Ceftriabol - instructions for use, dose, side effects, contraindications

Ceftriabol® is a third-generation cephalosporin antibiotic for parenteral use, has a bactericidal effect, inhibits the synthesis of the cell membrane, in vitro suppresses the growth of most gram-positive and gram-negative microorganisms. Resistant to beta-lactamase enzymes (both penicillinase and cephalosporinase, produced by most gram-positive and gram-negative bacteria). Effective against the following microorganisms:

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

Note: Staphylococcus spp., resistant to methicillin, is resistant to cephalosporins, including ceftriaxone. Most strains of enterococci (for example, Streptococcus faecalis) also resistant to ceftriaxone.

Gram-negative aerobes: 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, which in the presence of other antibiotics, for example, penicillins, first-generation cephalosporins and aminoglycosides, are multiplying steadily, sensitive to ceftriaxone. Treponema pallidum is sensitive to ceftriaxone as in vitro, and in animal experiments. According to clinical data, in the primary and secondary syphilis, a good efficacy of ceftriaxone is noted.

Anaerobic pathogens: Bacteroides spp. (including some strains AT. fragilis), Clostridium spp. (at Tom number of FROMl. difficile), Fusobacterium spp. (Besides F. mostiferum. F. varium), Peptococcus spp., Peptostreptococcus spp. Note: some strains of many Bacteroides spp. (eg, AT. fragilis), Developing beta-lactamase, resistant to ceftriaxone.To determine the sensitivity of microorganisms, discs containing ceftriaxone, since it is shown that in vitro to classical cephalosporins, certain strains of pathogens can be stable.

Pharmacokinetics:

The main pharmacokinetic parameters, except the half-life (T1 / 2), depend on the administered dose. After 1/2 hour after a single intravenous (iv) 0.5 g; 1 g; and 2 g of the drug concentration in serum are 82 mg / l. 151 mg / L and 257 mg / L, respectively. After 24 hours, the serum concentrations are 5 mg / L, 9 mg / L and 15 mg / L. After intramuscular administration of I cefabol® at a dose of 1 g, the maximum concentration (C max) is reached 2 hours after the injection and is 81 mg / l. Bioavailability with intramuscular injection is 100%. With repeated intravenous and / or injections, cumulation of the drug in the blood plasma is observed. With parenteral administration ceftriaxone well penetrates into tissues and body fluids. With intravenous administration ceftriaxone quickly diffuses into the interstitial fluid, where its bactericidal action against pathogens sensitive to it 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, the binding of ceftriaxone 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.

The half-life in healthy adults is about 8 hours. In newborns up to 8 days and in elderly people older than 75 years, the average half-life is approximately twice as large. In adults, 50-60% of ceftriaxone is excreted unchanged through the urinary system, and 40-50% is also unchanged through the gastrointestinal tract. Under the influence of intestinal flora ceftriaxone turns into an inactive metabolite. In neonates, approximately 70% of the administered dose is excreted by the kidneys. In renal failure or liver disease in adults pharmacokinetics ceftriaxone hardly changes, half-life period is lengthened slightly. If the kidney function is impaired, the secretion with bile increases, and if liver pathology takes place, then the excretion of ceftriaxone by the kidneys increases.

Penetration into the cerebrospinal fluid: in newborns and in 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 blood serum diffuses into the cerebrospinal fluid, which is approximately 4 times greater than with aseptic meningitis. 24 hours after intravenous administration of ceftriaxone in 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 body weight, the concentration of ceftriaxone was many times greater than the minimum oppressive dose that is necessary to suppress the pathogens most commonly causing meningitis.

Indications:

Infections caused by susceptible to ceftriaxone pathogens: -infection of the central nervous system (meningitis, brain abscess); -infection of the abdominal cavity (peritonitis, inflammatory diseases of the gastrointestinal tract, bile ducts); -sepsis;

-infection of bones, joints, connective tissue, skin;

-infection in patients with low immunity (febrile neutropenia and

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-infection of the kidneys and urinary tract (acute and exacerbation of chronic pyelonephritis, pyelitis);

-infection of the respiratory tract (including pneumonia), as well as infections of the LOP-organs;

-rogenital infections (including gonorrhea). Prevention of infections in the postoperative period.

Contraindications:Hypersensitivity to cephalosporins, penicillins and carbapenems. First trimester of pregnancy, lactation.

Carefully:Hyperbilirubinemia in newborns, premature babies, renal / hepatic insufficiency, ulcerative colitis, enteritis or colitis associated with the use of antibacterial drugs, pregnancy 2-3 trimester.

Dosing and Administration:

The drug is used intramuscularly and intravenously.

For adults and for children over 12 years old

The average daily dose is 1-2 g of ceftriaxone once a day or 0.5-1 g every 12 hours.

In severe cases or in cases of infections caused by moderately sensitive pathogens, the daily dose may be increased to 4 g.

For newborns

For a single daily dosage, the following scheme is recommended:

For newborns (up to 2 weeks of age): 20-50 mg / kg body weight in day (dose of 50 mg / kg body weight exceed is not recommended due to immature enzyme system of newborns).

For infants and children under 12 years of age

The daily dose is 20-75 mg / kg body weight.

Children with a body weight of 50 kg and above should adhere to the dosage for adults. A dose of more than 50 mg / kg body weight should be given as an intravenous infusion, for at least 30 minutes.

Duration of therapy

Depends on the course of the disease.

Meningitis

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

Causative agent	Duration of therapy
Neisseria meningitidis	4 days
Haemophilus influenzae	6 days
Streptococcus pneumoniae	7 days
Sensitive Enterobacteriacease	10-14 days

Gonorrhea

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

Prevention in the pre- and postoperative period

Before infected or presumptively infected surgical interventions forprevention of postoperative infections, depending on the risk of infection, a single administration of ceftriaxone in a dose of 1 -2 g is recommended 30-90 minutes prior to surgery.

Lack of kidney and liver function

In patients with impaired renal function, under the condition of normal liver function, a dose of ceftriaabol® is not necessary to reduce. Only with a deficiency of the kidneys in the preterminal stage is it necessary that the daily dose of Ceftriaabol® does not exceed 2 g.

In patients with impaired liver function, if the function of the kidneys is maintained, the dose of the drug 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. In patients undergoing hemodialysis, the dose of the drug after this procedure is not necessary to change.

Intramuscular injection

For intramuscular injection, 1 g of the drug should 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 administered intravenously!

Intravenous administration

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.

Intravenous infusion

Duration of intravenous infusion is at least 30 minutes. For intravenous infusion of 2 g of the powder should be diluted with approximately 40 ml of a solution free of calcium, such as 0.9% sodium chloride solution, 5% dextrose solution, 10% dextrose solution, 5% fructose solution.

Side effects:

allergic reactions: urticaria, chills and fever, rash, itching, rarely - bronchospasm, eosinophilia, polymorphic erythema exudative (including Stevens-Johnson syndrome), serum sickness, angioneurotic edema, anaphylactic shock;

from the digestive system: nausea, vomiting, diarrhea or constipation, flatulence, abdominal pain, taste disturbance, stomatitis, glossitis, enterocolitis, pseudomembranous, liver dysfunction (increased activity "liver" enzymes, at least - alkaline phosphatase, bilirubin, cholestatic icterus), gallbladder psevdoholelitiaz ("sludge" - a syndrome), a dysbacteriosis;

from the hematopoiesis: leukopenia, leukocytosis, neutropenia, granulocytopenia, lymphopenia, thrombocytosis, thrombocytopenia, hemolytic anemia, basophilia, hypocoagulation, decrease in plasma clotting factor concentration (II, VII, IX, X), prolongation of prothrombin time;

from the urinary system: renal dysfunction (azotemia, increased urea in the blood, hypercreatininaemia, glucosuria, cylindruria, hematuria), oliguria, anuria;

local reactions: phlebitis, soreness along the vein, soreness and infiltration at the site of intramuscular injection;

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

Overdose:Excessively high concentrations of ceftriaxone in plasma can not be reduced by hemodialysis or peritoneal dialysis. Symptomatic measures are recommended for the treatment of overdose cases.

Interaction:

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

Nonsteroidal anti-inflammatory drugs and other inhibitors of platelet aggregation increase the likelihood of bleeding.With simultaneous use with "loop" diuretics and other nephrotoxic drugs, the risk of developing nephrotoxic action increases.

Pharmaceutically incompatible with solutions containing other antibiotics.

Special instructions:

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

In patients who are on hemodialysis, it is necessary to monitor the concentration of ceftriaxone in the plasma, tk. they can decrease the rate of its excretion. 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 examination of the gallbladder, blackouts are noted that disappear after cancellation (even if this phenomenon is accompanied by pain in the right hypochondrium, recommend continued antibiotic prescription and symptomatic treatment). During treatment, the use of ethanol is contraindicated - disulfiramoid-like effects are possible (reddening of face, spasm in the stomach, nausea, vomiting, headache, lowering of 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 that requires immediate therapy - first intravenously injected epinephrine, then glucocorticoids.

Studies in vitro have shown that, like other cephalosporin antibiotics Tsefabol® able to displace bilirubin bound to albumin serum. Therefore, in newborns with hyperbilirubinemia and especially in premature infants, use Tsefabola® requires even more care. Elderly and debilitated patients may require the appointment of vitamin K.

Form release / dosage:

Powder for the preparation of solution for intravenous and intramuscular administration of 1000 mg.

Packaging:

Powder for the preparation of solution for intravenous and intramuscular administration of 1000 mg.

1000 mg of the active substance is placed in glass vials.

The solvent - "Water for Injection" in glass ampoules of 10 ml or 2 ampoules with a volume of 5 ml.

1. 1 bottle with the drug and instructions for use are placed in a pack of cardboard.

2. 1 vial with the drug, 1 ampoule with a solvent capacity of 10 ml or 2 ampoules with a solvent capacity of 5 ml and instructions for use are packed in a cardboard pack.

3. 1 vial with the drug and 1 ampoule with a solvent capacity of 10 ml or 2 ampoules with a solvent capacity of 5 ml are packed in a contour mesh box made of polyvinyl chloride film and aluminum lacquered or foil-foil. One contour mesh package and instructions for use are put in a cardboard pack.

4. 5 bottles of the drug are packed in contour mesh packaging from polyvinyl chloride film and foil of aluminum lacquered or without foil. One outline package and instructions for use are put in a cardboard pack.

5. 5 bottles with the preparation complete with 5 ampoules of a solvent with a capacity of 10 ml or 10 ampoules with a solvent capacity of 5 ml are packed in contour cell packs made of polyvinylchloride film and foil of aluminum lacquered or without foil. One outline package with the preparation, one outline package with a solvent and instructions for use are put in a cardboard pack.

Storage conditions:

In a dry, the dark place at a temperature of no higher than 25 ° C. Keep out of the reach of children.

Shelf life:2 years. Do not use after expiry date.

Terms of leave from pharmacies:On prescription

Registration number:P N001156 / 01

Date of registration:22.04.2008

The owner of the registration certificate:PREBAND PFC, LLCPREBAND PFC, LLC Russia

Manufacturer: & nbsp

PREBAND PFC LLC Russia

Information update date: & nbsp25.11.2015

Illustrated instructions

Instructions

Ceftriabol® (Ceftriabol®)