroblastopenia), secondary thrombocytopenia in adults, and idiopathic thrombocytopenic purpura in adults and hemolysis
- Indicated for the treatment of gastrointestinal disorders: ulcerative colitis, Crohn’s disease (Regional enteritis) when systemic therapy is required during a critical period of the disease. Long-term use is not recommended.
- Indicated for the treatment of dermatologic disorder: alopecia areata, atopic dermatitis, contact dermatitis, exfoliative dermatitis, bullous dermatitis herpetiformis, severe seborrheic dermatitis, severe erythema multiforme (Stevens-Johnson syndrome), granuloma annulare, keloids, lichen planus, lichen simplex chronicus, discoid lupus erythematosus, mycosis fungoides, necrobiosis lipoidica diabeticorum, pemphigus, severe psoriasis, psoriasis plaques, (severe eczema, localized cutaneous sarcoid, and pemphigoid.
- Methylprednisolone is indicated in the treatment of spinal cord injury. A large study concluded that patients receiving high-dose methylprednisolone therapy within 8 hours of acute spinal cord injury recover more motor and sensory function, as compared with those receiving naloxone or placebo. However, methylprednisolone did not improve patient prognosis when it was administered more than 8 hours after the spinal cord injury.
- Indicated during an acute exacerbation or as maintenance therapy (for collagen disorders): giant cell arteritis; acute rheumatic carditis; systemic (polymyositis) dermatomyositis; systemic lupus erythematosus, (relapsing polychondritis, mixed connective tissue disease, polyarteritis nodosa, relapsing polychondritis and vasulitis
- Methylprednisolone is indicated in the treatment of shock caused by adrenocortical insufficiency (addisonian shock).
- Methylprednisolone is indicated to relieve fever and inflammation from pericarditis.Indicated for the treatment of/ endocrine disorders: acute adrenocortical insufficiency and chronic primary adrenocortical insufficiency (Addison’s disease), secondary adrenocortical insufficiency, congenital adrenal hyperplasia, Cushing’s syndrome (diagnosis), hypercalcemia associated with neoplasms, and nonsuppurative thyroiditis.
- Indicated for the treatment of severe or incapacitating allergic disorders intractable to adequate trials of conventional treatment: drug induced allergic reactions, anahylactic or anaphylactoid reactions (treatment adjunct); acute noninfectious laryngeal edema (treatment adjunct); severe perennial or seasonal allergic rhinitis; serum sickness .
Contra Indications of Methylprednisolone
- Extreme Loss of Body Water
- Condition resulting from a defective immune system
- Decreased Function of Bone Marrow
- Low blood counts due to bone marrow failure
- Defective Growth of Bone Marrow
- Severe anemia
- Severely Decreased Platelets
- Decreased white blood cells
- Alcoholism
- Escape of Fluid into the Lungs
- Interstitial Pneumonitis
- Lung Fibrosis
- Canker Sore
- Ulcer from Stomach Acid
- Ulcerated Colon
- Hardening of the Liver caused by Alcohol
- Hardening of the Liver
- Excess Liver Fibrous Tissue
- Severe liver disease
- Kidney disease with reduction in kidney function
- Diarrhea
- Ascites
- Abnormal liver function tests
- Pregnancy
- A mother who is producing milk and breastfeeding
- Extreme Loss of Body Water
- Condition resulting from a defective immune system
- Decreased Function of Bone Marrow
- Low blood counts due to bone marrow failure
- Defective Growth of Bone Marrow
- Severe anemia
- Severely Decreased Platelets
- Decreased white blood cells
- Alcoholism
- Escape of Fluid into the Lungs
- Interstitial Pneumonitis
- Lung Fibrosis
- Canker Sore
- Ulcer from Stomach Acid
- Ulcerated Colon
- Hardening of the Liver caused by Alcohol
- Hardening of the Liver
- Excess Liver Fibrous Tissue
- Severe liver disease
- Kidney disease with reduction in kidney function
- Diarrhea
- Ascites
- Abnormal liver function tests
- Pregnancy
- A mother who is producing milk and breastfeeding
Dosage of Methylprednisolone
Allergic Rhinitis
Strengths: 80 to 120 mg IM
Alopecia
Alternatively, Methylprednisolone Dosepak
- Day 1: 24 mg orally (8 mg before breakfast; 4 mg after lunch; 4 mg after dinner; 8 mg at bedtime)
- Day 2: 20 mg orally (4 mg before breakfast; 4 mg after lunch; 4 mg after dinner; 8 mg at bedtime)
- Day 3: 16 mg orally (4 mg before breakfast; 4 mg after lunch; 4 mg after dinner; 4 mg at bedtime)
- Day 4: 12 mg orally (4 mg before breakfast; 4 mg after lunch; 4 mg at bedtime)
- Day 5: 8 mg orally (4 mg before breakfast; 4 mg at bedtime)
- Day 6: 4 mg orally (4 mg before breakfast)
Acetate suspension
- Initial dose: 40 to 120 mg IM once a week for 1 to 4 weeks
- For relief of acute severe dermatitis due to poison ivy: 80 to 120 mg IM; relief may occur within 8 to 12 hours
- For relief of chronic contact dermatitis: 80 to 120 mg IM every 5 to 10 days
- For relief of seborrheic dermatitis: 80 mg IM weekly to control condition
- Initial dose: 20 to 60 mg injected into lesion; for larger lesions, 1 to 4 injections of 20 to 40 mg should be used to
Dermatologic Lesion
- Initial dose: 4 to 48 mg orally once a day or in divided doses
Alternatively, Methylprednisolon
- Day 1: 24 mg orally (8 mg before breakfast; 4 mg after lunch; 4 mg after dinner; 8 mg at bedtime)
- Day 2: 20 mg orally (4 mg before breakfast; 4 mg after lunch; 4 mg after dinner; 8 mg at bedtime)
- Day 3: 16 mg orally (4 mg before breakfast; 4 mg after lunch; 4 mg after dinner; 4 mg at bedtime)
- Day 4: 12 mg orally (4 mg before breakfast; 4 mg after lunch; 4 mg at bedtime)
- Day 5: 8 mg orally (4 mg before breakfast; 4 mg at bedtime)
- Day 6: 4 mg orally (4 mg before breakfast)
Acetate suspension
- Initial dose: 40 to 120 mg IM once a week for 1 to 4 weeks
- For relief of acute severe dermatitis due to poison ivy: 80 to 120 mg IM; relief may occur within 8 to 12 hours
- For relief of chronic contact dermatitis: 80 to 120 mg IM every 5 to 10 days
- For relief of seborrheic dermatitis: 80 mg IM weekly to control condition
Psoriasis
- Initial dose: 4 to 48 mg orally once a day or in divided doses
Alternatively, Methylprednisolone
- weight gain,
- Day 1: 24 mg orally (8 mg before breakfast; 4 mg after lunch; 4 mg after dinner; 8 mg at bedtime)
- Day 2: 20 mg orally (4 mg before breakfast; 4 mg after lunch; 4 mg after dinner; 8 mg at bedtime)
- Day 3: 16 mg orally (4 mg before breakfast; 4 mg after lunch; 4 mg after dinner; 4 mg at bedtime)
- Day 4: 12 mg orally (4 mg before breakfast; 4 mg after lunch; 4 mg at bedtime)
- Day 5: 8 mg orally (4 mg before breakfast; 4 mg at bedtime)
- Day 6: 4 mg orally (4 mg before breakfast)
Acetate suspension
- Initial dose: 40 to 120 mg IM once a week for 1 to 4 weeks
Dermatological Disorders
- Initial dose: 4 to 48 mg orally once a day or in divided doses.
Alternatively, Methylprednisolone
- Day 1: 24 mg orally (8 mg before breakfast; 4 mg after lunch; 4 mg after dinner; 8 mg at bedtime)
- Day 2: 20 mg orally (4 mg before breakfast; 4 mg after lunch; 4 mg after dinner; 8 mg at bedtime)
- Day 3: 16 mg orally (4 mg before breakfast; 4 mg after lunch; 4 mg after dinner; 4 mg at bedtime)
- Day 4: 12 mg orally (4 mg before breakfast; 4 mg after lunch; 4 mg at bedtime)
- Day 5: 8 mg orally (4 mg before breakfast; 4 mg at bedtime)
- Day 6: 4 mg orally (4 mg before breakfast)
Acetate suspension
- Initial dose: 40 to 120 mg IM once a week for 1 to 4 week
- For relief of acute severe dermatitis due to poison ivy: 80 to 120 mg IM; relief may occur within 8 to 12 hours
- For relief of chronic contact dermatitis: 80 to 120 mg IM every 5 to 10 days
- For relief of seborrheic dermatitis: 80 mg IM weekly to control condition
- Initial dose: 20 to 60 mg injected into lesion; for larger lesions, 1 to 4 injections of 20 to 40 mg should be used to distribute dose.
Keloids
- Initial dose: 4 to 48 mg orally once a day or in divided doses
Alternatively, Methylprednisolone
- Day 1: 24 mg orally (8 mg before breakfast; 4 mg after lunch; 4 mg after dinner; 8 mg at bedtime)
- Day 2: 20 mg orally (4 mg before breakfast; 4 mg after lunch; 4 mg after dinner; 8 mg at bedtime)
- Day 3: 16 mg orally (4 mg before breakfast; 4 mg after lunch; 4 mg after dinner; 4 mg at bedtime)
- Day 4: 12 mg orally (4 mg before breakfast; 4 mg after lunch; 4 mg at bedtime)
- Day 5: 8 mg orally (4 mg before breakfast; 4 mg at bedtime)
- Day 6: 4 mg orally (4 mg before breakfast)
Acetate suspension
- Initial dose: 40 to 120 mg IM once a week for 1 to 4 weeks
- For relief of acute severe dermatitis due to poison ivy: 80 to 120 mg IM; relief may occur within 8 to 12 hours
- Initial dose: 20 to 60 mg injected into lesion; for larger lesions, 1 to 4 injections of 20 to 40 mg should be used to distribute dose.
Rheumatoid Arthritis
- Initial dose: 4 to 48 mg orally once a day or in divided doses
INTRA-ARTICULAR INJECTION Acetate suspension
- General guidance: Actual doses may vary with severity of condition
- Large joints (knee, angles, shoulders): 20 to 80 mg via intra-articular injection
- Medium joints (elbows, wrists): 10 to 40 mg via intra-articular injection
Acetate suspension
- Initial dose: 40 mg IM every 2 weeks
Acute Gout
- Initial dose: 4 to 48 mg orally once a day or in divided doses
Alternatively, methylprednisolone
- Day 1: 24 mg orally (8 mg before breakfast; 4 mg after lunch; 4 mg after dinner; 8 mg at bedtime)
- Day 2: 20 mg orally (4 mg before breakfast; 4 mg after lunch; 4 mg after dinner; 8 mg at bedtime)
- Day 3: 16 mg orally (4 mg before breakfast; 4 mg after lunch; 4 mg after dinner; 4 mg at bedtime)
- Day 4: 12 mg orally (4 mg before breakfast; 4 mg after lunch; 4 mg at bedtime)
- Day 5: 8 mg orally (4 mg before breakfast; 4 mg at bedtime)
- Day 6: 4 mg orally (4 mg before breakfast)
Parenteral
- Sodium succinate (IV or IM); in emergency situations, IV is preferres
- High dose therapy: 30 mg/kg IV over at least 30 minutes every 4 to 6 hours until condition has stabilized, generally no more than 48 to 72 hours; after initial emergency period, a longer-acting injectable or oral preparation should be considered
- Alternatively, when oral therapy is not feasible, IM or IV administration may be substituted.
- Acetate suspension (IM only): For prolonged systemic effect:
- Initial dose: 4 to 120 mg IM; may repeat dose depending upon the degree of relief obtained from original injection.
INTRA-ARTICULAR Administration
- General guidance: Actual doses may vary with severity of condition
- Large joints (knee, angles, shoulders): 20 to 80 mg via intra-articular injection
- Medium joints (elbows, wrists): 10 to 40 mg via intra-articular injection
- Small joints (metacarpophalangeal, interphalangeal, sternoclavicular, acromioclavicular): 4 to 10 mg via intra-articular injection
- For conditions of the tendinous or bursal structures: 4 to 30 mg
- Initial dose: 4 to 48 mg orally once a day or in divided doses
Alternatively, methylprednisolone
- Day 1: 24 mg orally (8 mg before breakfast; 4 mg after lunch; 4 mg after dinner; 8 mg at bedtime)
- Day 2: 20 mg orally (4 mg before breakfast; 4 mg after lunch; 4 mg after dinner; 8 mg at bedtime)
- Day 3: 16 mg orally (4 mg before breakfast; 4 mg after lunch; 4 mg after dinner; 4 mg at bedtime)
- Day 4: 12 mg orally (4 mg before breakfast; 4 mg after lunch; 4 mg at bedtime)
- Day 5: 8 mg orally (4 mg before breakfast; 4 mg at bedtime)
- Day 6: 4 mg orally (4 mg before breakfast)
Parenteral
- Sodium succinate (IV or IM); in emergency situations, IV is preferred
- High dose therapy: 30 mg/kg IV over at least 30 minutes every 4 to 6 hours until condition has stabilized, generally no more than 48 to 72 hours; after initial emergency period, a longer-acting injectable or oral preparation should be considered.
- Alternatively, when oral therapy is not feasible, IM or IV administration may be substituted.
Acetate suspension (IM only): For prolonged systemic effect
- Initial dose: 4 to 120 mg IM; may repeat dose depending upon the degree of relief obtained from original injection.
INTRA-ARTICULAR Administration
- General guidance: Actual doses may vary with severity of condition
- Large joints (knee, angles, shoulders): 20 to 80 mg via intra-articular injection
- Medium joints (elbows, wrists): 10 to 40 mg via intra-articular injection
- Small joints (metacarpophalangeal, interphalangeal, sternoclavicular, acromioclavicular): 4 to 10 mg via intra-articular injection
- Injections may be repeated every 1 to 5 or more weeks, depending upon the degree of relief obtained from the original injection.
Bursitis
- Initial dose: 4 to 48 mg orally once a day or in divided doses
Alternatively, methylprednisolone
- Day 1: 24 mg orally (8 mg before breakfast; 4 mg after lunch; 4 mg after dinner; 8 mg at bedtime)
- Day 2: 20 mg orally (4 mg before breakfast; 4 mg after lunch; 4 mg after dinner; 8 mg at bedtime)
- Day 3: 16 mg orally (4 mg before breakfast; 4 mg after lunch; 4 mg after dinner; 4 mg at bedtime)
- Day 4: 12 mg orally (4 mg before breakfast; 4 mg after lunch; 4 mg at bedtime)
- Day 5: 8 mg orally (4 mg before breakfast; 4 mg at bedtime)
- Day 6: 4 mg orally (4 mg before breakfast)
Parenteral
- Sodium succinate (IV or IM); in emergency situations, IV is preferred
- High dose therapy: 30 mg/kg IV over at least 30 minutes every 4 to 6 hours until condition has stabilized, generally no more than 48 to 72 hours; after initial emergency period, a longer-acting injectable or oral preparation should be considere
Acetate suspension (IM only): For prolonged systemic effect
- Initial dose: 4 to 120 mg IM; may repeat dose depending upon the degree of relief obtained from original injection.
INTRA-ARTICULAR Administration
- General guidance: Actual doses may vary with severity of condition
- Large joints (knee, angles, shoulders): 20 to 80 mg via intra-articular injection
- Medium joints (elbows, wrists): 10 to 40 mg via intra-articular injection
SOFT TISSUE Administration
- For conditions of the tendinous or bursal structures: 4 to 30 mg
Nephrotic Syndrome
- Initial dose: 4 to 48 mg orally once a day or in divided doses
Alternatively, methylprednisolone
- Day 1: 24 mg orally (8 mg before breakfast; 4 mg after lunch; 4 mg after dinner; 8 mg at bedtime)
- Day 2: 20 mg orally (4 mg before breakfast; 4 mg after lunch; 4 mg after dinner; 8 mg at bedtime)
- Day 3: 16 mg orally (4 mg before breakfast; 4 mg after lunch; 4 mg after dinner; 4 mg at bedtime)
- Day 4: 12 mg orally (4 mg before breakfast; 4 mg after lunch; 4 mg at bedtime)
- Day 5: 8 mg orally (4 mg before breakfast; 4 mg at bedtime)
- Day 6: 4 mg orally (4 mg before breakfast)
Parenteral
- Sodium succinate (IV or IM); in emergency situations, IV is preferred
- High dose therapy: 30 mg/kg IV over at least 30 minutes every 4 to 6 hours until condition has stabilized, generally no more than 48 to 72 hours; after initial emergency period, a longer-acting injectable or oral preparation should be considered
Acetate suspension (IM only); For prolonged systemic effect
- Initial dose: 4 to 120 mg IM; may repeat dose depending upon the degree of relief obtained from original injection.
INTRA-ARTICULAR Administration
- General guidance: Actual doses may vary with severity of condition
- Large joints (knee, angles, shoulders): 20 to 80 mg via intra-articular injection
- Medium joints (elbows, wrists): 10 to 40 mg via intra-articular injection
- Small joints (metacarpophalangeal, interphalangeal, sternoclavicular, acromioclavicular): 4 to 10 mg via intra-
- For conditions of the tendinous or bursal structures: 4 to 30 mg
Osteoarthritis
- Initial dose: 4 to 48 mg orally once a day or in divided doses
Alternatively, methylprednisolone
- Day 1: 24 mg orally (8 mg before breakfast; 4 mg after lunch; 4 mg after dinner; 8 mg at bedtime)
- Day 2: 20 mg orally (4 mg before breakfast; 4 mg after lunch; 4 mg after dinner; 8 mg at bedtime)
- Day 3: 16 mg orally (4 mg before breakfast; 4 mg after lunch; 4 mg after dinner; 4 mg at bedtime)
- Day 4: 12 mg orally (4 mg before breakfast; 4 mg after lunch; 4 mg at bedtime)
- Day 5: 8 mg orally (4 mg before breakfast; 4 mg at bedtime)
- Day 6: 4 mg orally (4 mg before breakfast)
Parenteral
- weight gain,
- Sodium succinate (IV or IM); in emergency situations, IV is preferred
- High dose therapy: 30 mg/kg IV over at least 30 minutes every 4 to 6 hours until condition has stabilized, generally no more than 48 to 72 hours; after initial emergency period, a longer-acting injectable or oral preparation should be considered
Acetate suspension (IM only): For prolonged systemic effect
- Initial dose: 4 to 120 mg IM; may repeat dose depending upon the degree of relief obtained from original injection.
INTRA-ARTICULAR Administration
- Large joints (knee, angles, shoulders): 20 to 80 mg via intra-articular injection
- Medium joints (elbows, wrists): 10 to 40 mg via intra-articular injection
- Small joints (metacarpophalangeal, interphalangeal, sternoclavicular, acromioclavicular): 4 to 10 mg via intra-articular injection
- Injections may be repeated every 1 to 5 or more weeks, depending upon the degree of relief obtained from the original injection.
SOFT TISSUE Administration
- For conditions of the tendinous or bursal structures: 4 to 30 mg
Tendonitis
- Initial dose: 4 to 48 mg orally once a day or in divided doses
Alternatively, methylprednisolone
- Day 1: 24 mg orally (8 mg before breakfast; 4 mg after lunch; 4 mg after dinner; 8 mg at bedtime)
- Day 2: 20 mg orally (4 mg before breakfast; 4 mg after lunch; 4 mg after dinner; 8 mg at bedtime)
- Day 3: 16 mg orally (4 mg before breakfast; 4 mg after lunch; 4 mg after dinner; 4 mg at bedtime)
- Day 4: 12 mg orally (4 mg before breakfast; 4 mg after lunch; 4 mg at bedtime)
- Day 5: 8 mg orally (4 mg before breakfast; 4 mg at bedtime)
- Day 6: 4 mg orally (4 mg before breakfast)
Parenteral
- Sodium succinate (IV or IM); in emergency situations, IV is preferred
- High dose therapy: 30 mg/kg IV over at least 30 minutes every 4 to 6 hours until condition has stabilized, generally no more than 48 to 72 hours; after initial emergency period, a longer-acting injectable or oral preparation should be considered
INTRA-ARTICULAR Administration
- General guidance: Actual doses may vary with severity of condition
- Large joints (knee, angles, shoulders): 20 to 80 mg via intra-articular injection
- Medium joints (elbows, wrists): 10 to 40 mg via intra-articular injection
- Small joints (metacarpophalangeal, interphalangeal, sternoclavicular, acromioclavicular): 4 to 10 mg via intra-articular injection
- Injections may be repeated every 1 to 5 or more weeks, depending upon the degree of relief obtained from the original injection.
SOFT TISSUE Administration
- For conditions of the tendinous or bursal structures: 4 to 30 mg
Neoplastic Diseases
- Initial dose: 4 to 48 mg orally once a day or in divided doses
Alternatively, methylprednisolone
- Day 1: 24 mg orally (8 mg before breakfast; 4 mg after lunch; 4 mg after dinner; 8 mg at bedtime)
- Day 2: 20 mg orally (4 mg before breakfast; 4 mg after lunch; 4 mg after dinner; 8 mg at bedtime)
- Day 3: 16 mg orally (4 mg before breakfast; 4 mg after lunch; 4 mg after dinner; 4 mg at bedtime)
- Day 4: 12 mg orally (4 mg before breakfast; 4 mg after lunch; 4 mg at bedtime)
- Day 5: 8 mg orally (4 mg before breakfast; 4 mg at bedtime)
- Day 6: 4 mg orally (4 mg before breakfast)
Parenteral
- Sodium succinate (IV or IM); in emergency situations, IV is preferred
- High dose therapy: 30 mg/kg IV over at least 30 minutes every 4 to 6 hours until condition has stabilized, generally no more than 48 to 72 hours; after initial emergency period, a longer-acting injectable or oral preparation should be considered
Acetate suspension (IM only): For prolonged systemic effect
- Initial dose: 4 to 120 mg IM; may repeat dose depending upon the degree of relief obtained from original injection.
INTRA-ARTICULAR Administration
- General guidance: Actual doses may vary with severity of condition
- Large joints (knee, angles, shoulders): 20 to 80 mg via intra-articular injection
- Medium joints (elbows, wrists): 10 to 40 mg via intra-articular injection
- Small joints (metacarpophalangeal, interphalangeal, sternoclavicular, acromioclavicular): 4 to 10 mg via intra-articular injection
SOFT TISSUE Administration
- For conditions of the tendinous or bursal structures: 4 to 30 mg
Epicondylitis
- Initial dose: 4 to 48 mg orally once a day or in divided doses
Alternatively, methylprednisolone
- Day 1: 24 mg orally (8 mg before breakfast; 4 mg after lunch; 4 mg after dinner; 8 mg at bedtime)
- Day 2: 20 mg orally (4 mg before breakfast; 4 mg after lunch; 4 mg after dinner; 8 mg at bedtime)
- Day 3: 16 mg orally (4 mg before breakfast; 4 mg after lunch; 4 mg after dinner; 4 mg at bedtime)
- Day 4: 12 mg orally (4 mg before breakfast; 4 mg after lunch; 4 mg at bedtime)
- Day 5: 8 mg orally (4 mg before breakfast; 4 mg at bedtime)
- Day 6: 4 mg orally (4 mg before breakfast)
Parenteral
- Sodium succinate (IV or IM); in emergency situations, IV is preferred
- High dose therapy: 30 mg/kg IV over at least 30 minutes every 4 to 6 hours until condition has stabilized, generally no more than 48 to 72 hours; after initial emergency period, a longer-acting injectable or oral preparation should be considered
Acetate suspension (IM only): For prolonged systemic effect
- Initial dose: 4 to 120 mg IM; may repeat dose depending upon the degree of relief obtained from original injection.
INTRA-ARTICULAR Administration
- General guidance: Actual doses may vary with severity of condition
- Large joints (knee, angles, shoulders): 20 to 80 mg via intra-articular injectio
- Injections may be repeated every 1 to 5 or more weeks, depending upon the degree of relief obtained from the original injection.
SOFT TISSUE Administration
- For conditions of the tendinous or bursal structures: 4 to 30 mg
- Initial dose: 4 to 48 mg orally once a day or in divided doses
Alternatively, methylprednisolone
- Day 1: 24 mg orally (8 mg before breakfast; 4 mg after lunch; 4 mg after dinner; 8 mg at bedtime
- Day 2: 20 mg orally (4 mg before breakfast; 4 mg after lunch; 4 mg after dinner; 8 mg at bedtime)
- Day 3: 16 mg orally (4 mg before breakfast; 4 mg after lunch; 4 mg after dinner; 4 mg at bedtime)
- Day 4: 12 mg orally (4 mg before breakfast; 4 mg after lunch; 4 mg at bedtime)
- Day 5: 8 mg orally (4 mg before breakfast; 4 mg at bedtime)
- Day 6: 4 mg orally (4 mg before breakfast)
Parenteral
- weight gain,
- Sodium succinate (IV or IM); in emergency situations, IV is preferred
- High dose therapy: 30 mg/kg IV over at least 30 minutes every 4 to 6 hours until condition has stabilized, generally no more than 48 to 72 hours; after initial emergency period, a longer-acting injectable or oral preparation should be considered
- Alternatively, when oral therapy is not feasible, IM or IV administration may be substituted.
Acetate suspension (IM only): For prolonged systemic effect
- Initial dose: 4 to 120 mg IM; may repeat dose depending upon the degree of relief obtained from original injection.
INTRA-ARTICULAR Administration
- General guidance: Actual doses may vary with severity of condition
- Large joints (knee, angles, shoulders): 20 to 80 mg via intra-articular injection
- Medium joints (elbows, wrists): 10 to 40 mg via intra-articular injection
- Small joints (metacarpophalangeal, interphalangeal, sternoclavicular, acromioclavicular): 4 to 10 mg via intra-articular injection
- Injections may be repeated every 1 to 5 or more weeks, depending upon the degree of relief obtained from the original injection.
SOFT TISSUE Administration
- For conditions of the tendinous or bursal structures: 4 to 30 mg
Asthma
- Burst therapy: 32 to 64 mg orally once a day or in 2 divided doses until symptoms resolve and PEF (peak expiratory flow) is at least 80 percent of personal best
.Parenteral
- Sodium succinate: IV administration may be used if rapid hormonal effect of maximum intensity is required.
- High dose therapy: 30 mg/kg IV over at least 30 minutes every 4 to 6 hours until condition has stabilized, generally 48 to 72 hours; following initial emergency period, a longer-acting injectable or oral preparation should be considered
- Alternatively, when oral therapy is not feasible, IM or IV administration may be substituted.
Acetate suspension: For prolonged systemic effect
- 240 mg IM once (guideline dosing); 80 to 120 mg IM (manufacturer dosing)
- Initial dose: 6 to 48 mg orally once a day or every other day
- Maintenance dose: Gradually in small decrements at appropriate intervals decrease to the lowest dose that maintains an adequate clinical response.
Multiple Sclerosis
160 mg orally once a day for 1 week; then 64 mg orally every other day for 1 month
Nephrotic Syndrome
- Initial dose: 4 to 48 mg orally once a day or in divided doses
Parenteral
- Sodium succinate: IV or IM; in emergency situations, IV is preferred
- Initial dose: 0.11 to 1.6 mg/kg/day (3.2 to 4.8 mg/m2/day) IM or IV divided in 3 or 4 doses (not less than 0.5 mg/kg/24 hours)
- As a temporary substitute for oral therapy, administer oral daily dose IV or IM divided in 3 or 4 doses
Acetate suspension: For prolonged systemic effect; IM
- Initial dose: 0.11 to 1.6 mg/kg/day IM
Inflammatory
- Initial dose: 4 to 48 mg orally once a day or in divided doses
Parenteral
- Sodium succinate: IV or IM; in emergency situations, IV is preferred
- Initial dose: 0.11 to 1.6 mg/kg/day (3.2 to 4.8 mg/m2/day) IM or IV divided in 3 or 4 doses (not less than 0.5 mg/kg/24 hours)
- As a temporary substitute for oral therapy, administer oral daily dose IV or IM divided in 3 or 4 doses
- Acetate suspension: For prolonged systemic effect; IM only
- Initial dose: 0.11 to 1.6 mg/kg/day IM.
Pediatric Neoplastic Diseases
- Initial dose: 4 to 48 mg orally once a day or in divided doses
Parenteral
- Sodium succinate: IV or IM; in emergency situations, IV is preferred
- Initial dose: 0.11 to 1.6 mg/kg/day (3.2 to 4.8 mg/m2/day) IM or IV divided in 3 or 4 doses (not less than 0.5 mg/kg/24 hours)
- As a temporary substitute for oral therapy, administer oral daily dose IV or IM divided in 3 or 4 doses
- Acetate suspension: For prolonged systemic effect; IM only
- Initial dose: 0.11 to 1.6 mg/kg/day IM
Pediatric Asthma
0 to 11 years of age
Initial dose: 0.8 to 1.6 mg/kg oral or IV (succinate) once a day or in 2 divided doses until symptoms resolve and PEF (peak expiratory flow) is at least 80 percent of personal best
- Therapy is usually required for 3 to 10 days but in some cases, may be longer
- Maximum dose: 48 mg
12 years or older
- Initial dose: 32 to 48 mg orally once a day or in 2 divided doses until symptoms resolve and PEF (peak expiratory
IM (acetate)
- 0 to 4 years of age: 7.5 mg/kg IM once (guideline dosing) OR 80 to 120 mg IM (manufacturer dosing)
- 5 years or older: 240 mg IM once (guideline dosing) OR 80 to 120 mg IM (manufacturer dosing)
Pediatric Juvenile Rheumatoid Arthritis
- Initial dose: 4 to 48 mg orally once a day or in divided doses
- Adjust or maintain initial dose until a satisfactory response is obtained; then, gradually in small decrements at appropriate intervals decrease to the lowest dose that maintains an adequate clinical response
Parenteral
- SUCCINATE: May administer IM or IV
- Initial dose: 0.11 to 1.6 mg/kg/day (3.2 to 4.8 mg/m2/day) IM or IV divided in 3 or 4 doses throughout the day
- As a temporary substitute for oral therapy, administer oral daily dose IV or IM divided in 3 or 4 doses throughout the day
ACETATE suspension: IM administration only
- Initial dose: 0.11 to 1.6 mg/kg IM once a day
Allergic Reaction
- Initial dose: 4 to 48 mg orally once a day or in divided doses
Parenteral
- When oral therapy is not feasible IV (succinate) or IM therapy (acetate or succinate) may be used.
Succinate
- Initial dose: 0.11 to 1.6 mg/kg/day IV or IM in 3 or 4 divided doses
- Alternatively, 3.2 to 4.8 mg/m2/day
- Initial dose: 0.11 to 1.6 mg/kg/day IM once a day
Pediatric Dose for Alopecia
- Initial dose: 4 to 48 mg orally once a day or in divided doses
Parenteral
- When oral therapy is not feasible IV (succinate) or IM therapy (acetate or succinate) may be used.
- Initial dose: 0.11 to 1.6 mg/kg/day IV or IM in 3 or 4 divided doses
- Alternatively, 3.2 to 4.8 mg/m2/day
- Initial dose: 4 to 48 mg orally once a day or in divided doses
Parenteral
- When oral therapy is not feasible IV (succinate) or IM therapy (acetate or succinate) may be used.
- Initial dose: 0.11 to 1.6 mg/kg/day IV or IM in 3 or 4 divided doses
- Alternatively, 3.2 to 4.8 mg/m2/day
Pediatric Psoriasis
- Initial dose: 4 to 48 mg orally once a day or in divided doses
Succinate
- Initial dose: 0.11 to 1.6 mg/kg/day IV or IM in 3 or 4 divided doses
- Alternatively, 3.2 to 4.8 mg/m2/day
- Initial dose: 0.11 to 1.6 mg/kg/day IM once a day
Dermatological Disorders
- Initial dose: 4 to 48 mg orally once a day or in divided doses
- When oral therapy is not feasible IV (succinate) or IM therapy (acetate or succinate) may be used.
Succinate
- Initial dose: 0.11 to 1.6 mg/kg/day IV or IM in 3 or 4 divided doses
- Alternatively, 3.2 to 4.8 mg/m2/day
- Initial dose: 0.11 to 1.6 mg/kg/day IM once a day
Allergic Urticaria
- Initial dose: 4 to 48 mg orally once a day or in divided doses.
Succinate
- Initial dose: 0.11 to 1.6 mg/kg/day IV or IM in 3 or 4 divided doses
- Alternatively, 3.2 to 4.8 mg/m2/day
- Initial dose: 0.11 to 1.6 mg/kg/day IM once a day
Side Effects of Methylprednisolone
The most common side effects
- Fluid retention
- Weight gain,
- Mouth sores,
- Drying of the skin
- Change in skin color
- Diarrhea
- Any signs of infection, or a skin rash.
- Stomach pain, especially if it comes along with fever and diarrhea or constipation
- Yellowing of the skin or eyes
- Loss of appetite
- Constipation
- Sleepiness or unusual drowsiness
- Clumsiness or unsteadiness
- Dizziness
- Drowsiness
- Dry mouth
- false sense of well-being
- increased watering of mouth
- lightheadedness
- constipation;
- vision changes;
- breast swelling (in men or women); or
- decreased sex drive, impotence, or difficulty having an orgasm.
- blurred vision, tunnel vision, eye pain or swelling, or seeing halos around lights;
- restless muscle movements in your eyes, tongue, jaw, or neck;
Common
- Drowsiness and lightheadedness the day after taking the medicine.
- Confusion.
- Numbed emotions.
- Visual disturbances such as blurred vision or double vision.
- Shaky movements and unsteady walk (ataxia).
- Loss of memory (amnesia).
- Muscle weakness.
- Dizziness.
- Headache.
- Skin rashes.
- Disturbances of the gut such as diarrhoea, constipation, nausea, vomiting or abdominal pain.
- Difficulty in passing urine (urinary retention).
- Changes in sex drive.
- Low blood pressure (hypotension).
- Blood disorders.
- Jaundice.
- Unexpected aggression, restlessness or irritability (tell your doctor if you experience this).
- Nightmares or hallucinations (tell your doctor if you experience this).
Rare
- agitation
- anxiety
- behavioural changes, including aggressiveness, angry outbursts, bizarre behaviour, or decreased inhibitions
- confusion
- increased trouble sleeping
- memory problems
- muscle spasms
- shortness of breath
Drug Interactions of Methylprednisolone
Methylprednisolone may interact with following drugs, supplyments, & may change the efficacy of drugs
- abatacept
- anakinra
- Amphotericin B
- Antibiotics
- Anticholinesterase agents such as donepezil, rivastigmine, and galantamine
- Anticoagulants such as warfarin
- Antidiabetic agents
- anti-tumour necrosis factor agents (e.g., adalimumab, etanercept, infliximab, )
- azathioprine
- “azole” antifungals (e.g., itraconazole, ketoconazole, voriconazole)
- beta-blockers (e.g., carvedilol, metoprolol, propranolol)
- carbamazepine
- clonidine
- clozapine
- corticosteroids (e.g.dexamethasone, hydrocortisone, prednisone)
- cyclosporine
- diltiazem
- imatinib
- Estrogens, including oral contraceptives
- macrolide antibiotics (e.g., clarithromycin, erythromycin)
- methotrexate
- methyldopa
- mycophenolate
- phenobarbital
- phenytoin
- rituximab
- tacrolimus
- verapamil
The avobe list is not the sufficient drugs interactions list, please always consult your doctor or pharmacist before taking this drug.
Pregnancy & Lactation
Pregnancy
There are no adequate or well-controlled studies of the use of methylprednisolone in pregnant women. Complications, including cleft palate, stillbirth, and premature abortion, have been reported when corticosteroids were administered during pregnancy in animals. If these drugs must be used during pregnancy, the potential risks should be discussed with the patient. Babies born to women receiving large doses of corticosteroids during pregnancy should be monitored for signs of adrenal insufficiency, and appropriate therapy should be initiated, if necessary. Corticosteroids have been shown to impair fertility in male rats.
Lactation
A patient who was 6 weeks postpartum and predominantly breastfeeding her infant received 24 mg of depot methylprednisolone plus 15 mg of lidocaine intralesionally for tenosynovitis of the wrist. Thirty hours after the injection, lactation ceased. Her breasts were soft and not engorged at that time. Thirty-six hours later, lactation resumed slowly, reaching normal milk production 24 hours later. The author hypothesized that the suppression might have occurred because the injection was in a highly mobile joint, which might have caused rapid release of the corticosteroid.[9] Large doses of triamcinolone injected into the shoulder and into the wrist have also been reported to cause temporary drop or cessation of lactation.
References
