CLINICAL USE

Antibacterial agent

DOSE IN NORMAL RENAL FUNCTION

7.5 mg/kg every 8 hours

PHARMACOKINETICS

  • Molecular weight                           :1118.3 (quinupristin); 787 (dalfopristin) – as mesilate
  • %Protein binding                           :55–78 (quinupristin); 11–26 (dalfopristin)
  • %Excreted unchanged in urine     : 15 (quinupristin); 19 (dalfopristin)
  • Volume of distribution (L/kg)       :0.45 (quinupristin); 0.24 (dalfopristin)
  • half-life – normal/ESRD (hrs)      :0.9 (quinupristin); 0.7 (dalfopristin)

    DOSE IN RENAL IMPAIRMENT

    GFR (mL/MIN)

  • 20 to 50     : 5–7.5 mg/kg 8–12 hourly
  • 10 to 20     : 5–7.5 mg/kg 8–12 hourly
  • <10           : 5 mg/kg 8–12 hourly

    DOSE IN PATIENTS UNDERGOING RENAL REPLACEMENT THERAPIES

  • CAPD                :Not dialysed.
  • 10 to 20     : mg/kg/day in 2 divided doses1
  • HD                     :Not dialysed. Dose as in GFR <10 mL/min
  • HDF/high flux   :Unknown dialysability. Dose as in GFR <10 mL/min
  • CAV/VVHD      :Unlikely to be dialysed. Dose as in GFR 10 to 20 mL/min

    IMPORTANT DRUG INTERACTIONS

    Potentially hazardous interactions with other drugs

  • Anti-arrhythmics: increased risk of ventricular arrhythmias with disopyramide and lidocaine – avoid concomitant useAnxiolytics and hypnotics: increased concentration of midazolam (risk of profound sedation); metabolism of zopiclone inhibited
  • Calcium-channel blockers: increased concentration of nifedipine
  • Ciclosporin: increased levels of ciclosporin
  • Ergot alkaloids: avoid concomitant use with ergotamine and methysergide
  • Tacrolimus: tacrolimus levels increased by 15%

    ADMINISTRATION

    Reconstition

    With 5 mL glucose 5% or water for injection

    Route

    IV infusion

    through a central line

    Rate of Administration

    Over 60 minutes

    Comments

    Central access is recommended: Dilute reconstituted solution further in —100 mL glucose 5% for central access Or 250 mL for peripheral access (for —emergency administration of 1st dose only). Stable for 5 hours at room temperature and 24 hours if refrigeratedIncompatible with saline solutions

    OTHER INFORMATION

    After the infusion, flush the line with glucose 5% to minimise venous irritationHas been administered intraperitoneally at a dose of 25 mg/L in alternate bags, in combination with intravenous treatmentSynercid is an inhibitor of CYP 3A4: caution is recommended when co-administering any drug also metabolised by this route

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