SULZONTSEF
Active material: Cefoperazone, Sulbactam
When ATH: J01DD62
CCF: III generation cephalosporin with beta-lactamase inhibitor
ICD-10 codes (testimony): A39, A40, A41, A54, G00, H66, I88, I89.1, J01, J02, J03, J04, J15, J20, J31, J32, J35.0, J37, J42, J85, J86, K65.0, K81.0, K81.1, K83.0, L01, L02, L03, L08.0, M00, M86, N10, N11, N30, N34, N41, N70, N71, N72, N73.0, Z29.2
When CSF: 06.02.03.01
Manufacturer: Synthesis of (Russia)
Pharmaceutical form, composition and packaging
Powder for solution for I / O, and the / m white or white with a yellowish tint.
| 1 fl. | |
| cefoperazone (sodium salt) | 1 g |
| sulbactam (sodium salt) | 1 g |
Vials 20 ml (1) – packs cardboard.
Vials 20 ml (5) – packs cardboard.
Vials 20 ml (5) – packings Valium planimetric (1) – packs cardboard.
Vials 20 ml (5) – packings Valium planimetric (2) – packs cardboard.
Vials 20 ml (10) – packs cardboard.
Vials 20 ml (50) – packs cardboard.
Pharmacological action
III generation cephalosporin with beta-lactamase inhibitor. Effective bactericidal, It has a broad spectrum of activity. Highly active against aerobic and anaerobic Gram-positive and Gram-negative microorganisms (incl. Pseudomonas aeruginosa), resistant to β-lactamases Gram positive and Gram negative microorganisms.
Sulbactam – irreversible inhibitor of β-lactamase, are released by microorganisms, resistant to beta-lactam antibiotics. It prevents the destruction of penicillins and cephalosporins by the action of β-lactamase resistant organisms. By binding to penicillin binding proteins, shows synergy while the use of penicillins and cephalosporins.
Combination sulybaktama and cefoperazone active against all microorganisms, sensitive to cefoperazone, and acts synergistically (reduces to 4 times the minimum inhibitory concentration (IGC) combination compared with the values for each component separately) against the following microorganisms: Haemophilus influenzae, Bacteroides spp., Staphylococcus spp., Acinetobacter calcoaceticus, Enterobacter aerogenes, Escherichia coli, Proteus is wonderful, Klebsiella pneumoniae, Morganella morganii, Citrobacter freundii, Citrobacter different, Enterobacter cloacae.
Sulzontsef® in vitro active against gram-positive aerobic bacteria: Staphylococcus aureus (incl. strains, forming and not forming penicillinase), Staphylococcus epidermidis, Streptococcus pneumoniae, Streptococcus pyogenes (beta-hemolytic strains of group A), Streptococcus agalactiae (beta-hemolytic group B strain), most strains of beta-hemolytic Streptococcus spp., Enterococcus faecalis; Gram-negative aerobic bacteria: Pseudomonas aeruginosa, Acinetobacter calcoaceticus, Escherichia coli, Klebsiella spp., Enterobacter spp., Citrobacter spp., Haemophilus influenzae, Proteus is wonderful, Morganella morganii, providencia spp. (incl. Rettgeri Providence), Serratia spp. (including Serratia marcescens), Salmonella spp., Shigella spp., Neisseria gonorrhoeae, Neisseria meningitidis, Bordetella pertussis, Yersinia enterocolitica; Anaerobic bacteria: Bacteroides fragilis, Clostridium spp., Fusobacterium spp., Peptococcus spp., Peptostreptococcus spp., Veillonella spp., Eubacterium spp., Lactobacillus spp.
To study the sensitivity is recommended to use discs, containing 30 g and sulbactam 75 g cefoperazone (Kirby-Bauer method).
Pharmacokinetics
Distribution
Cmax sulbactam and cefoperazone after the on / in the drug dose 2 g (1 Mr. and sulbactam 1 g cefoperazone) during 5 min averaged 130.2 ug / ml 236.8 ug / ml, respectively. This reflects higher Vd sulbactam (from 8 l to 27.6 l) compared with that of cefoperazone (from 10.2 l to 11.3 l). The serum concentration is proportional to the administered dose.
As ceftazidime, and sulbactam, well distributed in various tissues and body fluids, including bile, gallbladder, skin, appendix, fallopian tube, ovary, uterus.
Data on the presence of a pharmacokinetic interaction between sulbactam and cefoperazone when administered no drug.
Repeated use of significant changes in the pharmacokinetics of the two components of the drug is not indicated. With the introduction of the drug every 8-12 h accumulation was observed.
Deduction
About 25% dose and cefoperazone 84% sulbactam dose excreted by the kidneys. The rest of the cefoperazone is derived mainly from the bile. T1/2 cefoperazone is 1.7 no, sulbactam – an average of about 1 no.
Pharmacokinetics in special clinical situations
Cefoperazone is actively excreted in the bile. T1/2 cefoperazone is usually lengthened, kidneys and excretion of the drug is increased in patients with liver disease and / or biliary obstruction. Even with severe hepatic impairment in bile achieved therapeutic concentrations of cefoperazone, a T1/2 increases only 2-4 times.
In patients with various renal function, receiving Sulzontsef®, found a high correlation between the total clearance from the body and sulbactam calculated creatinine clearance. In patients with terminal renal insufficiency showed a significant lengthening of T1/2 sulbactam (average 6.9 and h 9.7 hours in various studies).
Hemodialysis causes significant changes in T1/2, total clearance from the body and Vd sulbactam.
The pharmacokinetics of the drug has been studied in older people with kidney failure and liver dysfunction. Compared with healthy volunteers showed an increase in the duration T1/2, reduction in clearance and increase in Vd how cefoperazone, and sulbactam. The pharmacokinetics of sulbactam correlated with the degree of renal impairment, and pharmacokinetics cefoperazone – with the degree of liver dysfunction.
In studies in children were no significant changes in the pharmacokinetic parameters of the components of the drug as compared to those in adults. Average T1/2 sulbactam in children ranged from 0.91 h to 1.42 no, Cefoperazone – from 1.44 h to 1.88 no.
Testimony
- Intra-abdominal infections (peritonitis, cholecystitis, kholangit);
- Urinary tract infections (pyelonephritis, cystitis);
- Pelvic infection (prostatitis, endometritis, gonorrhea, vulvovaginitis);
- Infections of the upper and lower respiratory tract (pharyngitis, tonsillitis, sinusitis, bronchitis, pneumonia, bronchopneumonia, empyema, lung abscess);
- Infections of upper respiratory tract (acute otitis media, sinusitis, sore throat);
- Infections of the skin and soft tissues (furunculosis, abscess, pyoderma, lymphadenitis, limfangit);
- Osteomyelitis, infections of the joints;
- Sepsis;
- Meningitis.
Prevention of infectious complications after abdominal, gynecology and orthopedic surgery, in Cardiovascular Surgery.
Dosage regimen
The drug is prescribed in / (bolus or infusion) or / m.
The following are the total dose of cefoperazone and sulbactam (in relation to 1:1).
Adults appoint 2-4 g / day with an interval of 12 no; at heavy, persistently occurring infections – to 8 g / day. The maximum daily dose – 8 g product (4 g cefoperazone + 4 g sulbactam).
Patients with chronic renal failure (CC less than 30 ml / min) shall adjust the dose. At CC 15-30 ml / min the maximum dose of sulbactam 1 g 2 times / day, at CC less than 14 ml / min – 500 mg 2 times / day.
At liver and biliary obstruction the maximum daily dose – no more 2 g.
Babies the drug is prescribed on the basis of 40-80 mg / kg / day 2-4 introduction, newborns during the first week of life – in 2 introduction; at heavy, long flowing infections – to 160 mg / kg / day. The maximum daily dose Sulzontsefa® – 160 mg / kg / day. When the need for more 80 mg / kg / day, calculated by the activity of cefoperazone, increasing the dose is achieved by the introduction of additional cefoperazone. The maximum daily dose of sulbactam children – no more 80 mg / kg / day.
Terms of preparation and administration
For in / bolus contents of the vial is dissolved in an adequate amount 5% dextrose (Glucose), 0.9% sodium chloride solution, 5% dextrose (Glucose) in 0.225% sodium chloride solution, 5% dextrose (Glucose) in 0.9% sodium chloride solution or sterile water for injection, and is administered for 3 m.
For in / infusion administration dissolved, as indicated above. Then diluted to 20-100 ml and administered for 15-60 m.
For the / m to dissolve using sterile water for injection. Preparation of the solution is carried out using lidocaine in 2 Phase: first with sterile water for injection, then – 2% lidocaine to obtain 0.5% lidocaine. The total volume of solvent 6.7 ml.
Side effect
From the digestive system: diarrhea, nausea, vomiting, psevdomembranoznыy colitis, increase in liver transaminases and alkaline phosphatase, giperʙiliruʙinemija.
From the side of hematopoiesis: anemia, neutropenia, thrombocytopenia, bleeding (vitamin K deficiency).
Laboratory findings: giperkreatininemiя, gipoprotrombinemii.
Allergic reactions: hives, maculo-papular rash, fever, eozinofilija; rarely – anaphylactic shock.
Local reactions: at / in the introduction – phlebitis; when i / m administration – tenderness at the injection site.
Contraindications
- Lactation;
- Hypersensitivity to the drug, incl. other beta-lactam antibiotics.
FROM caution should be prescribed in patients with renal and / or hepatic insufficiency, cars (incl. history), preterm infants, pregnancy.
Pregnancy and lactation
Use of the drug during pregnancy and lactation is carried out if, if the potential benefit outweighs the potential risk.
Cautions
Given the broad spectrum of activity, drug can be used as monotherapy.
With the simultaneous use of aminoglycoside antibiotics is necessary to monitor renal function.
In patients with liver disease and / or biliary tract obstruction T1/2 cefoperazone increases, increased excretion by the kidneys. When severe liver cefoperazone concentration in bile is therapeutic, T1/2 increases 2-4 times. Changing the dosage and concentration control cefoperazone serum is required in severe biliary obstruction, severe hepatic insufficiency (in these cases, the maximum daily dose – 2 g).
The risk of developing vitamin K deficiency susceptible patients, adhering to a diet deficient or have malabsorption of food (Patients with cystic fibrosis; Patients, It is for a long time on parenteral nutrition). These patients should be monitored prothrombin time; if necessary administered vitamin K. The mechanism of vitamin K deficiency is the suppression of intestinal microflora, which normally synthesize this vitamin.
Prolonged treatment is necessary to monitor renal function, hepatic, and hematopoietic systems.
During therapy may experience false-positive results of the determination of glucose in urine using Benedict's or Fehling's solutions, false positive Coombs' test.
Treatment of premature infants is carried out if, if the potential benefit outweighs the potential risk.
Overdose
Symptoms: neurological disorders, including seizures.
Treatment: symptomatic therapy (incl. sedation). Hemodialysis is effective.
Drug Interactions
The use of ethanol (simultaneously or during the subsequent 5 Days after treatment) It increases the risk of reaction disulfiramopodobnyh (tides, increased perspiration, headache, tachycardia).
Pharmaceutical interaction
The product is compatible with water for injection, 5% dextrose (Glucose), 0.9% sodium chloride solution, 5% dextrose (Glucose) in 0.225% sodium chloride solution, 5% dextrose (Glucose) in 0.9% sodium chloride solution.
The drug is not compatible with Ringer, 2% lidocaine hydrochloride (initial use of the water for injection leads to the formation of a compatible blend), aminoglikozidami (if you need combination therapy, it is performed by a sequence of fractional / infusion two drugs, Using 2 in separate systems / transfusion; in the interval between dosing system must be flushed with a compatible solvent).
Conditions of supply of pharmacies
The drug is released under the prescription.
Conditions and terms
List B. The drug should be stored in a dry, protected from light, reach of children, at a temperature no higher than 25 ° C. Shelf life – 2 year.
