Celecoxib
Celecoxib
CLINICAL USE
Cox 2 inhibitor and analgesic
DOSE IN NORMAL RENAL FUNCTION
200 mg once or twice daily
PHARMACOKINETICS
Molecular weight                           :381.4 %Protein binding                           :97 %Excreted unchanged in urine     : <3 Volume of distribution (L/kg)       :400 litreshalf-life – normal/ESRD (hrs)      :8–12/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 on dialysis DOSE IN PATIENTS UNDERGOING RENAL REPLACEMENT THERAPIES
CAPD                :Unlikely to be dialysed. Dose as in normal renal function HD                     :Unlikely to be dialysed. Dose as in normal renal function HDF/high flux   :Unknown dialysability. Dose as in normal renal function CAV/VVHD      :Unknown dialysability. Dose as in GFR 10 to 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 concentrationAntifungals: if used with fluconazole, halve the dose of celecoxib. Antivirals: 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: possibly increased risk of bleedingTacrolimus: increased risk of nephrotoxicity ADMINISTRATION
Reconstition
– Route
Oral 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 retentionInhibition 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 ERF on dialysis if they do not pass any urine. Use with caution in renal transplant recipients – can reduce intrarenal autocoid synthesisCelecoxib should be used with caution in uraemic patients predisposed to gastrointestinal bleeding or uraemic coagulopathiesContraindicated in patients with ischaemic heart disease or cerebrovascular disease and class II–IV NYHA congestive heart failure.
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