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Antiinfectives for Systemic Use

Rocilanem (Injections)
(Imipenem / Cilastatin)



CONTENT:
Vials. Vial contains imipenem 500 mg and cilastatin 500 mg or imipenem 250 mg and cilastatin 250 mg.
 
PHARMACOLOGICAL PROPERTIES:
PHARMACODYNAMICS. Imipenem/cilastatin is a broad spectrum antibiotic containing two components. Imipenem is a derivative of thienamycin, carbapenem. Imipenem inhibits bacterial cell wall synthesis and provides antimicrobial action against broad spectrum of gram-positive and gram-negative pathogens, both aerobic and anaerobic. Cilastatin is a specific enzyme inhibiting imepenem metabolism in kidneys and significantly increasing concentration of unchanged imipenem in urinary tract. Imipenem shows high resistance to the presence of p-lactamases, both penicillinases and cephalosporinases which are produced by gram-positive and gram-negative bacteria. Imipenem is a potent inhibitor of ^-lactamases produced by definite gram-negative bacteria such as Pseudomonas aeruginosa, Serratia spp. and Enterobacterspp., which show resistance to beta-lactam antibiotics. Imipenem has a more broad spectrum of action in comparison with other studied antibiotics. Imipinem shows both clinical activity and activity in vitro against most strains of microorganisms: gram-negative aerobes, gram-positive aerobes, anaerobes. Stenotrophomonas maltophilia and certain Burkholderia strains are not sensitive to the drug. In vitro tests show that Rocilanem has synergistic effect when used in combination with antibiotics belonging to the group of aminoglycosides against some isolates of Pseudomonas aeruginosa.
PHARMACOKINETICS. The highest concentrations are reached in pleural fluid, peritoneal and interstitial fluid and genital organs. It is found in low concentrations in cerebrospinal fluid. The volume of distribution in adults is 0.23-0.31 L/kg, in children aged 2-12 years - 0.7 L/kg and in newborns it is about 0.4-0.5 L/kg. Blocking of imipenem tubular secretion by cilastatin leads to inhibiting of its metabolism in kidneys and accumulation of unchanged drug in urine. Cilastatin is metabolized to N-acetyl conjugate. After intravenous administration imipenem and cilastatin elimination half-life (t1/2) in adults is 1 hour, in children aged 2-12 years - 1-1.2 hours. In new-borns: imipenem t1/2 - 1.7-2.4 hours, cilastatin t1/2 - 3.8-8.4 hours; in patients with renal impairment imipenem t1/2 is 2.9-4 hours and cilastatin t1/2 is 13.3-17.1 hours. The drug is excreted mainly by kidneys (70-76% during 10 hours) by glomerular filtration and active tubular secretion; 1-2% is excreted with faeces and 20-25% by extrarenal clearance (the mechanism is unknown).
 
THERAPEUTIC INDICATIONS:
- intra-abdominal infections;
- lower respiratory tract infections;
- gynecological and urinary tract infections;
- septicemia;
- bone and joint infections;
- skin and soft tissue infections;
- bacterial endocarditis;
- pelvic infections;
- mixed infections, hospital-acquired infections, including those caused by Bacteroides fragilis.
The prevention of postoperative infections in patients at high risk of development of such infections.
 
CONTRAINDICATIONS:
- hypersensitivity to the drug components;
- hypersensitivity to carbapenems and other beta-lactam antibiotics.
 
SIDE EFFECTS:
The drug is usually well tolerated. Clinical studies have shown that drug tolerance can be
compared to cefazolin, cefotaxim and cefalotin. Serious adverse effects are seldom
observed. Most adverse reactions develop slowly, last during short period of time and do
not require medical intervention.
 
DOSAGEAND ADMINISTRATION:
The drug is intended for intravenous administration.
The daily dose depends on the type and severity of infection. The dose is given in equally
divided doses throughout the day based on consideration of degree of susceptibility of
the pathogen, renal function and body weight. The recommended dosage for most
infection is 1-2 g per day given in 3 to 4 infusions. For infection with moderate severety
the dosage can be 1 g twice per day. The maximum
daily dose is 50 mg/kg/day or 4.0 g/day.
 
PACKAGING:
1 vial in an inner carton box.
 
 
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