Fortner C L, Finley R S, Schimpff S C
Pharmacotherapy. 1982 Nov-Dec;2(6):287-99. doi: 10.1002/j.1875-9114.1982.tb03202.x.
Piperacillin sodium is a beta lactam antibiotic with a broad range of antibacterial activity that includes gram-negative bacilli, gram-positive cocci (except penicillinase-producing S. aureus) and anaerobic pathogens such as Clostridium difficile, and Bacteroides fragilis. Piperacillin inhibits many of the members of the Enterobacteriaceae, including Klebsiella sp and Pseudomonas, at lower concentrations than required for carbenicillin and ticarcillin. Piperacillin sodium is administered by intramuscular and intravenous injection and is widely distributed throughout body fluids and tissues. Like other newer penicillins, piperacillin is excreted by both renal and biliary mechanisms. The primary route of elimination is by glomerular filtration, which results in high urinary concentrations of the unchanged compound. Piperacillin has been approved for patients with serious infection caused by susceptible strains of specific organisms in intra-abdominal, urinary tract, gynecologic, lower respiratory tract, skin and skin structure, bone and joint, and gonococcal infections and septicemia. As with other penicillins, piperacillin has a low frequency of toxicity. The usual dose of piperacillin in adults with serious infections with normal renal function is 3-4 g every 4-6 hr as a 20-30 min infusion, with a maximum dose of 24 g per day. It is stable in most large volume parenteral solutions. Less serious infectins (requiring smaller dosages) may be treated by intramuscular injection; however, no more than 2 g should be given at any one injection site. Overall, piperacillin has a greater degree of activity than other penicillins. Evidence from prospective studies indicates that piperacillin is a highly effective agent for the treatment of patients with infections caused by susceptible organisms.
哌拉西林钠是一种β-内酰胺类抗生素,抗菌活性范围广泛,包括革兰氏阴性杆菌、革兰氏阳性球菌(产青霉素酶的金黄色葡萄球菌除外)以及厌氧病原体,如艰难梭菌和脆弱拟杆菌。与羧苄西林和替卡西林相比,哌拉西林在较低浓度下就能抑制许多肠杆菌科细菌,包括克雷伯菌属和假单胞菌属。哌拉西林钠通过肌肉注射和静脉注射给药,广泛分布于体液和组织中。与其他新型青霉素一样,哌拉西林通过肾脏和胆汁机制排泄。主要消除途径是肾小球滤过,这导致尿液中未改变的化合物浓度很高。哌拉西林已被批准用于治疗由特定生物体的敏感菌株引起的严重感染,包括腹腔内、泌尿道、妇科、下呼吸道、皮肤及皮肤结构、骨与关节、淋球菌感染和败血症。与其他青霉素一样,哌拉西林的毒性发生率较低。肾功能正常的成人严重感染时,哌拉西林的常用剂量是每4 - 6小时3 - 4克,静脉滴注20 - 30分钟,最大剂量为每天24克。它在大多数大容量肠外溶液中稳定。不太严重的感染(需要较小剂量)可用肌肉注射治疗;然而,任何一个注射部位的剂量不应超过2克。总体而言,哌拉西林比其他青霉素具有更高的活性程度。前瞻性研究的证据表明,哌拉西林是治疗由敏感生物体引起感染患者的高效药物。