Piperacillin Sodium: Antibacterial Spectrum, Pharmacokinetics, Clinical Efficacy, and Adverse Reactions

Abstract

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.

Piperacillin-tazobactam versus imipenem-cilastatin for treatment of intra-abdominal infections

“…Piperacillin-resistant, piperacillin-tazobactam-susceptible microorganisms were isolated from 26 patients treated with piperacillintazobactam and 29 patients treated with imipenem-cilastatin. In the piperacillin-tazobactam group, the bacteria were eradicated from 24 patients and 2 patients showed persistence of microorganisms, while the bacteria were eradicated from 23 patients in the imipenem-cilastatin group, 1 patient developed a reinfection, and 5 5-072) in the imipenem-cilastatin group had enterococcal superinfections with susceptible organisms. Two hundred seventy aerobic and 164 anaerobic bacterial strains were isolated.…”

“…It is active against most enterobacteria and also shows good activity against enterococci and most anaerobic bacteria (5).…”

Penetration of piperacillin-tazobactam into cancellous and cortical bone tissues

“…Piperacillin sodium has been widely used in the treatment of serious infections, including bone and joint infections (4,14). Its effect, however, is limited by its susceptibility to 3-lactamase inactivation.…”

“…Fat, muscle, omentum, intestinal mucosa, prostate, lung, appendix, skin, gall bladder, and gynecological tissues have been obtained from patients undergoing abdominal or thoracic surgery, cholecystectomy, hysterectomy, or resection of the prostate; and blister fluid has been obtained from healthy volunteers. Piperacillin and tazobactam 4.52 ,ug/g for tazobactam). Our results are comparable to those for other ,-lactamase inhibitors, i.e., clavulanic acid has been reported to achieve concentrations in bone in excess of those necessary to inhibit 3-lactamases to a clinically significant extent (1,5,13).…”

Treatment of hospitalized patients with complicated skin and skin structure infections: double-blind, randomized, multicenter study of piperacillin-tazobactam versus ticarcillin-clavulanate. The Piperacillin/Tazobactam Skin and Skin Structure Study Group

“…broad spectrum of antibacterial activity, has been used widely in the treatment of serious infections (3,7). One disadvantage of piperacillin is its susceptibility to P-lactamase inactivation.…”