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

Cephalosporin antibiotic III generation for parenteral administration. It acts bactericidal, disrupting the synthesis of the cell wall of microorganisms. Has a wide spectrometer.

It is active against gram-positive and gram-negative microorganisms resistant to other antibiotics: Staphylococcus spp. (including Staphylococcus aureus (including strains forming penicillinase) and Staphylococcus epidermidis (with the exception of Staphylococcus epidermidis and Staphylococcus aureus, resistant to methicillin)), Streptococcus pneumoniae, Streptococcus pyogenes, Streptococcus agalactiae, Enterococcus spp., Enterobacter spp., Escherichia coli, Haemophilus influenzae (including strains forming penicillinase), Haemophilus parainflueazae, Moraxella catarrhalis, Klebsiella spp. (including Klebsiella pneumoniae), Morganella morganii, Neisseria gonorrhoeae (including strains forming penicillinase), Acinetobacter spp., Corynebacterium diphtheriae, Erysipelothrix rhusiopathiae, Eubacter spp., Propionibacterium spp., Clostridium spp. (including Clostridium per-fringens), Citrobacter spp., Proteus mirabilis, Proteus vulgaris, Providencia spp. (including Provi-dencia rettgeri), Serratia spp., some strains of Pseudomonas aeruginosa, Neisseria meningitidis, Bacteroides spp. (including some strains of Bacteroides fragilis), Fusobacterium spp. (including Fusobacterium nucleatum), Peptococcus spp., Peptostreptococcus spp. Most strains of Clostridium difficile are stable.

Resistant to most beta-lactamases of gram-positive and gram-negative microorganisms.

Pharmacokinetics:

After intramuscular injection of the drug in doses of 0.5 g and 1 g of C max is determined after 30 minutes and is 11 μg / ml and 21 μg / ml, respectively. Connection with blood plasma proteins - 30-50%. Bioavailability is 90-95%.

Creates therapeutic concentrations in most tissues (myocardium, bones, gall bladder, skin, soft tissues) and fluids (synovial, pericardial, pleural, cerebrospinal fluid, sputum, bile, urine) of the body. Penetrates into breast milk, passes through the placental barrier. The volume of distribution is 0.25-0.39 l / kg.

The half-life (T1 / 2) - 1-1.5 hours - with the / m introduction. It is excreted by the kidneys - 20-36% unchanged, the rest - in the form of metabolites (15-25% - in the form of pharmacologically active deacetylcefotaxime and 20-25% - in the form of 2 inactive metabolites - M2 and M3, deprived of antimicrobial action).

In chronic renal failure (CRF) and in elderly people, T1 / 2 increases by 2 times.

Indications:Infectious-inflammatory diseases caused by sensitive microorganisms: infections of the central nervous system (meningitis), respiratory tract and L0P-organs, urinary tract, bones, joints, skin and soft tissues,pelvic organs, pelvic organs, gonorrhea, infected wounds and burns, peritonitis, sepsis, abdominal infections, endocarditis, Lyme disease (borreliosis), salmonellosis, infection against immunodeficiency, prevention of infections after surgical operations (including urological, obstetrical, gynecological, on the gastrointestinal tract).

Contraindications:

Hypersensitivity to cefotaxime and other cephalosporins.

In the case of dissolution of the drug in a 1% solution of lidocaine:

- hypersensitivity to lidocaine or other local anesthetic of the amide type;

- intracardiac blockade without an established pacemaker;

- severe heart failure;

- intravenous administration;

- children under the age of 2.5 years (intramuscular injection).

Carefully:

Newborn period; chronic renal failure; ulcerative colitis (including in the anamnesis); in patients with increased sensitivity to penicillins in anamnesis due to the possibility of developing a cross-allergic reaction.

Pregnancy and lactation:The use of the drug during pregnancy is possible in cases where the intended use for the mother exceeds the potential risk to the fetus.If it is necessary to prescribe the drug during lactation, breastfeeding should be stopped for the time of drug admission.

Dosing and Administration:

Adults and children over 12 years of age (with a body weight of 50 kg or more):

- with uncomplicated infections, as well as with infections of the urinary tract - 1 g every 8-12 hours;

- with uncomplicated acute gonorrhea - 1 g once;

- for infections of medium severity - 1 - 2 g every 12 hours; The maximum daily dose is 12 g.

Duration of treatment is set individually.

For the purpose of preventing the development of infections before the surgical operation, enter 1 g during the initial general anesthesia. If necessary, the administration is repeated 6 to 12 hours later.

When creatinine clearance (CC) is 20 ml / min / 1.73 m2 or less, the daily dose is reduced by 2 times.

Children with body weight up to 50 kg (over the age of 2.5 years) -50 - 180 mg / kg in 4 to 6 injections. In severe infections, incl. meningitis, the daily dose to children is increased to 100-200 mg / kg, in 4 to 6 receptions, the maximum daily dose is 12 g. Rules for the preparation of the injection solution:

For the / m introduction use water for injection or 1% lidocaine (for a dose of 0.5 g - 2 ml, for a dose of 1 g - 4 ml).

Side effects:

Allergic peakcuu:

urticaria, chills or fever, rash, skin itch, rarely - bronchospasm, eosinophilia, malignant exudative erythema (Stevens-Johnson syndrome), toxic epidermal necrolysis (Lyell's syndrome), angioedema, rarely anaphylactic shock.

From the central nervous system: headache, dizziness.

From the gastrointestinal tract:

nausea, vomiting, diarrhea or constipation, flatulence, abdominal pain, dysbiosis, impaired liver function, rarely - stomatitis, glossitis, pseudomembranous enterocolitis.

From the urinary system:

disturbance of kidney function, oliguria, interstitial nephritis.

From the hematopoiesis:

hemolytic anemia, leukopenia, neutropenia, granulocytopenia, thrombocytopenia, hypocoagulation.

Laboratory indicators:

azotemia, increased urea concentration in the blood, increased activity of "liver" transaminases and alkaline phosphatase, hypercreatininemia, hyperbilirubinemia, Coombs positive reaction.

Local reactions:

morbidity and infiltration at the site of intramuscular injection.

Other:

Superinfection (in particular, candidal vaginitis).

Overdose:

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

Treatment: symptomatic, there is no specific antidote.

Interaction:

Increases the risk of bleeding when combined with antiaggregants, non-steroidal anti-inflammatory drugs.

The probability of kidney damage increases with simultaneous administration with aminoglycosides, polymyxin B and "loop" diuretics.

Drugs that block tubular secretion, increase the plasma concentrations of cefotaxime and slow down its excretion.

Pharmaceutically incompatible with solutions of other antibiotics in one syringe.

Special instructions:

In the first weeks of treatment, pseudomembranous colitis can occur, which is manifested by severe prolonged diarrhea. At the same time, stop taking the drug and prescribe adequate therapy, including vancomycin or metronidazole.

Patients who had a history of allergic reactions to penicillins may have increased sensitivity to the antibiotics of the cephalosporin group. When treating the drug for more than 10 days, it is necessary to monitor the peripheral blood picture.

During treatment with cefotaxime, it is possible to obtain a false positive sample of Coombs and a false positive urine reaction to glucose.

During treatment, use ethanol it is impossible because of the possibility of disulfiram-like reactions (facial hyperemia, abdominal and stomach cramps, nausea, vomiting, headache, lowering of blood pressure, tachycardia, dyspnea).

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 10 ml vials.

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:P N002159 / 01

Date of registration:26.12.2008

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

Manufacturer: & nbsp

KRASFARMA, JSC Russia

Information update date: & nbsp04.11.2015

Illustrated instructions

Instructions

Cefotaxime (Cefotaxime)