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Quinupristin/dalfopristin , or 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 [ edit ]
Intravenous , usually 7.5 mg/kg every 8 hours (infections/life threatening VRSA); every 12 hours (skin infections).
No renal dosing adjustments, hepatic dosing adjustments are not defined, consider reducing dose.
Mechanism of action [ edit ]
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 [ edit ]
Clearance by the liver CYP450:3A4 inhibitor, half-life quinupristin 0.8 hours, dalfopristin 0.7 hours (with persistence of effects for 9–10 hours).
Side effects [ edit ]
[2]
Serious:
C.diff-associated diarrhea
superinfection
anaphylactoid reactions
angioedema
Common:
Joint aches (arthralgia) or muscle aches (myalgia)
Nausea , diarrhea (C. diff associated) or vomiting
Rash or itching
Headache
Hyperbilirubinemia
Anemia
Thrombophlebitis
Drug interactions [ edit ]
The drug inhibits P450 and enhances the effects of terfenadine , astemizole , indinavir , midazolam , calcium channel blockers , warfarin , cisapride and ciclosporin .
References [ edit ]
Further reading [ edit ]
Lamb HM, Figgitt DP, Faulds D (December 1999). "Quinupristin/dalfopristin: a review of its use in the management of serious gram-positive infections". Drugs . 58 (6 ): 1061–97. doi :10.2165/00003495-199958060-00008 . PMID 10651391 . S2CID 209144323 .
Manzella JP (December 2001). "Quinupristin-dalfopristin: a new antibiotic for severe gram-positive infections". American Family Physician . 64 (11 ): 1863–6. PMID 11764864 . .
Paradisi F, Corti G, Messeri D (January 2001). "Antistaphylococcal (MSSA, MRSA, MSSE, MRSE) antibiotics" (PDF) . The Medical Clinics of North America . 85 (1 ): 1–17. doi :10.1016/s0025-7125(05 )70302-3 . hdl :2158/329747 . PMID 11190346 .
"Synercid" . U.S. Food and Drug Administration. Archived from the original on 2007-06-18.
R e t r i e v e d f r o m " https://en.wikipedia.org/w/index.php?title=Quinupristin/dalfopristin&oldid=1197167855 "
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