Ceftriaxone Kabi, 1 g 10 pcs

Pharmacotherapeutic group: Antibiotic-cephalosporin

ATC code: J01DD04

Pharmacodynamics:

A broad spectrum III generation cephalosporin antibiotic for parenteral administration. Bactericidal activity is caused by inhibition of bacterial cell wall synthesis. It is characterized by resistance to action of most beta-lactamases of gram-negative and gram-positive microorganisms.

Active against the following microorganisms: Gram-positive aerobes -Staphylococcus aureus (including strains producing penicillinase) Staphylococcus epidermidis Streptococcus pneumoniae Streptococcus pyogenes Streptococcus spp. viridans; Gram-negative aerobes: Acinetobacter calcoaceticus Enterobacter aerogenes Enterobacter cloacae Escherichia coli Haemophilus influenzae (including penicillinase-producing strains) Haemophilus parainfluenzae Klebsiella spp. Klebsiella pneumoniae) Moraxella catarrhalis (including penicillinase-producing strains) Morganella morganii Neisseria gonorrhoeae (including penicillinase-producing strains) Neisseria meningitidis Proteus mirabilis Proteus vulgaris Serratia spp. (including Serratia marcescens) Borrelia burgdorferi; some 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. Providencia rettgeri Salmonella spp. (including Salmonella typhi) Shigella spp.; Streptococcus agalactiae Bacteroides bivius Bacteroides melaninogenicus.

Methicillin resistant staphylococci are also resistant to cephalosporins including ceftriaxone many strains of group D streptococci and enterocococci including enterocococci.Enterococcus faecalis are also resistant to ceftriaxone.

Pharmacokinetics:

Bioavailability – 100% time of reaching maximum concentration after intravenous administration – at the end of infusion. Maximal concentration in 2 g dose is about 257 mcg/ml. In adults, 2-24 hours after administration at a dose of 50 mg/kg, the concentration in the cerebrospinal fluid (CSF) is many times higher than the minimum suppressive concentration (MSC) for the most common meningitis pathogens. It penetrates well into the CSF during cerebral membrane inflammation. Binding with plasma proteins is 83-96 %. Distribution volume – 012-014 l/kg (578-135 l) in children – 03 l/kg plasma clearance – 058-145 l/h renal 032-073 l/h.

Indications

Infectious and inflammatory diseases caused by microorganisms sensitive to ceftriaxone: abdominal infections (peritonitis inflammatory diseases of the gastrointestinal tract (GIT) biliary tract including cholangitis empyema of the gallbladder) pelvic infections infections of the lower respiratory tract (including pneumonia lung abscess empyema of the pleura)Bone and joint infections of the skin and soft tissues (including infected wounds and burns) Urinary tract infections (complicated and uncomplicated) Bacterial meningitis Bacterial septicemia Lyme disease (Borreliosis).

Prevention of postoperative infections. Infectious diseases in immunocompromised people.

Active ingredient

Ceftriaxone

Composition

1 vial contains:
Ceftriaxone sodium trisecquihydrate 1193 mg, (corresponding to ceftriaxone) 1000 mg.

How to take, the dosage

Intravenously by infusion. Do not use calcium-containing solutions for dilution!

Adults and children over 12 years old – 1-2 g once a day or 05-1 g every 12 hours total daily dose should not exceed 4 g.

Dosage for infants – 20-50 mg/kg/day. For infants and children under 12 years old the maximum daily dose is 50-75 mg/kg. In children with body weight 50 kg and more we use doses for adults.

Doses over 50 mg/kg of body weight should be administered as an intravenous infusion for 30 minutes. The duration of the course depends on the nature and severity of the disease. Lyme disease: For adults and children – 50 mg/kg (but not more than 2 g) once a day during 14 days.

For prevention of postoperative complications – once 1 g 30-60 minutes before the operation. For operations on the colon and rectum additional administration of 5-nitroimidazole group is recommended. In case of bacterial meningitis in children the initial dose is 100 mg/kg (but not more than 4 g) once a day and further 100 mg/kg/day (but not more than 4 g) once a day or divided into 2 doses (every 12 hours) or it can be reduced. The duration of treatment is 7-14 days.

In children with skin and soft tissue infections the recommended daily dose is 50-75 mg/kg once daily or 25-375 mg/kg every 12 hours. In severe infections of other localizations – 25-375 mg/kg every 12 hours. Maximal daily dose in children should not exceed 2 g.

In patients with chronic renal insufficiency (ChRI) a dose adjustment is required only in creatinine clearance (CK) less than 10 ml/min. In this case, the daily dose should not exceed 2 g. Patients on hemodialysis do not require additional dose administration after hemodialysis session, however, it is necessary to monitor ceftriaxone concentration in plasma as its excretion in these patients may be delayed (dose adjustment may be required).

In patients with renal-hepatic insufficiency daily dose should not exceed 2 g without plasma concentration determination. Treatment with ceftriaxone should be continued for at least 2 more days after symptoms and signs of infection have disappeared. The course of treatment is usually 4-14 days for complicated infections that may require longer administration. The course of treatment for infections caused by Streptococcus pyogenes should be at least 10 days.

Rules for preparation and administration of solutions: only freshly prepared solutions should be used. For intravenous infusions 2 g are dissolved in 40 ml of calcium-free solution (09% sodium chloride solution 5-10% dextrose solution 5% levulose solution).

Interaction

Bacteriostatic antibiotics reduce the bactericidal effect of ceftriaxone. Pharmaceutically incompatible with solutions containing calcium (including Hartmann’s and Ringer’s solutions) as well as with amsacrine vancomycin fluconazole and aminoglycosides.

Special Instructions

In concurrent severe renal and hepatic insufficiency and in patients on hemodialysis the drug concentration in plasma should be regularly determined.

During long-term treatment it is necessary to regularly monitor the peripheral blood picture indicators of liver and kidney functional state. In rare cases an ultrasound investigation (ultrasound) of gall bladder may show darkening (precipitates of calcium salt of ceftriaxone), which disappear after discontinuation of treatment. In case of development of symptoms or signs indicating possible gallbladder disease or in the presence of ultrasound signs of “slange phenomenon” it is recommended to stop the drug administration.

Rare cases of pancreatitis have been described during the drug administration. It may have been caused by biliary obstruction (prior therapy with the drug – severe concomitant diseases, parenteral nutrition). At the same time the triggering role of biliary precipitate formation caused by ceftriaxone cannot be excluded.

It does not contain N-methylthiotetrazole group which causes disulfiram-like effects upon simultaneous use of ethanol and hemorrhage characteristic of some cephalosporins.

Rare cases of changes in prothrombin time have been described during the use of the drug.

Patients with vitamin K deficiency (synthesis disorder) may require control of prothrombin time and administration of vitamin K (10 mg/week) if prothrombin time increases before or during therapy.

Cases of fatal reactions due to deposits of ceftriaxone-calcium precipitates in the lungs and kidneys of newborns have been described. Theoretically there is a possibility of interaction of ceftriaxone with calcium-containing solutions for intravenous administration and in other age groups of patients, so ceftriaxone should not be mixed with calcium-containing solutions (including for parenteral nutrition) and also administered simultaneously, including through separate accesses for infusion 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. During treatment with ceftriaxone false-positive results of the Coombs test for galactosemia may be observed when determining glucose in the urine (glucosuria is recommended to be determined only by enzymatic method).
Influence on the ability to drive trans. patients using ceftriaxone should exercise caution when driving a car and engaging in other potentially dangerous activities that require increased attention and rapid psychomotor reactions.