Table 2 The effect of artemisinin (QHS) on the activity of CYP2B6 (bupropion hydroxylation) and CYP3A4 (midazolam hydroxylation) in humans

BUP

1-day

0.35 ± 0.23

327.86 ± 180.54

2.1 (1.5, 4.0)

6.8 ± 1.9

3.73 ± 1.91

2-day

0.34 ± 0.18

305.93 ± 146.69

2.5 (0.8, 5.0)

6.1 ± 1.7

3.78 ± 2.05

Geometric mean ratios (90% CI)

0.96 (0.83, 1.12)

0.93 (0.77, 1.13)

N.A.

0.89 (0.80, 1.00)

1.01 (0.87, 1.17)

OH-BUP

1-day

3.98 ± 1.45**

517.77 ± 162.04**

5.2 (3.0, 11.0)

19.4 ± 1.4

0.29 ± 0.11**

2-day

8.22 ± 3.43**

856.60 ± 245.03**

7.6 (3.0, 24.0)

20.2 ± 1.5

0.14 ± 0.05**

Geometric mean ratios (90% CI)

2.05 (1.83, 2.30)**

1.65 (1.51, 1.82)**

N.A.

1.04 (1.00, 1.07)

0.49 (0.43, 0.55)**

MDZ

1-day

1.00 ± 0.33**

206.03 ± 114.68*

1.3 (0.3, 2.0)

4.1 ± 0.7

1.09 ± 0.33**

2-day

1.55 ± 0.42**

305.26 ± 114.80*

0.8 (0.3, 3.0)

4.2 ± 0.7

0.70 ± 0.21**

Geometric mean ratios (90% CI)

1.55 (1.35, 1.78)**

1.48 (1.12, 1.97)*

N.A.

1.04 (0.96, 1.14)

0.64 (0.55, 0.73)**

OH-MDZ

1-day

0.32 ± 0.09**

82.32 ± 50.26**

1.1 (0.3, 2.0)

3.7 ± 1.0

3.31 ± 0.84**

2-day

1.60 ± 0.26**

242.64 ± 81.98**

1.5 (0.8, 3.0)

4.2 ± 0.5

0.64 ± 0.11**

Geometric mean ratios (90% CI)

4.99 (4.66, 5.33)**

2.95 (2.44, 3.56)**

N.A.

1.14 (1.01, 1.28)

0.19 (0.18, 0.21)**

AUC_OH-BUP/AUC_BUP

1-day

13.36 ± 5.24**

N.A.

N.A.

N.A.

N.A.

2-day

27.33 ± 10.06**

N.A.

N.A.

N.A.

N.A.

Geometric mean ratios (90% CI)

2.05 (1.79, 2.33)**

N.A.

N.A.

N.A.

N.A.

AUC_OH-MDZ/AUC_MDZ

1-day

0.34 ± 0.09**

N.A.

N.A.

N.A.

N.A.

2-day

1.10 ± 0.29**

N.A.

N.A.

N.A.

N.A.

Geometric mean ratios (90% CI)

3.24 (2.84, 3.69)**

N.A.

N.A.

N.A.

N.A.