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

Cephalosporin antibiotic III generation for parenteral administration. It is bactericidal. violating the synthesis of the cell wall of microorganisms. Has a wide range of action.

Cefotaxime is usually sensitive: Aeromonas hydrophila; Bacillus subtilis; Bordetella pertussis; Borrelia burgdorferi; Moraxella catarrhalis; Citrobacrer diversus; Curobacler freundii *; Clostridium perfringens; Corynebacterium diphtheriae, Escherichia coli; Enterobacter spp. *; Erysipelothrix insidiosa; Eubacterium spp .; Haemophilus spp. (penicillinase-producing and non-producing penicillinase strains, including ampicillin-resistant ones): Klebsiella pneumoniae; Klebsiella oxytoca; Staphylococcus spp. (methicillin-sensitive, including producing and non-producing peninillinase strains); Morganella morganii, Neisseria gonorrhoea (including penicillinase-producing and non-producing penicillinase strains); Neisseria meningitidis: Propionibacterium spp; Proteus mirabilis; Proteus vulgaris: Providencia spp .; Streptococcus spp (including Streptococcus pneumoniae): Salmonella spp., Serratia spp *; Shigella spp. Veillonella spp *; Yersinia spp *; Pseudomonas spp. (except Pseudomonas aeruginosa, Pseudomonas cepacia).

* - sensitivity depends on epidemiological data and on the level of resistance in each country.

Cefotaxime is resistant to: Acinetobacter baumanii; Bacteroidcs fragilis; Clostridium difficile; Entcrococcus spp .; Gram-negative anaerobes: Listeria monocytogenes, Staphylococcus spp.(methicillin-resistant strains); Pseudomonas aeruginosa; Pscudomonas cepacia; Stenotrophomonas maltophilia.

Pharmacokinetics:

After a single intravenous injection at doses of 0.5, 1 and 2 g, the time to reach the maximum concentration (TCmax) is 5 minutes, the maximum concentration (Cmax) is 39, 101.7 and 214 μg / ml, respectively. After a / m (intramuscular) introduction to the vines, 0.5 and 1 g Tmax - 0.5 h and Cmax is 11 and 21 mcg / ml, respectively. Connection with plasma proteins - 30 - 50%. Biodidity - 90 - 95%

Creates therapeutic concentrations in most tissues (myocardium, bone, gallbladder, skin, soft tissue) and fluids (synovial, pericardial, pleural, sputum, bile, urine, cerebrospinal fluid (CSF) of the body. The volume of distribution is 0.25-0.39 l / kg.

The half-life (T1 / 2) is 1 hour with IV injection and 1-1.5 hours with the IM injection. 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).

In chronic renal failure and in elderly patients, T1 / 2 increases 2-fold. In newborns, T1 / 2 ranges from 0.75 to 1.5 hours, in preterm infants it increases to 6.4 hours.

Indications:Bacterial infections of severe course caused by microorganisms sensitive to cefotaxime: infections of the central nervous system (meningitis), respiratory tract and ENT - organs, urinary tract, bones, joints, skin and soft tissues, pelvic organs, gonorrhea, infected wounds and burns, peritonitis , sepsis, abdominal infections, endocarditis, Lyme disease, infections against immunodeficiency, prevention of infections after surgery (including urological, obstetric-gynecological, gastrointestinal tract).

Contraindications:Hypersensitivity to cefotaxime (including penicillins, other cephalosporins, carbapenems), pregnancy, lactation, children's age (IM for at least 2.5 years when lidocaine is used as a solvent).

Carefully:Patients with a history of allergy to penicillins (risk of developing cross-allergic reactions); with simultaneous use with aminoglycosides; with renal failure.

Pregnancy and lactation:Application during pregnancy and during breastfeeding is contraindicated.If it is necessary to prescribe the drug during breastfeeding, breastfeeding should be stopped.

Dosing and Administration:

Intravenous or intramuscular. The dose, method and frequency of administration should be determined by the severity of the infection, the sensitivity of the pathogen and the patient's condition. Treatment can be initiated before the results of the sensitivity test are obtained.

Adults and children over 12 years of age and weighing 50 kg or more:

- for infections of mild to moderate severity - 1 g every 12 h. The dose may vary depending on the severity of the infection, the sensitivity of the pathogen and the condition of the patient.

- in severe infections, the dose can be increased to 12 g per day, divided into 3 or 4 injections.

- for infections caused by Pseudomonas spp., the daily dose should be more than 6 g.

Children under 12 years of age and weighing up to 50 kg:

- the usual dose is 100-150 mg / day / day. divided into 2 - 4 introductions.

- with very severe infections, the dose can be increased to 200 mg / kg / day.

Newborns: 50 mg / day / day, divided into 2 to 4 injections.

- in severe infections, a dose of 150 to 200 mg / kg / day, divided into 2 to 4 injections.

With gonorrhea: 1 g once intravenously or intramuscularly.

For the purpose of prevention before surgery (from 30 to 90 minutes before the operation) 1 g intramuscularly or intravenously is administered.

When performing cesarean section at the time of application of the clamps to the umbilical vein, 1 g of the drug is intravenously injected, then after 1 and 6 h, 1 g is intravenous or intramuscularly repeated.

In renal failure: in cases where creatinine clearance less than 10 ml / min, it is necessary to reduce the dose. After the introduction of the initial single dose, the daily dose should be halved without changing the frequency of administration, i.e. instead of 1 g every 12 h -0.5 g every 12 h, instead of 1 g every 8 h - 0.5 g every 8 h, instead of 2 g every 8 h - 1 g every 8 h, etc. A further dose adjustment may be required depending on the course of the infection and the general condition of the patient.

Rules for the preparation of solutions: for intravenous injection, water for injection is used as a solvent (250 mg diluted in 2 ml of solvent: 500 mg diluted in 2 ml of solvent, 1 g in 4 ml: 2 g in 10 ml); with intravenous injection, the solution should be injected for 3 to 5 minutes. For intravenous infusion, 0.9% sodium chloride solution or 5% dextrose solution is used as the solvent (1 - 2 g diluted in 40 - 100 ml of the solvent). Ringer's lactate solution can also be used.Duration of infusions -20 - 60 min. For intramuscular injection, use water for injection or a 1% solution of lidocaine (250 mg diluted in 2 ml of solvent, 500 mg in 2 ml, 1 g in 4 ml, 2 g in 10 ml).

Side effects:

Classification of undesirable adverse reactions but the frequency of development, according to the recommendations of the World Health Organization: very often (> 10%): often (> 1% and <10%); infrequently (> 0.1% and <1%); rarely (> 0.01% and <0%); very rarely (<0.01%); the frequency is unknown (based on the available data it is impossible to estimate the incidence of side effects).

Infectious and parasitic diseases

Frequency unknown: superinfection. As with the appointment of other antibiotics, the use of cefotaxime, especially prolonged, can lead to an excessive growth of insensitive microorganisms. The patient's condition should be monitored regularly. If the development of superinfection occurs during therapy with cefotaxime, appropriate measures should be taken.

Violations of the blood and lymphatic system

Infrequently: leukopenia, eosinophilia, thrombocytopenia.

Frequency unknown: insufficiency of bone marrow hematopoiesis, pancytopenia, neutropenia, agranulocytosis, hemolytic anemia.

Immune system disorders

Infrequently: The reaction of Yarisch-Gerkeimer. As with the use of other antibiotics, in the treatment of borreliosis during the first days of therapy, the development of the Yarisch-Gerkeheimer reaction is possible. There are reports of the occurrence of one or more symptoms after a few weeks of treatment of borreliosis: skin rash, itching, fever, leukopenia, increased activity of "liver" enzymes, shortness of breath, discomfort in the joints. It should be borne in mind that to some extent, these manifestations are consistent with the symptoms of the underlying disease, over which the patient is receiving treatment.

Frequency unknown: anaphylactic reactions, angioedema, bronchospasm, anaphylactic shock.

Disorders from the nervous system

Infrequently: convulsions.

Frequency unknown encephalopathy (eg, impaired consciousness, impaired motor activity), headache, dizziness.

Heart Disease

Frequency unknown: arrhythmias (due to rapid bolus administration through the central venous catheter).

Disorders from the gastrointestinal tract

Infrequently: diarrhea

Frequency unknown: nausea, vomiting, abdominal pain, pseudomembranous colitis

Disturbances from the liver and bile ducts

Infrequently: an increase in the activity of "hepatic" enzymes (alanine aminotransferase (ALT), aspartate aminotransferase (ACT), lactate dehydrogenase (LDH), gamma-glutamyltransferase (gamma-GT), alkaline phosphatase (AFP), and / or bilirubin concentration. These deviations in laboratory indicators (which can also be explained by the presence of infection) rarely exceed the upper limit of the norm by a factor of 2 and indicate liver damage manifested by cholestasis and often asymptomatic.

Frequency unknown: hepatitis (sometimes with jaundice).

Disturbances from the skin and subcutaneous tissues

Infrequently: a rash, itching, hives.

Frequency unknown: erythema multiforme, Stevens - Johnson syndrome, toxic epidermal necrolysis, acute generalized exanthematous pustulosis.

Disorders from the kidneys and urinary tract

Infrequently: decreased renal function, increased creatinine concentration, especially when combined with aminoglycosides.

Frequency unknown: acute renal failure, interstitial nephritis.

General disorders and disorders in the place of attention

Often: pain at the injection site (with intramuscular injection).

Infrequently: fever inflammatory reactions at the injection site, including phlebitis / thrombophlebitis.

Frequency unknown: when administered intramuscularly, if the solvent is used lidocaine, it is possible to develop systemic reactions associated with lidocaine, especially in cases of unintentional intravenous administration of the drug, injection into highly vascularized tissue or overdose.

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

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 plasma concentrations of Cefotaxime and slow its elimination.

Pharmaceutically incompatible with solutions of other antibiotics in one syringe or dropper.

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 cephalosporin antibiotics.

When the drug is treated for more than 10 days, it is necessary to control the number of blood cells.

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

With the up-to-date use of cephalosporin antibiotics and ethanol, development of disulfiram-like reactions is possible, however, in clinical studies of cefotaxime (Claforan) no similar effect was observed when it was simultaneously used with ethanol.

Care must be taken when driving vehicles and engaging in other potentially hazardous activities that require increased attention and speed of psychomotor reactions.

During treatment with cefotaxime, leukopenia, neutropenia and, more rarely, bone marrow hematopoiesis deficiency, pancytopenia and agranulocytosis may develop. If the course of treatment is more than 10 days, the number of blood elements should be monitored. If the deviations from the norm of these blood parameters should be canceled drug.

Effect on the ability to drive transp. cf. and fur:In the case of the development of such a side effect as dizziness, the ability to concentrate attention and reactions may be impaired. In this case, patients should refrain from driving vehicles and working with mechanisms.

Form release / dosage:

Powder for the preparation of solution for intravenous and intramuscular injection, 500 mg and 1000 mg.

Packaging:

500 mg and 1000 mg in glass bottles.

For 1 or 10 bottles together with instructions for use in a pack of cardboard.

10 vials with instructions for use in a pack of cardboard with a cardboard insert for fixing the vials.

For hospitals: 270 vials, together 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.

A freshly prepared plant is suitable for use for 12 hours at room temperature not higher than 25 ° C.

Keep out of the reach of children.

Shelf life:

2 years.

It is recommended to use before the time specified on the package.

Terms of leave from pharmacies:On prescription

Registration number:LP-001790

Date of registration:06.08.2012

Date of cancellation:2017-08-06

The owner of the registration certificate:BORISOVSKIY FACTORY OF MEDPREPARATES, OJSC BORISOVSKIY FACTORY OF MEDPREPARATES, OJSC Republic of Belarus

Manufacturer: & nbsp

BORISOVSKIY FACTORY OF MEDPREPARATES, OJSC Republic of Belarus

Information update date: & nbsp02.11.2015

Illustrated instructions

Instructions

Cefotaxime (Cefotaxime)