Celecoxib
Mechanism :
Celecoxib is a nonsteroidal anti-inflammatory drug that exhibits anti-inflammatory, analgesic, and antipyretic activities. The mechanism of action is believed to be due to inhibition of prostaglandin synthesis, primarily via inhibition of cyclooxygenase-2 (COX-2. It does not inhibit the cyclooxygenase-1 (COX-1) isoenzyme.
Indication :
- For relief of the signs and symptoms of juvenile rheumatoid arthritis in patients 2 years and older
Contraindications :
Contraindicated in patients with known hypersensitivity to celecoxib, in patients who have demonstrated allergic-type reactions to sulfonamides, in patients who have experienced asthma, urticaria, or allergic-type reactions after taking aspirin or other NSAIDs. Severe, rarely fatal, anaphylactic-like reactions to NSAIDs have been reported in such patients. Contraindicated for the treatment of peri-operative pain in the setting of coronary artery bypass graft (CABG) surgery.
Dosing :
<2 years:
Safety and efficacy not established.
≥2 years:
10 kg to 25 kg: 50 mg capsule twice daily.
>25 kg:
100 mg capsule twice daily.
Adverse Effect :
Headache, hypertension, upper abdominal pain, nausea, diarrhea and vomiting.
Interaction :
General: Celecoxib metabolism is predominantly mediated via cytochrome P450 2C9 in the liver. Co-administration of celecoxib with drugs that are known to inhibit 2C9 should be done with caution.
ACE-inhibitors: NSAIDs may diminish the antihypertensive effect of Angiotensin Converting Enzyme (ACE) inhibitors. This interaction should be given consideration in patients taking Celebrex concomitantly with ACE-inhibitors.
Aspirin: Concomitant administration of aspirin increases the rate of GI ulceration or other complications.
Fluconazole: Concomitant administration of fluconazole at 200 mg QD resulted in a two-fold increase in celecoxib plasma concentration.
Furosemide: NSAIDs can reduce the natriuretic effect of furosemide and thiazides in some patients. This response has been attributed to inhibition of renal prostaglandin synthesis.
Lithium: Patients on lithium treatment should be closely monitored when Celecoxib is introduced or withdrawn.
Methotrexate: In an interaction study of rheumatoid arthritis patients taking methotrexate, Celecoxib did not have a significant effect on the pharmacokinetics of methotrexate.
Warfarin: Anticoagulant activity should be monitored, particularly in the first few days, after initiating or changing Celecoxib therapy in patients receiving warfarin or similar agents.
Renal Dose :
Dose in Renal Impairment GFR (mL/min)
| 30-50 | Dose as in normal renal function. Use with caution |
| 10-30 | 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=10–20 mL/min |
Hepatic Dose :
Moderate hepatic impairment: Reduce dose by 50%.
Severe hepatic impairment: Use is contraindicated.