Dalfopristin
Also known as: Pristinamycin IIA derivative, RP 54476, Synercid
Summary
Dalfopristin is a semisynthetic streptogramin B antibiotic used exclusively in combination with quinupristin (as Synercid) to treat serious infections caused by vancomycin-resistant Enterococcus faecium (VREF) and complicated skin/skin structure infections caused by susceptible Staphylococcus aureus or Streptococcus pyogenes. The combination exhibits synergistic bactericidal activity.
Mechanism of Action
Inhibits bacterial protein synthesis by binding to the 50S ribosomal subunit, blocking the elongation of peptide chains. Acts synergistically with quinupristin (streptogramin A), with the combination causing irreversible inhibition of protein synthesis.
Routes of Administration
Goals & Uses
- Vancomycin-resistant Enterococcus faecium (VREF) infectionsAntibacterialHigh
- Complicated skin and skin structure infections (cSSSI)AntibacterialHigh
- Hospital-acquired pneumonia (off-label)AntibacterialLow
Contraindications
- Concomitant use of CYP3A4-metabolized drugs with narrow therapeutic indexDrug InteractionHigh
- Hypersensitivity to streptograminsAllergyHigh
Adverse Effects
- Hypersensitivity reactionsImmunologicRare
- Elevated liver enzymes (AST/ALT)HepatotoxicityUncommon
- Infusion site reactions (pain, inflammation, thrombophlebitis)LocalCommon
- Nausea and vomitingGastrointestinalCommon
- Arthralgia and myalgiaMusculoskeletalCommon
- HyperbilirubinemiaHepaticCommon
Drug Interactions
- HMG-CoA reductase inhibitors (statins)Moderate
- MidazolamModerate
- WarfarinModerate
- CyclosporineHigh
- TacrolimusHigh
Population Constraints
- Hepatic impairmentOrgan FunctionRelative
- Pediatric patientsAgeRelative
- Pregnancy (Category B)PregnancyRelative
Regulatory Status
- European UnionApprovedApproved: Infections due to vancomycin-resistant Enterococcus faecium, Nosocomial pneumonia, Complicated skin and skin structure infectionsApproved by EMA as Synercid; indications may vary by member state
- United StatesApprovedApproved: Vancomycin-resistant Enterococcus faecium bacteremia, Complicated skin and skin structure infections due to S. aureus (MSSA) or S. pyogenesApproved by FDA in 1999 as part of Synercid combination (quinupristin/dalfopristin 30:70); accelerated approval pathway used
- United KingdomApprovedApproved: Vancomycin-resistant Enterococcus faecium infections, Complicated skin and skin structure infectionsAvailable as Synercid; used as reserve antibiotic for resistant organisms
Approved by the FDA in 1999 as part of the quinupristin/dalfopristin (Synercid) combination product. Received accelerated approval for VREF infections. Not used as a standalone agent.
Evidence & Sources
No sources recorded yet.