Cefazolin-Ferein - 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 Hnt its coccus 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 (Tcmah) with intramuscular (IM) administration in a dose of 500 and 1000 mg, respectively - 2 and 1 hour; maximum concentration (Сmax) 38 and 64 μg / ml; after intravenous (iv) introduction of TSmah - at the end of infusion, after intravenous administration of 1000 mg Cmah - 180 mcg / ml. It penetrates into the joints, tissues of the cardiovascular system, into the abdominal cavity, kidneys and urinary tracts, the placenta, the middle ear, the respiratory tract, skin and soft tissues. It penetrates the placental barrier and is found in the amniotic fluid. 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 introduction is 1.8 hours, with the intravenous administration of -2 hours. If the kidney function T 1/2 - 20-40 hours.

It is excreted mainly by the kidneys in an unchanged form: during the first 6h- 60-90%, after 24 hours - 70-95%. FROMmah in the urine of 1000 μg / ml and 4000 μg / ml after the / m administration at doses of 500 mg and 1000 mg respectively.

Indications:Infectious and inflammatory diseases of the 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, peritonitis, 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; newborn period.

Carefully:Renal / hepatic insufficiency, intestinal diseases (pseudomembranous enterocolitis, nonspecific ulcerative colitis in the anamnesis), children under 1 year.

Pregnancy and lactation:

The use of cefazolin in pregnancy is contraindicated.

If it is necessary to prescribe the drug during lactation, breastfeeding should be stopped.

Dosing and Administration:

Intravenous (jet and drip), intramuscularly.

The dose of the drug is set individually, taking into account the severity of the disease, the localization of infection and the sensitivity of the pathogen, as well as age and body weight, kidney function.

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 - I g for 30 minutes before the operation, 0.5 g - during the operation 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 a plasma creatinine content of 3-1.6 mg%, a full dose can be administered, but the intervals between injections can be increased to 12 hours. In the CC, 34-11 ml / min or with creatinine content in plasma 4.5-3.1 mg% - Ug doses at intervals 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 h. All recommended doses are administered after the initial dose.

The average daily dose for children (over 1 month) is 20-50 mg / kg; with severe course of infection, the dose of the drug 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. F Preparation of solutions:

For intramuscular injection, the drug is dissolved in 4-5 ml of water for injection, isotonic sodium chloride solution or 0.25-0.5% solution of novocaine. For intravenous drip, the drug is dissolved in 100-150 ml of isotonic sodium chloride solution or 5% glucose solution; 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 isotonic 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 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 the treatment is controlled by the dynamics of the nitrogen content of urea and creatinine in the blood).

From the gastrointestinal tract: nausea, vomiting, diarrhea, abdominal pain, pseudomembriosis enterocolitis, rarely - cholestatic jaundice, hepatitis.

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

Laboratory indicators: positive Coombs reaction, increased activity of "liver" transaminases, hypercreatininaemia, an increase in prothrombin time. Local reactions: with the / m introduction - soreness (at the injection site), with / in the introduction - phlebitis.

Other: dysbacteriosis, superinfection caused by antibiotic resistant strains, candidamycosis (including candidiasis stomatitis).

Overdose:

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

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) because of their antagonism.

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, increase the concentration of cefazolin in the blood plasma, slow the excretion of cefazolin, and increase the risk of developing toxic reactions.

Special instructions:

Patients with impaired renal excretory function need correction of the dosing regimen of cefazolin.

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

During treatment with cefazolin, positive direct and indirect Coombs probes can be obtained, as well as a false positive urine reaction 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, immediately stop cefazolin therapy and prescribe appropriate treatment (the 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 solution for intravenous and intramuscular injection, 1.0 g.

Packaging:Powder for the preparation of solution for intravenous and intramuscular injection of 1.0 g of active substance in the vial; powder for the preparation of a solution for intramuscular injection of 1.0 g of active substance in a vial. For 1 bottle with the drug, along with instructions for use in a pack of cardboard.

For 5 vials with the drug in a contour squamous packaging, 1 or 2 contour packs with instructions for use in a pack of cardboard. For 5 or 10 vials with the drug, along with instructions for use in a pack with an insert with cells for bottles in 1 or 2 rows of cardboard.

Storage conditions:

List B. In the dark place at a temperature of 15 - 30 ° C. Keep out of reach of children.

Shelf life:2 years. Do not use after the date shown on the package.

Terms of leave from pharmacies:On prescription

Registration number:P N000982 / 01

Date of registration:13.10.2008

The owner of the registration certificate:BRYNTSALOV-A, CJSC BRYNTSALOV-A, CJSC Russia

Manufacturer: & nbsp

BRYNTSALOV-A, CJSC Russia

Information update date: & nbsp15.10.2015

Illustrated instructions

Instructions

Cefazolin-Ferein® (Cefazolin-Ferein®)