Cefotaxime - 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) and Staphylococcus epidermidis (with the exception of Staphylococcus epidermidis and Staphylococcus aureus, resistant to methicillin)), 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, Neisseria gonorrhoeae (including strains forming penicillinase), Acinetobacter spp., Corynebacterium diphtheriae, Erysipelothrix rhusiopathiae, Eubercul spp., Propionibacterium spp.,. Clostridium spp. (incl.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 dose of 0.5 g, 1 g and 2 g, the maximum concentration in the blood plasma (Cmax) is determined after 5 minutes and is 39 μg / ml, 101.7 μg / ml and 214 μg / ml, respectively. After intramuscular injection of the drug in doses of 0.5 g and 1 g of C max is determined after 30 minutes and is 11 μg / ml and 21 μg / ml, respectively. Communication with blood plasma proteins is 30-50%. Bioavailability is 90-95%. Creates therapeutic concentrations in most tissues (myocardium, bones, gall bladder, skin, soft tissues) and fluids (synovial, pericardial, pleural, cerebrospinal fluid, sputum, bile, urine) of the body. The volume of distribution is 0.25-0.39 l / kg.

The half-life (T1 / 2) is 1 hour with IV injection and 1-1.5 hours with the IM. It is excreted by the kidneys - 20-36% unchanged, the rest amount - in the form of metabolites (12-25% - in the form of pharmacologically active deacetylcefotaxime and 20-25% in the form of 2 inactive metabolites - M2 and M3, devoid of antimicrobial action).

In chronic renal failure (CRF) and in elderly people, T1 / 2 increases by 2 times. T1 / 2 in newborn - 0.75-1.5 hours in premature neonates (body weight less than 1500 g) was increased to 4.6 hours; in children with a body weight of more than 1500 g - 3.4 hours. With repeated iv administration in doses of 1 g every 6 hours for 14 days cumulation is not observed. Penetrates into breast milk, passes through the placental barrier.

Indications:Infectious-inflammatory diseases, caused by susceptible microorganisms -th: infections of the central nervous system (meningitis), respiratory tract and LOP -organov, urinary tract, bones, joints, skin and soft tissue of the pelvic organs, gonorrhea, infected wounds and burns, peritonitis , sepsis, abdominal infection, endocarditis, Lyme disease (borreliosis), salmonellosis, infection on the background of immunodeficiency -ta, prevention of infection after surgery (including urological, obstetrical on gastrointestinal t cancer).

Contraindications:Hypersensitivity (including penicillins, etc.)cephalosporins, carbapenems), pregnancy, children under 2.5 years (for intramuscular route of administration).

Carefully:Newborn period (for intravenous administration), lactation period, chronic renal insufficiency, ulcerative colitis (including in the anamnesis).

Pregnancy and lactation:The use of the drug during pregnancy is contraindicated. If it is necessary to prescribe the drug during lactation, breastfeeding should be stopped.

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):

- with uncomplicated infections, as well as with 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.

For the purpose of preventing the development of infections before the surgical operation is introduced during the introductory general anesthesia once 1 g.If necessary, the administration is repeated after 6-12 hours.

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

When creatinine clearance (CC) is 20 ml / min / 1.73 m2 or less, the daily dose is reduced by 2 times.

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

Children from 1 month. (with a body weight of up to 50 kg) - in / in or / m (over the age of 2.5 years) 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, IM or IV in 4 to 6 receptions, the maximum daily dose is 12 g.

Rules for the preparation of injection solutions: for water injection, water for injection is used as a solvent (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% sodium chloride solution or 5% dextrose solution is used as the solvent (1-2 g diluted in 50-100 ml solvent); duration of infusion is 50-60 minutes; for the / m administration using 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 cardiovascular system:

potentially life-threatening arrhythmias after a rapid bolus injection into the central vein.

From the central nervous system: headache, dizziness.

From the gastrointestinal tract:

nausea, vomiting, diarrhea or constipation, flatulence, abdominal pain, dysbiosis, violation

liver function, rarely - stomatitis, glossitis, pseudomembranous enterocolitis.

From the urinary system:

disturbance of kidney function, oliguria, interstitial nephritis.

From the hematopoiesis:

hemolytic anemia, leukopenia, neutropenia, granulocytopenia, thrombocytopenia,

hypocoagulation.

Laboratory indicators:

azotemia, increased urea concentration in the blood, increased activity of "liver" transaminases. and alkaline phosphatase, hypercreatininaemia, hyperbilirubinemia, Coombs positive reaction.

Local reactions:

phlebitis, pain along the vein, soreness and infiltration in place

intramuscular injection.

Other: Superinfection (in particular, candidal vaginitis).

Overdose:Symptoms: convulsions, encephalopathy (in case of 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, 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 the plasma concentrations of cefotaxime and slow down its excretion.

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 the antibiotics of the cephalosporin group.

When the drug is treated for more than 10 days, it is necessary to monitor the pattern of peripheral blood.

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, use ethanol it is impossible because of the possibility of disulfiram-like reactions (facial hyperemia, abdominal and stomach cramps, nausea, vomiting, headache, lowering of blood pressure, tachycardia, dyspnea).

Form release / dosage:Powder for the preparation of solution for intravenous and intramuscular administration of 1000 mg.

Packaging:1000 mg of active substance in a vial of transparent glass, sealed with a stopper of chlorobutyl rubber, crimped with an aluminum cap with a safety plastic lid. 1 bottle with instructions for use in a cardboard box.

For hospitals: 50 bottles in a cardboard box.

Storage conditions:List B. In a dry, the 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 expiry date.

Terms of leave from pharmacies:On prescription

Registration number:П N012823 / 01

Date of registration:07.08.2008

The owner of the registration certificate:Aquarium EnterpriseAquarium Enterprise India

Manufacturer: & nbsp

AQUARIUS ENTERPRISES India

Representation: & nbspAquarium EnterpriseAquarium EnterpriseIndia

Information update date: & nbsp04.11.2015

Illustrated instructions

Instructions

Cefotaxime (Cefotaxime)