Biotrakson

General characteristics. Structure:

Active agent: a tseftriaksona of sodium трисесквигидрат (in terms of цефтриаксон) - 1000 mg.

Pharmacological properties:

Pharmacodynamics. The Tsefalosporinovy antibiotic of the III generation of a broad spectrum of activity for parenteral administration. Bactericidal activity is caused by suppression of synthesis of a cell wall of bacteria. Differs in resistance to action of the majority beta лактамаз gram-negative and gram-positive microorganisms.

It is active in the relation of the following microorganisms: gram-positive aerobes - Staphylococcus aureus (including the strains producing a penicillinase), Staphylococcus epidermidis, Streptococcus pneumoniae, Streptococcus pyogenes, Streptococcus spp. viridans groups;

gram-negative aerobes: Acinetobacter calcoaceticus, Borrelia burgdorferi, Enterobacter aerogenes, Enterobacter cloacae, Escherichia coli, Haemophilus influenzae (including the strains forming a penicillinase), Haemophilus parainfluenzae, Klebsiella spp. (including Klebsiella pneumoniae), Moraxella catarrhalis, (including penitsillinprodutsiruyushchy strains), Morganella morganii, Neisseria gonorrhoeae (including the strains forming a penicillinase), Neisseria meningitidis, Proteus mirabilis, Proteus vulgaris, Serratia spp. (including Serratia marcescens); separate strains of Pseudomonas aeruginosa are also sensitive; anaerobe bacterias: 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. (т.ч. Providencia rettgeri), Salmonella spp., including Salmonella typhi, Shigella spp.; Streptococcus agalactiae, Bacteroides bivius, Bacteroides melaninogenicus.

Metitsillinoustoychivye staphylococcus also many strains of streptococci of group D and enterococci, including Enterococcus faecalis are steady against cephalosporins, including against a tseftriakson, are also steady against a tseftriakson.

Pharmacokinetics. Bioavailability - 100%, TCmax after introduction in oil - 2-3 h, later in/in introductions - at the end of infusion. Cmax after introduction in oil in doses of 0.5 and 1 g - 38 and 76 mkg/ml respectively. Cmax at in/in in doses of 0.5, 1 and 2 g - 82, 151 and 257 mkg/ml respectively. At adults in 2-24 h after introduction in a dose of 50 mg/kg concentration in SMZh many times over surpasses MPK for the most widespread causative agents of meningitis. Well gets into SMZh at an inflammation of a meninx. Communication with proteins of plasma - 83-96%. Distribution volume - 0.12-0.14 l/kg (5.78-13.5 l), at children is 0.3 l/kg, plasma clearance - 0.58-1.45 l/h, renal - 0.32-0.73 l/h.

T1/2 after introduction in oil children have 5.8-8.7 h, later in/in introductions in a dose of 50-75 mg/kg with meningitis - 4.3-4.6 h; at patients, being on a hemodialysis (KK of 0-5 ml/min.), - 14.7 h, at KK of 5-15 ml/min. - 15.7 h, 16-30 ml/min. - 11.4 h, 31-60 ml/min. - 12.4 h.

It is removed in not changed look - 33-67% by kidneys; 40-50% - with bile in intestines where there is an inactivation. At newborn children through kidneys about 70% of drug are removed. The hemodialysis is inefficient.

Indications to use:

The infections caused by activators, sensitive to a tseftriakson:

- sepsis;

- meningitis;

- infections of abdominal organs (peritonitis, inflammatory diseases of digestive tract, biliary tract);

- infections of bones, joints, connecting fabric, skin;

- infections at patients with the lowered immunity;

- respiratory infections (including pneumonia);

- infections of kidneys and urinary tract;

- infections of ENT organs;

- urogenital infections (including gonorrhea).

Prevention of infections in the postoperative period.

Route of administration and doses:

Drug is used intramusculary and intravenously.

For adults and children 12 years are more senior. The average daily dose makes 1-2 g of a tseftriakson of 1 times a day or to 0,5-1 g there are each 12 hours. In hard cases or in cases of the infections caused by moderately sensitive pathogens, the daily dose can be increased to 4 g.

For newborns. At a one-time daily dosage the following scheme is recommended: for newborns (to two-year age) - 20-50 mg/kg of body weight a day (the dose of 50 mg/kg of body weight is not recommended to be exceeded in connection with unripe fermental system of newborns).

For babies and children up to 12 years. The daily dose makes 20-75 mg/kg of body weight. Children with body weight have 50 kg and it is necessary to adhere to a dosage for adults above. It is necessary to appoint a dose more than 50 mg/kg of body weight in the form of intravenous infusion, at least, within 30 minutes. Duration of therapy depends on the course of a disease.

Meningitis. At bacterial meningitis at newborns and at children the initial dose makes 100 mg/kg of body weight once a day (at most 4 g). As soon as the pathogenic microorganism was succeeded to allocate and to define his sensitivity a dose it is necessary to reduce respectively.

Gonorrhea. For treatment of the gonorrhea caused by the strains both forming, and not forming a penicillinase, the recommended dose makes 250 mg once intramusculary.

Insufficiency of function of kidneys and liver. At patients with an impaired renal function, on condition of normal function of a liver to reduce a dose of a tseftriakson there is no neobkhoimost. Only at insufficiency of kidneys in a preterminal stage it is necessary that the daily dose of a tseftriakson did not exceed 2 g. At patients with the broken function of a liver, on condition of preservation of function of kidneys to reduce a dose of a tseftriakson also there is no need.

Intramuscular introduction. For intramuscular maintaining 1 g препарарат it is necessary to dissolve in 3,5 ml 1% of solution of lidocaine for injections and to enter deeply into a gluteus, it is recommended to enter no more than 1 g of drug into one buttock.

Intravenous administration. 1 g of drug needs to be parted in 10 ml of sterile water for injections and to enter intravenously slowly within 2-4 minutes.

Intravenous infusion. Duration of intravenous infusion, at least, 30 minutes. 2 g of powder need to be parted approximately in 40 ml of solution free from calcium.

Features of use:

At a simultaneous heavy renal and liver failure, it is regularly necessary to define concentration of drug in plasma.

At the patients who are on a hemodialysis it is necessary to watch concentration of a tseftriakson in plasma since at them the speed of its removal can decrease.

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

During treatment the ethanol use is contraindicated.

Despite detailed collecting the anamnesis, it is impossible to exclude a possibility of development of an acute anaphylaxis which demands immediate therapy - at first intravenously enter Epinephrinum, then glucocorticoids.

Researches showed that цефтриаксон the bilirubin connected with blood serum albumine is capable to force out. Therefore at newborn and premature use of a tseftriakson demands a bigger care.

At appointment in the period of a lactation it is necessary to cancel breastfeeding.

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

Side effects:

Allergic reactions: rash, itch, heat or fever.

From a nervous system: headache, dizziness.

From the alimentary system: diarrhea, nausea, vomiting, taste disturbance, pseudomembranous colitis.

From bodies of a hemopoiesis: anemia (including hemolitic), leukopenia, lymphopenia, neutropenia, thrombocytopenia, thrombocytosis, eosinophilia.

From urinogenital system: vagina candidiasis, vaginitis.

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

Laboratory indicators: increase (reduction) in a prothrombin time, increase in activity of "hepatic" transaminases and ShchF, hyperbilirubinemia, giperkreatininemiya, increase in concentration of urea, existence of a deposit in urine.

Others: the increased sweating, blood "inflows".

Undesirable reactions with a frequency less than 0.1%: abdominal pain, agranulocytosis, allergic pneumonitis, anaphylaxis, basophilia, cholelithiasis, bronchospasm, colitis, dyspepsia, nasal bleeding, abdominal distention, "sladzh-phenomenon" of a gall bladder, glucosuria, hamaturia, jaundice, leukocytosis, lymphocytosis, monocytosis, nephrolithiasis, heartbeat, spasms, serum disease.

Post-marketing experience: stomatitis, glossitis, oliguria, rash, allergic dermatitis, small tortoiseshell, hypostasis, multiformny erythema, Stephens-Johnson's syndrome, Lyell's disease.

Interaction with other medicines:

It is incompatible with ethanol.

Non-steroidal anti-inflammatory drugs and other inhibitors of aggregation of thrombocytes increase probability of bleeding.

Pharmaceutical it is incompatible with the solutions containing other antibiotics.

Contraindications:

Hypersensitivity to cephalosporins, penicillin and karbalenema. First trimester of pregnancy.

Overdose:

High concentration of a tseftriakson in plasma cannot be excessive are lowered by means of a hemodialysis or peritoneal dialysis. For treatment of cases of overdose symptomatic measures are recommended.

Storage conditions:

To store in the place protected from light, at a temperature not above 25 °C. To store in the place, unavailable to children.

Issue conditions:

According to the recipe

Packaging:

Powder for preparation of solution for intravenous and intramuscular administration in bottles on 1000 mg. Each bottle together with the instruction on a medical use is placed in a cardboard pack.