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

Active substance: ceftriaxone

Type: Third generation cephalosporin

Manufacturer: MAKIZ-PHARMA (Russia) manufactured by Shijiazhuang Pharmaceutical Group Ouyi (China)
Composition, form of production and packaging
Powder for the preparation of solution for intravenous and / or injection of
crystalline, almost white or yellowish color.

1 f.

ceftriaxone (in the form of the sodium salt) 1 g

Glass bottles (1) - cardboard packs.

INSTRUCTION FOR THE SPECIALIST.

Description of the drug approved by the manufacturer for the printed edition of 2008.

PHARMACHOLOGIC EFFECT

Semisynthetic cephalosporin antibiotic III generation of a broad spectrum of action.

The bactericidal activity of ceftriaxone is due to the suppression of the synthesis of cell membranes.
The drug is highly resistant to the action of beta-lactamases (penicillinase and cephalosporinase) Gram-positive and Gram-negative microorganisms.
Ceftriaxone is active against gram-negative aerobic microorganisms: Enterobacter aerogenes, Enterobacter cloacae, Escherichia coli, Haemophilus influenzae (including strains resistant to ampicillin), Haemophilus parainfluenzae, Klebssiella spp.
(including Klebssiella pneumoniae), Neisseria gonorrhoeae (including strains that form and not prone penicillinase), Neisseria meningitidis, Proteus mirabilis, Proteus vulgaris, Morganella morganii, Serratia marcescens, Citrobacter freundii, Citrobacter diversus, Providencia spp. , Salmonella spp., Shigella spp., Acinetobacter calcoaceticus.
A number of strains of the above microorganisms that exhibit resistance to other antibiotics, such as penicillins, cephalosporins, aminoglycosides, are sensitive to ceftriaxone.

Individual strains of Pseudomonas aeruginosa are also sensitive to the drug.

The drug is active against Gram-positive aerobic microorganisms: Staphylococcus aureus (including strains forming penicillinase), Staphylococcus epidermidis (methicillin-resistant staphylococci, resistant to all cephalosporins, including ceftriaxone), Streptococcus pyogenes (group A beta beta-hemolytic streptococci ), Streptococcus agalactiae (Group B Streptococcus), Streptococcus pneumoniae;
anaerobic microorganisms: Bacteroides spp., Clostridium spp. (with the exception of Clostridium difficile).
PHARMACOKINETICS

Suction

With the / m introduction ceftriaxone is well absorbed from the injection site and reaches high concentrations in the serum.
Bioavailability of the drug is 100%.
The average concentration in the plasma is achieved 2-3 hours after the injection.
With repeated IM or IV injections in doses of 0.5-2.0 g with an interval of 12-24 hours there is accumulation of ceftriaxone in a concentration that is 15-36% higher than the concentration achieved with a single injection.
Distribution

When administered at a dose of 0.15 to 3.0 g, V d is from 5.78 to 13.5 liters.

Ceftriaxone reversibly binds to blood plasma proteins.

Excretion

When administered at a dose of 0.15 to 3.0 g, T1 / 2 ranges from 5.8 to 8.7 hours;
the plasma clearance is 0.58 - 1.45 l / h, the renal clearance is 0.32 - 0.73 l / h.
From 33% to 67% of the drug is excreted unchanged by the kidneys, the rest is excreted with bile into the intestine, where it is biotransformed into an inactive metabolite.

Pharmacokinetics in special clinical cases

In newborns and children with inflammation of the meninges, ceftriaxone penetrates into the cerebrospinal fluid, while in the case of bacterial meningitis, an average of 17% of the concentration of the drug in the plasma diffuses into the cerebrospinal fluid, which is approximately 4 times greater than with aseptic meningitis.Twenty four hours after intravenous administration of ceftriaxone at a dose of 50-100 mg / kg body weight, concentrations in the cerebrospinal fluid exceed 1.4 mg / L.
In adults with meningitis, 2-24 hours after the administration of 50 mg / kg of body weight, the concentration of ceftriaxone in the cerebrospinal fluid is many times greater than the minimum inhibitory concentrations for the most common meningitis pathogens.
INDICATIONS

Treatment of infections caused by microorganisms sensitive:

- sepsis;

- meningitis;

- disseminated borreliosis of Lyme (early and late stages of the disease);

- infections of the abdominal cavity (peritonitis, biliary tract infections and gastrointestinal tract);

- infections of bones and joints;

- skin and soft tissue infections;

- wound infections;

- infections in patients with weakened immunity;

- infection of the pelvic organs;

- infections of the kidneys and urinary tract;

- respiratory tract infections (especially pneumonia);

- infection of ENT organs;

- infections of the genitals, including gonorrhea.

Prevention of infections in the postoperative period.

DOSING MODE

The drug is given in / m or / in.

Adults and children over the age of 12 years are prescribed 1-2 grams 1 time / day (every 24 hours).
In severe cases or infections, the causative agents of which have only moderate sensitivity to ceftriaxone, the daily dose can be increased to 4 g.
Newborn (up to 2 weeks)
appoint 20-50 mg / kg of body weight 1 time / day. The daily dose should not exceed 50 mg / kg of body weight. When determining the dose, no distinction should be made between full and premature children.
Infants and young children (from 15 days to 12 years) are appointed by
20-80 mg / kg body weight 1 time / day.
Children with a body weight> 50 kg are prescribed doses intended for adults.

Doses of 50 mg / kg or more for intravenous administration should be administered drip for at least 30 minutes.

Older patients should be given usual doses intended for adults, without adjusting for age.

The duration of treatment depends on the course of the disease.
Ceftriaxone should be continued for at least 48-72 hours after the temperature is normalized and the eradication of the pathogen is confirmed.
In bacterial meningitis in infants and young children, treatment starts with a dose of 100 mg / kg (but not more than 4 g) 1 time / day.
After identifying the pathogen and determining its sensitivity, the dose can be reduced accordingly.
In meningococcal meningitis, the best results were achieved with a treatment duration of 4 days, with meningitis caused by Haemophilus influenzae 6 days,Streptococcus pneumoniae, 7 days.

With borreliosis Lyme: adults and children over 12 years of age are prescribed 50 mg / kg once a day for 14 days;
the maximum daily dose is 2 g.
With gonorrhea (caused by strains forming and non-treating penicillinase) - once / in a dose of 250 mg.

In order to prevent postoperative infections , depending on the degree of infectious risk, the drug is administered in a dose of 1-2 g once for 30-90 minutes before the operation.

In operations on the colon and rectum - effectively simultaneous (but separate) administration of Ceftriaxone and one of 5-nitroimidazoles, for example, ornidazole.

In patients with impaired renal function, there is no need to reduce the dose if the liver function remains normal .
In cases of preterminal renal failure of severe degree with CC <10 ml / min, the daily dose of the drug should not exceed 2 g.
In patients with impaired liver function, there is no need to reduce the dose if the kidney function remains normal .

When combined with severe renal and hepatic insufficiency , the concentration of ceftriaxone in the plasma should be determined regularly and, if necessary, its dose should be adjusted.

Patients who are on dialysis additional injection of the drug after dialysis is not required.
It should, however, control the concentration of ceftriaxone in the serum for the purpose of timely dose adjustment, since the rate of excretion of the drug in these patients may be reduced.
Rules for the preparation and administration of solutions

For the / m introduction

The contents of the vial (1 g) are dissolved in 3.6 ml of water for injection.
After preparation, 1 ml of the solution contains about 250 mg of ceftriaxone. If necessary, a more dilute solution may be used.
As with other intravenous injections, Ceftriaxone is injected into a relatively large muscle (gluteus);
Trial aspiration helps to avoid unintentional insertion into the blood vessel. It is recommended to inject no more than 1 g of the drug into one muscle. To reduce pain with I / m injections, the drug should be administered with a 1% solution of lidocaine. Do not inject lidocaine solution IV.
For intravenous administration

The contents of the vial (1 g) are dissolved in 9.6 ml of water for injection.
After preparation, 1 ml of the solution contains about 100 mg of ceftriaxone. The solution is administered slowly for 2-4 minutes.
For IV infusion

Dissolve 2 g of ceftriaxone in 40 ml of sterile water for injection or one of the infusion solutions that do not contain calcium (0.9% sodium chloride solution, 2.5%, 5% or 10% dextrose solution, 5% levulose solution, 6% dextran solution in dextrose) .
The solution is introduced for 30 minutes.
SIDE EFFECT

Allergic reactions: urticaria, chills or fever, rash, itching;
rarely - bronchospasm, eosinophilia, exudative erythema multiforme (including Stevens-Johnson syndrome), serum sickness, anaphylactic shock.
On the part of the digestive system: nausea, vomiting, diarrhea or constipation, flatulence, abdominal pain, taste disorder, stomatitis, glossitis, pseudomembranous enterocolitis, impaired liver function (increased activity of liver transaminases, less often - alkaline phosphatase or bilirubin, cholestatic jaundice), pseudo-cholelithiasis of the gallbladder ("sludge" -syndrome), a dysbacteriosis.

On the part of the hematopoiesis system: anemia, leukopenia, leukocytosis, neutropenia, granulocytopenia, lymphopenia, thrombocytosis, thrombocytopenia, hemolytic anemia, hypocoagulation, decrease in the concentration of fissile clotting 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

- Hypersensitivity to ceftriaxone and other cephalosporins, penicillins, carbapenems.

With caution appoint a drug with NNC, with violations of the liver and kidneys, with enteritis and colitis associated with the use of antibacterial drugs;
premature and newborn children with hyperbilirubinemia.
PREGNANCY AND LACTATION

The use of the drug during pregnancy is possible only in those cases when the intended use for the mother exceeds the potential risk for the fetus, because
ceftriaxone penetrates the placental barrier.
If it is necessary to use the drug during lactation, the question of stopping breastfeeding should be solved,
ceftriaxone is excreted in breast milk.
APPLICATION FOR FUNCTIONS OF THE LIVER

With caution appoint a drug for violations of kidney function.

With simultaneous severe renal and hepatic insufficiency, patients who are on hemodialysis should regularly determine the concentration of the drug in the plasma.

With prolonged treatment, it is necessary to regularly monitor the indicators of the functional state of the kidneys.

APPLICATION FOR VIOLATIONS OF THE FUNCTION OF KIDNEYS

With simultaneous severe renal and hepatic insufficiency, patients who are on hemodialysis should regularly determine the concentration of the drug in the plasma.

With long-term treatment, it is necessary to regularly monitor the indicators of the functional state of the liver.

In rare cases with ultrasound of the gallbladder, blackouts are observed, which disappear after the treatment is discontinued (even if this phenomenon is accompanied by pain in the right hypochondrium, it is recommended to continue the prescription of the antibiotic and to conduct symptomatic treatment).

SPECIAL INSTRUCTIONS

With simultaneous severe renal and hepatic insufficiency, in patients who are on hemodialysis, the concentration of the drug in the 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 with ultrasound of the gallbladder, blackouts are observed, which disappear after the treatment is discontinued (even if this phenomenon is accompanied by pain in the right hypochondrium, it is recommended to continue the prescription of the antibiotic and to conduct symptomatic treatment).

During treatment, alcohol can not be consumed, since disulfiramoid-like effects are possible (reddening of face, stomach and stomach spasm, nausea, vomiting, headache, lowering blood pressure, tachycardia, dyspnea).

Despite the detailed history, which is the rule for other cephalosporin antibiotics, we can not exclude the possibility of developing an anaphylactic shock, which requires immediate therapy - first I / O injected epinephrine, then GCS.

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.
Elderly and debilitated patients may require the appointment of vitamin K.

The prepared solution should be stored at room temperature no more than 6 hours or in a refrigerator at a temperature of 2-8 ° C not more than 24 hours.

OVERDOSE

When an overdose of hemodialysis and peritoneal dialysis does not reduce the concentration of the drug.
There is no specific antidote.
Treatment of an overdose is symptomatic.

DRUG INTERACTION

Ceftriaxone, suppressing the intestinal flora, prevents the synthesis of vitamin K.

With a simultaneous appointment with drugs that reduce platelet aggregation (NSAIDs, salicylates, sulfinpyrazone), the risk of bleeding increases.
With a simultaneous appointment with anticoagulants, the effect of the latter is noted.
With simultaneous administration with "loop" diuretics, the risk of developing nephrotoxic action increases.

Ceftriaxone and aminoglycosides have a synergistic effect on many Gram-negative bacteria.

Incompatible with ethanol.

Pharmaceutical interaction

Ceftriaxone solutions should not be mixed or administered concomitantly with other antimicrobial agents.
Ceftriaxone should not be mixed with solutions containing calcium.
TERMS OF RELEASE FROM PHARMACY

The drug is released by prescription.

TERMS AND CONDITIONS OF STORAGE

List B. The drug should be stored out of reach of children, dry, protected from light at a temperature of no higher than 25 ° C.
Shelf life - 3 years
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