. Author manuscript; available in PMC: 2018 Dec 14.

Published in final edited form as: Pharm Res. 2018 Oct 25;35(12):243. doi: 10.1007/s11095-018-2526-y

Table I.

Inhibition of the Human (h) OCT1 and OCT2-Mediated Morphine Uptake by the Drugs Commonly Co-Administered with Morphine

Drug	C_max,unbound^a [μM]	C_{max port,unbound}^b [μM]	hOCT I			hOCT2
			IC₅₀ [μM]	C_max,unbound/IC₅₀	C_max,unbound/IC₅₀	IC₅₀ [μM]	C_max,unbound/IC₅₀
Fluoxetine	0.01	0.7	9.06 ± 3.24	0.001	0.08	3.32 ± 0.76	0.003
Imipramine	0.07	4.5	4.03 ± 1.62	0.02	1.12	0.52 ± 0.1 1	0.13
Amitriptyline	0.01	4.3	1.89 ± 0.77	0.005	2.28	0.41 ± 0.05	0.02
Irinotecan	3.89	3.9	1.36 ± 0.43	2.86	2.87	0.3 1 ± 0.07	12.55
Ondansetron	0.08	0.08	0.27 ± 0.10	0.30	0.30	0.24 ± 0.05	0.33
Verapamil	0.06	1.7	9.62 ± 3.63	0.04	0.18	3.24 ± 0.70	0.02

C_max,unbound: maximal plasma concentration of the unbound drug; C_{max port,unbound}, maximal unbound plasma concentration in the portal vein

The maximal plasma concentration (C_max) was obtained from Goodman and Gilman’s The Pharmacological Basis of Therapeutics except for the C_max of ondansetron (Zofran, information for prescribers) and fluoxetine (23)

The maximal unbound plasma concentration in the portal vein (C_{max prot,unbound},) was calculated by Tzvetkov et al. (12)