Ticagrelor

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Ticagrelor Anticoagulant Guriga Gudihiisa 28984  

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Gundhig

Ticagrelor waa sheeko-naceyb cusub oo ka mid ah soo-qaadaha P2Y12 [1].

Ticagrelor ayaa lagu soo warramey inuu xakameynayo saameynta prothrombotic ee ADP ee platelet-ka kana soo horjeedo qaataha P2Y12. Ticagrelor wuxuu muujiyey joojinta dhammaystiran ee isu-ururinta platelet ex vivo. Intaa waxaa sii dheer Ticagrelor wuxuu soo jeediyay in la xakameeyo isku-darka isu-geynta platelet-ka ee aadanaha. Marka laga reebo kuwan, Ticagrelor wuxuu kaloo muujiyey hadal ahaan, firfircoon yahay, oo beddel ku-xiran antagonist. Si ka duwan kuwa kale ee ka hortagga ah, Ticagrelor ayaa sidoo kale soo wariyay inuu xakameynayo soo-qaadaha P2Y12 iyada oo aan isbeddel dheef-shiid kiimikaad ah. Taas ka sokow, Ticagrelor waa wakiilkii ugu horreeyay ee loo yaqaan 'thienopyridine anti-platelet' oo inta badan lagu beddelo CYP3A4 iyo CYP2C19 [1] [2].

Tixraacyo:
[1] Zhou D1, Andersson TB, Grimm SW. Qiimeynta fitamiinada ee isdhexgalka daroogada-daroogada ee ticagrelor: cytochrome P450 fal-celinta fal-celinta, ka-hortagga, soo-kicinta, iyo kinetics kala duwan. Daroogada Metab. Abriil 2011; 39 (4): 703-10.
[2] Li Y1, Landqvist C, Grimm SW. Bixinta iyo dheef-shiid kiimikaadka 'ticagrelor', sheeko-yaqaan 'P2Y12 antagonist antagonist', jiirka, jiirka, iyo marmosets-ka. Daroogada Metab. 2011 Sep; 39 (9): 1555-67. doi: 10.1124 / dmd.111.039669. Epub 2011 Jun 13.

Sharaxaad

Ticagrelor (AZD6140) waa dib-u-celin afka ah oo loo yaqaan 'P2Y12 receptor antagonist' oo loogu talagalay daaweynta isu-geynta platelet.

In Vitro

Ticagrelor wuxuu kobciyaa ka hortagga weyn ee adenosine 5'-diphosphate (ADP)-Ca2 + oo lagu sii daayay platelet-ka la dhaqay iyo kuwa kale ee P2Y12R. Saameyntan dheeriga ah ee ticagrelor ee ka baxsan P2Y12R antagonism ayaa qayb ka ah natiijada ticagrelor ee ka hortageysa isu-dheellitirka nucleoside 1 (ENT1) ee platelet, taasoo horseedaysa isku-uruurinta adenosine-ka ka baxsan iyo firfircoonida Gs-coupled adenosine A2A receptors [1]. Unugyada B16-F10 waxay soo bandhigaan isdhexgal yaraanta leh platelet-ka ka yimaada jiirka lagu daaweeyo ticagrelor marka la barbar dhigo jiirka lagu daaweeyay cusbada [2].

Noocyada 'B16-F10 melanoma intravenous and intrasplenic metastasis', jiirarka lagu daaweeyay qiyaasta daaweynta ee ticagrelor (10 mg / kg) waxay muujineysaa hoos u dhigista sambabada (84%) iyo beerka (86%) metastases. Intaa waxaa sii dheer, daaweynta ticagrelor waxay hagaajineysaa badbaadada marka la barbar dhigo xayawaanka lagu daaweeyo cusbada. Saameyn la mid ah ayaa lagu arkay qaabka 4T1 ee kansarka naasaha, iyadoo la dhimayo sambabada (55%) iyo dhuuxa lafta (87%) metastases ka dib daaweynta ticagrelor [2]. Maamulka kaliya ee afka ee ticagrelor (1-10 mg / kg) wuxuu keenaa saameyn xaddidan oo xaddidan oo ku saabsan isu-soo-saarka platelet. Ticagrelor, qiyaasta ugu sarreysa (10 mg / kg) waxay si weyn u xakameysaa isu-soo-ururinta platelet at 1 h ka dib qiyaasta iyo ka-hortagga ugu sarreeya waxaa lagu arkaa 4 h ka dib qiyaasta.

Kaydinta

4°C, ka ilaali iftiinka, ku hoos keydsan nitrogen

* Kala-baxa: -80°C, 6 bilood; -20°C, 1 bil (ka ilaali iftiinka, ku hoos kaydsan nitrogen)

Qaab dhismeedka kiimikada

Ticagrelor

SHAHAADO

2018 GMP-2
原料药GMP证书201811(captopril ,thalidomide etc)
GMP-of-PMDA-in-Chanyoo-平成28年08月03日 Nantong-Chanyoo-Pharmatech-Co
FDA-EIR-Letter-201901

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