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Subjects were prostatic hyperplasia patients prophylactically receiving a 0.5\u2010hour infusion of 1.5 g (1:0.5 g) or 3 g (2:1 g) ampicillin\u2010sulbactam before transurethral resection of the prostate. Ampicillin and sulbactam concentrations in plasma and prostate tissue were measured. The prostate tissue\/plasma ratios of both ampicillin and sulbactam were approximately 0.37 (area under the drug concentration\u2010time curve), and penetration was similar. The prostatic population pharmacokinetic model, which included a covariate analysis, adequately predicted prostate tissue concentrations in our patient population. For therapeutic use, aiming for a bactericidal target of 50% of time above minimum inhibitory concentration (T &gt; MIC) in prostate tissue, 3 g ampicillin\u2010sulbactam 4 times daily achieved \u226590% expected probability against only <jats:italic>Enterococcus faecalis<\/jats:italic> in typical patients with a creatinine clearance (CL<jats:sub>cr<\/jats:sub>) of 30\u00a0mL\/min. For prophylactic use, aiming for a bacteriostatic target of 30% T &gt; MIC, 3 g ampicillin\u2010sulbactam 4 times daily achieved \u226590% expected probability of attaining the bacteriostatic target against <jats:italic>E. faecalis<\/jats:italic> and <jats:italic>Proteus<\/jats:italic> species when CL<jats:sub>cr<\/jats:sub> was 30\u00a0mL\/min. Based on prostatic simulations, the present study provides helpful recommendations for the treatment of bacterial prostatitis and preoperative prophylaxis in prostatectomy.<\/jats:p>","DOI":"10.1002\/jcph.1800","type":"journal-article","created":{"date-parts":[[2020,12,13]],"date-time":"2020-12-13T07:28:28Z","timestamp":1607844508000},"page":"820-831","update-policy":"https:\/\/doi.org\/10.1002\/crossmark_policy","source":"Crossref","is-referenced-by-count":15,"title":["Prostatic Pharmacokinetic\/Pharmacodynamic Evaluation of Ampicillin\u2010Sulbactam for Bacterial Prostatitis and Preoperative Prophylaxis"],"prefix":"10.1002","volume":"61","author":[{"ORCID":"https:\/\/orcid.org\/0000-0003-1174-0787","authenticated-orcid":false,"given":"Tetsushu","family":"Onita","sequence":"first","affiliation":[{"name":"Department of Clinical Pharmacotherapy Hiroshima University  Minami\u2010ku Hiroshima Japan"},{"name":"Department of Pharmacy Shimane University Hospital  Izumo Shimane Japan"}],"role":[{"role":"author","vocabulary":"crossref"}]},{"given":"Kazuro","family":"Ikawa","sequence":"additional","affiliation":[{"name":"Department of Clinical Pharmacotherapy Hiroshima University  Minami\u2010ku Hiroshima Japan"}],"role":[{"role":"author","vocabulary":"crossref"}]},{"given":"Kogenta","family":"Nakamura","sequence":"additional","affiliation":[{"name":"Department of Urology Aichi Medical University School of Medicine  Nagakute Aichi Japan"}],"role":[{"role":"author","vocabulary":"crossref"}]},{"given":"Genya","family":"Nishikawa","sequence":"additional","affiliation":[{"name":"Department of Urology Aichi Medical University School of Medicine  Nagakute Aichi Japan"}],"role":[{"role":"author","vocabulary":"crossref"}]},{"given":"Ikuo","family":"Kobayashi","sequence":"additional","affiliation":[{"name":"Department of Urology Aichi Medical University School of Medicine  Nagakute Aichi Japan"}],"role":[{"role":"author","vocabulary":"crossref"}]},{"given":"Noriyuki","family":"Ishihara","sequence":"additional","affiliation":[{"name":"Department of Pharmacy Shimane University Hospital  Izumo Shimane Japan"}],"role":[{"role":"author","vocabulary":"crossref"}]},{"given":"Hiroki","family":"Tamaki","sequence":"additional","affiliation":[{"name":"Department of Pharmacy Shimane University Hospital  Izumo Shimane Japan"}],"role":[{"role":"author","vocabulary":"crossref"}]},{"given":"Takahisa","family":"Yano","sequence":"additional","affiliation":[{"name":"Department of Pharmacy Shimane University Hospital  Izumo Shimane Japan"}],"role":[{"role":"author","vocabulary":"crossref"}]},{"given":"Kohji","family":"Naora","sequence":"additional","affiliation":[{"name":"Department of Pharmacy Shimane University Hospital  Izumo Shimane Japan"}],"role":[{"role":"author","vocabulary":"crossref"}]},{"given":"Norifumi","family":"Morikawa","sequence":"additional","affiliation":[{"name":"Department of Clinical Pharmacotherapy Hiroshima University  Minami\u2010ku Hiroshima Japan"}],"role":[{"role":"author","vocabulary":"crossref"}]}],"member":"311","published-online":{"date-parts":[[2021,1,12]]},"reference":[{"key":"e_1_2_8_2_1","unstructured":"USP UNASYN (ampicillin sodium\/sulbactam sodium) Jan 2017.https:\/\/www.accessdata.fda.gov\/drugsatfda_docs\/label\/2017\/050608s044lbl.pdf. 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