Sulperazone, powder 2 g

Sulperazone is a combination drug with antibacterial effect.

Cefoperazone – cephalosporin antibiotic of III generation, acts bactericidal, has a broad spectrum of action; highly active against aerobic and anaerobic Gram-positive and Gram-negative microorganisms (including Pseudomonas aeruginosa), resistant to beta-lactamases of Gram-positive and Gram-negative microorganisms.

Sulbactam is an irreversible inhibitor of beta-lactamases that are released by microorganisms resistant to beta-lactam antibiotics; prevents degradation of penicillins and cephalosporins under the action of beta-lactamases of resistant microorganisms; binds to penicillin-binding proteins and shows synergism when used simultaneously with penicillins and cephalosporins.

The combination of sulbactam and cefoperazone is active against all microorganisms sensitive to cefoperazone and acts synergistically (reduces up to 4 times the MAC of the combination compared to the values for each component separately) against microorganisms: Haemophilus influenzae, Bacteroides spp, Staphylococcus spp., Acinetobacter calcoaceticus, Enterobacter aerogenes, Escherichia coli, Proteus mirabilis, Klebsiella pneumoniae, Morganella morganii, Citrobacter freundii, Enterobacter cloacae, Citrobacter diversus. Active in vitro against a wide range of microorganisms: Gram-positive bacteria – Staphylococcus aureus (incl. strains that form and do not form penicillinase), Staphylococcus epidermidis, Streptococcus pneumoniae, Streptococcus pyogenes (beta-hemolytic strain of group A), Streptococcus agalactiae (beta-hemolytic strain of group B), most strains of beta-hemolytic Streptococcus spp, Enterococcus faecalis; Gram-negative bacteria – Escherichia coli, Klebsiella spp., Enterobacter spp., Citrobacter spp., Haemophilus influenzae, Proteus mirabilis, Morganella morganii, Providencia rettgeri, Providencia spp., Serratia spp. (including Serratia marcescens), Salmonella spp., Shigella spp, Pseudomonas aeruginosa, Acinetobacter calcoaceticus, Neisseria gonorrhoeae, Neisseria meningitidis; Bordetella pertussis, Yersinia enterocolitica; anaerobic bacteria – Bacteroides fragilis, Fusobacterium spp, Peptococcus spp., Peptostreptococcus spp., Veillonella spp., Clostridium spp., Eubacter spp., Lactobacillus spp.

Indications

Infectious and inflammatory diseases caused by microorganisms sensitive to the drug:

Active ingredient

Composition

1 vial of powder for preparation of solution for injection contains:

acting substances:

sulbactam 1 g,

cefoperazone 1 g, in a ratio of 1:1

How to take, the dosage

In adults, Sulperazone is recommended in the following daily doses.

Sulbactam/cefoperazone ratioSulperazone (g)Sulbactam (g)Cefoperazone (g)1:12-41-21-2

The daily dose should be divided in equal parts and administered every 12 hours.

In severe or refractory infections, the daily dose of Sulperazone may be increased to 8 g with a 1:1 component ratio (i.e., 4 g of cefoperazone). Patients receiving Sulperazone in a 1:1 ratio may require additional administration of cefoperazone. The dose should be divided in equal parts and administered every 12 hours.

The recommended maximum daily dose of sulbactam is 4 g.

In children, Sulperazone is recommended in the following daily doses.

Sulbactam/cefoperazone ratioSulperazone (mg/kg/day)Sulbactam (mg/kg/day)Cefoperazone (mg/kg/day)1:140-8020-4020-40-40

The dose should be divided in equal parts and given every 6-12 hours.

In serious or refractory infections, doses may be increased to 160 mg/kg/day at a 1:1 component ratio. The daily dose is divided into 2 to 4 equal parts.

In newborns during the first week of life, the drug should be administered every 12 hours. The maximum daily dose of sulbactam in children should not exceed 80 mg/kg/day.

In patients with severe renal dysfunction (CKR 15-30 ml/minute), the maximum dose of sulbactam is 1 g every 12 hours (maximum daily dose of sulbactam is 2 g), and in patients with CKR less than 15 ml/minute the maximum dose of sulbactam is 500 mg every 12 hours (maximum daily dose of sulbactam is 1 g). In severe infections, additional administration of cefoperazone may be required. Since in hemodialysis pharmacokinetics of sulbactam is significantly changed and T1/2 of cefoperazone from serum is slightly reduced, the administration of Sulperazone should be planned after dialysis.

If regular monitoring of the serum concentration of cefoperazone is not performed, the minimum daily dose should not exceed 2 g.

Interaction

Disulfiram-like effects characterized by hot flashes, sweating, headache and tachycardia have been reported when using alcohol during treatment with cefoperazone and for up to 5 days after its administration. Similar reactions have been reported with some other cephalosporins, so patients should be warned about the possibility of their occurrence when drinking alcoholic beverages during Sulperazone treatment. In patients who require artificial nutrition (oral or parenteral) the use of solutions containing ethanol should be avoided.

Pharmaceutical interactions

Sulperazone and aminoglycosides solutions should not be directly mixed given the pharmaceutical incompatibility between them. If combined therapy with Sulperazone and aminoglycosides is given, the two drugs are administered by sequential infusions using separate secondary catheters, and the primary catheter is flushed sufficiently well with solution between drug doses. The intervals between the administration of Sulperazone and aminoglycoside during the day should be as long as possible.

Special Instructions

In patients treated with beta-lactam antibiotics, including cephalosporins, cases of serious hypersensitivity reactions (anaphylactic reactions) have been described, sometimes leading to death. The risk of such reactions is higher in patients with a history of hypersensitivity reactions. In case of allergic reactions it is necessary to discontinue the drug and administer adequate therapy.

In case of severe anaphylactic reactions it is necessary to administer epinephrine (adrenaline) urgently. GCS is administered intravenously and the airway is secured, including intubation.

In severe biliary obstruction, severe liver disease, and renal dysfunction combined with any of the above conditions, correction of the drug dosing regimen may be required.

In patients with hepatic impairment and concomitant renal impairment, the serum concentration of cefoperazone should be monitored and the dose adjusted if necessary. If regular monitoring of the serum concentration of cefoperazone is not performed in such cases, the daily dose should not exceed 2 g.

In treatment with cefoperazone, as with other antibiotics, vitamin K deficiency has rarely developed. It is probably caused by suppression of normal intestinal microflora that synthesizes this vitamin. Patients with malnutrition, malabsorption (e.g., cystic fibrosis) and long-term IV artificial nutrition can be included in the risk group. In these cases, as well as in patients receiving anticoagulants, prothrombin time should be monitored and vitamin K should be prescribed if indicated.

In prolonged treatment with Sulperazone (as well as other antibiotics) an overgrowth of insensitive microorganisms may be observed. Patients should be monitored closely during treatment.

In long-term therapy with Sulperazone, it is recommended that the function of internal organs, including the kidneys, liver, and hematopoietic system, be monitored periodically. This is especially important for newborns, especially premature infants and young children.

Contraindications

Allergy to penicillins, sulbactam, cefoperazone or any other cephalosporins.

Side effects

Allergic reactions: anaphylactic shock.

Digestive system disorders: diarrhea, nausea, vomiting, pseudomembranous colitis; transient increase of liver function parameters – AST, ALT, ALF, serum bilirubin.

Allergic reactions: maculopapular rash, pruritus, urticaria, Stevens-Johnson syndrome (the risk of these reactions is higher in patients with a history of allergic reactions).

Hematopoietic system disorders: decrease of neutrophil number, reversible neutropenia (during long-term treatment), decrease of hemoglobin and hematocrit level, transient eosinophilia, leukopenia, thrombocytopenia, hypoprotrombinemia; in single cases – positive Coombs’ test. False-positive reactions to glucose in the urine may be observed when using Benedict’s or Fehling’s solution.

Urinary system disorders: hematuria.

Local reactions: Sulperazone is well tolerated when administered in utero. Sometimes after I/m injection, transient pain and burning at the injection site are observed. When Sulperazone is injected intravenously with a catheter, phlebitis may develop at the site of infusion.

Others: headache, fever, chills, vasculitis.

Overdose

There is limited information on acute toxicity of cefoperazone sodium and sulbactam sodium in humans.

Symptoms: in case of overdose, adverse effects reported with the use of the drug can be expected. The fact that high concentrations of beta-lactam antibiotics in cerebrospinal fluid may lead to neurological disorders, including seizures, should be considered.

Treatment: symptomatic, hemodialysis is effective, especially in patients with impaired renal function.

Pregnancy use

Sulbactam and cefoperazone penetrate the placental barrier.

The use of Sulperazone in pregnancy and lactation is possible only if the estimated benefit to the mother exceeds the potential risk to the fetus or child.

Similarities