Parecoxib
CLINICAL USE
Cox 2 inhibitor:Short-term treatment of postoperative pain
DOSE IN NORMAL RENAL FUNCTION
40 mg initially then 20–40 mg every 6–12 hours if required; maximum dose 80 mg daily
PHARMACOKINETICS
Molecular weight                           :392.4 (as sodium salt) %Protein binding                           :98 %Excreted unchanged in urine     : <5 (as valdecoxib) Volume of distribution (L/kg)       :55 litreshalf-life – normal/ESRD (hrs)      :8 (as valdecoxib)/Unchanged DOSE IN RENAL IMPAIRMENT
GFR (mL/MIN)
30–50 Dose as in normal renal function. Use with caution10–30 Dose as in normal renal function, but avoid if possible <10           : Dose as in normal renal function, but only use if ERF on dialysis DOSE IN PATIENTS UNDERGOING RENAL REPLACEMENT THERAPIES
CAPD                :Not dialysed. Dose as in GFR <10 mL/min HD                     :Not dialysed. Dose as in GFR <10 mL/minHDF/high flux   :Not dialysed. Dose as in GFR <10 mL/minCAV/VVHD      :Not dialysed. Dose as in GFR=10–30 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: possible increased risk of convulsions with quinolonesAnticoagulants: enhanced anticoagulant effect of coumarins and phenindione; increased risk of bleeding with heparinAntidepressants: increased risk of bleeding with SSRIs and venlafaxineAntidiabetics: possibly enhanced effect of sulphonylureasAnti-epileptics: possibly enhanced effect of phenytoin Antifungals: if used with fluconazole reduce the dose of parecoxibAntivirals: increased risk of haematological toxicity with zidovudine; concentration possibly increased by ritonavirCiclosporin: potential for increased risk of nephrotoxicityCytotoxic agents: reduced excretion of methotrexate (possible increased risk of toxicity); increased risk of bleeding with erlotinib Diuretics: increased risk of nephrotoxicity; possible antagonism of diuretic effect; increased risk of hyperkalaemia with potassium-sparing diuretics Lithium: reduced excretion of lithium (risk of toxicity)Pentoxifylline: possibly increased risk of bleeding Tacrolimus: increased risk of nephrotoxicity ADMINISTRATION
Reconstition
2 mL sodium chloride 0.9% Route
IV, IM Rate of Administration
–Comments
OTHER INFORMATION
Clinical trials have shown renal effects similar to those observed with comparative NSAIDs. Monitor patient for deterioration in renal function and fluid retention.562 PArECoXiBInhibition 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 therapyUse normal doses in patients with ERF on dialysisUse with caution in renal transplant recipients (can reduce intrarenal autocoid synthesis)Parecoxib should be used with caution in uraemic patients predisposed to gastrointestinal bleeding or uraemic coagulopathiesWorks within 30 minutes Rapidly converted to valdecoxib Contraindicated in patients with ischaemic heart disease or cerebrovascular disease and class II-IV NYHA congestive heart failure.
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