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Are all COX-2 medicines the same? Pharmacokinetics and metabolism of coxibs t max (h) Bioavailabili ty (oral, %) t 50% (h) Primary metabolism 5 (cytochrome.

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Presentation on theme: "Are all COX-2 medicines the same? Pharmacokinetics and metabolism of coxibs t max (h) Bioavailabili ty (oral, %) t 50% (h) Primary metabolism 5 (cytochrome."— Presentation transcript:

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2 Are all COX-2 medicines the same?

3 Pharmacokinetics and metabolism of coxibs t max (h) Bioavailabili ty (oral, %) t 50% (h) Primary metabolism 5 (cytochrome P450 enzymes) Sulphonomides Celecoxib Oxidation (CY)2C9, 3A4) 2 Valdecoxib (Parecoxib 1 ) 2-4~ Oxidation to hydroxyvaldecoxib (CYP2C9, 3A4) 2 Methylsuphones Etoricoxib Rofecoxib ~1 2-4 ~100 ~ Oxidation to 6’-hydroxymethyletoricoxib (major role: CYP3A4; ancillary role: CYP2C9, 2D6, 1A2) Cytosolic reductase 3 Arylactic acid Lumiracoxib 1-3~742-6Oxidation to hydroxylumiracoxib 6 (CYP2C9)

4 COX-2 inhibitors versus non-selective NSAID and Congestive Heart Failure (CHF) Outcomes in elderly patients: a population-based cohort study (Mamdani M, et al. The Lancet 2004; 363: )

5 במחקר רטרוספקטיבי רחב היקף נערך מעקב שבדק אשפוזים בשל אי ספיקת לב חמורה של מטופלים בגילאי 66 ומעלה שהחלו טיפול תרופתי בתכשירים הבאים: (n=14,583) vs. Rofecoxib: (n=18,908) vs. Celecoxib: Non-selective NSAIDs: (n=11,606) קבוצת הביקורת האקראית כללה 100,000 נבדקים שכלל לא השתמשו ב-NSAID.

6 Conclusions: “These findings suggest a higher risk of admission for congestive heart failure in users of Rofecoxib and non-selective NSAIDs, but not Celecoxib, relative to non-NSAID controls.”

7 “Relationship between selective cyclooxygenase-2 inhibitors and Acute Myocardial Infarction (AMI) in older adults” Reference: Solomon D.H, et al. Circulation. 2004;109:

8 The Study: 54,475 patients 65 years or older Matched case-control study Complete information was available on prescription medication use and clinical encounters.

9 No elevated risk of AMI with Celecoxib “Celecoxib was not associated with an elevated risk of AMI in these comparisons”.

10 Blood Pressure Destabilization and Edema among 8538 Users of Celecoxib, Rofecoxib, and Nonselective NSAID and Nonusers of NSAID Receiving Ordinary Clinical Care Reference: Wolfe F, et al, J Rheumatol; 2004 ; 31 :

11 CONCLUSION: “Rofecoxib, but not celecoxib and NS NSAID, is associated with an increased risk of edema and blood pressure increase compared to nonusers of NSAID.”

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13 “Rofecoxib has a substantially longer elimination half-life than celecoxib. Further, celecoxib has linear pharmacokinetics with no evidence of accumulation, whereas rofecoxib has non-linear saturable pharmacokinetics. (26) These factors could contribute to a more pronounced hyprtensive effect for Rofecoxib than for celecoxib.” The Lancet, Vol 363, May 29, 2004.

14 Reduced risk of UGI ulcer with Celecoxib “The incidence UGI complications associated with Celecoxib was 8-fold lower than with non-specific NSAIDs. The incidence of ulcer complications observed in Celecoxib-treated was similar to that in patients receiving placebo”. Reference: Goldtein J.L et al, American J. Gastroenterology 2000;95:

15 DOSAGE AND ADMINISTRATION Osteoarthritis: 200mg per day administered as single dose or as 100mg twice a day. Rheumatoid arthritis: 100 to 200mg twice a day. These doses can be given without regard to timing of meals.

16 CELCOX Should not be given to patients with sulfonamide allergies. May be given to G6PD patients.

17 מחירי CELCOX לקהל בקופות החולים (נכון ל-( בטוח רגיל בטוח משלים שירותי בריאות כללית ₪26.20 ₪ מכבי שירותי בריאות55.70 ₪27.85 ₪ קופת חולים מאוחדת12.00 ₪ קופת חולים לאומית55.70 ₪32.70 ₪


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