Quinupristin/dalfopristin
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| File:Dalfopristin.png
Quinupristin (top) and dalfopristin (bottom)
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| Combination of | |
|---|---|
| Quinupristin | Streptogramin antibiotic |
| Dalfopristin | Streptogramin antibiotic |
| Clinical data | |
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| Legal status |
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| Routes of administration |
IV |
| Identifiers | |
| CAS Number | 126602-89-9  |
| ATC code | J01FG02 (WHO) |
| PubChem | CID: 23724510 |
| ChemSpider | 21106373  |
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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.
Contents
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
- ↑ 1.0 1.1 1.2 1.3 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
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- http://www.fda.gov/cder/consumerinfo/druginfo/SYNERCID.HTM
