What are the advantages of intravenous (IV) methylprednisolone over oral methylprednisolone?

From the Guidelines

Intravenous methylprednisolone is preferred over oral administration due to its immediate and complete bioavailability, allowing for rapid achievement of high serum concentrations, which is crucial in acute inflammatory conditions such as lupus nephritis, as recommended by the 2019 update of the joint European League Against Rheumatism and European Renal Association-European Dialysis and Transplant Association (EULAR/ERA-EDTA) recommendations for the management of lupus nephritis 1. The use of intravenous pulses of methylprednisolone, with a total dose of 500-2500 mg, depending on disease severity, is recommended to reduce cumulative glucocorticoid dose, followed by oral prednisone for up to 4 weeks, tapered to ≤7.5 mg/day by 3 to 6 months 1. This approach is supported by the fact that intravenous methylprednisolone provides higher drug concentrations reaching the target tissues, bypassing the first-pass metabolism in the liver that occurs with oral administration. Some key points to consider when using intravenous methylprednisolone include:

• The typical IV dosing for acute conditions ranges from 125-1000 mg daily, often given over several days depending on the condition being treated.
• IV administration ensures complete delivery of the medication in patients who may have impaired gastrointestinal absorption or who cannot take oral medications due to vomiting, unconsciousness, or being NPO (nothing by mouth) for procedures.
• Additionally, IV methylprednisolone sodium succinate is water-soluble and rapidly converts to the active form in the body, providing faster anti-inflammatory and immunosuppressive effects than oral preparations, as noted in a recent commentary on the 2021 KDIGO clinical practice guideline for the management of glomerular diseases 1. However, once the acute phase of illness has passed, transitioning to oral corticosteroids is appropriate for longer-term treatment.

From the FDA Drug Label

Following the initial emergency period, consideration should be given to employing a longer acting injectable preparation or an oral preparation The FDA drug label does not answer the question.

From the Research

Comparison of IV and Oral Methylprednisolone

• The provided studies do not directly compare the efficacy of IV methylprednisolone to oral methylprednisolone 2, 3, 4, 5, 6.
• However, the studies discuss the use of high-dose methylprednisolone sodium succinate (MPSS) in the treatment of acute spinal cord injury, which is typically administered intravenously 2, 3, 4, 5, 6.
• The studies suggest that high-dose MPSS may be effective in improving motor function and reducing complications when administered within 8 hours of injury 2, 3.
• The use of oral methylprednisolone is not mentioned in the provided studies, suggesting that IV administration may be the preferred route for acute spinal cord injury treatment 2, 3, 4, 5, 6.

Pharmacokinetics and Bioavailability

• The bioavailability of oral methylprednisolone is generally lower than that of IV administration, which may affect its efficacy in treating acute spinal cord injury 2, 3.
• IV administration of methylprednisolone allows for faster and more reliable delivery of the medication to the site of injury, which may be critical in the treatment of acute spinal cord injury 2, 3.

Clinical Guidelines and Recommendations

• The provided studies suggest that clinical guidelines and recommendations for the use of methylprednisolone in acute spinal cord injury are based on IV administration 3, 4, 5, 6.
• The studies recommend against routine administration of methylprednisolone in acute traumatic spinal cord injuries, citing lack of evidence for its efficacy and potential for increased complications 3, 6.