Table 1.

Data adapted with permission from Table 1 in Kenworthy et al. (1999), showing the percent inhibition achieved by 34 effectors for 11 different CYP3A4 substrates. Italicized values in parentheses represent percent activation.

	DX	DZ	MZ	TZ	TFA	TFZ	ER	CY	TS	NF	BROD	EROD
Astemizole	65	74	78	48	70	70	90	80	83	94	(221)	3
Budesonide	30	48	71	56	73	77	91	77	64	49	(3509)	(3)
Caffeine	8	(2)	0	(22)	(2)	1	3	2	(7)	(3)	34	9
Cisapride	41	72	48	66	43	52	24	52	54	78	(70)	11
Clotrimazole	100	100	100	100	100	100	100	100	100	100	100	64
Clozapine	20	23	26	9	15	14	31	19	43	50	49	11
Cyclosporin	90	87	75	85	68	77	90	93	90	82	90	2
Dextromethorphan	9	5	34	15	15	(17)	9	5	9	28	44	3
Diazepam	(62)	17	25	1	11	9	12	20	22	6	(159)	(3)
Digitoxin	31	27	21	(7)	26	33	57	28	49	47	35	8
Disopyramide	46	54	44	32	6	9	35	38	55	50	50	(3)
Erythromycin	71	63	44	33	23	24	60	64	28	37	71	5
Ethionamide	6	11	(2)	(9)	27	21	0	0	15	2	39	5
Fluconazole	42	59	65	46	35	42	42	53	37	44	90	11
Gentamycin	14	5	(11)	(21)	(10)	(18)	11	2	(1)	1	16	3
Haloperidol	(20)	3	2	52	17	27	33	36	29	96	(33)	1
Ibuprofen	16	(2)	(13)	(9)	(1)	6	0	0	(17)	(1)	25	10
Itraconazole	75	80	86	73	85	88	85	92	97	91	89	(4)
Ketoconazole	96	100	100	100	100	100	100	100	100	100	97	7
Metoclopramide	7	(5)	(8)	2	(7)	6	1	9	6	10	36	27
Metronidazole	(3)	10	0	(6)	(7)	(4)	(3)	3	(15)	3	27	2
Nifedipine	68	47	54	39	41	50	62	70	77	55	71	89
Nimodipine	69	89	60	74	78	76	100	96	96	85	85	27
Nitrendipine	74	63	60	60	43	51	79	84	82	66	28	3
Phenacetin	11	(13)	5	(30)	4	2	2	24	0	26	27	18
Phenytoin	1	4	6	(77)	(4)	6	(16)	3	16	3	36	(1)
Piroxicam	24	3	22	(13)	(3)	3	9	5	14	4	37	6
Procainamide	16	11	2	(15)	3	0	17	(15)	(7)	1	34	7
Propofol	(3)	18	3	11	37	17	7	(7)	19	30	51	8
Quinidine	30	29	47	34	16	20	37	32	49	88	61	13
Roxithromycin	52	37	40	7	11	14	30	37	20	20	71	0
Salbutamol	7	3	1	(9)	(6)	(2)	8	3	6	(1)	31	15
Terfenadine	64	67	77	77	86	86	94	89	88	84	(472)	9
Testosterone	(83)	(7)	28	(39)	35	29	74	60	38	3	(364)	2