Vareniklin

Vareniklin
(IUPAC) ime
	7,8,9,10-Tetrahudro-6,10-metano-6H-pirazino[2,3-h][3]benzazepin
Klinički podaci
Robne marke	Chantix
AHFS/Drugs.com	Monografija
MedlinePlus	a606024
Identifikatori
CAS broj	249296-44-4 375815-87-5
ATC kod	N07BA03
PubChem	5310966
DrugBank	DB01273
ChemSpider	4470510
UNII	W6HS99O8ZO
KEGG	D08669
ChEMBL	CHEMBL1076903
Hemijski podaci
Formula	C13H13N3
Mol. masa	211,267 g/mol
SMILES	eMolekuli & PubHem
InChI
	InChI=1S/C13H13N3/c1-2-16-13-5-11-9-3-8(6-14-7-9)10(11)4-12(13)15-1/h1-2,4-5,8-9,14H,3,6-7H2/t8-,9+ ; Key: JQSHBVHOMNKWFT-DTORHVGOSA-N
Farmakokinetički podaci
Vezivanje za proteine plazme	<20%
Metabolizam	Ograničen (<10%)
Poluvreme eliminacije	24 sata
Izlučivanje	Renalno (81–92%)
Farmakoinformacioni podaci
Licenca	EU EMEA:link, US FDA:link
Trudnoća	?(US)
Pravni status	℞ Prescription only
Način primene	Oralno

Vareniklin (Chantix, Champix) je lek na recepat koi se koristi za tretmant adikcije na pušenje.^[6]^[7] Vareniklin je parcijalni agonist nikotinski receptor|nikotinskog receptora.^[8] On stimulatiše nikotinske receptore slabije od nikotina. U tom pogledu je sličan sa citizinom, a razlikuje se od nikotinskog antagonista, bupropiona, i terapija nikotinske zamene (NRTs) poput nikotinskog flastera i nikotinske žvake.^[9] Kao parcijalni agonist on redukuje žudnju i umanjuje prijatne efekte cigareta i drugih duvanskih proizvoda. Na taj način on pomaže u ostavljanju pušenja.

Vareniklin je efektivniji od NRT i nikotinskih agonista.^[10]^[11] Klinička studija iz 2006. je pokazala da nakon jedne godine udeo osoba koje su prestale s pušenjem je: 10% za placebo, 15% za bupropion i 23% za vareniklin.^[10]

Reference

↑ Li Q, Cheng T, Wang Y, Bryant SH (2010). „PubChem as a public resource for drug discovery.”. Drug Discov Today 15 (23-24): 1052-7. DOI:10.1016/j.drudis.2010.10.003. PMID 20970519. edit
↑ Evan E. Bolton, Yanli Wang, Paul A. Thiessen, Stephen H. Bryant (2008). „Chapter 12 PubChem: Integrated Platform of Small Molecules and Biological Activities”. Annual Reports in Computational Chemistry 4: 217-241. DOI:10.1016/S1574-1400(08)00012-1.
↑ Hettne KM, Williams AJ, van Mulligen EM, Kleinjans J, Tkachenko V, Kors JA. (2010). „Automatic vs. manual curation of a multi-source chemical dictionary: the impact on text mining”. J Cheminform 2 (1): 3. DOI:10.1186/1758-2946-2-3. PMID 20331846. edit
↑ Joanne Wixon, Douglas Kell (2000). „Website Review: The Kyoto Encyclopedia of Genes and Genomes — KEGG”. Yeast 17 (1): 48–55. DOI:10.1002/(SICI)1097-0061(200004)17:1<48::AID-YEA2>3.0.CO;2-H.
↑ Gaulton A, Bellis LJ, Bento AP, Chambers J, Davies M, Hersey A, Light Y, McGlinchey S, Michalovich D, Al-Lazikani B, Overington JP. (2012). „ChEMBL: a large-scale bioactivity database for drug discovery”. Nucleic Acids Res 40 (Database issue): D1100-7. DOI:10.1093/nar/gkr777. PMID 21948594. edit
↑ „Chantix- varenicline tartrate tablet, film coated Chantix- varenicline tartrate kit”. DailyMed. Arhivirano iz originala na datum 27 September 2021. Pristupljeno 26 September 2021.
↑ „Champix EPAR”. European Medicines Agency (EMA). 17 September 2018. Arhivirano iz originala na datum 16 August 2018. Pristupljeno 26 September 2021. Text was copied from this source which is copyright European Medicines Agency. Reproduction is authorized provided the source is acknowledged.
↑ "Oyster Point Pharma Announces FDA Approval of Tyrvaya (varenicline solution) Nasal Spray for the Treatment of the Signs and Symptoms of Dry Eye Disease" (Press release). Oyster Point Pharma. 18 October 2021. Retrieved 22 October 2021 – via PR Newswire.
↑ Abelovska, Jana. „Champix Tablets Initiation Pack” (en-GB). C-Pharmacy. Pristupljeno 2024-07-01.
↑ ^10,0 ^10,1 Jorenby DE, Hays JT, Rigotti NA, Azoulay S, Watsky EJ, Williams KE, Billing CB, Gong J, Reeves KR (2006). „Efficacy of varenicline, an alpha4beta2 nicotinic acetylcholine receptor partial agonist, vs placebo or sustained-release bupropion for smoking cessation: a randomized controlled trial”. JAMA 296 (1): 56–63. DOI:10.1001/jama.296.1.56. PMID 16820547.
↑ Mills EJ, Wu P, Spurden D, Ebbert JO, Wilson K (2009). „Efficacy of pharmacotherapies for short-term smoking abstinance: a systematic review and meta-analysis”. Harm Reduct J 6: 25. DOI:10.1186/1477-7517-6-25. PMC 2760513. PMID 19761618.

Vanjske veze

	Portal Medicina
	Portal Hemija

[1] Li Q, Cheng T, Wang Y, Bryant SH (2010). „PubChem as a public resource for drug discovery.”. Drug Discov Today 15 (23-24): 1052-7. DOI:10.1016/j.drudis.2010.10.003. PMID 20970519. edit

[2] Evan E. Bolton, Yanli Wang, Paul A. Thiessen, Stephen H. Bryant (2008). „Chapter 12 PubChem: Integrated Platform of Small Molecules and Biological Activities”. Annual Reports in Computational Chemistry 4: 217-241. DOI:10.1016/S1574-1400(08)00012-1.

[3] Hettne KM, Williams AJ, van Mulligen EM, Kleinjans J, Tkachenko V, Kors JA. (2010). „Automatic vs. manual curation of a multi-source chemical dictionary: the impact on text mining”. J Cheminform 2 (1): 3. DOI:10.1186/1758-2946-2-3. PMID 20331846. edit

[4] Joanne Wixon, Douglas Kell (2000). „Website Review: The Kyoto Encyclopedia of Genes and Genomes — KEGG”. Yeast 17 (1): 48–55. DOI:10.1002/(SICI)1097-0061(200004)17:1<48::AID-YEA2>3.0.CO;2-H.

[5] Gaulton A, Bellis LJ, Bento AP, Chambers J, Davies M, Hersey A, Light Y, McGlinchey S, Michalovich D, Al-Lazikani B, Overington JP. (2012). „ChEMBL: a large-scale bioactivity database for drug discovery”. Nucleic Acids Res 40 (Database issue): D1100-7. DOI:10.1093/nar/gkr777. PMID 21948594. edit

[Chantix_FDA_label-6] „Chantix- varenicline tartrate tablet, film coated Chantix- varenicline tartrate kit”. DailyMed. Arhivirano iz originala na datum 27 September 2021. Pristupljeno 26 September 2021.

[Champix_EPAR-7] „Champix EPAR”. European Medicines Agency (EMA). 17 September 2018. Arhivirano iz originala na datum 16 August 2018. Pristupljeno 26 September 2021. Text was copied from this source which is copyright European Medicines Agency. Reproduction is authorized provided the source is acknowledged.

[8] "Oyster Point Pharma Announces FDA Approval of Tyrvaya (varenicline solution) Nasal Spray for the Treatment of the Signs and Symptoms of Dry Eye Disease" (Press release). Oyster Point Pharma. 18 October 2021. Retrieved 22 October 2021 – via PR Newswire.

[9] Abelovska, Jana. „Champix Tablets Initiation Pack” (en-GB). C-Pharmacy. Pristupljeno 2024-07-01.

[Jorenby2006-10] 10,0 ^10,1 Jorenby DE, Hays JT, Rigotti NA, Azoulay S, Watsky EJ, Williams KE, Billing CB, Gong J, Reeves KR (2006). „Efficacy of varenicline, an alpha4beta2 nicotinic acetylcholine receptor partial agonist, vs placebo or sustained-release bupropion for smoking cessation: a randomized controlled trial”. JAMA 296 (1): 56–63. DOI:10.1001/jama.296.1.56. PMID 16820547.

[Mills2009-11] Mills EJ, Wu P, Spurden D, Ebbert JO, Wilson K (2009). „Efficacy of pharmacotherapies for short-term smoking abstinance: a systematic review and meta-analysis”. Harm Reduct J 6: 25. DOI:10.1186/1477-7517-6-25. PMC 2760513. PMID 19761618.

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