Clarouct (Klaruktam)

Composition Pharmacodynamics Indications Carefully Contraindications Dosing and Administration Side effects Form release / dosage
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Dosage form: & nbsppowder for solution for intravenous and intramuscular administration
Composition:

AT 1 vial contains:

Cefotaxime sodium 1048 * mg (in terms of cefotaxime 1000 mg),

Sulbactam sodium 547 * mg (in terms of sulbactam 500 mg).

Note. * The mass of the contents of the bottle depends on the content of active substances and water in substances.

Description:

The powder is white or white with a yellowish hue. Sensitive to the action of light.

Pharmacotherapeutic group:Antibiotic-cephalosporin + beta-lactamase inhibitor
ATX: & nbsp
  • Cefotaxime in combination with other drugs
    • Pharmacodynamics:

    The antibacterial component of the drug cefotaxime+ sulbactam is cefotaxime - cephalosporin antibiotic III generation for parenteral administration. It acts bactericidal, disrupting the synthesis of the cell wall of microorganisms. Has a wide range of action.

    Sulbactam does not have clinically significant antibacterial activity (the exception is the family Neisseriaceae and Acinetobacter spp.). Is an irreversible inhibitor of most of the major beta-lactamases that are produced microorganisms resistant to beta-lactam antibiotics.

    The ability of sulbactam to prevent the destruction of penicillins and cephalosporins by resistant microorganisms has been confirmed in studies using resistant strains,in respect of which sulbactam possessed a pronounced synergism with penicillins and cephalosporins. In addition, sulbactam interacts with certain penicillin-binding proteins, so cefotaxime+ sulbactam often has a more pronounced effect on sensitive strains than one cefotaxime.

    The combination of cefotaxime and sulbactam is active against all microorganisms sensitive to cefotaxime. In addition, it has a synergistic effect on various microorganisms.

    Cefotaxime + sulbactam is active against gram-positive and gram-negative microorganisms resistant to other antibiotics: Aeromonas hydrophila, Bacillus subtilis, Bordetella pertussis, Borrelia burgdorferi, Moraxella catarrhalis, Citrobacter diversus, Citrobacter ffeundii, Clostridium perfringens, Corynebacterium diphteriae, Escherichia coli, Enterobacter spp., Erysipelotrhix insidiosa, Eubacterium spp., Haemophilus influenzae, Klebsiella pneumoniae, Klebsiella oxytoca, Morganella morganii, Neisseria gonorrhoeae, Neisseria meningitidis, Propionibacterium spp., Proteus mirabilis, Proteus vulgaris, Providencia spp., Staphylococcus spp., Streptococcus spp. (incl. Streptococcus pneumoniae), Salmonella spp., Shigella spp., Serratia spp., Veillonella spp., Yersinia spp., Pseudomonas spp. (Besides Pseudomonas cepacia, Pseudomonas aeruginosa). Sensitivity depends on epidemiological data and on the level of sustainability in each country. Resistant microorganisms: Acinetobacter baumanii, Bacteroides fragilis, Clostridium difficile, Enterococcus spp., gram negative anaerobes, Listeria monocytogenes, methicillin-resistant Staphylococcus spp., Pseudomonas cepacia, Pseudomonas aeruginosa, Stenotrophomonas maltophilia.

    Pharmacokinetics:

    Maximum Concentrations (Cmax) cefotaxime and sulbactam after intravenous administration (in / in) in adults after 5 minutes, 1.5 g of cefotaxime + sulbactam (1 g of cefotaxime and 0.5 g of sulbactam) averaged 100 μg / ml and 20 μg / ml, respectively. FROMmOh cefotaxime and sulbactam after intramuscular injection (in / m), 1.5 g of the preparation averaged 20-30 μg / ml and 6-24 μg / ml, respectively. The connection with plasma proteins cefotaxime - 25-40%, sulbactam - about 38 %.

    Bioavailability with intravenous injection 100%, with intramuscular injection - 90-95%. Therapeutic concentrations are created in most tissues (myocardium, bones, gall bladder, skin, soft tissues) and fluids (synovial, pericardial, pleural, sputum, bile, urine, cerebrospinal fluid) of the body. The volume of distribution of cefotaxime is 0.25-0.39 l / kg, sulbactam 0.29 l / kg. Sulbactam penetrates the placental barrier. Cefotaxime penetrates the placental barrier and is secreted into the mother's milk.

    With repeated use of significant changes in the pharmacokinetic parameters of both components of the drug was not noted. There is no data on the presence of any pharmacokinetic interaction between sulbactam and cefotaxime upon administration of the drug.

    The half-life (T1 / 2) of cefotaxime is 1 hour for IV administration and 1-1.5 hours for the IM injection. About 90% is excreted by the kidneys - 50% unchanged, the rest is in the form of metabolites (15-25% in pharmacologically active deacetylcefotaxime and 20-25% in the form of 2 inactive metabolites, M2 and M3). 10% of the administered dose is excreted by the intestine. The half-life of sulbactam averages about 1 hour. Approximately 84% of the dose of sulbactam is excreted by the kidneys unchanged. In patients with normal renal function, cumulation of the drug does not occur.

    In chronic renal failure (CRF) and in elderly patients older than 80 years, T1 / 2 cefotaxime is increased to 2.5 hours. T1 / 2 in children 0.75-1.5 hours, in newborns, including premature infants, children 1.4-6.4 hours. With CRF, a high correlation was found between the total clearance of sulbactam from the body and the estimated clearance of creatinine. In patients with terminal renal failure, a significant lengthening of the half-life of sulbactam (an average of 6.9 and 9.7 hours in various studies) was detected. Hemodialysis caused significant changes in T1 / 2, the overall clearance and the volume of distribution of sulbactam.

    Indications:

    Infectious-inflammatory diseases caused by microorganisms sensitive to the combination of cefotaxime with sulbactam: infections of the central nervous system (including meningitis, with the exception of listeriosis), lower respiratory tract and ENT organs, urinary tract, bones, joints, skin and soft tissues including infected wounds and burns), pelvic organs, gonorrhea, peritonitis, sepsis, intra-abdominal infections, endocarditis, Lyme disease (borreliosis), infection on the background of immunodeficiency.

    Prevention of infections after surgery (including urological, obstetric-gynecological, on the gastrointestinal tract).

    Contraindications:

    Hypersensitivity to sulbactam, cefotaxime, other cephalosporins.

    For forms containing as a solvent lidocaine; hypersensitivity to lidocaine or other local anesthetic of the amide type, intracardiac blockades without an established pacemaker, severe heart failure, intravenous administration, children under the age of 2.5 years (intramuscular injection).

    Carefully:

    In patients,having a history of allergy to penicillins (risk of developing cross-allergic reactions), simultaneous use with aminoglycosides, chronic renal failure, neonatal period (for IV).

    Pregnancy and lactation:

    Pregnancy

    Cefotaxime and sulbactam penetrate the placental barrier. Studies conducted on animals did not reveal a teratogenic or fetotoxic effect. However safety of application at pregnancy at the person is not established. Therefore, the drug should not be used during pregnancy.

    Breastfeeding period

    Cefotaxime penetrates into breast milk. Therefore, if you need to use the drug during lactation should stop breastfeeding.

    Dosing and Administration:

    Intravenous (jet, drip) and intramuscularly. The dose, method and frequency of administration should be determined by the severity of the infection, the sensitivity of the pathogen and the patient's condition. Treatment can be initiated before the results of the sensitivity test are obtained.

    Doses are given in terms of cefotaxime.

    Adults and children over 12 years of age with a body weight of 50 kg and more: for infections of mild to moderate severity - 1 g every 12 h. The dose may vary depending on the severity of the infection, the sensitivity of the pathogen and the patient's condition. In severe infections, the dose can be increased to 12 g per day, divided into 3-4 injections. In infections caused by Pseudomonas spp., The daily dose should be more than 6 g. The maximum daily dose of sulbactam is 4 g.

    If necessary, the introduction of more than 12 g of the drug (with a ratio of the main components cefotaxime+ sulbactam 2: 1), an increase in the dose is achieved through the additional administration of cefotaxime.

    Children under 12 years with a body weight of up to 50 kg: the usual dose is 100-150 mg / kg / day, divided into 2-4 injections. In very severe infections, the dose can be increased to 200 mg / kg per day.

    Newborns: the dose is 50 mg / kg per day, divided into 2-4 injections. In severe infections, a dose of 150-200 mg / kg per day, divided into 2-4 injections. The maximum daily dose of sulbactam in children should not exceed 80 mg / kg / day.

    With gonorrhea: 1 g once intravenously or intramuscularly.

    In order to prevent the development of infections before surgery (from 30 to 90 minutes before the operation) 1 g intravenously or intramuscularly.

    When performing cesarean section (at the time of application of the clamps on the umbilical vein) - intravenously 1 g, then 6 and 12 hours after the first dose again for 1 g.

    With renal insufficiency: with creatinine clearance (CK) of less than 10 ml / min, the daily dose of cefotaxime is reduced. After the introduction of the initial single dose, the daily dose should be reduced 2 times without changing the frequency of administration, i.e. instead of 1 g every 12 h - 0.5 g every 12 h, instead of 1 g every 8 h - 0.5 g every 8 h, instead of 2 g every 8 h - 1 g every 8 h, etc. A further dose adjustment may be required depending on the course of the infection and the general condition of the patient. In patients with creatinine clearance of 15-30 ml / min, the maximum daily dose of sulbactam is 2 g, and in patients with creatinine clearance less than 15 ml / min the maximum daily dose of sulbactam is 1 g. In severe infections, additional administration of cefotaxime may be required.

    Rules for the preparation of injection solutions.

    For intravenous injection as a solvent, water for injection is used (1000 mg + 500 mg is diluted in 10 ml of solvent (water for injections)). Enter in / in slowly (3-5 minutes).

    For IV infusion, the drug is first dissolved in water for injection in a ratio 1000 mg + 500 mg / 10 ml, and then diluted in 50 or 100 ml of the following solvents: 0.9% solution of sodium chloride,5% dextrose solution, 5% dextrose solution or 0.9% sodium chloride solution. The duration of the infusion is 20-60 min.

    For the / m administration, 1000 mg + 500 mg of the drug in 5 ml of water for injection or in 1% of lidocaine solution is dissolved. The solution is injected deep into a relatively large muscle.

    Side effects:

    From the nervous system: convulsions, headache, dizziness, encephalopathy (impaired consciousness, motor disorders).

    Local Reactions: fever, phlebitis / thrombophlebitis, inflammatory reactions at the injection site, tenderness and infiltration at the site of the IM. When administered intramuscularly, if a solvent is used lidocaine, it is possible to develop systemic reactions associated with lidocaine, especially in cases of unintentional intravenous administration of the drug, injection into highly vascularized tissue or overdose.

    From the urinary system: decreased renal function / hypercreatininaemia, especially when combined with aminoglycosides, acute renal failure, interstitial nephritis.

    From the digestive system: nausea, vomiting, diarrhea or constipation, flatulence, abdominal pain,increased activity of "hepatic" transaminases (alanine aminotransferase, aspartate aminotransferase, lactate dehydrogenase, gamma glutamyltransferase, alkaline phosphatase) and / or bilirubin concentration, pseudomembranous colitis, hepatitis (sometimes with jaundice). These deviations in laboratory indicators (which can also be explained by the presence of infection) rarely exceed the upper limit of the norm by a factor of two and indicate liver damage manifested by cholestasis and often asymptomatic.

    On the part of the organs of hematopoiesis: leukopenia, eosinophilia, thrombocytopenia, bone marrow hematopoiesis deficiency, pancytopenia, neutropenia, agranulocytosis, hemolytic anemia.

    From the side of the cardiovascular system: arrhythmias (due to rapid bolus injection into the central vein).

    From the immune system: the reaction of Jarisch-Gerxheimer. As with the use of other antibiotics, in the treatment of borreliosis during the first days of therapy, it is possible development of the Yarisch-Gerxheimer reaction. There are reports of the occurrence of one or more several symptoms after a few weeks of Borreliosis treatment, skin rash, itching, fever, leukopenia,increased activity of "liver" transaminases, shortness of breath, discomfort in the joints. It should be borne in mind that to some extent, these manifestations are consistent with the symptoms of the underlying disease, over which the patient is receiving treatment. Anaphylactic reactions, angioedema, bronchospasm, anaphylactic shock.

    From the skin: urticaria, rash, itchy skin, erythema multiforme, Stevens-Johnson syndrome, toxic epidermal necrolysis (Lyell's syndrome), acute generalized exanthematous pustules.

    Other: superinfection (in particular, candidal vaginitis, candidiasis of the oral mucosa).

    Overdose:

    Symptoms: convulsions, encephalopathy (in the case of the administration of large doses, especially in patients with renal insufficiency), tremor, neuromuscular excitability.

    Treatment: symptomatic. There is no specific antidote.

    Interaction:

    The probability of kidney damage increases with simultaneous administration with aminoglycosides, polymyxin B and "loop" diuretics.

    Drugs that block tubular secretion,increase plasma concentrations of the drug and slow its elimination.

    Pharmaceutically incompatible with solutions of other antibiotics in one syringe or dropper.

    Probenecid retards excretion and increases the concentration of cephalosporins in the blood plasma.

    Special instructions:

    Anaphylactic reactions

    The use of cephalosplorins requires the collection of an allergic anamnesis (allergic diathesis, hypersensitivity reactions to beta-lactam antibiotics). In case of an allergic reaction, it is necessary to cancel the drug. The use of the drug is contraindicated in the presence of a patient in an anamnesis reaction hypersensitivity immediate type of cephalosporins, sulbactam. Patients, who had a history of allergic reactions to penicillins, may have increased sensitivity to cephalosporin antibiotics (in 5-10% of cases).

    Anaphylactic reactions that develop in this situation can be serious or even fatal. Patients who have a history of having an allergy to penicillins should be treated with caution. Careful monitor the condition at the first administration of the drug due to a possible anaphylactic reaction. In case of development of the first symptoms and signs of anaphylactic shock, the drug should be stopped immediately and adequate therapy should be prescribed.

    Pseudomembranous colitis

    Against the background of the introduction of the drug or after the end of treatment, pseudomembranous colitis can appear, which manifests itself as severe long-term diarrhea, including with blood. At the same time, stop the drug administration and prescribe adequate therapy, including Vancomycin or metronidazole inside. Contraindicated the use of drugs that inhibit the intestinal peristalsis.

    The use of lidocaine as a solvent

    When using lidocaine as a solvent, the information provided in the section "Contraindications" should be taken into account.

    The rate of administration

    It is necessary to control the rate of administration of the drug (see section "Method of administration and dose").

    Renal insufficiency

    In renal failure, the dose should be adjusted depending on the creatinine clearance (see section "Method of administration and dose").

    Caution should be exercised when used simultaneously with aminoglycosides.Kidney function should be monitored in all cases of combined use with aminoglycosides, other nephrotoxic drugs in elderly patients or with renal insufficiency.

    Hemorrhage disorders

    During treatment with the drug may develop leukopenia, neutropenia and more rarely - bone marrow hematopoiesis deficiency, pancytopenia and agranulocytosis. When the drug is treated for more than 10 days, it is necessary to control the number of blood cells. If you deviate from these indicators, you should cancel the drug.

    The sodium content

    In patients requiring a restriction of sodium intake, the sodium content of the preparation (48 mg) should be taken into account.

    Laboratory indicators

    During treatment, it is possible to obtain a false-positive sample of Coombs and a false positive urine reaction to glucose (glucose oxidase methods for determining the concentration of glucose in the blood plasma are recommended).

    Effect on the ability to drive transp. cf. and fur:In the case of the development of such a side effect as dizziness, the ability to concentrate attention and reactions may be impaired.In this case, patients should refrain from controlling vehicles, mechanisms.
    Form release / dosage:

    Powder for the preparation of solution for intravenous and intramuscular injection, 1000 mg + 500 mg.

    Packaging:

    1000 mg + 500 mg of active substances into 20 ml glass bottles, hermetically sealed with rubber stoppers, crimped with aluminum caps or crimped caps with combined (aluminum caps with safety plastic caps).

    - 1 bottle with the drug and instructions for use are placed in a pack of cardboard.

    - 5 bottles of the drug are packed in a contour mesh box made of polyvinyl chloride film and aluminum foil lacquered or foil-free. Two contour squares with 5 bottles each and instructions for use are placed in a pack of cardboard.

    For hospitals:

    - 10 to 50 vials of the drug and an equal number of instructions for use are placed in a box of cardboard.

    When the preparation is packaged with a solvent

    The solvent - "Water for Injection" in glass ampoules of 10 ml.

    - 1 bottle with the drug and 1 ampoule with solvent are packed in a contour mesh box made of polyvinyl chloride film and foil of aluminum lacquered or without foil.

    One contour mesh package and instructions for use are placed in a pack of cardboard.

    Storage conditions:

    A drug

    In the dark place at a temperature of no higher than 25 ° C.

    Solvent

    At a temperature of no higher than 25 ° C.

    Keep out of the reach of children.

    Shelf life:

    A drug - 3 years.

    Solvent - 4 years.

    Do not use after the expiration date.

    Terms of leave from pharmacies:On prescription
    Registration number:LP-004552
    Date of registration:20.11.2017
    Expiration Date:20.11.2022
    The owner of the registration certificate:Pharmaceuticals, LLCPharmaceuticals, LLC Russia
    Manufacturer: & nbsp
    Information update date: & nbsp18.12.2017
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