Ceftriaxone Kabi - 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, Enterobacter aerogenes, Enterobacter cloacae, Escherichia coli, Haemophilus influenzae (including strains forming penicillinase), Haemophilus parainfluenzae, Klebsiella spp. (including Klebsiella pneumoniae), Moraxella catarrhalis, (including penicillinase-producing strains), Morganella morganii, Neisseria gonorrhoeae (including strains forming penicillinase), Neisseria meningitidis, Proteus mirabilis, Proteus vulgaris, Serratia spp. (including Serratia marcescens), Borrelia burgdorferi; individual strains of Pseudomonas aeruginosa are also sensitive; anaerobes: Bacteroides fragilis, Clostridium spp. (except 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 .; 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 injection. The maximum concentration after intramuscular injection at doses of 0.5 and 1 g is about 38 and 76 μg / ml, respectively. Maximum concentration for intravenous administration in doses of 0.5; 1 and 2 g - an average of 82, 151 and 257 μg / ml, respectively. In adults, 2-24 hours after dosing50 mg / kg concentration in the cerebrospinal fluid (CSF) many times exceeds the minimum inhibitory concentration (MIC) 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%. Volume 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 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 on hemodialysis (creatinine clearance 0-5 ml / min), -14.7 hours, with creatinine clearance of 5-15 ml / min - 15.7 hours, 16-30 ml / min - 11, 4 hours, 31-60 ml / min-12.4 hours.

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 and inflammatory diseases caused by microorganisms susceptible to ceftriaxone: infections of the abdominal cavity (peritonitis, inflammatory diseases of the gastrointestinal tract (GIT), bile ducts including cholangitis, gallbladder empyema), pelvic infection, lower respiratory infection ways (incl.pneumonia, lung abscess, pleural empyema), acute otitis media, infections of bones and joints, skin and soft tissues (including infected wounds and burns), urinary tract infections (complicated and uncomplicated), uncomplicated gonorrhea, bacterial meningitis, 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, who are shown intravenous administration of solutions containing calcium; lactation period.

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

Pregnancy and lactation:In pregnancy, the drug is used only if the intended benefit to the mother exceeds the potential risk to the fetus. When applying the drug, breast-feeding should be discontinued.

Dosing and Administration:

Intravenous (drip and jet) and intramuscularly.Do not use calcium-containing solutions for breeding!

Adults and children over 12 years of age - 1-2 grams once a day or 0.5-1 g every 12 hours, the total daily dose should not exceed 4 g. The dose for newborns is 20-50 mg / kg / day.

For infants and children under 12, the maximum daily dose is 50-75 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. Lyme disease: adults and children - 50 mg / kg (but not more than 2 g) 1 time per day for 14 days.

With uncomplicated gonorrhea - intramuscularly once 250 mg. For prophylaxis of postoperative complications - once 1g 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 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 divided doses 12 hours) or can be reduced. The duration of treatment is 7-14 days.

For children with skin and soft tissue infections, the recommended daily dose is 50-75 mg / kg once daily or 25-37.5 mg / kg every 12 hours.In severe infections of other localization, 25-37.5 mg / kg every 12 hours. The maximum daily dose for children should not exceed 2 g.

When treating acute otitis media in children - intramuscularly, once, 50 mg / kg, not more than 1 g.

Patients with chronic renal insufficiency (CRF) dose adjustment is required only with creatinine clearance (CC) 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 may be slowed down (dose correction 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 may require a longer introduction. 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 injection, 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 muscle.

For intravenous injection, 0.5 g is dissolved in 5 ml, a1 g-10 ml of water for injection. Enter intravenously 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% 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.

Local reactions: at intravenous introduction - phlebitis, soreness on a course of a vein; intramuscular injection - soreness, sensation of warmth, tightness or condensation at the injection site.

Co side of the central nervous system: headache, dizziness.

On the part of the reproductive system: candidiasis of the vagina, vaginitis.

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

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

Laboratory indicators: increase (decrease) in prothrombin time, hematuria, increased activity of "hepatic" transaminases and alkaline phosphatase (ALF), 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, hypersensitivity pneumonitis, anaphylaxis, basophils, cholelithiasis, bronchospasm, colitis, dyspepsia, nasal bleeding, bloating, "sladzh- phenomenon" of the gallbladder, glycosuria, hematuria, jaundice, leukocytosis, lymphocytosis, monocytosis / nephrolithiasis, 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.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, as well as in patients on hemodialysis, the concentration of the drug in 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, gallbladder marked darkening (precipitates the calcium salt of ceftriaxone) by ultrasound (US), which disappear after cessation of treatment. With the development of symptoms or signs indicating a possible gallbladder disease, or if there are ultrasound signs of a "slang phenomenon," it is recommended that the drug be discontinued. When the drug is used, rare cases of pancreatitis, which has developed, possibly due to obstruction of the biliary tract (previous drug therapy, severe co-morbidities, completely parenteral nutrition) are described;However, the starting role of precipitate formation in the biliary tract under the influence of ceftriaxone can not be ruled out.

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.

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 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 administration of 500 mg, 1000 mg, 2000 mg.

Packaging:

For 500 mg of active substance in a 15 ml glass injection vial, capped with a rubber stopper and an aluminum cap with a plastic cover to control the first opening. 1 or 10 vials together with the instruction for use are placed in a cardboard pack.

For 1000 mg of active substance in a 15 ml glass injection vial, capped with a rubber stopper and an aluminum cap with a plastic cover to control the first opening.1 or 10 vials together with the instruction for use are placed in a cardboard pack.

For 2000 mg of active substance in a 15 ml glass injection bottle capped with a rubber stopper and an aluminum cap with a plastic cover to control the first opening. 1 or 10 vials together with the instruction for use are placed in a cardboard pack.

Storage conditions:At a temperature of no higher than 25 ° C in a dark place. Keep out of the reach of children.

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

Terms of leave from pharmacies:On prescription

Registration number:LP-000047

Date of registration:22.11.2010

Date of cancellation:2015-11-22

The owner of the registration certificate:Fresenius Kabi Deutschland GmbHFresenius Kabi Deutschland GmbH Germany

Manufacturer: & nbsp

LABESFAL-LABORATORIOS ALMIRO, S.A. Portugal

Representation: & nbspFRESENIUS KABI DEYCHLAND GmbH FRESENIUS KABI DEYCHLAND GmbH Germany

Information update date: & nbsp18.11.2015

Illustrated instructions

Instructions

Ceftriaxone Kabi (Ceftriaxone Kabi)