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 litres

half-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 drugs

ACE 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: possibly increased risk of convulsions with quinolones

Anticoagulants: effects of coumarins enhanced; possibly increased risk of bleeding with heparins and coumarins

Antidepressants: increased risk of bleeding with SSRIs and venlafaxine

Antidiabetic agents: effects of sulphonylureas enhanced

Anti-epileptics: possibly increased phenytoin concentration

Antifungals: if used with fluconazole, halve the dose of celecoxib. Antivirals: increased risk of haematological toxicity with zidovudine; concentration possibly increased by ritonavir

Ciclosporin: may potentiate nephrotoxicity Cytotoxic agents: reduced excretion of methotrexate; increased risk of bleeding with erlotinib

Diuretics: increased risk of nephrotoxicity; antagonism of diuretic effect; hyperkalaemia with potassium-sparing diuretics

Lithium: excretion decreased Pentoxifylline: possibly increased risk of bleeding

Tacrolimus: increased risk of nephrotoxicity

ADMINISTRATION

Reconstition

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Route

Oral

Rate of Administration

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Comments

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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

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 ERF on dialysis if they do not pass any urine. Use with caution in renal transplant recipients – can reduce intrarenal autocoid synthesis

Celecoxib should be used with caution in uraemic patients predisposed to gastrointestinal bleeding or uraemic coagulopathies

Contraindicated in patients with ischaemic heart disease or cerebrovascular disease and class II–IV NYHA congestive heart failure.

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