Piperacillin Sodium is a broad-spectrum semisynthetic penicillin antibiotic used to treat a variety of infections caused by susceptible bacteria[1]. Piperacillin Sodium exerts its antibacterial action by inhibiting bacterial cell wall synthesis and is effective against a wide range of Gram-positive and Gram-negative bacteria, including some strains that produce β-lactamases[2]. Piperacillin Sodium is often used in combination with other drugs, such as tazobactam, to enhance antibacterial efficacy and broaden the spectrum of activity, better addressing resistant strains[3]. Piperacillin Sodium is commonly used to treat respiratory, urinary, intra-abdominal infections, and skin and soft tissue infections[4].
In vitro, Piperacillin Sodium (2μg/mL) inhibits Staphylococcus aureus with an efficacy rate of up to 93%, and Piperacillin Sodium (4μg/mL) inhibits Escherichia coli with an efficacy rate of up to 90%[5]. Piperacillin Sodium (2–8μg/mL) pre-treatment of various bacteria (Klebsiella pneumoniae, Streptococcus agalactiae, Proteus vulgaris, Haemophilus influenzae) for 18 hours significantly inhibits bacterial growth and reduces resistance[6].
In vivo, Piperacillin Sodium (2.5–5120mg/kg) in combination with the novel β-lactamase inhibitor IID572 (4–640mg/kg) administered subcutaneously three times daily was used in a neutropenic C57BL/6J mouse thigh infection model. The combination of Piperacillin/IID572 significantly reduced the infection burden caused by β-lactamase-producing Enterobacteriaceae and Staphylococcus aureus[7]. Subcutaneous injection of Piperacillin Sodium (10.7mg) in combination with oral β-lactamase (1 or 6mg/kg) was used in CF-1 mice. Compared with mice treated with Piperacillin Sodium alone, the combination with β-lactamase significantly reduced intestinal colonization by Piperacillin-resistant pathogens (including vancomycin-resistant Enterococcus faecium, Klebsiella pneumoniae, and Candida glabrata) and minimized disruption of the indigenous microbiota[8].
References:
[1] Fortner CL, Finley RS, Schimpff SC. Piperacillin sodium: antibacterial spectrum, pharmacokinetics, clinical efficacy, and adverse reactions. Pharmacotherapy. 1982 Nov-Dec;2(6):287-99.
[2] Holmes B, Richards DM, Brogden RN, et al. Piperacillin. A review of its antibacterial activity, pharmacokinetic properties and therapeutic use. Drugs. 1984 Nov;28(5):375-425.
[3] Eliopoulos GM, Moellering RC Jr. Azlocillin, mezlocillin, and piperacillin: new broad-spectrum penicillins. Ann Intern Med. 1982 Nov;97(5):755-60.
[4] Russo J Jr, Russo ME. Comparative review of two new wide-spectrum penicillins: mezlocillin and piperacillin. Clin Pharm. 1982 May-Jun;1(3):207-16.
[5] Frank U, Mutter J, Schmidt-Eisenlohr E, et al. Comparative in vitro activity of piperacillin, piperacillin-sulbactam and piperacillin-tazobactam against nosocomial pathogens isolated from intensive care patients. Clin Microbiol Infect. 2003 Nov;9(11):1128-32.
[6] Verbist L. In vitro activity of piperacillin, a new semisynthetic penicillin with an unusually broad spectrum of activity. Antimicrob Agents Chemother. 1978 Mar;13(3):349-57. doi: 10.1128/AAC.13.3.349.
[7] Growcott EJ, Gamboa L, Roth T, et al. Efficacy of piperacillin in combination with novel β-lactamase inhibitor IID572 against β-lactamase-producing strains of Enterobacteriaceae and Staphylococcus aureus in murine neutropenic thigh infection models. J Antimicrob Chemother. 2020 Jun 1;75(6):1530-1536.
[8] Stiefel U, Pultz NJ, Harmoinen J, et al. Oral administration of beta-lactamase preserves colonization resistance of piperacillin-treated mice. J Infect Dis. 2003 Nov 15;188(10):1605-9.
Piperacillin Sodium是一种广谱半合成青霉素类抗生素，用于治疗多种由敏感细菌引起的感染[1]。Piperacillin Sodium通过抑制细菌细胞壁的合成发挥抗菌作用，能够有效对抗多种革兰氏阳性菌和革兰氏阴性菌，包括一些产β-内酰胺酶的菌株[2]。Piperacillin Sodium通常与其他药物（如他唑巴坦）联合使用，以增强抗菌效果并扩大抗菌谱，更好地应对耐药菌株[3]。Piperacillin Sodium常用于治疗呼吸道感染、泌尿道感染、腹腔感染和皮肤软组织感染等[4]。
在体外，Piperacillin Sodium（2μg/mL）对Staphylococcus aureus的抑制率高达93%，Piperacillin Sodium（4μg/mL）对Escherichia coli的抑制率高达90%[5]。Piperacillin Sodium（2–8μg/mL）预处理多种细菌（Klebsiella pneumoniae、Streptococcus agalactiae、Proteus vulgaris、Haemophilus influenzae）18h，Piperacillin Sodium显著抑制细菌的生长，同时降低耐药性表现[6]。
在体内，Piperacillin Sodium（2.5–5120mg/kg）联合新型β-内酰胺酶抑制剂IID572（4–640mg/kg）每天三次皮下注射，用于处理中性粒细胞减少的C57BL/6J小鼠大腿感染模型。Piperacillin/IID572显著减少了由产β-内酰胺酶的肠杆菌科细菌和金黄色葡萄球菌引起的感染负担[7]。皮下注射Piperacillin Sodium（10.7mg）联合口服β-内酰胺酶（1或6mg/kg），用于处理CF-1小鼠。与仅接受Piperacillin Sodium的小鼠相比，联合β-内酰胺酶显著减少了由耐Piperacillin的病原体（包括vancomycin-resistant Enterococcus faecium、Klebsiella pneumoniae和Candida glabrata）引起的肠道定植，同时减少了对肠道菌群的干扰[8]。