Sulcef, 1 g+1 g 2.18g

Pharmacotherapeutic group : Antibiotic, cephalosporin + beta-lactamase inhibitor.

ATX: J.01.D.D.62

Pharmacodynamics :

Cefoperazone is a third generation cephalosporin that acts on sensitive microorganisms during their active multiplication by inhibiting the biosynthesis of cell wall mucopeptide. Sulbactam has no clinically significant antibacterial activity (except for Neisseriaceae and Acinetobacter) and is an irreversible inhibitor of most major beta-lactamases produced by microorganisms that are resistant to beta-lactam antibiotics. Sulbactam also binds to some penicillin-binding proteins, so the combination of cefoperazone and sulbactam often has a more pronounced effect on sensitive strains than cefoperazone alone
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The combination of sulbactam and cefoperazone is active against all microorganisms sensitive to cefoperazone. In addition, it is synergistic against various microorganisms, primarily: Haemophilus influenzae, Bacteroides spp., Staphylococcus spp., Acinetobacter calcoaceticus, Enterobacter aerogenes, Escherichia coli, Proteus mirabilis, Klebsiella pneumoniae, Morganella morganii, Citrobacter freundii, Enterobacter cloacae, Citrobacter ersus.

It is active in vitro against a wide range of clinically relevant microorganisms.

Gram-positive microorganisms:

Staphylococcus aureus (producing and not producing penicillinase), Staphylococcus epidermidis, Streptococcus pneumoniae, Streptococcus pyogenes (group A beta-hemolytic streptococcus), Streptococcus agalactiae (group B beta-hemolytic streptococcus), most other strains of beta-hemolytic streptococci, Streptococcus faecalis.

Gram-negative microorganisms:

Klebsiella spp., Enterobacter spp., Citrobacter spp., Proteus vulgaris, Providencia rettgeri, Providencia spp., Serratia spp. (including S. marcescens), Salmonella spp, Shigella spp., Pseudomonas aeruginosa, Neisseria gonorrhoeae, Neisseria meningitidis-, Bordetella pertussis, Yersinia enterocolitica.

Anaerobic microorganisms s Bacteroides fragilis, Fusobacterium spp., Peptococcus spp., Peptostreptococcus spp., Veillonella spp., Clostridium spp., Eubacterium spp., Lactobacillus spp.

Pharmacokinetics:

Cefoperazone and sulbactam are well distributed in various tissues and fluids, including
bile, gallbladder, skin, appendix, fallopian tubes, ovaries, uterus, etc. Maximum concentrations of cefoperazone and sulbactam after intravenous administration of 2 g of the drug for 5 min averaged 130.2 and 236.8 mcg/ml, respectively. The volume of distribution of sulbactam ranged from 18.0 to 27.6 L, cefoperazone from 10.2 to 11.3 L. About 84% of the dose of sulbactam and 25% of the dose of cefoperazone are excreted by the kidneys. The remaining part of cefoperazone is excreted mainly in bile. Half-life of cefoperazone is on average about 1.7 h, sulbactam – 1 h. Serum concentration of cefoperazone and sulbactam is proportional to the administered dose. Pharmacokinetic properties of the drug do not change when repeated administration. No cumulation is observed when the drug is administered every 8-12 hours.

Pharmacokinetics in hepatic dysfunction:

Cefoperazone is actively excreted with bile. Half-life of cefoperazone is usually prolonged and renal excretion of the drug is increased in patients with liver disease and/or biliary obstruction. Even with severe hepatic impairment, therapeutic concentration of cefoperazone is achieved in bile, and the half-life is increased by 2-4 times.

Pharmacokinetics in renal dysfunction:

In patients with various degrees of renal dysfunction receiving the drug, a high correlation between the total clearance of sulbactam from the body and estimated creatinine clearance has been found. In patients with terminal renal failure a significant prolongation of sulbactam elimination half-life was found (on average 6.9-9.7 hours in various studies). Hemodialysis causes significant changes in the elimination half-life, total clearance from the body and the volume of sulbactam distribution.

Pharmacokinetics in the elderly:

In the elderly with renal impairment and impaired liver function, there is an increase in the half-life, decrease in clearance and increased volume of distribution of both sulbactam and cefoperazone. Pharmacokinetics of sulbactam correlates with the degree of impaired renal function, and pharmacokinetics of cefoperazone with the degree of hepatic function.

Pharmacokinetics in children:

In children there are no significant differences in the pharmacokinetics of the drug components compared to adults. The average half-life of sulbactam in children is from 0.91 to 1.42 h, cefoperazone from 1.44 to 1.88 h.

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Indications

Active ingredient

Composition

How to take, the dosage

Interaction

Special Instructions

Contraindications

Side effects

Cardiovascular system: decreased blood pressure.

Gastrointestinal tract: diarrhea, nausea, vomiting, pseudomembranous colitis.

Allergic reactions: maculopapular rash, urticaria, pruritus, Stevens-Johnson syndrome, anaphylactic shock. The risk of reactions is higher in patients with a history of allergic reactions.

Hematopoietic system: decrease in the number of neutrophils. With long-term treatment reversible neutropenia develops, decrease of hemoglobin and hematocrit, transient eosinophilia, leukopenia, thrombocytopenia as well as hypoprothrombinemia, hypercreatininemia, anemia, bleeding are noted.

Laboratory parameters: increased activity of “liver” transaminases – aspartate aminotransferase (ACT), alanine aminotransferase (AJ1T), alkaline phosphatase, serum bilirubin, hematuria. False positive Coombs test was observed in some patients during treatment.

Local reactions: after intramuscular injection transient pain is possible. When administering the drug intravenously using a catheter, phlebitis may develop at the site of infusion.

Others: headache, fever, chills, vasculitis.

Overdose

Pregnancy use