Activities of 16-membered ring macrolides and telithromycin against different genotypes of erythromycin-susceptible and...
OBJECTIVES: To test four 16-membered macrolides (josamycin, spiramycin, midecamycin and rokitamycin) along with other compounds in the same class (erythromycin, clarithromycin, roxithromycin and azithromycin) plus clindamycin and telithromycin, against Streptococcus pyogenes and Streptococcus pneumoniae isolates with well-characterized resistance genotypes. METHODS: Four hundred and eighty-six isolates of S. pyogenes and 375 isolates of S. pneumoniae were assayed for their macrolide susceptibilities and investigated by PCR to detect their different erythromycin resistance genes. All strains had been isolated over the period 2002-2003 from specimens of different human origin obtained in 14 different Italian centres. RESULTS: All 16-membered macrolides showed very low MICs (MIC(50)s and MIC(90)s, , or =0.06-0.5 mg/L) for the erythromycin-susceptible isolates and for those with the M phenotype, but the telithromycin MICs for the M-type isolates ...https://pubblicazioni.unicam.it/handle/11581/235334
Resistance to Macrolides and Lincosamides | cmpt
Lincosamides specifically inhibit the peptidyl transferase reaction while macrolides block the exit tunnel inducing premature dissociation of peptidyl-tRNAs from the ribosome. (3,4). The binding sites for macrolides and lincosamide antibiotics lay in or near the active site of the peptide bond formation called peptidyl transferase center (PTC). (3) Because the binding sites for macrolides and lincosamides overlap, modification of any of these binding sites usually confers cross resistance to these antibiotics. (4,5). Spectrum of activity. Macrolides are active against gram positive bacteria and are effective against many of the pathogens associated with sexually transmitted diseases: Neisseria gonorrhoeae, Haemophilus ducreyi, Chlamydia trachomatis, and Ureaplasma urealyticum.. Gram negative bacilli are generally resistant; some exceptions include Bordetella perstusis, Campylobacter, ...http://cmpt.ca/resistance-to-macrolides-and-lincosamides/
Overview: Macrolides possess diverse natural activities and an capability to modulate - How NF-B is activated: the role of the...
90% after the widespread use of chronic erythromycin therapy (157). The characteristics of the clinical response to macrolide therapy are summarized as follows (71 157 202 258 (i) it takes up to 3 months of therapy for macrolides to show a significant effect; (ii) doses that are much lower than the MIC (i.e. low-dose macrolide therapy) are effective; (iii) the effect is seen even when patients are infected with macrolide-resistant bacteria such as (214) Mouse monoclonal to CD152(FITC). and (241 290 Clarithromycin has been shown to improve the transportability of secretions in human subjects (241 290 This mucoregulatory effect is seen even Aliskiren hemifumarate when hypersecretion is not induced by bacteria. Improved mucus transport may be associated with changes in the biophysical properties of secretions as well as with reduced inflammation. Ion transport. Tamaoki and coworkers (289) studied the effects of ...http://cancercurehere.com/?p=2115
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Antimicrobial drug use and macrolide-resistant **Streptococcus pyogenes**, Belgium - Institutional Repository University of...
In Belgium, decreasing macrolide, lincosamide, streptogramins B, and tetracycline use during 19972007 correlated significantly with decreasing macrolide-resistant Streptococcus pyogenes during 19992009. Maintaining drug use below a critical threshold corresponded with low-level macrolide-resistant S. pyogenes and an increased number of erm(A)-harboring emm77 S. pyogenes with low fitness costs. ...https://repository.uantwerpen.be/link/irua/101027
Table 1 - Macrolide Resistance in Adults with Bacteremic Pneumococcal Pneumonia - Volume 12, Number 8-August 2006 - Emerging...
We conducted a case-control study of adults with bacteremic pneumococcal pneumonia to identify factors associated with macrolide resistance. Study participants were identified through population-based surveillance in a 5-county region surrounding Philadelphia. Forty-three hospitals contributed 444 patients, who were interviewed by telephone regarding potential risk factors. In multivariable analyses, prior exposure to a macrolide antimicrobial agent (odds ratio [OR] 2.8), prior flu vaccination (OR 2.0), and Hispanic ethnicity (OR 4.1) were independently associated with an increased probability of macrolide resistance, and a history of stroke was independently associated with a decreased probability of macrolide resistance (OR 0.2). Fifty-five percent of patients with macrolide-resistant infections reported no antimicrobial drug exposure in the preceding 6 months. Among patients who reported taking antimicrobial agents in the ...https://wwwnc.cdc.gov/eid/article/12/8/06-0017-t1
Total synthesis of altohyrtin A (spongistatin 1): an alternative synthesis of the CD-spiroacetal subunit.
The CD-spiroacetal contg. C16-C28 subunit I, as used in the total synthesis of the potent cytotoxic macrolide altohyrtin A (spongistatin 1), was prepd. by an alternative route using substrate-based stereocontrol in the two aldol bond constructions generating the acyclic precursor II ...https://research-repository.griffith.edu.au/handle/10072/22614
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Improving Glycosyltransferase by RACHITT Gene Shuffling | SBIR.gov
DESCRIPTION (provided by applicant): Glycosyltransferases involved in linking polyketide macrolactones with deoxysugars are key enzymes for combinatorial biosynthesis of novel macrolide anti-infective agents. In this proposal, a new gene shuffling technology, RACHITT, is applied to the desosarninyl transferase (Des VII) from the pikromycin biosynthetic pathway of Streptomyces venezuelae. Des VII is an enzyme with remarkable inherent substrate flexibility, and we expect to expand further its substrate spectrum to include 16-membered ring macrolactones. This technology is expected to provide glycosyltransferase enzymes that can catalyze the biosynthesis of 12-, 14-, and 16-membered ring macrolides. Moreover, we expect to generate a recombinant DesVII that has a higher enzymatic activity toward the 14-membered ring macrolactone narbonolide. This will be a key step in combinatorial biosynthesis of ketolide antibiotics that have a potential to combat multi-drug ...https://www.sbir.gov/sbirsearch/detail/69495
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Notes from Dr. RW: Macrolides and mortality in critically ill patients with community acquired pneumonia
Conclusions:In observational studies of almost 10,000 critically ill patients with community-acquired pneumonia, macrolide use was associated with a significant 18% relative (3% absolute) reduction in mortality compared with nonmacrolide therapies. After pooling data from studies that provided adjusted risk estimates, an even larger mortality reduction was observed. These results suggest that macrolides be considered first-line combination treatment in critically ill patients with community-acquired pneumonia and support current guidelines ...http://doctorrw.blogspot.com/2014/08/macrolides-and-mortality-in-critically.html
Cempra Pharmaceuticals Presents New Data on Its Multi-Drug Resistant Anti-Infective Portfolio, Solithromycin (CEM-101) and...
Mechanism of telithromycin toxicity is proposed to be due to its inhibition of nicotinic acetylcholine receptors the novel fluoroketolide, solithromycin, like ohttps://www.drugs.com/clinical_trials/cempra-pharmaceuticals-presents-new-data-multi-resistant-anti-infective-portfolio-solithromycin-cem-10381.html
... can differ in their macrocyclic ring (modified to create clarithromycin (Biaxin©) and azithromycin (Zithromax©) with improved pharmacokinetic properties) and sugars. For telithromycin (Ketek®), the sugar at the 3-position was removed and replaced with a keto group - hence the class name of ketolides - and an additional modification allowed for binding to a secondary site on the bacterial ribosome, resulting in enhanced activity against resistant strains. ...http://www.aurametrix.com/topics/macrolides
Fidelta :: Novel Desosamine-Modified 14- and 15-membered Macrolides without Antibacterial Activity
Included was annelation of N-substituted 2-imino-1,3-oxazolidine 1 and 1,3-oxazolidin-2-one 2 moiety to the 2',3'-positions of desosamine ...http://fidelta.eu/resources/data-sheets/chemistry/novel-desosamine-modified-14-and-15-membered-macrolides-without-antibacterial-activity/
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In deciding to use a medicine, the risks of taking the medicine must be weighed against the good it will do. This is a decision you and your doctor will make. For this medicine, the following should be considered: Allergies Tell your doctor if you have ever had any unusual or allergic reaction to this medicine or any other medicines. Also tell your health care professional if you have any other types of allergies, such as to foods, dyes, preservatives, or animals. For non-prescription products, read the label or package ingredients carefully. Children Studies on this medicine have been only in adult patients, and there is no specific information comparing use of dirithromycin in children with use in other age groups. Older adults This medicine has been tested in a limited number of elderly patients and has not been shown to cause different side effects or problems in older people than it does in younger adults. Pregnancy ...https://www.allinahealth.org/CCS/doc/Thomson%20Detailed%20Drugs/47/600559.htm
Intravenous (IV) Administration of Cempra Pharmaceutical's Solithromycin (CEM-101) Demonstrates Excellent Systemic Tolerability...
Cempra Pharmaceuticals, a developer of differentiated antibiotics, today announced an oral presentation showing that intravenous (IV) solithromycin demonstrates excellent tolerabilityhttp://www.medindia.net/health-press-release/Intravenous-IV-Administration-of-Cempra-Pharmaceuticals-Solithromycin-CEM-101-Demonstrates-Excellent-Systemic-Tolerability-in-a-Phase-1-Clinical-Trial--102187-1.htm
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Macrolide Antibiotics - Health tips, Health care, Diseases treatment, Cancer, Blood Pressure
The Topic in which i am going to write today is a Topic on which you would have listen and read almost thousand of times because it is a ver ...http://health38.blogspot.com/2012/08/macrolide-antibiotics.html
Pharmacokinetics and Safety of Solithromycin Capsules in Adolescents - Full Text View - ClinicalTrials.gov
Choosing to participate in a study is an important personal decision. Talk with your doctor and family members or friends about deciding to join a study. To learn more about this study, you or your doctor may contact the study research staff using the contacts provided below. For general information, Learn About Clinical Studies. ...https://clinicaltrials.gov/ct2/show/NCT01966055?recr=Open&cond=%22Bacterial+Infections%22&rank=6
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