Dabigatran Etexilate Mesylate
Fa'amatalaga
Dabigatran etexilate mesylate (BIBR 1048MS) ose vailaʻau faʻamalosi tautala a Dabigatran. Dabigatran etexilate mesylate ei ai aʻafiaga anticoagulant ma faʻaaogaina mo le puipuia o le venousthromboembolism ma le stroke ona o le fibrillation atrial.
Talaaga
Faʻamatalaga: IC50 Taua: 4.5nM (Ki); 10nM(Thrombin-induced platelet aggregation) [1] O le Dabigatran o se mea e mafai ona toe fa'afo'i ma filifili, fa'atosina sa'o o le thrombin (DTI) o lo'o fa'aauau le atina'eina o falema'i e avea o ana vaila'au fa'amalosi tautala, dabigatran etexilate. in vitro: Dabigatran filifili ma toe faʻafefe le thrombin tagata (Ki: 4.5 nM) faʻapea foʻi ma le thrombin-induced platelet aggregation (IC(50): 10 nM), aʻo faʻaalia le leai o se aʻafiaga i luga o isi platelet-stimulating agents.Thrombin generation in platelet -mativa plasma (PPP), fuaina e pei o le gafatia o le thrombin endogenous (ETP) na taofia le faʻaogaina-faʻalagolago (IC(50): 0.56 microM). Na faʻaalia e Dabigatran aʻafiaga o le anticoagulant faʻalagolago i le faʻaogaina i ituaiga eseese i vitro, faʻaluaina le taimi o le thromboplastin faʻagaoioia (aPTT), taimi o le prothrombin (PT) ma le taimi o le ecarin clotting (ECT) i le PPP tagata i le faʻaogaina o le 0.23, 0.83 ma le 0.18 microM, i le faasologa. 1]. i vivo: Dabigatran faʻaumiina le aPTT dose-faʻalagolago pe a uma le faʻaogaina o le toto i isumu (0.3, 1 ma le 3 mg / kg) ma manuki rhesus (0.15, 0.3 ma le 0.6 mg / kg). O aʻafiaga faʻamalosi ma faʻalagolago i le taimi na matauina i le dabigatran etexilate e tuʻuina tautala i isumu (10, 20 ma le 50 mg / kg) poʻo manuki rhesus (1, 2.5 poʻo le 5 mg / kg), ma le maualuga o aʻafiaga na matauina i le va o le 30 ma le 120. min pe a uma le faʻatonuga, faʻasologa [1]. O ma'i na togafitia i le dabigatran etexilate na maua le itiiti ifo o ta'i ischemic (3.74 dabigatran etexilate vs 3.97 warfarin) ma le itiiti ifo o le toto tu'ufa'atasia ma le fa'ama'i toto (0.43 dabigatran etexilate vs 0.99 warfarin) i le 100 ma'i-tausaga]. Faʻataʻitaʻiga faʻapitoa: O se Iloiloga o Pharmacokinetics ma Pharmacodynamics o le Oral Dabigatran Etexilate i Maʻi Hemodialysis. Vaega1
Teuina
| O le pauta | -20°C | 3 tausaga |
| 4°C | 2 tausaga | |
| I solvent | -80°C | 6 masina |
| -20°C | 1 masina |
Tofotofoga Fa'afoma'i
| Numera NCT | Sponsor | Tulaga | Aso Amata | Vaega |
| NCT02170792 | Boehringer Ingelheim | Soifua maloloina | Fepuari 2001 | Vaega 1 |
| NCT02170974 | Boehringer Ingelheim | Soifua maloloina | Iulai 2004 | Vaega 1 |
| NCT02170831 | Boehringer Ingelheim | Soifua maloloina | Me 1999 | Vaega 1 |
| NCT02170805 | Boehringer Ingelheim | Soifua maloloina | Aperila 2001 | Vaega 1 |
| NCT02170610 | Boehringer Ingelheim | Soifua maloloina | Mati 2002 | Vaega 1 |
| NCT02170909 | Boehringer Ingelheim | Soifua maloloina | Tesema 2004 | Vaega 1 |
| NCT02171000 | Boehringer Ingelheim | Soifua maloloina | Aperila 2005 | Vaega 1 |
| NCT02170844 | Boehringer Ingelheim | Soifua maloloina | Iuni 2004 | Vaega 1 |
| NCT02170584 | Boehringer Ingelheim | Soifua maloloina | Ianuari 2001 | Vaega 1 |
| NCT02170935 | Boehringer Ingelheim | Venous Thromboembolism | Aperila 2002 | Vaega 2 |
| NCT02170636 | Boehringer Ingelheim | Soifua maloloina | Ianuari 2002 | Vaega 1 |
| NCT02170766 | Boehringer Ingelheim | Soifua maloloina | Oketopa 2000 | Vaega 1 |
| NCT02171442 | Boehringer Ingelheim | Soifua maloloina | Aperila 2002 | Vaega 1 |
| NCT02170896 | Boehringer Ingelheim | Soifua maloloina | Oketopa 2001 | Vaega 1 |
| NCT02173730 | Boehringer Ingelheim | Soifua maloloina | Novema 2002 | Vaega 1 |
| NCT02170623 | Boehringer Ingelheim | Soifua maloloina | Fepuari 2002 | Vaega 1 |
| NCT02170116 | Boehringer Ingelheim | Soifua maloloina | Novema 1998 | Vaega 1 |
| NCT02170597 | Boehringer Ingelheim | Soifua maloloina | Aokuso 2003 | Vaega 1 |
| NCT01225822 | Boehringer Ingelheim | Venous Thromboembolism | Novema 2002 | Vaega 2 |
| NCT02170701 | Boehringer Ingelheim | Venous Thromboembolism | Oketopa 2000 | Vaega 2 |
| NCT02170740 | Boehringer Ingelheim | Soifua maloloina | Novema 1999 | Vaega 1 |
| NCT02170922 | Boehringer Ingelheim | Soifua maloloina | Iulai 1999 | Vaega 1 |
Fa'asologa o vaila'au
Fautuaga18Poloketi Iloiloga Tulaga Tulaga Lelei ua fa'amaonia4, ma6galuega faatino o lo'o i lalo ole faamaoniga.
O faiga fa'ava-o-malo maualuga pulega lelei ua fa'ata'atia le fa'avae mautu mo fa'atauga.
O le va'aiga lelei e fa'atautaia i le taamilosaga atoa o le olaga o le oloa ina ia mautinoa le lelei ma le togafitiga.
E lagolagoina e le Vaega o Mataupu Tau Fa'apolofesa le tulaga lelei mana'omia ile taimi ole talosaga ma le resitalaina.
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