Review
Copyright ©The Author(s) 2016.
World J Gastroenterol. Jan 21, 2016; 22(3): 1260-1278
Published online Jan 21, 2016. doi: 10.3748/wjg.v22.i3.1260
Table 1 Differential inhibitory effects of fluvoxamine on systemic lidocaine and theophylline clearances, and on partial metabolic clearances of theophylline in healthy subjects and cirrhotic patients
ParameterHealthy subjects
Patients with cirrhosis
Child A
Child C
PlaceboFluvoxaminePlaceboFluvoxaminePlaceboFluvoxamine
CL lidocaine12.10 ± 3.384.85 ± 4.85c9.83 ± 3.995.06 ± 1.75c4.21 ± 1.56e3.65 ± 0.99
Inhibition (%)60 (53-77)44 (28-59)9 (0-19)e
Fluvoxamine AUC0-14866 ± 3311277 ± 3812316 ± 790d
CL theophylline0.825 ± 0.2010.302 ± 0.080c0.660 ± 0.2310.310 ± 0.104a0.296 ± 0.124d0.251 ± 0.151
Inhibition (%)64 (59-69)55 (46-66)14 (0-29)
CLf 3-MX0.192 ± 0.0690.008 ± 0.007c0.124 ± 0.0510.011 ± 0.017c0.037 ± 0.012d0.023 ± 0.013a
Inhibition (%)97 (93-100)92 (84-100)38 (18-58)
CLf 1-MU0.220 ± 0.0890.021 ± 0.019c0.178 ± 0.0720.026 ± 0.018c0.066 ± 0.025d0.039 ± 0.019a
Inhibition (%)93 (89-98)83 (73-93)36 (15-57)
CLf 1,3-DMU0.290 ± 0.0700.136 ± 0.024c0.222 ± 0.0580.138 ± 0.026c0.087 ± 0.040d0.079 ± 0.037
Inhibition (%)58 (49-67)43 (29-58)7 (0-22)
CLR theophylline0.123 ± 0.0330.136 ± 0.0300.136 ± 0.0500.135 ± 0.0430.106 ± 0.0470.110 ± 0.062
Inhibition (%)---
Fluvoxamine Css75 ± 2695 ± 40130 ± 26b
Table 2 Effect of erythromycin on the pharmacokinetic parameters of quinine and 3-hydroxyquinine in healthy subjects and cirrhotic patients
ParameterHealthy subjects
Patients with cirrhosis
Child A
Child C
PlaceboErythromycinPlaceboErythromycinPlaceboErythromycin
CL quinine1.775 ± 0.3101.161 ± 0.309a1.504 ± 0.3621.040 ± 0.303a1.281 ± 0.394b1.401 ± 0.534
Inhibition (%)33 (27-38)30 (26-34)-7 (-16-2)f
CLf 3-hydroxiquinine0.174 ± 0.0510.059 ± 0.017c0.140 ± 0.0770.056 ± 0.032c0.085 ± 0.028d0.037 ± 0.023c
Inhibition (%)65 (61-70)61 (56-67)59 (46-72)
Unbound quinine (%)6.7 ± 0.89.4 ± 1.0c7.1 ± 1.610.3 ± 2.8c11.9 ± 3.7f19.9 ± 5.5cf
Increase (%)41 (28-55)45 (33-55)76 (42-111)b
CLu quinine26.81 ± 11.4912.30 ± 3.16c21.18 ± 8.4510.10 ± 3.88c10.95 ± 2.19f7.24 ± 2.77bc
Inhibition (%)51 (44-59)50 (45-55)35 (21-48)b
CLuf 3-hydroxiquinine2.63 ± 0.880.64 ± 0.20c1.97 ± 1.090.55 ± 0.31c7.01 ± 3.33f4.06 ± 2.58ad
Inhibition (%)75 (70-80)73 (70-77)74 (64-84)
Erythromycin Css1.33 ± 0.251.18 ± 0.441.85 ± 1.00