Doksilamin: Perbedaan antara revisi
Konten dihapus Konten ditambahkan
Tidak ada ringkasan suntingan Tag: halaman dengan galat kutipan Suntingan perangkat seluler Suntingan peramban seluler Suntingan seluler lanjutan pranala ke halaman disambiguasi |
Tidak ada ringkasan suntingan Tag: halaman dengan galat kutipan Suntingan perangkat seluler Suntingan peramban seluler Suntingan seluler lanjutan |
||
Baris 92:
==Farmakologi==
===Farmakodinamik===
{| class="wikitable floatright" style="font-size:small;"
|+ Doxylamine<ref name=PDSP>{{cite web |title= PDSP K<sub>i</sub> Database |work= Psychoactive Drug Screening Program (PDSP)|author1-link=Bryan Roth | vauthors = Roth BL, Driscol J |publisher= University of North Carolina at Chapel Hill and the United States National Institute of Mental Health |access-date= 14 August 2017 |url= https://pdsp.unc.edu/databases/pdsp.php?knowID=0&kiKey=&receptorDD=&receptor=&speciesDD=&species=&sourcesDD=&source=&hotLigandDD=&hotLigand=&testLigandDD=&testFreeRadio=testFreeRadio&testLigand=doxylamine&referenceDD=&reference=&KiGreater=&KiLess=&kiAllRadio=all&doQuery=Submit+Query}}</ref>
|-
! Site !! K<sub>i</sub> (nM) !! Species !! Ref
|-
| {{abbrlink|SERT|Serotonin transporter}} || >10,000 || Human || <ref name=pmid23357028>{{cite journal | vauthors = Krystal AD, Richelson E, Roth T | title = Review of the histamine system and the clinical effects of H1 antagonists: basis for a new model for understanding the effects of insomnia medications | journal = Sleep Medicine Reviews | volume = 17 | issue = 4 | pages = 263–272 | date = August 2013 | pmid = 23357028 | doi = 10.1016/j.smrv.2012.08.001 }}</ref>
|-
| {{abbrlink|NET|Norepinephrine transporter}} || >10,000 || Human || <ref name=pmid23357028/>
|-
| {{abbrlink|DAT|Dopamine transporter}} || >10,000 || Human || <ref name=pmid23357028/>
|-
| [[5-HT2A receptor|5-HT<sub>2A</sub>]] || >10,000 || Human || <ref name=pmid23357028/>
|-
| [[5-HT2C receptor|5-HT<sub>2C</sub>]] || >10,000 || Human || <ref name=pmid23357028/>
|-
| [[Alpha-1B adrenergic receptor|α<sub>1B</sub>]] || >10,000 || Human || <ref name=pmid23357028/>
|-
| [[Alpha-2A adrenergic receptor|α<sub>2A</sub>]] || >10,000 || Human || <ref name=pmid23357028/>
|-
| [[Alpha-2B adrenergic receptor|α<sub>2B</sub>]] || >10,000 || Human || <ref name=pmid23357028/>
|-
| [[Alpha-2C adrenergic receptor|α<sub>2C</sub>]] || >10,000 || Human || <ref name=pmid23357028/>
|-
| [[Histamine H1 receptor|H<sub>1</sub>]] || 42 || Human || <ref name=pmid23357028/>
|-
| [[Histamine H2 receptor|H<sub>2</sub>]] || {{abbr|ND|No data}} || {{abbr|ND|No data}} || {{abbr|ND|No data}}
|-
| [[Histamine H3 receptor|H<sub>3</sub>]] || >10,000 || Human || <ref name=pmid23357028/>
|-
| [[Histamine H4 receptor|H<sub>4</sub>]] || {{abbr|ND|No data}} || {{abbr|ND|No data}} || {{abbr|ND|No data}}
|-
| [[Muscarinic acetylcholine receptor M1|M<sub>1</sub>]] || 490 || Human || <ref name=pmid23357028/>
|-
| [[Muscarinic acetylcholine receptor M2|M<sub>2</sub>]] || 2,100 || Human || <ref name=pmid23357028/>
|-
| [[Muscarinic acetylcholine receptor M3|M<sub>3</sub>]] || 650 || Human || <ref name=pmid23357028/>
|-
| [[Muscarinic acetylcholine receptor M4|M<sub>4</sub>]] || 380 || Human || <ref name=pmid23357028/>
|-
| [[Muscarinic acetylcholine receptor M5|M<sub>5</sub>]] || 180 || Human || <ref name=pmid23357028/>
|- class="sortbottom"
| colspan="4" style="width: 1px;" |Values are K<sub>i</sub> (nM), unless otherwise noted. The smaller the value, the more strongly the drug binds to the site.
|}
Doxylamine bertindak terutama sebagai antagonis atau agonis kebalikan dari reseptor histamin H1. Tindakan ini bertanggung jawab atas sifat antihistamin dan obat penenangnya. Pada tingkat lebih rendah, doxylamine bertindak sebagai antagonis reseptor asetilkolin muskarinik, suatu tindakan yang bertanggung jawab atas efek antikolinergik dan (pada dosis tinggi) mengigau.<ref name="pmid23229983">{{cite journal | vauthors = Vande Griend JP, Anderson SL | title = Histamine-1 receptor antagonism for treatment of insomnia | journal = Journal of the American Pharmacists Association | volume = 52 | issue = 6 | pages = e210–e219 | year = 2012 | pmid = 23229983 | doi = 10.1331/JAPhA.2012.12051 }}</ref><ref name="pmid23357028" />
===Farmakokinetik===
[[File:Doxylamine levels after a single 25 mg oral dose of doxylamine.png|thumb|left|450px|Konsentrasi doxylamine setelah dosis tunggal doksilamin oral 25 mg pada sukarelawan sehat. Sumbu X mewakili waktu dalam jam setelah dosis awal.<ref name="pmid29671128">{{cite journal | vauthors = Allison M, Hale C | title = A Phase I Study of the Pharmacokinetics and Pharmacodynamics of Intranasal Doxylamine in Subjects with Chronic Intermittent Sleep Impairment | journal = Drugs in R&D | volume = 18 | issue = 2 | pages = 129–136 | date = June 2018 | pmid = 29671128 | pmc = 5995792 | doi = 10.1007/s40268-018-0232-1 }}</ref>]]
==Kimia==
Doksilamin adalah anggota antihistamin kelas [[etanolamina]] yang juga terdiri dari bromodifenhidramin, karbinoksamin, klemastin, [[dimenhidrinat]], [[difenhidramin]], orfenadrin, dan feniltoloksamin.<ref name="SimonsSimons2011">{{cite journal | vauthors = Simons FE, Simons KJ | title = Histamine and H1-antihistamines: celebrating a century of progress | journal = The Journal of Allergy and Clinical Immunology | volume = 128 | issue = 6 | pages = 1139–1150.e4 | date = December 2011 | pmid = 22035879 | doi = 10.1016/j.jaci.2011.09.005 | doi-access = free }}</ref><ref name="pmid23173575">{{cite journal | vauthors = Kalpaklioglu F, Baccioglu A | title = Efficacy and safety of H1-antihistamines: an update | journal = Anti-Inflammatory & Anti-Allergy Agents in Medicinal Chemistry | volume = 11 | issue = 3 | pages = 230–237 | date = 2012 | pmid = 23173575 | doi = 10.2174/1871523011202030230 }}</ref>
| |||