Universal reference book for medicines
Product name: MEDAXONE (MEDAXONE)

Active substance: ceftriaxone

Type: Third generation cephalosporin

Manufacturer: MEDOCHEMIE (Cyprus)
Composition, form of production and packaging
Powder for the preparation of solution for iv and in / m introduction
from white to white with a yellowish hue of color, slightly hygroscopic.

1 f.

ceftriaxone (in the form of a sodium salt) 500 mg

- "- 1 g

Vials (1) - cardboard boxes.

Vials (100) - cardboard boxes.

INSTRUCTION FOR THE SPECIALIST.

The description of the drug was approved by the manufacturer for the 2006 print edition.

PHARMACHOLOGIC EFFECT

Cephalosporin antibiotic III generation for parenteral use.
Has a bactericidal effect, inhibits the synthesis of the cell membrane, in vitro inhibits the growth of most gram-positive and gram-negative microorganisms. Ceftriaxone is resistant to the action of? -lactamases (both penicillinase and cephalosporinase, produced by most gram-positive and gram-negative bacteria).
The drug is active against gram-positive microorganisms: Staphylococcus aureus, Staphylococcus epidermidis, Streptococcus pneumoniae, Streptococcus pyogenes, Streptococcus vulgaris, Streptococcus viridans, Streptococcus bovis.

The drug is active against gram-negative microorganisms: Aeromonas spp., Alcaligenes spp., Branhamella catarrhalis, Citrobacter spp., Enterobacter spp.
(some strains are resistant), Escherichia coli, Haemophilus influenzae, Haemophilus parainfluenzae, Klebssiella spp. (including Klebssiella 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., Vibrio spp ., (including Vibrio cholerae), Yersinia spp., (including Yersinia Enterocolitica). Many strains of the listed Gram-negative microorganisms, which in the presence of other antibiotics, for example, penicillins, cephalosporins of the first generations and aminoglycosides, are multiply stable, sensitive to ceftriaxone. Treponema pallidum is sensitive to ceftriaxone both in vitro and in animal experiments. According to clinical data, in the primary and secondary syphilis, a good efficacy of ceftriaxone is noted.
The drug is active against anaerobic microorganisms: Bacteroides spp.
(including some strains of Bacteroides fragilis), Clostridium spp. (including Clostridium difficile), Fusobacterium spp. (except for Fusobacterium mostiferum, Fusobacterium varium), Peptococcus spp., Peptostreptococcus spp.
The drug is resistant to: Staphylococcus strains resistant to methicillin;
most strains of enterococci (for example, Streptococcus faecalis); Some strains of many Bacteroides (for example, Bacteroides fragilis) that produce β-lactamase (to determine the sensitivity of microorganisms, it is necessary to use discs containing ceftriaxone, since it has been shown that certain strains of pathogens can be resistant in vitro to classical cephalosporins).
PHARMACOKINETICS

Suction

The values ​​of AUC for IV and IM are the same.
This means that the bioavailability of ceftriaxone with an IM is 100%.
Distribution

With parenteral administration, ceftriaxone penetrates well into the tissues and body fluids.

With iv introduction, ceftriaxone diffuses rapidly into the interstitial fluid, where the bactericidal action persists for 24 hours.

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

In healthy adults, T 1/2 is about 8 hours.

In adults, 50-60% of ceftriaxone is excreted unchanged in the urine, and 40-50% is also unchanged with bile.
Under the influence of intestinal flora, ceftriaxone is converted into an inactive metabolite.
In newborns, T 1/2 is up to 8 days, in the elderly over 75 years, the mean T 1/2 is approximately 2 times greater.

In neonates, approximately 70% of the administered dose is excreted by the kidneys.

With renal insufficiency or liver pathology in adults, the pharmacokinetics of ceftriaxone is almost unchanged, T 1/2 lengthens slightly.
If the kidney function is impaired, the secretion with bile increases, and if there is a liver pathology, then the excretion of ceftriaxone by the kidneys increases.
In newborns and children with inflammation of the meninges, ceftriaxone penetrates into the cerebrospinal fluid, while in the case of bacterial meningitis, on average 17% of the concentration of the drug in the blood serum diffuses into the cerebrospinal fluid, which is approximately 4 times greater than in aseptic meningitis.
At 24 hours after intravenous administration of ceftriaxone at a dose of 50-100 mg / kg body weight, the concentration in the cerebrospinal fluid exceeds 1.4 mg / l. In adults with meningitis, 2 to 25 hours after the administration of ceftriaxone at a dose of 50 mg / kg, the concentration of ceftriaxon was many times greater than the minimum dose necessary to suppress the pathogens of meningitis.
INDICATIONS

Infectious-inflammatory diseases caused by microorganisms sensitive to the preparation:

- sepsis;

- meningitis;

- infection of the abdominal cavity (peritonitis, inflammatory diseases of the gastrointestinal tract, bile ducts);

- infections of bones and joints;

- skin and soft tissue infections;

- infections of the kidneys and urinary tract;

- respiratory tract infections (including pneumonia);

- infection of ENT organs;

- infections of the genitals (including gonorrhea);

- infections in patients with low immunity.

Prevention of infections in the postoperative period.

DOSING MODE

The drug is used in / m and / in.

For adults and for children over 12 years, the average daily dose is 1-2 g 1 time / day (after 24 hours).
In severe cases or infections caused by moderately sensitive pathogens, a single daily dose can be increased to 4 g.
The following doses are recommended for newborns with the administration of the drug 1 time / day: at the age of 2 weeks - 20-50 mg / kg / day (a dose of 50 mg / kg of body weight is not recommended because of the immature enzyme system of newborns).

For infants and children under 12 years of age, the daily dose is 20-75 mg / kg;
Children with a body weight of 50 kg or more are prescribed in doses intended for adults. The drug at a dose of more than 50 mg / kg body weight should be given as an IV infusion, for at least 30 minutes.
The duration of therapy depends on the course of the disease.

In bacterial meningitis in children (including newborns), the initial dose is 100 mg / kg of body weight 1 time / day, the maximum dose - 4 g / day.
Once it was possible to isolate the pathogenic microorganism and determine its sensitivity, the dose should be reduced accordingly. The best results were achieved with the following periods of therapy:
Causation Duration of therapy

Neisseria meningitidis 4 days

Haemophilus influenzae 6 days

Streptococcus pneumoniae 7 days

Sensitive Enterobacteriacease 10-14 days

For the treatment of gonorrhea, caused by both generative and non-penicillinase-resistant strains , the recommended dose is 250 mg once-monthly.

In order to prevent pre- and post-operative pre-infected or presumptively infected surgical interventions, depending on the risk of infection, one-time administration of ceftriaxone in a dose of 1-2 g is recommended 30-90 minutes prior to surgery.

In patients with impaired renal function with KK greater than 10 ml / min, with normal liver function, there is no need to reduce the dose of ceftriaxone.
Withsevere renal failure (CC less than 10 ml / min), it is necessary that the daily dose of ceftriaxone does not exceed 2 g.
In patients with impaired liver function, if the function of the kidneys is preserved , a dose of ceftriaxone should not be reduced.
In cases of simultaneous presence of severe pathology of the liver and kidneys, the concentration of ceftriaxone in serum should be monitored regularly. Patients on hemodialysis do not need to change the dose after this procedure.
Rules for the preparation of solutions and the administration of the drug

For the / m introduction, 1 g of the drug must be diluted in 3.5 ml of a 1% solution of lidocaine and inserted deep into the gluteal muscle, it is recommended to inject no more than 1 g of the drug into one buttock.
A solution of lidocaine can never be injected in / in!
For intravenous injection, 1 g of the drug must be diluted in 10 ml of sterile distilled water and injected iv slowly for 2-4 minutes.

For intravenous infusion, 2 g of powder should be diluted in approximately 40 ml of calcium free solution, for example: in 0.9% solution of sodium chloride, in a 5% solution of dextrose, in a 10% solution of dextrose, 5% solution of fructose.

The duration of IV infusion is at least 30 minutes.

SIDE EFFECT

Allergic reactions: urticaria, chills or fever, rash, itching, rarely - bronchospasm, eosinophilia, polymorphic exudative erythema (including Stevens-Johnson syndrome), serum sickness, angioedema, anaphylactic shock.

On the part of the digestive system: nausea, vomiting, diarrhea or constipation, flatulence, abdominal pain, impaired taste, stomatitis, glossitis, pseudomembranous enterocolitis, impaired liver function (increased activity of hepatic transaminases, rarely - alkaline phosphatase or bilirubin, cholestatic jaundice), dysbacteriosis.

On the part of the hematopoiesis system: leukopenia, neutropenia, granulocytopenia, lymphopenia, thrombocytosis, thrombocytopenia, hemolytic anemia, hypocoagulation, decrease in the concentration of plasma coagulation factors (II, VII, IX, X), prolongation of prothrombin time.

On the part of the urinary system: renal dysfunction (azotemia, increased urea in the blood, hypercreatininaemia, glycosuria, cylindruria, hematuria), oliguria, anuria.

Local reactions: phlebitis, pain along the vein, soreness and infiltration at the site of the / m introduction.

Other: headache, dizziness, nosebleeds, candidiasis, superinfection.

CONTRAINDICATIONS

- I trimester of pregnancy;

- Hypersensitivity to cephalosporins and penicillins.

With caution, prescribe the drug for hyperbilirubinemia in newborns, premature babies, with kidney failure, liver failure, NJA, enteritis or colitis associated with the use of antibacterial drugs in the II and III trimesters of pregnancy, during lactation.

PREGNANCY AND LACTATION

With caution should be used in the II and III trimesters of pregnancy.

If it is necessary to use the drug during lactation, breastfeeding should be stopped.

APPLICATION FOR FUNCTIONS OF THE LIVER

In patients with impaired renal function with KK greater than 10 ml / min, with normal liver function, there is no need to reduce the dose of ceftriaxone.
Withsevere renal failure (CC less than 10 ml / min), it is necessary that the daily dose of ceftriaxone does not exceed 2 g. In patients who are on hemodialysis , the dose of the drug after performing this procedure is not necessary to change.
APPLICATION FOR VIOLATIONS OF THE FUNCTION OF KIDNEYS

In patients with impaired liver function, if the function of the kidneys is preserved, the dose of ceftriaxone should not be reduced.
In cases of simultaneous presence of severe pathology of the liver and kidneys, the concentration of ceftriaxone in serum should be monitored regularly.
APPLICATION FOR CHILDREN

For adults and for children over 12 years, the average daily dose is 1-2 g 1 time / day (after 24 hours).
In severe cases or infections caused by moderately sensitive pathogens, a single daily dose can be increased to 4 g.
The following doses are recommended for newborns with the administration of the drug 1 time / day: at the age of 2 weeks - 20-50 mg / kg / day (a dose of 50 mg / kg of body weight is not recommended because of the immature enzyme system of newborns).

For infants and children under 12 years of age, the daily dose is 20-75 mg / kg;
Children with a body weight of 50 kg or more are prescribed in doses intended for adults. The drug at a dose of more than 50 mg / kg body weight should be given as an IV infusion, for at least 30 minutes.
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 preterm infants, the use of ceftriaxone requires even greater caution.
APPLICATION IN ELDERLY PATIENTS

Elderly patients during the treatment may require the appointment of vitamin K.

SPECIAL INSTRUCTIONS

With simultaneous severe renal and hepatic insufficiency, the concentration of the drug in the blood plasma should be regularly monitored.

In patients who are on hemodialysis, it is necessary to monitor the concentration of ceftriaxone in the plasma, tk.
in such cases, the rate of its elimination can be reduced.
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 are observed that disappear after the drug is discontinued (even if this phenomenon is accompanied by pain in the right upper quadrant, it is recommended to continue the prescription of the antibiotic and conduct symptomatic treatment).

During treatment, the use of ethanol is contraindicated.
possible disulfiramoid-like effects (red face, spasm in the stomach, nausea, vomiting, headache, lowering blood pressure, tachycardia, dyspnea).
Despite the detailed history, which is the rule for other cephalosporin antibiotics, one can not exclude the possibility of developing an anaphylactic shock, which requires immediate therapy-first injected with epinephrine and then glucocorticoids.

Elderly and weakened patients during the treatment may require the appointment of vitamin K.

Use in Pediatrics

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 preterm infants, the use of ceftriaxone requires even greater caution.
OVERDOSE

Symptoms: may increase the side effects.

Treatment: symptomatic therapy.
Excessively high concentrations of ceftriaxone in plasma can not be reduced by hemodialysis or peritoneal dialysis.
DRUG INTERACTION

There is synergy between ceftriaxone and aminoglycosides against the effect on many gram-negative bacteria.
Although it is impossible to predict the effect of such combinations in advance, it is justified to jointly assign them in cases of severe and life-threatening infections (for example, caused by Pseudomonas aeruginosa).
Ceftriaxone is incompatible with ethanol.

NSAIDs and other platelet aggregation inhibitors increase the chance of bleeding.

With simultaneous use with "loop" diuretics and other nephrotoxic drugs, the risk of developing nephrotoxicity increases.

Pharmaceutical interaction

In connection with the pharmaceutical incompatibility of ceftriaxone and aminoglycosides, it is necessary to prescribe them separately in recommended doses.

Pharmaceutically incompatible with solutions containing other antibiotics.

Do not mix in one infusion bottle or in one syringe with another antibiotic (chemical incompatibility).

TERMS OF RELEASE FROM PHARMACY

The drug is released by prescription.

TERMS AND CONDITIONS OF STORAGE

List B. The drug should be stored in a dry, protected from light and out of reach of children at a temperature of no higher than 25 ° C.
Shelf life - 2 years.
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