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

Ceftriaxone is a third generation cephalosporin antibiotic for parenteral use, has a bactericidal effect, inhibits the synthesis of the cell wall, in vitro Suppresses the growth of many gram-negative and gram-positive microorganisms. Resistant to the action of beta-lactamase enzymes (both penicillinase and cephalosporinase, produced by the majority of gram positive and Gram-negative bacteria).Effective against the following microorganisms:

Gram-positive aerobes: Staphylococcus aureus (including strains producing penicillinase), Staphylococcus epidermidis, Streptococcus pneumoniae, Streptococcus pyogenes, Streptococcus spp. groups viridans.

Gram-negative aerobes: Acinetobacter calcoaceticus, Borrelia burgdorferi, Enterobacter aerogenes, Enterobacter cloacae, Escherichia coli, Haemophilus influenzae, Haemophilus parainfluenzae, Klebsiella spp. (at t.h. Klebsiella pneumoniae), Moraxella catarrhalis (including penicillinase-producing strains), Morganella morganii, Neisseria gonorrhoeae (at t.h. strains, generators penicillinase), Neisseria meningitidis, Proteus mirabilis, Proteus vulgaris, Serratia spp. (at Tom number of Serratia marcescens); some strains Pseudomonas aeruginosa also sensitive.

Anaerobes: Bacteroides fragilis, Clostridium spp. (Besides Clostridium difficile), Peptostreptococcus spp.

Has activity in vitro for most strains of the following microorganisms, although the clinical significance of this is unknown: Citrobacter diversus, Citrobacter freundii, Providencia spp., Providencia rettgeri, Salmonella spp. (at t.h. Salmonella typhi), Shigella spp., Streptococcus agalactiae, Bacteroides bivius, Bacteroides melaninogenicus. Staphylococcus spp., resistant to methicillin, resistant to cephalosporins, incl. and to ceftriaxone. Most streptococcal strains of the group D and enterococci (for example, Enterococcus faecalis) also resistant to ceftriaxone.

Pharmacokinetics:

Bioavailability is 100%.

The maximum concentration is achieved after intramuscular (IM) administration after 2-3 hours, after intravenous (IV) administration - at the end of infusion.

The maximum concentration (Cmax) after the / m administration at a dose of 0.5 g and 1 g is 38 and 76 μg / ml, respectively.Cmax for iv in doses of 0.5 g, 1 g and 2 g - 82, 151 and 257 μg / ml, respectively. The connection with plasma proteins is 83-96%. The volume of distribution is 0,12-0,14 l / kg (5,78-13,5 l), in children -0,3 l / kg, the plasma clearance is -0,58-1,45 l / h, the renal - 0.32-0.73 l / h. Ceftriaxone quickly penetrates into tissues and body fluids. Bactericidal concentrations of ceftriaxone persist for more than 24 hours in the following tissues and fluids (lungs, heart, bile ducts, liver, palatine tonsils, middle ear and nasal mucosa, bones, as well as pleural and synovial fluid and secretion of the prostate gland).

After iv introduction ceftriaxone penetrates into the cerebrospinal fluid (including with inflammation of the meninges), where bactericidal concentrations against sensitive microorganisms persist for 24 hours.

The elimination half-life after IM is 5.8-8.7 hours, after IV introduction at a dose of 50-75 mg / kg in children with meningitis - 4.3-4.6 hours; in patients who are on hemodialysis with the clearance of creatinine 0-5 ml / min - 14.7 h, at 5-15 ml / min - 15.7 h, at 16-30 ml / min - 11.4 h, with 31- 60 ml / min - 12.4 hours.

It is excreted unchanged - 33-67% by the kidneys; 40-50% - with bile in the intestine, where the inactivation occurs. In neonates, about 70% of the drug is excreted through the kidneys. Hemodialysis is ineffective.

Indications:Bacterial infections caused by sensitive microorganisms: infections of the abdominal cavity organs (peritonitis, inflammatory diseases of the gastrointestinal tract, bile ducts, including cholangitis, empyema of the gallbladder), infection of the pelvic organs, infections of the lower respiratory tract (including pneumonia, lung abscess, pleural empyema), acute otitis media, infections of bones and joints, skin and soft tissues (including infected wounds and burns), urinary tract infections (complicated and uncomplicated), uncomplicated gonorrhea, bactea ialny meningitis, bacterial septicemia, Lyme disease. Prevention of infections in the postoperative period. Infectious diseases in persons with weakened immunity.

Contraindications:Hypersensitivity (including to other cephalosporins, penicillins and carbapenems); Hyperbilirubinemia in newborns; Newborns, who showed intravenous administration of calcium-containing solutions.

Carefully:Premature babies; renal and / or liver failure; nonspecific ulcerative colitis, enteritis or colitis associated with the use of antibacterial drugs.

Pregnancy and lactation:When pregnancy is used only if the intended benefit for the mother exceeds the potential risk to the fetus. If it is necessary to prescribe the drug during lactation, breastfeeding should be stopped.

Dosing and Administration:

It is used in / m and in / (jet, drip).

Do not use calcium-containing solutions to dilute the preparation! Standard dosing regimen

In adults, the daily dose, depending on the type and severity of the infection, is 1-2 g once a day or divided into 2 doses (every 12 hours), the total daily dose should not exceed 4 g.

Lyme disease: adults and children - 50 mg / kg (but not more than 2 g) 1 time per day for 14 days. With uncomplicated gonorrhea - 250 mg IM once.

For the prevention of postoperative complications - once 1 g for 30-60 minutes before the operation. In operations on the colon and rectum, additional administration of a drug from the 5-nitroimidazole group is recommended. The dose for newborns is 20-50 mg / kg / day.

For the treatment of skin and soft tissue infections, the recommended daily intake in children is 50-75 mg / kg once a day or divided into 2 divided doses (every 12 hours). The total daily intake for children should not exceed 2 g.

For bacterial meningitis in children, the initial dose is 100 mg / kg (but not more than 4 g) once a day, then 100 mg / kg / day (but not more than 4 g) once a day or divided into 2 doses (every 12h). The duration of treatment is 7-14 days.

In the treatment of acute otitis media in children, a single IV IM is recommended in a dose of 50 mg / kg (but not more than 1 g).

In the treatment of other infections in children, the recommended daily dose is 50-75 mg / kg, divided into 2 divided doses (every 12 hours). The total daily dose should not exceed 2 g. In children with a body weight of 50 kg and above, doses for adults are used.

A dose of more than 50 mg / kg of body weight should be given as an IV infusion for 30 minutes. In chronic renal failure (creatinine clearance less than 10 ml / min), the daily dose should not exceed 2 g. Patients on hemodialysis do not require an additional dose after a hemodialysis session, but it is necessary to control the concentration of ceftriaxone in the plasma, since its excretion in such patients may be slowed down (dose adjustment may be required).

In patients with renal-hepatic insufficiency, the daily dose should not exceed 2 g without determining the concentration of the drug in the blood plasma.

Treatment with ceftriaxone should continue for at least 2 more days after the disappearance of symptoms and signs of infection. The course of treatment is usually 4-14 days; with complicated infections, a longer duration of administration may be required. The course of treatment for infections caused by Streptococcus pyogenes, must be at least 10 days.

Method of preparation of solutions:

Use only freshly prepared solutions.

For the / m introduction, 1 g of the drug is dissolved in 3.5 ml of a 1% solution of lidocaine and injected deep into the relatively large muscle. It is recommended to inject no more than 1 g of the drug into one muscle. The solution containing lidocaine, can not be administered intravenously. For IV administration, 1 g of the drug is dissolved in 10 ml of water for injection. Introduce intravenously slowly (for 2-4 minutes).

For intravenous infusions, dissolve 2 g of the drug in 40 ml of a solution that does not contain calcium ions. Usually, the following solutions are used: 0.9% solution of sodium chloride, 5-10% dextrose solution, 5% solution of levulose (fructose). Doses of 50 mg / kg or more should be administered intravenously drip, for 30 minutes.

Side effects:

allergic reactions: rash, itching, fever, or chills;

from the nervous system: headache, dizziness;

from the digestive system: diarrhea, nausea, vomiting, taste disorder, pseudomembranous colitis;

from the hematopoiesis system: anemia (including hemolytic), leukopenia, lymphopenia, neutropenia, thrombocytopenia, thrombocytosis, eosinophilia;

with the side of the genitourinary system: candidiasis of the vagina, vaginitis;

local reactions: phlebitis, soreness, compaction along the vein during intravenous administration; soreness, sensation of heat, tightness, or condensation at the site of intramuscular injection;

other: increased sweating, "hot flashes" of blood;

laboratory indicators: increase (decrease) prothrombin time, increased activity of "liver" transaminases and alkaline phosphatase, hyperbilirubinemia, hypercreatininemia, increased urea concentration, the presence of sediment in the urine.

Undesirable reactions with a frequency of less than 0.1%: abdominal pain, agranulocytosis, allergic pneumonitis, anaphylaxis, basophilia, cholelithiasis, bronchospasm, colitis, dyspepsia, epistaxis, bloating, "sluggish phenomenon" of the gallbladder, glucosuria, hematuria, jaundice, leukocytosis, lymphocytosis, monocytosis, nephrolithiasis, palpitations, convulsions, serum sickness.

Postmarketing experience: stomatitis, glossitis, oliguria, allergic dermatitis, urticaria, edema, erythema multiforme, Stevens-Johnson syndrome, Lyell's syndrome.

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:

Bacteriostatic antibiotics reduce the bactericidal effect of ceftriaxone. Antagonism with chloramphenicol.

Ceftriaxone, suppressing the intestinal flora, interferes with the synthesis of vitamin K. Therefore, with the simultaneous use with drugs that reduce platelet aggregation (non-steroidal anti-inflammatory drugs, salicylates, sulfinpyrazone), the risk of bleeding increases. For the same reason, with simultaneous use with anticoagulants, there is an increase in anticoagulant activity. With the simultaneous administration of ceftriaxone and looped diuretics, for example, furosemide, the risk of renal dysfunction increases.

Does not contain N-methylthiotetrazol group, therefore, when interacting with ethanol does not lead to the development of disulfiram-like reactions inherent in some cephalosporins.

The solution of ceftriaxone is pharmaceutically incompatible with solutions containing amsacrine, vancomycin, fluconazole and aminoglycosides.

The solution of ceftriaxone is pharmaceutically incompatible with solutions containing calcium (including Hartman and Ringer's solutions).

Special instructions:

Ceftriaxone is used only in a hospital.

With simultaneous severe renal and hepatic insufficiency, 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 picture of peripheral blood, indicators of the functional state of the liver and kidneys.

In rare cases with ultrasound of the gallbladder, blackouts (precipitates of the calcium salt of ceftriaxone) are observed, which disappear after the cessation of treatment. With the development of symptoms or signs indicating a possible gallbladder disease or if there are ultrasound signs of a "sluggish phenomenon," it is recommended that the drug be discontinued.

When using the drug, rare cases of pancreatitis, possibly due to obstruction of the biliary tract, are described.Most patients had risk factors for congestion in the biliary tract (previous drug therapy, severe co-morbidities, complete parenteral nutrition); However, the starting role of precipitate formation in the biliary tract under the influence of ceftriaxone can not be ruled out. When using the drug, rare cases of prothrombin time change are described. Patients with vitamin K deficiency (impaired synthesis, eating disorders) may need to monitor prothrombin time and prescribe vitamin K (10 mg / week) with an increase in prothrombin time before or during therapy. Cases of fatal reactions as a result of deposition of ceftriaxone-calcium precipitates in the lungs and kidneys of newborns are described. Theoretically there is a probability of interaction of ceftriaxone with calcium-containing solutions for intravenous administration and 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 with such solutions simultaneously, incl. through separate accesses for infusions at different sites.Theoretically, on the basis of 5 half-lives of ceftriaxone, the interval between the administration of ceftriaxone and caption-containing solutions should be at least 48 hours. Data on the possible interaction of ceftriaxone with oral calcium-containing preparations, as well as ceftriaxone for intramuscular administration with calcium-containing drugs (in / in and oral) are absent. In the treatment of ceftriaxone, false-positive results of Coombs test, a test for galactosemia, glucose in urine (glucosuria is recommended to be determined only by enzyme method).

Form release / dosage:

Powder for solution for intravenous and intramuscular injection, 1.0 g.

Packaging:

By 1.0 g of active substance in glass bottles of transparent colorless glass with a capacity of 10 ml, corked with rubber stoppers, rolled with aluminum caps and plastic lids.

1 bottle together with the instruction for use is placed in a pack of cardboard.

The solvent is "Water for Injection", 10 ml produced by OJSC "Pharmasintez", Russia (RU No. LP-001844).

1 bottle with the drug and 1 ampoule with a solvent have, with instructions for use, put in a pack of cardboardpartitions.

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

Shelf life:3 years. Do not use after the expiry date printed on the package.

Terms of leave from pharmacies:On prescription

Registration number:П N012292 / 01

Date of registration:05.10.2009

The owner of the registration certificate:FARMGID CJSCFARMGID CJSC Russia

Manufacturer: & nbsp

Laika Labs Limited India

FARMASINTEZ, JSC (Irkutsk) Russia

Information update date: & nbsp21.11.2015

Illustrated instructions

Instructions

Lifaxon (Lifaxon)