INJLIN

Indications

• Bacterial infections
• Pneumonia
• Sepsis
• Intra-abdominal infections
• Skin and soft tissue infections
• Urinary tract infections

Dosage

Children: Refer to the BNF for Children for specific dosage information.

Adults: Refer to the BNF for specific dosage information.

Mechanism of action

Cefoperazone binds to specific penicillin-binding proteins (PBPs) located inside the bacterial cell wall. This binding inhibits the third and final stage of bacterial cell wall synthesis. The result is cell lysis, which is facilitated by bacterial cell wall autolytic enzymes such as autolysins.

Pharmacodynamics

As a third generation cephalosporin, cefoperazone exerts a bactericidal effect by inhibiting bacterial cell wall synthesis. This mechanism is critical for its effectiveness against a range of pathogens, particularly those that are resistant to other antibiotics.

Pharmacokinetics

Cefoperazone is administered parenterally and has a half-life that allows for once or twice daily dosing. It is widely distributed in body tissues and fluids, including the central nervous system. Cefoperazone is primarily eliminated by the kidneys, with a portion also excreted in bile, making it suitable for treating infections in patients with renal impairment, although dosage adjustments may be necessary.

Contra-indications

• Hypersensitivity to cefoperazone or other beta-lactam antibiotics
• History of severe allergic reactions to any cephalosporin

Adverse effects

• Diarrhea
• Nausea
• Vomiting
• Rash
• Elevated liver enzymes
• Thrombocytopenia
• Neutropenia

Interactions

• Probenecid may increase cefoperazone levels by reducing renal excretion
• Concurrent use with aminoglycosides may enhance nephrotoxicity
• Potential interaction with anticoagulants leading to increased bleeding risk

Precautions

• Use with caution in patients with renal impairment
• Monitor liver function tests during therapy
• May cause false-positive results for urine glucose tests

Pregnancy

Cefoperazone should be used during pregnancy only if the potential benefit justifies the potential risk to the fetus.

Breast-feeding

Cefoperazone is excreted in breast milk; caution should be exercised when administered to nursing mothers.

Storage

Store at room temperature, away from light and moisture. Reconstituted solutions should be stored in the refrigerator and used within a specified time frame as per manufacturer guidelines.

Formulations

• Cefoperazone sodium for injection

Indications

• Pneumonia
• Urinary tract infections
• Septicemia
• Intra-abdominal infections
• Skin and soft tissue infections
• Bone and joint infections

Dosage

Children: Refer to the specific prescribing guidelines and pediatric dosing references for detailed dosing recommendations.

Adults: Refer to the specific prescribing guidelines and local protocols for detailed dosing recommendations.

Mechanism of action

Cefoperazone exerts its antibacterial effect by inhibiting bacterial cell wall synthesis. It achieves this by binding to penicillin-binding proteins (PBPs) located inside the bacterial cell wall, leading to the disruption of cell wall integrity and ultimately causing cell lysis and death. The drug is particularly effective against Gram-negative bacteria due to its ability to penetrate the outer membrane.

Pharmacodynamics

The pharmacodynamics of cefoperazone involve its time-dependent bactericidal activity, where the duration of time that plasma concentrations remain above the minimum inhibitory concentration (MIC) is critical for its effectiveness. Cefoperazone demonstrates a broad spectrum of activity against various bacteria, including organisms that produce beta-lactamase enzymes, which can inactivate many other beta-lactam antibiotics.

Pharmacokinetics

Cefoperazone is administered parenterally, with good distribution in body tissues and fluids. It is metabolized in the liver and has a half-life of approximately 2 hours, although this can vary with renal function. The drug is primarily excreted via the kidneys, with about 60% of the dose eliminated unchanged in the urine. Cefoperazone can achieve therapeutic concentrations in bile and urine, making it effective for treating infections in those areas.

Contra-indications

• Hypersensitivity to cefoperazone or any cephalosporin antibiotics
• Severe renal impairment with anuria
• History of cholestatic jaundice or hepatic dysfunction associated with cefoperazone

Adverse effects

• Diarrhea
• Nausea
• Vomiting
• Rash
• Allergic reactions
• Increased liver enzymes (transaminases)
• Thrombocytopenia
• Nephrotoxicity
• Superinfection

Interactions

• Probenecid may increase the plasma concentration of cefoperazone
• Cefoperazone may interfere with the effects of oral anticoagulants
• Concurrent use with aminoglycosides may increase the risk of nephrotoxicity
• May reduce the effectiveness of oral contraceptives

Precautions

• Use with caution in patients with a history of gastrointestinal disease, particularly colitis
• Monitor renal function in patients with pre-existing renal impairment
• Caution in patients with a history of allergy to penicillins due to potential cross-reactivity
• Regular monitoring of liver function tests is advisable during prolonged therapy

Pregnancy

Cefoperazone is classified as pregnancy category B, indicating that it is not expected to harm the fetus based on animal studies, but should be used only if clearly needed.

Breast-feeding

Cefoperazone is excreted in human milk in small amounts. Caution is advised when administering to breastfeeding women.

Storage

Store at room temperature, away from moisture and heat. Protect from light.

Formulations

• Cefoperazone sodium for injection
• Cefoperazone in combination with sulbactam

Mechanism of action

Like all beta-lactam antibiotics, cefoperazone binds to specific penicillin-binding proteins (PBPs) located inside the bacterial cell wall, causing the inhibition of the third and last stage of bacterial cell wall synthesis. Cell lysis is then mediated by bacterial cell wall autolytic enzymes such as autolysins.

Pharmacodynamics

Cefoperazone is a third generation cephalosporin antibiotic. Cefoperazone exerts its bactericidal effect by inhibiting the bacterial cell wall synthesis