Methylprednisolone

Methylprednisolone
	Methylprednisolone.svg
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[edit]

Methylprednisolone is prescribed for a variety of conditions, including:

Inflammatory and Autoimmune Disorders

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[edit]

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[edit]

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[edit]

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[edit]

Methylprednisolone should not be used in:

Systemic fungal infections
Uncontrolled infections
Hypersensitivity to corticosteroids
Live vaccine administration

Drug Interactions[edit]

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[edit]

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

Availability[edit]

Methylprednisolone is available under multiple brand names:

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