Sulbactam sodium 500mg and Cefoperazone sodium 500mg
Injection, dry powder for reconstitution
Antibiotic; Cefoperazone, a third generation Cephalosporin / Sulbactam, a beta-lactamase inhibitor
What is the medicine prescribed for?
Sulbactam/Cefoperazone 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
- Skin and Soft Tissue Infections
- Bone and Joint Infections
- Pelvic Inflammatory Disease, Endometritis, Gonorrhea, and Other Infections of the Genital Tract
Because of the broad spectrum of activity of sulbactam/cefoperazone, most infections can be treated adequately with there 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.
Medicines are sometimes prescribed for purposes other than those listed above. Use only for the condition for which it was prescribed. Do not give this medicine to other people even if they have the same symptoms you have, as it may not be right for them.
How to take medication?
The suitable dosage for each patient should be prescribed by a doctor.
Method of Administration:
For intermittent infusion, should be reconstituted with the appropriate amount of Dextrose 5% in Water, NaCl 0.9% Injection or Sterile Water for Injection and then diluted to 20 mL with the same solution followed by administration over 15-60 min.
For IV injection, each vial should be reconstituted as mentioned previously and administered over a minimum of 3 min.
Lactated Ringer’s Solution: Initial reconstitution with Lactated Ringer’s Solution should be avoided since this mixture has been shown to be incompatible. However, a 2-step dilution process involving initial reconstitution in water for injection will result in a compatible mixture when further diluted with Lactated Ringer’s Solution
IM: Dextrose 5% in Water, NaCl 0.9% Injection or Sterile Water for Injection should be used for reconstitution.
Lidocaine HCl 2% is a suitable vehicle for IM administration, however, not for initial reconstitution (see Incompatibilities).
A reaction characterized by flushing, sweating, headache and tachycardia has been reported when alcohol was ingested during and as late as the 5th day after cefoperazone administration.
A similar reaction has been reported with certain other cephalosporins and patients should be cautioned concerning ingestion of alcoholic beverages in conjunction with administration of SBT/CPZ.
For patients requiring artificial feeding orally or parenterally, solutions containing ethanol should be avoided.
Salbactam sodium; contains sodium 92mg (4mEq)/g. Cefoperazone sodium; contains sodium 34mg (1.5 mEq)/g.
Adults: 2-4 g/day IV/IM in divided doses 12 hourly up to a max daily dose of 8 g (equivalent to 4 g cefperazone).
The recommended maximum daily dose of sulbactam is 4g.
Children: 40-80 mg/kg/day, every 6-12 hrs in divided dose. In serious infection may be increased up to 160 mg/kg/day.
Neonates: For neonates in the 1st week of life, Sulperazon should be given every 12 hrs. The maximum daily dosage of sulbactam in pediatrics should not exceed 80 mg/kg/day (160 mg/kg/day sulbactam/cefoperazone). In cases where doses >80 mg/kg/day of cefoperazone activity are necessary, additional cefoperazone should be administered separately.
How does it work?
The antibacterial component of sulbactam/cefoperazone (SBT/CPZ) is cefoperazone, a 3rd 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. However, biochemical studies with cell-free bacterial systems have shown it to be an irreversible inhibitor of most important β-lactamases produced by β-lactam antibiotic-resistant organisms.
The potential for sulbactam’s preventing the destruction of penicillins and cephalosporins by resistant organisms was confirmed in whole-organism studies using resistant strains in which sulbactam exhibited marked synergy with penicillins and cephalosporins. 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 sulbactam and cefoperazone is active against all organisms sensitive to cefoperazone. In addition, it demonstrates synergistic activity (up to 4-fold reduction in minimum inhibitory concentrations for the combination versus those for each component) in a variety of organisms, most markedly the following: Haemophilus influenzae, Bacteroides sp and Staphylococcus sp, Acinetobacter calcoaceticus, Enterobacter aerogenes, Escherichia coli, Proteus mirabilis, Klebsiella pneumoniae, Morganella morganii, Citrobacter freundii, Enterobacter cloacae, Citrobacter diversus.
Patients with known allergy to penicillins, sulbactam, cefoperazone or any of the cephalosporins.
This medicine should not be used if you are allergic to any of its ingredients. Please inform your doctor or pharmacist if you have previously experienced such an allergy.
If you feel you have experienced an allergic reaction, stop using this medicine and inform your doctor or pharmacist immediately.
Important safety information
As with other antibiotics, vitamin K deficiency has occurred in a few patients treated with cefoperazone. The mechanism is most probably related to the suppression of gut flora which normally synthesize this vitamin. Those at risk include patients with poor diet, malabsorption states (eg, cystic fibrosis) and patients on prolonged IV alimentation regimens. Prothrombin time should be monitored in these patients, and patients receiving anticoagulant therapy, and exogenous vitamin K administered as indicated.
As with other antibiotics, overgrowth of nonsusceptible organisms may occur during prolonged use of sulbactam/cefoperazone. Patients should be observed carefully during treatment. As with any potent systemic agent, it is advisable to check periodically for organ system dysfunction during extended therapy; this includes renal, hepatic and hematopoietic systems. This is particularly important in neonates, especially when premature, and other infants.
Clostridium difficile-associated diarrhea (CDAD) has been reported with use of nearly all antibacterial agents, including sulbactam sodium/cefoperazone sodium, and may range in severity from mild diarrhea to fatal colitis. Treatment with antibacterial agents alters the normal flora of the colon leading to overgrowth of C. difficile.
Clostridium difficile produces toxins A and B which contribute to the development of CDAD. Hypertoxin producing strains of C. difficile cause increased morbidity and mortality, as these infections can be refractory to antimicrobial therapy and may require colectomy. CDAD must be considered in all patients who present with diarrhea following antibiotic use. Careful medical history is necessary since CDAD has been reported to occur over 2 months after the administration of antibacterial agents.
Hypersensitivity: Serious and occasionally fatal hypersensitivity (anaphylactic) reactions have been reported in patients receiving β-lactam or cephalosporin therapy. These reactions are more apt to occur in individuals with a history of hypersensitivity reactions to multiple allergens. If an allergic reaction occurs, Sulperazon should be discontinued and the appropriate therapy instituted.
Serious anaphylactic reactions require immediate emergency treatment with epinephrine. Oxygen, IV steroids and airway management, including intubation, should be administered as indicated.
Hepatic Dysfunction: Cefoperazone is extensively excreted in bile. The serum half-life of cefoperazone is usually prolonged and urinary excretion of the drug increased in patients with hepatic diseases and/or biliary obstruction. Even with severe hepatic dysfunction, therapeutic concentrations of cefoperazone are obtained in bile and only a 2- to 4-fold increase in half-life is seen.
Dose modification may be necessary in cases of severe biliary obstruction, severe hepatic disease or in cases of renal dysfunction coexistent with either of those conditions.
In patients with hepatic dysfunction and concomitant renal impairment, cefoperazone serum concentrations should be monitored and dosage adjusted as necessary. In these cases, dosage should not exceed 2 g/day of cefoperazone without close monitoring of serum concentrations.
Effects on the Ability to Drive or Operate Machinery: Clinical experience with sulbactam/cefoperazone indicates that it is unlikely to impair a patient’s ability to drive or use machinery.
Use in pregnancy: Reproduction studies have been performed in rats at doses up to 10 times the human dose and have revealed no evidence of impaired fertility and no teratological findings. Sulbactam and cefoperazone cross the placental barrier. There are, however, no adequate and well-controlled studies in pregnant women. Because animal reproduction studies are not always predictive of human response, Sulperazon should be used during pregnancy only if clearly needed.
Use in lactation: Only small quantities of sulbactam and cefoperazone are excreted in human milk. Although both drugs pass poorly into breast milk of nursing mothers, caution should be exercised when sulbactam/cefoperazone is administered to a nursing mother.
Use in children: Sulbactam/cefoperazone has been effectively used in infants. It has not been extensively studied in premature infants or neonates. Therefore, in treating premature infants and neonates, potential benefits and possible risks involved should be considered before instituting therapy (see Toxicology: Preclinical Safety Data under Actions).
Cefoperazone does not displace bilirubin from plasma protein-binding sites.
If you miss a dose
Take it as soon as you remember. If it is almost time for your next dose, skip the one you missed and go back to your regular schedule. Do not take 2 doses at the same time.
Pregnancy and breastfeeding
Certain medicines should not be used during pregnancy or breastfeeding. However, other medicines may be safely used in pregnancy or breastfeeding providing the benefits to the mother outweigh the risks to the unborn baby. Always inform your doctor if you are pregnant or planning a pregnancy, before using any medicine.
Reproduction studies have been performed in rats at doses up to 10 times the human dose and have revealed no evidence of impaired fertility and no teratological findings. Sulbactam and cefoperazone crosses the placental barrier. There are, however, no adequate and well-controlled studies in pregnant women. Because animal reproduction studies are not always predictive of human response, Sulperazone should be used during pregnancy only if clearly needed.
Only small quantities of sulbactam and cefoperazone are excreted in human milk.
Although both drugs pass poorly into the breast milk of nursing mothers, caution should be exercised when SBT/CPZ is administered to a nursing mother.Occasionally, disruption of the infant’s gastrointestinal flora, resulting in diarrhea or thrush, has been reported with penicillins, but these effects have not been adequately evaluated.
Possible side effects
Medicines and their possible side effects can affect individual people in different ways. The following are some of the side effects that are known to be associated with this medicine. Just because a side effect is stated here, it does not mean that all people using this medicine will experience that or any side effect.
Side effects may include:
Very common (≥10%)
Frequency not defined.
Cefoperazone contains an N-methylthiotetrazole (NMTT or 1-MTT) side chain. As the antibiotic is broken down in the body, it releases free NMTT, which can cause hypoprothrombinemia (likely due to inhibition of the enzyme vitamin K epoxide reductase) and a reaction with ethanol similar to that produced by disulfiram (Antabuse), due to inhibition of aldehyde dehydrogenase.
Anaphylactoid reactions (including shock), diarrhea, nausea & vomiting, pseudomembranous colitis. Maculopapular rash, urticaria, pruritus, Stevens Johnson syndrome. Headache, hypotension, leucopenia, hematuria & vasculitis.
Serious ADR (<1%)
Frequency not defined.
Hypersensitivity: Maculopapular rash, Urticaria, Pruritis, Anaphylaxis/angioedema, eosinophilia
Hematologic: Hypoprothrombinemia, Neutropenia, Leukopenia, Thrombocytopenia
GI: Diarrhea, C. difficile disease
Renal: Interstitial nephritis
The side effects listed above may not include all of the side effects reported by the medicine’s manufacturer.
For more information about any other possible risks associated with this medicine, please read the information provided with the medicine or consult your doctor or pharmacist.
Get emergency medical help if you have any of these signs of an allergic reaction: skin rash or hives; difficulty breathing; swelling of your face, lips, tongue, or throat.
Interaction with other medication
It is important to tell your doctor or pharmacist what medicines you are already taking, including those bought without a prescription and herbal medicines, before you start treatment with this medicine. Similarly, check with your doctor or pharmacist before taking any new medicines while having treatment with this one, to ensure that the combination is safe.
Store at temperatures not exceeding 25°C. Protect from light.
This information is a merely a general guideline and is not a substitute for a consultation with your doctor. If you have questions about the medicine you are taking or would like more information, check with your doctor, pharmacist, or other health care provider.