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, Seiratia spp., Anaerobic microorganisms, methicillin resistant strains of Staphylococcus spp.

Pharmacokinetics:

Time to reach the maximum concentration (TC_m_Oh) with a / m introduction of 1 g - 1h; the maximum concentration in the blood plasma (C_m_Oh) - 64 μg / 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 of the drug (T_1/2) with a / m introduction - 1.8 hours. If the function naboutcheck T_1/2 - 20-40 hours. It is mainly excreted by the kidneys in unchanged form: during the first 6h- 60-90%, after 24 hours - 70-95%. After the / m introduction in a dose of 1 g of C_m_Oh in urine 4 mg / ml.

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

Contraindications:Hypersensitivity to drugs group cephalosporin and other β-lactam antibiotics, children's age (up to 1 month). It is not recommended simultaneous reception with anticoagulants and diuretics.

Pregnancy and lactation:

The drug is contraindicated in pregnancy. Breastfeeding should be discontinued if it is necessary to prescribe the drug during this period.

Dosing and Administration:

Intramuscularly. The average daily intake for adults is 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.

To prevent postoperative infectious complications, 1 g of cefazolin is prescribed 30 minutes prior to surgery, 0.5-1 g during the operation (2 hours or more). 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 dosage regimen in accordance with the values of creatinine clearance (CC): with a CC 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 a plasma creatinine concentration of 3-1.6 mg%, a full dose can be administered,but the intervals between injections should be increased to 8 hours; with SC 34-11 ml / min or creatinine concentration in plasma of 4.5-3.1 mg% - 1/2 dose at intervals of 12 hours; with CC 10 ml / min or less, or with a plasma creatinine concentration of 4.6 mg% or more - 1/2 of the usual dose every 18-24 hours. All recommended doses are administered after the initial dose of 0.5 g. Children older than 1 month - 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 correction of the dosing regimen is performed depending on the values of the CC: at a CC of 70-40 ml / min - 60% of the average daily dose and injected 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 administered after the initial "shock" dose. "

Preparation of solutions for the / m introduction: 1 g of the drug is dissolved in 4 ml of water for injection or 0.5% solution of lidocaine. When treating children from 1 month to 1 year should not be dissolved cefazolin in solutions of lidocaine. During the dilution, vials should be vigorously shaken until completely dissolved.

Dosing regimen and duration of treatment are set individually, taking into account the indications, the severity of the infection, the sensitivity of the pathogen.

Precautions for use: Renal / hepatic insufficiency, intestinal diseases (including colitis in the anamnesis), children's age up to 1 year. If you have any of the listed diseases before using the drug, be sure to consult a doctor.

Side effects:

Allergic reactions: hyperthermia, skin rash, urticaria, skin itching, bronchospasm, eosinophilia, angioedema, arthralgia, anaphylactic shock, erythema multiforme exudative, 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 (dose is reduced and treatment is controlled by the dynamics of the concentration of urea nitrogen and creatinine in the blood).

On the part of the digestive system: nausea, vomiting, diarrhea, abdominal pain, pseudomembranous colitis, cholestatic jaundice, hepatitis.

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

With long-term treatment - dysbacteriosis, superinfection caused by antibiotic-resistant strains, candidamycosis, candidal stomatitis.

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

Local reactions: with the / m introduction - soreness in the injection site.

Overdose:

Symptoms of overdose: pain, inflammatory reactions at the injection site; dizziness, headache, paresthesia, the possible development of seizures (especially in patients with kidney disease).

Laboratory indicators: elevated concentrations of creatinine, blood urea nitrogen, liver enzymes and bilirubin; false-positive reaction of Coombs; 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:

Cefazolin, suppressing the intestinal flora, interferes with the synthesis of vitamin K. Therefore, when used simultaneously with drugs,reducing the aggregation of platelets (non-steroidal anti-inflammatory drugs (NSAIDs), salicylates), the risk of bleeding increases. For the same reason, with simultaneous use with anticoagulants, there is an increase in anticoagulant activity.

With the simultaneous use of cefazolin and "loop diuretics" (furosemide, ethacrynic acid) there is a blockage of his tubular secretion. Aminoglycosides increase the risk of kidney damage. Pharmaceutically incompatible with aminoglycosides (mutual inactivation). Drugs that block tubular secretion, increase concentration in the blood, slow down excretion and increase the risk of developing toxic reactions. 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.

Special instructions:

Patients who had a history of allergic reactions to penicillins, carbapenems, may have increased sensitivity to cephalosporin antibiotics.

During treatment with cefazolinum, false positive and indirect Coombs probes can be obtained, as well as a false positive urine reaction to glucose. When prescribing the drug may exacerbate the diseases of the gastrointestinal tract (GIT), especially colitis. When severe diarrhea, characteristic of pseudomembranous colitis, cefazolin sodium salt should be abolished and appropriate treatment. During treatment, patients should refrain from drinking alcohol. With prolonged use of the drug, control of the picture of peripheral blood and kidney function is necessary; should prevent dysbiosis.

Data on the adverse effects of the drug on the ability to drive vehicles and work with mechanisms, engage in other potentially hazardous activities that require increased concentration and speed of psychomotor reactions are absent.

Form release / dosage:

Powder for solution for intramuscular injection 1,0.

Packaging:

Powder for the preparation of a solution for intramuscular injection of 1.0 g in bottles from a glass tube for medicines with a capacity of 10 ml,hermetically sealed with plugs of rubber compound, crimped aluminum caps. 50 bottles are placed in boxes of cardboard with an attachment of 3 to 5 instructions for medical use of the drug (for hospitals).

1; 5 or 10 bottles are placed in an individual pack of cardboard along with instructions for medical use.

Packaging complete with a solvent - water for injection. The kit includes:

a) 1 bottle with the drug and an ampoule with water for injection for 5 ml;

b) 5 bottles of the drug and 5 ampoules of water for injection for 5 ml;

at) 10 vials of the drug and 10 ampoules of water for injection for 5 ml.

The kit is placed in individual packs of cardboard box along with instructions for medical use, with a ampoule or ampoule knife. When using ampoules with notches, rings or dots, the ampoule knife or ampoule scapegrator is not inserted.

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

Shelf life:2 years. Do not use the drug after the expiration date.

Terms of leave from pharmacies:On prescription

Registration number:PL-000885

Date of registration:18.10.2011

Date of cancellation:2016-10-18

The owner of the registration certificate:BIOCHEMIST, OJSC BIOCHEMIST, OJSC Russia

Manufacturer: & nbsp

BIOCHEMIST, OJSC Russia

Information update date: & nbsp13.10.2015

Illustrated instructions

Instructions

Cefazolin (Cefazolin)