Generic
Methylprednisolone
40 brands available in the market
At a glance
Methylprednisolone is a potent corticosteroid used to treat inflammation, allergies, rheumatic disorders, skin and eye diseases, and nephrotic syndrome.
Description
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. It has at least four times the anti-inflammatory potency of Hydrocortisone.
Indications
- Rheumatic Disorders (Rheumatoid Arthritis, Ankylosing Spondylitis, Gouty Arthritis)
- Collagen Diseases (Systemic Lupus Erythematosus, Dermatomyositis)
- Dermatologic Diseases (Pemphigus, Exfoliative Dermatitis, Psoriasis)
- Allergies (Bronchial Asthma, Contact Dermatitis)
- Ophthalmic Diseases (Iritis, Keratitis, Allergic Conjunctivitis)
- Respiratory Diseases (Sarcoidosis, Aspiration Pneumonitis)
- Hematologic Disorders (Idiopathic Thrombocytopenic Purpura, Hemolytic Anemia)
- Neoplastic Diseases (Leukemias, Lymphomas)
- Edematous States (Nephrotic Syndrome)
- CNS Diseases (Multiple Sclerosis)
- Endocrine Disorders (Adrenocortical Insufficiency)
Therapeutic class
Glucocorticoids
Pharmacological class
Synthetic Corticosteroid
Pharmacology
Methylprednisolone binds to and activates intracellular glucocorticoid receptors. Activated glucocorticoid receptors bind to promoter regions of DNA and activate transcription factors that result in gene inactivation through deacetylation of histones. It inhibits leukocyte infiltration at the site of inflammation, interferes with mediators of inflammatory response, and suppresses humoral immune responses.
Mechanism of action
Reduces inflammation by suppressing migration of inflammatory cells and decreasing capillary permeability.
Dosage
Adult Dose (Oral):
- Anti-inflammatory/Immunosuppressive: Initial: 4-48 mg daily (1-4 divided doses as needed)
- Allergic Conditions: 24 mg (Day 1), 20 mg (Day 2), 16 mg (Day 3), 12 mg (Day 4), 8 mg (Day 5), 4 mg (Day 6)
- Maintenance: Lowest effective dose based on patient response
- Multiple Sclerosis: 160 mg daily for 1 week, then 64 mg every other day for 1 month
Child Dose: 0.5-1.7 mg/kg daily or 5-25 mg/m² daily (6-12 hourly intervals)
Alternate-day therapy (ADT): Twice the daily dose every other morning (to minimize side effects in long-term use)
Administration
- Take with food (to avoid upset stomach)
- Swallow tablet whole; do not chew, crush or break
- Take at the same time each day
- Follow prescribed dose and duration
- Avoid dietary sodium
Missed dose
Not applicable
Side effects
Common Side Effects:
- Skin thinning
- Increased risk of infection
- Reduction in bone density
- Weight gain
- Mood changes
- Upset stomach
- Behavioral changes
Long-term/High-dose:
- Fluid retention, weight gain, hypertension
- Potassium loss, headache
- Muscle weakness, osteoporosis
- Glaucoma, cataracts
- Peptic ulcer, growth retardation (children)
- Convulsions, psychiatric disorders (depression, euphoria, insomnia)
Precautions & warnings
- Do not stop abruptly (risk of adrenal insufficiency)
- Inform doctor if signs of infection (fever, sore throat) occur
- Do not receive live vaccines
- Monitor blood glucose if diabetic
- Caution in osteoporosis, mood disorders, hypertension, liver disease
- Enhanced effect in hypothyroidism and cirrhosis
Contraindications
- Systemic fungal infections
- Known hypersensitivity to components
Drug interactions
- Aminoglutethimide: Loss of adrenal suppression
- K-depleting agents (amphotericin B, diuretics): Risk of hypokalemia
- Macrolide antibiotics: Decreased clearance
- Isoniazid: Decreased serum levels
- Cholestyramine: Increased clearance
- Cyclosporine: Risk of convulsions
- Digitalis glycosides: Risk of arrhythmias
- CYP3A4 Inhibitors/Inducers: Plasma concentration changes
- Aspirin/NSAIDs: Risk of GI effects
- Warfarin: Increased anticoagulant effect
- Antidiabetics: Reduced therapeutic effect
- Live vaccines: Diminished response (potentially fatal)
Food interactions
Avoid dietary sodium. Alcohol is unsafe.
Use in pregnancy
Use in Pregnancy (Category C): Possibly unsafe. Limited human studies; animal studies show harmful effects on developing baby. Your doctor will weigh benefits and risks.
Pregnancy Category: C — always consult a doctor before taking during pregnancy.
Use in lactation
Use in Lactation: Safe. Human studies suggest the drug does not pass into breastmilk in significant amounts and is not harmful to the baby.
Pediatric use
Pediatric dose: 0.5-1.7 mg/kg daily (6-12 hourly intervals). Monitor growth in long-term use.
Geriatric use
No dose adjustment required for elderly, but caution advised.
Renal / hepatic impairment
Renal Impairment: Safe - no dose adjustment required.
Hepatic Impairment: Limited information available. Consult your doctor.
Overdose effects
Reports of acute toxicity/death are rare. No specific antidote; supportive and symptomatic treatment. Monitor serum electrolytes.
Storage conditions
Store in a cool and dry place, away from light. Keep out of reach of children.
Chemical structure
Methylprednisolone