Cefazolin - instructions for use, dose, side effects, contraindications

Cephalosporin antibiotic of the first generation for parenteral use. It acts bactericidal, disrupting the synthesis of the cell wall of microorganisms.

Has a wide spectrum of action, is active against Gram-positive (Staphylococcus spp., Staphylococcus aureus (not producing and producing penicillinase), Streptococcus pneumoniae), Corynebacterium diphtheriae, Bacillus anthracis) and Gram-negative (Neisseria meningitidis, Neisseria gonorrhoeae, Shigella spp., Salmonella spp. , Escherichia coli, Klebsiella spp., Treponema spp., Leptospira spp.) Of microorganisms. It is active against Haemophilus influenzae, some strains of Enterobacter spp. and Enterococcus spp.

Ineffective against Pseudomonas aeruginosa, indolpositive strains of Proteus spp., Mycobacterium tuberculosis, Serratia spp., Anaerobic microorganisms, methicillin-resistant strains of Staphylococcus spp.

Pharmacokinetics:Time to reach the maximum concentration in the blood plasma (TCmax) with intramuscular (IM) administration in a dose of 0.5 g and 1 g, respectively - 2 hours and 1 hour; the maximum concentration in the blood plasma (Cmax) is 38 μg / ml and 64 μg / ml, respectively; after intravenous (iv) administration of TCmax - at the end of infusion, after intravenous administration of 1g Cmax -180mkg / ml. Penetrates into the joints, tissues of the heart and blood vessels, into the abdominal cavity, kidneys and urinary tracts, placenta, middle ear, respiratory tract, skin and soft tissues. In small amounts excreted in breast milk. Concentration in the tissue of the gallbladder and bile is much higher than in the serum. With obstruction of the gallbladder, the concentration in the bile is less than in the plasma. The volume of distribution is 0.12 l / kg. The connection with plasma proteins is 85%. The half-life period (T1 / 2) with the / m introduction is 1.8 hours, with the IV introduction - 2 hours. If the kidney function is T1 / 2-20-40h.

Excreted mainly by the kidneys in unchanged form: during the first 6 to 60-90%, after 24 hours - 70-95%. After the / m introduction in doses of 0.5 and 1 g Cmax in urine 1 mg / ml and 4 mg / ml, respectively.

Indications:

Infectious-inflammatory diseases caused by microorganisms sensitive to cefazolin:

- upper and lower respiratory tract;

- LOP - organs (including otitis media);

- urinary and biliary tract;

- pelvic organs;

- skin and soft tissues;

- bones and joints (including osteomyelitis);

- endocarditis;

- sepsis, peritonitis, mastitis;

- wound, burn and postoperative infections;

- gonorrhea, syphilis.

Preventing surgical infections in the pre - and postoperative period.

Contraindications:Hypersensitivity (including to other cephalosporins, penicillins), children under the age of one month.

Carefully:Renal failure, intestinal diseases (including colitis in the anamnesis), children age from 1 -12 months.

Pregnancy and lactation:Cefazolin can be used during pregnancy if the intended benefit to the mother is greater than the potential risk to the fetus. If it is necessary to use the drug during lactation, breastfeeding should be stopped.

Dosing and Administration:

In / in (spray or drip) and / m.

Use only freshly prepared and clear solutions. The possible yellowish color of the solution after dissolving the powder is not an indication of any change in the properties of the preparation or of differences in its therapeutic effectiveness.

The dosage regimen and the duration of the course of treatment are set individually, taking into account the indications, the severity of the course and the localization of the infection, the sensitivity of the pathogen.

The average daily intake for adults -1 - 4 g; the frequency of administration is 3-4 times a day. The maximum daily dose is 6 g. The average duration of treatment is 7-10 days.

For the prevention of postoperative infection - iv, 1 g for 0.5-1 h before the operation, 0.5-1 g - during the operation and 0.5-1 g every 8 h during the first day after the operation .

Patients with impaired renal function require a change in the dosage regimen in accordance with the values of creatinine clearance (CC): at a YS of 55 ml / min or more, or with a plasma creatinine concentration of 1.5 mg% or less, a full dose can be administered; with SC 54-35 ml / min or creatinine concentration in plasma of 3-1.6 mg% can be administered, a full dose, but the intervals between injections need to be increased to 8 hours; with SC 34-11 ml / min or creatinine concentration in the plasma of 4.5-3.1 mg% -1/2 doses at intervals of 12 h; with CC 10 ml / min or less, or with a plasma creatinine concentration of 4.6 mg% and more than 1/2 of the usual dose every 18-24 hours. All recommended doses are administered after the administration of an initial dose corresponding to the severity of the infection. Children 1 month.and older - 25 - 50 mg / kg / day; In severe infection, the dose can be increased to 100 mg / kg / day. Multiplicity of administration - 3 - 4 times a day. In children with impaired renal function, the dosage regimen is adjusted depending on the values of the CC: in the case of 70 to 40 ml / min, 60% of the average daily dose and administered every 12 hours; with KK 40 - 20 ml / min - 25% of the average daily dose with an interval of 12 hours; with KK 5-20 ml / min -10% of the average daily dose every 24 hours. All recommended doses are applied after the introduction of an initial dose corresponding to the severity of the infection.

Preparation of solutions

For intramuscular administration: 1 g of the drug is dissolved in 4 ml of water for injection or in a 0.9% solution of sodium chloride, or 0.25-0.5% solution of procaine. For intravenous drip, the drug is dissolved in 50-100 ml of a 0.9% solution of sodium chloride or 5-10% solution of dextrose, Ringer's solution, 5% sodium bicarbonate solution, depending on the dose of the drug; infusion is carried out for 20 - 30 minutes (rate of administration of 60 - 80 drops per minute).

For intravenous fluid administration, a single dose of the drug is diluted in. 10 ml of 0.9% sodium chloride solution and injected slowly over 3-5 min.

Side effects:

From the digestive system: loss of appetite, glossitis, heartburn, abdominal pain, nausea and vomiting, diarrhea, pseudomembranous colitis, cholestatic jaundice, hepatitis.

Allergic reactions: hyperthermia, skin rash, urticaria, skin itch, bronchospasm, eosinophilia, Quincke's edema, arthralgia, allergic nephritis, anaphylactic shock, multiform exudative erythema, including Stevens-Johnson syndrome.

From the nervous system: dizziness, convulsions.

On the part of the hematopoiesis system: reversible neutropenia and leukopenia, thrombocytopenia, thrombocytosis, hemolytic anemia.

From the urinary system: an increase in the concentration of urea nitrogen, blood, hypercreatininaemia (usually in patients with impaired renal function when treated in large doses (6 g) - in these cases, the dose is reduced and treatment is controlled by the dynamics of the concentration of urea nitrogen and creatinine in the blood).

Local reactions: with the / m introduction - soreness, tissue tightening at the injection site; with iv introduction - phlebitis.

Laboratory indicators: a false positive reaction - Coombs, reversible hypoprothrombinemia, an increase in prothrombin time,increased activity of "hepatic" transaminases and alkaline phosphatase, an increase in the concentration of total bilirubin.

Other: dysbacteriosis, superinfection caused by antibiotic resistant strains, candidiasis stomatitis and vaginitis.

Overdose:

Symptoms: dizziness, headache, paresthesia, possibly the development of seizures (especially in patients with kidney disease).

Laboratory indicators: increased concentration of creatinine, blood urea nitrogen, activity of liver enzymes and bilirubin; thrombocytosis.

Treatment: immediately stop the introduction of the drug, carefully monitor the vital functions of the body and the relevant laboratory indicators; therapy is symptomatic. In severe cases, hemodialysis is possible. Peritoneal dialysis is not effective.

Interaction:

Do not use cefazolin together with antibacterial drugs that have a bacteriostatic mechanism of action (tetracyclines, sulfonamides, macrolides, lincosamides, chloramphenicol), since in vitro studies have shown that antagonism exists between them.

With the simultaneous use of oral anticoagulants or high doses of heparin, it is necessary to monitor the parameters of blood coagulability ... Aminoglycosides increase the risk of kidney damage.

Pharmaceutically incompatible with aminoglycosides (mutual inactivation). Drugs that block tubular secretion, including probenecid, slow excretion, increases concentration in the blood and increase the risk of toxic reactions.Cefazolin can cause disulfiram-like reactions when used simultaneously with ethanol.

Cefazolin suppressing intestinal flora prevents the synthesis of vitamin K. Therefore, while the use of drugs that reduce platelet aggregation (non-steroidal anti-inflammatory drug (NSAID), salicylates), increases the risk of bleeding. For the same reason, with simultaneous use with anticoagulants, there is an increase in anticoagulant activity.

Special instructions:Patients who had a history of allergic reactions to penicillins, carbapenems, may be sensitive to the antibiotic tsofalosporinovym.

During treatment with cefazolinum, it is possible to obtain false positive and indirect Coombs probes, as well as a false positive urine reaction to glucose if they are performed using a Benedict solution or Felling solution. When prescribing the drug may exacerbate diseases of the gastrointestinal tract, especially colitis. In the presence of severe persistent diarrhea, it is necessary to consider the likelihood of developing pseudomembranous colitis associated with the use of an antibiotic. In this case, immediately cefazolin treatment is stopped and appropriate treatment is prescribed (use of drugs that affect peristalsis is contraindicated).

Safety of use in preterm infants and children of the first month of life is not established.

In case of signs of allergic reactions, cefazolin should be discontinued and appropriate symptomatic treatment should be prescribed (epinephrine; prednisolone, dexamethasone; antihistamines). Continuous use of any antibiotic can lead to the multiplication of insensitive microorganisms - superinfection.

With prolonged use of the drug, control of the picture of the peripheral blood picture and kidney function is necessary.

Effect on the ability to drive transp. cf. and fur:Patients should be careful when driving a car and engaging in other potentially hazardous activities that require increased attention and speed of psychomotor reactions.

Form release / dosage:

Powder for solution for intravenous and intramuscular injection, 1.0 g.

Packaging:

By 1.0 g of active substance (cefazolin) in a glass vial, hermetically sealed with a rubber stopper, followed by a cap of aluminum. 1 bottle with instructions for use in a pack of cardboard. 5 bottles with instructions for use in a cardboard box.

Storage conditions:In a dry, dark place at a temperature of 5 ° C to 25 ° C. Keep out of the reach of children.

Shelf life:3 years. Do not use after the expiration date printed on the package.

Terms of leave from pharmacies:On prescription

Registration number:LS-000084

Date of registration:16.02.2010

The owner of the registration certificate:LEKKO, ZAO LEKKO, ZAO Russia

Manufacturer: & nbsp

LEKKO, ZAO Russia

Information update date: & nbsp14.10.2015

Illustrated instructions

Instructions

Cefazolin (Cefazolin)