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

Pharmacodynamics:Cephalosporin antibiotic III generation for parenteral administration. It acts bactericidal, disrupting the synthesis of the mucopeptide 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-producing strains), Staphylococcus epidermidis (with the exception of Staphylococcus epidermidis and Staphylococcus aureus, methicillin-resistant), Streptococcus pneumoniae, Streptococcus pyogenes (group A beta-hemolytic streptococci), Streptococcus agalactiae (Group B streptococci ), Enterococeus spp., Enterobacter spp., Escherichia coli, Haemophilus influenzae (including strains forming penicillinase), Haemophilus parainfluenzae, Moraxella catarrhalis, Klebsiella spp. (including Klebsiella pneumoniae, Klebsiella oxytoca), 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, Neisseria gonorrhoeae, Bacteroides spp. (including some strains of Bacteroides fragilis), Fusobacterium spp. (including Fusobacterium nucleatum), Peptococcus spp., Peptostreptococcus spp. Some strains of Pseudomonas aeruginosa, Acinetobacter, Helicobacter pylori, Bacteroides fragilis, Clostridium difficile are influenced not constantly. 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 to reach the maximum concentration (Cmax) is 5 minutes, Cmax is 39, 101.7 and 214 μg / ml, respectively. After intramuscular injection in doses of 0.5 and 1 g, the time to reach Cmax is 0.5 h, and is 11 and 21 μg / 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 intravenous administration and 1-1.5 hours for intramuscular 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). 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. With repeated intravenous doses of 1 g every 6 hours for 14 days of cumulation is not observed. Cefotaxime passes through the placenta, in small concentrations penetrates into breast milk.

Indications:Severe bacterial infections caused by susceptible microorganisms: infections of the central nervous system (meningitis), respiratory tract and LOP tract, urinary tract, bones, joints, skin and soft tissues, organs of small t, oa, peritonitis, septicemia, endocarditis; gonorrhea; infected wounds and burns; abdominal infections, salmonellosis, Lyme disease, infections on the background of immunodeficiency, prevention of infections after surgery (including urological, obstetric-gynecological, on the organs of the gastrointestinal tract).

Contraindications:

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

- Pregnancy;

- Children's age of up to 2.5 years (for intramuscular injection).

Carefully:

- in the period of newborn;

- during lactation (in small concentrations is excreted with milk);

- with chronic renal insufficiency;

- with nonspecific ulcerative colitis (including anamnesis).

Dosing and Administration:

The drug is administered intravenously (jet or drip) and intramuscularly.

Adults and children over 12 years of age (with a body weight of 50 kg or more): for uncomplicated infections, as well as for infections of the urinary tract, either intramuscularly or intravenously, 1 g every 8-12 hours; with uncomplicated acute gonorrhea - intramuscularly, 1 g once; at infections of average gravity - intramuscularly or intravenously, 1-2 g every 12 h; in severe infections, for example, with meningitis - intravenously, 2 g every 4-8 hours, maximum daily dose - 12 g. Duration of treatment is set individually.

With the purpose of preventing the development of infections before the surgical operation is introduced during the initial anesthesia once 1 g. If necessary, the administration is repeated after 6-12 hours. With caesarean section - at the time of application of the clamps on the umbilical vein, intravenously, 1 g, then 6 and 12 h after the first dose - an additional 1 g.

With a creatinine clearance of 20 ml / min / 1.73 m² and less, the daily dose is reduced by 2 times.

Premature and newborn before 1 week - intravenously, 50 mg / kg every 12 hours; at the age of 1-4 weeks - intravenously, 50 mg / kg every 8 hours; children weighing up to 50 kg-intravenously or intramuscularly, 50-180 mg / kg in 4-6 injections. In severe infections, including meningitis, the daily dose to children is increased to 100-200 mg / kg, intramuscularly or intravenously, in 4-6 receptions, the maximum daily dose is 12 g.

Rules for the preparation of injection solutions:

for intravenous injection, water for injection is used as a solvent (0.5-1 g diluted in 4 ml of solvent, 2 g in 10 ml); the drug is injected slowly for 3-5 minutes.

for intravenous infusion, 0.9% NaCl solution or 5% dextrose solution is used as the solvent (1-2 g diluted in 50-100 ml of solvent). Duration of infusion - 50-60 minutes;

for intramuscular injection water for injection or 1% solution of lidocaine (for a dose of 0.5 g - 2 ml, for a dose of 1 g - 4 ml).

Side effects:

Allergic reactions: urticaria, chills or fever, rash, itching, rarely - 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 gastrointestinal tract: nausea, vomiting, diarrhea or constipation, flatulence, abdominal pain, dysbiosis, impaired liver function, rarely - stomatitis, glossitis, pseudomembranous enterocolitis.

On the part of the organs of hematopoiesis: hemolytic anemia, leukopenia, neutropenia, granulocytopenia, thrombocytopenia, agranulocytosis, 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 "liver" transaminases and alkaline phosphatase, hypercreatininaemia, hyperbilirubinemia, positive Coombs reaction.

Local Reactions: phlebitis, pain along the vein, soreness and infiltration at the site of intramuscular injection.

Other: superinfection (in particular, vaginal and oral candidiasis).

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 the simultaneous administration of 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 treating with a drug for more than 10 days, monitoring of the peripheral blood pattern is necessary.During treatment with cefotaxime, it is possible to obtain a false-positive Coombs test and a false positive urine reaction to glucose;

- if it is necessary to prescribe the drug during lactation, breastfeeding should be stopped;

- 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).

Form release / dosage:Powder for solution for intravenous and intramuscular injection 1 g.

Packaging:1 g (in terms of cefotaxime) in hermetically sealed vials of colorless transparent glass. The bottle is sealed with a rubber stopper, crimped with an aluminum cap with a plastic cap for monitoring the first opening or without it. 1 bottle together with the instruction for use is placed in a cardboard box.

For 10, 50, 100 vials together with the instruction for use are placed in a cardboard box (for hospitals).

Storage conditions:

Store in a dry, dark place at a temperature of no higher than 25 ° C. Keep out of the reach of children.

Shelf life:

2 years.Do not use after the expiration date.

Terms of leave from pharmacies:On prescription

Registration number:LSR-000024

Date of registration:07.11.2007

The owner of the registration certificate:North China Pharmaceutical Corporation Co., Ltd.North China Pharmaceutical Corporation Co., Ltd. China

Manufacturer: & nbsp

NORTH CHINA PHARMACEUTICAL CORPORATION China

Representation: & nbspVIAL, LLCVIAL, LLC

Information update date: & nbsp04.11.2015

Illustrated instructions

Instructions

Cefotaxime-Vial (Cefotaxime-Vial)