McCloskey R V, LeFrock J L, Smith B R, Aronoff G R
Pharmacotherapy. 1982 Nov-Dec;2(6):300-12. doi: 10.1002/j.1875-9114.1982.tb03204.x.
The acylureido penicillin mezlocillin is active against gram-positive, gram-negative, and anaerobic bacteria. It easily penetrates the outer membrane of gram-negative bacteria, and it has a strong affinity for penicillin binding protein 3. Its stability to beta-lactamases is weak. Mezlocillin is synergistic when given in combination with aminoglycoside antibiotics. In pharmacokinetic studies mezlocillin conforms to a two compartment open model; its pharmacokinetic properties are dose-dependent. The half-life of the drug is about 1 hour after intravenous injection and 1.5 hours after intramuscular injection. Protein binding ranges from 16 to 42%, and 55% of a dose is excreted in the urine. Biliary excretion ranges from 0.5 to 25%. Clinical trial cure rates were as follows: bacteremia (78%), respiratory tract (62%), urinary tract (81%), gynecological (86%), bone and joint (55%), intraabdominal (67%) and skin and soft tissue (59%). The frequency of adverse reactions was 7.7%. Interstitial nephritis, CNS toxicity, and bleeding have not been reported.
酰脲类青霉素美洛西林对革兰氏阳性菌、革兰氏阴性菌及厌氧菌均有活性。它能轻易穿透革兰氏阴性菌的外膜，且对青霉素结合蛋白3有很强的亲和力。其对β-内酰胺酶的稳定性较弱。美洛西林与氨基糖苷类抗生素联合使用时有协同作用。在药代动力学研究中，美洛西林符合二室开放模型；其药代动力学特性呈剂量依赖性。静脉注射后该药的半衰期约为1小时，肌肉注射后为1.5小时。蛋白结合率为16%至42%，55%的给药剂量经尿液排泄。胆汁排泄率为0.5%至25%。临床试验治愈率如下：菌血症（78%）、呼吸道感染（62%）、尿路感染（81%）、妇科感染（86%）、骨和关节感染（55%）、腹腔内感染（67%）以及皮肤和软组织感染（59%）。不良反应发生率为7.7%。尚未有间质性肾炎、中枢神经系统毒性及出血的报道。
