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

It has a wide spectrum of antimicrobial action. It is active both for Gram-positive (Staphylococcus aureus (not producing and producing penicillinase), Staphylococcus epidermidis, group A beta-hemolytic streptococcus pneumoniae, Streptococcus viridans, Corynebacterium diphtheriae, Bacillus anthracis) and Gram-negative microorganisms (Neisseria meningitidis, Neisseria gonorrhoeae, Shigella spp., Salmonella spp., Escherichia coli, Proteus mirabilis, Klebsiella species, Enterobacter aerogenes and Haemophilus influenzae).

It is active against Spirochaeta spp., Treponema spp. and Leptospira spp.

The drug is not effective against Pseudomonas aeruginosa, indolpositive strains of Proteus spp., Enterobacter cloacae, Morganell morganii, Providencia rettgeri, Mycobacterium tuberculosis, Serratia spp., Acinetobacter spp., Methicillin-resistant strains of Staphylococcus spp.

Pharmacokinetics:

With intramuscular (IM) and.intravenous (IV) administration, the drug is rapidly absorbed and distributed in tissues and body fluids. With the introduction of 500 mg cefazolin: the maximum concentration in the blood (Cmax) - 37 mcg / ml 1 hour after the administration and 3 mcg / ml - after 8 hours; with a / m introduction of 1 g of cefazolin - 64 mcg / ml and 7 mcg / ml, respectively. With iv injection of 1 g of cefazolin: Cmax - 185 μg / ml 5 minutes after the administration and 4 μg / ml - after 8 hours.

In therapeutic concentrations, it accumulates in bile, urine, tonsils, pleural exudate, pericardial, peritoneal and synovial fluids, as well as in bones. In patients, the normal concentration of cefazolin in bile is 5 times higher than the concentration in serum. With bile duct obstruction, the concentration of cefazolin in bile is lower than in serum.

Cefazolin does not penetrate the blood-brain barrier.

The drug penetrates the placental barrier. 35-69% of cefazolin contained in the mother's plasma is found in fetal plasma. In low concentrations cefazolin excreted in breast milk. With the introduction of 2 g, after 3 hours the concentration of cefazolin in breast milk is 1.2-1.5 ng / ml.

The half-life (T 1/2) is about 2 hours (with the / m introduction) and 1.8 hours (with IV introduction).

Cefazolin is not metabolized.It is allocated mainly by the kidneys (60% in the first 6 hours and 70-80% within 24 hours), creating high concentrations in the urine. The maximum concentration in urine is 2400 ng / ml with the introduction of 0.5 g and 4000 ng / ml - with the introduction of 1 g.

Indications:

- Infectious-inflammatory diseases caused by microorganisms sensitive to cefazolin:

- upper and lower respiratory tract, ENT - organs;

- kidney and urinary tract;

- organs of the small pelvis and genital organs (including syphilis and gonorrhea);

- sepsis, peritonitis, endocarditis;

- skin and soft tissues;

- bones and joints (including osteomyelitis).

- Prevention of postoperative complications (perioperative prophylaxis).

Contraindications:

- Hypersensitivity to preparations of cephalosporins and other beta-lactam antibiotics (penicillins, carbapenems) in the anamnesis;

- Pregnancy and lactation;

- Newborn children, incl. premature (efficacy and safety not studied).

Carefully:Diseases of the gastrointestinal tract (colitis), severe and moderate severity of kidney failure, children under 1 year.

Pregnancy and lactation:During pregnancy, the drug is prescribed only for life indications.If necessary, breast-feeding is stopped.

Dosing and Administration:

Intramuscular and intravenous (bolus or drop) administration.

The dose of Cefamezin depends on the severity of the disease, the age and function of the kidneys in the patient. Average daily dose for adults is from 1.5 g to 2 g; multiplicity of administration - 3 times a day. In severe infections - 3-4 g / day, the frequency of administration 3-4 times a day. The maximum daily dose -

6th

For the prevention of postoperative infectious complications appoint (in / in or / m) 1 g of cefazolin 30 minutes prior to surgery; 0,5-1 g during the operation (with the duration of surgery 2 and more hours) and 0.5-1 g every 6-8 hours during the first 24 hours after the operation.

Average daily dose for children 1 month and older is 25-50 mg / kg body weight, the frequency of administration 3-4 times a day; In severe infections, the dose may be increased to a maximum dose of -100 mg / kg per day. The average duration of treatment is 7-10 days.

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 (1 ml / s), the dosing regimen, as a rule, does not require correction.With SC 35-54 ml / min (0.58-0.9 ml / s), a single dose may remain unchanged, but the interval between administrations should be increased to 8 hours. With CC 11-34 ml / min (0.18-0.57 ml / s), the single dose should be reduced 2 times; the interval between administrations is 12 hours. When QC <10 ml / min (<0.17 ml / sec) is administered half the usual dose every 18-24 hours. All recommendations for prescribing low doses are applied after an initial loading dose corresponding to the severity of the infection is established.

In children with impaired renal function, the correction of the dosing regimen is performed depending on the values of CC: at a CC of 70-40 ml / min - 60% of the average daily dose and injected every 12 hours; with KK 40-20 ml / - 25% of the average daily dose with an interval of 12 hours; with KK 5-20 ml / min - 10% of the average daily dose every 24 hours. All recommended doses are administered after the initial dose, which corresponds to the nature and severity of the infection.

Preparation of solutions for injection and infusion:

During the dilution, vials should be vigorously shaken until completely dissolved. For intramuscular injection the drug is dissolved in 3-5 ml of water for injection, 0.9% solution of sodium chloride or 0.25 - 0.5% solution of novocaine.

For intravenous drip the drug is dissolved in 3 ml of water for injection, then it is further dissolved to 50 ml (when 1000 mg of Cefamezin is administered) or 100 ml (when more than 1000 mg of Cefamezin is administered) with isotonic sodium chloride solution or 5% or 10% dextrose solution. Enter in / in a drip, for 30 minutes (the rate of administration of 80 drops per minute).

For intravenous bolus administration a single dose of the drug (1000 mg) is diluted in 10 ml of isotonic sodium chloride solution and injected iv slowly, for 3-5 minutes.

Side effects:

Allergic reactions: skin rash, skin itch, eosinophilia, bronchospasm, angioedema or Quincke's edema, arthralgia, dyspnea, skin hyperemia, urticaria, hyperthermia, anaphylactic shock, erythema multiforme exudative (including Stevens-Johnson syndrome), toxic epidermal necrolysis.

From the digestive system: anorexia, diarrhea, nausea, vomiting, abdominal pain, transient increase in the activity of "liver" transaminases and alkaline phosphatase; very rarely - pseudomembranous colitis, cholestatic jaundice, hepatitis, candidomycosis (including candidal stomatitis).

From the central and peripheral nervous system: headache, dizziness, convulsions.

Laboratory indicators: neutropenia, leukopenia, thrombocytopenia,

gipoprotombinemiya, agranulocytosis, pancytopenia, thrombocytosis, haemolytic anemia, false-positive Coombs' test, hypercreatininemia, increased prothrombin time.

From the urinary system: impaired renal function (against kidney disease, when treated with large doses of cefazolin (6 g)). In these cases, the dose of the drug is reduced, and the treatment is controlled by levels of urea nitrogen and blood creatinine.

Other: at long treatment - a dysbacteriosis, a superinfection.

Locally: rarely phlebitis (at / in the introduction), soreness at the injection site (with the / m).

Overdose:

Symptoms: skin rash, skin itching, a violation of the digestive and respiratory systems.

Treatment: symptomatic. There is no specific antidote. It is recommended to monitor the body's vital functions, laboratory parameters of renal and liver function, prothrombin time and other hematologic parameters.

Interaction:

The drug is not recommended to be used simultaneously with loop diuretics (furosemide, ethacrynic acid) and aminoglycosides (risk of developing nephrotoxic effect). When used simultaneously with with oral anticoagulants (for example, warfarin) there is a risk of bleeding.

Probenecid reduces the elimination of cefazolin.

Pharmaceutically incompatible with the following drugs: aminoglycosides, cimetidine or famotidine!

Special instructions:

Patients who have a history of allergic reactions to beta-lactam antibiotics (penicillins, carbapenems) may have increased sensitivity to cephalosporin antibiotics.

It should be noted when developing the first symptoms of anaphylactic shock: anxiety, paresthesia around the mouth, shortness of breath, sweating. In these cases, the drug should be discontinued immediately and appropriate therapy should be carried out.

If severe and prolonged diarrhea occurs during or after treatment with cefazolin, the diagnosis of pseudomembranous colitis should be ruled out, which requires immediate discontinuation of the drug and the appropriate treatment. Possible development of exacerbation of diseases of the gastrointestinal tract (especially colitis).

The safety of use in preterm infants and children of the first year of life has not been studied. With cefazolin, false positive and indirect Coombs probes may appear.

With cefazolin, a false positive reaction to glucose in the urine is possible.

Effect on the ability to drive transp. cf. and fur:Data on the effect of cefazolin on the ability to drive and work with other mechanical means are absent.

Form release / dosage:

Powder for the preparation of solution for intravenous and intramuscular injection, 1000 mg.

Packaging:The drug is placed in a 10 ml vial, a clear glass (type 2, USP), sealed with a rubber stopper, an aluminum cap and covered with a polypropylene protective cap. 1 bottle is placed in a pack of cardboard along with instructions for use.

Storage conditions:Store at a temperature not exceeding 25 ° C. Keep out of the reach of children.

Shelf life:

3 years. Do not use the drug after the expiration date.

Terms of leave from pharmacies:On prescription

Registration number:П N014620 / 01

Date of registration:10.03.2009

The owner of the registration certificate:KRKA, dd, Novo mesto, AOKRKA, dd, Novo mesto, AO

Manufacturer: & nbsp

KRKA, d.d. Slovenia

Representation: & nbspKRKA, dd, Novo mesto, AOKRKA, dd, Novo mesto, AO

Information update date: & nbsp14.10.2015

Illustrated instructions

Instructions

Cefamesin® (Cefamezin®)