Tseftriakson Kabi

General characteristics. Structure:

Active ingredient: 500 mg, 1000 mg or 2000 mg of a tseftriakson in the form of a tseftriakson of sodium of a triseskvigidrat.

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 concerning 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, Enterobacter aerogenes, Enterobacter cloacae, Escherichia coli, Haemophilus influenzae (including the strains forming a penicillinase), Haemophilus parainfluenzae, Klebsiella spp. (including Klebsiella pneumoniae), Moraxella catarrhalis, (including penitsillinazoprodutsiruyushchy strains), Morganella morganii, Neisseria gonorrhoeae (including the strains forming a penitsnllinaza), Neisseria meningitidis, Proteus mirabilis, Proteus vulgaris, Serratia spp. (including Serratia marcescens), Borrelia burgdorferi; 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., 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%, time of achievement of Cmax later in / мо introductions - 2-3 h, later in/in introductions - at the end of an injection. Cmax after introduction in oil in doses of 0.5 and 1 g - about 38 and 76 m of kg/ml respectively. Cmax at in introduction in doses 0.5; 1 and 2 g - on average 82, 151 and 257 mkg/ml respectively. At adults in 2-24 h after introduction in a dose of 50 mg/kg concentration in cerebrospinal fluid (SMZh) many times over surpasses the minimum overwhelming concentration (MOC) 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%. Vd – 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 of 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 the patients who are on a hemodialysis (the clearance of creatinine (CC) of 0-5 ml/min.),-14.7 h at clearance of creatinine 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 infectious and inflammatory diseases caused by microorganisms, sensitive to a tseftrnakson: infections of abdominal organs (peritonitis, inflammatory diseases of the digestive tract (DT), biliary tract including a cholangitis, an empyema of a gall bladder), infections of bodies of a small pelvis, a lower respiratory tract infection (including pneumonia, lung abscess, a pleura empyema), acute average otitis, infections of bones and joints, skin and soft tissues (including contaminated wounds and burns), the infections of urinary tract (complicated and uncomplicated), uncomplicated gonorrhea, bacterial meningitis, a bacterial septicaemia, a disease Laima (borreliosis). Prevention of postoperative infections. Infectious diseases at persons with the weakened immunity.

Route of administration and doses:

In/in (kapelno and struyno) and in oil. Not to use kaltsiysoderzhashchy solutions for cultivation! To adults and children 12 years - on 1-2 g of 1 times in days or 0.5-1 g each 12 h are more senior, the general daily dose should not exceed 4 g. A dose for newborns - 20-50 mg/kg/days.
 
For babies and children up to 12 years the maximum daily dose - 50-75 mg/kg. Children with body weight have 50 kg and apply doses to adults above. It is necessary to appoint a dose more than 50 mg/kg of body weight in a look in/in infusion within 30 min. Duration of a course depends on character and disease severity. Lyme's disease: to adults and children — 50 mg/kg (but no more than 2 g) 1 time in days within 14 days.
 
At uncomplicated gonorrhea – in oil once 250 mg.
 
For prevention of postoperative complications - once 1 g in 30-60 min. prior to operation. At operations on thick and a rectum recommend additional administration of drug from group of 5-nntroimndazol.
 
At bacterial meningitis at children an initial dose - 100 mg/kg (but no more than 4 g) 1 time in days, further 100 mg/kg/days (but no more than 4 g) or divided in 2 receptions (each 12 h) or can be lowered once a day. Duration of treatment makes 7-14 days.
 
To children with infections of skin and soft tissues the recommended daily dose of 50-75 mg/kg of 1 times in days or 25-37,5 mg/kg each 12 h. At heavy infections of other localization - 25-37.5 mg/kg each 12 h. The maximum daily dose at children should not exceed 2 g.
 
At treatment of acute average otitis at children - in oil, once. 50 mg/kg, no more than 1 g.
 
Dose adjustment is required to patients with the chronic renal failure (CRF) only at the clearance of creatinine (CC) lower than 10 ml/min. In this case the daily dose should not exceed 2 g. The patients who are on a hemodialysis do not need introduction of an additional dose after the hemodialysis session, however, it is necessary to control concentration of a tseftriakson in plasma as its removal at such patients can be slowed down (dose adjustment can be required).
 
At patients with a renal liver failure the daily dose should not exceed 2 g without definition of concentration of drug in a blood plasma. Treatment tseftriaksony has to continue at least 2 more days after disappearance of symptoms and symptoms of an infection. The course of treatment usually makes 4-14 days, at the complicated infections more long introduction can be required. The course of treatment at the infections caused by Streptococcus pyogenes has to make not less than 10 days.
 
Rules of preparation and administration of solutions: it is necessary to use only freshly cooked solutions. For introduction in oil 0.5 g of drug dissolve in 2 ml, and 1 g - in 3.5 ml of 1% of solution of lidocaine. Recommend to enter no more than 1 g into one muscle.
 
For in/in an injection of 0.5 g dissolve in 5 ml, and 1 g - in 10 ml of water for injections. Enter in/in slowly (2-4 min.).
 
For in/in infusions dissolve 2 g in 40 ml of solution, not calciferous (0.9% solution of sodium of chloride, 5-10% solution of a dextrose, 5% levuloza solution). Doses of 50 mg/kg and more should be entered in/in kapelno, within 30 min.

Features of use:

Use at pregnancy and feeding by a breast.  At pregnancy drug is used only if the estimated advantage for mother exceeds potential risk for a fruit. At drug use feeding by a breast should be stopped

Use at abnormal liver functions.  With care: liver failure.

Use at renal failures.  With care: renal failure. Dose adjustment is required to patients with the chronic renal failure (CRF) only at the clearance of creatinine (CC) lower than 10 ml/min.

Use for children.  It is contraindicated at a hyperbilirubinemia at newborns. Not to apply at newborns to whom it is shown in/in administration of solutions, calciferous. With care: premature children

Special instructions. At a simultaneous heavy renal and liver failure, and also at the patients who are on a hemodialysis it is regularly necessary to define concentration of drug in 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 ultrasound examination (ultrasonography) of a gall bladder blackouts (precipitated calcium superphosphates of calcic salt of a tseftriakson) which disappear after the treatment termination are noted. At development of the symptoms or signs indicating a possible disease of a gall bladder or in the presence of an ultrasonography signs of "slanzh-phenomenon" it is recommended to stop administration of drug. At use of drug exceptional cases of the pancreatitis which developed perhaps, owing to obstruction of bilious ways are described (the previous therapy by drug, serious associated diseases, completely parenteral food), at the same time it is impossible to exclude a starting role of formation of precipitated calcium superphosphates in bilious ways under the influence of a tseftriakson. Does not support N-methylthiotetracindery group which causes disulfiramopodobny effects at simultaneous use of ethanol and bleeding which are inherent in some cephalosporins. At use of drug exceptional cases of change of a prothrombin time are described.
 
Control of a prothrombin time and purpose of vitamin K (10 mg/week) at increase in a prothrombin time prior to the beginning of can be required by patients with deficit of vitamin K (synthesis disturbance, disturbance of food) or during therapy.
 
Cases of fatal reactions as a result of adjournment of tseftriakson-calcium precipitated calcium superphosphates in lungs and kidneys of newborns are described. Theoretically, there is a probability of interaction of a tseftriakson with kaltsiysoderzhashchy solutions for intravenous administration and at other age groups of patients therefore цефтриаксон should not mix up with kaltsiysoderzhashchy solutions (including for parenteral food), and also is entered at the same time, including through separate accesses for infusions on various sites. Theoretically, on the basis of calculation of 5 elimination half-lives of a tseftriakson the interval between introduction of a tseftriakson and kaltsiysoderzhashchy solutions has to make not less than 48 h.
 
At treatment tseftriaksony false positive results of test of Koombs, test on a galactosemia can be noted, when determining glucose in urine (the glucosuria is recommended to be determined only by a fermental method).
 
Influence on ability to driving of motor transport and to control of mechanisms. The patients applying цефтриаксон should be careful during the driving of the car and occupations other potentially dangerous types of activity requiring special attention and speed of psychomotor reactions.

Side effects:

Allergic reactions: rash, itch, heat or fever.
 
Local reactions: at in introduction - phlebitis, morbidity on the vein course; introduction in oil - morbidity, a caumesthesia, tightness or consolidation in an injection site.
 
From the central nervous system: headache, dizziness.
 
From a reproductive system: vagina candidiasis, vaginitis.
 
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.
 
Laboratory indicators: increase (reduction) in a prothrombin time, hamaturia, increase in activity of "hepatic" transaminases and alkaline phosphatase (AP), 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, heart consciousness, spasms, serum disease, stomatitis, glossitis, oliguria, allergic dermatitis, small tortoiseshell, hypostasis, multiformny erythema, Stephens-Johnson's syndrome, Lyell's disease.

Interaction with other medicines:

Bacteriostatic anti-high overshoes reduce bactericidal effect of a tseftriakson. Pharmaceutical it is incompatible with solutions, calciferous (including Hartman and Ringer's solution), and also with amsakriny, Vancomycinum, flukonazoly and aminoglycosides.

Contraindications:

Hypersensitivity (including to other cephalosporins, penicillin, karbapenema); a hyperbilirubinemia at newborns; newborns to whom it is shown in/in administration of solutions, calciferous; lactation period.
 
With care. Premature children, a renal and/or liver failure, the ulcer colitis, enteritis or colitis connected using antibacterial medicines.
 
Use of drug at pregnancy and during feeding by a breast. At pregnancy drug is used only if the estimated advantage for mother exceeds potential risk for a fruit. At drug use feeding by a breast should be stopped.

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. There is no specific antidote.

Storage conditions:

At a temperature not above 25 °C in the place protected from light. To store in the place, unavailable to children. Period of validity. 3 years. Not to use after the period of validity specified on packaging.

Issue conditions:

According to the recipe

Packaging:

500 mg - bottles glass with a capacity of 15 ml (1) - packs cardboard.
500 mg - bottles glass with a capacity of 15 ml (10) - packs cardboard.