Antibiotic Pharmacokinetics and Prostate Penetration in Bacterial Prostatitis: A Systematic Review

Abstract Background Effective treatment of bacterial prostatitis is limited by poor antibiotic penetration into prostatic tissue due to anatomical and physiological barriers, including the blood–prostate barrier, pH-dependent ion trapping, and protein binding. Methods A systematic review was conducted to evaluate the intraprostatic pharmacokinetics of antibiotics. PubMed, Embase, and Medline were searched up to December 2024. In total, 44 studies reporting antibiotic concentrations in serum, prostate tissue, or prostatic fluids were included. Prostate tissue-to-serum ratios (PT/S) and pharmacokinetic parameters were analyzed to assess prostate penetration. Results A total of 44 studies were included. Fluoroquinolones consistently demonstrated favorable intraprostatic penetration (PT/S ≥ 1), supporting their role as first-line agents. Trimethoprim–sulfamethoxazole (TMP–SMX) showed moderate penetration driven primarily by trimethoprim, while macrolides and tetracyclines exhibited variable but measurable distribution. Most β-lactams penetrated poorly into non-inflamed prostate tissue, although selected cephalosporins achieved moderate concentrations in acute inflammatory settings. Fosfomycin showed variable intraprostatic exposure, indicating that tissue diffusion does not uniformly translate into clinical efficacy, particularly in chronic disease. Conclusions Antibiotic efficacy in prostatitis is strongly influenced by intraprostatic pharmacokinetics rather than drug class alone. Integrating physicochemical properties, disease subtype, and clinical guideline recommendations is essential for rational antibiotic selection and optimized treatment strategies.