Yoshikawa T T, Guze L B
Antimicrob Agents Chemother. 1976 Sep;10(3):462-3. doi: 10.1128/AAC.10.3.462.
Concentrations of trimethoprim (TMP) and sulfamethoxazole (SMZ) in blood were determined in seven healthy volunteers after ingestion of 720 mg of TMP and 3,600 mg of SMZ (nine tablets of TMP-SMZ, 1:5 ratio) as a single oral dose. The mean levels of drug in blood achieved during the first 8 h after drug administration ranged from 6.12 to 8.32 mug/ml for TMP and 98 to 120 mug/ml for SMZ. These concentrations easily exceeded the previously reported minimal inhibitory concentrations for clinical isolates of Neisseria gonorrhoeae. The combination of TMP-SMZ given as a single, large oral dose may be a useful therapeutic regimen for patients with uncomplicated gonorrhea and susceptible microorganisms.
在七名健康志愿者单次口服720毫克甲氧苄啶(TMP)和3600毫克磺胺甲恶唑(SMZ)(九片TMP - SMZ,比例为1:5)后,测定了他们血液中的TMP和SMZ浓度。给药后最初8小时内血液中药物的平均水平,TMP为6.12至8.32微克/毫升,SMZ为98至120微克/毫升。这些浓度很容易超过先前报道的淋病奈瑟菌临床分离株的最低抑菌浓度。单次大剂量口服给予TMP - SMZ组合可能是治疗无并发症淋病和易感微生物患者的一种有效治疗方案。