请输入您要查询的百科知识:

 

词条 Serotonin reuptake inhibitor
释义

  1. Comparison of SRIs

     Binding profiles  SERT occupancy 

  2. 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 

  3. See also

  4. References

{{About|serotonin reuptake inhibitors|SSRIs|selective serotonin reuptake inhibitor}}

A serotonin reuptake inhibitor (SRI) is a type of drug which acts as a reuptake inhibitor of the neurotransmitter serotonin (5-hydroxytryptamine (5-HT)) by blocking the action of the serotonin transporter (SERT). This in turn leads to increased 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 selective serotonin reuptake inhibitors (SSRIs), as the latter term is usually used to describe the 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 antidepressants (e.g., SSRIs, SNRIs, and TCAs), though they are also commonly used in the treatment of other psychological conditions such as anxiety disorders and eating disorders. Less often, SRIs are also used to treat a variety of other medical conditions including neuropathic pain and fibromyalgia (e.g., duloxetine, milnacipran), and premature ejaculation (e.g., dapoxetine) as well as for dieting (e.g., sibutramine). Additionally, some clinically used drugs such 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.

{{TOC limit|3}}

Comparison of SRIs

Binding profiles

MATs|monoamine transporters}}[1]
Medication SERT|Serotonin transporterNET|Norepinephrine transporterDAT|Dopamine transporter
Citalopram 1.16 4070 28100
Desmethylcitalopram 3.6 1820 18300
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[2] 19.0 10.5 ND|No data}}
Venlafaxine 8.9 1060 9300
Vilazodone[2] 1.6 ND|No data}}ND|No data}}
Vortioxetine[2] 5.4 ND|No data}}ND|No data}}
Amitriptyline 4.30 35 3250
Clomipramine 0.28 38 2190
Imipramine 1.40 37 8500

SERT occupancy

SERT|Serotonin transporter}} occupancy by SRIs at clinically approved dosages
Medication Dosage range
(mg/day)[3]
SERT|Serotonin transporter
occupancy
(mg/day)[4][5]
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 20–60 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 monoamine transporters (MATs) are listed below. For a list of SRIs that act at multiple MATs, see other monoamine reuptake inhibitor pages such as SNRI and 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 (Brintellix)

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

  • Chlorpheniramine (Chlor-Trimeton)[6][1]
  • Dextromethorphan (DXM; Robitussin)[7]
  • Dextropropoxyphene (Darvon)[8]
  • Dimenhydrinate (Dramamine)
  • Diphenhydramine (Benadryl)[9]
  • Mepyramine (pyrilamine) (Anthisan)[9]
  • Mifepristone (Korlym, Mifeprex)[10]

Never marketed

  • Delucemine (also an NMDA antagonist)
  • Mesembrenone (also a weak PDE4 inhibitor (found in Sceletium tortuosum (kanna))
  • Mesembrine (also a weak PDE4 inhibitor (found in Sceletium tortuosum (kanna))[11]
  • Roxindole (EMD-49,980) (also a 5-HT1A and D2-like receptor agonist)

See also

  • Monoamine reuptake inhibitor

References

1. ^{{cite journal | vauthors = Tatsumi M, Groshan K, Blakely RD, Richelson E | title = Pharmacological profile of antidepressants and related compounds at human monoamine transporters | journal = Eur. J. Pharmacol. | volume = 340 | issue = 2-3 | pages = 249–58 | year = 1997 | pmid = 9537821 | doi = 10.1016/s0014-2999(97)01393-9| url = }}
2. ^{{cite journal | vauthors = Deardorff WJ, Grossberg GT | title = A review of the clinical efficacy, safety and tolerability of the antidepressants vilazodone, levomilnacipran and vortioxetine | journal = Expert Opin Pharmacother | volume = 15 | issue = 17 | pages = 2525–42 | year = 2014 | pmid = 25224953 | doi = 10.1517/14656566.2014.960842 | url = }}
3. ^{{cite book|author1=Gerald P. Koocher|author2=John C. Norcross|author3=Beverly A. Greene Ph.D.|title=Psychologists' Desk Reference|url=https://books.google.com/books?id=Ox1wAgAAQBAJ&pg=PA442|date=4 September 2013|publisher=Oxford University Press|isbn=978-0-19-984550-7|pages=442–}}
4. ^{{cite journal | vauthors = Gründer G, Hiemke C, Paulzen M, Veselinovic T, Vernaleken I | title = Therapeutic plasma concentrations of antidepressants and antipsychotics: lessons from PET imaging | journal = Pharmacopsychiatry | volume = 44 | issue = 6 | pages = 236–48 | year = 2011 | pmid = 21959785 | doi = 10.1055/s-0031-1286282 | url = }}
5. ^{{cite journal | vauthors = Kasper S, Sacher J, Klein N, Mossaheb N, Attarbaschi-Steiner T, Lanzenberger R, Spindelegger C, Asenbaum S, Holik A, Dudczak R | title = Differences in the dynamics of serotonin reuptake transporter occupancy may explain superior clinical efficacy of escitalopram versus citalopram | journal = Int Clin Psychopharmacol | volume = 24 | issue = 3 | pages = 119–25 | year = 2009 | pmid = 19367152 | doi = 10.1097/YIC.0b013e32832a8ec8 | url = }}
6. ^{{cite journal | vauthors = Hellbom E | title = Chlorpheniramine, selective serotonin-reuptake inhibitors (SSRIs) and over-the-counter (OTC) treatment | journal = Med. Hypotheses | volume = 66 | issue = 4 | pages = 689–90 | year = 2006 | pmid = 16413139 | doi = 10.1016/j.mehy.2005.12.006 | url = }}
7. ^{{cite journal |author1=Werling LL |author2=Keller A |author3=Frank JG |author4=Nuwayhid SJ | title = A comparison of the binding profiles of dextromethorphan, memantine, fluoxetine and amitriptyline: treatment of involuntary emotional expression disorder | journal = Exp. Neurol. | volume = 207 | issue = 2 | pages = 248–57 | year = 2007 | pmid = 17689532 | doi = 10.1016/j.expneurol.2007.06.013 }}
8. ^{{cite journal | vauthors = Gillman PK | title = Monoamine oxidase inhibitors, opioid analgesics and serotonin toxicity | journal = Br J Anaesth | volume = 95 | issue = 4 | pages = 434–41 | year = 2005 | pmid = 16051647 | doi = 10.1093/bja/aei210 | url = http://bja.oxfordjournals.org/cgi/pmidlookup?view=long&pmid=16051647}}
9. ^{{cite journal |author1=Yeh SY |author2=Dersch C |author3=Rothman R |author4=Cadet JL | title = Effects of antihistamines on 3, 4-methylenedioxymethamphetamine-induced depletion of serotonin in rats| journal = Synapse | volume = 33 | issue = 3 | pages = 207–17 |date=September 1999 | pmid = 10420168 | doi = 10.1002/(SICI)1098-2396(19990901)33:3<207::AID-SYN5>3.0.CO;2-8 | url = }}
10. ^{{cite journal | vauthors = Li C, Shan L, Li X, Wei L, Li D | title = Mifepristone modulates serotonin transporter function | journal = Neural Regen Res | volume = 9 | issue = 6 | pages = 646–52 | year = 2014 | pmid = 25206868 | pmc = 4146234 | doi = 10.4103/1673-5374.130112 | url = http://www.nrronline.org/article.asp?issn=1673-5374;year=2014;volume=9;issue=6;spage=646;epage=652;aulast=Li}}
11. ^Pharmaceutical compositions containing mesembrine and related compounds. U.S. Patent 6,288,104 (PDF)
{{Antidepressants}}{{Anxiolytics}}{{OCD pharmacotherapies}}{{Monoamine reuptake inhibitors}}{{DEFAULTSORT:Serotonin Reuptake Inhibitor}}

2 : Serotonin reuptake inhibitors|Drugs acting on the nervous system

随便看

 

开放百科全书收录14589846条英语、德语、日语等多语种百科知识,基本涵盖了大多数领域的百科知识,是一部内容自由、开放的电子版国际百科全书。

 

Copyright © 2023 OENC.NET All Rights Reserved
京ICP备2021023879号 更新时间:2024/9/22 9:54:27