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

It is active against gram-positive and gram-negative microorganisms resistant to other antibiotics: Staphylococcus spp. (Including Staphylococcus aureus, including penicillinase forming strains), Staphylococcus epidermidis, Streptococcus pneumoniae, Streptococcus pyogenes, Streptococcus agalactiae, Enterococcus spccies, Enterobacter spp., Escherichia coli, Haemophilus influenzae (including strains forming penicillinase) , Haemophilus para influenzae, Klebssiclla spp. (Including Kl.pneumoniae), Morganella morganii, Neisseria gonorrhoeae (including strains forming penicillinase), Aeinetobacter species, Corynebacterium diphtheriae, Erysipelothrix insidiosa, Eubacterium spp., Propionibacterium spp., Bacillus subtilis, Clostridium spp . (Including Clostridium perfringens, Clostridium difficile strains most resistant to the drug), Escherichia coli, Citrobacter spp., Proteus mirabilis, Proteus indole, Proteus vulgaris, Providencia spp. (Including Providencia rettgeri), Serratia spp., Pseudomonas aeruginosa, Neisseria meningitidis, Bacteroides spp. (including some strains of Bacteroides fragilis), Fusobacterium spp. (including Fusobacterium nucleatum). Peptococcus spp., Peptostreptococcus spp.

It is resistant to most beta-lactamases of gram-positive and gram-negative microorganisms, penicillinase of staphylococci.

Pharmacokinetics:

After a single intravenous injection of 0.5, 1 and 2 g, the maximum concentration (C max) is reached after 5 minutes and is 39 μg / ml, 100 μg / ml and 214 μg / ml. respectively. After w / m 0.5 and 1 g of C max is achieved after 0.5 h and is 11 and 21 mcg / ml, respectively. The connection with plasma proteins is 25-40%. Creates therapeutic concentrations in most tissues (myocardium, bones, gallbladder, skin, soft tissues) and fluids (synovial, pericardial, pleural, sputum, bile, urine, spinal fluid) of the body. The volume of distribution is 0.25-0.39 l / kg.

The half-life (T1 / 2) for iv and / m administration is 1h.

It is excreted by the kidneys - 60% - 70% unchanged, the rest - in the form of metabolites (deacetylated derivative has bactericidal activity, and 2 other metabolites do not possess).

In chronic renal failure (XPS) and in the elderly, T1 / 2 increases 2-fold. T1 / 2 in newborns - 0.75-1.5 h, in preterm newborns it increases to 4.6 hours. For repeated IV injections, a dose of 1 g every 6 hours for 14 days of cumulation is not observed. Penetrates into breast milk.

Indications:Bacterial infections of severe course caused by sensitive microorganisms: infections of the central nervous system (meningitis),respiratory tract and ENT organs, urinary tract, bones, joints, skin and soft tissues, pelvic organs, chlamydia, gonorrhea, infected rashes and burns, peritonitis, sepsis, abdominal infections, endocarditis, Lyme disease (borreliosis), salmonellosis, infections against the background of immunodeficiency, the prevention of infections after surgical operations (including urological, obstetric-gynecological, on the gastrointestinal tract).

Contraindications:

Hypersensitivity (including to penicillins, other cephalosporins, carbapenems).

Children under 2.5 can not use intramuscular injection.

Carefully:Newborn period, lactation period (in small concentrations is excreted with milk); chronic renal failure, nonspecific ulcerative colitis (including anamnesis).

Pregnancy and lactation:

The use of the drug during pregnancy and lactation is possible only if the intended benefit to the mother exceeds the potential risk to the fetus.

Cefotaxime excreted in breast milk, so if you need to prescribe the drug during lactation should stop breastfeeding.

Dosing and Administration:

Intramuscularly and intravenously. For intramuscular injection, dissolve 1 g in 4 ml of sterile water for injection. Enter deep into the gluteal muscle. As a solvent, intramuscular injection also uses a 1% solution of lidocaine (per 1 g - 4 ml). For intravenous administration of 1 g cefotaxime and dissolved in 10 ml of sterile water for injection. Enter slowly for 3-5 minutes.

For drip administration (within 50-60 minutes), dissolve 2 g of the drug in 100 ml of isotonic sodium chloride solution or 5% glucose solution. The usual dose of cefotaxime for adults and children over 12 years is 1 g every 12 hours. In severe cases, the dose is increased to 3 or 4 g per day, the drug is administered 3 or 4 times 1 g. Depending on the severity of the disease, the daily dose can be increased to a maximum of 12 g.

The usual dose for newborns and children under 12 years is 50-100 mg / kg of body weight per day with intervals of administration from 6 to 12 hours. For premature babies, the daily dose should not exceed 50 mg / kg.

In the case of impaired renal function, the dose is reduced. With a creatinine clearance of 10 ml / min and a lesser daily dose of the drug is reduced by half.

Side effects:

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

On the part of the digestive system: nausea, vomiting, diarrhea or constipation, flatulence, abdominal pain, dysbiosis, impaired liver function (increased activity of "liver" transaminases, alkaline phosphogases, hypercreatininaemia, hyperbilirubinemia), stomatitis, glossitis, pseudomembranous enterocolitis.

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

On the part of the urinary system: a violation of the kidneys (azotemia, increased urea in the blood, oliguria, anuria, interstitial nephritis).

From the nervous system: headache, dizziness.

Laboratory indicators: false positive test of Coombs.

From the cardiovascular system: potentially life-threatening arrhythmias after a rapid bolus injection into the central vein.

Local reactions: phlebitis, pain along the vein, soreness and infiltration at the site of the / m introduction.

Other: superinfection (in particular, candidal vaginitis).

Overdose:Symptoms: convulsions, encephalopathy (in the case of the administration of large doses, especially in patients with renal insufficiency), tremor, increased neuromuscular excitability. Treatment: symptomatic therapy.

Interaction:

Increases the risk of bleeding when combined with anti-aggregates, non-steroidal anti-inflammatory drugs.

It does not lead to the development of disulfiram-like reactions when combined with ethanol.

The probability of kidney damage increases with simultaneous administration with 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.

Before prescribing the drug, you need to collect an allergic medical history, especially with regard to beta-lactam antibiotics. There is a cross-allergy between penicillins and cephalosporins. In persons who have a history of allergic reactions to penicillin, the drug is used with extreme caution (the possibility of developing severe anaphylactic reactions, up to a lethal outcome) should be considered.

With a duration of treatment with the drug for more than 10 days, it is necessary to monitor the picture of peripheral blood.

When determining glucose in the urine by a non-enzymatic method (for example, by the method of Benedict), false-positive results are possible.

Form release / dosage:

Powder for the preparation of a solution for intravenous and intramuscular injection of 1.0 g.

Packaging:

Powder for preparation of a solution for intravenous and intramuscular injection in vials of 1.0 g.

By 1.0 g in hermetically sealed vials of colorless clear glass according to K) ml. The bottle is sealed with a rubber stopper, crimped with an aluminum cap, and covered with a plastic lid.Each bottle is placed in a pack of cardboard along with instructions for medical use.

Storage conditions:At temperature ne above 25 ° C, in a dry place, protected from light and inaccessible to children.

Shelf life:2 years. Do not use after the expiry date indicated on the package.

Terms of leave from pharmacies:On prescription

Registration number:П N011901 / 01

Date of registration:09.07.2007

The owner of the registration certificate:M.Biotek LimitedM.Biotek Limited United Kingdom

Representation: & nbspSharan Pharma, LLCSharan Pharma, LLC

Information update date: & nbsp05.11.2015

Illustrated instructions

Instructions

Cefotaxime (Cefotaxime)