Dabigatran Etexilate Mesylate
Inkcazo
I-Dabigatran etexilate mesylate (BIBR 1048MS) yimveliso yomlomo esebenzayo ye-Dabigatran.I-Dabigatran etexilate mesylate ineempembelelo ze-anticoagulant kwaye isetyenziselwa i-prophylaxis ye-venousthromboembolism kunye ne-stroke ngenxa ye-fibrillation ye-atrial.
Imvelaphi
Inkcazo: Ixabiso le-IC50: 4.5nM (Ki);I-10nM(i-Thrombin-induced platelet aggregation) [1] I-Dabigatran yinto ebuyiselwa umva kwaye ikhetha, i-thrombin inhibitor ethe ngqo (DTI) iphantsi kophuhliso lwekliniki oluphezulu njengeprodrug esebenzayo ngomlomo, i-dabigatran etexilate.kwi-vitro: I-Dabigatran ikhetha kwaye ibuyele umva i-thrombin yomntu (Ki: 4.5 nM) kunye ne-thrombin-induced platelet aggregation (IC (50): 10 nM), ngelixa ingabonakali impembelelo yokuthintela kwezinye ii-agent ezivuselela i-platelet. -i-plasma embi (PPP), ilinganiswe njenge-thrombin engapheliyo (ETP) yayinqandekile i-concentration-dependently (IC (50): 0.56 microM).I-Dabigatran ibonise iziphumo ezixhomekeke kwi-concentration-dependent anticoagulant kwiintlobo ezahlukeneyo ze-vitro, ngokuphindwe kabini ixesha elisebenzayo le-thromboplastin (aPTT), ixesha le-prothrombin (PT) kunye nexesha le-ecarin lokuvala (ECT) kwi-PPP yabantu kwiimpawu ze-0.23, 0.83 kunye ne-0.18 microM, ngokulandelanayo [ 1].kwi-vivo: I-Dabigatran yandisa ixesha le-APTT-ngokuxhomekeka emva kokulawulwa kwe-intravenous kwiigundane (0.3, 1 kunye ne-3 mg / kg) kunye ne-rhesus monkeys (0.15, 0.3 kunye ne-0.6 mg / kg).I-dose- kunye nexesha elixhomekeke kwimiphumo ye-anticoagulant yabonwa kunye ne-dabigatran etexilate elawulwa ngomlomo kwiigundane eziqaphelayo (i-10, i-20 kunye ne-50 mg / kg) okanye i-rhesus monkeys (1, 2.5 okanye i-5 mg / kg), kunye nemiphumo ephezulu ebonwa phakathi kwe-30 kunye ne-120 imizuzu emva kolawulo, ngokulandelelana [1].Izigulane eziphathwe nge-dabigatran etexilate zifumana i-stroke ye-ischemic embalwa (i-3.74 dabigatran etexilate vs 3.97 warfarin) kunye ne-haemorrhages encinci ye-intracranial kunye ne-haemorrhagic strokes (0.43 dabigatran etexilate vs 0.99 warfarin] ngonyaka we-10) ngonyaka we-10.Ulingo lwezonyango: Uvavanyo lwe-Pharmacokinetics kunye ne-Pharmacodynamics ye-Oral Dabigatran Etexilate kwi-Hemodialysis Patients.Isigaba1
Ugcino
| Umgubo | -20°C | Iminyaka emi-3 |
| 4°C | iminyaka eyi-2 | |
| Kwi-solvent | -80°C | Iinyanga ezi-6 |
| -20°C | Inyanga eyi-1 |
Ulingo lwezonyango
| Inombolo ye-NCT | Umxhasi | Imeko | Umhla wokuqala | Isigaba |
| NCT02170792 | Boehringer Ingelheim | Usempilweni | NgoFebruwari 2001 | Inqanaba loku-1 |
| NCT02170974 | Boehringer Ingelheim | Usempilweni | Julayi 2004 | Inqanaba loku-1 |
| NCT02170831 | Boehringer Ingelheim | Usempilweni | Meyi 1999 | Inqanaba loku-1 |
| NCT02170805 | Boehringer Ingelheim | Usempilweni | Epreli 2001 | Inqanaba loku-1 |
| NCT02170610 | Boehringer Ingelheim | Usempilweni | Matshi 2002 | Inqanaba loku-1 |
| NCT02170909 | Boehringer Ingelheim | Usempilweni | Disemba 2004 | Inqanaba loku-1 |
| NCT02171000 | Boehringer Ingelheim | Usempilweni | Epreli 2005 | Inqanaba loku-1 |
| NCT02170844 | Boehringer Ingelheim | Usempilweni | NgoJuni 2004 | Inqanaba loku-1 |
| NCT02170584 | Boehringer Ingelheim | Usempilweni | NgoJanuwari 2001 | Inqanaba loku-1 |
| NCT02170935 | Boehringer Ingelheim | I-venous thromboembolism | Epreli 2002 | Inqanaba lesi-2 |
| NCT02170636 | Boehringer Ingelheim | Usempilweni | NgoJanuwari 2002 | Inqanaba loku-1 |
| NCT02170766 | Boehringer Ingelheim | Usempilweni | Okthobha 2000 | Inqanaba loku-1 |
| NCT02171442 | Boehringer Ingelheim | Usempilweni | Epreli 2002 | Inqanaba loku-1 |
| NCT02170896 | Boehringer Ingelheim | Usempilweni | Okthobha 2001 | Inqanaba loku-1 |
| NCT02173730 | Boehringer Ingelheim | Usempilweni | Novemba 2002 | Inqanaba loku-1 |
| NCT02170623 | Boehringer Ingelheim | Usempilweni | NgoFebruwari 2002 | Inqanaba loku-1 |
| NCT02170116 | Boehringer Ingelheim | Usempilweni | NgoNovemba 1998 | Inqanaba loku-1 |
| NCT02170597 | Boehringer Ingelheim | Usempilweni | Agasti 2003 | Inqanaba loku-1 |
| NCT01225822 | Boehringer Ingelheim | I-venous thromboembolism | Novemba 2002 | Inqanaba lesi-2 |
| NCT02170701 | Boehringer Ingelheim | I-venous thromboembolism | Okthobha 2000 | Inqanaba lesi-2 |
| NCT02170740 | Boehringer Ingelheim | Usempilweni | NgoNovemba 1999 | Inqanaba loku-1 |
| NCT02170922 | Boehringer Ingelheim | Usempilweni | NgoJulayi 1999 | Inqanaba loku-1 |
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