Celecoxib
Celecoxib.JPG

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

    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 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.



    See how to identify renal failure stages according to GFR calculation

    See how to diagnose irreversible renal disease

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