ACTZONE-S 1.5 Injection

Cefopera zone 1000 mg + Sulbactam 500 mg

Sulbactam and cefoperazone is a combination of beta-lactamase inhibitor plus beta-lactam. Sulbactam sodium/ cefoperazone sodium combination is available as a dry powder for reconstitution.

The antibacterial component of sulbactam/cefoperazone is cefoperazone, a third generation cephalosporin, which acts against sensitive organisms during the stage of active multiplication by inhibiting biosynthesis of cell wall mucopeptide.

Sulbactam does not possess any useful antibacterial activity, except against Neisseriaceae and Acinetobacter. As sulbactam also binds with some penicillin binding proteins, sensitive strains are also often rendered more susceptible to sulbactam/cefoperazone than to cefoperazone alone.

The combination of cefoperazone and sulbactam is active against all organisms sensitive to cefoperazone. In addition it demonstrates synergistic activity (up to fourfold reduction in minimum inhibitory concentrations for the combination versus those for each component) in a variety of organisms.

RATIONALE OF COMBINATION:

In March 2003, the Infectious Diseases Society of America (IDSA) established the Antimicrobial Availability Task Force (AATF), which prepeared a report entitled “BAD BUGS, NO DRUGS”.
The current particularly problematic MDR pathogens, as also identified by the AATF, are Acinetobacter baumannii, Pseudomonas aeruginosa and ESBLs producers. Unfortunately, owing to overuse and misue of antibiotic, a high percentage of A.baumannii and Pseudomonas has become resistant to most powerful weapons like carbapenems, cephalosporins and aminoglycosides.

The most prevalent mechanism of resistance exhibited by gram negative bacteria is production of the beta-lactamse enzyme that renders most beta-lactam antibiotics ineffective by distrubing their chemical structure.
To overcome this problem, the use of beta-lactamase inhibitors (clavulanate, sulbactam, tazobactam) is the most successful strategy to restore the efficacy of beta-lactam antibiotic.

Actzone-S is a combination of cefoperazone 500 mg (beta-lactam antibiotic) plus sulbactam 500 mg (beta-lactamase inhibitor).
Because of the broad spectrum of activity of sulbactam/cefoperazone, most infections can be treated adequately with this antibiotic alone. However sulbactam/cefoperazone may be used concomitantly with other antibiotics if such combinations are indicated. If an aminoglycoside is used, renal function should be monitored during the course of therapy.
The usual adult dose is 3 to 6 grams/day; however in severe infections it can be given uptil 12 grams/day. In case of renal impairment, dose of sulbactam should needs to be adjusted depending upon the creatinine clearance.

INDICATIONS

Mono-therapy

Actzone-S is indicated for the treatment of the following infections when caused by susceptible organisms: Respiratory Tract Infections (Upper and Lower) Urinary Tract Infections (Upper and Lower) Peritonitis, Cholecystitis, Cholangitis, and Other Intra-Abdominal Infections Septicemia.

i.) Meningitis

ii.) Skin and Soft Tissue Infections

iii.) Bone and Joint Infections

iv.) Pelvic Inflammatory Disease, Endometritis, Gonorrhea, and Other Infections of the Genital Tract

Combination Therapy

Because of the broad spectrum of activity of sulbactam/cefoperazone, most infections can be treated adequately with this antibiotic alone. However sulbactam/cefoperazone may be used concomitantly with other antibiotics if such combinations are indicated. If an aminoglycoside is used, renal function should be monitored during the course of therapy.

DOSAGE AND ADMINISTRATION

Actzone-S is administered intravenously.

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.

Use in Neonates:

For neonates in the first week of life, the drug should be given every 12 hours. The maximum daily dosage of sulbactam in paediatrics should not exceed 80 mg/kg/day. If more than 80 mg/kg/day of cefoperazone activity are necessary, additional cefoperazone should be administered separately.