Skip to main content
Log in

Antibacterial Activity of Quinupristin/Dalfopristin

Rationale for Clinical Use

  • Published:
Drugs Aims and scope Submit manuscript

Summary

Most Gram-positive organisms are highly susceptible to the streptogramin, quinupristin/dalfopristin (RP 59500; Synercid®). Minimum inhibitory concentrations for 90% of isolates (MIC90) were ≤ 1 mg/L for Staphylococcus aureus, S. epidermidis, S. haemolyticus, Streptococcus pneumoniae, S. pyogenes and Listeria monocytogenes. Importantly, quinupristin/dalfopristin shows similar activity against methicillin-susceptible and -resistant strains of S. aureus, and streptococci with benzylpenicillin (penicillin G)- or erythromycin-acquired resistance. Enterococci have varying susceptibility to quinupristin/dalfopristin, although most isolates tested are susceptible to the drug, including vancomycin-resistant and multiresistant Enterococcus faecium. E. faecalis are generally the least susceptible.

Among the Gram-negative respiratory pathogens Moraxella catarrhalis is susceptible and Haemophilus influenzae is moderately susceptible to quinupristin/dalfopristin; however, Enterobacteriaceae, Pseudomonas aeruginosa and Acinetobacter spp. are resistant. The drug is active against anaerobic organisms tested, including Clostridium perfringens, Lactobacillus spp., Bacteroides fragilis and Peptostreptococcus. Synergy has been demonstrated in vancomycin-resistant and multiresistant E. faecium, and methicillin-sensitive and -resistant S. aureus with the combination of vancomycin and quinupristin/dalfopristin.

Quinupristin/dalfopristin shows antibacterial activity in vivo in animal models of infection, including methicillin-sensitive and -resistant S. aureus infection in rabbits, S. aureus and S. pneumoniae in mice, and erythromycin-sensitive and -resistant viridans group streptococci infections in rats.

The drug is rapidly bactericidal against Gram-positive organisms (with the exception of enterococci) at concentrations similar to or within 4-fold of the MIC, and it has a long postantibiotic effect both in vitro and in vivo.

This is a preview of subscription content, log in via an institution to check access.

Access this article

Price excludes VAT (USA)
Tax calculation will be finalised during checkout.

Instant access to the full article PDF.

Similar content being viewed by others

References

  1. Fass RJ. In vitro activity of RP 59500, a semisynthetic injectable pristinamycin, against staphylococci, streptococci, and enterococci. Antimicrob Agents Chemother 1991; 35: 553–9.

    Article  PubMed  CAS  Google Scholar 

  2. Neu HC, Chin N, Gu J. The in-vitro activity of new streptogramins, RP 59500, RP 57669 and RP 54476, alone and in combination. J Antimicrob Chemother 1992; 30 Suppl. A: 83–94.

    PubMed  CAS  Google Scholar 

  3. Archer GL, Doern GV, Fuchs PC, et al. RP 59500, a new streptogramin highly active against recent isolates of North American staphylococci. Diagn Microbiol Infect Dis 1993; 16: 223–6.

    Article  PubMed  CAS  Google Scholar 

  4. Andrews JM, Wise R. The in-vitro activity of a new semi-synthetic streptogramin compound, RP 59500, against staphylococci and respiratory pathogens. J Antimicrob Chemother 1994; 33: 849–53.

    Article  PubMed  CAS  Google Scholar 

  5. Hoban DJ, Weshnoweski B, Palatnick L, et al. In-vitro activity of streptogramin RP 59500 against staphylococci, including bactericidal kinetic studies. J Antimicrob Chemother 1992; 30 Suppl. A: 59–65.

    PubMed  CAS  Google Scholar 

  6. Verbist L, Verhaegen J. Comparative in-vitro activity of RP 59500. J Antimicrob Chemother 1992; 30 Suppl. A: 39–44.

    PubMed  CAS  Google Scholar 

  7. Goto S, Miyazaki S, Kaneko Y. The in-vitro activity of RP 59500 against Gram-positive cocci. J Antimicrob Chemother 1992; 30 Suppl. A: 25–8.

    PubMed  CAS  Google Scholar 

  8. Inoue M, Okamoto R, Okubo T, et al. Comparative in-vitro activity of RP 59500 against clinical bacterial isolates. J Antimicrob Chemother 1992; 30 Suppl. A: 45–51.

    PubMed  CAS  Google Scholar 

  9. Appelbaum PC, Spangler SK, Jacobs MR. Susceptibility of 539 Gram-positive and Gram-negative anaerobes to new agents, including RP 59500, biapenem, trospectomycin and piperacillin/tazobactam. J Antimicrob Chemother 1993; 32: 223–31.

    Article  PubMed  CAS  Google Scholar 

  10. Nord CE, Lindmark A, Persson I. Susceptibility of anaerobic bacteria to the new streptogramin RP 59500 in vitro? Eur J Clin Microbiol Infect Dis 1989; 8 (12): 1064–7.

    Article  PubMed  CAS  Google Scholar 

  11. Aldridge KE, Schiro DD, Varaer LM. In vitro antistaphylococcal activity and testing of RP 59500, a new streptogramin, by two methods. Antimicrob Agents Chemother 1992; 36: 854–5.

    Article  PubMed  CAS  Google Scholar 

  12. Scriver SR, Tyrrell G, Willey BM, et al. In vitro assessment of RP 59500 (RP) against vancomycin-resistant enterococci [abstract]. 33rd Interscience Conference of Antimicrobial Agents and Chemotherapy; 1993 Oct 17–20; New Orleans: 312

  13. Leclercq R, Nantas L, Soussy C-J, et al. Activity of RP 59500, a new parenteral semi synthetic streptogramin, against staphylococci with various mechanisms of resistance to macrolide-lincosamide-streptogramin antibiotics. J Antimicrob Chemother 1992; 30 Suppl. A: 67–75.

    PubMed  CAS  Google Scholar 

  14. Fremaux A, Sissia G, Cohen R, et al. In-vitro antibacterial activity of RP 59500, a semi synthetic streptogramin, against Streptococcus pneumoniae. J Antimicrob Chemother 1992; 30 Suppl. A: 19–23.

    PubMed  CAS  Google Scholar 

  15. Spangler SK, Jacobs MR, Appelbaum PC. Susceptibilities of penicillin-susceptible and -resistant strains of Streptococcus pneumoniae to RP 59500, vancomycin, erythromycin, PD 131628, sparfloxacin, temafloxacin, Win 57273, ofloxacin, and ciprofloxacin. Antimicrob Agents Chemother 1992; 36: 856–9.

    Article  PubMed  CAS  Google Scholar 

  16. Johnson CC, Slavoski L, Schwartz M, et al. In vitro activity of RP 59500 (quinupristin/dalfopristin) against antibiotic-resistant strains of Streptococcus pneumoniae and enterococci. Diagn Microbiol Infect Dis 1995; 21: 169–73.

    Article  PubMed  CAS  Google Scholar 

  17. Barry AL, Fuchs PC. In vitro activities of a streptogramin (RP59500), three macrolides, and an azalide against four respiratory tract pathogens. Antimicrob Agents Chemother 1995; 39: 238–40.

    Article  PubMed  CAS  Google Scholar 

  18. Tarasi A, Tomasz A. Activity of RP59500 against multidrug resistant clones of Streptococcus pneumoniae [abstract no. E116]. 35th Interscience Conference on Antimicrobial Agents and Chemotherapy; 1995 Sep 17–20; San Francisco, California: 106

  19. Collins LA, Malanoski GJ, Eliopoulos GM, et al. In vitro activity of RP59500, an injectable streptogramin antibiotic, against vancomycin-resistant Gram-positive organisms. Antimicrob Agents Chemother 1993; 37: 598–601.

    Article  PubMed  CAS  Google Scholar 

  20. Freeman C, Robinson A, Cooper B, et al. In vitro antimicrobial susceptibility of glycopeptide-resistant enterococci. Diagn Microbiol Infect Dis 1995; 21: 47–50.

    Article  PubMed  Google Scholar 

  21. Scriver SR, Willey BM, Matsumara S. Susceptibility of glycopeptide-resistant enterococci including variant species to RP 59500 [abstract no. 13]. 2nd International Conference on Macrolides, Azalides and Streptogramins. 1994 Jan 19–21; Venice: 13

  22. Casewell MW, Seyed-Akhavani M, Wade J. In-vitro activity of RP 59500 against vancomycin-resistant Enterococcus faecium also resistant to > 512 mg/L of gentamicin [abstract]. 33rd Interscience Conference of Antimicrobial Agents and Chemotherapy; 1993 Oct 17–20; New Orleans: 313

  23. Mahayni R, Perri MB, Dembry LM, et al. Comparative in-vitro and bactericidal activity of RP59500 (quinupristin/ dalfopristin), against multi-drug resistant E. faecium [abstract]. 34th Interscience Conference of Antimicrobial Agents and Chemotherapy; 1994 Oct; Orlando: 27

  24. Goldsmith MF. New forms and new needs may make macrolides antibiotics of the decade? JAMA 1992; 267 (7): 903–4.

    Article  PubMed  CAS  Google Scholar 

  25. Lorian V, Fernandes F. Synergistic activity of injectable streptogramin RP59500-vancomycin combination [abstract no. E126]. 35th Interscience Conference on Antimicrobial Agents and Chemotherapy; 1995 Sep 17–20; San Francisco, California: 107

  26. Kang SL, Rybak MJ. In vitro bactericidal activity of RP59500 (quinupristin/dalfopristin; RP) alone and in various combinations against resistant strains of Enterococcus species and Staphylococcus aureus (SA) [abstract no. E121]. 35th Interscience Conference on Antimicrobial Agents and Chemotherapy; 1995 Sep 17–20; San Francisco, California: 107

  27. Pankuch GA, Jacobs MR, Appelbaum PC. Study of comparative antipneumococcal activities of penicillin G, RP 59500, erythromycin, sparfloxacin, ciprofloxacin, and vancomycin by using time-kill methodology. Antimicrob Agents Chemother 1994; 38: 2065–72.

    Article  PubMed  CAS  Google Scholar 

  28. Berthaud N, Charles Y, Gouin A-M, et al. In vitro bactericidal activity of RP59500 (quinupristin/dalfopristin) against adherent Staphylococcus aureus [abstract no. E122]. 35th Interscience Conference on Antimicrobial Agents and Chemotherapy; 1995 Sep 17–20; San Francisco, California: 107

  29. Desnottes JF, Diallo N. RP 59500: In vitro anti-staphylococcal bactericidal activity across platelet-fibrin matrices compared to that of vancomycin [abstract]. 33rd Interscience Conference of Antimicrobial Agents and Chemotherapy; 1993 Oct 17–20; New Orleans: 259

  30. Kang SL, Rybak MJ. Pharmacodynamics of RP 59500 alone and in combination with vancomycin against Staphylococcus aureus in an in vitro-infected fibrin clot model. Antimicrob Agents Chemother 1995; 39: 1505–11.

    Article  PubMed  CAS  Google Scholar 

  31. Johnson CC, Slavoski L, Schwartz M, et al. In vitro bactericidal activity of RP59500 (Synercid) against antibiotic resistant strains of Streptococcus pneumoniae and Enterococcus spp. [abstract]. 34th Interscience Conference of Antimicrobial Agents and Chemotherapy; 1994 Oct; Orlando: 28

  32. Hill RLR, Smith C, Casewell M. Bactericidal and inhibitory activity of RP 50500 (quinupristin/dalfopristin) and its components against vancomycin- and gentamicin-resistant Enterococcus faecium [abstract no. El 18]. 35th Interscience Conference on Antimicrobial Agents and Chemotherapy; 1995 Sep 17–20; San Francisco, California

  33. Boswell FJ, Andrews JM, Wise R. The postantibiotic effect of RP 59500 on Staphylococcus aureus including strains with a raised MBC. J Antimicrob Chemother 1994; 33: 1219–22.

    Article  PubMed  CAS  Google Scholar 

  34. Chin NX, Neu HC. Post-antibiotic effect of the new streptogramin RP 59500. Eur J Clin Microbiol Infect Dis 1992; 11: 642–5.

    Article  PubMed  CAS  Google Scholar 

  35. Nougayrede A, Berthaud N, Bouanchaud DH. Post-antibiotic effects of RP 59500 with Staphylococcus aureus. J Antimicrob Chemother 1992; 30 Suppl. A: 101–6.

    PubMed  CAS  Google Scholar 

  36. Fantin B, Leclercq R, Ottaviani M, et al. In vivo activities and penetration of the two components of the streptogramin RP 59500 in cardiac vegetations of experimental endocarditis. Antimicrob Agents Chemother 1994; 38: 432–7.

    Article  PubMed  CAS  Google Scholar 

  37. Chambers HF. Studies of RP 59500 in vitro and in a rabbit model of aortic valve endocarditis caused by methicillin-resistant Staphylococcus aureus. J Antimicrob Chemother 1992; 30 Suppl. A: 117–22.

    PubMed  CAS  Google Scholar 

  38. Craig W, Ebert S. Pharmacodynamic activities of RP 59500 in an animal infection model [abstract]. 33rd Interscience Conference of Antimicrobial Agents and Chemotherapy; 1993 Oct 17–20; New Orleans: 205

  39. L’Hériteau F, Entenza JM, Lacassin F, et al. RP 59500 prophylaxis of experimental endocarditis due to erythromycin-susceptible and -resistant isogenic pairs of viridans group streptococci. Antimicrob Agents Chemother 1995; 39: 1425–9.

    Article  PubMed  Google Scholar 

  40. Berthaud N, Montay G, Huet Y, et al. RP 59500, in vitro bactericidal activity in a model of S. aureus mouse infection: influence of varying dosage and the number of treatments. Proceedings of the 32nd Interscience Conference of Antimicrobial Agents and Chemotherapy; 1992 Oct; Anaheim: 69–71

  41. Berthaud N, Montay G, Conard BJ, et al. Bactericidal activity and kinetics of RP 59500 in a mouse model of Staphylococcus aureus septicaemia. J Antimicrob Chemother 1995; 36: 365–73.

    Article  PubMed  CAS  Google Scholar 

Download references

Author information

Authors and Affiliations

Authors

Rights and permissions

Reprints and permissions

About this article

Cite this article

Finch, R.G. Antibacterial Activity of Quinupristin/Dalfopristin. Drugs 51 (Suppl 1), 31–37 (1996). https://doi.org/10.2165/00003495-199600511-00007

Download citation

  • Published:

  • Issue Date:

  • DOI: https://doi.org/10.2165/00003495-199600511-00007

Keywords

Navigation