Parecoxib – kdc

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 litres

half-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/min

HDF/high flux :Not dialysed. Dose as in GFR <10 mL/min

CAV/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 hyperkalaemia

Analgesics: 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 quinolones

Anticoagulants: enhanced anticoagulant effect of coumarins and phenindione; increased risk of bleeding with heparin

Antidepressants: increased risk of bleeding with SSRIs and venlafaxineAntidiabetics: possibly enhanced effect of sulphonylureas

Anti-epileptics: possibly enhanced effect of phenytoin

Antifungals: if used with fluconazole reduce the dose of parecoxib

Antivirals: increased risk of haematological toxicity with zidovudine; concentration possibly increased by ritonavir

Ciclosporin: 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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