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

Pharmacodynamics:Cefotaxime is a third generation cephalosporin antibiotic for parenteral use. It is bactericidal. 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 penicillinase forming strains), Staphylococcus epidermidis, Streptococcus pneumoniae, Streptococcus pyogenes, Streptococcus agalactiae, Enterococcus species, Enterobacter spp., Escherichia coli, Haemophilus influenzae (including strains forming penicillinase) , Haemophilus parain-fluenzae, Klebssiella spp. (including Kl.pneumoniae), Morganella morganii, Neisseria gonorrhoeae (including strains forming penicillinase), Acinetobacter species, Corynebacterium diphtheriae, Erysipelothrix insidiosa, Eubacterium spp., Propionibacterium spp., Bacillus subtilis, Clostridium spp . (including Clostridium perfringens), Escherichia coli, Citrobacter spp., Proteus mirabilis, Proteus indole, Proteus vulgaris, Providencia spp. (including Providencia rettgeri), Serratia spp., Pseudo-monas aeruginosa, Neisseria meningitidis, Bacteroides spp. (including some strains of Bacteroides fragilis), Fusobacterium spp. (including Fusobacterium nuclea-tum), Peptococcus spp., Peptostreptococcus spp.

Resistant to most beta-lactamases of Gram-positive and Gram-negative microorganisms, Staphylococcus Penicillinase, Clostridium difficile.

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, cerebrospinal fluid) of the body. The volume of distribution is 0.25-0.39 l / kg. The half-life period (T1 / 2) with IV and I / im administration is 1 hour. It is excreted by the kidneys - 60% - 70% unchanged, the rest is metabolites (deacetylated derivative has bactericidal activity, and 2 other metabolites are not possess).

In chronic renal failure (CRF) and in elderly people, T1 / 2 increases by 2 times. 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 the severe course caused by sensitive microorganisms: infections of the central nervous system (meningitis), respiratory tract and LOP-organs, urinary tract, bones, joints,skin and soft tissues, pelvic organs, chlamydia, gonorrhea, infected wounds and burns, peritonitis, sepsis, abdominal infections, endocarditis, Lyme disease (borreliosis), salmonellosis, infection against immunodeficiency, prevention of infections after surgery (including urological, obstetric-gynecological, on the gastrointestinal tract).

Contraindications:

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

Children under 2.5 years of age should 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 0.5 g of the drug in 2 ml (respectively 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 (0.5 g - 2 ml, 1 g - 4 ml).

For intravenous administration, 0.5-1 g of cefotaxime is 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, face swelling, laryngeal edema, bronchospasm, eosinophilia, malignant exudative erythema (Stevens-Johnson syndrome), toxic epidermal necrolysis (Lyell's syndrome), bullous eruptions, angioedema, anaphylactic shock.

From the digestive system: nausea, vomiting, diarrhea or constipation, flatulence, abdominal pain, impaired liver function (increased activity of "liver" transaminases, alkaline phosphatase, hepatitis, jaundice, fecal blood, hypercreatininaemia, hyperbilirubinemia), stomatitis, glossitis, pseudomembranous colitis.

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

From the urinary system: renal dysfunction (azotemia, increased urea in the blood, oliguria, anuria, interstitial nephritis), hyper-crepticemia.

From the nervous system: headache, dizziness, fainting, seizures, increased fatigue, encephalopathy (when prescribed in high doses), motor disorders, weakness.

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

Laboratory indicators: false positive test of Coombs.

Local reactions: inflammatory reaction at the injection site, including phlebitis and thrombophlebitis, tenderness along the vein, soreness and infiltration at the site of the / m introduction, redness of the skin.

Other: superinfection (in particular, candidal vaginitis), excessive growth of organisms that are not susceptible to cefotaxime.

In the treatment of borreliosis: Jarish-Gerxheimer's reaction (during the first days of treatment), skin rash, itching, fever, leukopenia, increased activity of "liver" transaminases, shortness of breath and discomfort in the joints.

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 antiaggregants, non-steroidal anti-inflammatory drugs.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. With caution appoint persons who manage transport and engaged in activities that require increased concentration of attention and rapid motor reaction.

Form release / dosage:

Powder for the preparation of solution for intravenous and intramuscular injection of 1 g.

Packaging:

Powder for the preparation of a solution for intravenous and intramuscular injection of 1 g in bottles.

For 1, 5 or 10 bottles in a cardboard box, along with instructions for medical use.

50 bottles are placed in a carton box with 3-5 instructions for use (for hospitals).

Packaging complete with a solvent - water for injection. The kit includes:

a) 1 bottle with the drug and 1 ampoule with water for injection for 5 ml;

b) 5 bottles of the drug and 5 ampoules of water for injection for 5 ml;

at) 10 vials of the drug and 10 ampoules of water for injection for 5 ml. The kit is placed in individual packs of cardboard, along with instructions for medical use, an ampoule or ampoule knife with a knife.When using ampoules with notches, rings or dots, the ampoule opener or scarifier is not inserted.

Storage conditions:In dry, protected from light and out of reach of children at a temperature of no higher than 25 ° C.

Shelf life:

2 years.

Do not use after the expiration date.

Terms of leave from pharmacies:On prescription

Registration number:LS-002118

Date of registration:27.12.2011

The owner of the registration certificate:BIOCHEMIST, OJSC BIOCHEMIST, OJSC Russia

Manufacturer: & nbsp

BIOCHEMIST, OJSC Russia

Information update date: & nbsp01.11.2015

Illustrated instructions

Instructions

Cefotaxime (Cefotaxime)