Boc-Arg (Pbf) -OH yog arginine derivative.
Bivalirudine, ib qho hluavtaws anticoagulant uas yog 20-peptide kwv tij txheeb ze ntawm hirudin, tau pom zoo muag hauv Tebchaws Meskas hauv xyoo 2000. Kev txhaj tshuaj yog tshuaj dawb, xoob lossis cov khoom amorphous.Bivarudine tuaj yeem khi tshwj xeeb rau thrombin catalytic site thiab anion sab nraud khi qhov chaw, thiab ncaj qha inhibit qhov kev ua ntawm thrombin, yog li inhibiting cov tshuaj tiv thaiv catalyzed thiab induced los ntawm thrombin, thiab nws cov nyhuv yog thim rov qab.Bivarudine feem ntau yog siv los ua anticoagulant rau xaiv percutaneous coronary intervention (PCI) rau cov neeg laus.
Bivarudine yog ib qho ncaj qha inhibitor ntawm thrombin, uas tshwj xeeb khi rau cov chaw catalytic thiab anion exo-binding qhov chaw ntawm thrombin dawb thiab ntawm thrombus.Cov txheej txheem khi ntawm bivaludine thiab thrombin yog thim rov qab, thiab thrombin tuaj yeem rov qab ua cov haujlwm lom neeg ntawm thrombin los ntawm maj mam enzymolysis ntawm peptide daim ntawv cog lus ntawm bivaludine Arg3-Pro4.
Cov kev tshawb fawb hauv vitro tau pom tias bivarudine tuaj yeem tsis tsuas yog cuam tshuam rau sab nraud dawb thrombin, tab sis kuj inhibit cov thrombin khi nrog cov ntshav txhaws yam tsis muaj kev cuam tshuam los ntawm cov tshuaj tso tawm los ntawm platelets.Nws tuaj yeem ncua sijhawm ib nrab ntawm lub sijhawm prothrombin (APTT), lub sijhawm thrombin (TT), lub sijhawm prothrombin (PT) thiab lub sijhawm ua haujlwm coagulation (ACT) ua haujlwm los ntawm cov ntshav plasma.Muaj kev sib raug zoo nrog cov concentration ntawm bivarudine, tab sis seb qhov kev sib raug zoo no puas muaj nyob hauv daim ntawv thov kho mob tsis paub meej.
Nws tau raug tshaj tawm nyob rau hauv cov ntaub ntawv hais tias cov tshuaj pharmacokinetics ntawm cov neeg mob nyob rau hauv percutaneous coronary angioplasty (PTCA) yog linear tom qab intravenously tswj ntawm bivarudine.Tus neeg mob tau muab 1 mg / kg intravenously raws li kev thauj khoom, tom qab ntawd los ntawm lwm qhov IV infusion ntawm 2.5 mg / kg / teev rau 4 teev, uas ruaj khov ntawm 12.3 ± 1.7 mg / ml hauv vivo.Bivarudine yog tshem tawm ntawm plasma los ntawm lub raum hydrolysis thiab protease degradation.Kev tshem tawm ib nrab-lub neej ntawm cov neeg mob uas lub raum ua haujlwm li qub yog li 25 feeb, thiab qhov kev tshem tawm ib nrab-lub neej ntawm cov neeg mob uas muaj lub raum tsis txaus thiab mob hnyav tau txuas ntxiv.Txog 25% ntawm bivarudine tuaj yeem raug tshem tawm los ntawm kev lim ntshav thiab tshem tawm los ntawm hemodialysis.ACT yuav tsum tau saib xyuas hauv cov neeg mob lub raum tsis zoo.Hauv cov neeg ua haujlwm noj qab haus huv, cov nyhuv anticoagulant tau pom tam sim tom qab txhaj tshuaj ntawm bivarudine, nrog rau lub sijhawm ntev PT, ACT thiab APTT.Ib mus rau ob teev tom qab rho tawm, ACT rov qab mus rau qib ua ntej kev tswj hwm.