Cefotaxime DS - 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 range of action.

It is active against gram-positive and gram-negative microorganisms resistant to other antibiotics: Staphylococcus spp. (Including Staphylococcus aureus, including strains forming penicillinase), Staphylococcus epidermidis (except for Staphylococcus epidermidis and Staphylococcus, aureus, methicillin-resistant), Streptococcus pneumoniae, Streptococcus pyogenes, Streptococcus agalactiae, Enterococcus spp., Enterobacter spp., Escherichia coli, Haemophilus influenzae (including strains forming penicillinase), Haemophilus parainfluenzae, Moraxella catarrhalis, Klebsiella spp. (including Klebsiella pneumoniae), Morganella morganii, (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 injection at doses of 0.5, 1 and 2 g, the time required to reach the maximum concentration (TC_m_Oh) - 5. min, the maximum concentration (C_m_Oh) is 39, 101.7 and 214 μg / ml, respectively. After intramuscular injection at doses of 0.5 and 1 g of TC_m_Oh- 0.5 h and is 11 and 21 mcg / ml, respectively. The connection with plasma proteins is 30-50%. Bioavailability is 90-95%.

Creates therapeutic concentrations in most tissues (myocardium, bones, gallbladder, skin, soft tissues) and fluids (synovial, pericardial, pleural, sputum, bile, urine, cerebrospinal fluid) of the body. The volume of distribution is -0.25-0.39 l / kg. The half-life (T1 / 2) is 1 hour for IV injections and 1-1.5 hours for 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 the elderly, T1 / 2 increases by 2 times. T1 /2 in newborns - 0.75-1.5 h, in preterm 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. For repeated IV injections, a dose of 1 g every 6 hours for 14 days of cumulation is not observed. Penetrates into breast milk and passes through the placenta.

Indications:Bacterial infections of the severe course caused by susceptible microorganisms: infections of the central nervous system (meningitis), respiratory tract and LOP organs, urinary tract, bones, joints, skin and soft tissues, 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, obstetric-gynecological, gastrointestinal trauma kte).

Contraindications:Hypersensitivity (including penicillins, other cephalosporins, carbapenems), pregnancy, children under 2.5 years (for intramuscular injection).

Carefully:Newborn period (for intravenous administration), lactation period (in small concentrations is excreted with milk); chronic renal failure, nonspecific ulcerative colitis (including anamnesis).

Dosing and Administration:The drug is administered to adults and children with a body weight of 50 kg or more: for uncomplicated infections, as well as for infections of the urinary tract - in / m or / in, 1 g every 8-12 h; with uncomplicated acute gonorrhea - in / m, 1 g once; at infections of average gravity - in / m or in / in, on 1-2 g every 12 h; in severe infections, for example, with meningitis - in / in, 2 g every 4-8 hours, the maximum daily dose - 12 g.

Duration of treatment is set individually.

FROM prevention the development of infections before the surgical operation is administered during the introductory general anesthesia once 1 g. If necessary, the administration is repeated after 6-12 hours.

At cesarean section - at the time of application of the clamps to the umbilical vein - iv, 1 g, then 6 hours and 12 hours after the first dose - 1 g additionally.

With the clearance of creatinine (CC) 20 ml / min / 1.73 m2 and less than the daily dose is reduced by 2 times.

Premature and newborn before 1 week - IV, 50 mg / kg every 12 hours; at the age of 1-4 weeks - in / in, 50 mg / kg every 8 hours;

Children from 1 months to 2.5 years - iv 50-180 mg / kg in 4-6 injections.

Children older than 2.5 years, body weight up to 50 kg - in / in or / m 50-180 mg / kg in 4-6 injections. In severe infections, incl. meningitis, the daily dose to children is increased to 100-200 mg / kg, 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 used water for injection (1 g diluted in 4 ml of solvent), the drug is administered slowly for 3-5 minutes; for intravenous infusion, 0.9% sodium chloride solution or 5% dextrose solution is used as the solvent (1-2 g 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 solution (for a dose of 1 g - 4 ml).

Side effects:

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

From the nervous system: headache, dizziness.

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

From the urinary system: disturbance of kidney function, oliguria, interstitial nephritis.

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

From the hematopoiesis: hemolytic anemia, leukopenia, neutropenia, granulocytopenia, thrombocytopenia, hypocoagulation.

From the side of the cardiovascular system: potentially life-threatening arrhythmias after a rapid bolus injection into the central vein.

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

Other: superinfection (in particular, candidal vaginitis).

Overdose:Symptoms: seizures, encephalopathy (in the case of high 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 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.

During treatment can not be used ethanol - possible effects similar to the action of disulfiram (facial hyperemia, stomach and stomach spasms, nausea, vomiting, headache, lowering blood pressure, tachycardia, dyspnea). If it is necessary to prescribe the drug during lactation, breastfeeding should be stopped.

Form release / dosage:

Powder for solution for intramuscular and intravenous administration 1 g.

Packaging:

By 1.0 g in a bottle of 15 ml of clear glass, sealed with a gray stopper made of butyl rubber, crimped aluminum ring.

1 bottle with instructions for use in a cardboard box.

Storage conditions:In a dry, dark place at a temperature of no higher than 25 ° C. Keep out of the reach of children.

Shelf life:3 years. Do not use after the expiration date.

Terms of leave from pharmacies:On prescription

Registration number:LSR-005800/08

Date of registration:22.07.2008

The owner of the registration certificate:Mekofar Chemical-Pharmaceutical Joint Stock CompanyMekofar Chemical-Pharmaceutical Joint Stock Company Vietnam

Manufacturer: & nbsp

MEKOPHAR CHEMICAL-PHARMACEUTICAL, Joint Stock Company Vietnam

Representation: & nbspDominanta-Service CJSCDominanta-Service CJSC

Information update date: & nbsp04.11.2015

Illustrated instructions

Instructions

Cefotaxime DS (Cefotaxime DS)