Page last updated: 2024-11-13

quinupristin-dalfopristin

Description Research Excerpts Clinical Trials Roles Classes Pathways Study Profile Bioassays Related Drugs Related Conditions Protein Interactions Research Growth Market Indicators

Description

quinupristin-dalfopristin: RP 59500 is a combination of RP 57669 & RP 54476, which are water soluble derivatives of pristinamycin IA & pristinamycin IIB, respectively [Medical Subject Headings (MeSH), National Library of Medicine, extracted Dec-2023]

Cross-References

ID SourceID
PubMed CID23724510
CHEBI ID8733
MeSH IDM0173961

Synonyms (8)

Synonym
quinupristin-dalfopristin
126602-89-9
C08034
D00854
synercid (tn)
quinupristin - dalfopristin mixt
CHEBI:8733
Q1763990

Research Excerpts

Toxicity

ExcerptReferenceRelevance
" The most common systemic adverse events related to treatment were arthralgias (9."( The efficacy and safety of quinupristin/dalfopristin for the treatment of infections caused by vancomycin-resistant Enterococcus faecium. Synercid Emergency-Use Study Group.
Blumberg, EA; Bompart, F; Linden, PK; Moellering, RC; Reinhardt, J; Talbot, GH, 1999
)
0.3
" In comparative clinical trials, the most frequent systemic adverse events related to quinupristin/dalfopristin were nausea (4."( Safety and tolerability of quinupristin/dalfopristin: administration guidelines.
Prokocimer, P; Rubinstein, E; Talbot, GH, 1999
)
0.3
" Quinupristin/dalfopristin appears safe and efficacious in critically ill immunocompromised children with renal or hepatic impairment."( Glycopeptide-resistant Enterococcus faecium infections in paediatric liver transplant recipients: safety and clinical efficacy of quinupristin/dalfopristin.
Dhawan, A; Heaton, N; Philpott-Howard, J; Rela, M; Vergani, GM; Verma, A; Wade, J, 2001
)
0.31
" However, 80% of subjects reported venous adverse events probably related to treatment."( Multiple-dose pharmacokinetics and safety of two regimens of quinupristin/dalfopristin (Synercid) in healthy volunteers.
Chevalier, P; Harding, N; Montay, G; Pasquier, O; Rey, J; Rouzier-Panis, R, 2001
)
0.31

Pharmacokinetics

We evaluated a number of antimicrobial combinations, with a focus on quinupristin-dalfopristin (Q-D), cefepime, and linezolid. An in vitro pharmacodynamic model with simulated endocardial vegetations incorporating protein and a high inoculum was used to simulate the Michigan VRSA strain.

ExcerptReferenceRelevance
"The tolerance and pharmacokinetic behaviour of a new injectable streptogramin antibiotic, RP 59500 were evaluated on 26 healthy male volunteers in a double-blind, placebo-controlled, phase I study."( A phase I, double-blind, placebo-controlled study of the tolerance and pharmacokinetic behaviour of RP 59500.
Etienne, SD; Frydman, A; Garaud, JJ; Le Liboux, A; Montay, G, 1992
)
0.28
" aureus (MRSA) 67 were evaluated in an in vitro pharmacodynamic infected fibrin clot model."( Pharmacodynamics of RP 59500 alone and in combination with vancomycin against Staphylococcus aureus in an in vitro-infected fibrin clot model.
Kang, SL; Rybak, MJ, 1995
)
0.29
" aureus 1199), in an in vitro pharmacodynamic infection model."( Pharmacodynamics of RP 59500 (quinupristin-dalfopristin) administered by intermittent versus continuous infusion against Staphylococcus aureus-infected fibrin-platelet clots in an in vitro infection model.
Houlihan, HH; Kaatz, GW; Mercier, RC; Rybak, MJ, 1997
)
0.59
" We studied the activity of quinupristin-dalfopristin against two clinical strains of VREF (12311 and 12366) in an in vitro pharmacodynamic model with simulated endocardial vegetations (SEVs) to determine the potential for resistance selection and possible strategies for prevention."( Treatment of vancomycin-resistant Enterococcus faecium with RP 59500 (quinupristin-dalfopristin) administered by intermittent or continuous infusion, alone or in combination with doxycycline, in an in vitro pharmacodynamic infection model with simulated e
Aeschlimann, JR; Rybak, MJ; Zervos, MJ, 1998
)
0.83
" A similar moderate increase in Cmax and AUC (about 20%) of parent drugs was observed between the first and last day of treatment."( Multiple-dose pharmacokinetics and safety of two regimens of quinupristin/dalfopristin (Synercid) in healthy volunteers.
Chevalier, P; Harding, N; Montay, G; Pasquier, O; Rey, J; Rouzier-Panis, R, 2001
)
0.31
" We evaluated a number of antimicrobial combinations, with a focus on quinupristin-dalfopristin (Q-D), cefepime, and linezolid, using a previously described in vitro pharmacodynamic model."( In vitro activities of quinupristin-dalfopristin and cefepime, alone and in combination with various antimicrobials, against multidrug-resistant staphylococci and enterococci in an in vitro pharmacodynamic model.
Allen, GP; Cha, R; Rybak, MJ, 2002
)
0.86
" aureus (VRSA), an in vitro pharmacodynamic model with simulated endocardial vegetations incorporating protein and a high inoculum was used to simulate daptomycin, linezolid, quinupristin-dalfopristin, and vancomycin against the Michigan VRSA strain."( Bactericidal activities of daptomycin, quinupristin-dalfopristin, and linezolid against vancomycin-resistant Staphylococcus aureus in an in vitro pharmacodynamic model with simulated endocardial vegetations.
Brown, WJ; Cha, R; Rybak, MJ, 2003
)
0.78
"To compare pharmacodynamic indices and minimal inhibitory concentrations for vancomycin, gatifloxacin, moxifloxacin, linezolid, and combined quinupristin and dalfopristin for historic and current human coagulase-negative staphylococcus (CoNS) endophthalmitis isolates."( In vitro efficacy and pharmacodynamic indices for antibiotics against coagulase-negative staphylococcus endophthalmitis isolates.
Flynn, HW; Harper, T; Miller, D, 2007
)
0.34
" Peak concentration (C(max)) was defined as the maximum attainable aqueous concentration using topical or oral therapy, or both."( In vitro efficacy and pharmacodynamic indices for antibiotics against coagulase-negative staphylococcus endophthalmitis isolates.
Flynn, HW; Harper, T; Miller, D, 2007
)
0.34
" Pharmacokinetic indices (C(max)/MIC90) for topical dosing were all <1."( In vitro efficacy and pharmacodynamic indices for antibiotics against coagulase-negative staphylococcus endophthalmitis isolates.
Flynn, HW; Harper, T; Miller, D, 2007
)
0.34

Compound-Compound Interactions

Quinupristin-dalfopristin is a streptogramin antibiotic combination with activity against vancomycin-resistant Enterococcus faecium (VREF) emergence of resistance has been recently reported.

ExcerptReferenceRelevance
"Using a checkerboard assay, ampicillin, vancomycin, and RP 59500, each in combination with chloramphenicol, were tested for synergy against 23 isolates of vancomycin-resistant enterococci."( In vitro activity of chloramphenicol alone and in combination with vancomycin, ampicillin, or RP 59500 (quinupristin/dalfopristin) against vancomycin-resistant enterococci.
Messick, CR; Pendland, SL, 1997
)
0.3
"Quinupristin-dalfopristin is a streptogramin antibiotic combination with activity against vancomycin-resistant Enterococcus faecium (VREF), but emergence of resistance has been recently reported."( Treatment of vancomycin-resistant Enterococcus faecium with RP 59500 (quinupristin-dalfopristin) administered by intermittent or continuous infusion, alone or in combination with doxycycline, in an in vitro pharmacodynamic infection model with simulated e
Aeschlimann, JR; Rybak, MJ; Zervos, MJ, 1998
)
1.98
" It is concluded that DU-6859a and trovafloxacin are very potent against enterococci, especially when combined with gentamicin."( In vitro activity of quinupristin/dalfopristin and newer quinolones combined with gentamicin against resistant isolates of Enterococcus faecalis and Enterococcus faecium.
Giamarellos-Bourboulis, EJ; Giamarellou, H; Grecka, P; Sambatakou, H, 1998
)
0.3
"This in vitro study evaluated the activities of vancomycin, LY333328, and teicoplanin alone and in combination with gentamicin, rifampin, and RP59500 against Staphylococcus aureus isolates with intermediate susceptibilities to vancomycin."( Evaluation of bactericidal activities of LY333328, vancomycin, teicoplanin, ampicillin-sulbactam, trovafloxacin, and RP59500 alone or in combination with rifampin or gentamicin against different strains of vancomycin-intermediate Staphylococcus aureus by
Aeschlimann, JR; Hershberger, E; Moldovan, T; Rybak, MJ, 1999
)
0.3
"Using checkerboard and time-kill assays, we evaluated the in vitro activity of quinupristin-dalfopristin (RP 59500) alone and in combination with five other antimicrobial agents against 12 clinical strains of vancomycin-resistant Enterococcus faecium (VREF)."( Synergy testing of vancomycin-resistant Enterococcus faecium against quinupristin-dalfopristin in combination with other antimicrobial agents.
Louie, L; Louie, M; Matsumura, SO; Simor, AE, 1999
)
0.77
", (iv) Q-D combined with either cefamandole or cefepime."( Quinupristin-dalfopristin combined with beta-lactams for treatment of experimental endocarditis due to Staphylococcus aureus constitutively resistant to macrolide-lincosamide-streptogramin B antibiotics.
Entenza, JM; Féger, C; Glauser, MP; Moreillon, P; Vouillamoz, J, 2000
)
1.75
" Unequivocal synergistic or antagonistic interactions at clinically relevant concentrations were infrequently encountered when the streptogramin was combined with chloramphenicol, ampicillin, imipenem, vancomycin, or teicoplanin."( Antimicrobial activity of quinupristin-dalfopristin combined with other antibiotics against vancomycin-resistant enterococci.
Eliopoulos, GM; Wennersten, CB, 2002
)
0.61
" Only the group treated with quinupristin/dalfopristin combined with levofloxacin or doxycycline showed no evidence of staphylococcal infection."( Quinupristin/dalfopristin bonding in combination with intraperitoneal antibiotics prevent infection of knitted polyester graft material in a subcutaneous rat pouch model infected with resistant Staphylococcus epidermidis.
Cirioni, O; D'Amato, G; Del Prete, M; Ghiselli, R; Giacometti, A; Mocchegiani, F; Orlando, F; Saba, V; Scalise, G, 2002
)
0.31
"We compared the efficacy of quinupristin/dalfopristin versus vancomycin, alone or in combination with rifampicin, in a rabbit model of methicillin-resistant Staphylococcus aureus-induced arthritis."( Efficacy of quinupristin/dalfopristin versus vancomycin, alone or in combination with rifampicin, against methicillin-resistant Staphylococcus aureus in a rabbit arthritis model.
Batard, E; Caillon, J; Hamel, A; Jacqueline, C; Potel, G, 2008
)
0.35

Bioavailability

ExcerptReferenceRelevance
" The almost-complete bioavailability of linezolid permits oral administration."( Quinupristin-dalfopristin and linezolid: evidence and opinion.
Eliopoulos, GM, 2003
)
1.76

Dosage Studied

The main objective of this review is to compare the relative efficacies, dosing strategies, and side-effect profiles. The pharmacodynamic (postantibiotic effect) and pharmacokinetic characteristics of quinupristin-dalfopristin allow dosing at eight- to 12-hour intervals.

ExcerptRelevanceReference
" or once daily dosage regimens, good intracellular and tissue penetration, better activity against gram-negative microorganisms (some) and a low rate of adverse reactions."( Clinical use of the new macrolides, azalides, and streptogramins in pediatrics.
Adam, D, 1992
)
0.28
" Following discontinuation of QND, the cyclosporine blood concentration decreased and the dosage was subsequently increased to the previous regimen."( Interaction between quinupristin/dalfopristin and cyclosporine.
Richards, JG; Stamatakis, MK, 1997
)
0.3
" A one-third reduction in the cyclosporine dosage was required."( Interaction between quinupristin/dalfopristin and cyclosporine.
Richards, JG; Stamatakis, MK, 1997
)
0.3
"Frequent monitoring of cyclosporine concentrations with attention to the need for dosage modification is recommended when initiating or discontinuing QND therapy."( Interaction between quinupristin/dalfopristin and cyclosporine.
Richards, JG; Stamatakis, MK, 1997
)
0.3
" There were no significant differences found between the dosing frequencies and levels of killing when examining each isolate separately."( Pharmacodynamics of RP 59500 (quinupristin-dalfopristin) administered by intermittent versus continuous infusion against Staphylococcus aureus-infected fibrin-platelet clots in an in vitro infection model.
Houlihan, HH; Kaatz, GW; Mercier, RC; Rybak, MJ, 1997
)
0.59
" Intravenous dosing of this antibiotic combination is unlikely to be adequate for the treatment of peritonitis associated with peritoneal dialysis."( Pharmacokinetics of quinupristin-dalfopristin in continuous ambulatory peritoneal dialysis patients.
Baybutt, RI; Bridson, WE; Chevalier, P; Johnson, CA; Pasquier, O; Taylor, CA; Zimmerman, SW, 1999
)
0.63
" A prolonged post-antibiotic effect, good polymorphonuclear leucocyte/macrophage penetration and slow release, and active metabolites allow this agent to be used with an 8 or 12 h dosing interval."( Quinupristin/dalfopristin: therapeutic potential for vancomycin-resistant enterococcal infections.
Moellering, RC, 1999
)
0.3
" Therefore, plasma drug monitoring and/or dosage reduction of these agents is prudent."( Safety and tolerability of quinupristin/dalfopristin: administration guidelines.
Prokocimer, P; Rubinstein, E; Talbot, GH, 1999
)
0.3
" Despite a short half-life, an extended postantibiotic effect allows the agent to be dosed every 8-12 hours."( Quinupristin-dalfopristin: an overview.
Bearden, DT; Danziger, LH; Delgado, G; Neuhauser, MM, 2000
)
1.75
" The purpose of this open, nonrandomized, parallel-group, phase I trial was to evaluate Q/D pharmacokinetics after single and repeated doses under the two different dosing regimens corresponding to the effective doses and to evaluate tolerability."( Multiple-dose pharmacokinetics and safety of two regimens of quinupristin/dalfopristin (Synercid) in healthy volunteers.
Chevalier, P; Harding, N; Montay, G; Pasquier, O; Rey, J; Rouzier-Panis, R, 2001
)
0.31
" One hundred and nineteen animals were treated with one of the following antibiotic regimens: im procaine penicillin G at a dosage of 300,000 U/kg weight/12 h (16 animals); iv trovafloxacin, 13."( Comparative study of treatment with penicillin, ceftriaxone, trovafloxacin, quinupristin-dalfopristin and vancomycin in experimental endocarditis due to penicillin- and ceftriaxone-resistant Streptococcus pneumoniae.
Cortés Sanchez, R; García Alberola, A; Gómez Gómez, J; López Fornas, F; Martínez García, F; Pérez Salmeron, J; Roldán Conesa, D; Ruíz Gómez, J; Valdés Chávarri, M, 2001
)
0.54
" The prolonged PAEs also suggest that the drug could be used intermittently at more widely spaced dosing intervals against gram-positive organisms."( In vitro activity and post-antibiotic effect of quinupristin/dalfopristin (Synercid).
Cheng, AF; Fung, KS; Ling, TK,
)
0.13
" The pharmacodynamic (postantibiotic effect) and pharmacokinetic characteristics of quinupristin-dalfopristin allow dosing at eight- to 12-hour intervals."( Quinupristin-dalfopristin: a new antibiotic for severe gram-positive infections.
Manzella, JP, 2001
)
1.98
" Due to the considerable contribution of the metabolites to overall in vivo activities, additional studies are required to fully quantify their removal before final dosage modifications for patients undergoing CVVH can be recommended."( Clearance of quinupristin-dalfopristin (Synercid) and their main metabolites during continuous veno-venous hemofiltration (CVVH) with or without dialysis.
Banevicius, MA; Hu, M; Kim, MK; Nicolau, DP; Nightingale, CH; Shi, X; Zhong, M, 2002
)
0.68
"At the conclusion of this learning activity, participants should be familiar with the modes of action, clinical indications, dosage regimens, and contraindications and cautions for several novel antibacterial agents for skin and skin structure infections."( Novel antibacterial agents for skin and skin structure infections.
Schweiger, ES; Weinberg, JM, 2004
)
0.32
" Pharmacokinetic indices (C(max)/MIC90) for topical dosing were all <1."( In vitro efficacy and pharmacodynamic indices for antibiotics against coagulase-negative staphylococcus endophthalmitis isolates.
Flynn, HW; Harper, T; Miller, D, 2007
)
0.34
" Therefore, a correct dosing regimen for the time-dependent molecules (i."( [Pharmacological rationale for choice of antibiotics for intraabdominal infections].
Mazzei, T; Novelli, A, 2008
)
0.35
" The main objective of this review is to compare the relative efficacies, dosing strategies, and side-effect profiles of quinupristin-dalfopristin, linezolid, and daptomycin for VRE bacteremia in the pediatric population."( Optimizing therapy for vancomycin-resistant enterococcal bacteremia in children.
Hsu, AJ; Tamma, PD, 2014
)
0.61
[information is derived through text-mining from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Drug Classes (1)

ClassDescription
organic molecular entityAny molecular entity that contains carbon.
[compound class information is derived from Chemical Entities of Biological Interest (ChEBI), Hastings J, Owen G, Dekker A, Ennis M, Kale N, Muthukrishnan V, Turner S, Swainston N, Mendes P, Steinbeck C. (2016). ChEBI in 2016: Improved services and an expanding collection of metabolites. Nucleic Acids Res]

Research

Studies (409)

TimeframeStudies, This Drug (%)All Drugs %
pre-19901 (0.24)18.7374
1990's168 (41.08)18.2507
2000's197 (48.17)29.6817
2010's37 (9.05)24.3611
2020's6 (1.47)2.80
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Market Indicators

Research Demand Index: 45.43

According to the monthly volume, diversity, and competition of internet searches for this compound, as well the volume and growth of publications, there is estimated to be strong demand-to-supply ratio for research on this compound.

MetricThis Compound (vs All)
Research Demand Index45.43 (24.57)
Research Supply Index6.08 (2.92)
Research Growth Index6.91 (4.65)
Search Engine Demand Index69.20 (26.88)
Search Engine Supply Index2.00 (0.95)

This Compound (45.43)

All Compounds (24.57)

Study Types

Publication TypeThis drug (%)All Drugs (%)
Trials16 (3.82%)5.53%
Reviews70 (16.71%)6.00%
Case Studies33 (7.88%)4.05%
Observational0 (0.00%)0.25%
Other300 (71.60%)84.16%
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Clinical Trials (2)

Trial Overview

TrialPhaseEnrollmentStudy TypeStart DateStatus
Prospective Randomized Study to Compare Clinical Outcomes in Patients With Osteomyelitis Treated With Intravenous Antibiotics Versus Intravenous Antibiotics With an Early Switch to Oral Antibiotics [NCT02099240]Early Phase 111 participants (Actual)Interventional2014-03-06Terminated(stopped due to Not enough patient enrollment and lack of staffing)
[NCT00240747]Phase 30 participants Interventional2000-06-30Terminated
[information is prepared from clinicaltrials.gov, extracted Sep-2024]