Tseftriakson-BHFZ

General characteristics. Structure:

International and chemical names: Ceftriaxone; dinatrium (6R,7R)-7-[[(Z) - (2-aminothiazol-4-silt) (metoksiimino) acetyl] - amine]-3-[[(2-метил-6-оксидо-5-оксо-2,5-дигидро-1,2,4-триазин-3-ил) sulphonyl] marked] - 8-oxo-5-thia-1-azabitsiklo [4.2.0] Oct - 2 - ен - 2 - carboxylat; main physical and chemical properties: crystal powder of almost white or yellowish color, is slightly hygroscopic; structure: 1 bottle contains a tseftriakson of sodium salt sterile in terms of цефтриаксон 500 mg or 1000 mg.

Pharmacological properties:

Pharmacodynamics. Tseftriakson – a semi-synthetic antibiotic of group of beta lactams, generation cephalosporin III, possesses bactericidal action which mechanism is connected with oppression of activity of enzyme of transpeptidase, disturbance of biosynthesis of a peptidoglikan of a cell wall of microorganisms; possesses a broad spectrum of activity.
It is active concerning gram-positive aerobes: Staphylococcus aureus (including the strains producing a penicillinase), S.epidermidis, Streptococcus pneumoniae, beta and hemolitic streptococci of group A (S.pyogenes), group streptococci In (S.agalactiae), the Viridans groups, streptococci of neenterokokkovy group D; gram-negative aerobes: E.coli, Haemophilus influenzae, H.parainfluenzae, Klebsiella spp. (including K.pneumoniae), Morganella morganii, Neisseria gonorrhoeae (including and the strains producing a penicillinase), N. meningitidis, Proteus mirabilis., P.vulgaris, Providencia spp., Pseudomonas aeruginosa, Salmonella spp. (including S.typhi), Serratia spp. (including S.marcescens), Shigella spp., Yersinia spp. (including Y.enterocolitica), Treponema pallidum; anaerobe bacterias: Bacteroides spp. (including some strains of B.fragilis), Clostridium spp. (however the majority of strains of C.difficile have resistance), Peptococcus spp. Peptostreptococcus spp., Fusobacterium spp. (except for F.mortiferum and F.varium). Drug is active in the relation to the microorganisms resistant to penicillin, cephalosporins of the first generations, aminoglycosides.
Are steady against action of a praparat: staphylococcus, resistant to Methicillinum; majority of strains of enterococci (including St.faecalis) and group D streptococci; it is a lot of strains of the beta lactamazoproducing Bacteroides spp. (B.fragilis).

Pharmacokinetics. After intramuscular introduction Tseftriakson's bioavailability makes 100%, its maximum concentration in a blood plasma is observed in 2 - 3 hours. After intravenous administration drug quickly gets into an intercellular lymph where for 24 hours bactericidal concentration in relation to sensitive microorganisms are maintained. Contacts proteins of plasma for 85% - 95%, at the same time extent of binding decreases with increase in concentration. Tseftriakson well gets into bodies and liquids of an organism (peritoneal, pleural, spinal, synovial), in bone tissues, gets through a placenta, in a small amount (3 – 4%) is allocated with breast milk. At meningitis at children, including newborns, drug gets into the inflamed meninx, at the same time concentration it in cerebrospinal liquid makes 17% of concentration in plasma.
Drug is emitted in an invariable view of 50 – 60% with kidneys and 40 – 50% – with bile. At a renal failure the drug pharmacokinetics almost does not change, noted only insignificant increase in an elimination half-life. The elimination half-life at healthy adults makes about 8 hours, at newborns aged up to 8 days and at people of old age 75 years are more senior increases by two-three times.

Indications to use:

The infectious and inflammatory diseases caused by microorganisms, sensitive to drug:
• infections of ENT organs;
• respiratory infections (pneumonia, bronchitis, abscess of lungs, pleura empyema);
• infections to urinogenital system (pyelitis, cystitis, acute and chronic pyelonephritis, prostatitis, uncomplicated gonorrhea and other infections, sexually transmitted (venereal ulcer and syphilis));
• wound fevers, infectious diseases of skin and soft tissues;
• meningitis;
• infections of bones and joints;
• peritonitis, inflammation of a gall bladder, gastrointestinal infections;
• infectious diseases: disease Laima (spirochetosis), typhus fever, salmonellosis, salmonellonositelstvo.
Drug is used for prevention of infections which can arise after surgeries.

Route of administration and doses:

Tseftriakson-BHFZ enter intramusculary or intravenously.
For intramuscular introduction for the purpose of elimination of morbidity in the place of an injection drug is dissolved in 1% lidocaine solution in such ratio: bottle contents from 500 mg dissolve in 2 ml 1% of solution of lidocaine, from 1000 mg – in 3 – 5 ml. Enter deeply into a gluteus. Use of sterile water for injections is possible. The solution containing lidocaine cannot be entered intravenously.
For intravenous jet administration drug is dissolved in sterile water for injections in such ratio: bottle contents from 500 mg are dissolved in 5 ml of solvent, from 1000 mg – in 10 ml. Enter slowly within 2-4 minutes.
For preparation of solution for intravenous infusion dissolve 2 g Tseftriaksona-BHFZ in 40 ml of one of solvents: 0,9% solution of sodium of chloride, 5% solution of glucose, 10% glucose solution, sterile water for injections. Infusion has to continue not less than 30 minutes.
To adults and children 12 years are more senior appoint 1000 – 2000 mg in a daily dose (enter 1 time a day or in a half dose 2 times a day). In hard cases the daily dose makes up to 4000 mg, and this dose is entered into 2 receptions at an interval of 12 hours. For prevention of postoperative complications enter once 1000 – 2000 mg (depending on degree of danger of infection), in 30 – 90 minutes prior to operation. Dose adjustment only at clearance is necessary for patients with a renal failure lower than 10 ml/min.
For people of old age of a dose correspond to doses for adult patients.
At uncomplicated gonorrhea once intravenously enter 250 mg of drug.
The daily dose Tseftriaksona-BHFZ for premature children and children up to 2 weeks makes 20 – 50 mg/kg of body weight, for children from 2 weeks to 12 years - 20 – 80 mg/kg, 1 time a day is entered.
At bacterial meningitis at babies and children up to 12 years treatment begin with a dose 100 mg/kg (but no more than 4000 mg) 1 time a day. After identification of the activator and definition of its sensitivity the dose can be reduced respectively.
Treatment duration Tseftriaksonom-BHFZ depends on character and severity of pathological process and is defined, besides, by data of bacteriological researches. Usually duration of treatment makes 4 – 14 days, but at serious infectious diseases longer therapy can be required. At the majority of infectious diseases treatment continues at least 48 - 72 more hours after disappearance of symptoms of a disease and confirmation of effect of results of the bacteriological analysis.

Features of use:

Use only in the conditions of a hospital. At development of an acute anaphylaxis it is necessary to enter adrenaline and glucocorticoids intravenously. It is necessary to be circumspect at co-administration of "loopback" diuretics. At prolonged treatment it is necessary to control a blood pattern regularly.
It is necessary to remember a possibility of development of cross allergic reactions with others beta лактамными antibiotics.
Intramuscular injections in an upper outside quadrant of a big gluteus have to be deep. Before administration of solution of drug it is necessary to be convinced that the needle is out of a vessel.
It is necessary to apply with care at bleedings and diseases of a digestive tract in the anamnesis, especially at ulcer nonspecific colitis or enteritis.
At a liver and renal failure with heavy disturbances of functions of these bodies the dose of drug is reduced. For patients with clearance of creatinine less than 10 ml/min. the daily dose of an antibiotic should not exceed 2000 mg.
Patients with a renal and liver failure when treatment is carried out with a hemodialysis, need to carry out dose adjustment Tseftriaksona-BHFZ and monitoring of its concentration in a blood plasma.
At arterial hypertension and disturbance of water and electrolytic balance it is necessary to control the content of sodium in plasma.
At prolonged use the cytologic research is necessary for definition of dysbacteriosis.
In case of drug use by the women nursing feeding should be stopped.
With care appoint the newborn with a hyperbilirubinemia, to the newborns and patients inclined to allergic reactions. It is reasonable to the elderly people weakened by the patient to appoint vitamin K.

Side effects:

From side of a GIT: nausea, vomiting, stomatitis, a glossitis, taste loss, an abdominal pain, diarrhea, dysbacteriosis, change of biochemical indicators (increase in activity of hepatic transaminases and bilirubin in a blood plasma), cholestatic jaundice, it is rare – pseudomembranous colitis;
From system of a hemopoiesis: an eosinophilia, a leukopenia, a neutropenia, a lymphopenia, thrombocytopenia, it is rare – hemolitic anemia; in some cases the level of plasma factors of turning of blood decreases (ІІ, V ІІ, ІХ, X), the prothrombin time is extended;
From TsNS: headache, dizziness;
Allergic reactions: urticaria, an itch, dermatitis, a serum disease, a bronchospasm, hypostases, a multiformny exudative erythema, anaphylactic reactions, in some cases – an acute anaphylaxis;
Local reactions: pain or infiltrate in an injection site; in some cases – phlebitis or thrombophlebitis at intravenous administration;
From urinogenital system: increase in level of creatinine, emergence of cylinders, oliguria, anury;
The effects caused by biological effect: development of superinfection is possible;
Others: nasal bleedings, fever, a fever, it is very rare - an acute renal failure, arrhythmias.

Interaction with other medicines:

At use Tseftriaksona-BHFZ in a combination with aminoglycosides owing to a synergism raises efficiency in relation to gram-negative microorganisms, however the choice of their optimum doses is necessary. Non-steroidal anti-inflammatory drugs, antiagregant raise a possibility of bleeding, loopback diuretics and nephrotoxic drugs (aminoglycosides, polymyxin B) cause a renal failure. Solution Tseftriaksona-BHFZ should not be mixed or to enter at the same time with other germicides or solutions in connection with pharmaceutical incompatibility.

Contraindications:

Hypersensitivity to antibiotics of a tsefalosporinovy row and another beta лактамным to antibiotics, hypersensitivity to lidocaine (intramuscular introduction); pregnancy.

Overdose:

At overdose there is no specific antidote, treatment – symptomatic. A hemodialysis or peritoneal dialysis Tseftriaksona-BHFZ in a blood plasma does not reduce high concentration.

Storage conditions:

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

Period of validity - 2 years.

Issue conditions:

According to the recipe

Packaging:

Powder for injections in bottles on 500 mg or 1000 mg, on 5 bottles in a case.