Dabigatran Etexilate Mesylate
Tlhaloso
Dabigatran etexilate mesylate (BIBR 1048MS) ke sehlahisoa se sebetsang ka molomo sa Dabigatran.Dabigatran etexilate mesylate e na le litlamorao tsa anticoagulant mme e sebelisoa bakeng sa prophylaxis ea venousthromboembolism le stroke ka lebaka la fibrillation ea atrial.
Ka morao
Tlhaloso: IC50 Boleng: 4.5nM (Ki);10nM(Thrombin-induced platelet aggregation) [1] Dabigatran ke ntho e fetolehang hape e khetha, e tobileng thrombin inhibitor (DTI) e ntseng e tsoela pele ka tsoelo-pele ea bongaka e le prodrug ea eona ea molomo, dabigatran etexilate.in vitro: Dabigatran e thibela thrombin ea motho ka ho khetha le ka ho fetola (Ki: 4.5 nM) hammoho le ho kopana ha platelet e bakoang ke thrombin (IC(50): 10 nM), ha e sa bontše phello e thibelang lintho tse ling tse susumetsang platelet. -Poor plasma (PPP), e lekantsoeng e le endogenous thrombin potential (ETP) e ne e thibetsoe mahloriso-ho itšetlehile ka (IC (50): 0.56 microM).Dabigatran e bonts'itse litlamorao tsa anticoagulant tse itšetlehileng ka mahloriso mefuteng e fapaneng ea vitro, e imena habeli nako ea karolo ea thromboplastin (aPTT), nako ea prothrombin (PT) le nako ea ho koala ea ecarin (ECT) ho PPP ea motho maemong a 0.23, 0.83 le 0.18 microM, ka ho latellana [ 1].in vivo: Dabigatran e lelefatsa lethal dose ea aPTT ka mor'a ho tsamaisoa ka methapo ho likhoto (0.3, 1 le 3 mg/kg) le litšoene tsa rhesus (0.15, 0.3 le 0.6 mg/kg).Litlamorao tsa anticoagulant tse itšetlehileng ka nako le nako li ile tsa bonoa ka dabigatran etexilate e tsamaisoang ka molomo ho likhoto tse tsebang (10, 20 le 50 mg / kg) kapa litšoene tsa rhesus (1, 2.5 kapa 5 mg / kg), ka litlamorao tse kholo tse bonoang lipakeng tsa 30 le 120. metsotso ka mor'a tsamaiso, ka ho latellana [1].Bakuli ba tšoaroang ka dabigatran etexilate ba ile ba e-ba le lichapo tse fokolang tsa ischemic (3.74 dabigatran etexilate vs 3.97 warfarin) le ho fokotseha ho fokolang ho kopantsoeng ha mali a intracranial le liropo tsa haemorrhagic (0.43 dabigatran etexilate vs 0.99 warfarin) ka selemo sa 10.Teko ea meriana: Tlhahlobo ea Pharmacokinetics le Pharmacodynamics ea Oral Dabigatran Etexilate ho Bakuli ba Hemodialysis.Mokhahlelo oa 1
Polokelo
Phofo | -20°C | 3 lilemo |
4°C | lilemo tse 2 | |
Ka solvent | -80°C | Likhoeli tse 6 |
-20°C | 1 khoeli |
Teko ea Tleliniki
Nomoro ea NCT | Motšehetsi | Boemo | Letsatsi la qalo | Mokhahlelo |
NCT02170792 | Boehringer Ingelheim | Bophelo bo botle | Hlakola 2001 | Mokhahlelo oa 1 |
NCT02170974 | Boehringer Ingelheim | Bophelo bo botle | Phupu 2004 | Mokhahlelo oa 1 |
NCT02170831 | Boehringer Ingelheim | Bophelo bo botle | Ka May 1999 | Mokhahlelo oa 1 |
NCT02170805 | Boehringer Ingelheim | Bophelo bo botle | Mmesa 2001 | Mokhahlelo oa 1 |
NCT02170610 | Boehringer Ingelheim | Bophelo bo botle | Hlakubele 2002 | Mokhahlelo oa 1 |
NCT02170909 | Boehringer Ingelheim | Bophelo bo botle | December 2004 | Mokhahlelo oa 1 |
NCT02171000 | Boehringer Ingelheim | Bophelo bo botle | Mmesa 2005 | Mokhahlelo oa 1 |
NCT02170844 | Boehringer Ingelheim | Bophelo bo botle | Phuptjane 2004 | Mokhahlelo oa 1 |
NCT02170584 | Boehringer Ingelheim | Bophelo bo botle | Pherekhong 2001 | Mokhahlelo oa 1 |
NCT02170935 | Boehringer Ingelheim | Thromboembolism ea Venus | Mmesa 2002 | Mokhahlelo oa 2 |
NCT02170636 | Boehringer Ingelheim | Bophelo bo botle | Pherekhong 2002 | Mokhahlelo oa 1 |
NCT02170766 | Boehringer Ingelheim | Bophelo bo botle | October 2000 | Mokhahlelo oa 1 |
NCT02171442 | Boehringer Ingelheim | Bophelo bo botle | Mmesa 2002 | Mokhahlelo oa 1 |
NCT02170896 | Boehringer Ingelheim | Bophelo bo botle | Mphalane 2001 | Mokhahlelo oa 1 |
NCT02173730 | Boehringer Ingelheim | Bophelo bo botle | November 2002 | Mokhahlelo oa 1 |
NCT02170623 | Boehringer Ingelheim | Bophelo bo botle | Hlakola 2002 | Mokhahlelo oa 1 |
NCT02170116 | Boehringer Ingelheim | Bophelo bo botle | November 1998 | Mokhahlelo oa 1 |
NCT02170597 | Boehringer Ingelheim | Bophelo bo botle | Phato 2003 | Mokhahlelo oa 1 |
NCT01225822 | Boehringer Ingelheim | Thromboembolism ea Venus | November 2002 | Mokhahlelo oa 2 |
NCT02170701 | Boehringer Ingelheim | Thromboembolism ea Venus | October 2000 | Mokhahlelo oa 2 |
NCT02170740 | Boehringer Ingelheim | Bophelo bo botle | November 1999 | Mokhahlelo oa 1 |
NCT02170922 | Boehringer Ingelheim | Bophelo bo botle | July 1999 | Mokhahlelo oa 1 |
Sebopeho sa lik'hemik'hale
Tlhahiso18Merero ea Tlhahlobo ea Boleng e amohetsoeng4, le6merero e tlas'a tumello.
Sistimi e tsoetseng pele ea boleng ba machaba e thehile motheo o tiileng oa thekiso.
Tlhokomelo ea boleng e tsamaisana le potoloho eohle ea bophelo ba sehlahisoa ho netefatsa boleng le phello ea kalafo.
Sehlopha sa Litaba tsa Taolo ea Setsebi se tšehetsa litlhoko tsa boleng nakong ea kopo le ngoliso.