TABLE 1

Data 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
Gentamicin 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