I-Dabigatran Etexilate Mesylate
Incazelo
I-Dabigatran etexilate mesylate (BIBR 1048MS) iyisidakamizwa esisebenza ngomlomo se-Dabigatran. I-Dabigatran etexilate mesylate inemiphumela ye-anticoagulant futhi isetshenziselwa ukuvimbela i-venousthromboembolism kanye ne-stroke ngenxa ye-fibrillation ye-atrial.
Ingemuva
Incazelo: IC50 Inani: 4.5nM (Ki); I-10nM(i-Thrombin-induced platelet aggregation) [1] I-Dabigatran iyisivimbeli esiphendulekayo nesikhethayo, esiqondile se-thrombin inhibitor (DTI) esithuthuke kakhulu emtholampilo njenge-prodrug esebenza ngomlomo, i-dabigatran etexilate. ku-vitro: I-Dabigatran evinjelwa ngokukhetha nangokubuyisela emuva i-thrombin yomuntu (Ki: 4.5 nM) kanye ne-thrombin-induced platelet aggregation (IC(50): 10 nM), kuyilapho ingabonisi umphumela wokuvinjelwa kwamanye ama-agent avuselela i-platelet. -i-plasma empofu (PPP), ilinganiswa njengamandla e-thrombin engapheli (I-ETP) iye yavinjelwa ukugxila-okuncike (IC(50): 0.56 microM). I-Dabigatran ibonise imiphumela ye-anticoagulant encike ekugxiliseni ezinhlotsheni ezihlukahlukene ze-vitro, iphinda kabili isikhathi esicushiwe se-thromboplastin (aPTT), isikhathi se-prothrombin (PT) nesikhathi se-ecarin clotting (ECT) ku-PPP yomuntu ekugxilweni kwe-0.23, 0.83 kanye ne-0.18 microM, ngokulandelana [ 1]. ku-vivo: I-Dabigatran yelula umthamo we-aPTT ngokuncika ngemva kokuphathwa ngomthambo wamagundane (0.3, 1 kanye no-3 mg/kg) nezinkawu ze-rhesus (0.15, 0.3 kanye no-0.6 mg/kg). Imiphumela ye-anticoagulant encike kumthamo nesikhathi yabonwa nge-dabigatran etexilate elawulwa ngomlomo kumagundane aqaphile (10, 20 kanye ne-50 mg / kg) noma izinkawu ze-rhesus (1, 2.5 noma 5 mg / kg), enemiphumela ephezulu ebonwa phakathi kuka-30 no-120. iminithi ngemuva kokuphatha, ngokulandelana [1]. Iziguli ezelashwa nge-dabigatran etexilate zithole imivimbo ye-ischemic embalwa (3.74 dabigatran etexilate vs 3.97 warfarin) kanye nokopha okuhlanganisiwe kwe-intracranial kanye nemivimbo yokopha (0.43 dabigatran etexilate vs 0.99 isiguli se-warfarin] ngonyaka we-10). Isilingo somtholampilo: Ukuhlolwa kwe-Pharmacokinetics kanye ne-Pharmacodynamics ye-Oral Dabigatran Etexilate ku-Hemodialysis Patients. Isigaba1
Isitoreji
| Impushana | -20°C | 3 iminyaka |
| 4°C | iminyaka engu-2 | |
| Ku-solvent | -80°C | 6 izinyanga |
| -20°C | Inyanga engu-1 |
Ukuhlolwa Komtholampilo
| Inombolo ye-NCT | Umxhasi | Isimo | Usuku okuqalwa ngalo | Isigaba |
| I-NCT02170792 | Boehringer Ingelheim | Unempilo | February 2001 | Isigaba 1 |
| I-NCT02170974 | Boehringer Ingelheim | Unempilo | Julayi 2004 | Isigaba 1 |
| I-NCT02170831 | Boehringer Ingelheim | Unempilo | Meyi 1999 | Isigaba 1 |
| I-NCT02170805 | Boehringer Ingelheim | Unempilo | Ephreli 2001 | Isigaba 1 |
| I-NCT02170610 | Boehringer Ingelheim | Unempilo | Mashi 2002 | Isigaba 1 |
| I-NCT02170909 | Boehringer Ingelheim | Unempilo | Disemba 2004 | Isigaba 1 |
| I-NCT02171000 | Boehringer Ingelheim | Unempilo | Ephreli 2005 | Isigaba 1 |
| I-NCT02170844 | Boehringer Ingelheim | Unempilo | Juni 2004 | Isigaba 1 |
| I-NCT02170584 | Boehringer Ingelheim | Unempilo | Januwari 2001 | Isigaba 1 |
| I-NCT02170935 | Boehringer Ingelheim | I-venous thromboembolism | Ephreli 2002 | Isigaba 2 |
| I-NCT02170636 | Boehringer Ingelheim | Unempilo | Januwari 2002 | Isigaba 1 |
| I-NCT02170766 | Boehringer Ingelheim | Unempilo | Okthoba 2000 | Isigaba 1 |
| I-NCT02171442 | Boehringer Ingelheim | Unempilo | Ephreli 2002 | Isigaba 1 |
| I-NCT02170896 | Boehringer Ingelheim | Unempilo | Okthoba 2001 | Isigaba 1 |
| I-NCT02173730 | Boehringer Ingelheim | Unempilo | Novemba 2002 | Isigaba 1 |
| I-NCT02170623 | Boehringer Ingelheim | Unempilo | February 2002 | Isigaba 1 |
| I-NCT02170116 | Boehringer Ingelheim | Unempilo | Novemba 1998 | Isigaba 1 |
| I-NCT02170597 | Boehringer Ingelheim | Unempilo | Agasti 2003 | Isigaba 1 |
| I-NCT01225822 | Boehringer Ingelheim | I-venous thromboembolism | Novemba 2002 | Isigaba 2 |
| I-NCT02170701 | Boehringer Ingelheim | I-venous thromboembolism | Okthoba 2000 | Isigaba 2 |
| I-NCT02170740 | Boehringer Ingelheim | Unempilo | Novemba 1999 | Isigaba 1 |
| I-NCT02170922 | Boehringer Ingelheim | Unempilo | Julayi 1999 | Isigaba 1 |
Isakhiwo samakhemikhali
Isiphakamiso18Amaphrojekthi Wokuhlola Ukuvumelana Kwekhwalithi asegunyaziwe4, futhi6amaphrojekthi angaphansi kokugunyazwa.
Uhlelo lokuphatha ikhwalithi yamazwe ngamazwe oluthuthukile lwenze isisekelo esiqinile sokuthengisa.
Ukugadwa kwekhwalithi kusebenza kuwo wonke umjikelezo wempilo womkhiqizo ukuze kuqinisekiswe ikhwalithi nomphumela wokwelapha.
Ithimba Lezindaba Zokulawula Ochwepheshe lisekela izimfuno zekhwalithi ngesikhathi sokufaka isicelo nokubhaliswa.
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