Prasugrel
![]() | |||
(IUPAC) ime | |||
---|---|---|---|
(RS)-5-[2-ciklopropil-1-(2-fluorofenil)-2-oksoetil]-4,5,6,7- tetrahidrotieno[3,2-c]piridin-2-il acetat | |||
Klinički podaci | |||
Robne marke | Effient, Efient | ||
AHFS/Drugs.com | Monografija | ||
MedlinePlus | a609027 | ||
Identifikatori | |||
CAS broj | 150322-43-3 | ||
ATC kod | B01AC22 | ||
PubChem[1][2] | 6918456 | ||
DrugBank | DB06209 | ||
ChemSpider[3] | 5293653 | ||
UNII | 34K66TBT99 ![]() | ||
KEGG[4] | D05597 ![]() | ||
ChEMBL[5] | CHEMBL1201772 ![]() | ||
Hemijski podaci | |||
Formula | C20H20FNO3S | ||
Mol. masa | 373,442 g/mol | ||
SMILES | eMolekuli & PubHem | ||
| |||
Farmakokinetički podaci | |||
Bioraspoloživost | ≥79% | ||
Vezivanje za proteine plazme | Aktivni metabolit: ~98% | ||
Metabolizam | Brz intestinalni i serumski metabolizam | ||
Poluvreme eliminacije | ~7 sati (opseg 2-15 sata) | ||
Izlučivanje | Urin (~68% neaktivni metaboliti); izmet (27% neaktivni metaboliti) | ||
Farmakoinformacioni podaci | |||
Licenca | |||
Trudnoća | B(US) | ||
Pravni status | POM (UK) ℞-only (SAD) | ||
Način primene | Oralno |
Prasugrel (Effient, Efient) je antitrombotik koji je razvila kompanija Daiichi Sankyo Co. On je u prodaji za akutne koronarne sindrome usled perkutane koronarne intervencije (PCI). Prasugrel je odobren za upotrebu u Evropi februara 2009. Iste godine je FDA odobrila upotrebu ovog leka za redukciju učestalosti trombotičkih kardiovaskularnih događaja (uključujući stent trombozu) kod pacijenata sa akutnim koronarnim sindromom.[6]
Farmakologija
![](http://upload.wikimedia.org/wikipedia/commons/thumb/3/3d/Prasugrel_activation.svg/330px-Prasugrel_activation.svg.png)
Prasugrel je član tienopiridinske klase inhibitora ADP receptora, poput tiklopidina (Tiklida) i klopidogrela (Plaviksa). Ti agensi redukuju agregaciju (gzrušavanje) trombocita putem ireversizibilnog vezivanja za P2Y12 receptore. U poređenju sa klopidogrelom, prasugrel brže i konzistentnije inhibira adenozin difosfatom indukovanu agregaciju trombocita. On proizvodi taj efekat u većoj meri nego standardne i povišene doze klopidogrela kod zdravih volontera i pacijenata sa koronarnom arterijskom bolešću, uključujući pacijenate koji su bili podvrgnuti perkutanoj koronarnoj intervenciji.[7][8][9][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
- ↑ Baker WL, White CM. Role of Prasugrel, a Novel P2Y12 Receptor Antagonist, in the Management of Acute Coronary Syndromes. American Journal of Cardiovascular Drugs Aug 1, 2009; 9 (4): 213-229. Link text Arhivirano 2012-02-24 na Wayback Machine-u
- ↑ Wiviott SD, Braunwald E, McCabe CH i dr.. (2007). „Prasugrel versus clopidogrel in patients with acute coronary syndromes”. The New England Journal of Medicine 357 (20): 2001–15. DOI:10.1056/NEJMoa0706482.
- ↑ "FDA Announces New Boxed Warning on Plavix: Alerts patients, health care professionals to potential for reduced effectiveness" (Press release). Food and Drug Administration (United States). 2010-03-12. Retrieved 2010-03-12.
- ↑ „FDA Drug Safety Communication: Reduced effectiveness of Plavix (clopidogrel) in patients who are poor metabolizers of the drug”. Drug Safety and Availability. Food and Drug Administration (United States). 12. 3. 2010.. Pristupljeno 13. 3. 2010.
- ↑ Silvano M, et al. (2011). „A case of resistance to clopidogrel and prasugrel after percutaneous coronary angioplasty.”. J Thromb Thrombolysis 31(2): 233–4. PMID 21088983.
Spoljašnje veze
![]() | Portal Medicina |
![]() | Portal Hemija |
- Prasugrel information
- Use of prasugrel vs clopidogrel and other anti-aggregant drugs in ACS