Expiration date: 08/2025

Structure and Composition: 

Powder for solution for intravenous and intramuscular administration of 1 vial.

ceftriaxone (ceftriaxone in the form of disodium trisekvihydrate) 1000 mg

a stack of cardboard 10 vials.

Description pharmaceutical form:

The powder is white to yellowish-white in color.

Characteristic:

Cephalosporin antibiotic III generation broad-spectrum.

Pharmacokinetics:

After the / m of rapidly and completely absorbed. Bioavailability - 100%. It penetrates the tissues and fluids of the body: the respiratory tract, bone and joints, urinary tract, skin, subcutaneous tissue and abdominal organs. The stable blood concentration of the drug is achieved within 4 days. Cmax after the / m achieved in 2-3 hours after the on / in the - at the end of infusion. Cmax after the / m at a dose of 0.5 g - 38 ug / ml 1 g - 76 pg / ml at / in a dose of 500 mg - 82 g / ml 1 g - 151 mg / ml, 2 g - 257 ug / ml. It penetrates into the cerebrospinal fluid when the meninges are inflamed. In adults over 2-24 hours after administration of 50 mg / kg concentration in the cerebrospinal fluid many times greater than the MIC for the most common causes of meningitis. Reversibly bound to plasma albumin (83-59%). T1 / 2 of 6-9 hours, allowing one to use the drug once a day. T1 / 2 after i / in a dose of 50-75 mg / kg in children with meningitis - 4.3-4.6 hours in patients on hemodialysis (creatinine Cl - 0-5 ml / min) - 14.7 Cl creatinine hours at 5-15 ml / min - 15.7 h 16-30 ml / min - 11.4 h 31-60 ml / min - 12.4 hours.

The volume of distribution - 0,12-0,14 l / kg (5,78-13,5 l) in children - 0.3 l / kg, plasma Cl - 0,58-1,45 l / h, kidney - 0,32-0,73 l / h.

T1 / 2 significantly lengthened in people over 75 years of age, infants and patients with impaired renal and hepatic function. Displayed in the kidney for 48 hours - 50-60%, in an unmodified form and with bile - 40-50% in the intestine, where the transformation into an inactive metabolite. In newborn infants, is excreted through the kidneys approximately 70% of the drug. It does not appear in hemodialysis.

Description of the pharmacological actions:

It has bactericidal activity by inhibiting bacterial cell wall synthesis. Acetylated membrane-bound transpeptidase, violating thus crosslinks peptidoglycans necessary to provide strength and rigidity of the cell wall.

It is resistant to beta-lactamases produced by most gram-positive and gram-negative bacteria.

Active against gram-positive aerobes - Staphylococcus aureus, Staphylococcus epidermidis, Streptococcus pneumoniae, Streptococcus pyogenes, Streptococcus agalactiae, Streptococcus viridans, Streptococcus bovis aerobic Gram - Aeromonas spp, Alcaligenes spp, Branhamella catarrhalis (including strains beta form.. lactamase), Citrobacter spp., Enterobacter spp. (Some resistant strains), Escherichia coli, Haemophilus ducreyi, Haemophilus influenzae (including strains forming penicillinase), Haemophilus parainfluenzae, Klebsiella spp., (Including Klebsiella pneumoniae), Moraxella spp., Morganella morganii, Neisseria gonorrhoeae (including strains forming penicillinase), Neisseria meningitidis, Plesiomonas shigelloides, Proteus mirabilis, Proteus vulgaris, Providencia spp., Salmonella spp. (Including Salmonella typhi), Serratia spp. (Including Serratia marcescens), Shigella spp., Vibrio spp. (Including Vibrio cholerae), Yersinia spp. (Including Yersinia enterocolitica), Pseudomonas aeruginosa anaerobes - Bacteroides spp. (Including some strains of Bacteroides fragilis), Clostridium spp. (Except Clostridium difficile), Fusobacterium spp. (Except Fusobacterium mortiferum and Fusobacterium varium), Peptococcus spp., Peptostreptococcus spp.

Ceftriaxone resistant strains of Staphylococcus spp., Methicillin-resistant strains of Enterococcus spp. (Enterococcus faecalis), Clostridium difficile, many strains of Bacteroides spp., Producing beta-lactamases.

Not hydrolyzed R-plasma beta-lactamases, and a majority hromosomooposredovannyh penicillinases cephalosporinase and can act on the multidrug strains tolerant to penicillins and first-generation cephalosporins and aminoglycosides. Acquired resistance of certain strains of bacteria caused by the production of beta-lactamase inactivates ceftriaxone ( "tseftriaksonazy").

Testimony:

• Infectious-inflammatory diseases caused by susceptible to malaria infections:
  
• infections of the upper and lower respiratory tract (including pneumonia, lung abscess, empyema)
  
• skin and soft tissue infections
  
• bone and joint infections
  
• Urinary tract infections (including pyelonephritis)
  
• abdominal infections (peritonitis, inflammatory diseases of the gastrointestinal tract, biliary tract, including cholangitis, gallbladder empyema)
  
• infectious and inflammatory diseases of the pelvic organs
  
• prevention and treatment of infections in surgical interventions
  
• bacterial meningitis and endocarditis
  
• sepsis
  
• acute and complicated gonorrhea
  
• Lyme disease, shigellosis, salmonellosis.
  

Contraindications:

Hypersensitivity to ceftriaxone and other cephalosporins, penicillins, carbapenems.

Carefully:

• disruption of the liver and / or kidney (probability cumulation requires monitoring drug concentration in serum)
  
• in premature and newborn infants with hyperbilirubinemia (probability of gain manifestations)
  
• ulcerative colitis, enteritis or colitis associated with the use of antibacterial drugs.
  

Application of pregnancy and breastfeeding:

Perhaps if the expected effect of therapy outweighs the potential risk to the fetus (passes through the placenta). At the time of treatment should stop breastfeeding (excreted in breast milk).

Side effect:

Allergic reactions: urticaria, rash, pruritus, erythema multiforme exudative, fever, edema, eosinophilia, anaphylaxis, serum sickness, abdominal pain, bronchospasm.

From the nervous system: headache, dizziness.

From the urinary system: oliguria.

From the digestive system: nausea, vomiting, taste disturbance, flatulence, stomatitis, glossitis, diarrhea, pseudomembranous enterocolitis, psevdoholelitiaz gallbladder ( «sludge» -sindrom), goiter.

From the side of blood: anemia, leukopenia, leukocytosis, lymphopenia, neutropenia, granulocytopenia, thrombocytopenia, thrombocytosis, basophilia.

On the part of the hemostatic system: hematuria, epistaxis, hemolytic anemia.

Local reactions: with a / in the introduction - phlebitis, pain along the vein with the / m - pain at the injection site.

Other: candidiasis and other superinfection.

Laboratory indicators: increase (decrease) MF, increase in liver transaminases, alkaline phosphatase, hyperbilirubinemia, hypercreatininemia, increased urea, glycosuria.

Drug Interactions:

Ceftriaxone and aminoglycosides have synergistic against many gram-negative bacteria. Incompatible with ethanol. NSAIDs and other platelet aggregation inhibitors increase the chance of bleeding. While the use of loop diuretics and other risk of nephrotoxic effect increases nephrotoxic drugs. Pharmaceutically compatible with solutions containing other antibiotics.

Dosage and administration:

Preparation of solution / m administration: 1000 mg dissolved in 3.5 ml of a 1% solution of lidocaine hydrochloride.

V / m (in deep muscle). Do not enter more than 1000 mg in one muscle. You can not enter the solution of lidocaine hydrochloride / O.

Preparation of the solution for the on / in: 1000 mg dissolved in 9.6 ml of sterile water for injection.

B / by injection lasting 2-4 min.

Preparation of the infusion solution: 2 g of the drug is dissolved in 40 ml of a solution containing no calcium (0.9% sodium chloride, 0.45% chloride, 2.5% sodium solution or dextrose solution, 5% dextrose 10 6 % dextran solution in 5% dextrose, 10.6% HES, water for injection).

In / in infusion for at least 30 min.

Freshly prepared solutions Azarana stable for 6 hours at room temperature, and 24 hours - at 2-8 ° C.

standard dosing

Adults and children over 12 years, the usual dose is 1-2 g every 24 hours maximum daily dose for adults -. 4 years

Aged newborn to 14 days - 20-50 mg / kg one time a day. The maximum daily dose - not more than 50 mg / kg.

Children aged from 15 days to 12 years - 20-80 mg / kg, 1 time per day. B / in a dose equal to or greater than 50 mg / kg should be employed as infusion.

Course duration - no more than 10 days. The introduction of the drug is recommended to continue for another 2-3 days after normalization of body temperature and the disappearance of symptoms.

To prevent postoperative complications - once, 2.1 g (depending on the degree of danger of infection) 30-90 minutes prior to surgery. In operations on the colon recommend an additional injection of the drug from the group of 5-nitroimidazoles.

Bacterial meningitis - 100 mg / kg (but not more than 4 g) 1 time per day. The duration of treatment depends on the pathogen, and may vary from 4 days to Neisseria meningitidis to 10-14 days for sensitive Enterobacteriaceae strains.

Infections of skin and soft tissues: for children - 50-75 mg / kg / day once a day one or 25-37,5 mg / kg every 12 hours, but not more than 2 g / day. In severe infections at other sites - 25-37,5 mg / kg every 12 hours, but not more than 2 g / day. In otitis media - once in / m to 50 mg / kg, but no more than 1 year

Patients with renal impairment (Cl creatinine <10 ml / min) daily dose should not exceed 2 g

Gonorrhea - / m mono-, 250 mg.

Precautionary measures:

In simultaneous severe renal and hepatic impairment, in patients on hemodialysis, should be regularly to determine the concentration of drug in plasma.

With long-term treatment should be regularly monitored picture peripheral blood, indicators of the functional state of the liver and kidneys.

In rare cases, ultrasound gallbladder marked darkening, which disappear after cessation of treatment. Even if this phenomenon is accompanied by pain in the right upper quadrant, it is recommended to continue the use of the antibiotic and symptomatic therapy.

During treatment contraindicated use of ethanol (disulfiramopodobnye possible effects - redness of the face, abdominal cramps and in the stomach, nausea, vomiting, headache, decreased blood pressure, tachycardia, shortness of breath).

Elderly or debilitated patients the appointment of vitamin K may be required

Special instructions:

Preparation of the solution for the / m: 250 mg are dissolved in 1 ml of 0.9% lidocaine hydrochloride, 1,000 mg - 3.5 ml.

Do not enter more than 1000 mg in one muscle. You can not enter the solution of lidocaine hydrochloride / O.

Preparation of the solution for the on / in the 250 mg dissolved in 2.4 ml of sterile water for injection, 1000 mg - 9.6 ml.

Preparation of the solution for I / infusion: 2 g of the drug is dissolved in 40 ml of a solution containing no calcium (0.9% chloride and 2.5% sodium chloride, 0.45% sodium dextrose solution or 5% dextrose 10 6% dextran solution in 5% dextrose 6-10% HES solution water for injection).

Freshly prepared solutions Azarana stable for 6 hours at room temperature and for 24 hours at 2-8 ° C.

The following shall apply only in a hospital.