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., in t.ch. 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. Active with respect to Haemophilus influenzae, some strains Enterobacter spp. and Enterococcus spp.

Ineffective in relation to Pseudomonas aeruginosa, indol-positive strains Proteus spp., Mycobacterium tuberculosis, Serratia spp., anaerobic microorganisms, methicillin-resistant strains Staphylococcus spp.

Pharmacokinetics:

Time to reach the maximum concentration (TC_m_Oh) with intramuscular injection at a dose of 0.5 and 1 g, respectively - 2 and 1 hour; maximum concentration (С_m_Oh) - 38 and 64 μg / ml. Penetrates into the joints, tissues of the heart and vessels, into the abdominal cavity, the kidneys and urinary tracts, the placenta, the middle ear, the 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 blood plasma. 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 (T1 / 2) with the / m introduction is 1.8 hours. If the renal function T1 / 2 is disturbed, 20-40 hours. It is excreted mainly by the kidneys in the unchanged form: during the first 6h- 60-90%, after 24 hours - 70-95%. After the / m introduction in doses of 0.5 and 1 g of C_m_Ohin urine 1 mg / ml and 4 mg / ml, respectively.

Indications:

Infectious-inflammatory diseases caused by microorganisms sensitive to Cefazolin:

- upper and lower respiratory tract;

- ENT organs (including otitis media);

- urinary and biliary tract;

- pelvic organs;

- skin and soft tissues;

- bones and joints (incl.osteomyelitis);

- endocarditis;

- sepsis;

- peritonitis;

- mastitis;

- wound, burn and postoperative infections;

- syphilis;

- gonorrhea.

Contraindications:Hypersensitivity to cephalosporins and other beta-lactam antibiotics, children up to 1 month (safety of use of the drug is not established). It is not recommended simultaneous reception with anticoagulants and diuretics.

Carefully:Renal failure, intestinal diseases (including colitis in the anamnesis), children's age 1-12 months.

Pregnancy and lactation:

The appointment of cefazolin in pregnancy is permissible if the expected benefit to the mother exceeds the potential risk to the fetus.

When prescribing the drug during lactation, breastfeeding /

Dosing and Administration:

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

The average daily intake for adults is 1-4 g; the frequency of administration 3-4 times a day. The maximum daily dose is 6 g.

The average duration of treatment is 7-10 days.

Patients with impaired renal function require a change in the dosage regimen according towith values of creatinine clearance (CC):

Creatinine clearance (CC)	Plasma Creatinine	Daily dose	Interval between administrations
55 ml / min and more	1.5 mg% and less	Usual Dose	Without changes
54-35 ml / min	3-1.6 mg%	Usual Dose	8h
34-11 ml / min	4.5-3.1 mg%	1/2 of the usual dose	12h
10 ml / min and less	4.6 mg and more	1/2 of the usual dose	18-24h

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 dosage regimen is adjusted depending on the values of the CC:

Creatinine clearance (CC)	Daily dose	Interval between administrations
70-40 ml / min	60% of the average daily dose	12 h
40-20 ml / min	25% of the average daily dose	12 h
5-20 ml / min	10% of the average daily dose	24 h

Preparation of solutions for injection: 0.5 g of the drug is dissolved in 2 ml, 1 g in 4 ml of a 0.5% solution of lidocaine or water for injection. During the dilution, vials should be vigorously shaken until completely dissolved.

When treating children 1-12 months should not be dissolved cefazolin in solutions of lidocaine.

Side effects:

Allergic reactions: hyperthermia, skin rashes, urticaria, skin itching, bronchospasm, eosinophilia, angioedema, 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 of large doses (6 g) - renal dysfunction (in these cases, the dose is reduced, 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 colitis, rarely - cholestatic jaundice, hepatitis.

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

Other: arthralgia.

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

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

Local Reactions: soreness in the injection site.

Overdose:

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

Laboratory indicators: increased concentrations of creatinine, blood urea nitrogen, liver enzymes and bilirubin.

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 ineffective.

Interaction:

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 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 diseases of the gastrointestinal tract, especially colitis.

The drug does not affect the ability to drive and other mechanisms.

Form release / dosage:

Powder for the preparation of solution for intramuscular injection of 0.5 g and 1.0 g.

Packaging:

Powder for solution for intramuscular injection of 0.5 g and 1.0 g

active substance in vials with a capacity of 10 ml.

1 bottle with instructions for use in the pack.

10 bottles together with instructions for use in a cardboard box.

For the hospital: 50 bottles and 5 instructions for use in a cardboard box.

Vials without bundles with an equal number of instructions for use in a group package.

Storage conditions:

In 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 expiration date.

Terms of leave from pharmacies:On prescription

Registration number:P N003079 / 01

Date of registration:21.11.2008

The owner of the registration certificate:KRASFARMA, JSC KRASFARMA, JSC Russia

Manufacturer: & nbsp

KRASFARMA, JSC Russia

Information update date: & nbsp15.10.2015

Illustrated instructions

Instructions

Cefazolin (Cefazolin)