Table 4.
Pharmacokinetic parameters for DHE and 8′ OH-DHE
| Treatment | Mean (standard deviation)
|
|||
|---|---|---|---|---|
| Cmax (pg/mL) | Tmax (minutes) | AUC0–2h (pg*hour/mL) | AUC0–4h (pg*hour/mL) | |
| DHE | ||||
| IV DHE 1.0 mg, n = 18 | 58321.0 (9157.41) | 3.1 (0.24) | 8018.5 (1503.52) | 9020.1 (1708.87) |
| MAP0004 1.0 mg (first dose), n = 19 | 2474.7 (755.52) | 10.7 (3.00) | 1318.9 (492.51) | – |
| MAP0004 1.0 mg (second dose), n = 19 | 3063.0 (1351.30) | 9.2 (2.55) | 3041.6a,b (1237.48) | |
| 8′ OH-DHE | ||||
| IV DHE 1.0 mg, n = 17 | 328.6 (145.95) | 8.5 (4.33) | 214.2 (80.41) | 311.8 (129.54) |
| MAP0004 1.0 mg (first dose), n = 16 | 97.9 (37.78) | 19.4 (6.55) | 104.9 (40.68) | – |
| MAP0004 1.0 mg (second dose), n = 18 | 117.9 (51.40) | 15.1 (6.39) | 154.9 (81.90) | 277.9a,c (116.99) |
Notes:
a
AUC0–4h is the sum of AUC0–2h for the first and second doses;
b
n = 18;
c
n = 15; Subjects with values below the limit of quantitation were excluded.
Abbreviations: AUC, area under the curve; DHE, dihydroergotamine; IV, intravenous; OH-DHE, hydroxy-dihydroergotamine; Cmax, mean peak plasma concentration; Tmax, median time to peak plasma concentration.