Table 3.

Pharmacokinetic data in humans and rats

		Humans								Rats
		i.v. dose mg	oral dose mg	F	CL l/h	Vss l/kg	f up	R b	Urinary excretion (f e) % of dose	i.v. dose mg	oral dose mg	F	CL ml/min/kg	f up	R b
1	Alprazolam	1	1	0.96	3.11	0.72	0.29	0.78	20	0.48	2.67	0.28	133	0.35	0.81
2	Alprenolol	7.25	100	0.06	65.90	2.99	0.18	0.76	0.5	0.5	2.5	0.04	79		1.71
3	Chlorpromazine	10	50	0.31	76.6	8.88	0.06	1.2	< 1	2.5	2.5	0.02	52	0.01	1.48
4	Clozapine	25	200	0.86	13.02	1.6	0.06	0.86	< 1	0.96	3.84	0.05	77.5	0.1	**
5	Cyclosporine	111.45	371.5	0.39	16.50	1.1	0.07	1.36	< 1	1.18	1.18	0.2	2	0.06	1.28
6	Diltiazem	20	120	0.47	48.3	5.2	0.18	1.00	3	1.43	4.28	0.06	42	0.18	0.93
7	Domperidone	10	10	0.39	42.06	5.71	0.08	0.74	< 1	0.63	0.63	0.5	39.2	0.09	1.3
8	Erythromycin	500	500	0.21	18.73	0.60	0.1	0.91	12	0.58	5.63	0.14	105	0.48	**
9	Felodipine	2.5	27.5	0.25	49.4	4.4	0.004	0.7	< 1	0.03	0.74	0.1	61	0.001	0.68
10	Flumazenil	2	30	0.22	72.06	0.97	0.58	1	0.5	0.56	5.63	0.28	147	0.14	**
11	Itraconazole	100	100	0.76	22.86	7.4	0.002	*	< 1	3	3	0.35	9.1	0.009	**
12	Lidocaine	200	300	0.42	42	1.34	0.33	0.87	8	4.25	21.25	0.02	31.8	0.38	1.27
13	Metoprolol	5	5	0.36	65.34	5.18	0.88	1.1	10	0.23	0.23	0.23	65.2	0.80	1.5
14	Midazolam	10.5	20	0.7	19.38	0.74	0.02	0.75	< 1	2.75	4.13	0.25	46	0.06	0.81
15	Mirtazapine	3.5	15	0.4	38.3	3.52	0.15	0.67	4	0.55	2.75	0.07	29.4	0.11	**
16	Nalbuphine	20	60	0.12	90	4.63	0.5	*	7	0.66	6	0.01	63	0.25	**
17	Nicardipine	15	30	0.45	34.57	0.76	0.01	0.71	0	1.14	3.42	0.22	115	0.01	**
18	Nifedipine	1.46	20	0.47	36	1.67	0.04	0.67	0	0.25	0.75	0.46	8.7	0.004	**
19	Nimodipine	2.1	60	0.33	58.8	0.94	0.02	*	< 0.1	0.86	3.42	0.22	1.5	0.03	**
20	Nisoldipine	0.37	20	0.04	50.82	4.1	0.003	*	< 1	0.2	0.2	0.03	45.8	0.009	**
21	Nitrendipine	2	20	0.39	78.89	5.39	0.01	1.46	< 1	1	1	0.12	16.5	0.04	1.46
22	Omeprazole	10	10	0.32	39.48	0.24	0.05	0.59	0	1.33	5.3	0.09	39.2	0.13	0.66
23	Saquinavir	12	600	0.01	60.6	3.63	0.03	0.74	1	2.35	11.75	0.07	88.5	0.05	0.82
24	Sildenafil	50	50	0.41	40.08	1.4	0.04	0.64	0	2.85	2.85	0.06	38.5	0.05	0.56
25	Tacrolimus	1.55	3.88	0.21	78.75	1.74	0.01	35	< 1	0.43	2.13	0.11	16.5	**	1.4
26	Tolterodine	1.28	3.2	0.72	27.72	1.4	0.04	*	1	0.13	3	0.02	166.7	0.15	**
27	Triazolam	0.25	0.25	0.8	12.72	0.58	0.1	0.62	2	0.64	1.28	0.16	51.4	0.28	1.5
28	Venlafaxine	10	50	0.37	60.35	4.4	0.73	1.0	4.6	7.26	7.26	0.13	64.5	0.59	**
29	Verapamil	10	120	0.39	49.7	4	0.09	0.89	< 3	0.13	1.25	0.06	29.3	0.05	0.85
30	Zolmitriptan	3.5	10	0.7	43.06	1.8	0.75	*	8	0.13	0.13	0.41	29.4		**
31	Zolpidem	5	5	0.78	18.85	0.68	0.08	0.66	< 1	0.25	0.25	0.27	15	0.13	0.86

^* When no data were available, a value of R _b of 0.55 should be considered if the drug is an acid, or a value of R _b of 1 if the drug is basic or neutral 56.

^** When rat values were not available, human values were considered.

References for f _up, R _b and urinary excretion are found in Supplemental Table S1.

References for i.v. and oral dose, F, CL, Vss are found in Supplemental Table S2.

Note: Rat Vss values were not needed and human urinary excretion values were used for rat.