Pharmacological properties
Cefotaxime ((6r, 7r) -3 [(acetyloxy) methyl] -7 [[(z) -2- (2-aminothiazol-4-yl) -2- (methoxyimino-acetyl] amino] -8-oxo-5 -thia-1-azabicyclo [4,2,0] oct-2-ene-2-carboxylate sodium) is a semi-synthetic antibiotic of the 3rd generation cephalosporin group. The features of the chemical structure provide high activity of the drug against gram-negative bacteria, resistance to the effects of beta-lactamases produced by them. The drug acts bactericidally. It has a wide spectrum of action, including against microorganisms resistant to other cephalosporins and penicillin antibiotics.
Active against gram-positive microorganisms (Staphylococcus spp., including beta-lactamase-producing, Streptococcus spp., except group D); gram-negative microorganisms (Citrobacter spp., Enterobacter spp., E. coli, Haemophilus influenzae, Klebsiella spp., including K. pneumoniae, Moraxella spp., Neisseria gonorrhoeae, N. meningitidis, Proteus mirabilis., P. vulgaris, Providencia spp., Salmonella spp., Serratia spp., Shigella spp., Yersinia spp.); anaerobic microorganisms (Fusobacterium spp., Veilonella spp.). Pseudomonas aeruginosa, Acinetobacter spp., Helicobacter pylori, Bacteroides fragilis and Clostridium difficile are not consistently sensitive to the drug.
Group D streptococci, Listeria spp. and methicillin-resistant staphylococci are resistant to the drug.
In adults, 5 minutes after a single intravenous injection of 1 g, the plasma concentration is 100 μg/ml. After intramuscular injection of the same dose, the maximum plasma concentration is observed after 0.5 h and is 20-30 μg/ml. The half-life is 1 h after intravenous injection and 1-1.5 h after intramuscular injection. 25-40% of cefotaxime binds to plasma proteins (mainly albumin). About 90% of the administered dose is excreted in the urine, 50% in unchanged form and about 20% in the form of the metabolite desacetylcefotaxime. In the elderly, the half-life of cefotaxime increases to 2.5 h. In adults with impaired renal function, the volume of distribution does not change, the half-life does not exceed 2.5 h.
In children, plasma levels and volume of distribution are similar to those in adults receiving the same dose of the drug on a mg/kg basis. The elimination half-life is 0.75 to 1.5 hours.
Indication
Infections caused by microorganisms sensitive to the drug: respiratory system infections (bronchitis, pneumonia, pleurisy, lung abscess); meningitis, septicemia, endocarditis; ear, throat, nose infections; urinary tract, kidney infections;
gynecological infections; infections of the skin, soft tissues, bones and joints, abdominal organs; acute uncomplicated gonorrhea; infected wounds and burns.
In surgical practice, the drug is used to reduce the risk of developing postoperative infections, especially during operations on the digestive tract, urological and obstetric-gynecological interventions.
Application
Administered intramuscularly or intravenously (jet or drip).
For intramuscular injection, dissolve 0.25 g or 0.5 g of the drug in 2 ml (1 g in 3 ml) of sterile water for injection. Inject deeply into the gluteal muscle.
For intravenous injection, dissolve 0.25 g or 0.5 g in 2 ml (1 g in 4 ml) of sterile water for injection. Administer slowly over 3-5 minutes.
For intravenous drip administration, dissolve 2 g of the drug in 100 ml of isotonic sodium chloride solution or 5% glucose solution, and inject over 50-60 minutes.
The prepared solutions are stable for up to 24 hours when stored in a refrigerator (4-6 °C) and 12 hours at a temperature not exceeding 23 °C. The yellowish-amber color of the prepared solution does not indicate a decrease in the effectiveness and safety of the antibiotic.
The usual dose of the drug for adults is 1 g every 12 hours. In severe cases, the dose is increased to 2 g every 12 hours or the number of injections is increased to 3-4 times a day, bringing the total daily dose to the maximum - 12 g.
The usual daily dose for newborns and children weighing up to 50 kg is 50-100 mg per 1 kg of body weight and is divided into 3-4 intramuscular or intravenous injections. In severe infections, including meningitis, the daily dose is doubled.
Children weighing 50 kg or more are prescribed the drug in the same dose as adults.
For premature babies, the daily dose should not exceed 50 mg/kg. In case of impaired renal function, the dose is reduced (with creatinine clearance of 10 ml/min or less, half the dose of the drug is taken).
Contraindication
Hypersensitivity to cephalosporin drugs.
Side effects
Allergic reactions, dyspeptic phenomena, eosinophilia, leukopenia, increased liver function tests, LF activity, and nitrogen content in urine are possible. Irritation at the injection site and fever may occur.
Special instructions
Pseudomembranous colitis may occur in the first weeks of treatment, manifested by severe prolonged diarrhea. The diagnosis is confirmed by colonoscopy and / or the results of histological studies. Immediately stop the drug and prescribe adequate therapy, including oral vancomycin and metronidazole.
Cefotaxime-Darnitsa crosses the placental barrier. The safety of the drug during pregnancy has not been proven, so the drug should not be prescribed to pregnant women.
Cefotaxime-Darnitsa penetrates into breast milk, so if necessary, breastfeeding should be discontinued.
Interactions
When using cefotaxime-Darnitsa simultaneously with indirect anticoagulants, synergism is manifested. Aminoglycoside antibiotics and diuretics enhance the nephrotoxic properties of cefotaxime-Darnitsa.
The drug should not be mixed with other antibiotics either in the same syringe or in the same infusion solution.
Overdose
There is a risk of developing reversible encephalopathy when using cefotaxime-Darnitsa in high doses. There is no specific antidote. Treatment is symptomatic.
Storage conditions
In a dry, dark place at a temperature not exceeding 25 °C.
