Chison - instructions for use, dose, side effects, contraindications

Ceftriaxone is a third generation cephalosporin antibiotic for parenteral use, has a bactericidal effect, inhibits the synthesis of the cell membrane, in vitro Suppresses the growth of most gram-positive and gram-negative enzymes (both penicillinase and cephalosporinase, produced by most gram-positive and gram-negative bacteria). Effective against the following microorganisms:

Gram-positive

Staphylococcus aureus (including strains producing penicillinase), Staphylococcus epidermidis, Streptococcus pneumoniae, Streptococcus pyogenes, Streptococcus viridans;

Note: Staphylococcus spp., resistant to methicillin, is resistant to cephalosporins, including ceftriaxone. Most strains of enterococci (for example, Streptococcus faecalis) also resistant to ceftriaxone.

Gram-negative

Acinetobacter calcoaceticus, Enterobacter aerogenes, Enterobacter cloacae, Escherichia coli, Haemophilus influenzae (including strains that form penicillinase), Haemophilus parainfluenzae, Klebsiella spp. (including Klebsiella pneumoniae), Moraxella catarrhalis, (including penicillin-producing strains), Morganella morganii, Neisseria gonorrhoeae (including strains that form penicillinase), Neisseria meningitidis, Plesiomonas shigelloides, Proteus mirabilis, Proteus vulgaris, Providencia spp., Pseudomonas aeruginosa (some strains are resistant), Salmonella spti. (including Salmonella typhi), Serratia spp. (including Serratia marcescens), Shigella spp., Vibrio spp. (at Tom number of Vibrio cholerae), Yersinia spp. ( at Tom number of Yersinia enterocolitica).

Note: many strains of these microorganisms, which in the presence of other antibiotics, for example penicillins, first-generation cephalosporins and aminoglycosides, are multiplying steadily, are sensitive to ceftriaxone. Treponema pallidum is sensitive to ceftriaxone as in vitro, and in experiments on animals. According to clinical data, in the primary and secondary syphilis, a good efficacy of ceftriaxone is noted.

Anaerobic pathogens

Bacteroides spp. (including some strains Bacteroides fragilis), Clostridium spp. (at Tom number of Clostridium difficile), Fusobacterium spp. (Besides Fusobacterium mostiferum, Fusobacterium varium), Peptococcus spp., Peptostreptococcus spp.

Note: some strains of many Bacteroides spp. (eg, Bacteroides fragilis), Developing beta-lactamase, resistant to ceftriaxone. To determine the sensitivity of microorganisms, discs containing ceftriaxone, since it is shown that in vitro to classical cephalosporins, certain strains of pathogens can be stable.

Pharmacokinetics:

With parenteral administration ceftriaxone well penetrates into tissues and body fluids.

The area under the concentration curve - time in the blood serum for intravenous and intramuscular injection coincide. This means that the bioavailability of ceftriaxone when administered intramuscularly is 100%. With intravenous administration ceftriaxone quickly diffuses into the interstitial fluid, where its bactericidal action against pathogens sensitive to it persists for 24 hours.

Ceftriaxone reversibly binds to albumin and this binding is inversely proportional to the concentration: for example, when the drug concentration in the serum is less than 100 mg / l, ceftriaxone binding to proteins is 95%, and at a concentration of 300 mg / l - only 85%).Due to the lower the concentration of ceftriaxone in the interstitial fluid is higher in albumin than in serum.

The half-life in healthy adults is about 8 hours. In newborns up to 8 days and in elderly people older than 75 years, the average half-life is approximately twice as large. In adults, 50-60% of ceftriaxone is excreted unchanged in urine, and 40-50% is also unchanged in bile. Under the influence of intestinal flora ceftriaxone turns into an inactive metabolite. In neonates, approximately 70% of the administered dose is excreted by the kidneys. In renal failure or liver disease in adults pharmacokinetics ceftriaxone hardly changes, half-life period is lengthened slightly. If the kidney function is impaired, the secretion with bile increases, and if liver pathology takes place, then the excretion of ceftriaxone by the kidneys increases.

Penetration into the cerebrospinal fluid: in newborns and in children with inflammation of the meninges ceftriaxone penetrates into the cerebrospinal fluid, while in the case of bacterial meningitis, an average of 17% of the concentration of the drug in the blood serum diffuses into the cerebrospinal fluid, which is approximately 4 times greater than with aseptic meningitis.24 hours after intravenous administration of ceftriaxone in a dose of 50-100 mg / kg body weight, the concentration in the cerebrospinal fluid exceeds 1.4 mg / l. In adults with meningitis, 2 to 25 hours after the administration of ceftriaxone at a dose of 50 mg / kg body weight, the concentration of ceftriaxone was many times greater than the minimum oppressive dose that is necessary to suppress the pathogens most commonly causing meningitis.

Indications:Bacterial infections caused by sensitive microorganisms: infections of the abdominal cavity (peritonitis, inflammatory diseases of the gastrointestinal tract, bile ducts, including cholangitis, gallbladder empyema), diseases of the upper and lower respiratory tract (including pneumonia, lung abscess , empyema of the pleura), infections of bones, joints, skin and soft tissues, urogenital infections (including gonorrhea), infections of the kidneys and urinary tract, bacterial meningitis, sepsis. Prevention of infections in the postoperative period.

Contraindications:Hypersensitivity (including other cephalosporins, penicillins, carbapenems).

Carefully:Hyperbilirubinemia in newborns, premature infants, renal and / or hepatic insufficiency, ulcerative colitis, enteritis or colitis associated with antibiotic LS, pregnancy (II and III trimester), lactation.

Pregnancy and lactation:

Chizon penetrates the placenta.

Adequate and well-controlled studies of the safety of the use of the drug Hyson during pregnancy have not been conducted.

The use of the drug Chizon during pregnancy is possible only if the potential benefit to the mother exceeds the possible risk to the fetus. Chysone is excreted in breast milk in low concentrations, however, during the treatment the drug should stop breastfeeding.

Dosing and Administration:

Intravenous and intramuscular.

- Adults and children over 12 years of age - 1-2 grams once a day or 0.5-1 g every 12 hours, daily dose should not exceed 4 g.

- For newborns (up to 2 weeks) - 20-50 mg / kg / day. Doses of the drug in children born on time, and in preterm infants are the same.

- For infants and children under 12 years of age, the daily dose is 20-75 mg / kg. In children with a body weight of 50 kg and above, doses for adults are used.A dose of more than 50 mg / kg body weight should be administered as an intravenous infusion within 30 minutes.

The length of the course depends on the nature and severity of the disease.

- Gonorrhea - intramuscularly once, 250 mg.

- Prevention of postoperative complications - once, 1-2 g (depending on the degree of danger of infection) for 30-90 minutes before the operation.

- Bacterial meningitis in infants and young children - 100 mg / kg (but not more than 4 g) 1 time per day. As soon as it was possible to isolate the pathogenic microorganisms and determine its sensitivity, the dose of the drug can be reduced. The following duration of treatment with different pathogens is effective:

Causative agent	Duration of therapy
Neisseria meningitidis	4
Haemophilus influenzae	6
Streptococcus pneumoniae	7
Enterobacteriaceae (some sensitive strains)	10-14

- In patients with chronic renal failure, dose adjustment is required only when creatinine clearance is less than 10 ml / min. In this case, the daily dose should not exceed 2 g.

Rules for the preparation and administration of solutions: only freshly prepared solutions should be used.

For intramuscular administration, 1 g of the drug is diluted in 3.5 ml of a 1% solution of lidocaine. Recommend to enter no more than 1 g in one buttock. For intravenous injection, 1 g is dissolved in 10 ml of water for injection.Enter intravenously slowly (2-4 minutes).

For intravenous infusion, dissolve 2 g in 40 ml of a solution that does not contain Ca2 + ions (0.9% sodium chloride solution, 5-10% dextrose solution, 5% fructose solution). Doses of 50 mg / kg or more should be administered intravenously drip, for 30 minutes.

Side effects:

- Allergic reactions: fever or chills, eosinophilia, skin rash, hives, itching, erythema multiforme, angioneurotic edema, serum sickness, anaphylactic shock.

- Local reactions: with intravenous injection - phlebitis, tenderness along the vein; intramuscular injection - soreness at the injection site, infiltration.

- From the nervous system: headache, dizziness.

- From the urinary system: oliguria, anuria. Impaired renal function (azotemia, increased urea in the blood, hypercreatininaemia, glucosuria, cylindruria, hematuria).

- On the part of the digestive system: nausea, vomiting, taste disorder, flatulence, stomatitis, glossitis, diarrhea, pseudomembranous enterocolitis; pseudocholithiasis of the gallbladder ("sludge" - syndrome), increased activity of "liver" transaminases and alkaline phosphatases, hyperbilirubinemia.

- From the hemopoiesis: anemia, leukopenia, leukocytosis, lymphopenia, neutropenia, granulocytopenia, thrombocytopenia, thrombocytosis, basophilia, hematuria; hemolytic anemia, hypocoagulation, decrease in the concentration of plasma clotting factors (II, VII, IX, X), prolongation of prothrombin time.

- On the part of the respiratory system: interstitial pneumonia, pulmonary infiltration with eosinophilia can rarely occur (especially when the drug is combined with other cephalosporins).

Overdose:Excessively high concentrations of ceftriaxone in plasma can not be reduced by hemodialysis or peritoneal dialysis. Symptomatic measures are recommended for the treatment of overdose cases.

Interaction:

Chysone and aminoglycosides have a synergistic effect on many gram-negative bacteria. Incompatible with ethanol, non-steroidal anti-inflammatory drugs, with solutions containing calcium salts, fluconazole, vancomycin, amsacrine.

Inhibitors of platelet aggregation increase the likelihood of bleeding. When used simultaneously with loop diuretics and other nephrotoxic drugs, the risk of developingnephrotoxic action. Pharmaceutically incompatible with solutions containing other antibiotics.

Special instructions:

Chizon is used only in a hospital. With simultaneous severe renal and hepatic insufficiency, in patients who are on hemodialysis, the concentration of the drug in the plasma should be regularly determined. With long-term treatment, it is necessary to regularly monitor the picture of peripheral blood, indicators of the functional state of the liver and kidneys. In rare cases with ultrasound of the gallbladder, blackouts are observed, which disappear after the cessation of treatment. Even if this phenomenon is accompanied by pain in the right hypochondrium, it is recommended to continue the appointment of an antibiotic and conduct symptomatic treatment. During treatment, the use of ethanol is contraindicated - disulfiramoid-like effects are possible (face hyperemia, stomach and stomach spasms, nausea, vomiting, headache, lowering of blood pressure, tachycardia, dyspnea). Elderly and debilitated patients may require the appointment of vitamin K.

Form release / dosage:

Powder for solution for intravenous and intramuscular injection 1 g.

Packaging:

Powder for the preparation of solution for intravenous and intramuscular administration of 1 g in colorless glass type I bottles with a capacity of 10 ml, sealed with a rubber stopper under running-in with an aluminum cap with a red plastic safety lid. For 10 bottles separated by a foam partition, together with the instructions for use are placed in a cardboard box.

Storage conditions:

Store in a dark place at a temperature of no higher than 25 ° C. Keep out of the reach of children!

Shelf life:

Three years. Do not use after the expiration date printed on the package.

Terms of leave from pharmacies:On prescription

Registration number:LSR-001363/08

Date of registration:29.02.2008

The owner of the registration certificate:Shin Pung Pharmaceutical Co., Ltd.Shin Pung Pharmaceutical Co., Ltd. The Republic of Korea

Manufacturer: & nbsp

SHIN POONG PHARMACEUTICAL, Co. Ltd. The Republic of Korea

Representation: & nbspPharmInform Ltd.PharmInform Ltd.Russia

Information update date: & nbsp25.11.2015

Illustrated instructions

Instructions

Chizon (Hizone)