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

Pharmacodynamics:Cephalosporin antibiotic - III generation for parenteral administration. It acts bactericidal, breaking, the synthesis of the cell wall of microorganisms. Has a wide range of action. It is active against Gram-positive and Gram-negative microorganisms resistant to other antibiotics: Staphylococcus spp. (including Staphylococcus aureus, including penicillinase-forming staff), Staphylococcus epidermidis (with the exception of Staphylococcus epidermidis and Staphylococcus aureus, methicillin-resistant), Streptococcus pneumoniae, Streptococcus pyogenes (Group A beta beta-hemolytic streptococci), Streptococcus agalactiae (streptococci group B), Enterococcus spp., Enterobacter spp., Escherichiacoli, Haemophilus-influenzae (including penicillinase-forming strains), Haemophilus parainfluenzae, 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 perfringens), Citrobacter spp., Proteus mirabilis, Proteus vulgaris, Providencia spp. (including Providencia 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 a single intravenous (iv) dose of 1 g, the time to reach the maximum plasma concentration (TCmax) is 5 minutes, the maximum concentration of cefotaxime (Cmax) in plasma is about 101.7 μg / ml. After intramuscular (IM) in a dose of 1 g TCamax-0.5 h and is about 21 mcg / ml. The connection with plasma proteins is 30-50%. Bioavailability of 90-95%.

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

The half-life of cefotaxime (T1 / 2) -1h for IV administration and 1-1.5 h for IV administration. It is excreted by the kidneys, 20-36% unchanged, the rest is metabolites (15-25% in pharmacologically active deacetylcefotaxime and 20-25% in the form of 2 inactive metabolites).

In chronic renal failure and in the elderly, T1 / 2 increases by 2 times. T1 / 2 in newborns - 0.75-Oh h, in premature infants (body weight less than 1500 g) increases to 4.6 h, in children with a body weight of more than 1500 g - 3.4 h.With repeated iv injections in a dose of 1 g every 6 hours for 14 days cumulation is not observed. Cefotaxime passes through the placenta, in small concentrations penetrates into breast milk.

Indications:

Infectious-inflammatory diseases caused by sensitive drugs by microorganisms: central nervous system (meningitis), lower respiratory tract and ENT - organs, urinary tract, bones, joints, skin and soft tissues, pelvic organs; peritonitis, sepsis, endocarditis, gonorrhea, infected wounds and burns, intra-abdominal infections, salmonellosis, Lyme disease (borreliosis), infections with immunodeficiency.

Prevention of infections after surgical operations (including urological, obstetric-gynecological, on the organs of the gastrointestinal tract).

Contraindications:

- hypersensitivity (including penicillins, other cephalosporins, carbapenems);

- children's age to 2.5 years (for the / m introduction).

Carefully:

- in the period of neonatal (for intravenous administration);

- with chronic renal failure;

- with ulcerative colitis (including anamnesis).

Pregnancy and lactation:

During pregnancy, the drug is contraindicated.

If it is necessary to prescribe the drug during lactation, breastfeeding should be stopped.

Dosing and Administration:

Adults and children weighing 50 kg or more: with uncomplicated infections in / m or / in, 1 g every 12 h; with uncomplicated acute gonorrhea - in / m, 0.5-1 g once; with infections of medium severity - in / m or / in 1-2 g every 8 hours; with sepsis - in / in, 2 g every 6-8 hours, with life-threatening infections (with meningitis) - iv, 2 g every 4 hours, maximum daily dose - 12 g. Duration of treatment is set individually.

In order to prevent the development of infection before surgery, one is injected at the time of the initial general anesthesia, 1 g. If necessary, the administration is repeated after 6-12 hours. When the caesarean section (at the time of application of the clamps on the umbilical vein) -w, 1 g, 6 and 12 hours after the first dose - in addition to 1 g. With the creatinine clearance of 20 ml / min / 1.73 square meters or less, the daily dose is reduced by 2 times.

Premature and full-term newborns less than 7 days old - IV, 50 mg / kg every 12 hours; at the age of 1-4 weeks - in / in, 50 mg / kg every 8 l;

children older than 4 weeks, but with a body weight of up to 50 kg - in / in or / m 50-180 mg / kg in 4-6 injections.In severe infections, including meningitis, in / m or IV, in 4-6 receptions, the maximum daily dose is 12 g.

Rules for the preparation of injection solutions:

- for intravenous injection as a solvent water for injection is used (1 g diluted in 4 ml of solvent);

- For intravenous infusion, 0.9% sodium chloride solution or 5% dextrose solution is used as the solvent (1 -2 g is diluted in 50-100 ml of the solvent).

The duration of the infusion is 50-60 minutes.

- for the / m introduction use water for injection or 1% lidocaine (1 g - 4 ml).

Side effects:

Allergic reactions: urticaria, chills, rash, itching, bronchospasm, eosinophilia, malignant exudative erythema (Stevens-Johnson syndrome), toxic epidermal necrolysis (Lyell's syndrome), angioedema, anaphylactic shock.

From the central nervous system: headache, dizziness. From the urinary system: a violation of kidney function, oliguria, interstitial nephritis. From the hematopoiesis: hemolytic anemia, leukopenia (including granulocytopenia, neutropenia), thrombocytopenia, agranulocytosis, hypocoagulation. From the digestive system: nausea, vomiting, diarrhea or constipation, flatulence, abdominal pain, dysbiosis, impaired liver function, stomatitis, glossitis, pseudomembranous colitis. From the cardiovascular system: potentially life-threatening arrhythmias after a rapid bolus injection into the central vein.

Laboratory indicators: hyperaizotemia, increased urea concentration in the blood, increased activity of "liver" transaminases and alkaline phosphatase, hypercreatininemia, hyperbilirubinemia, false-positive Coombs reaction.

Local reactions: phlebitis, soreness along the vein, soreness and infiltration at the site of the / m introduction.

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 and 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 a single syringe or dropper.

Special instructions:

The preparation contains 51.75 mg (2.25 meq) of sodium.

- During 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 viacomycin or metronidazole. With the development of pseudomembranous colitis, it is contraindicated the use of drugs that inhibit intestinal peristalsis;

- the appointment of cephalosporins requires careful collection of allergic anamnesis: allergic diathesis, hypersensitivity reactions to beta-lactam antibiotics (for example, penicillins). A cross-allergy between cephalosporins and penicillins is known, which occurs in 5-10% of cases. Allergic (anaphylactic) reactions to penicillins and cephalosporins can be serious and endanger the life of the patient and may require appropriate medical interventions.The use of cefotaxime is strictly contraindicated in patients with a history of immediate hypersensitivity reaction to csphalosporins. In case of any doubt, the presence of a physician is necessary at the first administration of the drug, with the aim of immediate initiation of appropriate treatment in the event of the development of an anaphylactic reaction. If the patient develops a hypersensitivity reaction, the administration of cefotaxime should be immediately stopped and, if necessary, the appropriate treatment of the allergic reaction should be immediately initiated;

- when the drug is treated for more than 10 days, it is necessary to control the number of blood elements;

- during treatment with cefotaxime, it is possible to obtain a false positive Coombs test and a false positive urine reaction to glucose;

- during treatment can not be used ethanol Disulfiramoid-like effects are possible (facial hyperemia, stomach and stomach spasms, nausea, vomiting, lowering of blood pressure, headache, tachycardia, dyspnea). For a kit with a solvent: When using lidocaine as a solvent, the information given in the instructions for the use of lidocaine should be taken into account; and,that the lidocaine solution is used as a solvent only when administered intramuscularly.

Effect on the ability to drive transp. cf. and fur:According to the effect of the drug on the ability to drive vehicles and occupy other potentially dangerous activities that require increased concentration of data, there is no data, but taking into account the possibility of developing side effects from the central nervous system, care should be taken.

Form release / dosage:

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

Packaging:

Powder for the preparation of a solution for intravenous and intramuscular injection of 1000 mg in bottles with a capacity of 10, 20 ml, hermetically sealed with rubber stoppers and crimped with aluminum caps.

Solvent - "Lidocaine", injection for 10 mg / ml, produced by JSC "Dalhimpharm", Russia (registration certificate No. P N001261 / 01).

1. For 1, 2, 5 and 10 vials with the drug, together with the instructions for use, put in a pack of cardboard.

2. For 50 vials with the drug, together with 5 instructions for the use of 100 vials with the drug, along with 10 instructions for use, put in a box of cardboard (for hospitals).

3. 1 bottle with the drug and 1 ampoule with the solvent, along with instructions for medical use, are put in a pack of cardboard.

Storage conditions:

In a dry, the dark place at a temperature of 15 ° C to 25 ° C. Keep out of the reach of children.

Shelf life:

2 years. Do not use after the expiration date printed on the package.

Terms of leave from pharmacies:On prescription

Registration number:LP-000261

Date of registration:16.02.2011

Date of cancellation:2016-02-16

The owner of the registration certificate:RUZFARMA, LLC RUZFARMA, LLC Russia

Manufacturer: & nbsp

RUZFARMA, LLC Russia

DALHIMFARM, OJSC Russia

Information update date: & nbsp02.11.2015

Illustrated instructions

Instructions

Cefotaxime (Cefotaxime)