APR SUPERAZONE

Cefoperazone 1000mg and Sulbactam 500mg Injection

Read all of this information carefully before you start taking this medicine because it contains important information for you.

Keep this information. You may need to read it again.
If you have any further questions, ask your doctor, pharmacist or nurse.
This medicine is prescribed for you only. Do not pass it on to others. It may harm them, even if their signs of illness are the same as yours.
If you get any side effects, talk to your doctor, pharmacist or nurse. This includes any possible side effects not listed in this information.

COMPOSITION:
Each vial contains:

Cefoperazone – 1000mg
Sulbactam – 500mg

For intravenous use only.

1. DESCRIPTION:

Cefoperazone is an antibacterial that is highly useful in treating bacterial infections. It belongs to a class of drugs known as cephalosporins.

Sulbactam is a beta lactamase inhibitor and prevents the degradation of cefoperazone by bacterial enzymes.

1. PHARMACOLOGICAL ACTION:

The antibacterial component of sulbactam/cefoperazone is cefoperazone, a 3rd generation cephalosporin which acts against sensitive organisms during the stage of active multiplication by inhibiting the biosynthesis of cell wall mucopeptide. Sulbactam does not possess any useful antibacterial activity except against Neisseriaceae & Acinetobacter. Biochemical studies with cell-free bacterial synthesis have shown it to be an irreversible inhibitor of most important beta-lactamases produced by beta-lactam antibiotic-resistant organisms.

1. CLINICAL PHARMACOKINETICS:

Approx. 84% of the sulbactam dose & 25% of the cefoperazone dose administered as sulbactam/cefoperazone is excreted by the kidneys. Most of the remaining dose is excreted in the bile. After administration the mean half-life for sulbactam is about 1 hour while that for cefoperazone is 1.7 hours. Serum concentrations have been shown to be proportional to the dose administered.  Mean peak sulbactam & cefoperazone concentrations after the administration of 2g of sulbactam/cefoperazone (1 g sulbactam, 1 g of cefoperazone) IV over 5 minutes were 130.2 & 236.8 mcg/mL. This reflects the larger volume of distribution for sulbactam (Vd = 18.0-27.6 L) compared to cefoperazone (Vd = 10.2-11.3 L). After IM administration of 1.5g cefoperazone/sulbactam peak serum concentrations of sulbactam & cefoperazone are seen from 15 minutes-2 hours. Mean peak serum concentrations were 19.0-64.2 mcg /mL for sulbactam & cefoperazone. Both sulbactam & cefoperazone distribute well into a variety of tissues & fluids including the bile, gall bladder, skin, appendix, fallopian tubes, ovary, uterus & others. There is no evidence of any pharmacokinetic drug interaction between sulbactam & cefoperazone when administered together in the form of sulbactam/cefoperazone. After multiple dosing no significant changes in the pharmacokinetics of either component of sulbactam/cefoperazone have been reported & no accumulation has been observed when administered every 8-12 hours.

1. INDICATIONS:

Cefoperazone and sulbactam injection is indicated for:
– Respiratory tract infections (upper & lower)
– Urinary tract infections (upper & lower)
– Peritonitis, cholecystitis, cholangitis & other intra-abdominal infections
– Septicaemia
– Meningitis
– Skin & soft tissue infections
– Bone & joint infections

– Pelvic inflammatory disease, endometritis, gonorrhoea & other infections of the genital tract

1. CONTRAINDICATIONS:

Cefoperazone and sulbactam injection is contraindicated in the following cases:

• Hypersensitivity to the active substance or to any of its excipients.

1. WARNINGS AND PRECAUTIONS:

Serious hypersensitivity (anaphylactic) reactions have been reported in patients receiving beta-lactam or cephalosporin therapy.

Serious anaphylactic reactions require immediate emergency treatment with epinephrine. Oxygen, IV steroids & airway management including intubation should be administered as indicated.

Vitamin K deficiency has occurred in a few patients treated with cefoperazone.

Overgrowth of non-susceptible organisms may occur during the prolonged use of sulbactam/cefoperazone. Patients should be observed carefully during the treatment.

Clostridium difficile associated diarrhoea has been reported and may range in severity from mild diarrhoea to fatal colitis.

Has been effectively used in infants. It has not been extensively studied in premature infants/neonates. In treating premature infants & neonates the potential benefits & possible risks involved should be considered before instituting therapy.

Does not displace bilirubin from plasma protein binding sites

1. ADVERSE EFFECTS:

Common side effects include:

• Diarrhoea
• Hypersensitivity reactions
• Slight decrease in neutrophils
• Eadache/fever
• Pain at injection site
• Transient elevation in liver enzymes

1. DRUG INTERACTIONS:

Aminoglycosides: Solutions of sulbactam/cefoperazone & aminoglycosides should not be directly mixed since there is a physical incompatibility between them. If combination therapy with sulbactam/cefoperazone & an aminoglycoside is contemplated this can be accomplished by sequential intermittent IV infusion provided that a separate secondary IV tubing is used & that the primary IV tubing is adequately irrigated with an approved diluent between doses.

Lactated ringers solution: Initial reconstitution with Lactated Ringer’s Solution should be avoided since this mixture has been shown to be incompatible.

Lidocaine: Initial reconstitution with 2% lidocaine HCl solution should be avoided since this mixture has been shown to be incompatible.

1. DOSAGE:

The usual dose is 6gm of cefoperazone administered in equally divided doses every 12 hours.

1. ADMINISTRATION:

For Intravenous injection.
Administration to be done by a registered medical practitioner/nurse in a proper sterile & hospital setting only.

1. PRESENTATION:
2. STORAGE:

Store below 25°C in a cool & dry pace. Protect from direct sunlight. Keep away from the reach of children.

1. MANUFACTURED BY:
2. MARKETED BY:

This information was last revised on May 2019.