Kvetijapin — разлика између измена

Kvetijapin
IUPAC ime
	2-(2-(4-dibenzo[b,f][1,4]tiazepin- 11-il- 1-piperazinil)etoksi)etanol
Klinički podaci
Prodajno ime	Serokvel
Drugs.com	Monografija
MedlinePlus	a698019
Kategorija trudnoće	US: C (Mogući rizik) ; ;
Način primene	Oralnot
Pravni status
Pravni status	US: ℞-only ;
Farmakokinetički podaci
Bioraspoloživost	9%
Metabolizam	Hepatički
Poluvreme eliminacije	6 sata
Izlučivanje	Renalno
Identifikatori
CAS broj	111974-69-7
ATC kod	N05AH04 (WHO)
PubChem	CID 5002
IUPHAR/BPS	50
DrugBank	DB01224
ChemSpider	4827
UNII	BGL0JSY5SI
KEGG	D08456
ChEBI	CHEBI:8707
ChEMBL	CHEMBL716
Hemijski podaci
Formula	C21H25N3O2S
Molarna masa	383,5099 g/mol
	SMILES N\1=C(\c3c(Sc2c/1cccc2)cccc3)N4CCN(CCOCCO)CC4; ;
	InChI InChI=1S/C21H25N3O2S/c25-14-16-26-15-13-23-9-11-24(12-10-23)21-17-5-1-3-7-19(17)27-20-8-4-2-6-18(20)22-21/h1-8,25H,9-16H2 ; Key:URKOMYMAXPYINW-UHFFFAOYSA-N ;

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ВизуелноВикитекст

Инлајн

Тренутна верзија на датум 7. март 2024. у 23:20

Kvetijapin (Serokvel, Ketipinor) je atipični antipsihotik koji je odorobren za lečenje šizofrenije, bipolarnog poremećaja i kao dodatni tretman za depresiju.

Godišnja prodaja ovog leka je vredna oko USD $5,7 milijardi globalno, od čega je $2,9 milijardi u SAD-u.^[1] Američki patent,^[2] je trebalo da istekne 2011, ali je njegov vek produžen radi pedijatrijske ekskluzivnosti do marta 2012.^[3]^[4]^[5]

Farmakologija

Poređenje afiniteta (Ki, nM)^[6]
Receptor	Kvetijapin	Norkvetijapin
D₁	428	99.8
D₂	626	489
5-HT_1A	1040	191
5-HT_2A	38	2.9
α_1B	14.6	46.4
α₂	617	1290
H₁	4.41	1.15
M₁	1086	38.3
NET	>10000	34.8

Kvetijapin poseduje sledeća farmakološka dejstva:^[7]^[8]^[9]^[10]

D₁ (IC₅₀ = 1268nM), D₂ (IC₅₀ = 329nM), D₃, i D₄ receptor antagonist
5-HT_1A (IC₅₀ = 717nM), 5-HT_2A (IC₅₀ = 148nM), 5-HT_2C, and 5-HT₇ receptor antagonist
α₁-adrenergički (IC₅₀ = 94nM) i α₂-adrenergički receptor (IC₅₀ = 271nM) antagonist
H₁ receptor (IC₅₀ = 30nM) antagonist
mACh receptor (IC₅₀ = >5000nM) antagonist

Sinteza

Jedan od mogućih sintetičkih puteva je:^[11]

Reference

^ Details for Seroquel
^ Patent Document, U.S. Patent and Trademark Office Архивирано на сајту Wayback Machine (6. јануар 2017)
^ Blockbuster Drugs That Will Go Generic Soon
^ Seroquel patent expiration
^ „Quepin Full Prescribing Information in Drug Reference Encyclopedia”. Приступљено 3. 4. 2010.
^ AstraZeneca Pharmaceuticals LP (2011). „SEROQUEL (quetiapine fumarate) tablet, extended release”. DailyMed. National Library of Medicine. Section 12.2: Pharmacodynamics. Приступљено 26. 4. 2011.
^ AstraZeneca. „Seroquel (quietapine fumarate) tablets” (PDF). 276521. Архивирано из оригинала (PDF) 14. 04. 2008. г. Приступљено 23. 03. 2012.
^ Richelson E, Souder T (2000). „Binding of antipsychotic drugs to human brain receptors focus on newer generation compounds”. Life Sciences. 68 (1): 29—39. PMID 11132243. doi:10.1016/S0024-3205(00)00911-5.
^ Davis, Kenneth L; Neuropsychopharmacology, American College of (2002). Neuropsychopharmacology: the fifth ... - Google Books. ISBN 9780781728379.
^ Seroquel Official FDA information, side effects and uses
^ Warawa, E. J.; Migler, B. M.; 1988, U.S. Patent 4.879.288.

Literatura

Davis, Kenneth L; Neuropsychopharmacology, American College of (2002). Neuropsychopharmacology: the fifth ... - Google Books. ISBN 9780781728379.

Spoljašnje veze

„Quetiapine”. MedlinePlus. The American Society of Health-System Pharmacists, Inc. 1. 9. 2008.
NAMI pregled

Molimo Vas, obratite pažnju na važno upozorenje
u vezi sa temama iz oblasti medicine (zdravlja).

[1] Details for Seroquel

[2] Patent Document, U.S. Patent and Trademark Office Архивирано на сајту Wayback Machine (6. јануар 2017)

[3] Blockbuster Drugs That Will Go Generic Soon

[4] Seroquel patent expiration

[5] „Quepin Full Prescribing Information in Drug Reference Encyclopedia”. Приступљено 3. 4. 2010.

[dailymed_PI-6] AstraZeneca Pharmaceuticals LP (2011). „SEROQUEL (quetiapine fumarate) tablet, extended release”. DailyMed. National Library of Medicine. Section 12.2: Pharmacodynamics. Приступљено 26. 4. 2011.

[Seroquel-7] AstraZeneca. „Seroquel (quietapine fumarate) tablets” (PDF). 276521. Архивирано из оригинала (PDF) 14. 04. 2008. г. Приступљено 23. 03. 2012.

[pmid11132243-8] Richelson E, Souder T (2000). „Binding of antipsychotic drugs to human brain receptors focus on newer generation compounds”. Life Sciences. 68 (1): 29—39. PMID 11132243. doi:10.1016/S0024-3205(00)00911-5.

[urlNeuropsychopharmacology:_the_fifth_..._-_Google_Books-9] Davis, Kenneth L; Neuropsychopharmacology, American College of (2002). Neuropsychopharmacology: the fifth ... - Google Books. ISBN 9780781728379.

[10] Seroquel Official FDA information, side effects and uses

[11] Warawa, E. J.; Migler, B. M.; 1988, U.S. Patent 4.879.288.

[1]

[2]

[3]

[4]

[5]

[6]

[7]

[8]

[9]

[10]

[11]

@@ Ред 22: / Ред 22: @@
 <!--Identifiers-->
-| CASNo_Ref = {{cascite|correct|CAS}}
 | CAS_number_Ref = {{cascite|correct|}}
 | CAS_number = 111974-69-7
@@ Ред 46: / Ред 45: @@
 | molecular_weight = 383,5099 -{g/mol}-
 | smiles = N\1=C(\c3c(Sc2c/1cccc2)cccc3)N4CCN(CCOCCO)CC4
-| InChI = 1/C21H25N3O2S/c25-14-16-26-15-13-23-9-11-24(12-10-23)21-17-5-1-3-7-19(17)27-20-8-4-2-6-18(20)22-21/h1-8,25H,9-16H2
 | StdInChI_Ref = {{stdinchicite|correct|chemspider}}
 | StdInChI = 1S/C21H25N3O2S/c25-14-16-26-15-13-23-9-11-24(12-10-23)21-17-5-1-3-7-19(17)27-20-8-4-2-6-18(20)22-21/h1-8,25H,9-16H2
@@ Ред 52: / Ред 50: @@
 | StdInChIKey = URKOMYMAXPYINW-UHFFFAOYSA-N
 }}
-'''Kvetiapin''' (''Serokvel'', ''Ketipinor'') je [[atipični antipsihotik]] koji je odorobren za lečenje [[šizofrenija|šizofrenije]], [[Манично-депресивна психоза|bipolarnog poremećaja]] i kao dodatni tretman za [[Klinička depresija|depresiju]].
+'''Kvetijapin''' (''Serokvel'', ''Ketipinor'') je [[atipični antipsihotik]] koji je odorobren za lečenje [[šizofrenija|šizofrenije]], [[Манично-депресивна психоза|bipolarnog poremećaja]] i kao dodatni tretman za [[Klinička depresija|depresiju]].
-Godišnja prodaja ovog leka je vredna oko -{USD}- $5,7 milijardi globalno, do čega je $2.9 milijardi u SAD-u.<ref>-{[http://drugpatentwatch.com/ultimate/preview/tradename/index.php?query=SEROQUEL Details for Seroquel]}-</ref> Američki patent,<ref>-{[http://patft.uspto.gov/netacgi/nph-Parser?Sect1=PTO2&Sect2=HITOFF&p=1&u=%2Fnetahtml%2FPTO%2Fsearch-bool.html&r=1&f=G&l=50&co1=AND&d=PTXT&s1=4,879,288.PN.&OS=PN/4,879,288&RS=PN/4,879,288 Patent Document, U.S. Patent and Trademark Office]}-</ref> je trebalo da istekne [[2011]], ali je njegov vek produžen radi pedijatrijske ekskluzivnosti do marta [[2012]].<ref>[http://money.usnews.com/money/blogs/the-best-life/2011/04/29/blockbuster-drugs-that-will-go-generic-soon -{Blockbuster Drugs That Will Go Generic Soon}-]</ref><ref>-{[http://drugpatentwatch.com/ultimate/preview/patent/index.php?query=4879288 Seroquel patent expiration]}-</ref><ref>{{cite web |url=http://www.theodora.com/drugs/quepin_tablets_specifar.html |title=Quepin Full Prescribing Information in Drug Reference Encyclopedia |work= |accessdate=2010-04-03}}</ref>
+Godišnja prodaja ovog leka je vredna oko -{USD}- $5,7 milijardi globalno, od čega je $2,9 milijardi u SAD-u.<ref>-{[http://drugpatentwatch.com/ultimate/preview/tradename/index.php?query=SEROQUEL Details for Seroquel]}-</ref> Američki patent,<ref>-{[http://patft.uspto.gov/netacgi/nph-Parser?Sect1=PTO2&Sect2=HITOFF&p=1&u=%2Fnetahtml%2FPTO%2Fsearch-bool.html&r=1&f=G&l=50&co1=AND&d=PTXT&s1=4,879,288.PN.&OS=PN/4,879,288&RS=PN/4,879,288 Patent Document, U.S. Patent and Trademark Office] {{Wayback|url=http://patft.uspto.gov/netacgi/nph-Parser?Sect1=PTO2&Sect2=HITOFF&p=1&u=%2Fnetahtml%2FPTO%2Fsearch-bool.html&r=1&f=G&l=50&co1=AND&d=PTXT&s1=4,879,288.PN.&OS=PN/4,879,288&RS=PN/4,879,288 |date=20170106145854 }}}-</ref> je trebalo da istekne [[2011]], ali je njegov vek produžen radi pedijatrijske ekskluzivnosti do marta [[2012]].<ref>[http://money.usnews.com/money/blogs/the-best-life/2011/04/29/blockbuster-drugs-that-will-go-generic-soon -{Blockbuster Drugs That Will Go Generic Soon}-]</ref><ref>-{[http://drugpatentwatch.com/ultimate/preview/patent/index.php?query=4879288 Seroquel patent expiration]}-</ref><ref>{{cite web |url=http://www.theodora.com/drugs/quepin_tablets_specifar.html |title=Quepin Full Prescribing Information in Drug Reference Encyclopedia |work= |accessdate = 3. 4. 2010.}}</ref>
-==Farmakologija==
+== Farmakologija ==
 {| class="wikitable" align="right"
-|+ Poređenje afiniteta (-{Ki, nM}-)<ref name="dailymed PI">{{cite web |url=http://dailymed.nlm.nih.gov/dailymed/drugInfo.cfm?id=41375#section-15.2 |title=SEROQUEL (quetiapine fumarate) tablet, extended release |author=AstraZeneca Pharmaceuticals LP |year=2011 |month=March |work=DailyMed |publisher=National Library of Medicine |at=Section 12.2: Pharmacodynamics |accessdate=2011-04-26}}</ref>
+|+ Poređenje afiniteta (-{Ki, nM}-)<ref name="dailymed PI">{{cite web |url=http://dailymed.nlm.nih.gov/dailymed/drugInfo.cfm?id=41375#section-15.2 |title=SEROQUEL (quetiapine fumarate) tablet, extended release |author=AstraZeneca Pharmaceuticals LP |year=2011 |work=DailyMed |publisher=National Library of Medicine |at=Section 12.2: Pharmacodynamics |accessdate = 26. 4. 2011.}}</ref>
 ! scope="col" | Receptor
-! scope="col" | Kvetiapin
+! scope="col" | Kvetijapin
-! scope="col" | Norkvetiapin
+! scope="col" | Norkvetijapin
 |-
 | D<sub>1</sub> || 428 || 99.8
@@ Ред 69: / Ред 67: @@
 | 5-HT<sub>1A</sub> || 1040 || 191
 |-
-| <b>[[5-HT2A receptor|-{5-HT<sub>2A</sub>}-]]</b> || 38 || 2.9
+| '''[[5-HT2A receptor|-{5-HT<sub>2A</sub>}-]]''' || 38 || 2.9
 |-
 | [[Alfa-1B adrenergički receptor|&alpha;<sub>1B</sub>]] || 14.6 || 46.4
@@ Ред 81: / Ред 79: @@
 | [[Norepinefrinski transporter|NET]] || >10000 || 34.8
 |}
-Kvetiapin poseduje sledeća farmakološka dejstva:<ref name = Seroquel>{{Cite journal|author=AstraZeneca|id=276521 |title=Seroquel (quietapine fumarate) tablets |url=http://www1.astrazeneca-us.com/pi/Seroquel.pdf |format=[[Portable Document Format|PDF]]}}</ref><ref name="pmid11132243">{{cite journal | author = Richelson E, Souder T | title = Binding of antipsychotic drugs to human brain receptors focus on newer generation compounds | journal = Life Sciences | volume = 68 | issue = 1 | pages = 29–39 | year = 2000 | month = November | pmid = 11132243 | doi = 10.1016/S0024-3205(00)00911-5| url = http://linkinghub.elsevier.com/retrieve/pii/S0024320500009115}}</ref><ref name="urlNeuropsychopharmacology: the fifth ... - Google Books">{{cite book | url = http://books.google.com/?id=BKwkonZwZD0C&pg=PA778#v=onepage&q= | title = Neuropsychopharmacology: the fifth ... - Google Books | format = | work = | accessdate = | isbn = 9780781728379 | author1 = Davis, Kenneth L | author2 = Neuropsychopharmacology, American College of | year = 2002 }}</ref><ref>http://www.drugs.com/pro/seroquel.html</ref>
+Kvetijapin poseduje sledeća farmakološka dejstva:<ref name="Seroquel">{{Cite journal |author=AstraZeneca |id=276521 |title=Seroquel (quietapine fumarate) tablets |url=http://www1.astrazeneca-us.com/pi/Seroquel.pdf |format=[[Portable Document Format|PDF]] |journal= |access-date=23. 03. 2012 |archive-url=https://web.archive.org/web/20080414031803/http://www1.astrazeneca-us.com/pi/Seroquel.pdf |archive-date=14. 04. 2008 |url-status=dead |df= }}</ref><ref name="pmid11132243">{{cite journal | author = Richelson E, Souder T | title = Binding of antipsychotic drugs to human brain receptors focus on newer generation compounds | journal = Life Sciences | volume = 68 | issue = 1 | pages = 29–39 | year = 2000 | pmid = 11132243 | doi = 10.1016/S0024-3205(00)00911-5| url = http://linkinghub.elsevier.com/retrieve/pii/S0024320500009115}}</ref><ref name="urlNeuropsychopharmacology: the fifth ... - Google Books">{{Cite book | url = http://books.google.com/?id=BKwkonZwZD0C&pg=PA778#v=onepage&q= | title = Neuropsychopharmacology: the fifth ... - Google Books | format = | work = | accessdate = |isbn=9780781728379 | author1 = Davis, Kenneth L | author2 = Neuropsychopharmacology, American College of | year = 2002 }}</ref><ref>[http://www.drugs.com/pro/seroquel.html Seroquel Official FDA information, side effects and uses{{Ботовски наслов}}]</ref>
 * [[Dopaminski receptor D1|D<sub>1</sub>]] (-{IC<sub>50</sub> = 1268nM}-), [[Dopaminski receptor D2|D<sub>2</sub>]] (-{IC<sub>50</sub> = 329nM}-), [[Dopaminski receptor D3|D<sub>3</sub>]], i [[Dopaminski receptor D4|D<sub>4</sub> receptor]] [[Antagonist dopaminskog receptora|antagonist]]
 * [[5-HT1A receptor|5-HT<sub>1A</sub>]] (-{IC<sub>50</sub> = 717nM}-), [[5-HT2A receptor|5-HT<sub>2A</sub>]] (-{IC<sub>50</sub> = 148nM}-), [[5-HT2C receptor|5-HT<sub>2C</sub>]], and [[5-HT7 receptor|5-HT<sub>7</sub> receptor]] [[Serotoninski antagonist|antagonist]]
 * [[Alfa-1 adrenergički receptor|α<sub>1</sub>-adrenergički]] (-{IC<sub>50</sub> = 94nM}-) i [[Alfa-2 adrenergički receptor|α<sub>2</sub>-adrenergički receptor]] (-{IC<sub>50</sub> = 271nM}-) [[alfa bloker|antagonist]]
-* [[Histaminski receptor H1|-{H}-<sub>1</sub> receptor]] (-{IC<sub>50</sub> = 30nM}-) [[Антихистаминик|antagonist]]
+* [[Histaminski H1 receptor|-{H}-<sub>1</sub> receptor]] (-{IC<sub>50</sub> = 30nM}-) [[Антихистаминик|antagonist]]
 * [[Muskarinski acetilholinski receptor|-{mACh}- receptor]] (-{IC<sub>50</sub> = >5000nM}-) [[Muskarinski antagonist|antagonist]]
+== Sinteza ==
+Jedan od mogućih sintetičkih puteva je:<ref>-{Warawa, E. J.; Migler, B. M.; 1988, {{US Patent|4879288}}.}-</ref>
+[[Датотека:Quetiapine syn.png|600px]]
 == Reference ==
-{{reflist|2}}
+{{reflist}}
+== Literatura ==
+* {{Cite book |ref= harv|url = http://books.google.com/?id=BKwkonZwZD0C&pg=PA778#v=onepage&q= | title = Neuropsychopharmacology: the fifth ... - Google Books | format = | work = | accessdate = |isbn=9780781728379 | author1 = Davis, Kenneth L | author2 = Neuropsychopharmacology, American College of | year = 2002 }}
+== Spoljašnje veze ==
+* {{cite web|publisher=The American Society of Health-System Pharmacists, Inc.|work=[[MedlinePlus]]|title=Quetiapine|date = 1. 9. 2008.|url=http://nlm.nih.gov/medlineplus/druginfo/meds/a698019.html}}
+* [https://web.archive.org/web/20030925213951/http://www.nami.org/Template.cfm?Section=About_Medications&template=%2FContentManagement%2FContentDisplay.cfm&ContentID=8190 NAMI pregled]
+{{-}}
+{{Antipsihotici-lat}}
+{{Adrenergici-lat}}
+{{Holinergici-lat}}
+{{Dopaminergici-lat}}
+{{Serotonergici-lat}}
+{{Medicinsko upozorenje-lat}}
+{{Podnožje|lat=da|Medicina|Hemija}}
+[[Категорија:Атипични антипсихотици]]
+[[Категорија:Допамински антагонисти]]
+[[Категорија:Серотонински антагонисти]]
+[[Категорија:Хипнотици]]
+[[Категорија:Седативи]]
+[[Категорија:Пиперазини]]
+[[Категорија:Дибензотиазепини]]
+[[Категорија:Етри]]
+[[Категорија:Алкохоли]]

p r u Antipsihotici (neuroleptici) (N05A)
Tipični	Benzamidi: Levosulpirid · Nemonaprid · Sulpirid · Sultoprid · Tiaprid · Veraliprid Butirofenoni: Azaperon · Benperidol · Bromperidol · Droperidol · Fluanizon · Haloperidol # · Lenperon · Moperon · Pipamperon · Spiperon · Timiperon · Trifluperidol Difenilbutilpiperidini: Klopimozid · Fluspirilen · Penfluridol · Pimozid Fenotiazini: Acepromazin · Acetofenazin · Butaperazin · Karfenazin · Hloracizin · Hlorproetazin · Hlorpromazin · Cijamemazin · Diksirazin · Fluacizin · Flufenazin · Levomepromazin/Metotrimeprazin · Mezoridazin · Perazin · Pericijazin · Perfenazin · Piperacetazin · Pipotiazin · Prohlorperazin · Promazin · Prometazin · Propiomazin · Sulforidazin · Tietilperazin · Tiopropazat · Tioproperazin · Tioridazin · Trifluoperazin · Triflupromazin Tioksanten: Hlorprotiksen · Klopentiksol · Flupentiksol · Tiotiksen · Zuklopentiksol Triciklici: Butaklamol · Fluotracen · Loksapin · Trimipramin Drugi: Protipendil
Atipični	Benzamidi: Amisulprid · Remoksiprid‡ Butirofenoni: Cinuperon · Melperon · Setoperon Benzo(izo)oksazol piperidini: Iloperidon · Okaperidon · Paliperidon · Rispolept # Benzo(izo)tiazol piperazini: Lurasidon · Perospiron · Revospiron · Tiospiron · Ziprasidon Difenilbutilpiperazini: Amperozid Fenilpiperazini: Aripiprazol · Bifeprunoks · Brekspiprazol^† · Elopiprazol · Umespiron Triciklici: Amoksapin · Asenapin · Karpipramin · Klocapramin · Klorotepin · Klotiapin · Klozapin # · Fluperlapin · Gevotrolin · Metitepin · Mosapramin · NDMC · Olanzapin · Pihindon · Kvetijapin · Tenilapin · Zotepin Drugi: Blonanserin · Kariprazin · Molindon · Pimavanserin · Roksindol · Sarizotan · Sertindol · Spiramid · Zikronapin^†
Drugi	Alstonin · Azaciklonol · Kanabidiol · Mazapertin^§ · Mifepriston · Oksipertin · Reserpin · Rimkazol · Sekretin · Talnetant^§ · Tetrabenazin · Vabicaserin