What is the difference between prednisolone and prednisone (corticosteroids)?

From the Guidelines

Prednisolone and prednisone are considered equivalent and can be used interchangeably in the same dosage, with the choice between them often depending on the country of origin or specific patient needs, such as liver disease. When considering the use of these corticosteroids, it's essential to understand their mechanism of action: prednisone is a prodrug that must be converted by the liver into prednisolone before it becomes active, while prednisolone is already in its active form 1. This difference may make prednisolone a preferable choice for patients with liver disease who might have difficulty converting prednisone.

Key Points to Consider

• Dosing for both medications is typically similar, with common dosages ranging from 5-60 mg daily, depending on the condition being treated 1.
• Both medications are available in various forms, including tablets, oral solutions, and injectable formulations.
• Side effects are also similar for both medications and include increased appetite, weight gain, mood changes, elevated blood sugar, and with long-term use, osteoporosis and adrenal suppression 1.
• Neither medication should be stopped abruptly after prolonged use, as tapering is necessary to allow the body's natural cortisol production to resume.

Clinical Decision Making

In clinical practice, the decision between prednisolone and prednisone should be guided by the individual patient's needs and health status. For patients with liver disease, prednisolone may be preferred due to its direct action. However, for most patients, either medication can be used effectively, and the choice may come down to factors such as availability, cost, and patient preference. It's also important to consider the potential for side effects and the need for monitoring and tapering when discontinuing these medications.

Evidence Summary

The equivalence of prednisolone and prednisone, as well as their dosing and side effect profiles, is supported by various studies and guidelines, including those from the KDIGO and EASL 1. These sources emphasize the importance of individualizing treatment and considering the specific needs and health status of each patient when selecting a corticosteroid regimen.

From the FDA Drug Label

The systemic availability, metabolism and elimination of prednisolone after administration of single weight-based doses (0. 8 mg/kg) of intravenous (IV) prednisolone and oral prednisone were reported in a small study of 19 young (23 to 34 years) and 12 elderly (65 to 89 years) subjects. Results showed that the systemic availability of total and unbound prednisolone, as well as interconversion between prednisolone and prednisone were independent of age

The main difference between prednisolone and prednisone is that they are interconvertible in the body, with prednisone being converted to prednisolone after administration 2.

• Prednisolone is the active form of the drug.
• Prednisone is a prodrug that is converted to prednisolone in the body. There is no significant difference in their glucocorticoid properties or clinical effects.

From the Research

Difference between Prednisolone and Prednisone

• Prednisone is converted in the liver to the active metabolite, prednisolone 3
• The principal therapeutic action of prednisolone is to suppress cytokine gene expression and to inhibit the differentiation and proliferation of activated lymphocytes, and it also has anti-inflammatory effects 3
• Prednisone and prednisolone are interconvertible, and the interconversion of prednisone into prednisolone is not a limiting factor, even in patients with severely impaired liver function 4
• The conversion of prednisone to prednisolone and the degree of plasma protein binding of prednisolone can be affected by liver disease, with impaired reduction of the 11-oxo group of prednisone and impaired ring A reduction of prednisolone in patients with active liver disease 5
• The bioavailability of prednisone is about 62%, and there is a high degree of interconversion between prednisone and prednisolone, with 76% of the dose being recycled 6

Pharmacokinetics

• The pharmacokinetics of prednisone and prednisolone are nonlinear, with dose-dependent pharmacokinetics that can partly explain the clinical observation that an alternate-day regimen with prednisone yields fewer biological effects 4
• The total body clearances of total and unbound prednisolone increase with increasing concentrations of prednisolone, and standardized doses need to be administered to compare pharmacokinetic results between different subjects 4
• The plasma half-life of prednisolone can be prolonged in patients with chronic liver disease 5

Clinical Implications

• The differences in pharmacokinetics and conversion between prednisone and prednisolone can have important practical implications for the use of corticosteroids in patients with active liver disease 5
• Advanced liver disease does not sufficiently suppress hepatic conversion of prednisone to warrant the preferential use of prednisolone 3