Quinupristin/dalfopristin
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 (top) and dalfopristin (bottom) | |
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Quinupristin | Streptogramin antibiotic |
Dalfopristin | Streptogramin antibiotic |
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Routes of administration | IV |
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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 hours (infections/life threatening VRSA); every 12 hours (skin infections) no renal dosing adjustments hepatic dosing adjustments not defined, consider reducing dose
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 CYP450:3A4 inhibitor, half-life quinupristin 0.8 hours, dalfopristin 0.7 hours (with persistence of effects for 9–10 hours).
Excretion: Quinupristin: 85% feces, 15% urine; Dalfopristin: 81% feces, 19% urine
Side effects
[2]
Serious:
- C.diff-associated diarrhea
- superinfection
- anaphylactoid reactions
- angioedema
Common:
Drug interactions
The drug inhibits P450 and enhances the effects of terfenadine, astemizole, indinavir, midazolam, calcium channel blockers, warfarin, cisapride and ciclosporin.
References
- 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
- Epocrates v 19.5
Further reading
- Allington DR, Rivey M (Jan 2001). "Quinupristin/dalfopristin: a therapeutic review". Clin. Ther. 23 (1): 24–44. doi:10.1016/S0149-2918(01)80028-X. PMID 11219478.
- Lamb, H. M.; Figgitt, D. P.; 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..
- Manzella, J. P. (December 2001). "Quinupristin-dalfopristin: a new antibiotic for severe gram-positive infections". Am Fam Physician. 64 (11): 1863–6. PMID 11764864..
- Paradisi, Franco; Corti, Giampaolo; Messeri, Daniela (January 2001). "Antistaphylococcal (MSSA, MRSA, MSSE, MRSE) antibiotics". Med. Clin. North Am. (PDF). 85 (1): 1–17. doi:10.1016/s0025-7125(05)70302-3. hdl:2158/329747. PMID 11190346 https://flore.unifi.it/bitstream/2158/329747/1/Antistafilococcici.pdf
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