Quinupristin and Dalfopristin
- Atc Codes:J01FG02
- CAS Codes:120138-50-3#112362-50-2
- PHARMGKB ID:120138-50-3#112362-50-2
Table of contents
- Brand Names
- Chemistry
- Pharmacologic Category
- Mechanism of Action
- Therapeutic Use
- Pregnancy and Lactation Implications
- Contraindications
- Warnings and Precautions
- Adverse Reactions
- Inhibits
- Drug Interactions
- Dosage
- Pharmacokinetics and Pharmacodynamics
Brand Names
Europe
Austria: Synercid; Bulgaria: Synercid; Czech Republic: Synercid; France: Synercid; Germany: Synercid; Greece: Synercid; Hungary: Synercid; Ireland: Synercid; Italy: Synercid; Luxembourg: Synercid; Netherlands: Synercid; Poland: Synercid; Portugal: Synercid.
North America
USA: Synercid.
Asia
Japan: Synercid.
Drug combinations
Chemistry
Quinupristin: C~53~H~67~N~9~O~10~S. Mw: 1022.22. (1) Virginiamycin S~1~, 4-[4-(dimethylamino)-N-methyl-L-phenylalanine]-5-[5-[(1-azabicyclo[2.2.2]oct-3-ylthio)methyl]-4-oxo-L-2-piperidinecarboxylic acid]-, (S)-; (2) N-[(6R,9S,10R,13S,15aS,18R,22S,24aS)-22-[p-(Dimethylamino)benzyl]-6-ethyldocosahydro-10,23-dimethyl-5,8,12,15,17,21,24-heptaoxo-13-phenyl-18-[[(3S)-3-quinuclidinylthio]methyl]-12H-pyrido[2,1-f]pyrrolo[2,1-l][1,4,7,10,13,16]oxapentaazacyclononadecin-9-yl]-3-hydroxypicolinamide. CAS-120138-50-3 (1993).
Dalfopristin: C~34~H~50~N~4~O~9~S. Mw: 690.85. (1) Virginiamycin M~1~, 26-[[2-(diethylamino)ethyl]sulfonyl]-26,27-dihydro-, (26R,27S)-; (2)(3R,4R,5E,10E,12E,14S,26R,26aS)-26-[[2-(Diethylamino)ethyl]sulfonyl]-8,9,14,15,24,25,26,26a-octahydro-14-hydroxy-3-isopropyl-4,12-dimethyl-3H-21,18-nitrilo-1H,22H-pyrrolo[2,1-c][1,8,4,19]dioxadiazacyclotetracosine-1,7,16,22(4H,17H)-tetrone. CAS-112362-50-2 (1993).
Pharmacologic Category
Miscellaneous Antibacterials; Streptogramins. (ATC-Code: J01FG02).
Mechanism of action
Quinupristin/dalfopristin inhibits bacterial protein synthesis by binding to different sites on 50 S bacterial ribosomal subunit, thereby inhibiting protein synthesis.
Therapeutic use
Treatment of serious or life-threatening infections associated with vancomycin-resistant Enterococcus faecium bacteremia. Treatment of complicated skin and skin structure infections caused by methicillin-susceptible Staphylococcus aureus or Streptococcus pyogenes.
Pregnancy and lactiation implications
Adverse effects not observed in animal reproduction studies. There are no adequate, well-controlled studies in pregnant women. Caution if administering to a nursing woman.
Unlabeled use
Contraindications
Hypersensitivity to quinupristin, dalfopristin, pristinamycin, or virginiamycin, or any component of the formulation.
Warnings and precautions
May cause arthralgias and/or myalgias with use. May cause hyperbilirubinemia (>5 times ULN) possibly through competition for excretory pathways. May cause pain and phlebitis when infused through peripheral line. Prolonged use may result in fungal or bacterial superinfection, including C. difficile-associated diarrhea and pseudomembranous colitis. Concurrent therapy with cisapride (which may prolong QTc interval and lead to arrhythmias) should be avoided. May inhibit metabolism of many drugs metabolized by CYP3A4.