Risk of upper gastrointestinal bleeding among users of antidepressant compounds and the binding and selectivity characteristics of those compounds for the human serotonin transporter

Drug	*Adjusted Relative Risk (95% CI)**	Geometric mean of equilibrium dissociation constant for serotonin transporter K_D ± SEM (nmol)	Selectivity for serotonin transporter over norepinephrine transporter	Selectivity for serotonin transporter over dopamine transporter
Trazodone*	8.6 (2.1 to 35.1)	160 (20)	53	46
Paroxetine*	4.3 (2.2 to 8.3)	0.13 (0.01)	300	3700
Sertraline*	3.9 (1.1 to 8.3)	0.29 (0.01)	1400	86
Fluoxetine*	2.5 (1.4 to 4.7)	0.81 (0.02)	300	4300
Clomipramine*	2.1 (0.9 to 5.1)	0.28 (0.01)	130	7800
Imipramine	2.1 (0.7 to 6.2)	1.40 (0.03)	27	6100
Amitriptyline	1.9 (1.2 to 2.9)	4.30 (0.12)	8.1	760
Lofepramine	1.8 (0.8 to 4.0)	70 (4)	0.077	260
Trimipramine	1.2 (0.2 to 6.0)	149 (6)	16	25
Mianserine	1.1 (0.1 to 9.2)	4000 (300)	0.018	0.24
Dothiepin	1.0 (0.6 to 1.6)	8.6 (0.4)	5.3	620
Nortriptyline	0.3 (0.0 to 3.5)	18 (1)	0.24	62
Fluvoxamine*	Not available	2.2 (0.2)	580	4100
Venlafaxine	Not available	8.9 (0.3)	120	1000
Chlorpheniramine�	Not available	15.2 (0.8)	94.7	69.7
Diphenhydramine�	Not available	3800 (400)	0.25	0.58

* Compounds classified as selective serotonin reuptake inhibitors by de Abajo et al.⁴
� H₁ antihistamine compounds included for comparative purposes
Equilibrium dissociation constants and selectivity data derived from those published by Tatsumi et al.⁷