Buspiron

Buspiron
IUPAC ime
	8-[4-(4-pirimidin-2-ilpiperazin-1-il)butil]-8-azaspiro[4.5]dekan-7,9-dion
Klinički podaci
Prodajno ime	Buspar
Drugs.com	Monografija
MedlinePlus	a688005
Kategorija trudnoće	US: B (Bez rizika u ispitivanjima na životinjama) ; ;
Način primene	Oralno
Pravni status
Pravni status	℞ (Prescription only);
Farmakokinetički podaci
Bioraspoloživost	5%
Vezivanje proteina	95%
Metabolizam	Hepatic
Poluvreme eliminacije	2-3 sata
Izlučivanje	Urin (29-63%), izmet (18-38%)
Identifikatori
CAS broj	36505-84-7
ATC kod	N05BE01 (WHO)
PubChem	CID 2477
IUPHAR/BPS	36
DrugBank	DB00490
ChemSpider	2383
UNII	TK65WKS8HL
KEGG	D07593
ChEBI	CHEBI:3223
ChEMBL	CHEMBL49
Hemijski podaci
Formula	C21H31N5O2
Molarna masa	385,50314 g/mol
	SMILES O=C1N(C(=O)CC2(C1)CCCC2)CCCCN4CCN(c3ncccn3)CC4; ;
	InChI InChI=1S/C21H31N5O2/c27-18-16-21(6-1-2-7-21)17-19(28)26(18)11-4-3-10-24-12-14-25(15-13-24)20-22-8-5-9-23-20/h5,8-9H,1-4,6-7,10-17H2 ; Key:QWCRAEMEVRGPNT-UHFFFAOYSA-N ;

Buspiron (Buspar) je anksiolitički psihoaktivni lek iz azapironske hemijske klase. On se prvenstveno koristi za tretiranje generalizovanog anksioznog poremećaja.

Medicinska upotreba

Generalizovani anksiozni poremećaj blagog do umerenog intenziteta.^[1]
Studije su pokazale da je buspiron efektivan kao pojačavajući agens selektivnih inhibitora preuzimanja serotonina (SSRI) u lečenju depresije. Lek nije odobren za ovu vrstu primene.^[2]^[3]^[4]

Hemija

Sinteza buspirona počinje sa N-alkilacijom 1-(2-pirimidil)piperazina sa 4-hlorobutironitrilom čemu sledi hidrogenacija nitrila preko Ranejev nikal katalizatora. Primarni aminski produkt prethodnog koraka sa spirocikličnim kiselim anhidridom daje buspiron.^[5]

Reference

^ „Buspirone monograph”. Drugs.com. Приступљено 27. 8. 2011.
^ National Institute Of Health. „Questions and Answers about the NIMH Sequenced Treatment Alternatives to Relieve Depression (STAR*D) Study — All Medication Levels”. Архивирано из оригинала 19. 08. 2012. г. Приступљено 12. 8. 2012.
^ Trivedi MH, Fava M, Wisniewski SR, Thase ME, Quitkin F, Warden D, Ritz L, Nierenberg AA, Lebowitz BD, Biggs MM, Luther JF, Shores-Wilson K, Rush AJ (2006). „Medication augmentation after the failure of SSRIs for depression”. N. Engl. J. Med. 354 (12): 1243—52. PMID 16554526. doi:10.1056/NEJMoa052964.
^ Appelberg BG, Syvälahti EK, Koskinen TE, Mehtonen OP, Muhonen TT, Naukkarinen HH (2001). „Patients with severe depression may benefit from buspirone augmentation of selective serotonin reuptake inhibitors and in a Class of Drugs called Benzodiazepines and effects similar if not idenical to Alprazelam,Lorazepam etc : results from a placebo-controlled, randomized, double-blind, placebo wash-in study”. J Clin Psychiatry. 62 (6): 448—52. PMID 11465522.
^ Wu YH, Rayburn JW, Allen LE, Ferguson HC, Kissel JW (1972). „Psychosedative agents. 2. 8-(4-Substituted 1-piperazinylalkyl)-8-azaspiro(4.5)decane-7,9-diones”. J. Med. Chem. 15 (5): 477—9. PMID 5035267. doi:10.1021/jm00275a009. ;
DE 2057845, Rayburn JW, Wu YH, "Heterocyclische Azaspirodecandione und Verfahren zu ihrer Herstellung", published 9. 6. 1971. ;
US 3717634, Rayburn JW, Wu YH, "N-(heteroarcyclic)piperazinylalkyl-azaspiroalkanediones", published 20. 2. 1973. ;
US 3907801, Rayburn JW, Wu YH, "N8 (4-pyridyl-piperazino)-alkyl9-azaspiroalkanediones", published 23. 9. 1975. ;
US 3976776, Rayburn JW, Wu YH, "Tranquilizer process employing N-(heteroarcyclic)piperazinylalkylazaspiroalkanediones", published 24. 8. 1976.

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[mono-1] „Buspirone monograph”. Drugs.com. Приступљено 27. 8. 2011.

[2] National Institute Of Health. „Questions and Answers about the NIMH Sequenced Treatment Alternatives to Relieve Depression (STAR*D) Study — All Medication Levels”. Архивирано из оригинала 19. 08. 2012. г. Приступљено 12. 8. 2012.

[pmid16554526-3] Trivedi MH, Fava M, Wisniewski SR, Thase ME, Quitkin F, Warden D, Ritz L, Nierenberg AA, Lebowitz BD, Biggs MM, Luther JF, Shores-Wilson K, Rush AJ (2006). „Medication augmentation after the failure of SSRIs for depression”. N. Engl. J. Med. 354 (12): 1243—52. PMID 16554526. doi:10.1056/NEJMoa052964.

[pmid11465522-4] Appelberg BG, Syvälahti EK, Koskinen TE, Mehtonen OP, Muhonen TT, Naukkarinen HH (2001). „Patients with severe depression may benefit from buspirone augmentation of selective serotonin reuptake inhibitors and in a Class of Drugs called Benzodiazepines and effects similar if not idenical to Alprazelam,Lorazepam etc : results from a placebo-controlled, randomized, double-blind, placebo wash-in study”. J Clin Psychiatry. 62 (6): 448—52. PMID 11465522.

[5] Wu YH, Rayburn JW, Allen LE, Ferguson HC, Kissel JW (1972). „Psychosedative agents. 2. 8-(4-Substituted 1-piperazinylalkyl)-8-azaspiro(4.5)decane-7,9-diones”. J. Med. Chem. 15 (5): 477—9. PMID 5035267. doi:10.1021/jm00275a009. ;
DE 2057845, Rayburn JW, Wu YH, "Heterocyclische Azaspirodecandione und Verfahren zu ihrer Herstellung", published 9. 6. 1971. ;
US 3717634, Rayburn JW, Wu YH, "N-(heteroarcyclic)piperazinylalkyl-azaspiroalkanediones", published 20. 2. 1973. ;
US 3907801, Rayburn JW, Wu YH, "N8 (4-pyridyl-piperazino)-alkyl9-azaspiroalkanediones", published 23. 9. 1975. ;
US 3976776, Rayburn JW, Wu YH, "Tranquilizer process employing N-(heteroarcyclic)piperazinylalkylazaspiroalkanediones", published 24. 8. 1976.

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