Azawounds

General characteristics. Structure:

Active agent: цефтриаксон (in the form of sodium salt) 1 g.

Pharmacological properties:

Tsefalosporinovy antibiotic of the III generation of a broad spectrum of activity for parenteral administration. Works bakteritsidno, oppressing synthesis of a cell wall of bacteria. Acetylates membrane-bound transpeptidases, breaking thus the cross stitching of peptidoglikan necessary for ensuring durability and rigidity of a cell wall. It is steady in the relation β-лактамаз, the gram-positive and gram-negative bacteria produced by the majority.
It is active concerning gram-positive aerobic bacteria: Staphylococcus aureus, Staphylococcus epidermidis, Streptococcus pneumoniae, Streptococcus pyogenes, Streptococcus agalactiae, Streptococcus viridans, Streptococcus bovis; gram-negative aerobic bacteria: Acinetobacter lwoffii, Acinetobacter anitratus, Aeromonas hydrophila, Alcaligenes faecalis, Alcaligenes odorans, Citrobacter spp., Enterobacter spp. (some strains of a rezistentna), Escherichia coli, Haemophilus ducreyi, Haemophilus influenzae (including the strains producing a penicillinase), Haemophilus parainfluenzae, Klebsiella spp. (including Klebsiella pneumoniae), Moraxella spp., Morganella morganii, Neisseria gonorrhoeae (including the strains producing a penicillinase), Neisseria meningitidis, Plesiomonas shigelloides, Proteus mirabilis, Proteus vulgaris, Providencia spp., Salmonella spp. (including Salmonella typhi), Serratia spp. (including Serratia marsescens), Shigella spp., Vibrio spp. (including Vibrio cholerae), Yersinia spp. (including Yersinia enterocolitica), Pseudomonas aeruginosa (some strains); gram-negative anaerobic bacteria: Bacteroides spp. (including some strains of Bacteroides fragilis), Clostridium spp. (except Clostridium difficile), Fusobacterium spp. (except Fusobacterium mortiferum and Fusobacterium varium), Peptococcus spp., Peptostreptococcus spp.

Are steady against drug Methicillinum - resistant strains of Staphylococcus spp., Enterococcus spp strains. (Enterococcus faecalis), Clostridium difficile, many strains of Bacteroides spp. (the producing β-lactamelements).

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%.

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.
Gets through a placental barrier in small amounts.

Removal. T1/2 makes 6-9 h that allows to use drug of 1 times /
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 excrete 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 (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.
Tseftriakson is not brought at a hemodialysis.

Indications to use:

Treatment of the infectious and inflammatory diseases caused by sensitive microorganisms:

— infections of upper and lower parts of respiratory tracts (including pneumonia, abscess of lungs, pleura empyema);
— infections of skin and soft tissues;
— infections of bones and joints;
— infections of urinary tract (including pyelonephritis);
— inflammatory gastrointestinal diseases and biliary tract (including cholangitis, empyema of a gall bladder);
— infections of bodies of a small pelvis;
— peritonitis;
— bacterial meningitis;
— bacterial endocarditis;
— sepsis;
— acute uncomplicated gonorrhea;
— Lyme's disease;
— shigellosis;
— salmonellosis.

Prevention and treatment of infectious postoperative complications.

Route of administration and doses:

The drug is administered in oil or in/in struyno or kapelno.
For adults and children 12 years an average daily dose are more senior makes 1-2 g of 1 times / the Maximum daily dose for adults - 4 g.
For newborns aged up to 14 days the dose makes 20-50 mg/kg / the Maximum daily dose of 50 mg/kg.
For children aged from 15 days and up to 12 years the daily dose makes 20-80 mg/kg.
To children with body weight more than 50 kg appoint doses for adults.
The daily dose of 50 mg/kg and more should be applied in the form of infusions within 30 min.
Course duration usually does not exceed 10 Administration of drug it is necessary to continue within 2-3 days after normalization of body temperature and disappearance of symptoms.
For prevention of infections in the postoperative period the drug is administered once in 30-90 min. prior to operation in a dose of 1-2 g (depending on degree of infectious risk). At operational interventions 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 the dose makes 100 mg/kg of 1 times / the Maximum daily dose – 4 g. Duration of therapy depends on a type of the activator and can make of 4 days at the meningitis caused by Neisseria meningitidis up to 10-14 days at the meningitis caused by sensitive strains of Enterobacteriaceae.
At acute uncomplicated gonorrhea the drug is administered in oil once in a dose of 250 mg.
At Lyme's disease appoint to adults and children in a dose of 50 mg/kg of 1 times/, the maximum daily dose - 2 g. Treatment duration - 14 days.
With renal failures dose adjustment is required from patients only at a renal failure of heavy degree (KK less than 10 ml/min.), in this case the daily dose of a tseftriakson should not exceed 2 g.
Patients with renal failures have no need of dose adjustment if function of a liver remains normal.
Patients with abnormal liver functions have no need of dose adjustment if function of kidneys remains normal.
At a combination of a renal failure and liver failure it is regularly necessary to control concentration of a tseftriakson in plasma and if necessary to adjust its dose.
To the patients who are on a hemodialysis, additional introduction after carrying out dialysis is not required since цефтриаксон is not removed at a hemodialysis. Speed of removal of a tseftriakson at such patients can change therefore it is necessary to control concentration of a tseftriakson in a blood plasma regarding possible dose adjustment.

Rules of preparation and administration of solution for injections

Preparation of solution for introduction in oil
1 g of drug dissolve in 3.6 ml of water for injections, 1 ml of the received solution contains about 250 mg of a tseftriakson. If necessary it is possible to use more weak solution.
1 g of drug dissolve 1% of solution of lidocaine of chloride in 3.5 ml. Enter deeply into rather large muscle (in a gluteus or in a hip muscle). It is not necessary to enter more than 1 g into one muscle. It is necessary to remember that it is impossible to enter solution of lidocaine of chloride in / century.

Preparation of solution for in/in injections
1 g of drug dissolve in 9.6 ml of sterile water for injections, 1 ml of the received solution contains about 100 mg of a tseftriakson. Solution is entered in/in slowly within 2-4 min.

Preparation of solution for in/in infusions
2 g of drug dissolve in 40 ml of one of the solutions which are not containing in the composition of calcium (0.9% chloride sodium solution; 0.45% chloride sodium solution + 2.5% dextrose solution; 5% dextrose solution; 10% dextrose solution; 6% dextran solution in 5% dextrose solution; 6-10% solution of hydroxyethylated starch). Duration in/in infusion makes not less than 30 min.

Freshly cooked solutions of a tseftriakson are stable during 6 h at the room temperature and during 24 h at storage in the refrigerator at a temperature from 2 ° to 8 °C.

Features of use:

Drug is used only in the conditions of a hospital.
At a simultaneous heavy renal and liver failure at the patients who are on a hemodialysis it is regularly necessary to control concentration of a tseftriakson in a blood 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 drug withdrawal are noted (even if this phenomenon is followed by pains in right hypochondrium, recommend to continue purpose of an antibiotic and carrying out a symptomatic treatment).
At use of drug it is impossible to use ethanol since development of disulfiramopodobny effects is possible (face reddening, spastic abdominal pains and in a stomach, nausea, vomiting, a headache, decrease in the ABP, tachycardia, short wind).
Against the background of Azaran's use purpose of vitamin K can be required by elderly people and the weakened patients.
Despite detailed collecting the anamnesis that is the rule and for other tsefalosporinovy antibiotics, it is impossible to exclude a possibility of development of anafilatichesky shock that demands immediate therapy: at first enter into Epinephrinum, then - GKS.
The researches in vitro showed that it is similar to other cephalosporins, цефтриаксон is capable to force out the bilirubin connected with blood serum albumine. Therefore at newborns with a hyperbilirubinemia and, especially at premature newborns, use of a tseftriakson demands a bigger care.

Side effects:

From TsNS: headache, dizziness.

From an urinary system: a renal failure (an azotemia, increase in content of urea in blood, a giperkreatininemiya, a glucosuria, a cylindruria, a hamaturia, an oliguria, an anury).

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

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

From coagulant system of blood: hypocoagulation, decrease in maintenance of plasma blood-coagulation factors (II, VII, IX, X), nasal bleeding, increase in a prothrombin time.

Allergic reactions: urticaria, rash, itch, fever, fever; seldom - a bronchospasm, hypostases, an eosinophilia, an exudative mnogoformny erythema (including Stephens-Johnson's syndrome), an acute anaphylaxis, a serum disease.

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

Others: superinfection (including candidiasis).

Interaction with other medicines:

Tseftriakson and aminoglycosides possess a synergism concerning many gram-negative bacteria (including Pseudomonas aeruginosa), the drugs should be administered separately in the recommended doses.
Tseftriakson, suppressing an indestinal flora, interferes with vitamin K synthesis. Therefore at simultaneous use with the drugs reducing aggregation of thrombocytes (NPVS, salicylates, Sulfinpyrazonum) the risk of development of bleedings increases.
At simultaneous use with anticoagulants strengthening of anticoagulating action is noted.
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 (including Vancomycinum and aminoglycosides) and with the solutions containing флуконазол.
Tseftriakson it is impossible to mix with solutions, calciferous (including with Ringer's solution).

Contraindications:

— hypersensitivity to drug components;
— hypersensitivity to other cephalosporins, penicillin and karbapenema.

With care appoint drug at abnormal liver functions and/or kidneys, to premature and newborn children with a hyperbilirubinemia, at NYaK, and also at the enteritis or colitis connected using antibacterial drugs.

Use of drug AZARAN at pregnancy and feeding by a breast
Azaran's use at pregnancy is possible only when the estimated advantage for mother exceeds potential risk for a fruit (цефтриаксон gets through a placental barrier).
In need of Azaran's use in the period of a lactation it is necessary to resolve an issue of the breastfeeding termination since цефтриаксон it is allocated with breast milk.

Use at abnormal liver functions
At patients with abnormal liver functions of T1/2 considerably increases.

Use at renal failures
With renal failures dose adjustment is required from patients only at a renal failure of heavy degree (KK less than 10 ml/min.), in this case the daily dose of a tseftriakson should not exceed 2 g.

Use for children
With care appoint drug to premature and newborn children.
Correction of the mode of dosing depending on age of the child is necessary.

Overdose:

Now about drug overdose cases Azaran it was not reported.
Treatment: performing symptomatic therapy. There is no specific antidote. For removal of a tseftriakson from an organism the hemodialysis and peritoneal dialysis are not effective.

Storage conditions:

List B. Drug should be stored in the unavailable to children, protected from light place at a temperature from 15 to 25 °C.

Issue conditions:

According to the recipe

Packaging:

Powder for пригот. solution for in/in and introductions of 1 g in oil: фл. 1, 10 or 50 pieces.