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同: quinupristin/dalfopristin

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出典(authority):フリー百科事典『ウィキペディア（Wikipedia）』「2016/06/13 13:57:30」(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

The drug inhibits P450 and enhances the effects of terfenadine, astemizole, indinavir, midazolam, calcium channel blockers, warfarin, cisapride and ciclosporin.

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. 小児におけるメチシリン耐性黄色ブドウ球菌感染：侵襲性感染症の治療 methicillin resistant staphylococcus aureus in children treatment of invasive infections
3. 腸球菌感染症の治療 treatment of enterococcal infections
4. 腸球菌における抗菌薬耐性の機構 mechanisms of antibiotic resistance in enterococci
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

Antimicrobial Resistance and Molecular Characteristics of Nasal Staphylococcus aureus Isolates From Newly Admitted Inpatients.

Chen X1, Sun K1, Dong D2, Luo Q1, Peng Y3, Chen F4.
Annals of laboratory medicine.Ann Lab Med.2016 May;36(3):250-4. doi: 10.3343/alm.2016.36.3.250.
Staphylococcus aureus, or methicillin-resistant S. aureus (MRSA), is a significant pathogen in both nosocomial and community infections. Community-associated MRSA (CA-MRSA) strains tend to be multi-drug resistant and to invade hospital settings. This study aimed to assess the antimicrobial resistanc
PMID 26915614

Occurrence of vancomycin-resistant and -susceptible Enterococcus spp. in reclaimed water used for spray irrigation.

Carey SA1, Goldstein RE1, Gibbs SG2, Claye E1, He X3, Sapkota AR4.
Environmental research.Environ Res.2016 May;147:350-5. doi: 10.1016/j.envres.2016.02.030. Epub 2016 Mar 1.
Reclaiming municipal wastewater for agricultural, environmental, and industrial purposes is increasing in the United States to combat dwindling freshwater supplies. However, there is a lack of data regarding the microbial quality of reclaimed water. In particular, no previous studies have evaluated
PMID 26942838

In Vitro Antimicrobial Susceptibility of Staphylococcus pseudintermedius Isolates of Human and Animal Origin.

Humphries RM1, Wu MT2, Westblade LF3, Robertson AE4, Burnham CA5, Wallace MA5, Burd EM6, Lawhon S7, Hindler JA8.
Journal of clinical microbiology.J Clin Microbiol.2016 May;54(5):1391-4. doi: 10.1128/JCM.00270-16. Epub 2016 Mar 9.
MIC results for 115 Staphylococcus intermedius group isolates are presented. Of these, 33% were methicillin resistant, among which 51.4% were susceptible to doxycycline, 29.7% to clindamycin, and 21.6% to trimethoprim-sulfamethoxazole. All of the isolates were susceptible to ceftaroline, daptomycin,
PMID 26962087

Japanese Journal

Design of a Novel Mammalian Screening System for the Detection of Bioavailable, Non-cytotoxic Streptogramin Antibiotics.

AUBEL DOMINIQUE,MORRIS ROWAN,LENNON BARBARA,RIMANN MARKUS,KAUFMANN HITTO,FOLCHER MARC,BAILEY JAMES E.,THOMPSON CHARLES J.,FUSSENEGGER MARTIN
The Journal of Antibiotics 54(1), 44-55, 2001
… Quinupristin-dalfopristin (Synercid®), a synthetically modified Streptogramin, is presently the sole effective agent in the treatment of some MDR nosocomial infections. …
NAID 130003503809

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関連記事	「SYNERCID」

「SYNERCID」

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

[hugo-1] 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

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synercid