同: Synercid

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出典(authority):フリー百科事典『ウィキペディア（Wikipedia）』「2015/09/29 05:27:52」(JST)

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Quinupristin/dalfopristin (pronunciation: kwi NYOO pris tin / dal FOE pris tin) (trade name Synercid) is a combination of two antibiotics used to treat infections by staphylococci and by vancomycin-resistant Enterococcus faecium.

Quinupristin and dalfopristin are both streptogramin antibiotics, derived from pristinamycin. Quinupristin is derived from pristinamycin IA; dalfopristin from pristinamycin IIA. They are combined in a weight-to-weight ratio of 30% quinupristin to 70% dalfopristin.

Administration

Intravenous, usually 7.5 mg/kg every 8–12 hours

Mechanism of action

Quinupristin and dalfopristin are protein synthesis inhibitors in a synergistic manner. While each of the two is only a bacteriostatic agent, the combination shows bactericidal activity.

Dalfopristin binds to the 23S portion of the 50S ribosomal subunit, and changes the conformation of it, enhancing the binding of quinupristin^[1] by a factor of about 100. In addition, it inhibits peptidyl transfer.^[1]
Quinupristin binds to a nearby site on the 50S ribosomal subunit and prevents elongation of the polypeptide,^[1] as well as causing incomplete chains to be released.^[1]

Pharmacokinetics

Clearance by the liver, half-life 1–3 hours (with persistence of effects for 9–10 hours).

Side effects

Joint aches (arthralgia) or muscle aches (myalgia)
Nausea, diarrhea or vomiting
Rash or itching
Headache
Phlebitis
Hyperbilirubinemia

Drug interactions

Inhibits P450 and enhances the effects of terfenadine, astemizole, indinavir, midazolam, Ca channel blockers, warfarin, cisapride and cyclosporine.

References

^ ^a ^b ^c ^d Page 212 in: Title: Hugo and Russell's pharmaceutical microbiology Authors: William Barry Hugo, Stephen P. Denyer, Norman A. Hodges, Sean P. Gorman Edition: 7, illustrated Publisher: Wiley-Blackwell, 2004 ISBN 0-632-06467-6, ISBN 978-0-632-06467-0 Length: 481 pages

UpToDate Contents

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1. メチシリン耐性黄色ブドウ球菌およびバンコマイシン耐性腸球菌の治療のための抗菌薬の
薬理 pharmacology of antimicrobial agents for treatment of methicillin resistant staphylococcus aureus and vancomycin resistant enterococcus
2. 腸球菌感染症の治療 treatment of enterococcal infections
3. 腸球菌における抗菌薬耐性の機構 mechanisms of antibiotic resistance in enterococci
4. 小児における侵襲的メチシリン耐性黄色ブドウ球菌感染の治療 treatment of invasive methicillin resistant staphylococcus aureus infection in children
5. 成人における侵襲性メチシリン耐性黄色ブドウ球菌感染症の治療 treatment of invasive methicillin resistant staphylococcus aureus infections in adults

English Journal

Genetic features of livestock-associated Staphylococcus aureus ST9 isolates from Chinese pigs that carry the lsa(E) gene for quinupristin/dalfopristin resistance.

Yan X1, Li Z2, Chlebowicz MA3, Tao X1, Ni M2, Hu Y4, Li Z2, Grundmann H5, Murray S6, Pascoe B7, Sheppard SK7, Bo X2, Dijl JM3, Du P1, Zhang M2, You Y1, Yu X8, Meng F1, Wang S9, Zhang J10.
International journal of medical microbiology : IJMM.Int J Med Microbiol.2016 Aug 10. pii: S1438-4221(16)30209-0. doi: 10.1016/j.ijmm.2016.08.001. [Epub ahead of print]
Whole-genome sequencing (WGS) was used to investigate the genetic features of the recently identified lsa(E) gene in porcine S. aureus ST9 isolates. Three quinupristin/dalfopristin-resistant isolates harboring the lsa(E) gene (two MRSA and one MSSA) were sequenced. Phylogenetic analysis of 184S. aur
PMID 27528592

Newer antibiotics for the treatment of peritoneal dialysis-related peritonitis.

Ma TK1, Leung CB1, Chow KM1, Kwan BC1, Li PK1, Szeto CC1.
Clinical kidney journal.Clin Kidney J.2016 Aug;9(4):616-23. doi: 10.1093/ckj/sfw059. Epub 2016 Jul 4.
Peritonitis is a debilitating infectious complication of peritoneal dialysis (PD). Drug-resistant bacterial peritonitis typically has a lower response rate to antibiotics. In the past 15 years, newer antibiotics with activities against drug-resistant Gram-positive bacteria have been developed. In mo
PMID 27478608

Susceptibility Profile of Staphylococcus epidermidis and Staphylococcus haemolyticus Isolated from Blood Cultures to Vancomycin and Novel Antimicrobial Drugs over a Period of 12 Years.

Pinheiro L1, Brito CI1, Pereira VC1, Oliveira A1, Bartolomeu AR1, Camargo CH1,2, Cunha ML1.
Microbial drug resistance (Larchmont, N.Y.).Microb Drug Resist.2016 Jun;22(4):283-93. doi: 10.1089/mdr.2015.0064. Epub 2015 Dec 1.
The aim of this study was to evaluate the antimicrobial susceptibility profile of 85 Staphylococcus epidermidis and 84 Staphylococcus haemolyticus strains isolated from blood cultures to oxacillin, vancomycin, tigecycline, linezolid, daptomycin, and quinupristin/dalfopristin over a period of 12 year
PMID 26623676

Japanese Journal

バンコマイシン耐性腸球菌 (特集外科領域における耐性菌)

高倉俊二
日本外科感染症学会雑誌 10(3), 293-298, 2013-06
NAID 40019764950

Isolation and Molecular Characterization of Methicillin-Resistant Staphylococci from Horses, Personnel and Environmental Sites at an Equine Hospital in Turkey

, , [他], ,
Journal of Veterinary Medical Science 74(12), 1583-1588, 2012
… All isolates were found to be susceptible against vancomycin, quinupristin-dalfopristin and rifampicin. …
NAID 130001879704

各種抗菌薬に対する２００４年臨床分離好気性グラム陽性球菌および嫌気性菌の感受性サーベイランス

藤村享滋他
日本化学療法学会雑誌 56(5), 543-561, 2008
… MRSAおよびMRSEに対して良好な抗菌力を示したのは, vancomycin (VCM), linezolid (LZD) およびquinupristin/dalfopristin (QPR/DPR) で, MIC<SUB>90</SUB>は2μg/mL以下であった。 …
NAID 130004102773

Related Pictures

: synercid Quinupristin/dalfopristin Inj 350 MG-150 MG Figure 1. SYNERCID（QUINUPRISTIN/DALFOPRISTIN） Quinupristin-dalfopristin Quinupristin-Dalfopristin ( Synercid Quinupristin - Dalfopristin

★リンクテーブル★

リンク元	「synercid」「SYNERCID」
関連記事	「dalfopristin」

「synercid」

Quinupristin/dalfopristin
	Quinupristin (top) and dalfopristin (bottom)
Combination of
Quinupristin	Streptogramin antibiotic
Dalfopristin	Streptogramin antibiotic
Clinical data
Pregnancy; category	B (U.S.);
Legal status	℞-only (U.S.);
Routes of; administration	IV
Identifiers
CAS Registry Number	126602-89-9
ATC code	J01FG02
PubChem	CID: 23724510
ChemSpider	21106373
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