Methylprednisolone
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Methylprednisolone
Medrol (oral), Solu-Medrol (IV/IM), Depo-Medrol (depot injection)
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Summary
Common uses
Autoimmune disease flare0, Asthma/COPD exacerbation (IV in severe disease)0, Multiple sclerosis relapse (high-dose IV pulse)0, Transplant rejection0, Intra-articular for arthritis (Depo-Medrol)0
Pharmacy
Starting dose
PO Medrol Dosepak (5-day taper from 24 mg to 4 mg) is the prototypic short-course outpatient regimen; IV pulse 1 g daily for 3-5 days for MS relapse; intra-articular 4-80 mg per joint q1-5 weeks
Preparations
2, 4, 8, 16, 32 mg oral tablets; 40, 125, 500, 1000 mg IV vials; Depo-Medrol 20, 40, 80 mg/mL IM depot
US FDA Max
Indication-specific
Pharmacology
Routes
Oral, IM, IV, intra-articular, intrathecal (rare and controversial)
Onset
IV pulse: hours; PO: hours; intra-articular: days
Duration
Biologic 12-36 hours (intermediate-acting); Depo-Medrol depot weeks
Half-life
Plasma 2-3 hours; biologic ~18-36 hours[1]
Bioavailability
~80-99% (oral)[1]
Pregnancy
Use when benefits outweigh; small association with oral clefts in first trimester debated.[citation needed]
Legal status
Rx-only in US
Purported mechanism
Methylprednisolone is a synthetic glucocorticoid agonist intermediate in potency between prednisone/prednisolone and dexamethasone, with negligible mineralocorticoid activity (less sodium/water retention than hydrocortisone).0 Activates the glucocorticoid receptor to broadly remodel inflammatory, immune, and metabolic transcription. Unlike prednisone, it does not require hepatic activation, making it the preferred oral choice in severe hepatic dysfunction[1].
References
- ↑ 1.0 1.1 1.2 FDA Prescribing Information, Medrol (methylprednisolone), Pfizer/Pharmacia, current revision. https://www.accessdata.fda.gov/drugsatfda_docs/label/2018/011153s080lbl.pdf