Quinupristine-dalfopristine

The Antibiotic combination of both S, the quinupristine and the dalfopristine , are synthesized starting from the Pristinamycine. They are drugs of the antibiotic class of the Streptogamine S. the trade description in North America is the synercid.

Mechanism of action

The 2 antibiotics are bacteriostatic. The combination of the 2 will give a bactericidal activity, except for the Enterococcus faecium which remains a bacteriostatic action.

The drug will inhibit the early and late phases of the synthesis of bacterial proteins. There is a stable complex which is formed with the bacterial Ribosome, which gets the bactericidal activity.

Indications

  • serious Infections of Enterococcus faecium resistant to the vancomycine.

  • complicated Infections of the skin and soft fabrics with Staph aureus sensitive to the oxacilline and with Streptococcus pyogenes .

Medicamentous interactions

The quinupristine-dalfopristine is a substrate with high affinity of the CYP3A4 and can inhibit the metabolism of substances to weaker affinity for this cytochrome.

  1. Rise of the plasmatic concentrations of cyclosporine

  2. Rise of the plasmatic concentrations of nifédipine
  3. Rise of the plasmatic concentrations of midazolam

It is necessary to check the plasmatic concentrations of the drugs with less strong affinity and to take precautions with the other drugs which one makes pass by the CYP3A4.

Spectrum of activity

Sensitive bacteria gram positive: Enterococcus faecium , Staphylococcus aureus , Staphylococcus epidermidis , Streptococcus pyogenes , Streptococcus pneumoniae

Sensitive bacteria gram negative: Legionella spp. , Moraxella catarrhalis , Neisseria spp.

Pharmacokinetic

  • Time of half-life: between 0,75 and 1 hour

  • Volume of hepatic distribution of 1L/kg
  • Elimination with less than 20% of renal elimination.

Undesirable effects

  1. Turbid Headaches

  2. of the gastro-intestinal Tract: nauseas, diarrhea, vomiting
  3. Reactions to the site of injection: ignition, thrombophlébite (decrease when one injects into a larger vein)
  4. Joint pains
  5. Hyperbilirubinémie

Counter-indication

Pregnancy, breast feeding, and at less than 18 years.

Administration

The report/ratio of the amount is 70:30 for the dalfopristine and the quinupristine, respectively.

Injection IV: 7,5 mg/kg the every 8-12 hours.

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