Pharmacology · Corticosteroids (glucocorticoids)
Methylprednisolone !
An intermediate-acting corticosteroid given by mouth or as high-dose IV «pulses» for severe flares such as multiple sclerosis relapses.
Updated 2026-11-01
The figure shows cortisol (hydrocortisone) in the ligand-binding pocket of the human glucocorticoid receptor; methylprednisolone binds the same pocket.
Mechanism of action
Methylprednisolone is a methylated prednisolone that binds the glucocorticoid receptor. The complex enters the nucleus, switches on anti-inflammatory genes and represses NF-κB and AP-1. At very high IV doses it rapidly suppresses inflammation and immune activity, which is why it is used in pulses for severe autoimmune flares.
- Methylprednisolone binds the glucocorticoid receptor
- The drug-receptor complex moves into the nucleus
- It switches on anti-inflammatory genes and represses NF-κB and AP-1
- Fewer cytokines, prostaglandins and immune cells reach the tissue
Pharmacokinetics
- Absorption
- Oral tablets; the sodium succinate salt is given IV or IM; the acetate is a depot suspension
- Metabolism
- In the liver, partly by CYP3A4
- Half-life
- Intermediate-acting glucocorticoid
Indications
- Acute exacerbations of multiple sclerosis (IV pulses) Multiple sclerosis →
- Severe lupus and other systemic autoimmune flares Systemic lupus erythematosus →
- Severe asthma Asthma →
- Giant cell arteritis and other vasculitides Giant cell arteritis →
- Acute transplant rejection, with other immunosuppressants
Adverse effects
Common
- Hyperglycaemia, sometimes marked after pulses
- Insomnia, agitation and mood changes
- Fluid retention and higher blood pressure
Contraindications
- Systemic fungal infections
- Hypersensitivity to the product
- Live or live attenuated vaccines during immunosuppressive doses
- Intrathecal use
Key interactions
- CYP3A4 inducers (rifampicin, phenytoin, carbamazepine, barbiturates)
- Faster clearance and a weaker corticosteroid effect
- Strong CYP3A4 inhibitors (ketoconazole)
- Higher corticosteroid levels and more side effects
- Aspirin and other NSAIDs
- Higher risk of gastrointestinal ulcer and bleeding
- Potassium-depleting drugs (loop or thiazide diuretics, amphotericin B)
- Hypokalaemia; with digoxin, more risk of arrhythmia
- Ciclosporin
- Mutual inhibition of metabolism; seizures have been reported
What is monitored
- Blood glucose
- Blood pressure and weight
- Potassium
- Signs of infection
- Eye pressure and bone density with long use
- Heart rhythm during high-dose IV infusion
Administration and safety
- High IV doses are infused slowly over the time the protocol sets, never as a rapid push
- Sodium succinate (IV/IM) and acetate (depot suspension, not IV) are different products
- Formulations with benzyl alcohol are not used in neonates
- Epidural injection of corticosteroids has caused serious neurological events
Nursing care
- During pulses, check blood pressure, heart rate and glucose
- Watch for infection: fever and other signs may be blunted
- Watch mood and sleep; report agitation, depression or confusion
- Teach that a long course is not stopped suddenly; it is tapered under medical supervision
- Check the product label to confirm the salt and route before giving it
Pregnancy and breastfeeding
Used in pregnancy when the benefit justifies it; newborns of mothers on substantial doses are watched for adrenal insufficiency.
Test yourself
Think of the answer, then tap the question to see it.
Why must high-dose IV methylprednisolone be infused slowly?
Rapid injection of large doses has been linked to arrhythmias, circulatory collapse and cardiac arrest.
What do IV methylprednisolone pulses do in a multiple sclerosis relapse?
They suppress the inflammation of the relapse quickly, which speeds recovery from that episode.
Which methylprednisolone salt is never given IV?
The acetate, a depot suspension for IM or intra-articular use. The sodium succinate is the IV form.
Related drugs
Related conditions
← Back to the class: Corticosteroids (glucocorticoids)
Educational content on how drugs work; not a prescribing guide and no substitute for a health professional's advice. No doses are given.
Sources: Methylprednisolone: MedlinePlus Drug Information (MedlinePlus (U.S. National Library of Medicine), 2017); DailyMed - METHYLPREDNISOLONE SODIUM SUCCINATE injection, powder, for solution (DailyMed (U.S. National Library of Medicine), 2026); ATCDDD - ATC/DDD Index (WHO Collaborating Centre for Drug Statistics Methodology, 2026); eEML - Electronic Essential Medicines List (World Health Organization, 2025).
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Representative model, for educational purposes only.