Pimobendan Capsule,uas yog ib qho tshuaj siv los kho cov kab mob plawv thiab muaj cov phosphodiesterase III (PDE3) inhibitors. Hauv kev faib tshuaj, nws belongs rau qeb ntawm cov tshuaj tiv thaiv lub plawv tsis ua haujlwm, uas txhim kho lub plawv ua haujlwm los ntawm kev txhim kho myocardial contractility thiab vasodilation. Cov tshuaj npe ntawm Pimobedan yog 6- [2- (4-methoxyphenyl) -1H-benzimidazol-5-yl] -5-methyl-4,5-dihydro-3 (2H) - pyridazinone, nrog rau cov mis molecular ntawm C19H18N4O2, CAS 27419-15-2 334.37 Nws. Nws yog cov hmoov dawb rau me ntsis daj crystalline hmoov uas yuav luag insoluble hauv dej los yog ethyl, tab sis muaj qee yam solubility hauv cov kuab tshuaj organic, xws li dawb soluble hauv formic acid lossis acetic acid, thiab me ntsis soluble hauv ethanol lossis methanol. Muaj feem ntau yog ua los ntawm kev sib xyaw pimobedan nrog cov khoom tsim nyog los tsim daim ntawv tshuaj ntsiav rau kev tswj qhov ncauj.
Peb cov khoom
Cov ntaub ntawv ntxiv ntawm chemical compound:
Peb Cov Khoom
Pimobendan +. COA
Pharmacokinetic zog
Kev nqus
Tom qab qhov ncauj tswj hwm ntawmPimobendan ntsiav tshuaj, cov tshuaj yog absorbed nyob rau hauv lub plab zom mov. Qhov nqus tau thiab qib yuav cuam tshuam los ntawm ntau yam, xws li kev noj zaub mov, pH tus nqi ntawm lub plab zom mov, thiab lwm yam. Feem ntau hais lus, cov ntshav concentration ntawm pimobedan nce mus txog qhov siab tshaj li 0.8 teev tom qab noj qhov ncauj.
Kev faib tawm
Pimobedan yog dav faib nyob rau hauv lub cev thiab muaj ib tug siab binding tus nqi nrog plasma proteins. Nws tuaj yeem nkag mus rau cov hlwb myocardial thiab vascular du leeg hlwb, ua rau nws cov tshuaj pharmacological.
Metabolism
Pimobedan yog metabolized nyob rau hauv daim siab, thiab nws cov nquag metabolite (UD{0}}CG212) muaj zog dua Pimobedan nws tus kheej. Cov metabolites feem ntau yog tawm los ntawm cov kua tsib mus rau hauv lub plab zom mov thiab tawm nrog cov quav.
Kev tso tawm
Lub excretion ntawm pimobedan thiab nws cov metabolites feem ntau yog los ntawm quav, nrog ib tug me me npaum li cas tej zaum yuav excreted los ntawm cov zis. Nws tshem tawm ib nrab- lub neej luv luv, nrog rau t1/2 ntawm li 1 teev rau cov tib neeg noj qab haus huv tom qab tswj qhov ncauj. Tom qab daim ntawv thov tas mus li rau ib lub lim tiam, tsis muaj cov ntshav ntau ntxiv.
Cov tshuaj sib cuam tshuam thiab ceev faj
Cov tshuaj sib cuam tshuam
Kev sib tham nrog cov tshuaj digitalis
Thaum ua ke nrog cov tshuaj digitalis, nws tuaj yeem txhim kho qhov txiaj ntsig zoo inotropic ntawm digitalis thiab ua rau muaj kev pheej hmoo ntawm arrhythmia. Yog li ntawd, kev soj ntsuam ze ntawm tus neeg mob lub electrocardiogram thiab ntshav tshuaj concentration yog qhov tsim nyog thaum siv kev sib xyaw ua ke.
Kev sib tham nrog calcium channel blockers
Calcium channel blockers tuaj yeem ua rau tsis muaj txiaj ntsig zoo inotropic ntawm pimobedan, thaum pimobedan kuj tseem tuaj yeem cuam tshuam cov txiaj ntsig ntawm calcium channel blockers. Yog li ntawd, yuav tsum tau ceev faj txog kev kho cov koob tshuaj thaum siv kev kho ua ke.
Kev sib cuam tshuam nrog lwm yam tshuaj
Nws kuj tseem tuaj yeem cuam tshuam nrog lwm cov tshuaj, xws li beta blockers, angiotensin -hloov cov enzyme inhibitors, thiab lwm yam. Thaum siv kev sib xyaw ua ke, nws yuav tsum ua tib zoo xav txog cov txheej txheem ntawm kev ua thiab kev tsis zoo ntawm cov tshuaj, kom tsis txhob muaj kev phiv los yog txo qhov ua tau zoo.
Cov kev ceev faj
Kev ntsuam xyuas ua ntej noj tshuaj
Ua ntej sivPimobendan ntsiav tshuaj, nws yog ib qho tsim nyog yuav tsum tau ua qhov kev ntsuam xyuas lub cev ntawm tus neeg mob, suav nrog kev ntsuas kev ua haujlwm ntawm lub plawv, kev kuaj mob siab thiab lub raum, thiab lwm yam, txhawm rau txiav txim siab seb tus neeg mob puas haum rau kev siv tshuaj.
Kev tshuaj xyuas cov txheej txheem
Thaum lub sijhawm siv tshuaj, nws yuav tsum tau ua tib zoo saib xyuas tus neeg mob qhov kev xav thiab kev hloov pauv ntawm lawv tus mob, ntsuas cov cim tseem ceeb xws li lub plawv dhia thiab ntshav siab, thiab kho cov phiaj xwm kho raws sijhawm. Yog tias muaj kev phiv loj heev tshwm sim, cov tshuaj yuav tsum tau nres tam sim ntawd thiab yuav tsum tau siv cov kev kho mob sib xws.
Tshuaj rau cov neeg tshwj xeeb
Rau cov neeg tshwj xeeb xws li cov neeg laus thiab cov neeg mob uas muaj lub siab thiab lub raum tsis ua haujlwm, nws yog ib qho tsim nyog yuav tsum ua tib zoo kho cov tshuaj thiab ua tib zoo saib xyuas qhov tsis zoo ntawm cov tshuaj thaum siv cov khoom.
Cov kev sib xyaw ua ke ntawm pimobedan feem ntau koom nrog ntau -cov tshuaj lom neeg cov tshuaj tiv thaiv kab mob. Hauv qab no yog ib qho kev piav qhia ntawm ib qho ntawm cov kev sib txuas ntau dua:
Pib cov ntaub ntawv thiab cov tshuaj tiv thaiv ua ntej
Cov ntaub ntawv pib: Lub synthesis ntawm pimobedan feem ntau pib nrog cov organic tebchaw xws li chlorobenzene lossis acetanilide. Cov ntaub ntawv nyoos no dhau los ua cov tshuaj tiv thaiv tshuaj maj mam tsim cov qauv molecular ntawm pimobedan.
Cov tshuaj tiv thaiv ua ntej: Cov khoom pib ua ntej dhau los ua cov kauj ruam xws li acetylation, nitration, bromination, thiab lwm yam los tsim cov tshuaj nruab nrab. Cov tshuaj tiv thaiv no feem ntau xav tau cov catalysts, cov kuab tshuaj, thiab cov tshuaj tiv thaiv kom ua tiav.
Kev hloov pauv ntawm cov khoom nruab nrab
Kev npaj ntawm cov tshuaj nruab nrab: Los ntawm cov tshuaj tiv thaiv ntxiv xws li cov tshuaj tiv thaiv nucleophilic hloov pauv, hydrolysis decarboxylation cov tshuaj tiv thaiv, thiab lwm yam, cov tshuaj nruab nrab uas tsim los ntawm cov tshuaj tiv thaiv thawj zaug tau hloov mus rau hauv ntau cov tshuaj intermediates.
Purification ntawm intermediates: Thaum lub sij hawm hloov dua siab tshiab, tej zaum yuav tsim nyog los ntxuav cov intermediates kom tshem tawm impurities thiab txhim kho cov purity ntawm cov khoom. purification txoj kev feem ntau muaj xws li rho tawm, recrystallization, kem chromatography, thiab lwm yam.
Cov kauj ruam tseem ceeb thiab cov xwm txheej tshwm sim
Cov kauj ruam tseem ceeb: Hauv kev sib txuas ntawm pimobedan, muaj qee cov kauj ruam tseem ceeb uas txiav txim siab qhov zoo thiab qhov txiaj ntsig ntawm cov khoom kawg. Piv txwv li, kev sib txuas sib txuas, cov tshuaj tiv thaiv ester hydrolysis, thiab cov tshuaj decarboxylation ntawm qee cov tshuaj nruab nrab.
Cov kev mob tshwm sim: Cov kauj ruam tseem ceeb no feem ntau xav tau cov tshuaj tiv thaiv tshwj xeeb, xws li kub, siab, hom catalyst thiab ntau npaum li cas. Qhov kev ua kom zoo ntawm cov tshuaj tiv thaiv yog qhov tseem ceeb rau kev txhim kho cov txiaj ntsig thiab purity ntawm cov khoom.
Synthesis thiab purification ntawm cov khoom kawg
Lub synthesis ntawm cov khoom kawg: Tom qab ib tug series ntawm cov tshuaj tiv thaiv, Pimobendn yog thaum kawg tsim. Thaum lub sij hawm tus txheej txheem no, nws yuav tsum tau kho kom zoo tune cov tshuaj tiv thaiv tej yam kev mob los xyuas kom meej qhov zoo thiab tawm los ntawm cov khoom.
Purification ntawmPimobendan tshuaj ntsiav: Lub generated pimobendn feem ntau yuav tsum tau purification kho kom tshem tawm cov seem impurities thiab catalyst. Txoj kev ua kom huv tuaj yeem suav nrog recrystallization, kem chromatography, thiab lwm yam.
keeb kwm kev loj hlob
Cov keeb kwm kev loj hlob tuaj yeem taug qab rov qab mus rau qhov kev tshawb nrhiav thaum ntxov ntawm kev txhim kho tshuaj, uas tau dhau los ntawm kev tshawb fawb yooj yim, kev siv tshuaj kho mob, thiab kev siv dav dav, maj mam dhau los ua cov tshuaj tseem ceeb hauv kev kho mob plawv.
1. Kev tshawb fawb ntxov thiab kev tshawb fawb txog kev tshawb fawb (1980s txog 1990s)
Txoj kev loj hlob ntawm Pimobendn tau pib thaum xyoo 1980, nrog cov kws tshawb fawb tau mob siab rau nrhiav cov tshuaj uas ua ke nrog cov teebmeem inotropic zoo thiab cov teebmeem vasodilatory. Nws cov qauv molecular yog benzimidazole pyridazine derivative, uas ua haujlwm los ntawm ob lub tswv yim: ntawm ib sab, nws ua raws li phosphodiesterase III (PDE3) inhibitor, txo cov degradation ntawm cyclic adenosine monophosphate (cAMP), nce intracellular cAMP concentration, thiab txhim kho myocardial contraction; Ntawm qhov tod tes, raws li calcium sensitizer, nws ncaj qha nce rhiab heev ntawm myocardial contractile proteins rau calcium ions, txhim kho myocardial contraction efficiency. Cov txheej txheem tshwj xeeb no txhim kho myocardial contractility thaum zam kev pheej hmoo ntawm arrhythmia uas yuav tshwm sim los ntawm cov tshuaj zoo inotropic.
Cov kev sim tsiaj thaum ntxov tau lees paub tias pimobedan tuaj yeem txhim kho cov kev ua haujlwm ntawm lub plawv hauv cov qauv canine plawv tsis ua haujlwm, xws li nce sab laug ventricular ejection feem (LVEF), txo qis sab laug ventricular kawg diastolic siab, thiab txo qis pulmonary thiab systemic vascular resistance. Cov kev tshawb fawb tshawb fawb no tau tsim lub hauv paus rau lawv cov kev siv tshuaj kho mob tom ntej.
2. Kev Siv Tshuaj Kho Mob thiab Kev Tshaj Tawm Txog Kev Tshaj Tawm (1999 tam sim no)
Nyob rau hauv 1999, Pimobedan tau pom zoo nyob rau hauv Teb chaws Europe rau kev kho mob ntawm congestive lub plawv tsis ua hauj lwm nyob rau hauv cov dev, kos nws official nkag mus rau hauv lub chaw kho mob daim ntawv thov theem. Nyob rau hauv thawj theem, nws tsuas yog tsom rau lub plawv tsis ua hauj lwm theem nrab rau dilated cardiomyopathy (DCM) thiab mob mitral valve insufficiency (CMVI). Los ntawm kev txhim kho myocardial contractility thiab txo qis ua ntej - thiab postcardiac load, nws ho txhim kho lub neej zoo thiab prognosis ntawm cov dev cuam tshuam.
Nrog rau qhov tob ntawm kev tshawb fawb soj ntsuam, cov cim qhia ntawm pimobedan tau maj mam nthuav mus suav nrog mucinous / degenerative mitral valve kab mob (MMVD / DMVD). Kev tshawb fawb tau pom tias cov tshuaj tuaj yeem txo qis lub nra ntawm sab laug ventricular tshwm sim los ntawm mitral valve insufficiency, txhim kho lub plawv dhia ua haujlwm, thiab ncua kev kis kab mob. Tsis tas li ntawd, pimobedan tau tshawb nrhiav rau kev cuam tshuam rau theem ua ntej lub plawv tsis ua haujlwm lossis lub plawv tsis ua haujlwm preclinical, nrog rau kev kho nrog angiotensin -hloov pauv enzyme inhibitors (ACEIs), txhawm rau txhim kho kev mob plawv ntxiv los ntawm ntau yam - lub hom phiaj ua haujlwm.
3. Kev txhim kho thiab kev tshawb fawb txog kev nyab xeeb (txij thaum pib ntawm lub xyoo pua 21st txog tam sim no)
Txhawm rau txhim kho cov tshuaj bioavailability thiab kev ua raws li tus neeg mob, daim ntawv ntau npaum li cas ntawm pimobedan yog qhov ua tau zoo tsis tu ncua. Tam sim no, feem ntau yog cov tshuaj ntsiav thiab ntsiav tshuaj nyob rau hauv kev ua lag luam, ntawm cov tshuaj ntsiav tuaj yeem txo cov kab mob plab hnyuv thiab txhim kho cov tshuaj stability. Cov zaub mov muaj feem cuam tshuam rau qhov ncauj bioavailability ntawm pimobedan, yog li nws raug nquahu kom muab nws rau ntawm lub plab khoob kom ntseeg tau tias muaj txiaj ntsig.
Cov kev tshawb fawb txog kev nyab xeeb tau pom tias pimobendn muaj tsawg dua qhov tsis zoo tshwm sim, feem ntau yog gastrointestinal intolerance. Txawm li cas los xij, cov tshuaj no yog contraindicated nyob rau hauv cov dev uas paub txog cov kab mob ntawm cov hlab ntsha tawg (xws li aortic valve stenosis) vim nws yuav ua rau cov tsos mob ntawm kev cuam tshuam. Tsis tas li ntawd, pimobedan tsis tau pom zoo siv rau hauv miv, thiab txawm hais tias qee qhov kev tshawb fawb rov qab tau pom tias muaj kev zam tau zoo hauv miv, tsis muaj pov thawj tseeb ntawm kev ua tau zoo.
Lub zeem muag yav tom ntej thiab cov lus qhia tshawb fawb
Nrog rau kev nkag siab tob txog cov txheej txheem ntawm kev ua ntawm pimobendn, kev tshawb fawb yav tom ntej yuav tsom mus rau nws cov peev txheej hauv kev cuam tshuam thaum ntxov ntawm cov kab mob plawv. Piv txwv li, tshawb txog qhov cuam tshuam ntawm pimobendn ntawm preclinical survival lub sij hawm nyob rau hauv cov dev nrog occult DCM los yog DMVD theem B2, nrog rau nws cov kev kho mob ua ke nrog lwm yam tshuaj. Tsis tas li ntawd, kev siv cov tshuab xa tshuaj tshiab xws li nanotechnology tuaj yeem txhim kho lub hom phiaj thiab bioavailability ntawm pimobendn, txo cov kev mob tshwm sim.
Kev ua lag luam thiab kev muag khoom
Manufacturers thiab muag khoom channel
Ua los ntawm ntau lub tuam txhab tshuaj, cov khoom lag luam los ntawm cov tuam txhab sib txawv tuaj yeem muaj qhov sib txawv ntawm qhov zoo, nqe, specifications, thiab lwm yam. Hauv txawv teb chaws, cov qauv tsim los ntawm cov tuam txhab xws li Boehringer Ingelheim muaj ntau dua. Nws yog muag los ntawm cov chaw xws li chaw kho tsiaj, tsev kho mob tsiaj, thiab cov chaw muag tshuaj.
Cov nqi lag luam thiab cov xwm txheej sib tw
Cov nqi lag luam sib txawv vim muaj ntau yam xws li cheeb tsam, chaw tsim khoom, specifications, thiab lwm yam. Hauv kev ua lag luam, muaj kev sib tw ntawm ntau hom kev muag khoom. Cov neeg siv khoom tuaj yeem xav txog lawv tus kheej cov kev xav tau thiab cov peev nyiaj thaum txiav txim siab, thaum tseem ua tib zoo xaiv cov kev cai raws cai los xyuas kom meej cov tshuaj zoo thiab kev nyab xeeb.
Kev Lag Luam Kev Lag Luam thiab Kev Pom Zoo
Nrog rau kev txhim kho tas mus li ntawm kev lag luam tsiaj thiab tib neeg txoj kev mloog zoo rau cov tsiaj noj qab haus huv, qhov tshwm sim ntawm cov kab mob plawv hauv cov dev kuj maj mam nce. Yog li ntawd, kev lag luam xav tau nyob rau hauv cov kws kho tsiaj yuav tsum tau nce ntxiv. Nyob rau hauv lub neej yav tom ntej, nrog kev nce qib ntawm kev siv tshuaj thev naus laus zis thiab kev sib sib zog nqus ntawm kev siv tshuaj kho mob, kev ua lag luam zeem muag ntawmPimobendan ntsiav tshuajyuav dav dua.
FAQ
1. Lub hom phiaj tseem ceeb ntawm Pimobendan (Pimobendan) capsules yog dab tsi?
Nws yog cov kws kho tsiaj (tsuas yog rau cov dev) tshuaj siv los kho mob plawv tsis ua hauj lwm los ntawm dilated cardiomyopathy (DMD) lossis degenerative mitral valve disease (MMVD). Nws txhim kho lub plawv ua haujlwm los ntawm kev txhim kho lub plawv contractility thiab dilating cov hlab ntsha.
2. Thaum twg cov tshuaj no yuav tsum pib lossis tso tseg?
Feem ntau, cov tshuaj no yog siv thaum tus dev pom cov tsos mob ntawm lub plawv tsis ua hauj lwm (xws li hnoos, ua tsis taus pa, thiab tsis ua haujlwm). Nws yuav tsum tau pib tom qab kuaj mob veterinary. Tsis txhob tso tshuaj rau koj tus kheej. Txhua qhov kev hloov kho lossis kev txiav tawm yuav tsum tau ua raws li tus kws kho tsiaj; txwv tsis pub, tus mob yuav deteriorate sai.
3. Dab tsi yog kev ceev faj tseem ceeb uas yuav tsum tau ua thaum siv tshuaj?
Nws yog ib qho tsim nyog yuav tsum tsis tu ncua saib xyuas lub raum ua haujlwm thiab lub plawv mob ntawm tus dev; nws tuaj yeem siv ua ke nrog lwm yam tshuaj (xws li diuretics, ACEI); cov tshuaj yuav tsum tau muab nruj me ntsis raws li cov tshuaj thiab lub sijhawm teem tseg (feem ntau yog noj ua ntej noj mov); saib xyuas cov kev mob tshwm sim xws li tsis qab los noj mov, raws plab lossis qaug zog thiab qhia rau tus kws kho tsiaj kom sai.
4. Yuav khaws cov tshuaj li cas?
Nws yuav tsum tau muab khaws cia rau hauv lub thawv kaw ntawm chav tsev kub (feem ntau pom zoo kom nyob nruab nrab ntawm 15-25 degree), nyob rau hauv qhov chaw qhuav thiab tsaus, tsis ncav cuag cov menyuam yaus thiab tsiaj txhu, thiab xyuas kom cov pob khoom tsis zoo.
Cim npe nrov: pimobendan capsule, lwm tus neeg, manufacturers, hoobkas, lag luam wholesale, yuav, nqe, tej, kev muag khoom