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Quinupristin/dalfopristin

quinupristin/dalfopristin, quinupristin/dalfopristin (synercid)
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

Contents

  • 1 Administration
  • 2 Mechanism of action
  • 3 Pharmacokinetics
  • 4 Side effects
  • 5 Drug interactions
  • 6 References
  • 7 Further reading

Administration

Intravenous, usually 75 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 by a factor of about 100 In addition, it inhibits peptidyl transfer
  • Quinupristin binds to a nearby site on the 50S ribosomal subunit and prevents elongation of the polypeptide, as well as causing incomplete chains to be released

Pharmacokinetics

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

Side effects

  1. Joint aches arthralgia or muscle aches myalgia
  2. Nausea, diarrhea or vomiting
  3. Rash or itching
  4. Headache
  5. Phlebitis
  6. Hyperbilirubinemia

Drug interactions

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

References

  1. ^ 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

Further reading

  • Allington DR, Rivey M Jan 2001 "Quinupristin/dalfopristin: a therapeutic review" Clin Ther 23 1: 24–44 doi:101016/S0149-29180180028-X PMID 11219478 
  • "Quinupristin/dalfopristin: a review of its use in the management of serious gram-positive infections" Drugs 58 6: 1061–97 December 1999 doi:102165/00003495-199958060-00008 PMID 10651391 
  • "Quinupristin-dalfopristin: a new antibiotic for severe gram-positive infections" Am Fam Physician 64 11: 1863–6 December 2001 PMID 11764864 
  • "MRSA" Med Clin North Am 85 1: 1–17 January 2001 doi:101016/s0025-71250570302-3 PMID 11190346 
  • https://webarchiveorg/web/20070618100658/http://wwwfdagov/cder/consumerinfo/druginfo/SYNERCIDhtm

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Quinupristin/dalfopristin


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    29.10.2014


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