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

Ceftriaxone is resistant to beta-lactamase enzymes (both penicillinase and cephalosporinase, produced by the majority of Gram-positive and Gram-negative bacteria). Has a wide spectrum of antimicrobial action, which includes various aerobic and anaerobic gram-positive and gram-negative microorganisms. In vitro in vitro, as well as in the treatment of clinical infections, ceftriaxone demonstrated a high level of antimicrobial activity when exposed to most known strains of the following microorganisms:

Gram-positive aerobic: Staphylococcus aureus (including strains producing penicillinase), Staphylococcus epidermidis, Streptococcus pneumoniae, Streptococcus A (Str. Pyogenes), Streptococcus viridans.

Aerobic Gram-negative: Acinetobacter calcoaceticus, Enterobacter aerogenes, Enterobacter cloacae, Escherichia coli, Haemophilus influenzae (including strains with established ampicillin resistance and strains producing beta-lactamase), Haemophilus parainfluenzae, Klebsiella oxytoca, Klebsiella pneumoniae, Moraxella catarrhalis (including strains, beta-lactamase), Morganella morganii, Neisseria gonorrhoeae (including strains producing and non-producing penicillinase), Neisseria meningitidis, Proteus mirabilis, Proteus vulgaris, Pseudomonas aeruginosa (most known strains), Serratia marcescens.

Anaerobic microorganisms: Bacteroides fragilis, Clostridium species, Peptostreptococcus species.

Pharmacokinetics:

After intramuscular injection quickly and completely absorbed. Bioavailability is 100%. The maximum concentration in blood plasma is observed after 1.5 hours. Reversibly binds to albumin plasma (85-95%). The drug remains in the body for a long time. The minimum antimicrobial concentrations are determined in the blood for 24 hours or more. Easily penetrates into the organs, body fluids (peritoneal, pleural, synovial, with inflammation of the meninges - into the spinal cord), into the bone tissue.In breast milk, 3-4% of the serum concentration is determined (more intramuscularly than with intravenous administration). The half-life period (T1 / 2) 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 (creatinine clearance 0-5 ml / min) - 14.7 hours, with KK 5-15, ml / min - 15.7 h, 16-30 ml / min - 11.4 h; 31-60 ml / min - 12.4 hours. In active form, up to 50% of the kidneys are released within 48 hours. Partially excreted with bile. If the kidney function is insufficient, excretion slows down, cumulation is possible.

Indications:Infectious-inflammatory diseases caused by microorganisms sensitive to ceftriaxone: sepsis, meningitis, infections of the abdominal cavity (peritonitis, inflammatory diseases of the gastrointestinal tract, bile ducts), infections of bones, joints, connective tissue, skin, infection in patients with low immunity, infection kidney and urinary tract infections, respiratory tract infections (including pneumonia), as well as infections of LOP-organs, urogenital infections (including gonorrhea). Prevention of infections in the postoperative period.

Contraindications:

Hypersensitivity (including to others.cephalosporins, penicillins, carbapenems), hyperbilirubinemia in newborns, newborns, which are shown in / in the introduction of solutions containing calcium ions.

Carefully:Premature infants, renal / hepatic insufficiency, ulcerative colitis, enteritis or colitis associated with the use of antibacterial drugs.

Pregnancy and lactation:

Application in the first trimester of pregnancy is contraindicated.

In pregnancy in II, III trimester apply only if the intended benefit to 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:

The drug is used intramuscularly and intravenously.

For newborns - 20-50 mg / kg / day.

For the treatment of skin and soft tissue infections recommended daily dose in children - 50-75 mg / kg, divided into 2 doses (every 12 hours).

With 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 divided doses (every 12 hours). Duration of treatment is 7-14 days.

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

When treating other infections recommended daily dose in children - 50-75 mg / kg, divided into 2 doses (every 12 hours). The total daily intake for children 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.

For adults and children over 12 years the average daily dose is 1-2 g 1 time per day. In severe cases or in cases of infections caused by moderately sensitive pathogens, the daily dose may be increased to 4 g.

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

Before infected and presumptively infected surgical interventions to prevent postoperative infections, depending on the danger of infection, a single administration of the drug in a dose of 1-2 g is recommended for 30-90 minutes before the operation.

In operations on the colon and rectum, additional administration of a drug from the 5-nitroimidazole group is recommended.

In patients with impaired renal function, under the condition of normal liver function, the dose of the drug is not necessary to reduce. Only if the kidney function in the terminal stage is insufficient (creatinine clearance below 10 ml / min), that the daily dose does not exceed 2 in

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 who are on hemodialysis, the dose of the drug after this procedure there is no need to change.

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 with a single injection. A solution of lidocaine can never be administered intravenously!

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

Duration of intravenous infusion is at least 30 minutes. For intravenous infusion, 2 g of powder should be diluted in approximately 40 ml of the solution free of calcium, for example, in a 0.9% solution of sodium chloride, in a 5% solution of dextrose, in a 10% solution of dextrose, 5% solution of fructose (levulose).

Side effects:

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

From the nervous system: convulsions.

On the part of the digestive system: nausea, vomiting, diarrhea or constipation, flatulence, abdominal pain, taste disorder, stomatitis, glossitis, pseudomembranous colitis, impaired liver function (increased activity of "liver" transaminases, less alkaline phosphatase, or bilirubin, cholestatic jaundice) , dysbacteriosis, colitis, dyspepsia, "sludge phenomenon" of the gallbladder, cholelithiasis.

From the hematopoiesis: leukopenia, neutropenia, granulocytopenia, lymphopenia, thrombocytosis, thrombocytopenia, agranulocytosis, basophilia, leukocytosis, lymphocytosis, monocytosis, hemolytic anemia, hypocoagulation, decrease in the plasma clotting factor concentration (II, VII, IX, X), lengthening prothrombin time.

On the part of the genitourinary system: vaginitis, nephrolithiasis, renal dysfunction (azotemia, increased urea in the blood, hypercreatininaemia, glucosuria, cylindruria, hematuria), oliguria, anuria.

Local reactions: with iv introduction - phlebitis, tenderness, compaction along the vein; Intramuscular injection - soreness, sensation of warmth, tightness or condensation at the injection site.

Laboratory indicators: reduction of prothrombin time, increase in urea concentration, presence of sediment in urine.

Other: increased sweating, "hot flashes" of blood, palpitations, headache, dizziness, nosebleeds, candidiasis, superinfection.

Overdose:Symptoms: nausea, vomiting, diarrhea, confusion, convulsions, increased other dose-related side effects. 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.

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

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.

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.

It is pharmaceutically incompatible with solutions containing other antibiotics, with amsacrine, vancomycin, with solutions containing calcium ions (including Hartman and Ringer's solution), as well as with fluconazole and aminoglycosides.

Special instructions:

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 Ca2 + -containing solutions for intravenous administration and other age groups of patients, therefore ceftriaxone should not be mixed with Ca2 + -containing solutions (including for parenteral nutrition), and also administered simultaneously, incl. through separate accesses for infusions at different sites. Theoretically, based on the calculation of 5 T1 / 2 ceftriaxone, the interval between, the introduction of ceftriaxone and Ca2 + -containing solutions should be at least 48 hours. Data on the possible interaction of ceftriaxone with oral Ca2 + -containing preparations, as well as ceftriaxone for IM administration with Ca2 + -containing drugs (in / in and oral) are absent.

When the drug is used, rare cases of pancreatitis have been described, possibly due to obstruction of the biliary tract. Most patients had risk factors for congestion of the biliary tract (previous drug therapy, severe co-morbidities, completely parenteral nutrition); However, the starting role of precipitate formation in the biliary tract under the influence of ceftriaxone can not be ruled out.

In rare cases, with ultrasound of the gallbladder, blackouts (precipitates of calcium solceftfrioxone) are observed, which disappear after discontinuation of treatment. With the development of the symptoms or signs indicating the possible gallbladder disease, or in the presence of ultrasound signs "sludge phenomenon" is recommended to stop administering the drug.

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).

Precautionary measures

When concomitant severe renal and hepatic failure, as well as in patients on hemodialysis, should be regularly to determine the concentration of drug in plasma.

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. Despite the detailed collection of anamnesis, which is the rule for other cephalosporin antibiotics,it is impossible to exclude the possibility of developing an anaphylactic shock, which requires immediate therapy: first intravenously injected epinephrine, then glucocorticoids.

In vitro studies have shown that, like other cephalosporin antibiotics ceftriaxone is able to displace bilirubin, associated with serum albumin. Elderly and debilitated patients may require the appointment of vitamin K.

Effect on the ability to drive transp. cf. and fur:Data on the effect of the drug on the ability to drive vehicles and work with mechanisms are not available.

Form release / dosage:

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

Packaging:

The amount of the preparation, equivalent to 1.0 g of ceftriaxone in a vial of colorless glass, sealed with a rubber stopper, rolled up with an aluminum cap and closed with a plastic lid.

1 bottle with instructions for use in a cardboard box.

Storage conditions:In a dry, protected from light 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 N014935 / 01

Date of registration:27.10.2011

The owner of the registration certificate:Lupine Co., Ltd.Lupine Co., Ltd. India

Manufacturer: & nbsp

LUPIN, Ltd. India

Representation: & nbspLUPIN LIMITEDLUPIN LIMITED

Information update date: & nbsp16.11.2015

Illustrated instructions

Instructions

Cefaxon (Cefaxone)