Torotsef

General characteristics. Structure:

Active ingredient: 250 mg or 1000 mg of powder of a tseftriakson anhydrous.

Tsefalosporinovy antibiotic of a broad spectrum of activity.

Pharmacological properties:

Pharmacodynamics. Torotsef (a tseftriaksona sodium salt) - a semi-synthetic tsefalosporinovy antibiotic of the III generation of a broad spectrum of activity.

Bactericidal activity of Torotsef is caused by suppression of synthesis of cellular membranes. Drug differs in big resistance to action beta лактамаз (penicillinases and tsefalosporinaza) gram-positive and gram-negative microorganisms. Torotsef is active concerning the following microorganisms:

Gram-negative aerobes: Enterobacter aerogenes, Enterobacter cloacae, E. coli, H. influenzae (including strains steady against ampicillin), N. of parainfluenzae, Klebssiela spp. (including K. pneumoniae), N. gonorrhoeae (including the strains which are forming and not forming a penicillinase), N. meningitidis, P. mirabilis, P. vulgaris, Morganella morganii, Serratia marcescens, Citrobacter freundii, Citrobacter diversus, Providencia spp., Salmonella spp., Shigella spp., Acinetobacter calcoaceticus.

A number of strains of above-mentioned microorganisms which show resistance to other antibiotics, such as penicillin, cephalosporins, aminoglycosides are sensitive to Torotsef. Separate strains of Pseudomonas aerugenosa are also sensitive to drug.

Gram-positive aerobes: Staph. aureus (including the strains forming a penicillinase), Staph. epidermidis (staphylococcus, steady against Methicillinum, show all cephalosporins resistance, including Torotsef), Strep. pyogenes (beta and hemolitic streptococci of group A), Strep. agalactiae (group B streptococci), Strep. pneumoniae.

Anaerobe bacterias: Bacteroides spp., Clostridium spp. (except for Cl.difficile).

Pharmacokinetics. Torotsef is completely soaked up at intramuscular introduction. Average concentration in plasma is reached in 2-3 hours after an injection. At repeated in oil or in introduction in doses of 0,5-2,0 g to an interval from 12 to 24 hours there is Torotsef's accumulation in concentration which for 15%-36% exceeds the concentration reached at single introduction.

At Torotsef's introduction to healthy adult patients in a dose from 0,15 to 3,0 g the elimination half-life makes from 5,8 to 8,7 hours; distribution volume - from 5,78 to 13,5 l; the clearing coefficient of plasma makes from 0,58 to 1,45 l/hour, and coefficient of renal clarification - from 0,32 to 0,73 l/hour Torotsef reversibly contact proteins of a blood plasma. From 33% to 67% of drug it is removed in an invariable view with urine, other part - and decides on bile in excrements in the form of microbiological inactive components.

Indications to use:

• Lower respiratory tract infections, the caused Strep. pneumoniae, Streptococcus spp. (including Enterococci), Staph. aureus, H. influenzae, H. parainfluenzae, Klebssiela spp. (including K. pneumoniae), E. coli, E. aerogenes, P. mirabilis and S. marcescens.
• The infections of skin and soft tissues caused by Staph. aureus, Staph. epidermidis, Streptococcus spp. (including Enterococci), E. cloacae, Klebssiela spp. (including K. pneumoniae), P. mirabilis and P. aeruginosa.
• The infections of urinary tract caused by E. coli, P. mirabilis, P. vulgaris, M. Morganii and Klebssiela spp. (including K. pneumoniae).
• The uncomplicated gonorrhea (cervical/urethral and rectal) caused by N. gonorrhoeae (including the strains which are forming and not forming a penicillinase).
• The infections of bodies of a small pelvis caused by N. gonorrhoeae.
• The sepsis caused by Staph. aureus, Strep. pneumoniae, E. coli, H. influenzae and K. pneumoniae.
• The infections of bones and joints caused by Staph. aureus, Strep. pneumoniae, Streptococcus spp. (including Enterococci), E. coli, P. mirabilis, K. pneumoniae and Enterobacter spp.
• The infections of an abdominal cavity caused by E. coli and K. pneumoniae.
• The meningitis caused by H. influenzae, N. meningitidis, Strep. pneumoniae, Staph. epidermidis and E. coli.
• Prevention of postoperative infectious complications.

Route of administration and doses:

Usually appoint adult 1-2 g of Torotsef 1 or 2 times a day. Totally daily dose should not exceed 4 g. To babies and children aged up to 12 years: 20-80 mg/kg/days. To premature/newborn children: no more than 50 mg/kg/days.

At gonorrhea it is recommended to enter once 250 mg in oil. It is necessary to continue Torotsef's introduction according to the same scheme within 72 hours after normalization of body temperature or emergence of signs of elimination of the center of an infection.

For reduction of pain at injections in oil the drug should be administered with 1% lidocaine solution (vnutriyagodichno).

For treatment of serious infections at children, except for meningitis, the recommended daily dose makes 50-75 mg/kg of body weight (no more than 2 g), divided into 2 introductions.

For prevention of infections during surgeries it is recommended to enter 1 g once in 0.5-2 hours prior to operation.

At the infections caused by Strep. pyogenes, duration of treatment makes 10 days.

The abnormal liver function or kidneys does not demand correction of a dose, however at the patients having at the same time heavy renal and liver failure and also at the patients who are on a hemodialysis it is regularly necessary to check concentration of drug in a blood plasma.

In oil: Contents of a bottle are dissolved as follows:

Bottle contents	Solvent
250 mg	0,9 ml
1 g	3,6 ml

After preparation each ml of solution contains about 250 mg in terms of цефтриаксон. If necessary it is possible to use more weak solution. As well as at other injections in oil Torotsef enter into rather large muscle; trial aspiration helps to avoid inadvertent introduction to a blood vessel.

In/in: Torotsef appoint in/in way of infusional injection within 30 minutes. The recommended concentration makes from 10 mg/ml to 40 mg/ml, but at desire concentration can be reduced. Contents of a bottle are dissolved as follows:

Bottle contents	Solvent
250 mg	2,4 ml
1 g	9,6 ml

After preparation each ml of solution contains about 100 mg in terms of цефтриаксон.

Features of use:

With extra care drug is appointed to persons with hypersensitivity to a beta laktamnym to antibiotics. Also with care drug is appointed to patients with allergic reactions, especially to medicines.

Precautionary measures. At a renal failure dose adjustment is not obligatory, but it is regularly necessary to define concentration of drug in a blood plasma and if necessary to reduce a dose.

At a liver failure dose adjustment is also not obligatory, but for patients with a simultaneous heavy renal and liver failure in the absence of regular control of concentration in plasma the daily dose of Torotsef should not exceed 2 g.

In rare instances at patients change of a prothrombin ratio is observed, at the same time at the same time appoint Vitamin K (10 mg a week).

At prolonged use which can lead to the overgrowth of microorganisms, not sensitive to drug, development of superinfection is possible.

With care appoint to patients with gastrointestinal diseases, especially colitis, to newborn and premature children with a giperbilmrubinemiya.

Use at pregnancy and a lactation. As clinical tests of drug at pregnant women were not carried out, Torotsef appoint during pregnancy and a lactation only in urgent cases. Tseftriakson is allocated with milk in low concentration. To nursing mothers appoint with extra care.

Side effects:

Usually Torotsef is well had. In the course of clinical tests the following reactions which could be connected were observed or are not connected using drug.

Local reactions: morbidity, consolidation, burning in the place of an injection (1%). In rare instances at in introduction phlebitis is possible.

Allergic reactions: rash (1.7%), itch, fever/fever (1%), Stephen-Johnson's syndrome, erythema.

From system of a hemopoiesis: eosinophilia (6%), thrombocytosis (5.1%), leukopenia (2.1%), hemolitic anemia, neutropenia, lymphopenia, thrombocytopenia (<1%).

From a GIT: diarrhea (2.7%), nausea, vomiting, dysgeusia (<1%), pseudomembranous colitis.

From a liver: increase in level of nuclear heating plant (3.1%), ALT (3.3%), alkaline phosphatases / bilirubin (<1%).

From kidneys: increase in an urea nitrogen (1.2%), creatinine (<1%), existence of cylinders in urine (<1%).

From TsNS: head pain / dizziness (<1%).

From urinogenital system: moniliasis/vaginitis (<1%).

Treatment by antibiotics of a broad spectrum of activity breaks normal flora of a large intestine and can sposobstvovoat to Clostridia growth.

Interaction with other medicines:

Torotsef it is impossible to mix with other antimicrobic means.

Tseftriakson, suppressing an indestinal flora, interferes with vitamin K synthesis. Therefore at co-administration with the drugs reducing aggregation of thrombocytes (non-steroidal anti-inflammatory drugs, salicylates, Sulfinpyrazonum) the risk of development of bleedings increases. For the same reason at co-administration with anticoagulants strengthening of action of the last is noted.

At co-administration with "loopback" diuretics the risk of development of nephrotoxic action increases.

Contraindications:

Hypersensitivity to cephalosporins. First trimester of pregnancy. In need of use in the period of a lactation breastfeeding is stopped. Nespetsefichesky ulcer colitis.

Storage conditions:

Torotsef it is necessary to store at a temperature not above 30 °C. The prepared solution in oil remains stable within 24 hours at a temperature of 25 °C and within 3 days at storage in the refrigerator (4 °C). Prepared in/in solution remains stable within 3 days at a temperature of 25 °C and within 10 days at storage in the refrigerator (4 °C). The frozen solution before use is defrozen at the room temperature and after the use thrown out. Not to freeze repeatedly. To store in the places unavailable to children.

Issue conditions:

According to the recipe

Packaging:

Powder in glass bottles which contain 250 mg and 1 g of a tseftriakson, respectively.