Mbiri

Ticagrelor ndi mdani watsopano wa P2Y12 receptor [1].

Ticagrelor yanenedwa kuti imalepheretsa zotsatira za prothrombotic za ADP pa platelet potsutsana ndi P2Y12 receptor. Ticagrelor wasonyeza kuletsa kwathunthu kwa platelet aggregation ex vivo. Kuwonjezera apo, Ticagrelor wanena kuti kulepheretsa kudalira mlingo wa platelet aggregation mwa munthu. Kupatula izi, Ticagrelor wawonetsanso mdani womanga pakamwa, mwachangu, mosinthika. Mosiyana ndi zoletsa zina, Ticagrelor adanenanso kuti amaletsa P2Y12 receptor popanda kusintha kwa metabolic. Kupatula apo, Ticagrelor ndiye woyamba thienopyridine anti-platelet agent ndipo makamaka amapangidwa ndi CYP3A4 ndi CYP2C19 [1] [2].

Zolozera:
[1] Zhou D1, Andersson TB, Grimm SW. Kuwunika kwa in vitro komwe kungatheke kuyanjana ndi mankhwala osokoneza bongo ndi ticagrelor: cytochrome P450 reaction phenotyping, inhibition, induction, and differential kinetics. Mankhwala Metab Dispos. 2011 Apr; 39(4):703-10.
[2] Li Y1, Landqvist C, Grimm SW. Makhalidwe ndi metabolism ya ticagrelor, buku la P2Y12 receptor antagonist, mu mbewa, makoswe, ndi marmosets. Mankhwala Metab Dispos. 2011 Sep; 39 (9): 1555-67. doi: 10.1124/dmd.111.039669. Epub 2011 Jun 13.

Kufotokozera

Ticagrelor (AZD6140) ndi wotsutsana ndi oral P2Y12 receptor antagonist pochiza kuphatikizika kwa mapulateleti.

Mu Vitro

Ticagrelor imalimbikitsa kuletsa kwakukulu kwa adenosine 5'- diphosphate (ADP)-idapangitsa Ca2+ kumasulidwa mu mapulateleti a ished motsutsana ndi otsutsa ena a P2Y12R. Izi zowonjezera za ticagrelor kupitirira P2Y12R antagonism ndi mbali imodzi monga chotsatira cha ticagrelor kuletsa equilibrative nucleoside transporter 1 (ENT1) pa mapulateleti, zomwe zimapangitsa kuti adenosine amtundu wa extracellular ndi activation ya Gs-coupled adenosine A2A receptors [1]. Maselo a B16-F10 amasonyeza kuchepa kwa kuyanjana ndi mapulateleti kuchokera ku mbewa zowonongeka ndi ticagrelor poyerekeza ndi mbewa za saline [2].

Mu B16-F10 melanoma intravenous and intrasplenic metastasis zitsanzo, mbewa zothandizidwa ndi mlingo wachipatala wa ticagrelor (10 mg / kg) zimasonyeza kuchepa kwa mapapo (84%) ndi chiwindi (86%) metastases. Komanso, chithandizo cha ticagrelor chimapangitsa kuti moyo ukhale wabwino poyerekeza ndi nyama zamtundu wa saline. Zotsatira zofananazi zikuwonetsedwa mu chitsanzo cha khansa ya m'mawere ya 4T1, ndi kuchepa kwa mapapo (55%) ndi mafupa a mafupa (87%) metastases kutsatira chithandizo cha ticagrelor [2]. Kulamulira kwapakamwa kamodzi kwa ticagrelor (1-10 mg / kg) kumayambitsa kuletsa kwa mlingo wokhudzana ndi mlingo pamagulu a platelet. Ticagrelor, pa mlingo wapamwamba kwambiri (10 mg / kg) imalepheretsa kwambiri kuphatikizika kwa mapulateleti pa 1 h pambuyo pa dosing ndipo kulepheretsa kwakukulu kumawonedwa pa 4 h pambuyo pa dosing.

Kusungirako

4°C, kuteteza ku kuwala, kusungidwa pansi pa nayitrogeni

*Mu zosungunulira: -80°C, miyezi 6; -20°C, mwezi umodzi (chitetezo ku kuwala, kusungidwa pansi pa nayitrogeni)

Kapangidwe ka mankhwala