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

Cephalosporin antibiotic III generation of a broad spectrum of action for parenteral administration. Bactericidal activity is due to the suppression of bacterial cell wall synthesis. It is characterized by resistance to the action of most beta-lactamases of gram-negative and gram-positive microorganisms.

It is active against the following microorganisms: Gram-positive aerobes -Staphylococcus aureus (including strains producing penicillinase), Staphylococcus epidermidis, Streptococcus pneumoniae, Streptococcus pyogenes, Streptococcus viridans;

Gram-negative aerobes: Acinetobacter calcoaceticus, Enterobacter aerogenes, Enterobacter cloacae, Escherichia coli, Haemophilus influenzae (including strains forming penicillinase), Haemophilus parainfluenzae, Klebsiella spp. (including Klebsiella pneumoniae), Moraxella catarrhalis, (including penicillin-producing strains), Morganella morganii, Neisseria gonorrhoeae (including strains forming penicillinase), Neisseria meningitidis, Proteus mirabilis, Proteus vulgaris, Serratia spp. (including Serratia mareescens); individual strains of Pseudomonas aeruginosa are also sensitive; anaerobes: Bacteroides fragilis, Clostridium spp. (except Clostridium difficile), Peptostreptococcus spp.

It has in vitro activity against most strains of the following microorganisms, although the clinical significance of this is unknown: Citrobacter diversus, Citrobacter freundii, Providencia spp., Providencia rettgeri, Salmonella spp., (Including Salmonella typhi), Shigella spp .; Streptococcus agalactiae, Bacteroides bivius, Bacteroides melaninogenicus.

Methicillin-resistant staphylococci are resistant to cephalosporins, incl. to ceftriaxone, many Streptococcus strains of group D and enterococci, incl. Enterococcus faecalis, also resistant to ceftriaxone.

Pharmacokinetics:

Bioavailability is 100%. The time to reach the maximum concentration (TCmax) after the / m introduction is 2-3 hours, after IV introduction - at the end of the infusion. The maximum concentration (Сmах) after the / m introduction in doses of 0.5 and 1 g -38 and 76 mcg / ml, respectively. Stam at iv in doses of 0.5, 1 and 2 g - 82, 151 and 257 μg / ml, respectively.In adults, 2-24 hours after the administration of a dose of 50 mg / kg, the concentration in the cerebrospinal fluid (CSF) is many times greater than the minimal inhibitory concentration (MIC) for the most common meningitis pathogens. It penetrates well into CSF with inflammation of the meninges. The connection with plasma proteins is 83-96%. The volume of distribution - 0.12-0.14 l / kg (5.78-13.5 l), in children - 0.3 l / kg, plasma clearance - 0.58-1.45 l / h, renal - 0.32-0.73 l / h.

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

Indications:

Bacterial infections caused by susceptible to ceftriaxone pathogens:

- infections of the abdominal cavity (peritonitis, inflammatory diseases of the gastrointestinal tract, bile ducts, including cholangitis, empyema of the gallbladder)

- diseases of the upper and lower respiratory tract (including pneumonia, lung abscess, pleural empyema)

- infections of bones, joints, skin and soft tissues

- infection of the urogenital zone (including gonorrhea, pyelonephritis)

- bacterial meningitis and endocarditis, sepsis

- infected wounds and burns

- soft chancre and syphilis

- Lyme disease (borreliosis)

- typhoid fever

- salmonellosis and salmonella carriage

- prevention of postoperative infections

- infectious diseases in persons with weakened immunity.

Contraindications:Hypersensitivity (including to other cephalosporins, penicillins, carbapenems).

Carefully:Hyperbilirubinemia in newborns, premature infants, renal and / or hepatic insufficiency, ulcerative colitis, enteritis or colitis associated with the use of antibacterial drugs, pregnancy, lactation.

Pregnancy and lactation:The use of ceftriaxone during pregnancy is only possible 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:

Intravenous and intramuscular.

Adults and children over 12 years of age - for 1-2 g once a day or 0.5-1 g every 12 hours,

daily dose should not exceed 4 g.

For newborns (up to 2 weeks) - 20-50 mg / kg / day.

For infants and children under 12 years of age The daily dose is 20-80 mg / kg. 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. The length of the course depends on the nature and severity of the disease. With gonorrhea - in / m once, 250 mg.

For the prevention of postoperative complications - once, 1-2 g (depending on the degree of danger of infection) for 30-90 minutes before the operation. In operations on the colon and rectum, additional administration of the drug from the group of 5-nitroimidazoles is recommended.

In bacterial meningitis in infants and young children - 100 mg / kg (but not more than 4 g) 1 time per day. The duration of treatment depends on

pathogen and can range from 4 days for Neisseria meningitidis up to 10-14 days for sensitive strains Enterobacteriaceae.

Children with infections of the skin and soft tissue - in a daily dose of 50-75 mg / kg once a day or 25-37.5 mg / kg every 12 hours, not more than 2 g / day.

In severe infections of other localization - 25-37.5 mg / kg every 12 hours, not more than 2 g / day.

At the average otitis media - in / m, once, 50 mg / kg, not more than 1 g.

In patients with CRF, dose adjustment is required only with QC below 10 ml / min. In that the daily dose should not exceed 2 g.

Rules for the preparation and administration of solutions:

Use only freshly prepared solutions!

For the / m introduction, 0.25 or 0.5 g of the drug is dissolved in 2 ml, and 1 g in 3.5 ml of 1% lidocaine solution. Recommend to enter no more than 1 g in one buttock.

For intravenous injection, 0.25 or 0.5 g is dissolved in 5 ml, and 1 g - in 10 ml of water for injections. Enter into / in slowly (2-4 minutes).

For intravenous infusions, dissolve 2 g in 40 ml of a solution that does not contain Ca2 + (0.9% solution NaCl, 5-10% dextrose solution, 5% solution of levulose). Doses of 50 mg / kg or more should be administered intravenously in drip, for 30 minutes.

Side effects:

Allergic reactions: fever, eosinophilia, skin rash, urticaria, skin itching, multiform exudative erythema, edema, anaphylactic shock, serum sickness, chills.

Local Reactions: with iv introduction - phlebitis, tenderness along the vein; w / m Introduction - soreness at the injection site.

From the nervous system: headache, dizziness.

From the urinary system: oliguria, impaired renal function.

From the digestive system: nausea, vomiting, taste disorder, flatulence, stomatitis, glossitis, diarrhea, constipation, pseudomembranous enterocolitis, stomach ache; pseudocholithiasis of the gallbladder ("sludge''-syndrome), candidamycosis and other superinfections.

From the hematopoiesis: anemia, leukopenia, leukocytosis, lymphopenia, neutropenia, granulocytopenia, thrombocytopenia, thrombocytosis, basophilia; nasal bleeding, hemolytic anemia.

Laboratory indicators: an increase (decrease) in prothrombin time, an increase in the activity of "hepatic" transaminases and alkaline phosphatase, hyperbilirubinemia, hypercreatininemia, increased urea concentration, hematuria, and glucosuria.

Overdose:Excessively high concentrations of ceftriaxone in the plasma can not be reduced by hemodialysis. 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.

NSAIDs and other inhibitors of platelet aggregation increase the chance 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:

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.

Studies in vitro have shown that, like other cephalosporin antibiotics ceftriaxone is able to displace bilirubin, associated with serum albumin. Therefore, in newborns with hyperbilirubinemia and, especially, in preterm infants, the use of ceftriaxone requires even greater caution.

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 cessation of treatment. Even if this phenomenon is accompanied by pain in the right hypochondrium, it is recommended to continue the appointment of an antibiotic and conduct symptomatic treatment.

During treatment, the use of ethanol is contraindicated - disulfiramoid-like effects are possible (flushing of the face,spasm in the abdomen and in the stomach, nausea, vomiting, headache, lowering blood pressure, tachycardia, dyspnea). Freshly prepared ceftriaxone solutions are physically and chemically stable for 6 hours at room temperature.

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

Form release / dosage:

Powder for the preparation of solution for intravenous and intramuscular injection 0.5 g, 1 g and 2 g.

Packaging:

Powder for the preparation of solution for intravenous and intramuscular injection of 0.5 g, 1 g and 2 g in bottles with a capacity of 10 ml or 20 ml.

1, 5 or 10 bottles with instructions for use in a pack of cardboard.

50 bottles with an equal number of instructions for use in a cardboard box for delivery to hospitals.

Solvent - "Water for injection" in glass ampoules of 5 ml.

1 bottle with the preparation, 1 or 2 ampoules with a solvent in a contoured cell pack from a polyvinyl chloride film. 1 contour pack with instructions for use and ampoule ampoule in a pack of cardboard.

When using ampoules with a kink ring or with a notch and a dot the ampoule scaper is not inserted.

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 the product after the expiry date printed on the package.

Terms of leave from pharmacies:On prescription

Registration number:P N000750 / 01

Date of registration:26.10.2007

The owner of the registration certificate:SYNTHESIS, OJSC SYNTHESIS, OJSC Russia

Manufacturer: & nbsp

SYNTHESIS, OJSC Russia

Information update date: & nbsp25.11.2015

Illustrated instructions

Instructions

Ceftriaxone (Ceftriaxone)