Fontem paginae Quetiapinum inspicere

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{| class="wikitable floatright"
|+ '''Quetiapinum'''
|-
| style="text-align: center" colspan="2" | [[Fasciculus:Quetiapine.svg|200px|Quetiapinum]]
|-
| style="text-align: center" colspan="2" | [[Fasciculus:Quetiapine-from-xtal-3D-balls.png|200px|Quetiapinum]]
|-
! colspan="2" | Natura chemica
|-
| style="font-size: 85%" | [[Formula chemica]] || style="font-size: 85%" | {{chem|C|21|H|25|N|3|O|2|S}}
|-
| style="font-size: 85%" | [[Massa molaris]] || style="font-size: 85%" | 383.5099 g/mol
|-
| style="font-size: 85%" | [[PubChem]] || style="font-size: 85%" | [https://pubchem.ncbi.nlm.nih.gov/compound/5002 5002]
|-
| style="font-size: 85%" | [[DrugBank]] || style="font-size: 85%" | [https://www.drugbank.ca/drugs/DB01224 DB01224]
|-
! colspan="2" | Natura pharmacologica
|-
| style="font-size: 85%" | Codex ATC || style="font-size: 85%" | {{ATC|N05AH|04}}
|-
| style="font-size: 85%" | [[Tempus semivitae biologicum]] || style="font-size: 85%" | 7 h <br />Norquetiapinum: 9-12 h
|-
| style="font-size: 85%" | [[Metabolismus]] || style="font-size: 85%" | [[iecur|iecore]] (hepaticus):<br />[[CYP3A4]]
|-
| style="font-size: 85%" | [[Metabolitus]] || style="font-size: 85%" | Norquetiapinum<br />(N-Desalcylquetiapinum)
|-
| style="font-size: 85%" | Excretio || style="font-size: 85%" | [[ren]]ibus (73%),<br />[[Faeces|faecibus]] (20%)
|-
! colspan="2" | Ad usum therapeuticum
|-
| style="font-size: 85%" | Applicatio || style="font-size: 85%" | per os
|-
| style="font-size: 85%" | MedlinePlus || style="font-size: 85%" | [https://medlineplus.gov/druginfo/meds/a698019.html a698019] {{Ling|Anglice}}
|}
'''Quetiapinum''' est substantia antipsychotica et propterea [[medicamentum]], quod cogitari potest, ad therapiam [[schizophrenia]]rum, interruptionum bipolarium<ref>Anglice: ''bipolar disorder''; hic formae fem. pluralis, quia haec diagnosis duas interruptiones saltim postulat</ref> sicut [[Depressio (psychiatria)|depressionum]] velut [[delirium|delirii]]<ref>{{cite journal |authors=Hawkins SB, Bucklin M, Muzyk AJ |title=Quetiapine for the treatment of delirium |journal=J Hosp Med |year=2013 |volume=8 |issue=4 |pages=215-20 |url=https://www.ncbi.nlm.nih.gov/pubmed/23468358}}.</ref>. Interdum [[insomnia]]e quoque adhibetur, quamquam usus illius non ubilibet approbatur<ref>{{cite journal |authors=Gugger JJ, Cassagnol M |title=Low-dose quetiapine is not a benign sedative-hypnotic agent |journal=Am J Addict |year=2008 |volume=17(5) |pages=454-5 |url=https://www.ncbi.nlm.nih.gov/pubmed/18770092}}</ref><ref>{{cite journal |authors=Tak LM, van Berlo-van de Laar IR, Doornbos B |title=Geen quetiapine bij slaapstoornissen |journal=Ned Tijdschr Geneeskd |year=2013 |volume=157 |pages=A5740 |url=https://www.ntvg.nl/artikelen/geen-quetiapine-bij-slaapstoornissen}} {{Ling|Batavice}}.</ref>. 

== Historia ==
Ab anno [[1970]] diversae substantiae antipsychoticae ''atypica'' quoque vocatae sunt, primo enim [[Clozapinum]]. Haec "atypica", cum [[Olanzapinum|Olanzapino]] (1971, demum in usu [[medicus|medici]] ab 1996), cum [[Receptorium dopamini D2|receptoria D<sub>2</sub>]] tum [[Receptorium 5-HT1A serotonini|receptoria serotonini 5-HT<sub>1A</sub>]] obsidentes, praeterea minius effectus adversaria ostendentes. Anno [[1985]] [[dibenzothiazepinum|dibenzothiazepino]] derivata Quetiapinum, simul Clozapino Olanzapinoque simile sed cum grege adiecto, divulgatum est.<ref>{{cite book |author=Raviña E |title=The Evolution of drug discovery, Wiley-VCH |year=2010}}.</ref>

== Synthesis ==
Synthesis Quetiapini ab uno dibenzothiazepinonorum orditur. Ad fabricandum [[dibenzothiazepinum]] primo [[lactamum]] cum phosphoryl chlorido tractatur. Deinde per substitutionem nucleophilicam molecula lateraliter additur. 
[[Fasciculus:Quetiapine syn.png|600px|center|Synthesis moleculi]]

== Natura Quetiapini ==

=== Natura chemica ===
Quetiapinum est thiazepinum. Nomen [[Unio internationalis chemiae purae applicatae|IUPAC]] suum est 2-(2-(4-dibenzo[b,f][1,4]thiazepine-11-yl-1-piperazinyl)ethoxy)ethanol, 
quod est thiazepinum (anulus chemicus cum [[Sulphur|sulphure]] et [[Nitrogenium|nitrogenio]] et quinque [[atomus|atomis]] [[Carbonium|carboniorum]]), cum duobus anulis aromatici ([[benzenum]]) et piperazino (anulus heterocyclus cum duobus [[atomus|atomis]] nitrogeniorum) et [[Ethanol|ethanolo]]. 

Quetiapinum est substantia [[Albus|alba]] et [[Crystallum|crystallina]], [[massa molaris]] sua 383.5099 g/mol. 

=== Natura pharmacologica ===
Quetiapinum est medicamentum cum virtutibus antipsychoticis et antidepressivis. 
[[Systema classificationis Anatomicum Therapeuticum Chemicumque|Codex ATC]] est {{ATC|N05AH|04}}.

=== Pharmacodynamica ===
{| class="wikitable floatright" style="font-size:small;"
|-
! [[Receptorium neurotransmissoris|Receptorium]] !! Quetiapini affinitas<br />ligandi, ''K''<sub>i</sub> (nM)<ref>https://web.archive.org/web/20131108013656/http://pdsp.med.unc.edu/pdsp.php</ref>!! Norquetiapini affinitas<br />ligandi, ''K''<sub>i</sub> (nM) !! Actio
|-
| [[Receptorium dopamini D1|dopamini D<sub>1</sub>]] || 712<ref name="JENSEN">{{cite journal |authors= Jensen NH, Rodriguiz RM, Caron MG, Wetsel WC, Rothman RB, Roth BL |title= N-Desalkylquetiapine, a Potent Norepinephrine Reuptake Inhibitor and Partial 5-HT<sub>1A</sub> Agonist, as a Putative Mediator of Quetiapine's Antidepressant Activity |journal= Neuropsychopharmacology |year=2008 |volume=33 |pages=2303-12 |url=http://www.nature.com/articles/1301646}}.</ref> - 994.5 || 99.8 (receptorium [[Rattus|ratti]]) || antagonista
|-
|  [[Receptorium dopamini D2|D<sub>2</sub>]] || 245<ref name="JENSEN" /> - 379 || 196 || antagonista
|-
|  [[Receptorium dopamini D2|D<sub>2L</sub>]] || 712<ref name="JENSEN" /> || || antagonista
|-
|  [[Receptorium dopamini D2|D<sub>2S</sub>]] || 390<ref name="JENSEN" /> || || antagonista
|-
|  [[Receptorium dopamini D3|D<sub>3</sub>]] || 340 || - || antagonista
|-
| [[Receptorium dopamini D4|D<sub>4</sub>]] || 1,202<ref name="JENSEN" /> - 2,019 || 1297 || antagonista
|-
|  [[Receptorium serotonini 1A|5-HT<sub>1A</sub>]] || 394.2 || 45 || antagonista partialis
|-
|  [[Receptorium serotonini 2A|5-HT<sub>2A</sub>]] || 118 || 48 || antagonista
|-
|  [[Receptorium serotonini 2C|5-HT<sub>2C</sub>]] || 1,843 || 107 || antagonista
|-
|  [[Receptorium serotonini 4|5-HT<sub>4</sub>]] || nondum determinata|| nondum determinata || antagonista
|-
|  [[Receptorium serotonini 6|5-HT<sub>6</sub>]] || 33 / 1,864 || - || antagonista
|-
|  [[Receptorium serotonini 7|5-HT<sub>7</sub>]] || 307 || 76 || antagonista
|-
| [[Receptorium adrenergicum alpha-1|α<sub>1A</sub>]] || 22 || 144 || antagonista
|-
|  [[Receptorium adrenergicum alpha-1|α<sub>1B</sub>]] || 14.6 || 46.4 (receptorium [[Rattus|ratti]]) || antagonista
|-
|  [[Receptorium adrenergicum alpha-2A|α<sub>2A</sub>]] || 3,630 || 237 || antagonista
|-
|  [[Receptorium adrenergicum alpha-2C|α<sub>2C</sub>]] || 28.85 || - || antagonista
|-
|  [[Receptorium adrenergicum beta-1|ß<sub>1</sub>]] || > 10,000 || > 10,000 || nondum inquisita
|-
|  [[Receptorium adrenergicum beta-2|ß<sub>2</sub>]] || > 10,000 || > 10,000 || nondum inquisita
|-
|  [[receptorium histamini H1|H<sub>1</sub>]] || 6.9 || 3.5 || antagonista
|-
|  [[receptorium histamini H2|H<sub>2</sub>]] || 41.24 || - || antagonista
|-
| H<sub>3</sub> || >10,000 || >10,000 || nondum inquisita
|-
| H<sub>4</sub> || >10,000 || >1,660 || nondum inquisita
|-
|  [[Receptorium muscarinicum M1 acetylcholini|M<sub>1</sub>]] || 489 - 858 || 38.3 (receptorium [[Rattus|ratti]]) || antagonista
|-
|  [[Receptorium muscarinicum M2 acetylcholini|M<sub>2</sub>]] || 1,339 - 1,631.5 || 453 || nondum inquisita
|-
|  [[Receptorium muscarinicum M3 acetylcholini|M<sub>3</sub>]] || 1,631.5 - >10,000 || 23 || antagonista
|-
|  [[Receptorium muscarinicum M4 acetylcholini|M<sub>4</sub>]] || 542 || 110 || nondum inquisita
|-
|  [[Receptorium muscarinicum M5 acetylcholini|M<sub>5</sub>]] || 1,942 || 23 || antagonista
|-
|  [[Transportator Serotonini|SERT]] || >10000<ref name="JENSEN" /> || 927 || situm obsidens
|-
|  [[Transportator noradrenalini|NET]] || >10000<ref name="JENSEN" /> || 12 || situm obsidens
|}
Mementote et Quetiapinum et metabolitum suum Norquetiapinum effectus pharmacologicos exercere. Quetiapinum potissime [[receptorium histamini H1|receptoria H<sub>1</sub>]], praeterea [[metabolitus]] activus Norquetiapinum (quod est N-Desalcylquetiapinum) receptoria D<sub>2</sub> et [[Transportator Noradrenalini|noradrenalini transportatorem]] (breve: ''NET'', inhibitio noradrenalini<ref>noradrenalinum = norepinephrinum</ref> reabsorptionis) et receptoria 5-HT<sub>2A</sub> serotonini et 5-HT<sub>2c</sub> serotonini obsidet.
==== Receptorium histamini 1 ====
Antagonista [[receptorium histamini|receptoriorum H<sub>1</sub>]] (H1R) ut Quetiapinum lassitudinem, famis incrementum efficit<ref>{{cite journal |authors=Sato H, Ito C, Hiraoka K, Tashiro M, Shibuya K, H1 Funaki Y, Yoshikawa T, Iwata R, Matsuoka H, Yanai K |title=Histamine H1 receptor occupancy by the new-generation antipsychotics olanzapine and quetiapine: a positron emission tomography study in healthy volunteers |journal=Psychopharmacology (Berl) |year=2015 |volume=232 |issue=19 |pages=3497-505 |url=https://www.ncbi.nlm.nih.gov/pubmed/26146015}}.</ref>.

=== Pharmacocinetica ===
[[Tempus semivitae biologicum]] <math>t_{\frac{1}{2}}</math>.<ref>http://goldbook.iupac.org/B00658.html</ref> circa 7 h (norquetiapinum 9-12 h) est. 
Excretio est per urinas (73%) et biles (20%). 

== Effectus Quetiapini ==
Cum uso Quetiapini animum advertere ad [[Effectus adversus|effectus secundarios]] et interactiones necesse est. 
=== Effectus secundarii ===
Exempla sunt: 

'''[[Adversa drogae reactio#Crebritas|Saepissmime]]''' (>10%) 
{{div col|1}}
* [[Xerostomia|Siccitas oris]] (xerostomia)
* [[Vertigo (symptoma)|Vertigo]], dysequilibrium, (prae-)syncope
* [[Cephalalgia|Capitis dolor]] (cephalalgia)
* [[Somnolentia (symptoma)|Somnolentia]]
{{div col end}}

'''[[Adversa drogae reactio#Crebritas|Saepe]]''' (1%-10%) 
{{div col|3}}
* [[Hypertensio|Pressio sanguinis nimia]]
* [[Hypotensio orthostatica]]
* [[Tachycardia|Pulsus celer]]
* [[Hypercholesterolaemia|Cholesteroli copiae nimiae]] in sanguine
* [[Hypertriglycerinaemia|Triglyceridorum copiae nimiae]] in sanguine
* [[Dolor abdominalis (symptoma)|Dolor abdominalis]]
* Dysphagia
* [[Fatigatio (symptoma)|Fatigatio]]
* [[Insomnia]]
{{div col end}}

'''Alia''' (<1%)
{{div col|3}}
* Symptomata extrapyramidalia
* [[Hyponatraemia]]
* [[Intervallum QT]] prolongatum<ref>{{cite journal |authors=Hasnain M, Vieweg WV, Howland RH, Kogut C, Breden Crouse EL, Koneru JN, Hancox JC, Digby GC, Baranchuk A, Deshmukh A, Pandurangi AK |title=Quetiapine, QTc interval prolongation, and torsade de pointes: a review of case reports |journal=Ther Adv Psychopharmacol |volume=4(3) |year=2014 |pages=130-8 |url=https://www.ncbi.nlm.nih.gov/pubmed/25057346?dopt=Abstract}}.</ref>
* [[Incrementum ponderis|Ponderis incrementum]]
{{div col end}}

=== Interactiones ===
Cum Quetiapinum subtratum enzymi [[CYP3A4]] esset, inhibitores CYP3A4 effectus Quetiapini augere possint, inductores invicem diminuere, per exemplum:
{| class="wikitable"
|-
| colspan=3| <center>Pharmaca cum effectibus Quetiapini substrati</center>
|-
| Inhibitores cum '''Quetiapini''' effectibus '''fortioribus''' || Inductores cum '''Quetiapini''' effectibus '''minoribus'''
|- style="vertical-align: top;"
| 
{{CYP3A4 Inhibitores}}
|
{{CYP3A4 Inductores}}
|}

== Notae ==
<references/>

[[Categoria:Antipsychotica]]
[[Categoria:Intervallum QT prolongatum]]