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

Cefotaxime is a third generation cephalosporin antibiotic for parenteral use. It acts bactericidal, disrupting the synthesis of the cell wall of microorganisms. It has a wide spectrum of antimicrobial 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 (for

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 meningitidis, Neisseria gonorrhoeae (including strains forming penicillinase), Acinetobacter spp., Corynebacterium diphthenae, Erysipelothrix rhusiopathiae, Eubacterium 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, Bacteroides spp. (including some strains of Bacteroides fragilis), Fusobacterium spp. (including Fusobacterium nucleatum), Peptococcus spp., Peptostreptococcus spp.

Most strains of Clostridium are difficile-resistant.

Resistant to most beta-lactamases of gram-positive and gram-negative microorganisms.

Pharmacokinetics:

After a single intravenous injection of the drug at doses of 0.5 g, 1.0 g and 2.0 g, the time required to reach the maximum concentration (Cmax) is 5 minutes and the maximum concentration is about 39, 101.7 and 214 μg / ml, respectively. After intramuscular injection of the drug at doses of 0.5 g and 1.0 g, the maximum concentration is reached after 0.5 h and is about 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, bone, 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.

Half-life (T1 / 2) - about 1 hour with intravenous administration and about 1-1.5 hours - with 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, which retains bactericidal activity, 20-25% - in the form of 2 metabolites - M2 and M3, not having antimicrobial action).

In chronic renal failure (CRF) and in elderly people, the elimination half-life is doubled. The half-life period (T1 / 2) in newborns is about 0.75-1.5 hours, in preterm infants (body weight less than 1500 g) increases to 4.6 hours, in children weighing more than 1500 g - about 3, 4 hours For repeated intravenous doses of 1.0 g every 6 hours for 14 days of cumulation is not observed.

Indications:

Infectious-inflammatory diseases caused by microorganisms susceptible to cefotaxime: 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, salmonellosis, infection against the background of immunodeficiency.

Prevention of infections after surgery (including urological, obstetric-gynecological, on the gastrointestinal tract).

Contraindications:

- increased sensitivity (including penicillins, other cephalosporins, carbapenems);

- pregnancy I trimester;

- intracardiac blockade without an established pacemaker;

- severe heart failure;

- children's age to 2.5 years (for intramuscular injection).

When using lidocaine as a solvent: increased sensitivity to lidocaine or other local anesthetic of the amide type.

Carefully:

Newborn period (for intravenous administration), chronic renal failure, ulcerative colitis (including in the anamnesis).

Pregnancy and lactation:

Cefotaxime penetrates the placental barrier and is excreted in breast milk. Application in the II and III trimesters of pregnancy is possible in the event that the intended benefit to the mother exceeds the potential risk to the fetus; 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 weighing 50 kg or more:

- with uncomplicated infections - intramuscularly or intravenously, 1 g every 12 hours;

- with uncomplicated acute gonorrhea intramuscularly 0.5 - 1 g once;

- for infections of moderate severity intravenously or intramuscularly, 1-2 g every 8 hours;

- with sepsis - intravenously 2 g every 6-8 h;

- with life-threatening infections (meningitis) - intravenously 2 g every 4 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, enter 1 g during the initial general anesthesia. If necessary, the administration is repeated after 6-12 hours.

At caesarean section (at the moment of imposing of clamps on an umbilical vein) -

intravenously, 1 g, then 6 and 12 hours after the first dose - an additional 1 g.

With a creatinine clearance of 20 mL / min / 1.73 square meters or less, the daily dose is reduced by a factor of 2.

For children:

- premature and newborns 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 from 1 month to 12 years with a body weight of less than 50 kg - intravenously or intramuscularly (children over 2,5 years) 50-180 mg / kg in 4-6 injections.

At a serious current of infections, incl. meningitis, intravenously or intramuscularly 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 the solvent (1 g of the preparation is diluted in 10 ml of the solvent). Enter slowly for 3-5 minutes.

For intravenous infusion 0.9% solution of sodium chloride or 5% dextrose solution is used as the solvent (1 g is diluted in 50 ml of solvent). The duration of the infusion is 50-60 minutes.

For intramuscular injection use water for injection or 1% lidocaine solution (1 g of the drug diluted in 4 ml of the solvent). Enter deep into the gluteal muscle.

Side effects:

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

From the nervous system: headache, dizziness, encephalopathy, movement disorders, convulsions;

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

From the digestive system: nausea, vomiting, diarrhea or constipation, flatulence, abdominal pain, dysbiosis, impaired liver function, hepatitis, jaundice, stomatitis, glossitis, pseudomembranous colitis.

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

Co cardiovascular system: Potentially life-threatening arrhythmias after a fast bolus injection into the central vein.

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

Laboratory indicators: azotemia, increased urea concentration in the blood, increased activity of "liver" transaminases and alkaline phosphatase, hypercreatininaemia, hyperbilirubinemia, false-positive Coombs 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 therapy.

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 (incl. allopurinol, diuretics), increase plasma concentrations of cefotaxime and slow its elimination.

Cefotaxime is pharmaceutically incompatible with solutions of other antibiotics in a single 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.

When treating cefotaxime for more than 10 days, control of the number of blood elements is necessary.

Older and weaker patients are recommended to prescribe vitamin K (prevention of hypocoagulation).

During treatment with cefotaxime, it is possible to obtain a false-positive Coombs test and a false positive urine reaction to glucose (when determining glucose in the urine by a non-enzymatic method, for example - by the method of Benedict).

When combined with ethanol, disulfiram-like reactions are possible.

Effect on the ability to drive transp. cf. and fur:

Given the potential for side effects, patients during treatment with cefotaxime should be careful when driving vehicles and engaging in other potentially dangerous activities that require increased concentration and speed of psychomotor reactions.

Form release / dosage:

Powder for solution for intravenous and intramuscular injection, 1.0 g.

Packaging:

By 1.0 g of active substance (cefotaxime) into 10 ml vials hermetically sealed with rubber stoppers, crimped with aluminum or combined caps.

1 bottle with instruction for use is placed in an individual pack of cardboard.

50 bottles with an equal number of instructions for use are placed in a box of cardboard (for hospitals).

Storage conditions:

In a dry, protected from light 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 expiry date printed on the package.

Terms of leave from pharmacies:On prescription

Registration number:LP-001545

Date of registration:28.02.2012

Date of cancellation:2017-02-28

The owner of the registration certificate:Company DEKO, LLC Company DEKO, LLC Russia

Manufacturer: & nbsp

Company DEKO, LLC Russia

Information update date: & nbsp01.11.2015

Illustrated instructions

Instructions

Cefotaxime (Cefotaxime)