Quinupristin/dalfopristin

Quinupristin/dalfopristin
Combination of
Quinupristin Antibiotic
Dalfopristin Antibiotic
Clinical data
Pregnancy cat. B (U.S.)
Legal status ℞-only (U.S.)
Routes IV
Identifiers
CAS number 126602-89-9 N
ATC code J01FG02
PubChem CID 23724510
ChemSpider 21106373 Y
ChEMBL CHEMBL1200649 N
 N(what is this?)  (verify)
Quinupristin/dalfopristin
Systematic (IUPAC) name
N-{(6R,9S,10R,13S,15aS,18R,22S,24aS)-18-

{[(3S)-1-azabicyclo[2.2.2]oct-3-ylthio]methyl-22-[4-(dimethylamino)benzyl]- 6-ethyl-10,23-dimethyl-5,8,12,15,17,21,24-heptaoxo-13-phenyldocosahydro-12H- pyrido[2,1-f]pyrrolo-[2,1-l][1,4,7,10,13,16] oxapentaazacyclononadecin-9-yl}-3- hydroxypyridine-2-carboxamide

Clinical data
Pregnancy cat.  ?
Legal status  ?
Pharmacokinetic data
Half-life 3.1 hours
Identifiers
CAS number 120138-50-3
ATC code  ?
PubChem CID 5388937
Chemical data
Formula C53H67N9O10S 
Mol. mass 1022.24 g/mol

Quinupristin/dalfopristin (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 synergestic manner. While each of the two is only a bacteriostatic agent, the combination shows bactericidal activity.

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

Inhibits P450 and enhances the effects of terfenadine, astemizole, indinavir, midazolam, Ca channel blockers, warfarin, cisapride and cyclosporine.

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: 0632064676, 9780632064670 Length: 481 pages

Further reading