PRAZONE S 1GM

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

• Intra-abdominal infections
• Skin and soft tissue infections
• Respiratory tract infections
• Urinary tract infections
• Gynecological infections

Dosage

Children: Refer to the BNF for Children for appropriate paediatric dosing guidance, as it varies based on the child's age, weight, and specific condition being treated.

Adults: Refer to the BNF for specific dosing recommendations, which vary based on the infection being treated and the antibiotic used in combination with sulbactam.

Mechanism of action

Sulbactam works by irreversibly binding to the active site of beta-lactamase enzymes, thereby inhibiting their ability to hydrolyze and deactivate beta-lactam antibiotics. This action results in increased levels of these antibiotics in the presence of resistant bacteria, allowing them to maintain their antibacterial activity.

Pharmacodynamics

Sulbactam has no intrinsic antibacterial activity on its own but enhances the activity of beta-lactam antibiotics. Its action allows for higher concentrations of antibiotics like ampicillin or amoxicillin to remain effective against resistant strains of bacteria. The combination therapy leads to a synergistic effect, improving the overall therapeutic outcome.

Pharmacokinetics

Sulbactam is generally well absorbed when administered intravenously. Its distribution is widespread throughout body tissues, and it is known to cross the blood-brain barrier to some extent. Sulbactam is primarily excreted unchanged in the urine, with a half-life of approximately 1 hour, necessitating regular dosing to maintain effective levels in the bloodstream.

Contra-indications

• Hypersensitivity to sulbactam or any component of the formulation
• Severe allergic reactions to beta-lactam antibiotics

Adverse effects

• Allergic reactions, including rash, pruritus, and anaphylaxis
• Gastrointestinal disturbances, such as diarrhea, nausea, and vomiting
• Hematologic reactions, including thrombocytopenia and eosinophilia
• Liver enzyme elevations
• Renal impairment

Interactions

• May enhance the effects of warfarin, leading to increased risk of bleeding
• Potential interaction with probenecid, which may inhibit renal excretion of sulbactam
• Concurrent use with other antibiotics may lead to altered efficacy

Precautions

• Use with caution in patients with a history of penicillin allergy
• Monitor renal function in patients with pre-existing renal impairment
• Caution in patients with severe hepatic impairment
• Evaluate for signs of superinfection with prolonged use

Pregnancy

Sulbactam is classified as pregnancy category B. Animal reproduction studies have not shown a risk to the fetus, but there are no well-controlled studies in pregnant women.

Breast-feeding

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

Storage

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

Formulations

• Sulbactam injection for intravenous or intramuscular use
• Combination formulations with beta-lactam antibiotics, such as ampicillin-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