Drug | Dose | AUC Parent Drug | AUC Acylglucuronide | Average Therapeutic Dose | Estimated AUC Acylglucuronide at Therapeutic Dosea | Acylglucuronide t1/2 at pH 7.4, 37°Cb |
---|---|---|---|---|---|---|
mg | nmol × h/ml | mg/day | nmol × h/ml | h | ||
Beclobratec | 100 | 230 | 21.6d | 100 | 21.6 | 22.7 (−), 25.7 (+) |
Carprofene | 50 | 86.1 | 40.9 | 300 | 245 | 1.7 (R), 1.9 (S) |
Dabigatranf | 150 | 2.48 | 0.36d | 300 | 0.7 | 1 |
Fenoprofeng | 600 | 1785 | 66.7 | 2400 | 267 | 1 (R), 2 (S) |
Ibuprofenh | 800 | 703 | 27.7d | 3200 | 111 | 3.3 |
Ketoprofeng | 50 | 56.1 | 13.1 | 300 | 78.6 | 0.7 (R), 1.4 (S) |
Naproxeng | 250 | 2553 | 30.5 | 1650 | 201 | 0.9 (R), 1.8 (S) |
Tolmeting | 400 | 289 | 6.30 | 1800 | 28.4 | 0.26 |
Zomepiracg | 100 | 9.4 | 10.3 | 600 | 61.8 | 0.45–0.5 |
↵a Assuming linear dose-exposure relationships.
↵b Data for acylglucuronide half-lives are taken from Shipkova et al. (2003) and Ebner et al. (1999).
↵c Data from Mayer et al. (1993).
↵d AUC data from repeated dose study.
↵e Data from Iwakawa et al. (1989).
↵f Dosed as dabigatran etexilate (Stangier et al., 2008).
↵g Data from Spahn-Langguth et al. (1992).
↵h Data from Castillo et al. (1995).