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INTRODUCTION
Cefoperazone sodium is a semi synthetic, broad-spectrum, cephalosporin antibiotic. Sulbactam sodium is a derivative of the basic Penicillin nucleus.
Clinical Pharmacology :

Mechanism of Action:
Cefoperazone, a third generation Cephalosporin acts by inhibiting biosynthesis of cell wall mucopeptide. Sulbactam acts a beta-lactamase inhibitor, thus restoring Cefoperazone activity against beta-lactamase producing strains.

Pharmacokinetics :
Absorbtion: The mean serum concentration obtained at 30 min after 1 g I.V. Cefoperazone is 114 mcg/ml. The mean serum concentration obtained at 15 min. after 500 mg and 1000 mg IV Sulbactam are 21-40 mcg/ml and 48-88 mcg/ml respectively.
The average peak plasma concentration at 5 minutes after intravenous dose of 1g is 81mg/litre.
Distribution
The protein binding of Cefoperazone is 82-93% and that of Sulbactam is 38%.
Metabolism and Excretion
No significant quantity of metabolites of Cefoperazone has been found in the urine. The mean serum half-life of Cefoperazone and Sulbactam are about two hours and one hour respectively. Cefoperazone is excreted mainly in the bile. About 75-85% of Sulbactam is excreted in the urine during the first eight hours of administration.
Pharmacokinetics in Special Groups

Renal Insufficiency in Patients
No significant changes observed compared to normal patients.
Hepatic Insufficiency Patients:
In patients with hepatic dysfunction, the serum half life is prolonged and urinary excretion is increased. In patients combined with renal and hepatic insufficiency, Cefoperazone may accumulate in the serum.

Low Birth weight neonates
The half-life of Cefoperazone in low birth weight neonates is 6-10 hours.
Indications :
The combination of Cefoperazone sodium and Sulbactam sodium is indicated for the treatment of the following infections caused by susceptible organisms.
Respiratory tract infections (Upper and Lower), Urinary Tract Infections, Peritonitis, Cholecystitis, Cholangitis and other intra-abdominal infections, Bacterial sinusitis, Meningitis, Skin and soft tissue infections, Bone and Joint infections, Pelvic Inflammatory disease - endometritis, gonorrhea and other infections of the genital tract.
Contraindications :
Allergy to Penicillins or Cephalosporins.
Warnings:
Cefoperazone should be cautiously administered to penicillin sensitive patients. Pseudomembranous colitis has been reported with the use of Cephalosporins and other broad spectrum antibiotics.
Precautions :
A disulfiram-like reaction reported when alcohol was ingested within 72 hours of Cefoperazone administration. Patients should be advised not to take alcohol with Cefoperazone.
Adults:
The usual adult dose of the combination is 2 to 4 g/day (i.e, 1-2 g/day each of Cefoperazone and Sulbactam) given IV or IM in equally divided doses every 12 hours.

In severe or refractory infections the daily dosage may be increased to 8g (i.e, 4g/day each of Cefoperazone and Sulbactam) given IV in equally divided doses every 12 hours. The recommended maximum daily dosage of Sulbactam is 4g (8g of the combination). Dosage regimens should be adjusted in patients with marked decrease in renal function.
Children:
The usual dosage in children is 40-80mg/kg/day (20 to 40 mg/kg/day each of Cefoperazone and Sulbactam) every six to twelve hours. In serious or refractory infections, these dosages may be increased up to 160 mg/kg/idea of the combination. (i.e., 80 mg/kg/day each of Cefoperazone and Sulbactam) every six to twelve hours.
Intravenous Administration:
For intermittent infusion, each vial should be reconstituted with the appropriate amount of Sterile Water for Injections and then diluted to 20 ml with the same solution followed by administration over 15 to 60 minutes.

For IV injection, each vial should be reconstituted as above and administered over a minimum period of three minutes.
Intramuscular Administration:
Sterile Water for Injection should be used for reconstitution. For a concentration of Cefoperazone of 250 mg/ml or larger, a two step dilution is required using Sterile Water for Injection followed by 2% Lidocaine.
Storage:
Till reconstitution, store below 25 deg C. Protect from light.
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