XTRACEF INJECTION 1G

Indications

• Bacterial infections
• Respiratory tract infections
• Urinary tract infections
• Skin and soft tissue infections
• Bone and joint infections
• Intra-abdominal infections

Dosage

Children: Refer to the BNF for Children for appropriate dosing information in paediatric patients.

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

Mechanism of action

Cefoprazone works by inhibiting bacterial cell wall synthesis. It binds to penicillin-binding proteins (PBPs) located inside the bacterial cell wall, disrupting the transpeptidation process, which is crucial for cell wall integrity. This leads to cell lysis and ultimately bacterial death. Its activity against both Gram-positive and Gram-negative bacteria is due to its ability to penetrate the outer membrane of Gram-negative bacteria.

Pharmacodynamics

Cefoprazone exhibits time-dependent antibacterial activity, meaning that the efficacy is related to the time the drug concentration remains above the minimum inhibitory concentration (MIC) of the target organism. It has a wide spectrum of activity and is particularly effective against certain strains of Escherichia coli, Klebsiella pneumoniae, and Staphylococcus aureus.

Pharmacokinetics

Cefoprazone is administered parenterally and is well-distributed throughout the body. It has a half-life of approximately 2 to 3 hours, allowing for multiple daily dosing. The drug is primarily excreted by the kidneys, with a small percentage eliminated through bile. Its elimination can be affected in patients with renal impairment, necessitating dosage adjustments.

Contra-indications

• Hypersensitivity to cefoprazone or other cephalosporins
• Severe renal impairment
• History of cholestatic jaundice or hepatic dysfunction associated with cefoprazone

Adverse effects

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

Interactions

• Probenecid may increase cefoprazone levels
• Anticoagulants may have increased effects and bleeding risk
• Concurrent use with aminoglycosides may increase nephrotoxicity

Precautions

• Use with caution in patients with a history of gastrointestinal disease
• Monitor renal function in patients with renal impairment
• Caution in patients with known allergies to penicillins, as cross-reactivity may occur

Pregnancy

Cefoprazone should only be used in pregnancy if the benefits outweigh the risks, as there is limited data on its safety.

Breast-feeding

Cefoprazone is excreted in breast milk. Caution is advised when administering to nursing mothers.

Storage

Store at controlled room temperature, away from moisture, and protect from light.

Formulations

• Injection: cefoprazone sodium 1 g, 2 g vials for reconstitution

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

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.