Composition, form of production and packaging
Powder for solution for iv and in / m introduction white or white with a yellowish tinge.
1 f.
cefotaxime (in the form of the sodium salt) 500 mg
Vials (1) - packs of cardboard.
Bottles (50) - packs of cardboard.
Powder for solution for iv and in / m introduction white or white with a yellowish tinge.
1 f.
cefotaxime (in the form of the sodium salt) 1 g
Vials (1) - packs of cardboard.
Bottles (50) - packs of cardboard.
Powder for solution for iv and in / m introduction white or white with a yellowish tinge.
1 f.
cefotaxime (in the form of the sodium salt) 2 g
Vials (1) - packs of cardboard.
Bottles (50) - packs of cardboard.
INSTRUCTION FOR THE SPECIALIST.
Description of the drug approved by the manufacturer for the printed edition of 2008.
PHARMACHOLOGIC EFFECT
Cephalosporin antibiotic III generation of a broad spectrum of action. It acts bactericidal, disrupting the synthesis of the bacterial cell wall.
Cefosin is active against gram-positive bacteria: Staphylococcus spp. (including Staphylococcus aureus (including strains forming penicillinase), Staphylococcus epidermidis), Streptococcus spp. (including Streptococcus pneumoniae, Streptococcus pyogenes, Streptococcus agalactiae), Enterococcus spp., Corynebacterium diphtheriae, Erysipelothrix insidiosa, Bacillus subtilis; Gram-negative bacteria: Enterobacter spp., Escherichia coli, Haemophilus influenzae (including strains forming penicillinase), Haemophilus parainfluenzae, Citrobacter spp., Proteus spp. (including Proteus mirabilis, Proteus vulgaris, Proteus indole), Providencia spp.(including Providencia rettgeri), Klebsiella spp. (including Klebsiella pneumoniae), Serratia spp., Pseudomonas aeruginosa, Morganella morganii, Neisseria gonorrhoeae (including strains producing penicillinase), Neisseria meningitidis, Acinetobacter spp .; anaerobic bacteria: Clostridium spp. (including Clostridium perfringens), Eubacterium spp., Bacteroides spp. (including some strains of Bacteroides fragilis), Fusobacterium spp. (including Fusobacterium nucleatum), Peptococcus spp., Peptostreptococcus spp, Propionibacterium spp.
Cefotaxime is resistant to the action of? -lactamases of Gram-positive and Gram-negative bacteria, incl. to penicillinase of staphylococci and Clostridium difficile.
PHARMACOKINETICS
Suction
After a single intravenous administration of Cefosin at a dose of 500 mg, 1 g and 2 g of C max is achieved after 5 minutes and is 39 Ојg / ml, 100 Ојg / ml and 214 Ојg / ml, respectively.
After a / m administration of Cefosin in a dose of 500 mg and 1 g of C max is achieved after 5 minutes and is 11 Ојg / ml and 21 Ојg / ml, respectively.
Distribution
The binding with plasma proteins is 25-40%.
It is found in therapeutic concentrations in most tissues (myocardium, bones, gall bladder, skin, soft tissues) and fluids (pleural, peritoneal, synovial, urine, bile, spinal fluid, sputum).
V d = 0.25-0.39 l / kg.
With repeated iv administration in a dose of 1 g every 6 hours for 14 days of cumulation is not observed.
Cefotaxime excreted in breast milk.
Excretion
T 1/2 of cefotaxime for IV and IM is 1 hour.
Cefotaxime is excreted in the urine (60-70% - unchanged, the rest - in the form of metabolites / and the deacetylated derivative has bactericidal activity, and other metabolites - do not possess /).
Pharmacokinetics in special clinical cases
In chronic renal failure and in elderly patients, T 1/2 increases by a factor of 2.
In newborns, T 1/2 is from 0.75 h to 1.5 h, in preterm infants it increases to 4.6 h.
INDICATIONS
Bacterial infections caused by susceptible microorganisms:
- respiratory tract infections;
- urinary tract infections;
- infection of ENT organs;
- infections of bones and joints;
- skin and soft tissue infections;
- peritonitis;
- abdominal infections;
- infection of the pelvic organs;
- sepsis;
- endocarditis;
- CNS infections (including meningitis);
- Chlamydia;
- Gonorrhea;
- Lyme disease;
- salmonellosis;
- infected wounds and burns;
- infection in patients with immunodeficiency.
Prevention of infections after surgical interventions (including urological, obstetric-gynecological, on the digestive tract).
DOSING MODE
The drug is given in / m or in / in (jet or drip).
Adults and children over the age of 12 years are usually prescribed 1 g every 12 hours.
In severe cases - 3-4 g / day (injected 1 g 3-4 times / day).
The maximum daily dose is 12 g.
Newborns and children under 12 years of age, the drug is prescribed in a dose of 50-100 mg / kg body weight every 6-12 hours.
Premature babies are prescribed 50 mg / kg body weight.
In case of violations of kidney function, the dose is reduced. With KK? 10 ml / min, the daily dose of the drug is reduced by half.
Rules for the preparation and administration of solutions
For an intravenous injection, 500 mg of powder is dissolved in 2 ml (respectively 1 g in 4 ml) of sterile water for injection. As a solvent with the / m administration, 1% lidocaine can be used in the same proportions.
For intravenous administration of 0.5-1 g of powder is dissolved in 10 ml of sterile water for injection. Enter slowly for 3-5 minutes.
For intravenous drip, 2 g of powder is dissolved in 100 ml of isotonic sodium chloride solution or 5% dextrose (glucose) solution. Enter for 50-60 minutes.
SIDE EFFECT
On the part of the digestive system: nausea, vomiting, diarrhea, constipation, flatulence, abdominal pain, dysbiosis, liver dysfunction (increased activity of ALT, AST, AF in blood plasma, hypercreatinemia, hyperbilirubinemia); rarely - stomatitis, glossitis, pseudomembranous colitis.
On the part of the hematopoiesis system: leukopenia, neutropenia, granulocytopenia, thrombocytopenia, hemolytic anemia, hypocoagulation.
On the part of the urinary system: azotemia, oliguria, anuria, an increase in urea in the blood, interstitial nephritis.
From the side of the central nervous system: headache, dizziness.
From the side of the cardiovascular system: with the rapid bolus injection into the central vein, the development of potentially dangerous arrhythmias is possible.
Local reactions: phlebitis, tenderness along the vein during when in / in the introduction, soreness and infiltration - with the / m introduction.
Allergic reactions: urticaria, chills, fever, rash, itching; rarely - bronchospasm, eosinophilia, Stevens-Johnson syndrome, toxic epidermal necrolysis, angioedema, anaphylactic shock.
Other: superinfection (including candidal vaginitis), false-positive test of Coombs.
CONTRAINDICATIONS
- Hypersensitivity to cephalosporins, penicillins, carbapenems.
The drug is not administered to children under the age of 2.5 years.
With caution should prescribe the drug to newborns, patients with chronic kidney failure, ulcerative colitis (including in history), during lactation.
PREGNANCY AND LACTATION
The use of cefosin during pregnancy is possible only in cases where the intended use for the mother exceeds the potential risk to the fetus.
Cefotaxime excreted in breast milk. If necessary, the appointment in the lactation period should resolve the issue of stopping breastfeeding.
APPLICATION FOR FUNCTIONS OF THE LIVER
In case of violations of kidney function, the dose is reduced. With KK? 10 ml / min, the daily dose of the drug is reduced by half.
SPECIAL INSTRUCTIONS
Before prescribing the drug, you need to collect an allergic medical history, especially with regard to beta-lactam antibiotics. It should be borne in mind that it is possible to develop a cross-allergy between penicillins and cephalosporins. The drug is administered with caution to patients who have a history of allergic reactions to penicillin (should take into account the possibility of developing severe anaphylactic reactions, up to a lethal outcome).
In the first weeks of treatment, pseudomembranous colitis can develop, manifested by severe diarrhea. If this situation develops, cefosin should be discontinued and appropriate therapy should be prescribed, including metronidazole and vancomycin inside.
When determining glucose in the urine by a non-enzymatic method (for example, by the method of Benedict), false-positive results are possible.
If the duration of therapy is more than 10 days, the peripheral blood picture should be monitored.
OVERDOSE
Symptoms: convulsions, encephalopathy (with the administration of the drug in large doses, especially in renal failure), tremor, increased excitability.
Treatment: symptomatic therapy.
DRUG INTERACTION
With the simultaneous use of Cefosin and nephrotoxic drugs (aminoglycoside antibiotics, "loop" diuretics, polymyxin B), nephrotoxic effect may be enhanced.Therefore, it is necessary to monitor the kidney function with the simultaneous use of these drugs.
With the simultaneous appointment of Cefosin with antiplatelet agents, NSAIDs increase the risk of bleeding.
When combined with cefosin drugs blocking tubular secretion, plasma concentrations of cefotaxime increase and its excretion slows down.
Simultaneous application of Cefosin with ethanol does not lead to the development of disulfiram-like reactions.
Pharmaceutical interaction
The solution of Cefosin is incompatible with solutions of other antibiotics in one syringe or dropper.
TERMS OF RELEASE FROM PHARMACY
The drug is released by prescription.
TERMS AND CONDITIONS OF STORAGE
List B. The drug should be stored out of reach of children, dry, protected from light at a temperature of no higher than 25 В° C. Shelf life - 2 years.
