TABLE 4

Summary of predictions of drug-drug interactions for CYP1A2

Inhibiting Drug	IC₅₀^a	f_u	Affected Drug	Predicted Magnitude of Drug Interaction							Actual Drug Interaction
Inhibiting Drug	IC₅₀^a	f_u	Affected Drug					[I] = C_sys	[I] = f_u × C_sys	[I] = C_{hep,inlet(est)}	Actual Drug Interaction	[I] = f_u × C_{hep,inlet(est)}
	μM
Cimetidine	>300	0.79	Theophylline	1.02	1.01	1.12	1.09	1.63
Citalopram	>300	0.20	Theophylline	1.00	1.00	1.00	1.00	1.04
Clarithromycin	>300	0.30	Theophylline	1.01	1.00	1.08	1.02	1.05
Diltiazem	>300	0.22	Theophylline	1.00	1.00	1.01	1.00	1.28
Disulfiram	1.3	0.04	Theophylline	1.00	1.00	4.58	2.02	1.44
Enoxacin	220	0.45	Theophylline	1.06	1.03	1.39	1.19	3.67
Erythromycin	>300	0.16	Theophylline	1.01	1.00	1.04	1.01	1.38
Fluconazole	>300	0.89	Theophylline	1.03	1.02	1.05	1.04	1.19
Fluoxetine	240	0.05	Clozapine	1.00	1.00	1.01	1.00	1.58
Fluvoxamine	0.035	0.23	Theophylline	4.08	2.74	4.95	4.79	3.33
Ketoconazole	25	0.01	Theophylline	1.19	1.00	1.92	1.01	1.11
Metronidazole	>300	0.89	Theophylline	1.14	1.13	1.35	1.31	0.96
Nefazodone	52	0.009	Theophylline	1.11	1.00	1.57	1.01	0.97
Paroxetine	8.4	0.05	Clozapine	1.02	1.00	1.31	1.02	1.31
Propranolol	17	0.10	Theophylline	1.05	1.00	3.31	1.48	2.08
Ranitidine	>300	0.85	Theophylline	1.00	1.00	1.03	1.03	1.00
Risperidone	>300	0.11	Clozapine	1.00	1.00	1.00	1.00	0.92
Roxithromycin	>300	0.14	Theophylline	1.02	1.00	1.03	1.00	1.16
Sertraline	13	0.02	Clozapine	1.02	1.00	1.45	1.01	1.11
Terbinafine	12	0.01	Theophylline	1.65	1.01	2.56	1.03	1.16
Ticlopidine	11	0.02	Theophylline	1.44	1.01	3.43	1.12	1.58
Troleandomycin	>300	0.15^b	Theophylline	1.00	1.00	1.04	1.01	2.00

↵ a Used a value of IC₅₀ = 1000 μM for those drugs for which the measured value was greater than 300 μM
↵ b Used an estimated fraction unbound value for troleandomycin of 0.15