Cefazolin, powder of solution vial 1g

Composition

Active ingredient:

Cefazolin in the form of a sodium salt of 1.0 g

Pharmacological action

Cefazolin is a semi-synthetic cephalosporin antibiotic of the first generation of a broad spectrum of action for parenteral use. It acts bactericidal, suppressing the biosynthesis of the bacterial cell wall. Active against gram-positive bacteria:  Staphylococcus spp. (excluding methicillin-resistant strains), Streptococcus spp. (excluding Streptococcus faecalis); gram-negative bacteria:  Escherichia coli, Proteus mirabilis, Klebsiella spp., Neisseria gonorrhoeae, Treponema spp., Enterobacter aerogenes, Haemophilus influenzae.

It is not effective against Pseudomonas aeruginosa, indole-positive strains of Proteus spp., Mycobacterium tuberculosis, Serratia spp., anaerobic microorganisms, methicillin-resistant strains of Staphylococcus spp.

Pharmacokinetics

Cefazolin is poorly absorbed from the gastrointestinal tract and is therefore used for intravenous and intramuscular use. After intramuscular use at a dose of 500 mg, Cmax in plasma is reached in 1-2 hours and is 30 mcg / ml. Binding to plasma proteins is about 85%.

Cefazolin penetrates into bone tissue, ascitic fluid, pleural and synovial fluids, but is not detected in the central nervous system. T1 / 2 of cefazolin from plasma is about 1.8 hours.

Cefazolin is excreted unchanged in the urine, mainly by glomerular filtration and to a small extent by tubular secretion. After intramuscular use, at least 80% of the dose after intramuscular use is eliminated in 24 hours.

After intramuscular use at doses of 500 mg and 1 g, Cmax in the urine is 1 mg/ml and 4 mg/ml, respectively. There is evidence of a high concentration of cefazolin in the bile, although it is excreted in this way in small amounts. T1 / 2 from plasma increases in patients with impaired renal function.

Indications

• bronchitis, pneumonia
• ear, throat and nose infections
• mastitis
• cholecystitis
• skin and soft tissue
• infections genitourinary system
• infections wound and burn infections.

Contraindications

Hypersensitivity to cephalosparin antibiotics.

Side effects

From the digestive system:  nausea, vomiting, diarrhea are possible; rarely-a transient increase in the activity of hepatic transaminases.

Allergic reactions:  possible hives, pruritus, eosinophilia, fever; in some cases – angioedema, arthralgia, anaphylactic shock.

Effects due to chemotherapeutic action:  candidiasis, pseudomembranous colitis.

From the hematopoietic system:  rarely-reversible leukopenia, neutropenia, thrombocytopenia.

From the urinary system:  rarely-impaired renal function.

Local reactions:  possible soreness at the site of intramuscular injection.

Interaction

Concomitant use with anticoagulants and diuretics is not recommended.

With the simultaneous use of cefazolin and “loop diuretics”, its tubular secretion is blocked.

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

Drugs that block tubular secretion increase blood concentrations, slow down excretion, and increase the risk of toxic reactions.

How to take, course of use and dosage

Intravenously, intramuscularly (jet and drip). The average daily dose for adults is 1 g, the frequency of use is 2 times a day. The maximum daily dose is 6 g (in rare cases-12 g); the frequency of use can be increased to 3-4 times a day. The average duration of treatment is 7-10 days.

For the prevention of postoperative infection:  30 minutes before surgery,0.5-1 g. During the operation and 0.5-1 g every 6-8 hours during the day after the operation.

Use in patients with impaired renal function:  if the creatinine clearance is 55 ml / min or more, or if the plasma creatine content is 1.5 mg% or less, the full dose can be administered. With a creatinine clearance of 54-35 ml / min or with a plasma creatinine content of 3-1.6 mg%, the full dose can be used, but the intervals between injections can be increased to 8 hours. Patients with creatinine clearance of 34-11 ml / min or a plasma creatinine content of 4.5-3.1 mg%-1 / 2 doses at intervals of 12 hours. Patients with creatinine clearance of 10 ml / min or less, or with a plasma creatinine content of 4.6 mg% or more-1/2 of the average dose every 18-24 hours.

Use in children: the average daily dose for children is 20-50 ml / kg; in severe cases of infection, the dose can be increased to 100 mg/day. The frequency of maintenance is 3-4 times a day.

Use in children with impaired renal function:  in children with impaired renal function, the dosage regimen is adjusted depending on the values of creatinine clearance. With a creatinine clearance of 70-40 ml / min – 60% of the average daily dose and removed after 12 hours. With a creatinine clearance of 40-20 ml / min – 25% of the average daily dose with an interval of 12 hours. Children with creatinine clearance of 5-20 ml / min – 10% of the average daily dose every 24 hours. All recommended doses are administered after the initial shock dose.

Preparation of solutions:  for intramuscular use, the drug is dissolved in 4-5 ml of water for injection, an isotonic solution of sodium chloride or 0.25-0.5% novocaine solution. For intravenous drip use, the drug is dissolved in 100-250 ml of isotonic sodium chloride solution or 5% glucose solution; the injection is carried out for 20-30 minutes (the rate of use is 60-80 drops per minute). For intravenous jet use, a single dose of the drug is diluted in 10 ml of isotonic sodium chloride solution and administered slowly for 3-5 minutes. During dilution, the vials are shaken vigorously until completely dissolved.

Special instructions

Patients who have had a history of allergic reactions to penicillins, carbapenems, may have an increased sensitivity to cephalosporin antibiotics.

During treatment with cefazolin, it is possible to obtain positive direct and indirect Coombs tests, as well as a false positive reaction of urine to sugar.

When prescribing the drug, an exacerbation of gastrointestinal diseases, especially colitis, is possible. The safety of use in premature children and children of the first year of life has not been established.

Form of production

Powder for preparing a solution for intravenous and intramuscular use.

Storage conditions

Store in a dry place, protected from light, at a temperature not exceeding 25°C.

Shelf

life is 2 years.

Active ingredient

Cefazolin

Conditions of release from pharmacies

By prescription

Dosage form

solution for injection and infusion

Description

For children older than 1 month, For adults as prescribed by a doctor

Indications

Skin infections, Sinusitis, Otitis media, Urinary Tract Infections, Bronchitis, Burns, Inflammation of the female genital organs, Biliary tract infections, Tonsillitis, Purulent wounds, Osteomyelitis, Pneumonia