Boc-Arg (Pbf) -OH bụ ihe nrụpụta arginine.
Bivalirudine, ọgwụ mgbochi sịntetik nke bụ nwa nwanne 20-peptide nke hirudin, ka akwadoro maka ire ere na United States na 2000. Ngwunye ahụ bụ ihe na-acha ọcha, ihe na-adịghị mma ma ọ bụ ihe siri ike amorphous.Bivarudine nwere ike jikọta kpọmkwem na saịtị thrombin catalytic na anion mpụga njikọ, ma gbochie ọrụ thrombin ozugbo, si otú a na-egbochi mmeghachi omume catalyzed na thrombin, na mmetụta ya na-agbanwe.A na-ejikarị Bivarudine eme ihe dị ka ọgwụ mgbochi ọbara maka ahọpụtara percutaneous coronary intervention (PCI) na ndị okenye.
Bivarudine bụ onye na-egbochi thrombin kpọmkwem, nke na-ejikọta kpọmkwem na saịtị catalytic na anion exo-binding saịtị nke thrombin n'efu yana na thrombus.Usoro njikọ dị n'etiti bivaludine na thrombin na-agbanwe agbanwe, na thrombin nwere ike weghachite ọrụ mbụ nke thrombin site na iji nwayọọ nwayọọ enzymolysis nke njikọ peptide n'etiti bivaludine Arg3-Pro4.
Nnyocha ọmụmụ vitro egosila na bivarudine nwere ike ọ bụghị naanị igbochi thrombin n'akụkụ, kamakwa na-egbochi njikọ nke thrombin na mkpụkọ ọbara na-ewepụghị ya site na ihe ndị platelet wepụtara.Ọ nwere ike ịgbatị oge prothrombin akụkụ (APTT), oge thrombin (TT), oge prothrombin (PT) na oge coagulation na-arụ ọrụ (ACT) nke plasma na-arụ ọrụ.Enwere mmekọrịta kwụ ọtọ na ntinye nke bivarudine, mana ma njikọ a dị na ngwa ụlọ ọgwụ amabeghị.
A kọwo n'akwụkwọ akụkọ na pharmacokinetics nke ndị ọrịa na-arịa ọrịa angioplasty percutaneous (PTCA) bụ ahịrị mgbe nchịkwa intravenous nke bivarudine gasịrị.Enyere onye ọrịa ahụ 1 mg / kg intravenously dị ka ibu ibu, na-esote ntinye IV ọzọ nke 2.5 mg / kg / hr maka awa 4, nke kwadoro na 12.3 ± 1.7 mg / ml na vivo.A na-ehichapụ Bivarudine na plasma site na renal hydrolysis na mmebi protease.Nchapụta ọkara ndụ nke ndị ọrịa nwere ọrụ gbasara akụrụ nkịtị bụ ihe dị ka nkeji iri abụọ na ise, na mkpochapụ ọkara ndụ nke ndị ọrịa nwere oke ụkọ gbasara akụrụ na-agbatịkwu.Ihe dị ka 25% nke bivarudine nwere ike wepụ ya site na dialysis wee kpochapụ site na hemodialysis.Ekwesịrị ileba anya na ACT na ndị ọrịa nwere nsogbu gbasara akụrụ.N'ime ndị ọrụ afọ ofufo ahụ siri ike, a na-ahụ mmetụta anticoagulant ozugbo mgbe nchịkwa intravenous nke bivarudine gasịrị, yana PT, ACT na APTT ogologo oge.Otu awa ma ọ bụ abụọ ka ewepụrụ, ACT laghachiri n'ọkwa nchịkwa tupu oge eruo.