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Serotonin reuptake inhibitor

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From Wikipedia, the free encyclopedia

Class of drug

This article is about serotonin reuptake inhibitors. For SSRIs, seeselective serotonin reuptake inhibitor.

Aserotonin reuptake inhibitor (SRI) is a type ofdrug which acts as areuptake inhibitor of theneurotransmitter serotonin (5-hydroxytryptamine, or 5-HT) by blocking theaction of theserotonin transporter (SERT). This in turn leads to increasedextracellular concentrations of serotonin and, therefore, an increase inserotonergic neurotransmission. It is a type ofmonoamine reuptake inhibitor (MRI); other types of MRIs includedopamine reuptake inhibitors andnorepinephrine reuptake inhibitors.

SRIs are not synonymous withselective serotonin reuptake inhibitors (SSRIs), as the latter term is usually used to describe theclass ofantidepressants of the same name, and because SRIs, unlike SSRIs, can either beselective or non-selective in theiraction. For example,cocaine, which non-selectively inhibits the reuptake ofserotonin,norepinephrine, anddopamine, is an SRI but not an SSRI.

SRIs are used predominantly asantidepressants (e.g., SSRIs,SNRIs, andTCAs), though they are also commonly used in the treatment of other psychological conditions such asanxiety disorders andeating disorders. Less often, SRIs are also used to treat a variety of othermedical conditions includingneuropathic pain andfibromyalgia (e.g.,duloxetine,milnacipran), andpremature ejaculation (e.g.,dapoxetine) as well as for dieting (e.g.,sibutramine). Additionally, some clinically used drugs such aschlorpheniramine,dextromethorphan, andmethadone possess SRI properties secondarily to their primarymechanism of action(s) and this contributes to theirside effect anddrug interaction profiles.

A closely related type of drug is aserotonin releasing agent (SRA), an example of which isfenfluramine.

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

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

v t e Anxiolytics (N05B)
5-HT_1ARTooltip 5-HT1A receptoragonists	Buspirone Gepirone Tandospirone
GABA_ARTooltip GABAA receptor PAMsTooltip positive allosteric modulators	Benzodiazepines:Adinazolam Alprazolam Bromazepam Camazepam Chlordiazepoxide Clobazam Clonazepam Clorazepate Clotiazepam Cloxazolam Diazepam^# Ethyl loflazepate Etizolam Fludiazepam Halazepam Ketazolam Lorazepam^# Medazepam Nordazepam Oxazepam Pinazepam Prazepam;Others:Alpidem^‡ Barbiturates (e.g.,phenobarbital) Carbamates (e.g.,meprobamate) Carisoprodol Chlormezanone^‡ Ethanol (alcohol) Etifoxine
Gabapentinoids (α₂δ VDCC blockers)	Gabapentin Gabapentin enacarbil Phenibut Pregabalin
Antidepressants	SSRIsTooltip Selective serotonin reuptake inhibitors (e.g.,escitalopram) SNRIsTooltip Serotonin-norepinephrine reuptake inhibitors (e.g.,duloxetine) SARIsTooltip Serotonin antagonist and reuptake inhibitors (e.g.,trazodone) TCAsTooltip Tricyclic antidepressants (e.g.,clomipramine^#) TeCAsTooltip Tetracyclic antidepressants (e.g.,mirtazapine) MAOIsTooltip Monoamine oxidase inhibitors (e.g.,phenelzine);Others:Agomelatine Bupropion Tianeptine Vilazodone Vortioxetine
Sympatholytics (Antiadrenergics)	Alpha-1 blockers (e.g.,prazosin) Alpha-2 agonists (e.g.,clonidine,dexmedetomidine,guanfacine) Beta blockers (e.g.,propranolol,atenolol,betaxolol,nadolol,oxprenolol,pindolol)
Others	Benzoctamine Cycloserine Fabomotizole Hydroxyzine Lorpiprazole Mebicar Mepiprazole Nicotine (tobacco) Opipramol Oxaflozane^‡ Phenaglycodol Phenibut Picamilon Selank Tiagabine Tofisopam Validolum
^#WHO-EM ^‡Withdrawn from market Clinical trials: ^†Phase III ^§Never to phase III

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Comparison of SRIs

Binding profiles

SERT occupancy

List of SERT-selective SRIs

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