Serotonin reuptake inhibitor
(Redirected from
Serotonin reuptake inhibitors
)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
Medication | SERT | NET | DAT |
---|---|---|---|
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
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
- Citalopram (Celexa)
- Dapoxetine (Priligy)
- Escitalopram (Lexapro, Cipralex)
- Fluoxetine (Prozac)
- Fluvoxamine (Luvox)
- Paroxetine (Paxil, Seroxat)
- Sertraline (Zoloft, Lustral)
Discontinued
- Indalpine (Upstene)
- Zimelidine (Normud, Zelmid)
Never marketed
- Alaproclate (GEA-654)
- Cericlamine (JO-1017)
- Desmethylcitalopram
- Didesmethylcitalopram
- Femoxetine (FG-4963; Malexil)
- Ifoxetine (CGP-15,210-G)
- Omiloxetine
- Panuramine (WY-26,002)
- Pirandamine (AY-23,713)
- RTI-353
- Seproxetine ((S)-norfluoxetine)
Dual serotonin reuptake inhibitors and serotonin receptor modulators
Marketed
- Trazodone (Desyrel)
- Vilazodone (Viibryd)
- Vortioxetine (Trintellix)
Never marketed
- Cianopramine (Ro 11-2465)
- Litoxetine (SL-810,385)
- Lubazodone (YM-992, YM-35,995)
- SB-649,915
Serotonin reuptake inhibition as a weaker/unintended secondary effect
Marketed
- Dextromethorphan (DXM; Robitussin)[7]
- Dextropropoxyphene (Darvon)[8]
- Dimenhydrinate (Dramamine)
- Diphenhydramine (Benadryl)[9]
- Mepyramine (pyrilamine) (Anthisan)[9]
- Mifepristone (Korlym, Mifeprex)[10]
Never marketed
- 4′-Fluorococaine (also a Dopamine reuptake inhibitor)
- NMDA antagonist)
- Sceletium tortuosum(kanna))
- Sceletium tortuosum (kanna))[11]
- Roxindole (EMD-49,980) (also a 5-HT1A and D2-like receptor agonist)
See also
References
- PMID 9537821.
- S2CID 11247427.
- ^ S2CID 12581442.
- ISBN 978-0-19-984550-7.
- S2CID 30691618.
- S2CID 17470375.
- S2CID 38476281.
- PMID 16051647.
- ^ S2CID 16399789.
- PMID 25206868.
- ^ Pharmaceutical compositions containing mesembrine and related compounds. U.S. Patent 6,288,104 Archived 2017-08-21 at the Wayback Machine (PDF)