Prednisone absorption primarily occurs in the small intestine, reaching peak plasma concentrations within 1-2 hours post-oral administration. Bioavailability is approximately 80-90%, meaning a significant portion of the ingested dose enters the bloodstream.

Following absorption, prednisone undergoes rapid and extensive first-pass hepatic metabolism, primarily converting to its active metabolite, prednisolone. This conversion significantly affects the overall pharmacological effect. Prednisolone then distributes widely throughout the body, crossing most biological membranes.

Plasma protein binding is substantial, with approximately 70-90% binding to albumin. This binding influences the distribution volume and the amount of free, pharmacologically active drug. Factors like age, liver function, and protein status modify this binding and thus impact drug distribution and efficacy.

Prednisolone’s distribution volume is relatively large, indicating its presence in various tissues and compartments throughout the body. High concentrations accumulate in tissues like the liver, kidneys, and lungs. The concentration in other tissues varies depending on tissue-specific characteristics.

Clinical Significance: Understanding these pharmacokinetic properties is critical for optimizing prednisone dosing strategies, especially in patients with impaired hepatic or renal function, or those with altered protein binding. These conditions can impact both absorption and distribution, leading to altered therapeutic responses.

Note: This information is for educational purposes only and does not constitute medical advice. Consult a healthcare professional for personalized guidance regarding prednisone use.