Cefazolin-AKOS - 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 (TCmax) with intramuscular injection at a dose of 0.5 and 1 g, respectively - 2 and 1 hour; the maximum concentration (C max) is 38 and 64 μg / ml; after intravenous administration of TCSax - at the end of infusion, after intravenous administration of 1 g of C max - 180 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 (T1 / 2) for intramuscular injection is 1.8 hours, with intravenous administration -2 hours. If the renal function T1 / 2 is disturbed, 20-40 hours. It is mainly excreted by the kidneys in the unchanged form: during the first 6 to 60-90% , after 24 hours - 70-95%. After intramuscular injection in doses of 0.5 and 1 g of Cmax in urine 1 mg / ml and 4 mg / ml, respectively.

Indications:Infectious and inflammatory diseases caused by microorganisms sensitive to the preparation: bacterial infections of the upper and lower respiratory tract, LOP-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 antibiotics of cephalosporin series and other beta-lactam antibiotics, newborns (up to 1 month), pregnancy, lactation.

Carefully:Renal and / or hepatic insufficiency, intestinal diseases (including colitis in history), children's age (up to 1 year).

Dosing and Administration:

Intravenous (jet or drip), intramuscularly.

The average daily intake for adults is 1-4 g; the frequency of administration is 2-4 times a day. The maximum daily dose is 6 g (in rare cases - 12 g). The average duration of treatment is 7-10 days. For the prevention of postoperative infection, intravenously, 1 g for 0.5-1 h before surgery, 0.5-1 g during surgery and 0.5-1 g every 8 hours during the first 24 hours 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 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 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 dose. For intramuscular injection, 0.5 g of the drug is dissolved in 2-3 ml of 0.9% sodium chloride solution, 0.25-0.5% procaine solution, or water for injection, 1 g in 4-5 ml sodium chloride solution 0.9 %, a procaine solution of 0.25-0.5%, or water for injection.The resulting solution is injected deep into the muscle.

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. When intravenous drip introduction of the drug (0.5 g and 1 g) is diluted in 100-250 ml of 0.9% sodium chloride solution or 5% dextrose solution and administered for 20-30 minutes (rate of administration of 60-80 drops per minute ).

During the dilution, vials should be vigorously shaken until completely dissolved.

Side effects:

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

From the digestive system: nausea, vomiting, diarrhea, abdominal pain, pseudomembranous enterocolitis, rarely - cholestatic jaundice, hepatitis.

On the part of the organs of hematopoiesis: leukopenia, neutropenia, thrombocytopenia, thrombocytosis, hemolytic anemia.

With long-term treatment - dysbacteriosis, superinfection caused by antibiotic-resistant strains, candidiasis (including candidiasis stomatitis).

Laboratory indicators: a positive Coombs reaction, an increase in the activity of "liver" transaminases, hypercreatininaemia, an increase in prothrombin time.

Local Reactions: with intramuscular injection - soreness (at the injection site), with intravenous injection - phlebitis.

Interaction:It is not recommended simultaneous reception with anticoagulants and diuretics. With the simultaneous use of cefazolin and "loop diuretics", a blockade of its tubular secretion occurs. 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.

Special instructions:Patients who had a history of allergic reactions to penicillins, carbapenems, may have increased 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 glucose. When prescribing the drug may exacerbate diseases of the gastrointestinal tract, especially colitis.

Form release / dosage:Powder for the preparation of solution for intravenous and intramuscular injection 0.5 g, 1 g.

Packaging:

0.5 g and 1 g of active substance in a vial of colorless glass with a capacity of 10 ml or 20 ml or in a bottle of dark glass with a capacity of 10 ml or 20 ml.

1, 5 and 10 vials with instructions for use in a pack of cardboard. 50 . vials with an equal number of instructions for use in a cardboard box for hospitals.

Solvent:

- "Water for injection" in glass ampoules of 5 ml;

- "Sodium chloride solvent for the preparation of medicinal forms for injection 0.9%" in glass ampoules of 5 ml;

1 bottle with the drug, 1 or 2 ampoules of the solvent in a contoured cell pack from a polyvinyl chloride film.

1 contour mesh package with instructions for use with a scarifier ampoule in a pack of cardboard.

1 vial with drug, 1 or 2 ampoules with a solvent,with instruction for use and a scapegrator ampoule in a pack or box of cardboard.

5 bottles of the drug in a contour cell pack from a polyvinyl chloride film.

1, 2 contour mesh packings with vials of the preparation and instructions for use in a pack of cardboard.

1 contour mesh package with vials of the preparation, 1 or 2 contour mesh packages with solvent ampoules (5 ampoules each), instructions for use and ampoule ampoule in a pack of cardboard.

When using ampoules with a kink ring or with an incision and a point, the scarifier is not inserted.

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

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

Terms of leave from pharmacies:On prescription

Registration number:P N002895 / 01

Date of registration:20.03.2009

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

Manufacturer: & nbsp

SYNTHESIS, OJSC Russia

Information update date: & nbsp14.10.2015

Illustrated instructions

Instructions

Cefazolin-AKOS (Cefazolin-AKOS)