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. 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:The time to reach the maximum concentration (TCmax) with intramuscular (IM) administration in a dose of 1g is 1h; maximum concentration (C max) -64 μg / ml; after intravenous (iv) administration of TCmax at the end of infusion, after iv injection of 1g Cmax - 180 mcg / ml. Penetrates into joints, tissues of the cardiovascular system, into the abdominal cavity, kidneys and urinary tract, 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 (Т 1/2) with the / m administration is 1.8 hours, with the iv administration of -2 hours. If the renal function T1 / 2 is disturbed, 20-40 hours.

Excreted mainly by the kidneys in unchanged form: during the first 6 to 60-90%, after 24 hours - 70-95%. Stam in urine 4000 μg / ml after intravenous injection of 1 g.

Indications:

Bacterial infections caused by microorganisms sensitive to cefazolin: upper and lower respiratory tract, urinary and biliary tract, pelvic organs, skin and soft tissues,bones and joints; endocarditis, sepsis, peritonitis, otitis media, osteomyelitis, mastitis; wound, burn and postoperative infections; syphilis, gonorrhea. Preventive maintenance of surgical infections in the pre- and postoperative period.

Contraindications:Hypersensitivity to cephalosporins and other beta-lactam antibiotics; pregnancy and lactation; newborns (up to 1 month).

Carefully:Renal / hepatic failure, pseudomembranous enterocolitis, children under 1 year.

Dosing and Administration:

Intravenous (jet and drip), intramuscularly.

- The average daily intake for adults is -1 g; the frequency of administration is 2 times a day.

- The maximum daily dose is 6 g (in rare cases - 12 g); the frequency of administration can be increased up to 3-4 times a day.

- The average duration of treatment is 7-10 days.

- For the prevention of postoperative infection - 1 g 30 minutes prior to surgery, 0.5-1 g during surgery and 0.5-1 g every 6-8 hours during the day after the operation.

- Patients with impaired renal function require a change in the dosing regimen, in accordance with the values of creatinine clearance (CK).With SC 55 ml / min or more, or with a plasma creatinine content of 1.5 mg% or less, a full dose can be administered. With SC 54-35 ml / min or with creatinine in plasma 3 - 1.6 mg% - you can enter the full dose with an interval between injections 12 hours. With SC 34 - 11 ml / min or creatinine content in plasma of 4.5-3.1 mg% - 14 medium dose with an interval of 12 hours. Patients with CC 10 ml / min or less, or with a plasma creatinine content of 4.6 mg% and more - 1/2 of the average dose every 18-24 hours. All recommended doses are administered after the initial dose.

The average daily dose for children (over 1 month) is 20-50 mg / kg; 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, correction of the dosing regimen is performed depending on the values of the CC. With SC 70-40 ml / min - 60% of the average daily dose administered after 12 hours. At KK 40-20 ml / min - 25% of the average daily dose with an interval of 12 hours. Children with KK 5-20 ml / min - 10 % of the average daily dose every 24 hours. All recommended doses are administered after the initial dose.

Preparation of solutions:

For intramuscular injection, the drug is dissolved in 4-5 ml of water for injection, 0.9% solution of sodium chloride or 0.25-0.5% solution of procaine.

For intravenous drip, the drug is dissolved in 100 -250 ml of 0.9% solution of sodium chloride or 5% solution of dextrose; 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 for 3-5 minutes.

During the dilution, the vials are vigorously shaken until completely dissolved.

Side effects:

Allergic reactions: hyperthermia, skin rash, urticaria, skin itching, bronchospasm, eosinophilia, Quincke's edema, arthralgia, anaphylactic shock, erythema multiforme, malignant exudative erythema (Stevens-Johnson syndrome).

From the nervous system: convulsions.

From the side of the urinary system: in patients with kidney disease in the treatment of large doses (6 g) - renal dysfunction (in these cases, the dose is reduced and treatment is controlled by the dynamics of urea nitrogen and creatinine in the blood).

On the part of the gastrointestinal tract: nausea, vomiting, diarrhea, abdominal pain, rarely - cholestatic jaundice, pseudomembranous enterocolitis, hepatitis.

From the hematopoiesis: leukopenia, neutropenia, thrombocytopenia, thrombocytosis, hemolytic anemia.

Laboratory indicators: positive Coombs reaction, increased activity of "liver" transaminases, hypercreatininaemia, increased prothrombin time.

Local reactions: with the / m introduction - pain at the injection site, with iv injection - phlebitis.

Others - dysbacteriosis, superinfection caused by antibiotic resistant strains, candidomycosis (including candidiasis stomatitis).

Overdose:

Symptoms: pain, inflammatory reactions and phlebitis at the site of administration; dizziness, headache, paresthesia, possibly the development of seizures (especially in patients with kidney disease).

Laboratory indicators: increased levels of creatinine, blood urea nitrogen, liver enzymes and bilirubin; a positive Coombs reaction; thrombocytosis and thrombocytopenia, eosinophilia, leukopenia, and an increase in prothrombin time.

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, erythromycin, chloramphenicol), since in vitro studies have shown that antagonism exists between them.

With the simultaneous use of cefazolin and "loop diuretics", a blockade of its tubular secretion occurs.

With the simultaneous use of oral anticoagulants or high doses of heparin, control of blood clotting parameters is necessary.

Aminoglycosides increase the risk of kidney damage. Pharmaceutically incompatible with aminoglycosides (mutual inactivation).

Drugs that block tubular secretion, slow down excretion, increase concentration in the blood and increase the risk of developing toxic reactions.

Special instructions:

Patients who had a history of allergic reactions to penicillins, carbapenems, may have increased sensitivity to cephalosporin antibiotics (especially in patients with allergic diseases).

During treatment with cefazolin, positive direct and indirect Coombs probes can be obtained, as well as false positive reactions of urine to sugar.

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, cefazolin is immediately discontinued and appropriate treatment is prescribed (use of drugs that affect peristalsis is contraindicated).

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

Form release / dosage:

Powder for the preparation of solution for intravenous and intramuscular injection of 1 g.

Packaging:

Powder for the preparation of a solution for intravenous and intramuscular injection of 1g in vials of 10 ml and 20 ml. For 1,2, 5 and 10 vials together with the instructions for use are placed in a pack of cardboard.

For 50 bottles together with instructions for use are placed in a box of cardboard (for hospitals).

Storage conditions:

List B. In a dry, the dark place at a temperature of no higher than 25 ° C. Keep out of the reach of children.

Shelf life:

3 years. Do not use after the expiration date.

Terms of leave from pharmacies:On prescription

Registration number:LSR-009187/08

Date of registration:20.11.2008

The owner of the registration certificate:RUZFARMA, LLC RUZFARMA, LLC Russia

Manufacturer: & nbsp

RUZFARMA, LLC Russia

Information update date: & nbsp15.10.2015

Illustrated instructions

Instructions

Cefazolin (Cefazolin)