Table 5.
Pharmacokinetic estimates of prasugrel's active metabolite (Pras-AM) in healthy subjects and in patients with sickle cell disease across the three doses of prasugrel
Parameter | Healthy subjects | Patients with sickle cell disease | ||||
---|---|---|---|---|---|---|
10 mg (n = 13) | 7.5 mg (n = 9) | 5 mg (n = 4) | 10 mg (n = 12) | 7.5 mg (n = 8) | 5 mg (n = 4) | |
Pras-AM AUC(0–tlast) (ng h ml−1) | 67.5 (28) | 50.4 (23) | 39.8 (21) | 66.8 (36) | 45.2 (32) | 36.0 (7) |
Pras-AM Cmax (ng ml−1) | 71.8 (49) | 62.5 (21) | 40.9 (20) | 63.0 (48) | 38.2 (59) | 42.0 (19) |
Pras-AM CL/F (l h−1) | 148.1 (28) | 148.7 (23) | 125.6 (21) | 149.7 (36) | 166.1 (32) | 138.8 (7) |
Median (minimum–maximum) | ||||||
---|---|---|---|---|---|---|
Pras-AM tmax (h) | 0.75 (0.50–1.00) | 0.75 (0.50–0.75) | 0.63 (0.50–1.00) | 0.65 (0.25–2.08) | 0.50 (0.25–1.50) | 0.51 (0.50–1.00) |
Data expressed as geometric mean (%CV).
Abbreviations are as follows: AUC(0–tlast), area under the plasma concentration–time curve from time of dosing to the sampling time of the last quantifiable concentration; Cmax, maximal observed concentration; CL, clearance; CV, coefficient of variance; F, bioavailability; Pras-AM, prasugrel active metabolite; and tmax, time of Cmax.