I-Boc-Arg (Pbf) -OH iphuma e-arginine.
I-Bivalirudine, i-anticoagulant yokwenziwa engu-20-peptide umzala we-hirudin, yagunyazwa ukudayiswa e-United States ngo-2000. Umjovo uyinto emhlophe, evulekile noma i-amorphous solid.I-Bivarudine ingakwazi ukubopha ngokuqondile indawo ye-thrombin catalytic kanye ne-anion yangaphandle yokubopha isayithi, futhi ivimbele ngokuqondile umsebenzi we-thrombin, ngaleyo ndlela ivimbele ukusabela okubangelwa futhi okubangelwa i-thrombin, futhi umphumela wayo uyahlehla.I-Bivarudine isetshenziswa ngokuyinhloko njenge-anticoagulant ye-elective percutaneous coronary intervention (PCI) kubantu abadala.
I-Bivarudine iyi-inhibitor eqondile ye-thrombin, ebophezela ngokuqondile kumasayithi e-catalytic kanye ne-anion exo-binding sites of thrombin free kanye ne-thrombus.Inqubo yokubopha phakathi kwe-bivaludine ne-thrombin iyabuyiseleka emuva, futhi i-thrombin ingabuyisela umsebenzi wasekuqaleni webhayoloji we-thrombin ngokuthi i-enzymolysis kancane ye-peptide bond phakathi kwe-bivaludine Arg3-Pro4.
Ucwaningo lwe-in vitro lubonise ukuthi i-bivarudine ayikwazi nje ukuvimbela i-thrombin yamahhala yangemuva, kodwa futhi ivimbele ukubopha kwe-thrombin ngamahlule egazi ngaphandle kokuphazanyiswa yizinto ezikhishwe ama-platelet.Ingandisa isikhathi se-prothrombin (APTT), isikhathi se-thrombin (TT), isikhathi se-prothrombin (PT) nesikhathi sokuhlangana esisebenzayo (ACT) esicushwe yi-plasma evamile.Kukhona ubudlelwano bomugqa nokugcwala kwe-bivarudine, kodwa ukuthi ngabe lokhu kuhlobana kukhona yini ekusetshenzisweni komtholampilo akucacile.
Kuye kwabikwa ezincwadini ukuthi i-pharmacokinetics yeziguli ezibhekene ne-percutaneous coronary angioplasty (PTCA) i-linear ngemuva kokuphathwa kwe-intravenous ye-bivarudine.Isiguli sanikezwa i-1 mg / kg nge-intravenously njengomthamo womthwalo, kulandelwa enye infusion ye-IV ye-2.5 mg / kg / hr ngamahora we-4, egxilile ku-12.3 ± 1.7 mg / ml ku-vivo.I-Bivarudine isuswa ku-plasma nge-renal hydrolysis kanye nokuwohloka kwe-protease.Ingxenye yempilo yeziguli ezinomsebenzi wezinso ojwayelekile icishe ibe yimizuzu engama-25, kanti isigamu sempilo yeziguli ezinokwehluleka kwe-renal okumaphakathi nokubi kuyanwetshwa.Cishe i-25% ye-bivarudine ingasuswa nge-dialysis futhi isuswe nge-hemodialysis.I-ACT kufanele iqashwe ezigulini ezinokukhubazeka kwezinso.Kumavolontiya anempilo, umphumela we-anticoagulant wabonwa ngokushesha ngemuva kokuphathwa kwe-bivarudine nge-intravenous, nge-PT, ACT kanye ne-APTT ende.Ihora elilodwa kuya kwamabili ngemva kokuhoxa, i-ACT ibuyele ezingeni langaphambi kokuphatha.