scholarly journals Bronchopulmonary Disposition of the Ketolide Telithromycin (HMR 3647)

2001 ◽  
Vol 45 (11) ◽  
pp. 3104-3108 ◽  
Author(s):  
Claudette Muller-Serieys ◽  
Paul Soler ◽  
Cathy Cantalloube ◽  
Françoise Lemaitre ◽  
Hai Pham Gia ◽  
...  

ABSTRACT Telithromycin (HMR 3647) is the first member of a new family of antimicrobials, the ketolides, developed specifically for the treatment of community-acquired respiratory tract infections. Telithromycin has proven in vitro activity against both common and atypical respiratory tract pathogens. The penetration of telithromycin into bronchopulmonary tissues and subsequent elimination from these sites were evaluated in four groups (groups A, B, C, and D) of six healthy male subjects who received telithromycin at 800 mg once daily for 5 days. Subjects in groups A, B, C, and D underwent fiberoptic bronchoscopy and bronchoalveolar lavage 2, 8, 24, and 48 h after receipt of the last dose, respectively. The concentration of telithromycin in the alveolar macrophages, epithelial lining fluid (ELF), and plasma was determined by the agar diffusion method with Bacillus subtilis ATCC 6633 as the test organism. The concentration of telithromycin in alveolar macrophages markedly exceeded that in plasma, reaching up to 146 times the concentration in plasma 8 h after dosing (median concentration, 81 mg/liter). Telithromycin was retained in alveolar macrophages 24 h after dosing (median concentration, 23 mg/liter), and it was still quantifiable 48 h after dosing (median concentration, 2.15 mg/liter). Telithromycin median concentrations in ELF also markedly exceeded concentrations in plasma (median concentration in ELF, 3.7 mg/liter 8 h after dosing). Telithromycin achieves high and sustained concentrations in ELF and in alveolar macrophages, while it maintains adequate levels in plasma, providing an ideal pharmacokinetic profile for effective treatment of community-acquired respiratory tract infections caused by either common or atypical, including intracellular, respiratory tract pathogens.

2003 ◽  
Vol 47 (8) ◽  
pp. 2703-2705 ◽  
Author(s):  
Saskia Priebe ◽  
Stefan Schwarz

ABSTRACT Florfenicol in vitro activities for a total of 756 bacterial isolates from respiratory tract infections of cattle and swine were comparatively investigated by the agar diffusion method and the microdilution broth method. Florfenicol showed high in vitro activity against Pasteurella multocida, Mannheimia haemolytica, Actinobacillus pleuropneumoniae, and Streptococcus suis, with all of the isolates inhibited by ≤2 μg of florfenicol per ml.


2021 ◽  
Vol 7 (1) ◽  

Respiratory tract infections (RTIs) are the most common and severe infectious diseases in developing countries. Acinetobacter baumannii is the bacterium known as causative organism for respiratory tract infections in human populations. The Report suggests that co-infection of Acinetobacter baumannii with Mycobacterium tuberculosis together increases health complications in multidrug resistant tuberculosis (MDR-TB) positive patients and creates fatal damage to the ailing population. In our study, 106 sputum samples of MDR-TB positive patients from Northern Punjab were studied. The isolation of A. baumannii from sputum of MDR-TB patients was done on selective media and initially screened by Oxidase and Catalase based identification followed by microscopic examination. Afterward, only ten suspected isolates of A. baumannii were again selected for further characterization for MDR by using Disc diffusion method. Antibiograms against number of antibiotics were accurately determined. Of these 10 isolates, 8 sample were found resistant to levofloxacin and subjected to molecular characterization using bla-OXA-51 primers. Only 3 out of 106 (2.83 %) isolates were confirmed as MDR strains of A. baumannii. These results show the coexistence of MDR A. bauminnii with MDR-TB patients of Northern Punjab, Pakistan. In Northern Punjab regions a higher percentage (3 cases) of MDR- TB were detected, which were co-infected with Acinetobacter baumannii among hospitalized patients. These findings may show unhygienic hospital environment or practices which leads to the co-infection.


2002 ◽  
Vol 36 (3) ◽  
pp. 452-464 ◽  
Author(s):  
Christopher S Shain ◽  
Guy W Amsden

OBJECTIVE: To review the chemistry, spectrum of activity, pharmacology, clinical efficacy, and safety of telithromycin. DATA SOURCES: A MEDLINE search from 1966 to December 2000 was performed via OVID and PubMed using the following search terms: HMR 3647, HMR3647, Ketek, RU 66647, and telithromycin. An extensive review of retrieved literature, abstracts from international scientific conferences, and minutes from regulatory authority meetings was also performed. DATA EXTRACTION: Medicinal chemistry, in vitro, animal, and human trials were reviewed for information on the antimicrobial activity, clinical efficacy, pharmacology, and safety of telithromycin. DATA SYNTHESIS: Several chemical modifications to the macrolide structure have led to the development of telithromycin, the first ketolide antimicrobial that demonstrates improved activity against penicillin- and macrolide/azalide-resistant Streptococcus pneumoniae due to its unique binding to the ribosomal target site. Although telithromycin may be useful in the treatment of community-acquired respiratory tract infections due to its activity against common typical and atypical pathogens, questions concerning its reliable activity against Haemophilus influenzae need to be addressed. Telithromycin's pharmacokinetics permit once-daily dosing for abbreviated periods and good distribution into lung tissue and phagocytic cells. Clinical and bacteriologic cure rates have been similar to those of comparator agents in human efficacy trials; however, the incidence of adverse gastrointestinal events were generally higher with telithromycin patients. Like other macrolides and many newer fluoroquinolones, telithromycin's ability to prolong the QTc interval is a potential safety issue, especially in elderly patients with predisposing conditions or those who are concurrently receiving drugs that are substrates for CYP2D6 and 3A4. Liver function test elevations demonstrated during clinical trials, although not overtly severe, may warrant monitoring in some patients taking multiple hepatically metabolized/cleared agents. CONCLUSIONS: Telithromycin offers potential advantages over traditional macrolides/azalides for community-acquired respiratory tract infections caused by macrolide-resistant pathogens. Further studies are needed to elucidate its clinical efficacy against H. influenzae, potential drug interactions, and safety in various subpopulations.


2018 ◽  
Vol 159 (1) ◽  
pp. 23-30
Author(s):  
Emese Juhász ◽  
Miklós Iván ◽  
Júlia Pongrácz ◽  
Katalin Kristóf

Abstract: Introduction: Glucose non-fermenting Gram-negative bacteria are ubiquitous environmental organisms. Most of them are identified as opportunistic, nosocomial pathogens in patients. Uncommon species are identified accurately, mainly due to the introduction of matrix-assisted laser desorption-ionization time of flight mass spectrometry (MALDI-TOF MS) in clinical microbiology practice. Most of these uncommon non-fermenting rods are isolated from lower respiratory tract samples. Their significance in lower respiratory tract infections, such as rules of their testing are not clarified yet. Aim: The aim of this study was to review the clinical microbiological features of these bacteria, especially their roles in lower respiratory tract infections and antibiotic treatment options. Method: Lower respiratory tract samples of 3589 patients collected in a four-year period (2013–2016) were analyzed retrospectively at Semmelweis University (Budapest, Hungary). Identification of bacteria was performed by MALDI-TOF MS, the antibiotic susceptibility was tested by disk diffusion method. Results: Stenotrophomonas maltophilia was revealed to be the second, whereas Acinetobacter baumannii the third most common non-fermenting rod in lower respiratory tract samples, behind the most common Pseudomonas aeruginosa. The total number of uncommon non-fermenting Gram-negative isolates was 742. Twenty-three percent of isolates were Achromobacter xylosoxidans. Beside Chryseobacterium, Rhizobium, Delftia, Elizabethkingia, Ralstonia and Ochrobactrum species, and few other uncommon species were identified among our isolates. The accurate identification of this species is obligatory, while most of them show intrinsic resistance to aminoglycosides. Resistance to ceftazidime, cefepime, piperacillin-tazobactam and carbapenems was frequently observed also. Conclusions: Ciprofloxacin, levofloxacin and trimethoprim-sulfamethoxazole were found to be the most effective antibiotic agents. Orv Hetil. 2018; 159(1): 23–30.


2002 ◽  
Vol 46 (4) ◽  
pp. 1117-1118 ◽  
Author(s):  
R. Wise ◽  
J. M. Andrews ◽  
J. Ashby

ABSTRACT The activities of six peptide deformylase (PDF) inhibitors against 107 respiratory tract pathogens were studied and compared to those of ciprofloxacin and amoxicillin-clavulanate. Against Streptococcus pneumoniae, BB-83698 and BB-83815 were the most active PDF inhibitors (MIC at which 90% of the organisms tested were inhibited [MIC90], 0.25 μg/ml). Five of the agents showed similar activity against Moraxella catarrhalis (MIC90, 0.12 μg/ml). All PDF inhibitors were less active against Haemophilus influenzae; BB-3497 was the most active agent (MIC90, 2 μg/ml). Five agents were studied against Chlamydia spp. and showed activity similar to that of ciprofloxacin (MIC, 0.5 to 4 μg/ml). This study demonstrates that PDF inhibitors have the potential to be developed for the treatment of respiratory tract infections.


2013 ◽  
Vol 6 ◽  
pp. MBI.S12996 ◽  
Author(s):  
Makhtar Camara ◽  
Assane Dieng ◽  
Cheikh Saad Bouh Boye

Group A Streptococcus (GAS) is one of the major causes of respiratory tract infections. The objectives of this study were to identify isolates of S. pyogenes obtained from respiratory tract infections, and to assess their susceptibility to several antibiotics. A total of 40 strains were isolated and their susceptibility to 17 antibiotics was tested using a standard disk diffusion method. The minimum inhibitory concentrations (MICs) were determined using the E-test. All isolates were sensitive to β-lactam antibiotics including penicillin, amoxicillin, and cephalosporins. Macrolides remain active with the exception of spiramycin, which showed reduced susceptibility. Out of the 40 isolates, 100% of the isolates were resistant to tetracycline. Interestingly, isolates were sensitive to chloramphenicol, teicoplanin, vancomycine, and levofloxacin, providing potential alternative choices of treatment against infections with S. pyogenes.


Sign in / Sign up

Export Citation Format

Share Document