Sulperacef - Instructions For Use, Price, Antibiotic Analogues, Reviews

2024 Author: Rachel Wainwright | [email protected]. Last modified: 2023-12-15 07:39

Sulperacef

Sulperacef: instructions for use and reviews

1. 1. Release form and composition
2. 2. Pharmacological properties
3. 3. Indications for use
4. 4. Contraindications
5. 5. Method of application and dosage
6. 6. Side effects
7. 7. Overdose
8. 8. Special instructions
9. 9. Application during pregnancy and lactation
10. 10. Use in childhood
11. 11. In case of impaired renal function
12. 12. For violations of liver function
13. 13. Drug interactions
14. 14. Analogs
15. 15. Terms and conditions of storage
16. 16. Terms of dispensing from pharmacies
17. 17. Reviews
18. 18. Price in pharmacies

Latin name: Sulperacef

ATX code: J01DD62

Active ingredient: cefoperazone (Cefoperazone), sulbactam (Sulbactam)

Producer: LLC "ABOLmed" (Russia)

Description and photo update: 2020-16-01

Sulperacef is an antibacterial agent.

Release form and composition

Dosage form - powder for preparation of a solution for intravenous (intravenous) and intramuscular (intramuscular) administration: white or white with a yellowish tinge [250 mg + 250 mg, 500 mg + 500 mg, 1000 mg + 1000 mg per glass vials with a capacity of 10 or 20 ml, in a cardboard box or 1 bottle, or 1 bottle complete with 1 ampoule of solvent (separately or in a blister), or 5 bottles in a blister, or 5 bottles in a blister, complete with 5 ampoules of solvent. Each pack also contains instructions for the use of Sulperacef].

The composition of the active substances of the drug in 1 bottle: cefoperazone (in the form of sodium salt) - 250, 500 or 1000 mg and sulbactam (in the form of sodium salt) - 250, 500 or 1000 mg (respectively).

Solvent: water for injection - 5 ml.

Pharmacological properties

Pharmacodynamics

The action of Sulperacef is due to the properties of its active components:

• cefoperazone is a third-generation cephalosporin that affects sensitive microorganisms during the period of their active reproduction due to the ability to inhibit the biosynthesis of the cell wall mucopeptide;
• sulbactam is an irreversible inhibitor of most of the major beta-lactamases that produce microorganisms that exhibit resistance to beta-lactam antibiotics. It has clinically significant antibacterial activity only against Acinetobacter and Neisseriaceae. It binds to some penicillin-binding proteins, as a result of which it enhances the effect of cefoperazone on sensitive strains.

Sulperacef is active against all microorganisms that are sensitive to cefoperazone. Also, due to the combination of two active components, the drug exhibits synergism with respect to various microorganisms, especially Acinetobacter calcoaceticus, Bacteroides species, Citrobacter diversus, Citrobacter freundii, Escherichia coli, Enterobacter aerogenes, Enterobacter cloacae, Haemophilus influenzae, Klebsiella morbidoniae, Morgan species …

In vitro, Sulperacef has a broad spectrum of action against many clinically significant microorganisms:

• anaerobic microorganisms: gram-positive and gram-negative cocci (including Peptostreptococcus, Peptococcus, Veillonella species), gram-positive rods (including Eubacterium, Clostridium, Lactobacillus species), gram-negative rods (including Fusobacterium fragil species, Bacides)
• gram-negative microorganisms: Acinetobacter calcoaceticus, Bordetella pertussis, Citrobacter species, Escherichia coli, Enterobacter species, Haemophilus influenzae, Klebsiella species, Morganella morganii, Neisseria meningitides, Neisseria gonorrhoeae, Proteidencia mirabasis retisis, Proteidencia species retinosa, Providencia species retinosa,, Salmonella, Serratia species (including S. marcescens), Yersinia enterocolitica;
• gram-positive microorganisms: Streptococcus agalactiae (group B beta-hemolytic streptococcus), Streptococcus pyogenes (group A beta-hemolytic streptococcus), Streptococcus pneumoniae, Staphylococcus epidermidis, Staphylococcus aureus (including most of the bacillus producing) pests other strains of beta-hemolytic streptococci.

Pharmacokinetics

Both active substances of Sulperacef are well distributed in various body fluids and tissues, including the gallbladder, bile, ovaries, fallopian tubes, uterus, appendix, skin.

After intravenous administration of 2000 mg of the drug (1000 mg of cefoperazone and sulbactam), the maximum plasma concentrations (C _max) of active substances within 5 minutes averaged 236.8 and 130.2 μg / ml, respectively. The volume of distribution (V _d) of cefopereson is 10.2–11.3 liters, of sulbactam - 18–27.6 liters. Serum concentration is proportional to the dose administered.

After the administration of Sulperacef, approximately 25% of the dose of cefoperazone and 84% of the dose of sulbactam are excreted by the kidneys, the rest of the cefoperazone - mainly with bile.

The half-life (T _1/2) of cefoperazone averages 1.7 hours, sulbactam - 1 hour.

With subsequent injections of the drug, no significant changes in the pharmacokinetic parameters of both active substances of Sulperacef were noted.

Pharmacokinetics in special cases:

• liver function: since most of cefoperazone is excreted in the bile, in patients with liver disease and obstruction of the biliary tract, its T _{1/2 is} lengthened. Even with a severe functional impairment of the liver, the therapeutic concentration of the drug in the bile is achieved, while T _1/2 increases by 2-4 times;
• renal function: for various functional disorders of the kidneys, a high correlation was found between the calculated creatinine clearance and the total clearance of sulbactam from the body. In end- stage renal failure, T _{1/2 of} sulbactam significantly increases (up to 6.9-9.7 hours). Significant changes in V _d, T _1/2 and total clearance from the body of sulbactam causes hemodialysis;
• old age: in the presence of concomitant renal and liver dysfunctions, T _1/2 and V _d increase, the clearance of both active substances of Sulperacef decreases. The pharmacokinetics of cefoperazone correlates with the degree of impaired hepatic function, and the pharmacokinetics of sulbactam correlates with the degree of impaired renal function;
• children's age: in children, there were no significant differences in the pharmacokinetics of sulbactam and cefoperazone. The average T _{1/2 of} cefoperazone is 1.44–1.88, sulbactam is 0.91–1.42 hours.

Indications for use

Sulperacef is used as the only antibiotic (monotherapy) for the treatment of mixed aerobic-anaerobic infections of various localizations, including cases when the pathogen is resistant to other cephalosporins, penicillins, aminoglycosides, fluoroquinolones, lincosamides. In particular, the drug is prescribed for diseases such as:

• bacterial meningitis;
• infections of bones and joints;
• septicemia;
• urinary tract infections, including pyelitis and pyelonephritis;
• intra-abdominal infections (including complicated ones), including cholangitis, cholecystitis, abdominal abscess and peritonitis;
• infections of the skin and soft tissues;
• infections of the respiratory tract, including sinusitis, pneumonia, lung abscess, pleural empyema;
• inflammatory diseases of the pelvic organs (including endometritis, pelvioperitonitis, salpingo-oophoritis), infections of the genital tract (including gonorrhea).

Contraindications

The antibiotic Sulperacef is contraindicated in patients who are allergic to penicillins, cefoperazone, sulbactam, or other cephalosporins.

The drug is used with caution in severe liver diseases and severe obstruction of the biliary tract, as well as in patients with renal and hepatic insufficiency or a combination of these pathologies.

In exceptional cases and under close supervision, an antibiotic is used to treat pregnant and breastfeeding women.

Sulperacef, instructions for use: method and dosage

The solution prepared from Sulperacef powder is injected intramuscularly or intravenously.

For i / m administration, the powder is dissolved with sterile water for injection. It is injected deep into the muscle in areas of the body with a pronounced muscle layer (for example, the upper-outer quadrant of the buttocks). At a dose of 250 mg / ml, dilution is carried out in two stages:

1. For primary dilution, sterile water is used: for Sulperacef 500 mg (250 mg of cefoperazone and sulbactam) - 1.5 ml, for Sulperacef 1000 mg (500 mg of cefoperazone and sulbactam) - 2.4 ml, for Sulperacef 2000 mg (1000 mg of cefoperazone and sulbactam) - 4.7 ml.
2. For secondary dilution, a 2% lidocaine solution is used (provided that there is no allergy to local anesthetics): 0.5 ml of a 2% lidocaine solution is added to the initially obtained solution for Sulperacef 500 mg, for Sulperacef 1000 mg - 1 ml, for Sulperacef 2000 mg - 2 ml.

For intravenous jet injection, powder in doses of 500 and 1000 mg is dissolved in 10 ml, and powder in a dose of 2000 mg is dissolved in 20 ml of 0.9% sodium chloride solution or injection water. Enter within 3-5 minutes. When infused with compatible solutions, Sulperacef can be administered through the injection site of the intravenous infusion system.

For intravenous drip infusion, the powder in doses of 500 and 1000 mg is dissolved in 10–20 ml of 0.9% sodium chloride solution or injection water. Then this solution is added to 50-100 ml of 0.9% sodium chloride solution or 5% dextrose solution. Administered using an intravenous infusion system.

Adults and children over 12 years of age are prescribed 1000-2000 mg of Sulperacef (500-1000 mg of cefoperazone and sulbactam) every 12 hours. For severe life-threatening infections, the dose is increased to 4000 mg (2000 mg of cefoperazone and sulbactam) every 12 hours In some cases, additional administration of a drug containing only cefoperazone may be required.

For patients with renal insufficiency, the dose of the drug is adjusted. Depending on the creatinine clearance, Sulperacef is prescribed:

• 15-30 ml / min - 1000 mg (500 mg of cefoperazone and sulbactam) every 12 hours;
• <15 ml / min - 500 mg (250 mg of cefoperazone and sulbactam) every 12 hours.

In severe infections, patients with severe renal impairment are additionally prescribed a drug containing only cefoperazone. Patients receiving hemodialysis, Sulperacef is required to be administered immediately after the end of dialysis.

For patients with functional hepatic impairment, dose adjustment of the drug is required in severe liver disease and severe obstruction of the biliary tract, as well as in the case of a combination of liver failure with renal failure. During treatment, it is necessary to control the serum concentration of cefoperazone and, if necessary, adjust its dose. If it is not possible to monitor the content of cefoperazone in the blood serum, a daily dose of 2000 mg (1000 mg of cefoperazone and sulbactam) should not be exceeded.

For children from 1 month to 12 years old, Sulperacef is administered in a daily dose of 40–80 mg / kg, dividing it into 2–4 injections at intervals of 12 or 6 hours, respectively. In severe infectious processes, the dose can be increased to 160 mg / kg per day.

When treating newborns, the daily dose of sulbactam 80 mg / kg should not be exceeded. For children of the first week of life, it is recommended to inject Sulperacef at 12-hour intervals.

Side effects

• laboratory parameters: hyperbilirubinemia, hypercreatininemia, hypothrombinemia, increased alkaline phosphatase and hepatic enzyme activity;
• gastrointestinal tract: nausea, pseudomembranous colitis, diarrhea, vomiting;
• hematopoietic system: a decrease in the number of neutrophils, vitamin K deficiency (bleeding); with long-term treatment - reversible neutropenia; in rare cases - positive Coombs' test, decreased hematocrit and hemoglobin levels, hypothrombinemia, transient thrombocytopenia / leukopenia;
• skin reactions: itching, urticaria, maculopapular rash, Stevens-Johnson syndrome (especially in patients with a history of penicillin allergy);
• allergic reactions: fever, transient eosinophilia, anaphylactic shock;
• local reactions: transient pain at the intramuscular injection site, phlebitis at the intravenous infusion site;
• others: fever, headache, chills, vasculitis, hematuria.

Overdose

In case of an overdose, the appearance of reactions recorded with the usual use of Sulperacef (side effects) is expected. Due to the increased concentration of cefoperazone, neurological disorders, including convulsions, may develop.

Overdose treatment is symptomatic and supportive. For neurological disorders, sedative therapy is performed. With anaphylactic shock, epinephrine is administered intravenously, glucocorticosteroids and oxygen inhalation are used. In severe cases, as well as in patients with impaired renal function, hemodialysis is performed.

special instructions

Like other antibiotics, cefoperazone can cause vitamin K deficiency. The risk group is represented by patients with malabsorption syndrome (for example, with cystic fibrosis), as well as patients receiving malnutrition or long-term artificial intravenous nutrition. In these cases, regular monitoring of prothrombin time is required, if necessary, additional prescription of drugs containing vitamin K. The same precautions are needed for patients taking anticoagulants.

In the case of long-term treatment with Sulperacef, like any other antibiotic, excessive growth of insensitive microorganisms is possible. It is necessary to monitor the indicators of the functions of internal organs, including the circulatory system, kidneys and liver, especially in premature babies, newborns and young children. More frequent monitoring of serum cefoperazone concentration is necessary in patients in whom liver dysfunction is combined with renal failure.

Sulperacef may distort the results of tests for glucose in urine when using Fehling's or Benedict's solution. It is possible to get a false positive Coombs' test.

Cases of serious hypersensitivity reactions have been reported in patients treated with beta-lactam antibiotics. The risk is increased in patients with a history of allergic reactions. When signs of hypersensitivity to the drug appear, the administration of Sulperacef is immediately stopped and epinephrine is immediately injected, if necessary, glucocorticosteroids are administered intravenously, oxygen is prescribed, or airway patency is ensured.

Due to the wide spectrum of activity, Sulperacef is used mainly as a monopreparation. However, if necessary, it can be prescribed in combination with aminoglycosides, only more careful monitoring of renal function is required.

Influence on the ability to drive vehicles and complex mechanisms

No information available.

Application during pregnancy and lactation

The antibiotic Sulperacef is prescribed for pregnant / breastfeeding women only when the benefits of treatment are clearly higher than the potential risks to the fetus / baby.

Pediatric use

Sulperacef, according to indications, is used to treat children from birth, in accordance with age recommendations for dosing. However, when prescribing to newborns, especially premature infants, the expected benefits and possible risks should be assessed.

With impaired renal function

In case of renal failure, Sulperacef is used with caution. Dose adjustment is required depending on creatinine clearance, as well as in the case of a combination of renal and hepatic failure.

For violations of liver function

In case of hepatic insufficiency, Sulperacef is used with caution. Dose adjustment is required in severe liver disease and severe obstruction of the biliary tract, as well as in the case of a combination of liver failure with renal failure.

Drug interactions

Cefoperazone, like disulfiram, causes alcohol intolerance, which is manifested by headache, sweating, hot flashes, tachycardia. Patients should be warned about the need to abstain from drinking alcoholic beverages for 5 days after the end of treatment. Patients receiving artificial nutrition should avoid the introduction of solutions containing ethanol.

With the simultaneous use of aminoglycosides, there is a synergism of the bactericidal effect against gram-negative and gram-positive bacteria. Do not mix solutions with each other in the same syringe or the same infusion medium, since they are physically incompatible. In combination therapy, intravenous administration of these drugs is carried out through separate intravenous catheters, or by two separate infusions (between the administration of doses of drugs, the catheter is washed with an adequate solution), intramuscular injections are performed in different parts of the body. The time intervals between infusions (injections) should be as long as possible.

Sulperacef is pharmaceutically incompatible with protein hydrolysates and blood products, as well as with lactated Ringer's solution, therefore it is not recommended to use it for the primary dissolution of the drug.

Analogs

The analogues of Sulperacef are Bakperazon, Bakcefort, Broadsef-S, Zavicefta, Zerbaxa, Claruktam, Maksiktam-AF, Paktocef, Sulzontsef, Sulmover, Sulmagraf, Sulcef, Sulperazon, Tsebanex, Cefbaktam, Cefoperazon, and drvitsefactam + Zulbaktam.

Terms and conditions of storage

Store in a dry, dark place where the ambient temperature does not exceed 25 ° C.

Shelf life is 2 years.

Terms of dispensing from pharmacies

Dispensed by prescription.

Reviews about Sulperacef

Currently, there are no reviews about Sulperacef either from patients or from medical specialists, so there is no way to assess the degree of its effectiveness, safety and tolerance.

The price of Sulperacef in pharmacies

At the moment, the drug is not available in pharmacies, but there is a registered price for Sulperacef, since it is included in the list of Vital and Essential Medicines (Vital and Essential Medicines). The cost of the solution for intramuscular and intravenous administration is:

• dosage 250 mg + 250 mg: in a pack 1 bottle - 201 rubles, in a pack 1 bottle complete with a solvent ampoule - 222.87 rubles, in a pack 1 bottle and a solvent in a blister strip - 233 rubles, in a pack 5 bottles in a blister strip - 1006 rubles; in a pack of 5 bottles with 5 ampoules of solvent in blisters - 1081 rubles;
• dosage of 500 mg + 500 mg: in a pack 1 bottle - 315 rubles, in a pack 1 bottle with an ampoule of solvent in a blister strip - 347 rubles, in a pack of 5 bottles - 1575 rubles, in a pack of 5 bottles with 5 ampoules of solvent in blisters - 1655 rubles;
• dosage 1000 mg + 1000 mg: in a pack 1 bottle - 398 rubles, in a pack 1 bottle complete with an ampoule of solvent - 419.85 rubles, in a pack 1 bottle and a solvent in a blister strip - 430 rubles, in a pack 5 bottles in a blister strip - 1991 rubles, in a pack of 5 bottles complete with 5 ampoules of solvent in blisters - 2080 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!