Table II.
Analyte | C max (ng/mL) | T max (h) | T 1/2 (h) | AUC (ng h/mL) | V d (L/kg) | Clearance (mL/[min kg]) | AUC ratio metabolite: cocaine |
---|---|---|---|---|---|---|---|
Dose | Mean (SEM) range | Mean (SEM) range | Mean (SEM) range | Mean (SEM) range | Mean (SEM) range | Mean (SEM) range | Mean (SEM) range |
COC | |||||||
IV 40 mg | 301 (61.6)a | 0.17 (0.03)a | 1.1 (0.1)a | 306 (32.2)a | 1.3 (0.2)a | 32.7 (2.7)a | NA |
111–925 | 0.05–0.33 | 0.8–1.5 | 182–656 | 0.3–2.5 | 10.8–53.3 | ||
Oral 100 mg | 115 (14.7)b | 1.3 (0.1)b | 1.2 (0.1)b | 235 (30.0)a | 4.2 (0.5)b | 116.2 (13.1)b | NA |
45.1–201 | 0.8–2.0 | 0.8–1.4 | 115–448 | 1.6–7.5 | 51.5–190.2 | ||
Oral 200 mg | 268 (33.2)a | 1.3 (0.2)b | 1.3 (0.1)c | 654 (90.0)b | 2.9 (0.5)c | 87.5 (12.9)b | NA |
67.0–570 | 0.8–3.0 | 1.0–2.0 | 151–1,510 | 1.2–7.6 | 38.9–221.4 | ||
BZE | |||||||
IV 40 mg | 274 (29)a | 2.0 (0.3)a | 6.0 (0.3)a | 2,886 (204)a | – | – | 10.1 (0.8)a |
172–614 | 0.8–4.0 | 4.7–8.2 | 2,051–4,604 | 5.5–16.2 | |||
Oral 100 mg | 587 (37)b | 2.0 (0.2)a | 5.8 (0.3)b | 5,782 (441)b | – | – | 27.1 (1.9)b |
353–826 | 1.0–3.0 | 4.5–8.2 | 3,785–9,351 | 16.2–38.2 | |||
Oral 200 mg | 951 (56)c | 3.0 (0.2)b | 6.2 (0.3)c | 11,132 (786)c | – | – | 20.1 (2.4)c |
586–1,296 | 1.5–4.0 | 4.8–9.1 | 6,892–16,453 | 8.8–45.9 | |||
EME | |||||||
IV 40 mg | 24 (3)a | 1.9 (0.2) | 5.4 (0.7)a | 226 (32)a | – | – | 0.8 (0.1)a |
7–52 | 1.0–3.0 | 2.9–11.7 | 77–507.1 | 0.3–1.3 | |||
Oral 100 mg | 179 (15)b | 1.9 (0.2) | 3.2 (0.2)b | 1,019 (68.2)b | – | – | 5.2 (0.7)b |
122–277 | 1.0–3.0 | 2.3–4.5 | 680.5–1,524 | 1.8–9.3 | |||
Oral 200 mg | 301 (18)c | 2.2 (0.2)c | 3.4 (0.2)b | 1,976 (119.5)c | – | – | 4.3 (1.1)b |
227–408 | 1.0–4.0 | 2.6–4.2 | 1,176–2,930 | 1.3–17.4 |
*Data are typically means of n = 14. There was a dose effect for all listed parameters (except for EME Tmax), with P values ranging from <0.0001 to 0.027. Values within each analyte that do not share a letter are significantly different.
COC = Cocaine; BZE = Benzoylecgonine; EME = Ecgonine methyl ester; NA = Not applicable.