Sulperazon
Sulperazon: instructions for use and reviews
- 1. Release form and composition
- 2. Pharmacological properties
- 3. Indications for use
- 4. Contraindications
- 5. Method of application and dosage
- 6. Side effects
- 7. Overdose
- 8. Special instructions
- 9. Application during pregnancy and lactation
- 10. For violations of liver function
- 11. Drug interactions
- 12. Analogs
- 13. Terms and conditions of storage
- 14. Terms of dispensing from pharmacies
- 15. Reviews
- 16. Price in pharmacies
Latin name: Sulperason
ATX code: J01DD62
Active ingredient: cefoperazone + sulbactam (cefoperazone + sulbactam)
Producer: Pfizer Ilachlari Ltd Sti (Turkey)
Description and photo update: 2019-14-08
Sulperazon is an antibacterial drug. Refers to third generation cephalosporins with beta-lactamase inhibitors.
Release form and composition
The antibiotic Sulperazon is available in the form of a powder for the preparation of a solution for intramuscular and intravenous administration: white or almost white, with a slight yellowish tinge (2 g each in transparent colorless glass bottles, 1 bottle in a cardboard box).
Composition for 1 bottle:
- cefoperazone (as cefoperazone sodium) - 1 g;
- sulbactam (as sodium sulbactam) - 1 g.
Pharmacological properties
Pharmacodynamics
The antibacterial component of Sulperazon is cefoperazone, which belongs to the third generation of cephalosporins. It is active against sensitive microorganisms during the period of their active reproduction by suppressing the biosynthesis of the cell wall mucopeptide.
Sulbactam has no clinically significant antibacterial activity, with the exception of Acinetobacter and Neisseriaceae. However, it has been shown to be an irreversible inhibitor of most of the major beta-lactamases, which are produced by microorganisms that are resistant to beta-lactam antibiotics. The ability of sulbactam to prevent the destruction of cephalosporins and penicillins by resistant microorganisms has been proven by studies of resistant strains, for which this substance has shown pronounced synergism with cephalosporins and penicillins. Sulbactam also interacts with certain penicillin-binding proteins, which explains the more pronounced effect of sulperazone on sensitive strains compared to the use of sulbactam and cefoperazone in a 1: 1 ratio in agar or broth media.
When determining the MIC by the disc diffusion method, it is preferable to use a disc containing 75 μg of cefoperazone and 30 μg of sulbactam. These quality control guidelines are recommended when using discs like this:
- for Staphylococcus aureus, the zone diameter is 23‒30;
- for the control strain Acinetobacter spp. - 26‒32;
- for Escherichia coli - 27‒33;
- for Pseudomonas aeruginosa - 22-28.
Pharmacokinetics
After intravenous administration of 2 g of the drug (1 g of cefoperazone and 1 g of sulbactam), the maximum concentrations of cefoperazone and sulbactam were 236.8 and 130.2 μg / ml, respectively, and were reached within 5 minutes. This indicates a higher volume of distribution of sulbactam (range 18-27.6 L) compared to that of cefoperazone (range 10.2-11.3 L).
If Sulperazon at a dose of 1.5 g (includes 1 g of cefoperazone and 0.5 g of sulbactam) was administered intramuscularly, the maximum concentrations of these substances in the blood serum were recorded in the period from 15 minutes to 2 hours after administration. The maximum serum levels of cefoperazone and sulbactam were 64.2 and 19 μg / ml, respectively.
Both cefoperazone and sulbactam are well distributed in various tissues and fluids and are determined in bile, gallbladder, uterus, fallopian tubes, ovaries, appendix, skin, etc. Approximately 25% of the dose of cefoperazone and 84% of the dose of sulbactam, administered as the combined drug Sulperazon, excreted in the urine. Most of the remaining cefoperazone ingested is excreted in the bile. When bound to plasma proteins, cefoperazone does not displace bilirubin. The half-life of cefoperazone is 1.7 hours and that of sulbactam is about 1 hour. There is a linear dependence of the concentrations of active components in the blood serum on the administered dose. There is no information on the presence of any pharmacokinetic interaction between cefoperazone and sulbactam with the introduction of Sulperazone. With repeated use, clinically significant changes in the pharmacokinetics of both substances were not observed. When the drug is administered every 8–12 hours, the cumulation of cefoperazone and sulbactam does not occur.
Due to the active excretion of cefoperazone in the bile, its half-life is usually lengthened, and the excretion of the drug in the urine is increased in patients with obstruction of the biliary tract and / or liver disease. Even with severe liver dysfunctions in the bile, the therapeutic concentration of cefoperazone is determined, and the half-life increases by no more than 2–4 times.
In patients with varying degrees of renal dysfunction taking Sulperazon, there is a high correlation between the calculated creatinine clearance and the total clearance of sulbactam in the body. In patients with end-stage renal failure, a significant increase in the half-life of sulbactam was revealed (approximately 6.9 and 9.7 hours in various studies). Hemodialysis leads to significant changes in the volume of distribution, total clearance and half-life of sulbactam.
The pharmacokinetics of Sulperazone was studied in elderly patients with liver dysfunctions and renal failure. In contrast to healthy volunteers, they showed an increase in the volume of distribution, a decrease in clearance and a prolongation of the half-life of both cefoperazone and sulbactam. The pharmacokinetics of cefoperazone in this case correlates with the degree of liver dysfunction, and the pharmacokinetics of sulbactam - with the degree of renal dysfunction.
Studies carried out in children did not reveal clinically significant differences in the pharmacokinetics of the active components of Sulperazon in comparison with these indicators in adult patients. The approximate half-life of cefoperazone in children is 1.44–1.88 hours, and for sulbactam, 0.91–1.42 hours.
Indications for use
According to the instructions, Sulperazon is used for infectious and inflammatory diseases caused by microorganisms sensitive to cefoperazone and / or sulbactam:
- respiratory system infections;
- infections of soft tissues and skin;
- intra-abdominal infections (including cholecystitis, peritonitis, and cholangitis);
- infections of the urinary system;
- joint and bone infections;
- meningitis;
- inflammatory diseases of the pelvic organs (including endometritis);
- sepsis.
Contraindications
The antibiotic Sulperazon is contraindicated for use in patients allergic to cefoperazone, sulbactam, other cephalosporins and penicillins.
Instructions for use of Sulperazon: method and dosage
Sulperazon is administered intravenously or intramuscularly.
To prepare a solution for intravenous injection, 2 g of powder is diluted in 6.7 ml of solvent and injected over 3 or more minutes.
To prepare a solution for intravenous infusion for initial dissolution, mix 2 g of powder and 6.7 ml of solvent, and then dilute the resulting solution to 20 ml. The duration of the infusion is 15-60 minutes.
The following solutions can be used as a solvent: isotonic sodium chloride solution, sterile water for injection, 5% dextrose solution in water, physiological saline or 0.225% sodium chloride solution. Lactated Ringer's solution can be used to prepare the solution for infusion, but it cannot be used for initial dissolution. For this, Sulperazone powder is first mixed with water for injection, and then diluted with Ringer's lactate solution in the ratio of 2 ml (4 ml) of the initial solution to 50 ml (100 ml) of lactated Ringer's solution.
The solution for intramuscular administration is also prepared in two stages. First, the powder is dissolved in water for injection, then mixed with 2% lidocaine solution. The total volume of the solvent is 6.7 ml.
Adult patients are prescribed 2-4 g of Sulperazon per day. The daily dose is divided into two equal parts and administered every 12 hours. With persistent or severe infections, it is possible to increase the dose to 8 g per day, while patients who receive the drug in a 1: 1 ratio (4 g of cefoperazone and 4 g of sulbactam) may require additional administration of cefoperazone. The maximum dose of sulbactam is 4 g per day.
For children Sulperazon is prescribed at a dose of 40–80 mg / kg of body weight per day. The recommended dose is divided into 2–4 equal parts and injected every 6–12 hours. With resistant to treatment and severe infections, it is possible to increase the dose to 160 mg / kg of body weight per day. Newborns in the first week of life are injected with Sulperazon every 12 hours. The maximum dose of sulbactam in children is 80 mg / kg of body weight per day.
With pronounced impaired renal function (creatinine clearance 15-30 ml / min), the maximum dose of sulbactam should not exceed 2 g per day (1 g every 12 hours), and with creatinine clearance less than 15 ml / min - 1 g per day (by 0.5 g every 12 hours).
Side effects
- digestive system: vomiting, nausea, pseudomembranous colitis, diarrhea;
- urinary system: hematuria;
- hematopoietic system: decreased hematocrit and hemoglobin, leukopenia, hypoprothrombinemia, transient eosinophilia, thrombocytopenia; with prolonged use - reversible neutropenia;
- allergic reactions: itching, Stevens-Johnson syndrome, maculopapular rash, urticaria, anaphylactic shock (in patients with a history of allergies, the risk of developing such reactions is higher);
- laboratory indicators: increased liver function indicators (transient); when using Fehling's or Benedict's solution - a false positive reaction to glucose in the urine; isolated cases - positive Coombs test;
- local reactions: after intramuscular injection - burning and transient pain at the injection site; with intravenous administration - phlebitis at the infusion site;
- other reactions: fever, vasculitis, headache, chills.
Overdose
Information on acute overdose of sulbactam and cefoperazone when used in humans is currently limited. When taking too large doses of Sulperazone, one can assume the development of undesirable side effects indicated by the manufacturer in the description of the drug. It should also be borne in mind that high levels of beta-lactam antibiotics in cerebrospinal fluid can provoke neurological disorders, including seizures. In case of an overdose, Sulperazon is prescribed symptomatic therapy. The effectiveness of hemodialysis in the elimination of drug components has been proven, especially in patients with renal dysfunction.
special instructions
With the development of allergic reactions, Sulperazon should be canceled and adequate treatment should be prescribed.
In the absence of regular monitoring of the serum concentration of cefoperazone, the daily dose of Sulperazone should not exceed 2 g.
In patients with malabsorption, patients who do not receive adequate nutrition, and patients using anticoagulants, prothrombin time should be monitored, and in case of vitamin K deficiency, this vitamin should be prescribed additionally.
With prolonged antibiotic therapy, the sensitivity to the drug may decrease.
With prolonged treatment, especially in newborns and young children, it is recommended to regularly monitor the function of the kidneys, liver and hematopoietic system.
Influence on the ability to drive vehicles and complex mechanisms
Clinical experience with the use of Sulperazon confirms that its impact on the ability to drive vehicles and perform complex types of work is unlikely.
Application during pregnancy and lactation
Appropriate clinical studies of the use of Sulperazone in pregnant women have not been conducted. Cefoperazone and sulbactam cross the placental barrier and into breast milk. During pregnancy and lactation, this drug is used only under strict indications and in cases where the potential benefits of treatment for the mother significantly outweigh the possible negative consequences for the fetus or child.
For violations of liver function
In patients with severe liver disease and biliary obstruction, it may be necessary to adjust the dosage regimen of the drug. In patients with liver dysfunctions and concomitant renal dysfunctions, constant monitoring of the concentration of cefoperazone in the blood serum is required and its dose adjustment, if necessary. If the regular monitoring of the content of cefoperazone in the blood serum in such cases is not carried out, then its daily dose should not exceed 2 g.
Drug interactions
With simultaneous use with ethanol, as well as within 5 days after the administration of Sulperazon, disulfiram-like reactions may occur, characterized by headache, tachycardia, sweating and hot flashes, therefore it is not recommended to consume alcoholic beverages during treatment. Patients on artificial nutrition (parenteral or oral) should avoid the use of ethanol-containing solutions.
It is necessary to observe the largest possible intervals during the day between the administration of aminoglycosides and Sulperazon, since the solutions of these drugs are pharmaceutically incompatible.
Analogs
Analogues of Sulperazon are: Cefosin, Ceftriaxone, Medaxon, Loprax, Lendacin, Fortum, Azaran, Zedex, Bestum, Tizim, Vicef, Suprax, Ixim, Orzid, Lorazidim, Medocef, Loraxon.
Terms and conditions of storage
Store at a temperature not exceeding 25 ° C. Keep out of the reach of children. Shelf life is 2 years.
The reconstituted solution can be stored at room temperature for 24 hours.
Terms of dispensing from pharmacies
Dispensed by prescription.
Reviews about Sulperazone
The available reviews about Sulperazone do not allow to unambiguously assess its effectiveness and safety of use. This is most likely due to the prescription of the drug as part of the course of treatment for infectious diseases caused by microorganisms resistant to it.
However, specialists often use Sulperazon when choosing a course of therapy, and many of them are satisfied with the results obtained. In this case, it is recommended to conduct an analysis to determine the causative agent of the disease and strictly follow the instructions of a specialist.
Price for Sulperazon in pharmacies
On average, the price for Sulperazon in pharmacies is 341-352 rubles.
Maria Kulkes Medical journalist About the author
Education: First Moscow State Medical University named after I. M. Sechenov, specialty "General Medicine".
Information about the drug is generalized, provided for informational purposes only and does not replace the official instructions. Self-medication is hazardous to health!
