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Chemical Compound Review

AC1NSJWH     (3R,4S,5R,6R,7R,9R,11R,12R,13S ,14R)-6-[(3R...

Synonyms: SureCN13486224
 
 
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Disease relevance of clarithromycin

  • Clarithromycin (CLM) and azithromycin (AZM) are important agents in the treatment of disseminated Mycobacterium avium complex disease; however, monotherapy with these macrolides often leads to clinically significant resistance [1].
  • Administered in five daily doses of 100 mg/kg of body weight, HMR appeared slightly more bactericidal than CLARI [2].
  • BACKGROUND: Studies demonstrating the efficacy of short-term low-dose triple therapies including omeprazole (O), clarithromycin (C) and a nitroimidazole (tinidazole, T) for Helicobacter pylori eradication have largely been open and uncontrolled, and have not assessed antibiotic sensitivity [3].
  • FIC values indicated a synergistic effect with GM, MRPM and CPFX against E. coli and P. rettgeri and an additive effect for the combination HPF plus CLTM or indifference with HPF plus GM and CPFX against S. aureus [4].
 

High impact information on clarithromycin

  • ISS-ODN significantly enhanced the therapeutic effect of CLA in both human and mouse macrophages and in C57BL/6 mice [5].
  • Bactericidal activities of HMR 3647 (HMR), moxifloxacin (MXFX), and rifapentine (RPT) against Mycobacterium leprae, measured by the proportional bactericidal technique in the mouse footpad system, were compared with those of the established antileprosy drugs clarithromycin (CLARI), ofloxacin (OFLO), and rifampin (RMP) [2].
  • The underlying resistance mechanism was investigated by comparing 23S rRNA gene sequences in the domain V region of 10 CLM-susceptible strains included in this study [1].
  • AZI at 200 mg/kg was more active than CLA at 200 mg/kg against organisms in spleens [6].
  • The eradication rate was 93.8% in group OCT, 59.4% in group CT, 31.3% in group OC and 6.3% in group C. Pre-treatment metronidazole resistance was 12.8%, clarithromycin 1.1% and, to both antibiotics, 2.1% [3].
 

Chemical compound and disease context of clarithromycin

 

Associations of clarithromycin with other chemical compounds

  • Four of these seven CLM-resistant strains emerged during monotherapy with CLM and two emerged during AZM monotherapy, showing that resistance selected by either macrolide was associated with mutation of the 23S rRNA gene [1].
  • In vitro, S. pneumoniae was incubated with 1, 2 and 4 microg.mL(-1) of clarithromycin (CLR) and azithromycin (AZM) for 8 h [8].
  • After monotherapy, only AMI and CLA displayed bacteriostatic and/or moderate bactericidal effects in spleens and lungs, while CIP and RFB were totally inactive and CLO and EMB showed intermediate effects against the isolate tested [9].
 

Gene context of clarithromycin

  • Resistance to both antibiotics occurred in 22.2% of the failures in group CT and in none of group OCT. CONCLUSIONS: (i) The high efficacy of the OCT regimen is proved and each of the individual components of the regimen is essential to the result, possibly via a synergistic effect [3].

References

  1. Genetic basis of macrolide resistance in Mycobacterium avium isolated from patients with disseminated disease. Nash, K.A., Inderlied, C.B. Antimicrob. Agents Chemother. (1995) [Pubmed]
  2. Bactericidal activities of HMR 3647, moxifloxacin, and rifapentine against Mycobacterium leprae in mice. Consigny, S., Bentoucha, A., Bonnafous, P., Grosset, J., Ji, B. Antimicrob. Agents Chemother. (2000) [Pubmed]
  3. Evaluation of short-term low-dose triple therapy for the eradication of Helicobacter pylori by factorial design in a randomized, double-blind, controlled study. Bazzoli, F., Zagari, M., Pozzato, P., Varoli, O., Fossi, S., Ricciardiello, L., Alampi, G., Nicolini, G., Sottili, S., Simoni, P., Roda, A., Roda, E. Aliment. Pharmacol. Ther. (1998) [Pubmed]
  4. Antibacterial activity of human pleural fluid: alone and in combination with antibiotics. Miglioli, P.A., Allerberger, F., Walderberg, I., Hasse, J. Int. J. Antimicrob. Agents (1998) [Pubmed]
  5. Enhancement of innate immunity against Mycobacterium avium infection by immunostimulatory DNA is mediated by indoleamine 2,3-dioxygenase. Hayashi, T., Rao, S.P., Takabayashi, K., Van Uden, J.H., Kornbluth, R.S., Baird, S.M., Taylor, M.W., Carson, D.A., Catanzaro, A., Raz, E. Infect. Immun. (2001) [Pubmed]
  6. Intermittent azithromycin for treatment of Mycobacterium avium infection in beige mice. Klemens, S.P., Cynamon, M.H. Antimicrob. Agents Chemother. (1994) [Pubmed]
  7. In vitro activity of levofloxacin against Helicobacter pylori isolates from patients after treatment failure. Yahav, J., Shmuely, H., Niv, Y., Bechor, J., Samra, Z. Diagn. Microbiol. Infect. Dis. (2006) [Pubmed]
  8. Effects of macrolides on pneumolysin of macrolide-resistant Streptococcus pneumoniae. Fukuda, Y., Yanagihara, K., Higashiyama, Y., Miyazaki, Y., Hirakata, Y., Mukae, H., Tomono, K., Mizuta, Y., Tsukamoto, K., Kohno, S. Eur. Respir. J. (2006) [Pubmed]
  9. Activities of eighteen antimicrobial regimens against Mycobacterium avium infection in beige mice. Fattorini, L., Xiao, Y., Mattei, M., Li, Y., Iona, E., Thoresen, O.F., Orefici, G. Microb. Drug Resist. (1999) [Pubmed]
 
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