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 (non-producing and producing penicillinase, including 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 and Enterococcus.

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

Pharmacokinetics:The period of maximum concentration with intramuscular injection at a dose of 0.5 and 1 g, respectively - 2 and 1 hour; the maximum concentration is 38 and 64 μg / ml; after intravenous administration, the period of maximum concentration is at the end of infusion, after intravenous administration of 1 g the maximum concentration is 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 with intramuscular injection is 1.8 hours, with intravenous administration - 2 hours. When the renal function is impaired, the half-life period is 20-40 hours. It is excreted mainly by the kidneys in unchanged form: within the first 6 hours -60-90%, after 24 hours - 70-95%. After intramuscular injection at doses of 0.5 and 1 g, the maximum concentration in urine is 1 mg / ml and 4 mg / ml, respectively.

Indications:

Bacterial infections of the upper and lower respiratory tract, JIOP-organs (including otitis media), urinary and biliary tract, pelvic organs (including gonorrhea), skin and soft tissues, bones and joints (including osteomyelitis), endocarditis , sepsis, peritonitis, mastitis, wound, burn and post-surgical infections, syphilis.

Preventive maintenance of surgical infections in the pre- and postoperative period.

Contraindications:Hypersensitivity; the period of newborns (up to 1 month).

Carefully:Renal failure, intestinal diseases (including colitis in history), children under 1 year.

Pregnancy and lactation:

At pregnancy appoint or nominate only on vital indications (strictly controlled researches it was not spent).

The action category for fetus by FDA is B.

If it is necessary to prescribe the drug during lactation, breastfeeding should be stopped (cefazolin penetrates into breast milk).

Dosing and Administration:

Intramuscularly, intravenously (struyno and drip). 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.

For the prevention of postoperative infection - intravenously, 1 g for 0.5-1 hour 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 creatinine concentration in plasma of 3-1.6 mg%, a full dose can be administered but intervals between injections should 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 dose at intervals of 12 hours; 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 initial dose of 0.5 g.

Children from 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 creatinine clearance (CC): in the case of CC 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 5-20ml / min - 10% of the average daily dose every 24 hours. All recommended doses are given after the initial "shock" dose. For infections of moderate severity caused by sensitive Gram-positive microorganisms, a single dose for adults is 0.25-0.5 g every 8 hours. With pneumococcal pneumonia - 0.5 g every 12 hours, with acute uncomplicated urinary tract diseases - 1 g every 12 hours.

Preparation of solutions for injection and infusion: 0.5 g of the drug is dissolved in 2 ml of water for injection, 1 g in 4 ml of water for injection. For intravenous bolus administration, the resulting solution is diluted with 5 ml of water for injection, then injected slowly, for 3-5 minutes. For intravenous drip, 50-100 ml of 5-10% dextrose solution, 0.9% sodium chloride solution, Ringer's solution, 5% sodium bicarbonate solution are diluted with the drug.

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

Side effects:

Allergic reactions: hyperthermia, skin rash, urticaria, skin itch, toxic epidermal necrosis, bronchospasm, eosinophilia, fever, angioedema, Quincke's edema, arthralgia, anaphylactic shock, multiforme exudative erythema (including Stevens-Johnson syndrome).

From the nervous system: convulsions.

From the urinary system: in patients with kidney disease in the treatment high doses (6 g) - a violation of kidney function (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).

From the digestive system: nausea, vomiting, diarrhea, abdominal pain, pseudo-membranous colitis, cholestatic jaundice, hepatitis.

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

Local reactions: the formation of infiltrates and abscesses, phlebitis, thrombophlebitis.

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

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

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 and indirect

samples of Coombs, as well as a false positive urine reaction to sugar. When prescribing the drug may exacerbate diseases of the gastrointestinal tract, especially colitis. During the period of treatment, care must be taken when driving vehicles and engaging in other potentially hazardous activities requiring 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 into 10 ml glass vials, hermetically sealed with rubber stoppers,Crimped aluminum caps or caps aluminum combined.

Vials with a preparation of 50 pieces are placed in a group package in boxes of cardboard with partitions with an equal number of instructions for the use of the drug.

1 bottle with the drug and instructions for use are placed in a pack of cardboard.

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 after the expiry date printed on the package.

Terms of leave from pharmacies:On prescription

Registration number:LS-002273

Date of registration:29.11.2011

The owner of the registration certificate:BIOSINTEZ, PAO BIOSINTEZ, PAO Russia

Manufacturer: & nbsp

BIOSINTEZ, PAO Russia

Information update date: & nbsp13.10.2015

Illustrated instructions

Instructions

Cefazolin (Cefazolin)