Table 3.
Pharmacokinetic parameters of intact LDX after oral administration of LDX in the therapeutic range
| Alimentation | LDX dose, mg | N | C max, ng/mL | T max, h | AUC0–t, ng·h/mL | AUC0–∞, ng·h/mL | t ½, h | ||||||||
|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|
| Mean (SD) | % CV | Mean (SD) | % CV | Median (range) | Mean (SD) | % CV | t, h | Mean (SD) | % CV | Mean (SD) | % CV | ||||
| Children with ADHD (aged 6–12 years), single dose | |||||||||||||||
| Boellner et al. [14] | Fasted | 30 | 17 | 21.9 (5.97) | 27.3 | 0.97 (0.14) | 14.4 | NR | 25.54 (8.37) | 32.8 | 48 | 27.88 (9.29) | 33.3 | 0.50 (0.19) | 37.9 |
| Fasted | 50 | 17 | 46.0 (20.7) | 44.9 | 0.98 (0.06) | 6.2 | NR | 56.20 (21.51) | 38.3 | 48 | 57.90 (21.03) | 36.3 | 0.60 (0.44) | 72.8 | |
| Fasted | 70 | 17 | 89.5 (38.5) | 43.0 | 1.07 (0.17) | 16.3 | NR | 107.4 (50.25) | 46.8 | 48 | 108.90 (50.46) | 46.3 | 0.51 (0.19) | 37.6 | |
| Biederman et al. [24] | NR | 70 | 8 | NR | – | NR | – | NR | NR | – | – | NR | – | NR | – |
| Healthy adults (aged 18–55 years), single dose | |||||||||||||||
| Ermer et al. [16] | Fasted | 50 | 20 | 25.6 (13.16) | 51.4 | NR | – | 1 (1–2) | 28.1 (16.1) | 57.3 | 96 | 62.1 (31.4) | NR | 0.6 (0.1) | 16.7 |
| Ermer et al. [10, 33] | Fasted | 50 | 18 | 19.8 (5.6) | 28.3 | 1.2 (0.4) | 28.9 | 1.0 | 23.4 (7.46) | 31.8 | 72 | 25.2 (7.21) | 28.6 | NR | – |
| Haffey et al. [26] | Fasted | 50 | 24 | NR | – | NR | – | NR | NR | – | – | NR | – | NR | – |
| Roesch et al. [43] | NR | 50 | 41 | NR | – | NR | – | NR | NR | – | – | NR | – | NR | – |
| Krishnan and Zhang [23] | Fasted | 70 | 18 | 48.0 (23.8) | NR | 1.15 (0.28) | 24.3 | NR | 59.47 (24.85) | NR | 72 | 66.84 | NR | 0.41 (0.07) | NR |
| Feda | 70 | 18 | 26.2 (11.9) | NR | 2.08 (0.65) | 31.3 | NR | 53.68 (17.72) | NR | 72 | 58.81 | NR | 0.63 (0.20) | NR | |
| Fasted | 70b | 18 | 46.5 (17.0) | NR | 0.97 (0.27) | 27.8 | NR | 53.07 (16.56) | NR | 72 | 55.10 | NR | 0.44 (0.10) | NR | |
| Krishnan et al. [87] | Fasted | 70c | 6 | 58.2 (28.1) | 48.36 | NR | 99.69 | 1.0 (0.5–4.0) | 70.21 (19.80) | 28.19 | 120 | 67.04 (18.94) | 28.26 | 0.47 (0.16) | 34.58 |
| Ermer et al. [40] | Fasted | 70d | 29 | 43.88 (17.96) | NR | 1.5 (0.7) | NR | NR | NR | – | 72 | 62.0 (21.4)e | NR | 0.56 (0.26)e | NR |
| Healthy adults (aged 18–55 years), multiple doses | |||||||||||||||
| Ermer et al. [28] | Fasted | 70f | 40 | 49.1 (32.25) | 65.7 | 1.1 (0.3) | 27.3 | NR | 65.5 (44.0) | 67.2 | 24 | NR | – | 0.4 (0.1) | 25.0 |
| Krishnan and Stark [15] | Fasted | 70g | 11 | 47.9 (18.6) | 38.8 | 1.0 (0.3) | 28.5 | 1 (1–2) | 60.7 (21.0) | 34.6 | 24 | NR | – | 0.4 (NR) | NR |
| Healthy older adults (aged ≥55 years), single dose; Ermer et al. [18] | |||||||||||||||
| 55–64 years, women | NR | 50 | 9 | 41.3 (11.6) | NR | NR | – | 1.0 | NR | – | – | 43.8 (10.4) | NR | 0.5 (0.1) | NR |
| 55–64 years, men | NR | 50 | 8 | 24.7 (9.8) | NR | NR | – | 1.5 | NR | – | – | 35.3 (9.8) | NR | 0.6 (0.2) | NR |
| 65–74 years, women | NR | 50 | 8 | 27.5 (13.0) | NR | NR | – | 1.5 | NR | – | – | 28.5 (8.3) | NR | 0.9 (1.1) | NR |
| 65–74 years, men | NR | 50 | 8 | 33.6 (8.5) | NR | NR | – | 1.0 | NR | – | – | 38.7 (14.2) | NR | 0.6 (0.4) | NR |
| ≥75 years, women | NR | 50 | 6 | 43.0 (17.1) | NR | NR | – | 1.8 | NR | – | – | 51.9 (18.9) | NR | 0.7 (0.4) | NR |
| ≥75 years, men | NR | 50 | 8 | 25.4 (14.0) | NR | NR | – | 1.8 | NR | – | – | 37.6 (13.3) | NR | 0.7 (0.2) | NR |
ADHD attention-deficit/hyperactivity disorder, AUC 0–∞ area under the plasma concentration-time curve from time 0 to infinity, AUC 0–t area under the plasma concentration-time curve from time 0 to the last sampling time at which the analyte was measurable, C max maximum plasma concentration, CV coefficient of variation, LDX lisdexamfetamine dimesylate, NR not reported, SD standard deviation, t last sampling time in the study, t ½ elimination half-life, T max time to C max
aThe high-fat meal used in this study consisted of 1 English muffin with butter, 1 fried egg, 1 slice of American cheese, 1 slice of Canadian bacon, 2 oz (57 g) of hash brown potatoes, and 8 fl oz (240 mL) of whole milk
bOral solution
cRadiolabelled oral solution
dCo-administered with oral Cooperstown cocktail: caffeine 200 mg, dextromerthorphan 30 mg, omeprazole 40 mg, midazolam 0.025 mg/kg
e N = 16
fFifth day of administration
gSeventh day of administration