pethidine hydrochloride
pethidine hydrochloride.JPG

CLINICAL USE

Opiate analgesia

DOSE IN NORMAL RENAL FUNCTION

IV: 25–50 mg every 4 hoursOral: 50–150 mg every 4 hoursS/C, IM: 25–100 mg every 4 hours

PHARMACOKINETICS

  • Molecular weight                           :283.8
  • %Protein binding                           :60–80
  • %Excreted unchanged in urine     : 5
  • Volume of distribution (L/kg)       :4.17
  • half-life – normal/ESRD (hrs)      :3–6/7–32

    DOSE IN RENAL IMPAIRMENT

    GFR (mL/MIN)

  • 20 to 50     : Dose as in normal renal function
  • 10 to 20     : Use small doses – increase dosing interval to 6 hours and decrease dose by 25%
  • <10           : Avoid if possible. If not, use small doses: increase dosing interval to 8 hours and decrease dose by 50%

    DOSE IN PATIENTS UNDERGOING RENAL REPLACEMENT THERAPIES

  • CAPD                :Unknown dialysability. Dose as in GFR <10 mL/min
  • 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 dialysability. Dose as in GFR 10 to 20 mL/min

    IMPORTANT DRUG INTERACTIONS

    Potentially hazardous interactions with other drugs
  • Anti-arrhythmics: delayed absorption of mexiletine
  • Antidepressants: possible CNS excitation or depression with MAOIs and moclobemide – avoid concomitant use; possibly increased serotonergic effects with duloxetine; increased sedative effects with tricyclics
  • Antipsychotics: enhanced sedative and hypotensive effect
  • Antivirals: concentration reduced by ritonavir but concentration of toxic pethidine metabolite increased – avoid concomitant use
  • Dopaminergics: risk of CNS toxicity with rasagiline – avoid concomitant use; hyperpyrexia and CNS toxicity reported with selegiline – avoid concomitant useSodium oxybate: enhanced effect of sodium oxybate – avoid concomitant use

    ADMINISTRATION

    Reconstition

    Route

    IV, oral, SC, IM

    Rate of Administration

    IV: Bolus 3–4 minutes

    Comments

    OTHER INFORMATION

    Risk of CNS and respiratory depression or convulsions, particularly in ERF patients receiving regular doses, due to accumulation of active metabolite, norpethidine. Norpethidine levels can be measured



    See how to identify renal failure stages according to GFR calculation

    See how to diagnose irreversible renal disease

    Home

  • other drugs