Dexibuprofen

CLINICAL USE


NSAID and analgesic

DOSE IN NORMAL RENAL FUNCTION

Initially: 600–900 mg daily in divided doses, after food; Maximum 1.2 g daily (900 mg daily for dysmenorrhoea);Maximum single dose: 400 mg (300 mg for dysmenorrhoea)

PHARMACOKINETICS

  • Molecular weight &nbsp &nbsp &nbsp &nbsp &nbsp &nbsp &nbsp &nbsp &nbsp &nbsp &nbsp &nbsp &nbsp :206.3
  • %Protein binding &nbsp &nbsp &nbsp &nbsp &nbsp &nbsp &nbsp &nbsp &nbsp &nbsp &nbsp &nbsp &nbsp :>99
  • %Excreted unchanged in urine &nbsp &nbsp : 82 (mainly as inactive metabolites)
  • Volume of distribution (L/kg) &nbsp &nbsp &nbsp :10–11 litres
  • half-life – normal/ESRD (hrs)&nbsp &nbsp &nbsp :1.6–1.9/Unchanged

    DOSE IN RENAL IMPAIRMENT

    GFR (mL/MIN)

  • 20 to 50 &nbsp &nbsp : Dose as in normal renal function, but avoid if possible
  • 10 to 20 &nbsp &nbsp : Dose as in normal renal function, but avoid if possible
  • <10 &nbsp &nbsp &nbsp &nbsp &nbsp : Dose as in normal renal function, but only use if on dialysis

    DOSE IN PATIENTS UNDERGOING RENAL REPLACEMENT THERAPIES

  • CAPD &nbsp &nbsp &nbsp &nbsp &nbsp &nbsp &nbsp &nbsp:Not dialysed. Dose as in GFR <10 mL/min

  • HD &nbsp &nbsp &nbsp &nbsp &nbsp &nbsp &nbsp &nbsp &nbsp &nbsp :Not dialysed. Dose as in GFR <10 mL/min
  • HDF/high flux &nbsp :Unknown dialysability. Dose as in GFR <10 mL/min
  • CAV/VVHD &nbsp &nbsp &nbsp:Not dialysed. Dose as in GFR=10–20 mL/min

    IMPORTANT DRUG INTERACTIONS

    Potentially hazardous interactions with other drugsACE inhibitors and angiotensin-II antagonists: antagonism of hypotensive effect, increased risk of nephrotoxicity and hyperkalaemiaAnalgesics: avoid concomitant use of 2 or more NSAIDs, including aspirin (increased side effects); avoid with ketorolac (increased risk of side effects and haemorrhage)Antibacterials: possibly increased risk of convulsions with quinolonesAnticoagulants: effects of coumarins enhanced; possibly increased risk of bleeding with heparins and coumarinsAntidepressants: increased risk of bleeding with SSRIs and venlafaxineAntidiabetic agents: effects of sulphonylureas enhancedAnti-epileptics: possibly increased phenytoin concentrationAntivirals: increased risk of haematological toxicity with zidovudine; concentration possibly increased by ritonavirCiclosporin: may potentiate nephrotoxicity Cytotoxic agents: reduced excretion of methotrexate; increased risk of bleeding with erlotinibDiuretics: increased risk of nephrotoxicity; antagonism of diuretic effect; hyperkalaemia with potassium-sparing diureticsLithium: excretion decreased Pentoxifylline: increased risk of bleeding Tacrolimus: increased risk of nephrotoxicity

    ADMINISTRATION

    Reconstition

    Route

    Oral

    Rate of Administration

    Comments

    OTHER INFORMATION

    S (+)– enantiomer of racemic ibuprofen Inhibition of renal prostaglandin synthesis by NSAIDs may interfere with renal function, especially in the presence of existing renal disease – avoid if possible; if not, check serum creatinine 48–72 hours after starting NSAID – if raised, discontinue NSAID therapy. Use normal doses in patients with CKD 5 on dialysisUse with caution in renal transplant recipients – can reduce intrarenal autocoid synthesis.