Ceftriaxone Danson - instructions for use, dose, side effects, contraindications

Cephalosporin antibiotic III generation of a broad spectrum of action for parenteral administration. Bactericidal activity is due to the suppression of bacterial cell wall synthesis. It is characterized by resistance to the action of most beta-lactamases of gram-negative and gram-positive microorganisms. It is active against the following microorganisms: Gram-positive aerobes-Staphylococcus aureus (including strains producing penicillinase), Staphylococcus epidermidis, Streptococcus pneumoniae, Streptococcus pyogenes, Streptococcus spp.groups of viridans; Gram-negative aerobes: Acinetobacter calcoaceticus, Borrelia burgdorferi, Enterobacter aerogenes, Enterobacter cloacae, Escherichia coli, Haemophilus influenzae (including _ penicillinase producing strains), Haemophilus parainfluenzae, Klebsiella spp. (including Klebsiella pneumoniae), Moraxella catarrhalis (including penicillinase producing strains, Morganella morganii, Neisseria gonorrhoeae (including strains producing penicillinase), Neisseria meningitidis, Proteus mirabilis, Proteus vulgaris, Serratia spp. (in tons Serratia marcescens), individual strains of Pseudomonas aeruginosa are also sensitive, anaerobes: Bacteroides fragilis, Clostridium spp. (except Clostridium difficile), Peptostreptococcus spp.

Has in vitro activity against most strains of the following microorganisms, although the clinical significance of this is unknown: Citrobacter diversus, Citrobacter freundii, Providencia spp. (including Providencia rettgeri), Salmonella spp., including Salmonella typhi, Shigella spp .; Streptococcus agalactiae, Bacteroides bivius, Bacteroides melaninogenicus.

Methicillin-resistant staphylococci are resistant to cephalosporins, incl. to ceftriaxone, many Streptococcus strains of group D and enterococci, incl. Enterococcus faecalis, also resistant to ceftriaxone.

Pharmacokinetics:Bioavailability is 100%, the time to reach the maximum concentration after intramuscular injection is 2-3 hours, after intravenous administration - at the end of the infusion. The maximum concentration after intramuscular injection at doses of 0.5 and 1 g is 38 and 76 μg / ml, respectively. The maximum concentration after intravenous administration in doses of 0.5, 1 and 2g-82, 151 and 257 μg / ml, respectively. Well penetrates into the cerebrospinal fluid with inflammation of the meninges.In adults, 2-24 hours after administration at a dose of 50 mg / kg, the concentration in the cerebrospinal fluid is many times greater than the minimal inhibitory concentration for the most common pathogens of meningitis. The plasma protein binding is 83-96%. The volume of distribution - 0.12-0.14 l / kg (5.78-13.5 l), in children - 0.3 l / kg, plasma clearance - 0.58-1.45 l / h, renal - 0.32-0.73 l / h.

The half-life (T1 / 2) after intramuscular injection is 5.8-8.7 hours, after intravenous administration at a dose of 50-75 mg / kg in children with meningitis - 4.3-4.6 hours; in patients who are on hemodialysis, with the clearance of creatinine (CC) 0-5 ml / min -14.7 h, with KK 5-15 ml / min - 15.7 h, with KK 16-30 ml / min - 11.4 h, with KK 31 -60 ml / min - 12.4 h. It is excreted unchanged - 33-67% by the kidneys; 40-50% - with bile in the intestine, where the inactivation occurs. About 70% of the drug is excreted through the kidneys in newborn infants. Hemodialysis is ineffective.

Indications:Infectious-inflammatory diseases caused by microorganisms sensitive to ceftriaxone: infections of the abdominal cavity organs (peritonitis, inflammatory diseases of the digestive tract, bile ducts, including cholangitis, empyema of the gallbladder), pelvic infection, lower respiratory tract infection (incl. h. pneumonia, lung abscess, pleural empyema), acute otitis media, infections of bones and joints, skin and soft tissues (incl.infected wounds and burns), urinary tract infections (complicated and uncomplicated), uncomplicated gonorrhea, bacterial meningitis, bacterial septicemia, Lyme disease. Prevention of postoperative infections. Infectious diseases in persons with weakened immunity.

Contraindications:Hypersensitivity (including to other cephalosporins, penicillins, carbapenems), hyperbilirubinemia in newborns, newborns, which showed intravenous administration of solutions containing calcium, lactation.

Carefully:Premature infants, renal and / or hepatic insufficiency, ulcerative colitis, enteritis or colitis associated with the use of antibacterial drugs, pregnancy.

Pregnancy and lactation:

Dosing and Administration:

The drug is used intramuscularly and intravenously (drip and jet). Do not use calcium-containing solutions to dilute the preparation! In adults, the daily dose, depending on the type and severity of the infection, is 1-2 g once a day or divided into 2 doses (every 12 hours), the total daily dose should not exceed 4 g.

Lyme disease: adults and children - 50 mg / kg (but not more than 2 g) 1 time per day for 14 days. With uncomplicated gonorrhea - 250 mg intramuscularly once.

For the prevention of postoperative complications - once 1 g for 30-60 minutes before the operation. In operations on the colon and rectum, additional administration of a drug from the 5-nitroimidazole group is recommended. The dose for newborns is 20-50 mg / kg / day.

For the treatment of skin and soft tissue infections, the recommended daily intake in children is 50-75 mg / kg divided into 2 divided doses (every 12 hours). The total daily intake for children should not exceed 2 g.

For bacterial meningitis in children, the initial dose is 100 mg / kg (but not more than 4 g) once a day, then 100 mg / kg / day (but not more than 4 g) once a day or divided into 2 doses (every 12 hours). The duration of treatment is 7-14 days.

In the treatment of acute otitis media in children, a single IV IM is recommended in a dose of 50 mg / kg (but not more than 1 g).

In the treatment of other infections in children, the recommended daily dose is 50-75 mg / kg, divided into 2 divided doses (every 12 hours). The total daily intake for children should not exceed 2 g.

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.

In chronic renal failure (creatinine clearance less than 10 ml / min), the daily dose should not exceed 2 g; patients on hemodialysis do not require an additional dose after a hemodialysis session, however, it is necessary to control the concentration of ceftriaxone in the plasma, since its excretion in such patients can be slowed down (dose adjustment may be required).

In patients with renal-hepatic insufficiency, the daily dose should not exceed 2 g without determining the concentration of the drug in the blood plasma.

Treatment with ceftriaxone should continue for at least 2 more days after the disappearance of symptoms and signs of infection. The course of treatment is usually 4-14 days; with complicated infections, a longer duration of administration may be required. The course of treatment for infections caused by Streptococcus pyogenes should be at least 10 days.

Rules for the preparation and administration of solutions: use only freshly prepared solutions. For intramuscular administration, 1 g of the drug is dissolved in 3.5 ml of a 1% solution of lidocaine. Recommend to enter no more than 1 g in one muscle. 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 calcium (0.9% sodium chloride solution, 5-10% dextrose solution, 5% levulose solution). Doses of 50 mg / kg or more should be administered intravenously drip, for 30 minutes.

Side effects:

Allergic reactions: rash, itching, fever, or chills.

From the nervous system: headache, dizziness.

From the digestive system: diarrhea, nausea, vomiting, taste disorder, pseudomembranous colitis.

From the hematopoiesis: anemia (including hemolytic), leukopenia, lymphopenia, neutropenia, thrombocytopenia, thrombocytosis, eosinophilia.

From the genitourinary system: candidiasis of the vagina, vaginitis.

Local reactions: with intravenous injection - phlebitis, soreness, tightening along the veins; intramuscular injection - soreness, sensation of warmth, tightness, or condensation at the injection site.

Laboratory indicators: increase (decrease) prothrombin time, increased activity of "liver" transaminases and alkaline phosphatase, hyperbilirubinemia, hypercreatininemia, increased urea concentration, the presence of sediment in the urine.

Other: increased sweating, "hot flashes" of blood.

Undesirable reactions with a frequency of less than 0.1%: abdominal pain, agranulocytosis, allergic pneumonitis, anaphylaxis, basophilia, cholelithiasis, bronchospasm, colitis, dyspepsia, epistaxis, bloating, "sluggish phenomenon" of the gallbladder, glucosuria, hematuria, jaundice, leukocytosis, lymphocytosis, monocytosis, nephrolithiasis, palpitation , convulsions, serum sickness.

Post-marketing experience: stomatitis, glossitis, oliguria, rash, allergic dermatitis, urticaria, edema, erythema multiforme, Stevens-Johnson syndrome, Lyell's syndrome.

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. There is no specific antidote.

Interaction:

Bacteriostatic antibiotics reduce the bactericidal effect of ceftriaxone. Antagonism with chloramphenicol in vitro.

Pharmaceutically incompatible with solutions containing calcium (including Hartman and Ringer's solution), as well as with amsacrine, vancomycin, fluconazole and aminoglycosides.

It does not contain N-metiltiotetrazolnoy group, therefore the interaction with ethanol did not lead to the development disulfiramopodobnyh reactions inherent in some cephalosporins.

Special instructions:

When concomitant severe renal and hepatic failure, as well as in patients on hemodialysis, should be regularly to determine the concentration of drug in plasma.

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 (precipitates of the calcium salt of ceftriaxone) are observed, which disappear after the cessation of treatment. With the development of the symptoms or signs indicating the possible gallbladder disease, or in the presence of ultrasound signs "sludge phenomenon" is recommended to stop administering the drug.

When using the drug, rare cases of pancreatitis, which developed, possibly, as a result of obstruction of the biliary tract, are described. Most patients had risk factors for congestion of the biliary tract (previous drug therapy, severe co-morbidities,completely parenteral nutrition); However, the starting role of precipitate formation in the biliary tract under the influence of ceftriaxone can not be ruled out. Ceftriaxone does not contain an N-methylthiotetrazol group, which causes disulfiram-like effects with simultaneous use of ethanol and bleeding, which are inherent some

cephalosporins.

When pregnancy is used only if the intended benefit for the mother exceeds the risk to the fetus. If it is necessary to prescribe the drug during lactation, breastfeeding should be stopped.

When using the drug, rare cases of prothrombin time change are described. Patients with vitamin K deficiency (impaired synthesis, eating disorders) may need to monitor prothrombin time and prescribe vitamin K (10 mg / week) with an increase in prothrombin time before or during therapy. Cases of fatal reactions as a result of deposition of ceftriaxone-calcium precipitates in the lungs and kidneys of newborns are described. Theoretically there is a probability of interaction of ceftriaxone with calcium-containing solutions for intravenous administration and in other age groups of patients, therefore ceftriaxone should not be mixed with calcium-containing solutions (including for parenteral nutrition), and also injected simultaneously, incl. through separate accesses for infusions at different sites. Theoretically, based on the calculation of 5 T1 / 2 ceftriaxone interval between the administration of ceftriaxone and calcium-containing solutions should be at least 48 hours. Data on the possible interaction of ceftriaxone with oral calcium-containing drugs, as well as ceftriaxone for intramuscular injection with calcium-containing drugs (intravenous and oral) are absent . In the treatment of ceftriaxone, false-positive results of Coombs test, a test for galactosemia, glucose in urine (glucosuria is recommended to be determined only by enzyme method).

Effect on the ability to drive transp. cf. and fur:Given the likelihood of side effects from the central nervous system, care should be taken when driving vehicles and working with mechanisms.

Form release / dosage:

Powder for solution for intravenous and intramuscular injection, 1.0 g.

Packaging:

By 1.0 g in a bottle of 15 ml of clear glass, sealed with a gray plug of butyl rubber, crimped aluminum ring with a plastic cover to control the first opening.

1 bottle with instructions for use in a cardboard box. 10 vials with instructions for use in a cardboard box.

Storage conditions:In a dry, protected from light place at a temperature of no higher than 25 ° C. Keep out of the reach of children.

Shelf life:

3 years. Do not use after the expiration date.

Terms of leave from pharmacies:On prescription

Registration number:LSR-008335/10

Date of registration:18.08.2010

The owner of the registration certificate:Danson Trading Pharmaceutical Company LimitedDanson Trading Pharmaceutical Company Limited Vietnam

Manufacturer: & nbsp

Fujian Fukang Pharmaceutical, Co.Ltd China

Representation: & nbspDominanta-Service CJSCDominanta-Service CJSC

Information update date: & nbsp19.11.2015

Illustrated instructions

Instructions

Ceftriaxone Danson (Ceftriaxone DanhSon)