Tseftriaksona natrivy salt

General characteristics. Structure:

Active ingredient: 0,5 g or 1 g of a tseftriakson in the form of sodium salt (in terms of цефтриаксон).

The antimicrobic means possessing antibacterial (bactericidal action).

Pharmacological properties:

Pharmacodynamics. Possesses antibacterial (bactericidal action). Inhibits synthesis of a cell wall of bacteria. Acetylates membrane-bound transpeptidases, breaking thus the cross stitching of peptidoglikany chains necessary for ensuring durability and rigidity of a cell wall of bacteria.

Tseftriakson is steady against action beta лактамаз, the gram-positive and gram-negative bacteria produced by the majority. Possesses a broad spectrum of activity. It is active concerning gram-positive aerobes - Staphylococcus aureus, Staphylococcus epidermidis, Streptococcus pneumoniae, Streptococcus pyogenes, Streptococcus agalactiae, Streptococcus viridans, Streptococcus bovis; gram-negative aerobes - Aeromonas spp., Alcaligenes spp., Branchamella catarhales (including and the strains forming beta lactamelements), Citobacter spp., Enterobacter spp., (some strains resistant), Escherichia coli, Haemophilus ducreyi, Haemophilus influenzae (including the strains forming a penicillinase), Haemophilus parainfluenzae, Klebsiella spp., (including Klebsiella pneumonia), Moraxella spp., Morganella morgani, Neisseria gonorrhoeae (including the strains forming a penicillinase), Neiseria meningitis, Plesiomonas shigelloides, Proteus mirabilis, Proteus vulgaris, Providensia spp., Proteus aeruginisa, Salmonella spp., (including Salmonella typhi), Serratia spp., (including Serratia marcescens), Shigella spp. Vibrio spp., (including Vibrio cholerae), Yersinia spp., (including Yersinia enterocolitica); anaerobe bacterias - Bacteroides spp. (including some strains of Bacteroides fragilis), Clostridium spp., (except Clostridium difficile), Fusobacterium spp., (except Fusobacterium mortiferum, Fusobacterium verium), Peptococcus spp., Peptostreptococcus spp.

Staphylococcus spp strains are steady against a tseftriakson., steady against Methicillinum; Enterococcus spp strains. (Enterococcus faecalis), Clostridium difficile, Bacteiodes spp., the producing beta lactamelements.

It is not hydrolyzed by R-plasmid beta lactamelements, and also the majority of chromosomal penicillinases and цефалоспориназ, can affect multiresistant strains, tolerant to penicillin, cephalosporins of the first generations and aminoglycosides. The acquired stability of some strains of bacteria is caused by a producing beta lactamelements, ("tseftriaksonaza") inactivating цефтриаксон.

Pharmacokinetics. It is not soaked up from a GIT at intake. After intramuscular introduction it is quickly and fully soaked up, the peak of concentration in a blood plasma is noted in 1,5 hours. The minimum antimicrobic concentration are found within 24 hours and more. Drug well gets into bodies, organism liquids (peritoneal, pleural, spinal, synovial), into bone and cartilaginous tissues. Passes through a placenta and in insignificant quantities gets into breast milk (3-4%). Stable concentration of drug is reached within 4 days. Smakh after introduction in oil is reached in 2-3 hours, later in/in introductions – at the end of infusion. Smakh after introduction of a tseftriakson in oil in a dose of 0,5 g – 38 mkg/ml, 1 g – 76 mkg/ml; at in introduction of 0,5 g – 82 mkg/ml, 1 g-151 mkg/ml, 2 g - 257 mkg/ml. At adults after introduction of 50 mkg/kg concentration in medullispinal liquid many times over surpasses MPK for the most widespread causative agents of meningitis. Reversibly contacts albumine (59-83%). T1/2 makes 6-9 hours that allows to use drug of 1 times a day. T1/2 at children with meningitis – 4,3-4,6 hours; at the patients who are on a hemodialysis (creatinine 0-5ml/min Cl) of-14,7 hours; at Cl of creatinine of 5-15 ml/min. – 15,7 hours; at Cl of creatinine of 16-30 ml/min. – 11,4 hours; at Cl of creatinine of 31-60 ml/min. – 12,4 hours.

The volume of distribution is 0,12-0,14 l/kg (5,78-13,5 l), children have 0,3 l/kg, plasma Cl of 0,58-1,45 l/h, renal 0,32-0,73 l/h.

At newborn, elderly people and patients with an abnormal liver function and kidneys of T1/2 it is considerably extended, cumulation is possible. It is removed by kidneys (50-60% of drug in not changed look, (40-50%) are excreted together with bile in intestines) where further it biotransformirutsya in an inactive metabolite. At newborns through kidneys more than 60% of drug are removed.

Indications to use:

Infections of upper and lower parts of respiratory tracts (including pneumonia, abscess of lungs, pleura empyema); infections of skin, soft tissues, bones and joints; infections of abdominal organs (peritonitis, inflammatory gastrointestinal diseases, biliary tract, cholangitis, empyema of a gall bladder); infectious and inflammatory diseases of bodies of a small pelvis and urinary tract (including pyelitis, pyelonephritis, cystitis, prostatitis, epididymite); bacterial meningitis and endocarditis, sepsis, Lyme's disease, shigellosis, salmonellosis, salmonellonositelstvo, typhus fever; the acute and complicated gonorrhea, and other infections, sexually transmitted (including a venereal ulcer and syphilis); prevention and treatment of infections at surgical interventions.

Route of administration and doses:

In oil (it is deep in a muscle), in/in way of an injection lasting 2-4 minutes. For adults and children 12 years a daily dose are more senior makes 1-2 g. The maximum daily dose for adults – 4 g. The newborn aged up to 14 days on 20-50 mg/kg of 1 times a day. The maximum daily dose - no more than 50 mg/kg. To children aged from 15 days and up to 12 years – 20-80 mg/kg of 1 times a day. At children weighing 50 kg and more drug is used in recommended for adult doses. It is necessary to appoint doses more than 50 mg/kg of body weight in the form of intravenous infusion within 30 min. Treatment should be continued within 2-3 days after disappearance of clinical signs of an infection. Therapy duration – from 4 to 14 days; at the complicated infections more long treatment can be required.

For prevention of postoperative complications – once, 1-2 g (depending on degree of danger of infection) in 30-90 minutes prior to operation.

At bacterial meningitis – in a dose of 100 mg/kg of 1 times a day, (but no more than 4 g a day). Duration of treatment depends on the activator and can make of 4 days for Neiseria meningitis up to 10-14 days for sensitive strains of Enterobacteriactae.

Infections of skin and soft tissues: to children – 50-75 mg/kg/days or to 25-37,5 mg/kg/days are once a day each 12 hours (no more than 2 g/days). At heavy infections of other localization of 25-37,5 mg/kg/days each 12 hours (no more than 2 g/days). At average otitis – 50 mg/kg in oil once a day, no more than 1 g a day.

At gonorrhea – in oil, once 250 mg.

To patients with a renal failure (creatinine Cl <10ml/mines) the daily dose should not exceed 2 g.

Features of use:

For in/in introductions drug is dissolved in sterile water for injections in the ratio 1:10 (0,5 g of drug dissolve in 5 ml; 1 g of drug in 10 ml of sterile water).

For intravenous infusion drug is dissolved in solution, free from calcium ions. Duration in/in infusion no more than 15-30 minutes.

For introduction in oil – in 1% lidocaine solution (0,5 g of drug in 2 ml or 1 g – in 3,5 ml). The received solution cannot be entered intravenously! At intramuscular introduction, it is recommended to enter no more than 1 g of drug into one gluteus.

Freshly cooked solutions of drug are stable within 6 hours at the room temperature and within 24 hours at 2-8 degrees of Page.

Precautionary measures. At a simultaneous renal and liver failure, at the patients who are on a hemodialysis it is regularly necessary to define concentration of drug in plasma. At prolonged treatment to control hematologic indicators of blood, indicators of a functional condition of a liver and kidneys. Elderly and weakened purpose of vitamin K can be required.

Restrictions to use. A renal liver failure, bleedings and gastrointestinal diseases (the nonspecific ulcer colitis, enteritis or colitis connected using antibacterial drugs), premature children.

Use during pregnancy and a lactation. Contraindicated in the I trimester of pregnancy. For the period of treatment it is necessary to stop breastfeeding.

Side effects:

Allergic reactions: urticaria, rash, itch, erythema, fever, hypostases, eosinophilia, acute anaphylaxis, serum disease, abdominal pain, bronchospasm

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

From a nervous system: dizziness and headache

From an urinary system: oliguria

From the alimentary system: nausea, vomiting, taste disturbances, meteorism, stomatitis, glossitis, diarrhea, dysbacteriosis

From bodies of a hemopoiesis: anemia, leukopenia, granulocytopenia, thrombocytosis, basophilia, lengthening of a prothrombin time

From system of a hemostasis: hamaturia, nasal bleedings, hemolitic anemia

Other: candidiasis and other superinfections

Laboratory indicators: increase in activity of hepatic transaminases, alkaline phosphatase, hyperbilirubinemia, hypercreatinemia, increase in content of urea, glucosuria.

Interaction with other medicines:

Together with aminoglycosides possesses a synergism concerning many gram-negative bacteria.

It is incompatible with alcohol (perhaps face reddening, a spasm in a stomach and area of a stomach, nausea, vomiting, a headache, decrease in the ABP, tachycardia, an otdyshka).

NPVS and other inhibitors of aggregation of thrombocytes increase probability of bleeding.

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

Pharmaceutical it is incompatible with solutions of other antibiotics.

Contraindications:

Hypersensitivity to a tseftriakson or to other drugs of group of cephalosporins, penicillin, Carbapenums; pregnancy (I trimester), hypoalbuminemia, acidosis or reduced binding of bilirubin; jaundice of newborns.

Overdose:

Symptoms. At long introduction emergence of allergic reactions, dispeptic frustration is possible.

Treatment. There is no specific antidote, a symptomatic treatment.

Issue conditions:

According to the recipe

Packaging:

Powder for preparation of solution for injections of 0,5 g and 1,0 g in bottles in packaging No. 1, No. 40.