Tseftriakson

General characteristics. Structure:

Active agent: цефтриаксон sodium (in terms of цефтриаксон) - 0,5 g; 1 g; 2 g .

Pharmacological properties:

Tsefalosporinovy antibiotic of the III generation of a broad spectrum of activity. Works bakteritsidno, oppressing synthesis of a cell wall of microorganisms. It is steady in the relation β-лактамаз the majority of gram-positive and gram-negative bacteria.

It is active concerning gram-positive aerobic bacteria: Staphylococcus aureus (including the strains producing a penicillinase), Staphylococcus epidermidis, Streptococcus pneumoniae, Streptococcus pyogenes, Streptococcus viridans; gram-negative aerobic bacteria: Acinetobacter calcoaceticus, Enterobacter aerogenes, Enterobacter cloacae, Escherichia coli, Haemophilus influenzae (including the strains producing a penicillinase), Haemophilus parainfluenzae, Klebsiella spp. (including Klebsiella pneumoniae), Moraxella catarrhalis (including the strains producing a penicillinase), Morganella morganii, Neisseria gonorrhoeae (including the strains producing a penicillinase), Neisseria meningitidis, Proteus mirabilis, Proteus vulgaris, Serratia spp. (including Serratia marcescens), Pseudomonas aeruginosa (separate strains); anaerobic bacteria: Bacteroides fragilis, Clostridium spp. (except Clostridium difficile), Peptostreptococcus spp.

Has activity of in vitro concerning the majority of strains of the following microorganisms though clinical value of it is unknown: Citrobacter diversus, Citrobacter freundii, Providencia spp. (including Providencia rettgeri), Salmonella spp. (including Salmonella typhi), Shigella spp., Streptococcus agalactiae, Bacteroides bivius, Bacteroides melaninogenicus.

Methicillinum-steady staphylococcus are steady also against cephalosporins, including against a tseftriakson. Many strains of streptococci of group D and enterococci (including Enterococcus faecalis) are also steady against a tseftriakson.

 

Pharmacokinetics. Absorption and distribution

After introduction in oil цефтриаксон it is quickly and completely soaked up in a system blood stream. Well gets into fabrics and fluid mediums of an organism: airways, bones, joints, urinary path, skin, hypodermic cellulose and abdominal organs. At an inflammation of meningeal covers well gets into cerebrospinal fluid. Bioavailability of a tseftriakson at introduction in oil makes 100%. After introduction in oil Cmax is reached in 2-3 h, at in introduction - at the end of infusion.

At introduction of a tseftriakson in oil in a dose of 500 mg and 1 g of Cmax in a blood plasma makes 38 mkg/ml and 76 mkg/ml respectively, at in introduction in a dose of 500 mg, 1 g and 2 g - 82 mkg/ml, 151 mkg/ml and 257 mkg/ml respectively. At adults in 2-24 h after administration of drug in a dose of 50 mg/kg concentration in cerebrospinal fluid many times over surpasses MPK for the most widespread causative agents of meningitis.

The equilibrium state is established within 4 days of administration of drug.

Reversible linkng with proteins of plasma (albumine) makes 83–95%.

Vd makes 5.78-13.5 l (0.12-0.14 l/kg), children have 0.3 l/kg.

Removal

T1/2 makes 6-9 h. Plasma clearance – 0.58-1.45 l/h, renal clearance – 0.32-0.73 l/h.

At adult patients the current of 48 h 50-60% of drug is removed by kidneys in not changed look, 40-50% are excreted with bile in intestines where it biotransformirutsya in an inactive metabolite.

Pharmacokinetics in special clinical cases

At newborn children kidneys remove about 70% of drug.

At newborns and at elderly people (75 years are aged more senior), and also at patients with renal failures and a liver of T1/2 considerably increases.

At the patients who are on a hemodialysis at KK of 0-5 ml/min., T1/2 makes 14.7 h; at KK of 5-15 ml/min. - 15.7 h; at KK of 16-30 ml/min. - 11.4 h; at KK of 31-60 ml/min. - 12.4 h.

At children with meningitis of T1/2 later in/in introductions in a dose of 50-75 mg/kg makes 4.3-4.6 h.

Indications to use:

The bacterial infections caused by sensitive microorganisms:

— infections of abdominal organs (peritonitis, inflammatory gastrointestinal diseases, biliary tract, including cholangitis, empyema of a gall bladder);

— diseases of upper and lower parts of respiratory tracts (including pneumonia, abscess of lungs, pleura empyema);

— infections of bones and joints;

— infections of skin and soft tissues;

— infections of urinary tract (including pyelonephritis);

— bacterial meningitis;

— endocarditis;

— sepsis;

— gonorrhea;

— syphilis;

— venereal ulcer;

— disease Laima (borreliosis);

— typhoid;

— salmonellosis and salmonellonositelstvo;

— contaminated wounds and burns.

Prevention of a postoperative infection.

Infectious diseases at persons with the weakened immunity.

Route of administration and doses:

Intravenously and intramusculary. To adults and children 12 years - on 1-2 g of 1 times a day or 0.5-1 g each 12 h are more senior, the daily dose should not exceed 4 g. For newborns (to 2 weeks) - 20-50 mg/kg/days. For babies and children up to 12 years a daily dose - 20-80 mg/kg. Children with body weight have 50 kg and apply doses to adults above. It is necessary to appoint a dose more than 50 mg/kg of body weight in a look in/in infusion within 30 min. Duration of a course depends on character and disease severity. At gonorrhea - in oil once, 250 mg. For prevention of postoperative complications - once, 1-2 g (depending on degree of danger of infection) in 30-90 min. prior to operation. At operations on thick and a rectum recommend additional administration of drug from group 5 of nitroimidazoles. At bacterial meningitis at babies and children of younger age - 100 mg/kg (but no more than 4 g) 1 time a day. Duration of treatment depends on the activator and can make of 4 days for Neisseria meningitidis up to 10-14 days for sensitive strains of Enterobacteriaceae. To children with infections of skin and soft tissues - in a daily dose of 50-75 mg/kg of 1 times a day or 25-37.5 mg/kg each 12 h, no more than 2 g/days. At heavy infections of other localization - 25-37.5 mg/kg each 12 h, no more than 2 g/days. At average otitis - in oil, once, 50 mg/kg, no more than 1 g. Dose adjustment is required to patients with HPN only at KK lower than 10 ml/min. In this case the daily dose should not exceed 2 g. Rules of preparation and administration of solutions: It is necessary to use only freshly cooked solutions! For introduction in oil 0.25 or 0.5 g of drug dissolve in 2 ml, and 1 g - in 3.5 ml of 1% of solution of lidocaine. Recommend to enter no more than 1 g into one buttock. For in/in an injection of 0.25 or 0.5 g dissolve in 5 ml, and 1 g - in 10 ml of water for injections. Enter in/in slowly (2-4 min.). For in/in infusions dissolve 2 g in 40 ml of the solution which is not containing Ca2 + (0.9% NaCl solution, 5-10% solution of a dextrose, 5% levuloza solution). Doses of 50 mg/kg and more should be entered in/in kapelno, within 30 min.

Features of use:

At use of drug it is necessary to consider risk of development of an acute anaphylaxis and need of carrying out the corresponding emergency treatment.

In the researches in vitro it is shown that цефтриаксон (like other cephalosporins) the bilirubin connected with blood serum albumine is capable to force out. Therefore at newborns with a hyperbilirubinemia and, especially, at premature newborns, use of a tseftriakson demands a bigger care.

At a combination of a renal failure of heavy degree and a heavy liver failure at the patients who are on a hemodialysis it is regularly necessary to define concentration of drug in plasma.

At prolonged treatment it is regularly necessary to control a pattern of peripheral blood, indicators of a functional condition of a liver and kidneys.

In rare instances at ultrasonography of a gall bladder blackouts which disappear after the treatment termination are noted. Even if this phenomenon is followed by pains in right hypochondrium, continuation of therapy by Tseftriakson and carrying out a symptomatic treatment is recommended.

Purpose of vitamin K can be required by the elderly and weakened patients.

During treatment alcohol intake since disulfiramopodobny effects are possible is contraindicated (a hyperemia of the person, a spasm in a stomach and in a stomach, nausea, vomiting, a headache, decrease in the ABP, tachycardia, short wind).

Side effects:

From TsNS: headache, dizziness.

From an urinary system: oliguria, renal failure, glucosuria, hamaturia, giperkreatininemiya, increase in content of urea.

From the alimentary system: nausea, vomiting, taste disturbance, meteorism, stomatitis, glossitis, diarrhea, pseudomembranous coloenteritis, pseudo-cholelithiasis (sladzh-syndrome), dysbacteriosis, abdominal pain, increase in activity of hepatic transaminases and ShchF, hyperbilirubinemia.

From system of a hemopoiesis: anemia, leukopenia, leukocytosis, lymphopenia, neutropenia, granulocytopenia, thrombocytopenia, thrombocytosis, basophilia, hemolitic anemia.

From coagulant system of blood: nasal bleedings, increase (reduction) in a prothrombin time.

Allergic reactions: urticaria, rash, itch, exudative mnogoformny erythema, fever, fever, hypostases, eosinophilia, acute anaphylaxis, serum disease, bronchospasm.

Others: superinfection (including candidiasis).

Local reactions: at in introduction - phlebitis, morbidity on the vein course; at introduction in oil - morbidity in an injection site.

Interaction with other medicines:

Tseftriakson and aminoglycosides possess a synergism concerning many gram-negative bacteria.

At combined use with NPVS and other antiagregant the probability of developing of bleedings increases.

At simultaneous use with "loopback" diuretics and other nefrotoksichny drugs the risk of nephrotoxic action increases.

Drug is incompatible with ethanol.

Pharmaceutical interaction

Pharmaceutical it is incompatible with the solutions containing other antibiotics.

Contraindications:

— hypersensitivity to drug components;

— hypersensitivity to other cephalosporins, penicillin, karbapenema.

With care appoint drug to newborn children with a hyperbilirubinemia, to premature children, at a renal and/or liver failure, NYaK, enteritis or colitis connected using antibacterial drugs at pregnancy, in the period of a lactation.

 

Use of drug TsEFTRIAKSON at pregnancy and feeding by a breast

Use of drug at pregnancy is possible only in that case when the estimated advantage for mother surpasses potential risk for a fruit. In need of use of drug in the period of a lactation it is necessary to stop breastfeeding.

 

Use at abnormal liver functions

At the expressed abnormal liver functions it is necessary to watch concentration of a tseftriakson in a blood plasma since at them the speed of its allocation can decrease.

 

Use at renal failures

At heavy degree of a renal failure (KK less than 10 ml/min.) the daily dose of a tseftriakson should not exceed 2 g.

At the expressed renal failures, and also at the patients who are on a hemodialysis it is necessary to watch concentration of a tseftriakson in a blood plasma since at them the speed of its allocation can decrease.

 

Use for elderly patients

Use according to indications is possible. It is necessary to estimate function of kidneys.

 

Use for children

With care appoint drug to newborn children with a hyperbilirubinemia, to premature children. Drug is used at children of more advanced age according to indications and in the recommended doses.

Overdose:

For removal of drug from an organism the hemodialysis is inefficient. In the presence of clinical manifestations of overdose performing symptomatic therapy is recommended.

Storage conditions:

List B. Drug should be stored in the unavailable to children, dry, protected from light place at a temperature not above 25 °C. A period of validity - 2 years.

Issue conditions:

According to the recipe

Packaging:

Powder for preparation of solution for injections on 0,5, 1,0 or 2,0 g in bottles.