Monograph
M01AH01 - Celecoxib |
Propably not porphyrinogenic |
PNP |
Rationale
Celecoxib is a substrate of CYP2C9, but does not inhibit CYP2C9 or 3A4. No reports of CYP-inducing effect.
Chemical description
Celecoxib is a diaryl substituted pyrazole derivative containing a sulfonamide substituent.
Therapeutic characteristics
Celecoxib is an NSAID used in the treatment of rheumatoid arthritis including juvenile idiopathic arthritis, osteoarthritis, and ankylosing spondylitis. It is administered orally. Common adverse reactions of celecoxib that can be confused with an acute porphyric attack are abdominal pain, dyspepsia, diarrhoea, and insomnia.
Metabolism and pharmacokinetics
The metabolism of celecoxib is mediated mainly by the cytochrome P450 isoenzyme CYP2C9. Minor substrate of CYP3A4 (Rendic, 2002; Zhou, 2007). Less than 3 % recovered as unchanged rug. Inhibitor of the isoenzyme CYP2D6, but the drug does not inhibit CYP2C9, CYP2C19, or CYP3A4. No observations pointing to CYP-induction in clinical use. Not listed as CYP-inducer.
Personal communication
One report of uneventful use (C.Andersson; patient report).
IPNet drug reports
Uneventful use reported in 3 patients with acute porphyria.
References
| # | Citation details | PMID |
|---|---|---|
| * | Scientific articles | |
| 1. | Rendic, S. Summery of information on human CYP enzymes: human P450 metabolism. Drug metabolism reviews 2002; 34(1&2), 83-448.
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| 2. | Zhou, S.F., Xue, C.C., et al. Clinically important drug interactions potentially involving mechanism-based inhibition of cytochrome P450 3A4 and the role of therapeutic drug monitoring. Ther Drug Monit 2007; 29(6):687:710.
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| * | Drug reference publications | |
| 3. | McEvoy GK, editor. Celecoxib. The AHFS Drug Information 2008. Bethesda, MD: American Society of Health-System Pharmacists; 2009. Electronic version (21.06.10).
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| 4. | Sweetman SC, editor. Martindale: The complete drug reference. Celecoxib. Pharmaceutical Press 2009.
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