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

Cephalosporin antibiotic III generation, 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. Active in relation to:

- Gram-positive aerobes - Staphylococcus aureus (including strains producing penicillinase), Staphylococcus epidermidis, Streptococcus pneumoniae,Streptococcus pyogenes, Streptococcus spp. groups viridans;

- gram-negative aerobes - Acinetobacter calcoaceticus, Borrelia burgdorferi, Enterobacter aerogenes, Enterobacter cloacae, Escherichia coli, Haemophilus influenzae (including strains that form penicillinase), Haemophilus parainfluenzae, Klebsiella spp. (incl. Klebsiella pneumoniae), Moraxella catarrhalis (including strains forming penicillinase), Morganella morganii, Neisseria gonorrhoeae (including strains that form penicillinase), Neisseria meningitidis, Proteus mirabilis, Proteus vulgaris, Serratia spp. (incl. Serratia marcescens); individual strains Pseudomonas aeruginosa are also sensitive;

- anaerobes - Bacteroides fragilis, Clostridium spp. (Besides Clostridium difficile), Peptostreptococcus spp.

It 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, in, for example. 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 in the plasma (TCmax) after intramuscular (IM) administration is 2-3 hours, after intravenous (IV) administration - at the end of the infusion.

The maximum concentration (Cmax) after the / m introduction is 76 mcg / ml. Stach at IV in doses of 1 and 2 g-151 and 257 μg / ml, respectively.

In adults, 2-24 hours after the administration of a dose of 50 mg / kg, the concentration in the cerebrospinal fluid (CSF)minimum inhibitory concentration for the most common pathogens of meningitis. It penetrates well into CSF with inflammation of the meninges.

The connection with plasma proteins 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 period (T1 / 2) after IM was 5.8-8.7 hours after IV injection at a dose of 50-75 mg / kg in children with meningitis - 4.3-4.6 hours; in patients on hemodialysis (creatinine clearance 0-5 ml / min), -14.7 hours, with SC 15-15 ml / min - 15.7 hours, 16-30 ml / min - 11.4 h, 31-60ml / min-12.4h.

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 susceptible to ceftriaxone

microorganisms:

- infections of the abdominal cavity (peritonitis, inflammatory diseases of the gastrointestinal tract, bile ducts, including cholangitis, empyema of the gallbladder);

- Diseases of the respiratory tract (including pneumonia, lung abscess, pleural empyema);

- acute otitis media;

- bacterial meningitis;

- uncomplicated gonorrhea;

- urinary tract infections;

- infections of the skin and soft tissues;

- infection of bones, joints;

- infections of the pelvic organs;

- bacterial septicemia;

- Lyme disease (borreliosis).

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 calcium-containing solutions.

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

Pregnancy and lactation:Ceftriaxone can be used during pregnancy if the intended benefit to the mother is greater than the potential risk to the fetus. If it is necessary to prescribe the drug during lactation, breastfeeding should be stopped.

Dosing and Administration:

In / in, / m. Use only freshly prepared solutions! Do not use calcium-containing solutions to dilute the preparation!

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

In children with a body weight of 50 kg and above, doses for adults are used. The length of the course depends on the nature and severity of the disease. With uncomplicated gonorrhea - in / m once, 250 mg.

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

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 the drug from the group of 5-nitroimidazoles is recommended.

For newborns - 20-50 mg / kg / day.

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 h) or can be reduced. The duration of treatment is 7-14 days. Children with skin and soft tissue infections - in a daily dose of 50-75 mg / kg once a day or 25-37.5 mg / kg every 12 hours, not more than 2 g / day.

In severe infections of other locations, 25-37.5 mg / kg every 12 hours, not more than 2 g / day. 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).

When treating others.infections in children older than 1 month and up to 12 years of age, the recommended daily dose is 50-75 mg / kg, divided into two doses (every 12 hours). The total daily dose in children should not exceed 2 g. A dose of more than 50 mg / kg of body weight should be given as an IV infusion within 30 minutes.

Patients with chronic renal insufficiency correction of the dose is required only with QC below 10 ml / min. In this case, 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-liver failure, 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 the / m introduction, 0.5 g of the drug is dissolved in 2 ml, and 1 g - in 3.5 ml of a 1% solution of lidocaine. Recommend to enter no more than 1 g in one buttock.

For intravenous injection of 0.5 g, dissolved in 5 ml, alg-in 10 ml of water for injection. Enter into / in slowly (2-4 minutes).

For intravenous infusions dissolve 2 g in 40 ml of a solution that does not contain calcium (0.9% sodium chloride solution, 5-10% dextrose solution, 5% solution of levulose). 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: when in / in the introduction - phlebitis, soreness, seals along the vein; with the / m introduction - soreness, sensation of warmth, tightness or condensation at the injection site.

Laboratory indicators: increase (decrease) prothrombin time, increased activity, "liver" transaminases and alkaline phosphatase, hyperbilirubinemia,hyperkreatininemia, 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, "sludge phenomenon" of the gallbladder, glucosuria, hematuria, jaundice, leukocytosis. lymphocytosis, monocytosis, nephrolithiasis,

heart palpitations, seizures, serum sickness, stomatitis, glossitis, oliguria, 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.

Special instructions:

With simultaneous severe renal and hepatic insufficiency, hemodialysis patients should regularly determine the concentration of the drug in the 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 symptoms or signs indicating a possible gallbladder disease, or if there are signs of a "sluggish phenomenon", it is recommended that the drug be discontinued.

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-methylthio-tetrazole group,which causes disulfiramoid-like effects with the simultaneous use of ethanol and bleeding, which are inherent in some cephalosporins.

When using the drug, rare cases of prothrombin time change are described. 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 (Yumg / 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 administered simultaneously, incl. through separate accesses for infusions at different sites. Theoretically, based on the calculation of 5 half-lives of ceftriaxone, the interval between the administration of ceftriaxone and calcium-containing solutions should be at least 48 hours.

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:Patients using ceftriaxone, care should be taken when driving a car and engaging in other potentially hazardous activities requiring increased attention and speed of psychomotor reactions.

Form release / dosage:

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

Packaging:By 1.0 g of active substance (ceftriaxone) in a glass vial, hermetically sealed with a rubber stopper, followed by an aluminum cap. 1 bottle with instructions for use in a pack of cardboard. For 5 or 30 bottles with instructions for use in a cardboard box.

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

Shelf life:2 years. Do not use after the expiration date printed on the package.

Terms of leave from pharmacies:On prescription

Registration number:LS-000140

Date of registration:23.12.2009

The owner of the registration certificate:LEKKO, ZAO LEKKO, ZAO Russia

Manufacturer: & nbsp

Pharmaceutical firm LEKKO, ZAO Russia

Information update date: & nbsp21.11.2015

Illustrated instructions

Instructions

Ceftriaxone (Ceftriaxone)