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CEFAZOLIN-BHFZ powder for solution for injection 500 mg, powder for solution for injection 1000 mg

Instruction manual

For medical use of the drug

Structure:

Active ingredient: cefazolin;

1 vial contains cefazolin (in the form of cefazolin sodium salt) 500 mg or 1000 mg.

Dosage form.

Powder for injection.

Basic physical and chemical properties: white or almost white powder. Very hygroscopic.

Pharmacotherapeutic group.

Antimicrobial agents for systemic use. cephalosporins. code atx j01d b04.

Pharmacological properties.

Pharmacodynamics

Cefazolin is a first-generation semisynthetic cephalosporin antibiotic for parenteral administration. The mechanism of antimicrobial action is associated with the suppression of the transpeptidase enzyme, the blockade of mucopeptide biosynthesis in the bacterial cell wall. Cefazolin is a broad-spectrum antibiotic that is active against many gram-positive and gram-negative microorganisms. Gram-positive microorganisms are sensitive to the drug: Staphylococcus aureus (including penicillinase producing strains), Staphylococcus epidermidis (methicillin-resistant staphylococci are also resistant to cefazolin), group A β-hemolytic streptococci, and many streptococcus straptides Streptococcus (Diplococcus) pneumoniae, Corynebacterium diphtheriae, Bacillus anthracis; and gram-negative microorganisms: Escherichia coli, Proteus mirabilis, Klebsiella spp., Enterobacter aerogenes, Haemophilus influenzae, Neisseria meningitidis, Neisseria gonorrhoeae, Shigella spp., Salmonella spp., Treponema spp., Leptospira spp.

Most indole-positive strains of Proteus (Proteus vulgaris), as well as Enterobacter cloacae, Morganella morganii, Providencia rettgeri, Serratia, Pseudomonas spp., Acinetobacter spp., As well as anaerobic cocci Peptococcus, Peptostreptococcus, are resistant to C. Rickettsia, viruses, fungi and protozoa are resistant to the action of the drug.

Pharmacokinetics

With intramuscular administration, the drug is rapidly absorbed; about 90% of the administered dose binds to plasma proteins. The maximum concentration in the blood during intramuscular administration is observed 1 hour after injection and is 37–64 μg / ml. With intravenous administration, the maximum concentration of the drug is determined immediately after administration and is 185 μg / ml.

The therapeutic concentration in the blood lasts 8-12 hours. The drug penetrates well into tissues and body fluids, penetrates through the inflamed synovial membrane into the joints and into the abdominal cavity. Cefazolin easily crosses the placental barrier. The drug is metabolized in an insignificant amount in the liver and excreted with bile. A significant portion of the administered dose of the drug (about 60–90%) is excreted in the first 6 hours, after 24 hours - 70–95% and excreted unchanged in the urine. A small amount of the drug is excreted in breast milk.

The elimination half-life is about 2 hours after intramuscular administration, 1.8 hours after intravenous administration. In case of impaired renal function, the elimination half-life is 3–42 hours.

Clinical characteristics.

Indications.

Infectious and inflammatory diseases caused by microorganisms sensitive to the drug:

  • respiratory tract infections;
  • urinary tract infections;
  • infections of the skin and soft tissues;
  • biliary tract infections;
  • infections of bones and joints;
  • endocarditis;
  • sepsis;
  • prevention of infections during surgery.

Contraindications

  • Hypersensitivity to cefazolin, to any antibiotic of the cephalosporin series. history of severe hypersensitivity reactions (e.g., anaphylactic reactions) to any other type of beta-lactam antibacterial agents (penicillins, monobactams, carbapenems).

Interaction with other drugs and other types of interactions.

Probenecid: a decrease in renal clearance of cefazolin, which contributes to its cumulation and a prolonged increase in the concentration of the drug in the blood.

Anticoagulants (e.g. warfarin, heparin): increased effect of oral anticoagulants and increased risk of bleeding.During the use of cefazolin with anticoagulants in high doses, coagulation parameters should be monitored.

Vitamin K: Some cephalosporins, such as cefazolin, can lead to impaired metabolism of vitamin K, especially in cases of deficiency, which may require additional administration of vitamin K.

Aminoglycosides, loop diuretics (furosemide, ethacrine acid), other nephrotoxic drugs (including colistin, polymyxin B, vancomycin): increased risk of nephrotoxicity due to blockage of tubular secretion of cefazolin. Concomitant treatment with nephrotoxic drugs should be avoided. If such a combination is necessary, the dose should be reduced and treatment should be carried out under the control of renal function (urea nitrogen, blood creatinine).

Bacteriostatic antibacterial agents (tetracyclines, sulfanilamides, erythromycin, chloramphenicol): should not be used together, it is possible to reduce the bactericidal effect of cefazolin.

Other beta-lactam antibiotics: may develop cross-allergic reactions.

Hormonal contraceptives: as with other antibiotics, the effectiveness of hormonal contraceptives decreases, therefore it is recommended to use additional (non-hormonal) methods of contraception during treatment.

Live typhoid vaccine, BCG vaccine: like other antibiotics, cefazolin can reduce the therapeutic effect of live vaccines. An interval of at least 24 hours between the last dose of the antibiotic and the live vaccine should be observed.

Ethanol: disulfiram-like reactions are possible.

Laboratory studies: a false-positive result of glucosuric tests is possible when using non-enzymatic methods using solutions of Benedict, Feling or Clinitest tablets; cefazolin does not affect the enzymatic methods for measuring glucose in the urine. Direct and indirect Coombs test can give false positive results.

The cefazolin solution cannot be mixed in one container with other antibiotics.

Features of the application.

When prescribing cefazolin, official recommendations for antibiotic therapy and recommendations for the prevention of antibiotic resistance should be followed.

Hypersensitivity. As with other beta-lactam antibiotics, cases of severe acute hypersensitivity reactions (anaphylaxis) have been reported, sometimes with fatal outcome, even if the detailed history did not have appropriate indications. With the development of such reactions, the use of the drug should be discontinued immediately, enter adrenaline (epinephrine), glucocorticoids and other appropriate emergency measures.

Before starting any new course of treatment, the patient should be asked about the history of hypersensitivity reactions to cefazolin, to other cephalosporins, or to any other beta-lactam antibiotic, or other drug. With caution, cefazolin should be used in patients with a history of mild hypersensitivity reactions to penicillins or other beta-lactam antibiotics due to the possibility of cross-allergic reactions between them and cephalosporins.

Cefazolin should be administered with extreme caution to patients with allergic reactivity (for example, allergic rhinitis or bronchial asthma, any form of allergic reactions, especially drugs), since the risk of developing serious hypersensitivity reactions increases.

Antibiotic-associated colitis / excessive growth of insensitive microorganisms. Treatment with antibacterial drugs, especially in severe diseases in elderly patients, as well as in weakened patients, children, can lead to antibiotic-associated diarrhea, colitis, including pseudomembranous colitis.The severity of manifestations of pseudomembranous colitis can range from mild to life-threatening, therefore it is important to consider the possibility of this diagnosis in all patients who have diarrhea during or after the use of cefazolin. It is necessary to discontinue cefazolin therapy in case of severe and / or admixture of blood diarrhea and apply specific therapy against Clostridium difficile. In the absence of the necessary treatment, toxic megacolon, peritonitis, shock can develop. Medicines that suppress peristalsis should not be used.

Broad-spectrum antibiotics should be used with caution in patients with a history of gastrointestinal diseases, especially colitis.

Long-term use of antibacterial drugs, including cefazolin, can lead to excessive growth of insensitive microorganisms, fungi and the development of superinfection. Patients should be carefully monitored to identify possible superinfection. If superinfection develops during treatment, appropriate measures should be taken, in particular, periodically examine the sensitivity of microflora to the drug.

Renal failure. In patients with renal failure, the dose and / or the interval between the use of the drug can be adjusted depending on the degree of impaired renal function.

In case of renal failure with a glomerular filtration rate of up to 55 ml / min, the possibility of cumulation of cefazolin should be taken into account. Therefore, the daily dose should be reduced accordingly or the interval between injections of the drug should be extended to prevent its toxic effect.

Although cefazolin is rarely a cause of impaired renal function, it is recommended to evaluate renal function, especially in critically ill patients receiving the maximum dose of the drug, patients receiving concomitant therapy with other potentially nephrotoxic drugs (including aminoglycosides, potent diuretics).

The use of high doses of cefazolin in patients with renal failure may be associated with a risk of seizures.

Patients in the geriatric group with normal renal function do not need dose adjustment.

Blood clotting disorder. Cefazolin can occasionally lead to bleeding disorders. Therefore, patients with diseases that can cause bleeding (for example, ulcers of the digestive tract), patients with coagulation defects (inherited: for example, hemophilia; acquired: for example, with thrombocytopenia, patients with impaired synthesis or vitamin K deficiency with parenteral nutrition, malnutrition, chronic diseases of the liver, kidneys or elderly patients), as well as patients with prolonged antibiotic therapy, patients with preliminary long-term therapy with anticoagulants, it is possible to control prothrombin time (or the International Normalized Ratio). If indicated, exogenous vitamin K (10 mg per week) should be prescribed.

Influence on the results of laboratory tests. During treatment with the drug, false-positive results of glucosuric tests carried out by non-enzymatic methods can be noted. The drug does not affect the results of glucosuric tests carried out by enzymatic methods.

Cephalosporins can be absorbed on the surface of red blood cell membranes and interact with antibodies directed against the drug. This can lead to a false positive Coombs test (for example, in children whose mothers were treated with cefazolin) and very rarely - to the development of hemolytic anemia. With this reaction, cross-reactivity with penicillins may occur.

Intrathecal administration. Intrathecal administration of cefazolin is not recommended.There were reports of severe toxic reactions from the central nervous system, including seizures, when using exactly this route of administration.

With prolonged treatment with the drug, it is recommended to regularly monitor the blood picture, indicators of the functional state of the liver and kidneys.

Sodium. Each gram of Cefazolin-BCHPZ contains 2.2 mmol (50.61 mg) of sodium, which should be considered for patients who follow a diet with a controlled sodium content.

Only transparent, freshly prepared solutions of the preparation are suitable for use. The cefazolin solution cannot be mixed in one volume with other antibiotics.

Incompatibility.

Do not mix in the same syringe with other medicines.

The cefazolin solution should not be mixed with other antibiotics in the same syringe or in the same infusion system.

Use during pregnancy or lactation.

The drug is contraindicated during pregnancy.

If it is necessary to use the drug, breast-feeding should be discontinued.

The ability to influence the reaction rate when driving vehicles or other mechanisms.

Until the patients individual reaction to the drug is clarified, one should refrain from driving motor vehicles or other mechanisms, given that during treatment such disorders of the nervous system as dizziness, convulsions can be observed.

Dosage and administration.

Before starting therapy, it is necessary to exclude the patients hypersensitivity to the antibiotic by making a skin test.

Cefazolin should be administered intramuscularly or intravenously (drip and stream). Cefazolin cannot be administered intrathecal!

Preparation of solutions for injection and infusion

For intramuscular injection, dissolve the contents of a 500 mg vial (1000 mg) in 2-3 ml (4-5 ml) of 0.9% sodium chloride solution or sterile water for injection, shaking thoroughly until completely dissolved. Enter deep into the upper outer quadrant of the gluteus maximus muscle.

For intravenous jet administration, dissolve a single dose of the drug in 10 ml of 0.9% sodium chloride solution or sterile water for injection and slowly administer for 3-5 minutes.

With intravenous drip, 500 mg or 1000 mg of the drug should be diluted in 50-100 ml of water for injection or 0.9% sodium chloride solution, or in one of the following solutions: 5% glucose solution, 10% glucose solution, 5% glucose solution in sodium lactate solution for infusion, 0.9% sodium chloride solution with 5% glucose solution for intravenous infusion, 0.45% sodium chloride solution with 5% glucose solution for intravenous infusion, 5% sodium lactate solution or 10% invert sugar solution in water for injection, Ringers solution for injection with lactate sludge without lactate; should be administered within 20-30 minutes (injection rate - 60-80 drops / min). Shake vials vigorously until complete dissolution. The daily doses for intravenous administration remain the same as for intramuscular administration.

A freshly prepared solution (333 mg / ml) of yellow color, transparent, retains its physical and chemical stability for 24 hours at room temperature.

Dosage

The average daily dose for adults is usually 1000-4000 mg, the maximum daily dose is 6000 mg.

Type of infection Single dose Frequency
Gram-positive Infections 250-500 mg every 8 hours
Moderate airway infections caused by pneumococci and urinary tract infections 1 g every 12 hours
Gram-negative infections 500 mg - 1 g every 6-8 hours
Life-threatening infections (sepsis, endocarditis, peritonitis, destructive pneumonia, acute hematogenous osteomyelitis, complicated urological infections). 1–1.5 g every 6-8 hours

For the prevention of postoperative infectious complications in adults, it is recommended to administer Cefazolin-BCPP intramuscularly or intravenously:

  • at a dose of 1000 mg for 0.5-1 hour before the start of surgery;
  • with long-term operations (2 hours or more) - an additional 500–1000 mg during the operation;
  • after surgery - at a dose of 500-1000 mg every 6-8 hours for the first 24 hours.

In some cases (for example, open heart surgery, joint prosthetics), the prophylactic use of cefazolin may continue 3–5 days after surgery.

In adult patients with impaired renal function, the dosage regimen should be set depending on the creatinine clearance. After a loading dose appropriate to the severity of the infection, the recommendations below can be used.

With creatinine clearance:

  • 55 ml / min or more - dose adjustment is not required;
  • 35–54 ml / min - a single dose does not change, but the interval between administrations should be at least 8 hours;
  • 11–34 ml / min - a single standard dose should be reduced by 2 times, the interval between administrations is 12 hours;
  • less than 10 ml / min - appoint half the therapeutic dose every 18-24 hours.

Elderly patients: dosage as in adults (subject to normal renal function).

For children older than 1 month, the drug should be prescribed at a dose of 25-50 mg / kg per day (in severe cases, up to 100 mg / kg per day), divided into 3-4 doses.

The maximum daily dose for children is 100 mg / kg body weight.

In children with impaired renal function, dose adjustment should be carried out depending on the creatinine clearance.

With creatinine clearance:

  • 40–70 ml / min - 60% of the daily dose distributed for administration with an interval of 12 hours;
  • 20–40 ml / min - 25% of the daily dose distributed for administration with an interval of 12 hours;
  • 5–20 ml / min - 10% of the average daily dose every 24 hours.

All recommended doses should be prescribed after the initial loading dose.

The average duration of treatment is 7-10 days.

Children.

The drug should not be used in children under 1 month of age and premature babies.

Overdose.

Symptoms parenteral administration of high doses of cephalosporins may cause dizziness, paresthesia, and headache. the development of allergic reactions is possible; neurotoxic effects are possible, including increased convulsive readiness, generalized convulsions, vomiting and tachycardia, especially in patients with chronic renal failure. laboratory deviations are possible such as an increase in creatinine, blood urea nitrogen, liver enzymes and bilirubin, a positive Coombs test, thrombocytosis / thrombocytopenia, eosinophilia, leukopenia and prolongation of prothrombin time.

Treatment. Stop using the drug, if necessary, conduct anticonvulsant, desensitizing therapy. In case of severe overdose, maintenance therapy and monitoring of hematological, renal, hepatic functions and the blood coagulation system are recommended until the patients condition is stabilized. There is no specific antidote. The drug is excreted by hemodialysis; peritoneal dialysis is less effective.

Adverse Reactions

Digestive tract: nausea, vomiting, anorexia, diarrhea, flatulence, cramping / abdominal pain; with prolonged use, dysbiosis, pseudomembranous enterocolitis may develop.

Hepatobiliary system: transient increase in hepatic transaminase activity, bilirubin and / or lactate dehydrogenase and alkaline phosphatase levels in blood plasma, transient cholestatic jaundice, transient hepatitis.

Blood system and lymphatic system: neutropenia, leukopenia / leukocytosis, thrombocytopenia / thrombocytosis, eosinophilia, lymphopenia, basophilia, monocytosis, granulocytosis / granulocytopenia, agranulocytosis, decreased hemoglobin and / or hematocrit, anemia, etc.aplastic, hemolytic, pancytopenia, hypoprothrombinemia, lengthening of prothrombin time, coagulopathy and hemorrhage, positive direct and indirect Coombs reaction.

Nervous system: headache, dizziness, fatigue, weak

Tags: Cefazolin