Ceftriaxone solution 1g, 1pc – Krasnopharma

Composition

One bottle contains 1.0 g of Ceftriaxone sodium salt.

Pharmacological action

Ceftriaxone is a third-generation cephalosporin antibiotic for parenteral use, has a bactericidal effect, inhibits cell membrane synthesis, and in vitro suppresses the growth of most Gram-positive and Gram-negative microorganisms. Ceftriaxone is resistant to beta-lactamase enzymes (both penicillinase and cephalosporinase, produced by most Gram-positive and Gram-negative bacteria). In vitro and in clinical practice, ceftriaxone is usually effective against the following microorganisms: :  

Gram-positive results:  Staphylococcus aureus, Staphylococcus epidermidis, Streptococcus pneumoniae, Streptococcus A (Str. pyogenes), Streptococcus V (Str. agalactiae), Streptococcus viridans, Streptococcus bovis.

Note:  Methicillin-resistant Staphylococcus spp. is also resistant to cephalosporins, including ceftriaxone. Most enterococcal strains (such as Streptococcus faecalis) are also resistant to ceftriaxone.

Gram-negative numbers:  Aeromonas spp., Alcaligenes spp., Branhamella catarrhalis, Citrobacter spp., Enterobacter spp. (some strains are resistant), Escherichia coli, Haemophilus ducreyi, Haemophilus influenzae, Haemophilus parainfluenzae, Klebsiella spp. (including Kl. pneumoniae), Moraxella spp., Morganella morganii, Neisseria gonorrhoeae, Neisseria meningitidis, Plesiomonas shigelloides, Proteus mirabilis, Proteus vulgaris, Providencia spp., Pseudomonas aeruginosa (some strains are resistant), Salmonella spp. (including S. typhi), Serratia spp. (including S. marcescens), Shigella spp., Vibrio spp. (including V. cholerae), Yersinia spp. (including Y. enterocolitica)

Note:  Many strains of these microorganisms that multiply steadily in the presence of other antibiotics, such as penicillins, first-generation cephalosporins, and aminoglycosides, are sensitive to ceftriaxone. Treponema pallidum is sensitive to ceftriaxone both in vitro and in animal experiments. According to clinical data, ceftriaxone is highly effective in primary and secondary syphilis.

Anaerobic pathogens:  Bacteroides spp. (including some strains of B. fragilis), Clostridium spp. (including CI. difficile), Fusobacterium spp. (except F. mostiferum. F. varium), Peptococcus spp., Peptostreptococcus spp.

Note:  Some strains of many Bacteroides spp. (e. g., B. fragilis) that produce beta-lactamase are resistant to ceftriaxone. To determine the sensitivity of microorganisms, it is necessary to use disks containing ceftriaxone, since it has been shown that certain strains of pathogens can be resistant to classical cephalosporins in vitro.

Pharmacokinetics:

When administered parenterally, ceftriaxone penetrates well into tissues and body fluids. In healthy adult subjects, ceftriaxone is characterized by a long half-life of about 8 hours. The areas under the concentration – time curve in blood serum during intravenous and intramuscular use coincide. This means that the bioavailability of ceftriaxone with intramuscular use is 100%. When administered intravenously, ceftriaxone quickly diffuses into the interstitial fluid, where it retains its bactericidal effect against pathogens sensitive to it for 24 hours.

The elimination half-life in healthy adult subjects is about 8 hours. In newborns under 8 days of age and in elderly people over 75 years of age, the average half-life is approximately twice as long. In adults,50-60% of ceftriaxone is excreted unchanged in the urine, and 40-50% is also excreted unchanged in the bile. Under the influence of the intestinal flora, ceftriaxone is converted to an inactive metabolite. In newborns, approximately 70% of the administered dose is excreted by the kidneys. With renal insufficiency or liver pathology in adults, the pharmacokinetics of ceftriaxone almost does not change, the elimination half-life is slightly extended. If the kidney function is impaired, bile excretion increases, and if there is a liver pathology, then the excretion of ceftriaxone by the kidneys increases.

Ceftriaxone reversibly binds to albumin and this binding is inversely proportional to the concentration: for example, at a serum concentration of less than 100 mg/l, the binding of ceftriaxone to proteins is 95%, and at a concentration of 300 mg/l-only 85%. Due to the lower albumin content in the interstitial fluid, the concentration of ceftriaxone in it is higher than in the blood serum.

Penetration into the cerebrospinal fluid: In newborns and children with inflammation of the meninges, ceftriaxone penetrates the cerebrospinal fluid, while in the case of bacterial meningitis, an average of 17% of the drug concentration in the blood serum diffuses into the cerebrospinal fluid, which is approximately 4 times more than in aseptic meningitis.

24 hours after intravenous use of ceftriaxone at a dose of 50-100 mg / kg of body weight, the concentration in the cerebrospinal fluid exceeds 1.4 mg/l. In adult meningitis patients,2-25 hours after use of ceftriaxone at a dose of 50 mg / kg of body weight, the concentration of ceftriaxone was many times higher than the minimum inhibitory dose required to suppress the pathogens that most often cause meningitis.

Indications

Infections caused by ceftriaxone-sensitive pathogens: sepsis, meningitis, abdominal infections (peritonitis, inflammatory diseases of the gastrointestinal tract, biliary tract), infections of bones, joints, connective tissue, skin, infections in patients with reduced immune system function, kidney and urinary tract infections, respiratory tract infections, especially pneumonia, as well as ear, throat and nose infections, genital infections, including gonorrhea.

Prevention of infections in the postoperative period.

Contraindications

Hypersensitivity to cephalosporins and penicillins. First trimester of pregnancy.

Side effects

Systemic side effects:

from the gastrointestinal tract (about 2% of patients): diarrhea, nausea, vomiting, stomatitis and glossitis.

Changes in the blood picture (about 2% of patients) in the form of eosinophilia, leukopenia, granulocytopenia, hemolytic anemia, thrombocytopenia.

Skin reactions (about 1% of patients) in the form of exanthema, allergic dermatitis, urticaria, edema, erythema multiforme.

Other rare side effects: headaches, dizziness, increased liver enzyme activity, gallbladder congestion, oliguria, increased serum creatinine, mycosis in the genital area, chills, anaphylaxis or anaphylactic reactions. Pseudomembranous enterocolitis and blood clotting disorders are extremely rare.

Local side effects:

Phlebitis has been reported in some cases after intravenous use.

This phenomenon can be prevented by slow (within 2-4 minutes) use of the drug. The described side effects usually disappear after discontinuation of therapy.

How to take, course of use and dosage

For adults and children over 12 years of age: The average daily dose is 1-2 g of ceftriaxone once a day (after 24 hours). In severe cases or in cases of infections caused by moderately sensitive pathogens, the single daily dose may be increased to 4 g.

For newborns, children and children under 12 years of age:  For a single daily dosage, the following scheme is recommended: :  For newborns (up to two weeks of age):  20-50 mg / kg of body weight per day (the dose of 50 mg/kg of body weight is not allowed to be exceeded due to the immature enzyme system of newborns).

For children and children under 12 years of age:  the daily dose is 20-75 mg / kg of body weight. In children with a body weight of 50 kg and above, the adult dosage should be followed. A dose greater than 50 mg / kg of body weight should be administered as an intravenous infusion for at least 30 minutes.

Duration of therapy:  depends on the course of the disease.

Combination therapy:

Experiments have shown that there is a synergistic effect on many Gram-negative bacteria between ceftriaxone and aminoglycosides. Although it is impossible to predict the potentiated effect of such combinations in advance, in cases of severe and life-threatening infections (for example, caused by Pseudomonas aeruginosa), their combined use is justified.

Due to the physical incompatibility of ceftriaxone and aminoglycosides, it is necessary to prescribe them separately at the recommended doses! 

Gonorrhea:  For the treatment of gonorrhea caused by both penicillinase-forming and non-forming strains, the recommended dose is 250 mg once intramuscularly.

Prevention in the pre-and postoperative period:  Before infected or suspected infected surgical procedures to prevent postoperative infections, depending on the risk of infection,30-90 minutes before surgery, a single use of ceftriaxone in a dose of 1-2 g is recommended.

Renal and hepatic insufficiency:  In patients with impaired renal function, if the liver function is normal, the dose of ceftriaxone should not be reduced. Only with preterminal renal insufficiency (creatinine clearance below 10 ml/min), it is necessary that the daily dose of ceftriaxone does not exceed 2 g.

In patients with impaired liver function, if renal function is maintained, the dose of ceftriaxone should also not be reduced.

In cases of simultaneous presence of severe liver and kidney pathology, the concentration of ceftriaxone in the blood serum should be regularly monitored.In patients undergoing hemodialysis, there is no need to change the dose of the drug after this procedure.

Intramuscular use: For intramuscular use,1 g of the drug should be diluted in 3.5 ml of 1% Lidocaine solution and injected deep into the gluteal muscle, it is recommended to inject no more than 1 g of the drug into one buttock. Lidocaine solution should never be administered intravenously!

Intravenous use: For intravenous injection,1 g of the drug should be diluted in 10 ml of sterile distilled water and administered intravenously slowly for 2-4 minutes.

The duration of intravenous infusion is at least 30 minutes. For intravenous infusion,2 g of powder should be diluted in approximately 40 ml of a calcium-free solution, for example: in 0.9% sodium chloride solution, in 5% glucose solution, in 10% glucose solution, in 5% levulose solution.

Overdose

Excessively high plasma concentrations of ceftriaxone cannot be reduced by hemodialysis or peritoneal dialysis.

Symptomatic measures are recommended to treat cases of overdose.

Special instructions

Despite a detailed medical history, which is the rule for other cephalosporin antibiotics, one cannot exclude the possibility of developing anaphylactic shock, which requires immediate therapy – first intravenous epinephrine is administered, then glucocorticoids.

Sometimes an ultrasound examination of the gallbladder shows the presence of a shadow indicating precipitation. This symptom disappears after the end or temporary discontinuation of ceftriaxone therapy. Even in the presence of pain, such cases do not require surgical intervention, and conservative treatment is sufficient.

In vitro studies have shown that, like other cephalosporin antibiotics, ceftriaxone is able to displace bilirubin bound to serum albumin. Therefore, in newborns with hyperbilirubinemia, and especially in premature newborns, the use of ceftriaxone requires even greater caution. Since the drug penetrates into breast milk, breast-feeding should not be continued during treatment with ceftriaxone.

With prolonged use, periodic monitoring of the blood formula is necessary. Ceftriaxone is used only in a hospital setting.

See expiration date. on the packaging.

Active ingredient

Ceftriaxone

Conditions of release from pharmacies

By prescription

Dosage form

solution for injection and infusion

Purpose

For adults as prescribed by a doctor, Pregnant women in the second and third trimester as prescribed by a doctor, Nursing mothers as prescribed by a doctor, Children as prescribed by a doctor

Indications

Biliary Tract Infections, Salmonellosis, Skin Infections, Infectious Diseases, Intestinal Infections, Bronchitis, Pneumonia, Urinary Tract Infections, Sinusitis, Osteomyelitis, Respiratory Tract Infections, Cholecystitis, Otitis