Methylprednisolone

Corticosteroid medication

Methylprednisolone
INN
Drug class
Routes of administration	By mouth, intramuscular, intra-articular, intravenous
Pregnancy category
Bioavailability
Metabolism	Liver (CYP3A4)
Elimination half-life	1.8–2.6 hours
Excretion	Urine
Legal status
CAS Number	83-43-2
PubChem	6741
DrugBank	DB00959
ChemSpider
KEGG

Methylprednisolone is a synthetic glucocorticoid primarily used for its anti-inflammatory and immunosuppressive properties.

Methylprednisolone is on the World Health Organization’s List of Essential Medicines.

Medical Uses

Methylprednisolone is prescribed for a variety of conditions, including:

Inflammatory and Autoimmune Disorders

• Rheumatoid arthritis
• Systemic lupus erythematosus (SLE)
• Psoriatic arthritis
• Multiple sclerosis (MS)
• Ulcerative colitis
• Crohn’s disease

Allergic and Respiratory Conditions

• Severe allergies – including angioedema and anaphylaxis.
• Asthma and COPD exacerbations – Used as an oral or IV corticosteroid in severe cases.

Endocrine and Oncological Uses

• Adrenal insufficiency – As an alternative to hydrocortisone when mineralocorticoid activity is not required.
• Cancer therapy – Used in the management of leukemia, lymphoma, and multiple myeloma.

Neurological Disorders

• Multiple sclerosis (MS) relapses – Administered as high-dose IV methylprednisolone.
• Spinal cord injury (off-label) – Used to reduce inflammation in acute cases.

Ophthalmic Conditions

• Optic neuritis (often linked to MS)
• Uveitis, iritis, and scleritis

Administration and Dosage

Methylprednisolone is available in oral tablets, intramuscular, intra-articular, and intravenous formulations. Dosage depends on the condition being treated:

• Mild to moderate inflammation – 4–16 mg/day (oral)
• Severe inflammation or autoimmune flares – IV pulse therapy (e.g., 500–1000 mg IV)
• Acute asthma exacerbation – 40–80 mg/day PO or IV

Side Effects

Common Side Effects

• Weight gain
• Mood changes (insomnia, agitation)
• Increased blood sugar levels (hyperglycemia)
• Fluid retention

Serious Adverse Effects Long-term or high-dose use may lead to:

• Osteoporosis and fractures
• Adrenal suppression (requiring tapering)
• Glaucoma and cataracts
• Cushing’s syndrome (moon face, buffalo hump)
• Infections due to immune suppression

Pharmacology

Mechanism of Action Methylprednisolone is a glucocorticoid receptor agonist that: 1. Suppresses inflammation by inhibiting pro-inflammatory cytokines (IL-1, IL-6, TNF-alpha). 2. Suppresses the immune response by reducing T-cell activation. 3. Regulates metabolism by increasing glucose levels and altering fat distribution.

Metabolism and Elimination

• Metabolized in the liver (CYP3A4 pathway).
• Eliminated via the kidneys.
• Half-life: 1.8–2.6 hours.

Contraindications

Methylprednisolone should not be used in:

• Systemic fungal infections
• Uncontrolled infections
• Hypersensitivity to corticosteroids
• Live vaccine administration

Drug Interactions

• NSAIDs – Increased risk of gastric ulcers.
• Diabetes medications – May require higher insulin doses.
• Live vaccines – Risk of severe infection.
• Anticoagulants – May alter warfarin levels.

History

Methylprednisolone was first synthesized by The Upjohn Company (now Pfizer) and FDA-approved in 1957.

Availability

Methylprednisolone is available under multiple brand names:

• Medrol (oral tablets)
• Depo-Medrol (intramuscular injection)
• Solu-Medrol (intravenous formulation)

See Also

• Glucocorticoid
• Prednisolone
• Cushing's syndrome
• Adrenal insufficiency

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