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Antidepressants - Receptor affinities

Date Created: 05/04/1999 Last Modified: 11/10/1999 Last Checked: 21/10/2002

Potency as 5 HT reuptake inhibitors (highest to lowest)

Paroxetine 0.13 Clomipramine 0.28
Sertraline 0.29 Fluoxetine 0.81
Citalopram 1.16 Imipramine 1.4

Fluvoxamine 2.2 Amitriptyline 4.3
Dothiepin 8.6 Venlafaxine 8.9

Nortriptyline 18 Doxepin 68
Lofepramine 70 Trimipramine 149
Trazodone 160 Nefazodone 200
Mianserin 4000 Bupropion 9100

Note- venlafaxine appears weaker as an ‘SRI’ than is imipramine, at least by this receptor data.

No drug that is weaker than amitryptiline as an serotonin reuptake inhibitor has caused serotonin syndrome, except for venlafaxine.

Nefazodone is 1,500 times weaker than paroxetine; it would be surprising if this was not clinically significant. Other evidence concerning nefazodone’s modest degree of effectiveness suggests that this is, indeed, of relevance.