Rectally administered prednisolone--evidence for a predominantly local action

Area of Science:

• Pharmacology
• Gastroenterology
• Drug Metabolism

Background:

• Idiopathic proctocolitis is an inflammatory bowel disease.
• Prednisolone is a common treatment for proctocolitis.
• Different formulations of prednisolone may have varying systemic absorption and efficacy.

Purpose of the Study:

• To compare plasma prednisolone levels after administration of two different prednisolone enema formulations.
• To assess the efficacy of prednisolone metasulphobenzoate versus prednisolone-21-phosphate in treating proctocolitis.
• To investigate the pharmacokinetic and therapeutic profiles of topical prednisolone in proctocolitis.

Main Methods:

• Administration of retention enemata containing prednisolone-21-phosphate or prednisolone metasulphobenzoate sodium.
• Measurement of plasma prednisolone levels in healthy volunteers and proctocolitis patients.
• Clinical assessment of treatment effectiveness in a subset of patients.

Main Results:

• Plasma prednisolone levels were significantly lower following administration of prednisolone metasulphobenzoate.
• This difference was observed regardless of disease activity.
• Prednisolone metasulphobenzoate demonstrated comparable efficacy to prednisolone-21-phosphate in the limited patient comparisons.

Conclusions:

• Prednisolone metasulphobenzoate exhibits reduced systemic absorption compared to prednisolone-21-phosphate.
• The therapeutic benefits of prednisolone enemas in proctocolitis may be primarily due to local action.
• Prednisolone metasulphobenzoate is a viable alternative for proctocolitis treatment with potentially lower systemic side effects.