Tseftriakson-Dzhodas

General characteristics. Structure:

Active ingredient: 1 g of sterile sodium salt of a tseftriakson (equivalent to a tseftriakson) in 1 bottle.

Tseftriakson - a semi-synthetic tsefalosporinovy antibiotic of the III generation of a broad spectrum of activity.

Pharmacological properties:

Pharmacodynamics. Bactericidal activity of a tseftriakson 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.

Tseftriakson is active concerning the following microorganisms:
- Gram-negative aerobes: Enterobacter aerogenes, Enterobacter cloacae, Escherichia coli, Haemophilus influenzae (including strains steady against ampicillin), Haemophilus parainfluenzae, Klebssiella spp. (including Klebssiella pneumoniae), Neisseria gonorrhoeae (including the strains which are forming and not forming a penicillinase), Neisseria meningitidis, Proteus mirabilis, Proteus 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 a tseftriakson. Separate strains of Pseudomonas aerugenosa are also sensitive to drug.

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

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

Pharmacokinetics. At intramuscular introduction цефтриаксон it is well absorbed from an injection site and reaches high concentration in serum. Bioavailability of drug - 100%.

Average concentration in plasma is reached in 2-3 hours after an injection. At repeated intramuscular or intravenous administration in doses of 0,5-2,0 g to an interval from 12 to 24 hours there is an accumulation of a tseftriakson in concentration which for 15%-36% exceeds the concentration reached at single introduction. At introduction 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 plasma clearance – 0.58-1.45 l/h, renal clearance – 0.32-0.73 l/h Tseftriakson reversibly contacts proteins of a blood plasma. From 33% to 67% of drug it is removed in an invariable view with urine, other part is excreted with bile in intestines where it biotransformirutsya in an inactive metabolite.

Penetration into cerebrospinal fluid: at newborns and at children at a meninx inflammation цефтриаксон gets into liquor, at the same time in case of bacterial meningitis on average 17% of concentration of drug in plasma diffuse in cerebrospinal fluid that is about 4 times more, than at aseptic meningitis. In 24 hours after intravenous administration of a tseftriakson in a dose of 50-100 mg/kg of body weight of concentration in cerebrospinal fluid exceed 1.4 mg/l. At adult patients with meningitis in 2-24 hours, after introduction of a dose of 50 mg/kg of body weight, concentration of a tseftriakson in cerebrospinal fluid many times over surpass the minimum overwhelming concentration for the most widespread causative agents of meningitis. 

Indications to use:

The infectious and inflammatory diseases caused by sensitive activators: sepsis; meningitis; the disseminated Lyme's borreliosis (early and late stages of a disease); infections of abdominal organs (peritonitis, infections of bilious ways and digestive tract); infections of bones, joints, soft tissues, skin, and also wound fevers; infections at patients with the weakened immunity; infections of bodies of a small pelvis; infections of kidneys and urinary tract; respiratory infection and ENT organs; infections of generative organs, including gonorrhea. Perioperatsionny prevention of infections.

Route of administration and doses:

The drug is administered intramusculary or intravenously. Standard mode of dosing. Adults and children are more senior than 12 years: on 1-2 g once a day (each 24 hours). In hard cases or at infections which causative agents have only moderate sensitivity to a tseftriakson it is possible to increase a daily dose to 4 g.

Newborns (up to 2 weeks): 20-50 mg/kg of body weight once a day. The daily dose should not exceed 50 mg/kg of body weight. When determining a dose it is not necessary to do distinctions between the full-term and premature children.

Babies and children of younger age (from 15 days to 12 years): 20-80 mg/kg of body weight once a day. To children with body weight over 50 kg appoint doses for adults. Intravenous doses or should be entered into 50 mg/kg kapelno above within not less than 30 minutes.

Patients of senile age: usual doses for adults, without amendments on age. Duration of treatment depends on the course of a disease. As well as always at an antibioticotherapia, introduction of a tseftriakson should be continued the patient within at least 48-72 hours after normalization of temperature and confirmation of an eradikation of the activator.

Dosing in special cases:
• At bacterial meningitis at babies and children of younger age treatment begin with a dose 100 mg/kg (but no more than 4 g) 1 time a day. After identification of the activator and definition of its sensitivity, the dose can be reduced respectively. The best results at a spotted fever were achieved lasting treatment of 4 days, at the meningitis caused by Haemophilus influenzae - 6 days, Streptococcus pneumoniae - 7 days.
• Lyme's borreliosis: 50 mg/kg (the highest daily dose - 2 g) to adults and children are more senior 12 years within 14 days once a day.
• The gonorrhea (caused by penitsillinazoobrazuyushchy and penitsillinazoneobrazuyushchy strains): single intramuscular introduction of 250 mg of drug.
• Prevention of postoperative infections, depending on degree of infectious risk, is entered by 1-2 g of a tseftriakson once in 30-90 min. prior to operation. At operations on thick and a rectum well proved simultaneous (but separate) introduction of a tseftriakson and one of 5 nitroimidazoles, for example, of an ornidazol.
• Patients with a renal failure have no need to reduce a dose if function of a liver remains normal. The daily dose of a tseftriakson should not exceed 2 g only in cases of a preterminal renal failure (clearance of creatinine less than 10 ml/min.). • Patients with an abnormal liver function have no need to reduce a dose if function of kidneys remains normal.
• At a combination of a heavy renal and liver failure it is regularly necessary to define concentration of a tseftriakson in plasma and if necessary to adjust its dose.
• On dialysis of additional administration of drug after dialysis it is not required to patients. It is necessary to control, however, concentration of a tseftriakson in serum regarding possible dose adjustment as the speed of removal of drug at these patients can decrease.

Route of administration. For intramuscular introduction: Contents of a bottle are dissolved as follows: 250 mg of contents of a bottle dissolve in 0,9 ml of water for injections, 1 g of contents of a bottle - in 3,6 ml of water for injections. 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 intramuscular injections Tseftriakson-Dzhodas enter into rather large muscle; trial aspiration helps to avoid inadvertent introduction to a blood vessel. It is recommended to enter no more than 1000 mg of drug into one buttock. For reduction of pain at intramuscular injections the drug should be administered with 1% lidocaine solution (vnutriyagodichno). It is impossible to enter lidocaine solution intravenously.

For intravenous administration: Contents of a bottle are dissolved as follows: 250 mg of contents of a bottle rastovryat in 2,4 ml of water for injections, 1 g of contents of a bottle - in 9,6 ml of water for injections. After preparation each ml of solution contains about 100 mg in terms of цефтриаксон. Solution is entered slowly within 2-4 min.

For intravenous infusion dissolve 2 g of Tseftriaksona-Alp in 40 ml of sterile water for injections or one of the infusion solutions which are not containing calcium (0.9% solution of sodium of chloride, 2.5%, 5% or 10% solution of a dextrose, 5% solution of a levuloza, 6% dextran solution in Dextrosum). Solution is entered within 30 min.

Features of use:

Use at pregnancy and in the period of a lactation. Use of drug 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 use of drug in the period of a lactation it is necessary to resolve an issue of the breastfeeding termination (цефтриаксон it is allocated with breast milk).

At a simultaneous heavy 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 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 the treatment termination are noted (even if this phenomenon is followed by pains in right hypochondrium, continuation of purpose of an antibiotic and carrying out a symptomatic treatment is recommended).

During treatment ethanol use is contraindicated - disulfiramopodobny effects are possible (face reddening, a spasm in a stomach and in a stomach, nausea, vomiting, a headache, a lowering of arterial pressure, tachycardia, short wind).

Despite detailed collecting the anamnesis that is the rule and for other tsefalosporinovy antibiotics, it is impossible to exclude a possibility of development of an acute anaphylaxis which demands immediate therapy – at first intravenously enter Epinephrinum, then glucocorticosteroids.

The researches in vitro showed that it is similar to other tsefalosporinovy antibiotics, цефтриаксон is capable to force out the bilirubin connected with blood serum albumine. Therefore with a hyperbilirubinemia and, especially, at premature newborns use of a tseftriakson demands a bigger care from newborns.

Purpose of vitamin K can be required by the elderly and weakened patients.

To store the prepared solution at the room temperature no more than 6 hours or in the refrigerator at a temperature of 2-8 °C no more than 24 watch.

Side effects:

Allergic reactions: a small tortoiseshell, a fever or fever, rash, an itch, it is rare - a bronchospasm, an eosinophilia, an erythema exudative multiformny (including Stephens-Johnson's syndrome), a serum disease, an acute anaphylaxis.

From the alimentary system: nausea, vomiting, diarrhea or a lock, a meteorism, abdominal pains, taste disturbance, stomatitis, a glossitis, a pseudomembranous coloenteritis, an abnormal liver function (increase in activity of "hepatic" transaminases, is more rare - an alkaline phosphatase or bilirubin, cholestatic jaundice), a pseudo-cholelithiasis of a gall bladder ("sludge" - a syndrome), dysbacteriosis.

From bodies of a hemopoiesis: anemia, leukopenia, leukocytosis, neutropenia, granulocytopenia, lymphopenia, thrombocytosis, thrombocytopenia, hemolitic anemia, hypocoagulation, decrease in concentration of flame blood-coagulation factors (II, VII, IX, X), lengthening of a prothrombin time.

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.

Local reactions: phlebitis, morbidity on the vein course, morbidity and infiltrate in the place in oil of introduction.

Others: headache, dizziness, nasal bleedings, candidiasis, superinfection.

Interaction with other medicines:

Tseftriakson, suppressing an indestinal flora, interferes with vitamin K synthesis. At co-administration with the drugs reducing aggregation of thrombocytes (non-steroidal anti-inflammatory drugs, salicylates, Sulfinpyrazonum) the risk of development of bleedings increases. 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.

Tseftriakson and aminoglycosides possess a synergism concerning many gram-negative bacteria.

It is incompatible with ethanol.

Pharmaceutical interaction: solutions of a tseftriakson should not be mixed or entered along with other antimicrobic drugs. Tseftriakson it is impossible to mix with solutions, calciferous

Contraindications:

Hypersensitivity including to others to cephalosporins, penicillin, karbapenema.

With care: appoint drug at nonspecific ulcer colitis, at abnormal liver functions and kidneys, at the enteritis and colitis connected using antibacterial drugs; to premature and newborn children with a hyperbilirubinemia, pregnancy and in the period of a lactation.

Overdose:

At overdose the hemodialysis and peritoneal dialysis will not reduce concentration of drug. There is no specific antidote.

Overdose treatment symptomatic.

Storage conditions:

Period of validity 3 years. Not to use after the expiry date specified on packaging. Storage conditions: to store in dry, protected from light and the place, unavailable to children, at a temperature not above 25 °C.

Issue conditions:

According to the recipe

Packaging:

Powder for preparation of solution for intravenous and intramuscular administration of 1.0 g. On 1,0 g in the bottle of transparent glass corked by a stopper from the chlorbutyl rubber which is pressed out by an aluminum ring with a safety plastic cap. On 1 bottle together with the application instruction in a cardboard pack. For hospitals: on 10,20,48 and 100 bottles together with the application instruction in a cardboard box.