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. It has a wide spectrum of action, is active against gram-positive (Staphylococcus spp., Including Staphylococcus aureus (not producing and producing peicillinase), 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, methicillin resistant strains of Staphylococcus spp.

Pharmacokinetics:

Time to reach the maximum concentration (TC_m_Oh) with intramuscular injection at a dose of 0.5 g and 1.0 g, respectively - 2 and 1 h; maximum concentration (С_m_Oh) - 38 and 64 μg / ml. After intravenous administration of TC_m_Oh at the end of infusion, C_m_Oh- 180 mcg / 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 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 (T1 / 2) at the / m - 1.8 h, at / in the introduction -2 h If the kidney function T1 / 2 - 20-40 hours is derived primarily by the kidneys in unchanged form within the first 6h- 60-90%, after 24 hours - 70-95%. After the / m introduction in doses of 0.5 g and 1.0 g of C_m_Oh in urine 1 mg / ml and 4 mg / ml, respectively.

Indications:Infectious-inflammatory diseases caused by microorganisms susceptible to cefazolin: upper and lower respiratory tract, LOP-organs (including otitis media), urinary and biliary tract, pelvic organs, skin and soft tissues, bones and joints (including .h.osteomyelitis), endocarditis, sepsis, peritonitis, mastitis; wound, burn and postoperative infections; syphilis, gonorrhea. Preventive maintenance of surgical infections in the pre- and postoperative period.

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

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

Pregnancy and lactation:

The use of cefazolin in pregnancy is permissible if the expected benefit to the mother exceeds the potential risk to the fetus. Stop breastfeeding for the duration of the drug.

Dosing and Administration:

Intramuscularly (in / m), intravenously (intravenously) (struino and drip).

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

Severity of course of infection	Single dose	Frequency of introductions	Daily dose
Infections of mild degree	500 mg	every 8 hours	1.5 g
gravity	1 g	every 12 hours	2 grams
Uncomplicated infections	1 g	every 12 hours	2 grams
Infections of moderate severity and severe infections	1 g	every 6-8 hours	3 - 4 g
Life-threatening infections	1 g-1.5 g	every 6 hours	4-6 g

The maximum daily dose is 6 in

The average duration of treatment is 7-10 days.

For the prevention of postoperative infection - in / in, 1.0 g for 0.5 -1 h before surgery, 0.5-1.0 g - during the operation and 0.5-1.0 g every 8 h for the first day after the operation.

Patients with impaired renal function require a change in the dosage regimen in accordance with the 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	12 h
34-11 ml / min	4.5-3.1 mg%	1/2 of the usual dose	12 h
10 ml / min and less	4.6 mg and more	1/2 of the usual dose	24 h

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:

For the / m introduction, 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, do not dissolve cefazolin in solutions of lidocaine.

For IV bolus injection, the resulting solution is diluted in 5 ml of water for injection, then injected slowly, within 3-5 minutes. For intravenous drip, 50-100 ml of a 5-10% solution of dextrose, 0.9% sodium chloride solution, Ringer's solution, 5% sodium bicarbonate solution are diluted with the drug.

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.

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,treatment is carried out under the control of 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, rarely - cholestatic jaundice, hepatitis.

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

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

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

Laboratory indicators: a false positive test of Coombs, an increase in the activity of "hepatic" transaminases, hypercreatininaemia, an increase in prothrombin time, and a false positive urine reaction to glucose.

Overdose:

Symptoms: 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.

Measures to deal with overdose: immediately stop the introduction of the drug, monitor the vital functions of the body and the corresponding 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. Cefazolin, suppressing the intestinal flora, interferes with the synthesis of vitamin K. Therefore, with the simultaneous use with drugs that reduce platelet aggregation (nonsteroidal anti-inflammatory drugs (NSAIDs), salicylates), the risk of bleeding increases. For the same reason, with simultaneous use with anticoagulants, there is an increase in anticoagulant activity. Do not use cefazolin together with antibacterial drugs that have a bacteriostatic mechanism of action (tetracyclines, sulfonamides, erythromycin, chloramphenicol), since in vitro studies have shown that antagonism exists between them.

Special instructions:

When the drug is used, there may be an exacerbation of diseases of the gastrointestinal tract (GI tract), especially colitis. When there is severe diarrhea, characteristic of pseudomembranous colitis, cefazolin should be canceled and appropriate treatment prescribed. During the treatment period, patients should refrain from drinking alcohol. With long-term use of the drug, control of the peripheral blood picture and kidney function is necessary.

Effect on the ability to drive transp. cf. and fur:Use caution to drivers of vehicles and people whose activities require increased concentration of attention and good coordination of movements.

Form release / dosage:

Powder for solution for intravenous and intramuscular injection 0.5 g, 1.0 g.

Packaging:

0.5 g, 1.0 g of active substance in bottles with a capacity of 10 ml.

1 bottle with instructions for use in a pack of cardboard.

10 bottles with instructions for use in a cardboard box.

For hospital:

- 50 bottles and 5 instructions for use in a cardboard box;

- 1 bottle with instructions for use (from 1 to 50 bottles with an equal number of instructions for use) in a cardboard box.

Storage conditions:

In the dark place at a temperature of no higher than 25 ° C. Keep out of the reach of children.

After the expiry date of the drug, unused vials should be carefully opened, the contents dissolved in a large amount of water and drained into the drain.

Shelf life:

2 years. Do not use after the expiration date.

Terms of leave from pharmacies:On prescription

Registration number:LS-001383

Date of registration:31.01.2011

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

Manufacturer: & nbsp

KRASFARMA, JSC Russia

Information update date: & nbsp13.10.2015

Illustrated instructions

Instructions

Cefazolin (Cefazolin)