Cefazolin - instructions for use, dose, side effects, contraindications

Pharmacodynamics: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) 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, metitsillin-resistant strains of Staphylococcus spp.

Pharmacokinetics:

Time to reach the maximum concentration (TC_max) with intramuscular (IM) administration in a dose of 0.5 g and 1 g for 2 hours and 1 hour, respectively; maximum concentration (С_max) Were 38 μg / ml and 64 μg / ml, respectively. After intravenous (iv) introduction of TS_max - at the end of the infusion, after intravenous administration of 1 g of C_max -180 mcg / ml.

It 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. It penetrates the placental barrier and is found in the amniotic fluid. In the milk of nursing mothers is detected in low concentrations. 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 (T_1/2) with the / m introduction - 1.8 hours, with the / in the introduction - 2 hours. If the kidney T_1/2 - 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 the / m introduction in doses of 0.5 g and 1 g of C_max in urine - 1 mg / ml and 4 mg / ml, respectively.

Indications:Infectious and inflammatory diseases of the upper and lower respiratory tract, upper respiratory organs (including otitis media), urinary and biliary tract, pelvic, skin, soft tissue, bone and joints (including osteomyelitis); endocarditis, sepsis, peritonitis, mastitis; wounded, burn infections; syphilis, gonorrhea. Preventive maintenance of surgical infections in the pre- and postoperative period.

Contraindications:Hypersensitivity to cephalosporin drugs and other beta-lactam antibiotics, novorozhdennocti period (up to 1 month).

Carefully:Chronic kidney failure, intestinal diseases (history of ulcerative colitis), 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:

Enter in / m or in / in (struyno or drip).

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

Average daily dose for adults - 1 g; the frequency of administration is 2 times a day. The maximum daily dose is 6 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 infectious complications prescribe 1 g of cefazolin 30 minutes prior to surgery; 0.5-1 g during the operation and 0.5-1 g every 6-8 hours during the day after the operation.

In patients with impaired renal function, the dosage regimen of cefazolin is set taking into account the values of creatinine clearance (CC). With SC more than 55 ml / min, the dosing regimen, as a rule, does not require correction. With SC 54-35 ml / min, a single dose may remain unchanged with an interval between administrations of 12 hours. With QA 34-11 ml / min, single dose should be reduced by 2 times with intervals between administrations

11 hours. With QC less than 10 ml / min, one half of the usual dose is prescribed every 18-24 hours. All recommendations for correction of the dosing regimen are applied after the establishment of an initial dose corresponding to the severity of the infection.

Average daily dose for children over 1 month old - 20-50 mg / kg; In severe infection, the dose may be increased to 100 mg / kg per 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. 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 "shock" dose corresponding to the severity of the infection.

Preparation of solutions

For the / m introduction, water for injection, 0.9% sodium chloride solution or 0.25-0.5% procaine solution is used as the solvent. 0.5 g of the preparation is dissolved in 2 ml of solvent, 1 g in 4 ml of solvent).

For intravenous administration, a single dose of the drug is dissolved in 10 ml of 0.9% sodium chloride solution and injected slowly for 3-5 minutes.

For IV injection, the drug is dissolved in 50-100 ml of a 5-10% solution of dextrose or 0.9% solution of sodium chloride; infusion is carried out for 20-30 minutes (rate of administration of 60-80 drops per minute).

During the dilution, the vials are vigorously shaken until completely dissolved.

Side effects:

Allergic reactions: hyperthermia, skin rash, urticaria, skin itching, bronchospasm, eosinophilia, angioedema, arthralgia, anaphylactic shock, erythema multiforme,malignant exudative erythema (Stevens-Johnson syndrome).

Co side of the nervous system: convulsions.

Co side of the urinary system: in patients with kidney disease in the treatment of large doses (6 g) - a violation of kidney function (in these cases, the dose is reduced and treatment is controlled by the dynamics of the content of urea nitrogen and creatinine in the blood).

Co side of the gastrointestinal tract: nausea, vomiting, diarrhea, abdominal pain, rarely - pseudomembranous colitis, cholestatic jaundice, hepatitis.

Co sides of hemopoiesis: leukopenia, neutropenia, thrombocytopenia, thrombocytosis, hemolytic anemia.

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

Local reactions: with the / m introduction - pain in the injection site, with / in the introduction - phlebitis.

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

Overdose:

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

Laboratory indicators: increased concentration of creatinine, blood urea nitrogen, activity of 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:

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, blockade of its tubular secretion occurs.

With the simultaneous use of indirect anticoagulants or high doses of heparin, blood coagulation parameters control is necessary.

Aminoglycosides increase the risk of kidney damage. Pharmaceutically incompatible with aminoglycosides (mutual inactivation).

Drugs that block tubular secretion, slow the release of cefazolin, increase its concentration in the blood plasma, and increase the risk of developing toxic reactions.

Special instructions:

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

In patients who have a history of allergic reactions to penicillins, there is a cross-sensitivity to cephalosporins.

During treatment with cefazolinum it is possible to obtain false positive and indirect samples of Coombs, as well as a false positive reaction of urine to sugar. In prescribing the drug, the escalation of diseases of the gastrointestinal tract, especially colitis, is possible. 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).

Effect on the ability to drive transp. cf. and fur:Given the likelihood of side effects from the nervous system,During the treatment period, 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 the preparation of solution for intravenous and intramuscular injection 0.5 g and 1 g.

Packaging:

By 0.5 g or 1 g of active substance into a colorless glass vial (type I USP) with a capacity of 10 or 20 ml, sealed with a rubber stopper with aluminum rolling and a plastic lid.

1 The bottle together with the instruction for use is placed in a pack of cardboard.

Storage conditions:Store in a dry, dark place at a temperature of no higher than 20 ° 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:П N012330 / 01

Date of registration:19.02.2010

The owner of the registration certificate:M. J. Biofarm Pvt. Ltd.M. J. Biofarm Pvt. Ltd. India

Manufacturer: & nbsp

M.J.Biofarm Pvt.Ltd India

Representation: & nbspM.J. BIOFARM Pvt. Ltd. division of the corporation MJ Group M.J. BIOFARM Pvt. Ltd. division of the corporation M.J.Group India

Information update date: & nbsp14.10.2015

Illustrated instructions

Instructions

Cefazolin (Cefazolin)