ალიმენტური ტრაქტი და მეტაბოლიზმი
სისტემური გამოყენების ინფექციის საწინააღმდეგო
სისხლი და სისხლ-წარმომქმნელი ორგანოები
სამომავლოდ დაგეგმილი პროდუქტები
Antiinfectives for Systemic Use
Vials. Vial contains ceftriaxone (as sodium salt) 0.5 g /1.0 g /2.0 g.
PHARMACODYNAMICS. Rotacef is antibiotic of third generation of cephalosporins
with wide spectrum of action. It shows bactericidal action due to inhibition of
bacterial cellular wall synthesis. It is active against majority of gram-negative,
many gram-positive pathogens and some anaerobes. It is resistant to action of
beta-lactamases, produced by bacteria. Many strains of above mentioned organisms,
which persistently prolifirate in presence of other antibiotics, for example,
penicillins, second generations of cephalosporins, and aminoglycosides, are
susceptible to Rotacef. Ceftriaxone is drug of choice for many infections caused
by gram-negative bacteria. Good effectiveness against primary and secondary
syphilis of the preparation is noted on the basis of clinical data.
PHARMACOKINETICS. The bioavailability after intramuscular administration is
100%. Maximum concentration in blood plasma is achieved within 2-3 hours after
intramuscular administration. It reversibly binds to plasma albumins by 85-95%,
and the binding is inverse as its blood concentration. Half-life period is long
and makes 8 hours in adults, it becomes 2 times longer in elderly people at the
age more than 75 years, it is 6.5 - 8 days in infants. 50-60% of Rotacef is
excreted in unchanged form with urine, 40-50% with bile. In newborn about 70% of
administered Rotacef dose is excreted by kidneys. Ceftriaxone is widely
distributed into body tissues and fluids including the gallbladder, lungs, bone,
heart, bile, prostate adenoma tissue, uterine tissue, appendix, sputum, tears,
middle ear fluid, and pleural, peritoneal, synovial, ascitic, and blister fluids.
Rotacef pharmacokinetics doesn't change at renal or hepatic function impairments
(not significant half-life period prolongation is possible) due to
redistribution of functions: if the renal function is impaired, bile excretion
increases, at liver pathology-renal excretion increases.
- respiratory tract infections (pneumonia, lung abscess, pleural empyema);
- infections of abdominal organs (including cholangitis,
gallbladder empyema, inflammatory diseases of gastrointestinal tract,
- bones and joints infections;
- skin and soft-tissues infections;
- urinary tracts infections (including pyelonephritis);
- sexually-transmitted infections (including gonorrhea);
- infected wounds and burns;
- meningitis, sepsis;
- prophylaxis of post-operational infections;
- ceftriaxone is used for the treatment of native valve or prosthetic valve
endocarditis caused by viridans streptococci.
hypersensitivity to cephalosporins and penicilins;
first trimester of pregnancy;
the drug should be prescribed with care to newborn babies especially to
premature children due to high risk of hyperbilirubinemia development.
Rotacef is well tolerated in most cases. Adverse effects, as a rule, are
disappear after the preparation cancellation.
DOSAGE AND ADMINISTRATION:
Rotacef is administered intramuscularly and intravenously.
For newborn (before two weeks) Rotacef is prescribed at a dose 20-50 mg/kg of
body weight one time per day. For infants and children at the age before 12
years Rotacef daily dose is 20-80 mg/kg of body weight 1 time per day. Usual
adult doses are used for children with body mass of 50 kg and more. Usual doses
for adults and children at the age of 12 years and older are 1-2 g of Rotacef
one time per day. In severe cases daily dose may be increased to 4 g. During
treatment of gonorrhea the recommended single dose is 250 mg of Rotacef
intramuscularly. In patients with renal function impairments hepatic function
impairments it is not necessary to reduce preparation dose. In case of expressed
renal insufficiency (creatinine clearance <10 ml/min) Rotacef dose should not
exceed 2 g per day. For the prophylaxis of post-operational infections single
administration of 1-2 g of Rotacef 30-90 minutes before operation is recommended.
1 vial with powder for the preparation of injection solution and 1 ampoule with
solvent in carton box with leaflet.
Rotacef 0.5 g, or 1.0 g. 10 vials in contour cellular package. 1 contour
cellular package in carton box with leaflet.