VAXCEL CEFOBACTAM 1G INJECTION

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

• Infections caused by beta-lactamase producing organisms
• Complicated skin and soft tissue infections
• Intra-abdominal infections
• Respiratory tract infections
• Urinary tract infections

Dosage

Children: Refer to BNF for Children for specific dosing recommendations based on the child's age, weight, and the type of infection.

Adults: Refer to BNF for specific dosing recommendations based on the type and severity of the infection.

Mechanism of action

Sulbactam is a competitive, irreversible inhibitor of bacterial beta-lactamases, particularly potent against class C beta-lactamases. It binds to the active site of the enzyme, preventing it from hydrolyzing beta-lactam antibiotics, which enhances the effectiveness of these antibiotics against resistant bacterial strains.

Pharmacodynamics

When administered with beta-lactam antibiotics, sulbactam broadens their antibacterial spectrum by inhibiting the enzymes responsible for their hydrolysis. Although sulbactam has weak intrinsic antibacterial activity on its own, it can effectively bind to penicillin-binding proteins in certain bacteria, contributing to its therapeutic effect. It helps restore the activity of beta-lactam antibiotics against a wide range of beta-lactamase-producing gram-positive and gram-negative bacteria.

Pharmacokinetics

Sulbactam is administered parenterally and is typically well absorbed. It has a short half-life, necessitating frequent dosing when used alone. The drug is primarily excreted unchanged in the urine. Its pharmacokinetic profile may vary based on the formulation used and the presence of co-administered antibiotics.

Pregnancy

There is limited data on the use of sulbactam in pregnancy. It should only be used if the potential benefit justifies the potential risk to the fetus.

Breast-feeding

It is not known if sulbactam is excreted in human milk. Caution is advised when administering to breastfeeding women.

Storage

Store in a cool, dry place, away from direct light. Protect from moisture.

Formulations

• Injectable solution

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

Mechanism of action

Sulbactam is a competitive, irreversible bacterial beta (β)-lactamase inhibitor. It is reported to be more potent against class C beta-lactamases.

Pharmacodynamics

When given together with beta-lactam antibiotics, sulbactam broadens their antibacterial spectrum by blocking the enzyme involved in their hydrolysis. Sulbactam alone possesses weak intrinsic antibacterial activity except against the _Neisseriaceae_, _Acinetobacter spp._, and _Bacteroides fragilis_ as it can bind to the penicillin-binding proteins. Sulbactam restores the activity of beta-lactam antibiotics against a range of beta-lactamase-producing gram-positive and gram-negative bacteria.