Ceftriaxone powder for injection 1000mg bottle №1

Active ingredient and dosage form

Powder for solution for injection white or white with a yellowish tint color.
1 vial contains Ceftriaxone (in the form of disodium salt) 500 mg, 1 or 2 g;

Bottles of 10 ml; 1, 5, 10 or 50 bottles in a box;
Bottles of 20 ml; 1, 5, 10 or 50 bottles in a box.

Mechanism of action

Cephalosporin antibiotic III generation broad-spectrum. Effective bactericidal, inhibiting the synthesis of the cell membrane of microorganisms. In vitro inhibits the growth of most gram-positive and gram-negative bacteria. Resistant to b-lactamase.
Active against gram-positive aerobic bacteria: Staphylococcus aureus, Staphylococcus epidermidis, Streptococcus pneumoniae, Streptococcus pyogenes, Streptococcus agalactiae, Streptococcus viridans, Streptococcus bovis; Gram-negative aerobic bacteria: Aeromonas spp., Alcaligenes spp., Branhamella catarrhalis (forming and non-forming beta-lactamase), Citrobacter spp., Enterobacter spp., (Some strains are resistant), Escherichia coli, Haemophilus ducreyi, Haemophilus influenzae (es), (Escherichia coli, Haemophilus ducreyi, Haemophilus influenzae). penicillinase), Haemophilus parainfluenzae, Klebsiella spp. (Including Klebsiella pneumoniae), Moraxella spp., Morganella morganii, Neisseria gonorrhoeae (including strains producing penicillinase), Neisseria meningitidis, Plesiomonas shigelloides, Proteus mirabilis, Proteus vulgaris, Providencia spp., Salmonella spp. (including Salmonella typhi), Serratia spp. (including Serratia marsescens), Shigella spp., Vibrio spp. (including Vibrio cholerae), Yersinia spp. (including Yersinia enterocolitica), Pseudomonas aeruginosa (some strains); anaerobic bacteria: 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.
To drug are resistant methicillin-resistant strains of Staphylococcus spp., Enterococcus spp., Bacteroides fragilis (strains producing b-lactamases).

Suction
When administered parenterally, ceftriaxone penetrates well into tissues and body fluids. The bioavailability of ceftriaxone when i / m administration is 100%. After i / m administration C_max is achieved in 2-3 hours. When inflammation of the meningeal membranes penetrates well into the cerebrospinal fluid.
C_max with intramuscular administration of ceftriaxone in a dose of 50 mg / kg in the blood plasma is 216 mcg / ml, in the cerebrospinal fluid - 5.6 mcg / ml. In adults, 2–24 hours after administration of the drug at a dose of 50 mg / kg, the concentration in the cerebrospinal fluid many times exceeds the minimum inhibitory concentrations for the most common causative agents of meningitis.
Distribution and elimination
Plasma protein binding - 85%.
V_d 5.78-13.5 l.
T_1/2 - 5.8-8.7 h, plasma clearance - 0.58-1.45 l / h, renal clearance - 0.32-0.73 l / h.
In adult patients, 50-60% of the drug is excreted in the urine within 48 hours in the active form, partly with bile.
In newborns, approximately 70% of the administered dose is excreted by the kidneys.
Pharmacokinetics in special clinical situations
In newborns up to 8 days and in elderly people over the age of 75 years T_1/2 increases about 2 times.
In renal insufficiency, excretion slows down.

Bacterial infections caused by susceptible microorganisms:
- peritonitis;
- sepsis;
- meningitis;
- infections of the abdominal organs (inflammatory diseases of the gastrointestinal tract, biliary tract, including cholangitis, empyema of the gall bladder);
- diseases of the upper and lower respiratory tract (including pneumonia, lung abscess, pleural empyema);
- infections of bones and joints;
- infections of the skin and soft tissues;
- urinary tract infections (including pyelonephritis);
- gonorrhea;
- infected wounds and burns.
Prevention of postoperative infection.
Infectious diseases in immunocompromised persons.

Contraindications

- hypersensitivity to ceftriaxone;
- pregnancy (I term).

Dosage and administration

The drug is administered in / m or / in (jet or drip).
For adults and children over 12 years old the average daily dose is 1-2 g ceftriaxone 1 time / day.
In severe cases or in cases of infections caused by moderately sensitive pathogens, daily dose can be increased to 4 g (2 g 2 times / day).
For newborns (up to two weeks of age) the dose is 20-50 mg / kg / day.
For babies and children up to 12 years the daily dose is 20-80 mg / kg.
In children with a body weight of 50 kg and more apply doses for adults.
A dose of more than 50 mg / kg of body weight should be prescribed in the form of intravenous infusion (drip). The duration of treatment depends on the nature of the disease.
With bacterial meningitis in infants and young children The initial dose is 100 mg / kg 1 time / day. The maximum daily dose - 4 g.
For the treatment of acute gonorrhea the dose is 250 mg, once in / m.
For the prevention of infections in the preoperative and postoperative periods 30-90 minutes before the operation, 1-2 g of ceftriaxone are injected.
In renal failure (creatinine clearance less than 10 ml / min) Ceftriaxone daily dose should not exceed 2 g.
When expressed violations of the liver and kidneysas well as patients on hemodialysis, it is necessary to monitor the concentration of ceftriaxone in the blood plasma, since they may decrease the rate of its release.

For intramuscular administration, 1 g of the drug is diluted in 3.5 ml of 1% Lidocaine solution and injected deep into the gluteus muscle.
For iv administration, the contents of one vial are diluted in 10 ml of sterile distilled water and injected slowly over 2-4 minutes.
For intravenous infusion, 2 g of the powder is diluted in 40 ml of 0.9% sodium chloride solution, 0.45% sodium chloride solution containing 2.5% glucose, in 5% glucose solution, in 10% glucose solution, 5% fructose solution, in 6% solution dextran. Duration of intravenous infusion is at least 30 minutes.

Allergic reactions: about 1% - urticaria, fever, chills, eosinophilia, rash, pruritus, exanthema, allergic dermatitis, exudative erythema multiforme, edema, anaphylactic shock.
Gastrointestinal: nausea, vomiting, stomatitis, glossitis, diarrhea, pseudomembranous enterocolitis, cholestasis, increased activity of hepatic transaminases, hyperazotemia, hypercreatininemia, increased urea.
From the side of the central nervous system: headache, dizziness.
Hemic and lymphatic: leukopenia, neutropenia, granulocytopenia, thrombocytopenia, hemolytic anemia.
Local reactions: with a / in the introduction - phlebitis, pain along the vein, with a / m injection - pain at the injection site.
Other: superinfection (including candidosis, mycosis of the genital organs); oliguria, hypocoagulation.

Pregnancy and breastfeeding

The drug is contraindicated for use in the first trimester of pregnancy. When prescribed during lactation, breastfeeding should be canceled.

Cautions

With caution, the drug is prescribed to newborns (including premature babies) in connection with a high risk of developing hyperbilirubinemia and ulcerative colitis.
With simultaneous severe renal and hepatic insufficiency, it is necessary to regularly determine the concentration of the drug in the blood plasma.
With long-term treatment, it is necessary to regularly monitor the picture of peripheral blood, indicators of the functional state of plasma and kidneys.
In rare cases with ultrasound of the gallbladder, there are blackouts that disappear after withdrawal (even if this phenomenon is accompanied by pain in the right hypochondrium, it is recommended to continue the prescription of the antibiotic and symptomatic treatment).

Currently, cases of an overdose of Ceftriaxone have not been reported.

Ceftriaxone and aminoglycosides possess synergism against many gram-negative bacteria.
Concurrent administration with Metronidazole, fluoroquinolones, Vancomycin, rifampicin is possible (but not in the same syringe).
With simultaneous use with loop diuretics (eg, furosemide), renal impairment is not observed.
Pharmaceutical Interaction
Pharmaceutically incompatible with solutions containing other antibiotics.

List B. The drug should be stored in a dry, dark place at a temperature of 15-25 ° C.

2 years.
Freshly prepared ceftriaxone solutions are physically and chemically stable for 6 hours at room temperature and for 24 hours when stored in a refrigerator at a temperature of 2 ° to 8 ° C.
Pharmacy sales terms
The drug is available on prescription.