cefoperazone

Cefoperazone is a broad-spectrum cephalosporin antibiotic in the third generation of the beta-lactam class. It is commonly given by intravenous or intramuscular injection and is often used in combination with a beta-lactamase inhibitor, such as sulbactam, in products marketed for extended activity against resistant organisms and anaerobes (for example, cefoperazone/sulbactam).

Mechanism and spectrum: Cefoperazone inhibits bacterial cell wall synthesis by binding to penicillin-binding proteins, leading to cell lysis. It has good activity against many gram-negative bacteria, including some Pseudomonas species, and weaker activity against gram-positive cocci. When combined with a beta-lactamase inhibitor, its spectrum broadens to include anaerobes and beta-lactamase–producing organisms. It is less reliable against certain resistant organisms such as many strains producing extended-spectrum beta-lactamases.

Pharmacokinetics: The drug is administered IV or IM and distributes widely in body tissues and fluids. Excretion occurs through both renal and biliary routes, with the latter being prominent for cefoperazone. The elimination half-life is typically a few hours in adults, and dose adjustments are needed in renal impairment; hepatic considerations may influence clearance in some patients.

Indications and cautions: Cefoperazone is used for serious infections caused by susceptible bacteria, including pneumonia, intra-abdominal and gynecologic infections, septicemia, and skin or soft tissue infections, particularly when anaerobes or resistant gram-negatives are a concern (often in combination therapy). Caution is advised in patients with coagulation disorders or those on anticoagulants due to potential hypoprothrombinemia associated with certain side chains; disulfiram-like reactions with alcohol have been reported with some related cephalosporins and may occur. Contraindications include hypersensitivity to cephalosporins or penicillins. Resistance can arise from beta-lactamase production or other mechanisms, limiting usefulness in some settings.