Serotonin reuptake inhibitor

Source: Wikipedia, the free encyclopedia.
This article is about serotonin reuptake inhibitors. For SSRIs, see selective serotonin reuptake inhibitor.
Serotonin

A serotonin reuptake inhibitor (SRI) is a type of

extracellular concentrations of serotonin and, therefore, an increase in serotonergic neurotransmission. It is a type of monoamine reuptake inhibitor (MRI); other types of MRIs include dopamine reuptake inhibitors and norepinephrine reuptake inhibitors
.

SRIs are not synonymous with

class of antidepressants of the same name, and because SRIs, unlike SSRIs, can either be selective or non-selective in their action. For example, cocaine, which non-selectively inhibits the reuptake of serotonin, norepinephrine, and dopamine
, is an SRI but not an SSRI.

SRIs are used predominantly as

chlorpheniramine, dextromethorphan, and methadone possess SRI properties secondarily to their primary mechanism of action(s) and this contributes to their side effect and drug interaction
profiles.

A closely related type of drug is a serotonin releasing agent (SRA), an example of which is fenfluramine.

Comparison of SRIs

Binding profiles

Binding affinities of SRIs at MATs[1][2]
Medication SERTTooltip Serotonin transporter NETTooltip Norepinephrine transporter DATTooltip Dopamine transporter
Citalopram 1.16 4070 28100
Desmethylcitalopram 3.6 1820 18300
Escitalopram 1.1 7841 27410
Femoxetine 11.0 760 2050
Fluoxetine 0.81 240 3600
Fluvoxamine 2.2 1300 9200
Norfluoxetine
 1.47 1426 420
Paroxetine 0.13 40 490
Sertraline 0.29 420 25
Desmethylsertraline 3.0 390 129
Zimelidine 152 9400 11700
Levomilnacipran[3] 19.0 10.5 ND
Venlafaxine 8.9 1060 9300
Vilazodone[3] 1.6 ND ND
Vortioxetine[3] 5.4 ND ND
Amitriptyline 4.30 35 3250
Clomipramine 0.28 38 2190
Imipramine 1.40 37 8500

SERT occupancy

SERT occupancy by SRIs at clinically approved dosages
Medication Dosage range
(mg/day)[4]		 ~80% SERT
occupancy
(mg/day)[5][6]		 Ratio (dosage /
80% occupancy)
Citalopram 20–40 40 0.5–1
Escitalopram 10–20 10 1–2
Fluoxetine 20–80 20 1–4
Fluvoxamine 50–350 70 0.71–5
Paroxetine 10–60 20 0.5–3
Sertraline 25–200 50 0.5–4
Duloxetine 20–120 30 0.67–2
Venlafaxine 75–375 75 1–5
Clomipramine 50–250 10 5–25

List of SERT-selective SRIs

Many SRIs exist, an assortment of which are listed below. Note that only SRIs selective for the SERT over the other

SNDRI
.

Selective serotonin reuptake inhibitors (SSRIs)

Marketed

Discontinued

Never marketed

Dual serotonin reuptake inhibitors and serotonin receptor modulators

Marketed

Never marketed

Serotonin reuptake inhibition as a weaker/unintended secondary effect

Marketed

Never marketed

See also

References

  1. PMID 9537821
    .
  2. S2CID 11247427
    .
  3. ^
    S2CID 12581442
    .
  4. ISBN 978-0-19-984550-7
    .
  5. S2CID 30691618
    .
  6. S2CID 17470375
    .
  7. S2CID 38476281
    .
  8. PMID 16051647
    .
  9. ^
    S2CID 16399789
    .
  10. PMID 25206868
    .
  11. ^ Pharmaceutical compositions containing mesembrine and related compounds. U.S. Patent 6,288,104 Archived 2017-08-21 at the Wayback Machine (PDF)
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