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: infections of the abdominal organs (peritonitis, inflammatory diseases of the gastrointestinal tract (GIT) of the biliary tract, including cholangitis, empyema of the gallbladder), infections of the pelvic organs, infections of the lower respiratory tract (including pneumonia, lung abscess, empyema of the pleura), infections of bones and joints, skin and soft tissues (including 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 people with weakened immune systems.

Pharmacological effect

Pharmacotherapeutic group: Antibiotic-cephalosporin

ATX code: J01DD04

Pharmacodynamics:

Broad-spectrum cephalosporin antibiotic of the third generation for parenteral administration. Bactericidal activity is due to the suppression of bacterial cell wall synthesis. It is resistant to the 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 groups; gram-negative aerobes: 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 penicillinase-producing strains) Morganella morganii Neisseria gonorrhoeae (including penicillinase-producing strains) Neisseria meningitidis Proteus mirabilis Proteus vulgaris Serratia spp. (including Serratia marcescens) Borrelia burgdorferi; certain strains of Pseudomonas aeruginosa are also susceptible; 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 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. to ceftriaxone, many strains of group D streptococci and enterococci, including Enterococcus faecalis is also resistant to ceftriaxone.

Pharmacokinetics:

Bioavailability – 100% time to reach maximum concentration after intravenous administration – at the end of the infusion. The maximum concentration at a dose of 2 g 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 inhibitory concentration (MIC) for the most common pathogens of meningitis. Penetrates well into the CSF during inflammation of the meninges. Communication with plasma proteins is 83-96%. Volume of distribution – 012-014 l/kg (578-135 l) in children – 03 l/kg plasma clearance – 058-145 l/h renal 032-073 l/h.

Special instructions

In case of simultaneous severe renal and liver failure, 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 peripheral blood picture and indicators of the functional state of the liver and kidneys. In rare cases, during ultrasound examination of the gallbladder, darkening (precipitates of ceftriaxone calcium salt) is observed, which disappear after cessation of treatment. If symptoms or signs indicating a possible gallbladder disease develop or if there are ultrasound signs of a “slung phenomenon,” it is recommended to stop administering the drug.

When using the drug, rare cases of pancreatitis that developed possibly due to obstruction of the biliary tract have been described (previous drug therapy with severe concomitant diseases, complete parenteral nutrition), while the triggering role of the formation of precipitates in the biliary tract under the influence of ceftriaxone cannot be excluded.

Does not contain an N-methylthiotetrazole group, which causes disulfiram-like effects with simultaneous use of ethanol and bleeding that is inherent in some cephalosporins.

Rare cases of changes in prothrombin time have been described when using the drug.

Patients with vitamin K deficiency (impaired synthesis, malnutrition) may require monitoring of prothrombin time and administration of vitamin K (10 mg/week) with an increase in prothrombin time before or during therapy.

Cases of fatal reactions resulting from the deposition 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 in other age groups of patients; therefore, ceftriaxone should not be mixed with calcium-containing solutions (including for parenteral nutrition) and should not be administered simultaneously, incl. through separate access 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. When treating 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 the enzyme method).

Impact on the ability to drive vehicles. Wed and fur.:
Patients using ceftriaxone should be careful when driving a car and engaging in other potentially hazardous activities that require increased attention and speed of psychomotor reactions.

Active ingredient

Ceftriaxone

Composition

1 bottle contains:

Ceftriaxone sodium trisesquihydrate 1193 mg, (equivalent to ceftriaxone) 1000 mg.

Pregnancy

During pregnancy, the drug is used only if the expected benefit to the mother outweighs the potential risk to the fetus. When using the drug, breastfeeding should be stopped.

Contraindications

Hypersensitivity (including to other cephalosporins, penicillins, carbapenems); hyperbilirubinemia in newborns; newborns who are indicated for intravenous administration of solutions containing calcium; lactation period.
With caution:
Premature children, renal and/or liver failure, ulcerative colitis, enteritis or colitis associated with the use of antibacterial drugs.

Side Effects

Allergic reactions: rash, itching, fever or chills.

Local reactions: with intravenous administration – phlebitis, pain along the vein.

From the central nervous system: headache, dizziness.

From the reproductive system: vaginal candidiasis, vaginitis.

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

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

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

Other: increased sweating, flushes of blood.

Adverse reactions with a frequency of less than 01%: 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 palpitations cramps serum sickness stomatitis glossitis oliguria allergic dermatitis urticaria edema erythema multiforme Stevens-Johnson syndrome Lyell’s syndrome.

Interaction

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

Overdose

Excessively high plasma concentrations of ceftriaxone cannot be lowered by hemodialysis or peritoneal dialysis. Symptomatic measures are recommended to treat cases of overdose. There is no specific antidote.

Storage conditions

At a temperature not exceeding 25 ° C in a place protected from light. Keep out of the reach of children.

Shelf life

3 years. Do not use after the expiration date indicated on the package.

Manufacturer

Labesfal Laboratorios Almiro S.A, Portugal