Loperamide hmoov CAS 53179-11-6

Loperamide hmoov, tseem hu ua loperamide hydrochloride thiab lopharma, yog ib qho dawb los yog quasi dawb hmoov tshuaj. Lub npe tshuaj: 4-p-chlorobenzene-4-hydroxy-n, N-dimethyl- , - Diphenyl-1-p-piperidinybutylamide, cov mis mos molecular yog c29h33cln2o2, thiab qhov hnyav molecular yog 477.03800. Loperamide yog cov tshuaj tiv thaiv kab mob ntev ntev. Clinically, nws tsuas yog kho mob raws plab thiab mob raws plab tshwm sim los ntawm ntau yam ua rau, tshwj xeeb tshaj yog haum rau kev kho mob raws sij hawm ntev.

Synthetic loperamide:

1. Nrog Diphenylacetonitrile ua raw khoom, nws reacts nrog ethylene oxide nyob rau hauv lub xub ntiag ntawm sodium amino, hydrolyzes nrog hydrochloric acid, qhib lub nplhaib nrog 48% HBr HAC ntawm chav tsev kub, thiab condenses nrog 4-p-chlorophenyl{{ 4}}hydroxypiperidine nyob rau hauv muaj methyl isobutyl ketone thiab sodium carbonate los tsim loperamide. Tag nrho cov txiaj ntsig yog 13.4% raws li Diphenylacetonitrile.

2. Tom qab cov tshuaj tiv thaiv ntawm Diphenylacetonitrile (I) thiab sodium amino, ethylene oxide yog qhia ntawm 5 ~ 10 degree . Tom qab dhau mus, cov tshuaj tiv thaiv tau nqa tawm ntawm chav tsev kub tom qab kev txuag hluav taws xob, thiab cov khoom sib xyaw (II) tau txais nrog cov txiaj ntsig ntawm 66%. Ntxiv 36% glacial acetic acid tov ntawm hydrogen bromide rau compound (I) thiab do ntawm 25 ~ 30 degree. Lim thiab ntxuav nrog dej rau pH 5. Cov tshuaj (ⅲ) tau los ntawm kev ziab nrog cov txiaj ntsig ntawm 88%. Compound (III) yog chlorinated nrog thionyl chloride rau compound (IV) hauv 95% tawm los. Compound (IV) thiab sodium carbonate yog yaj hauv toluene thiab dej, thiab dimethylamine yog qhia ntawm 0 ~ 5 degree rau kev txuag hluav taws xob. Cov dej txheej yog muab rho tawm nrog chloroform thiab cov extract yog concentrated. Cov residue tau recrystallized nrog methyl isobutyl ketone kom tau cov compound (V) nyob rau hauv ib tug yield ntawm 56%. Compound (V), compound (VI), sodium carbonate thiab potassium iodide yog yaj hauv methyl isobutyl ketone thiab dehydrated los ntawm reflux. Rov qab cov kuab tshuaj nyob rau hauv lub siab txo, ntxiv isopropanol rau cua sov thiab yaj cov residue, hla lub alumina kem ntawm 40 degree, decolorize thiab lim, thiab ntxiv hydrogen chloride isopropanol tov rau pH nqi 3. Nws tau txias rau 5 degree, lim thiab crystallized. , ntxuav nrog isopropanol rau pH 6, thiab lub tshuab nqus tsev qhuav kom qhov hnyav tas li ntawm 80 degree kom tau txais Loperamide, nrog cov txiaj ntsig ntawm 58%

Cov khoom kawg ntawm cov tshuaj no tsuas yog rau cov nyhuv ntawm txoj hnyuv du, uas tuaj yeem cuam tshuam qhov kev cog lus ntawm txoj hnyuv du thiab txo txoj hnyuv peristalsis. Nyob rau tib lub sijhawm, nws tuaj yeem txo cov neurotransmitters tso tawm los ntawm cov paj hlwb ntawm txoj hnyuv thiab ncaj qha inhibit peristaltic reflex. Thiab cov tshuaj tuaj yeem ua kom ntev lub sijhawm nyob ntawm cov zaub mov hauv cov hnyuv, txhawb kev nqus dej, electrolyte thiab qabzib, yog li nws kuj muaj txiaj ntsig zoo rau cov kab mob zais zis. Txawm li cas los xij, cov tshuaj no tsis haum rau kev kis kab mob raws plab, uas yog, thaum muaj kab mob tshwm sim, raws plab nyob rau lub sijhawm no yog kev tiv thaiv ntawm lub cev. Yog hais tias ntau dhau inhibition ntawm raws plab, nws yuav ua rau aggravation ntawm o thiab txawm kub taub hau.

Pharmacological teebmeem: Cov qauv tshuaj ntawmLoperamide hmoovzoo ib yam li haloperidol thiab pethidine, tab sis cov tshuaj kho tsis muaj kev cuam tshuam rau hauv nruab nrab paj hlwb. Cov nyhuv ntawm txoj hnyuv du yog zoo ib yam li cov tshuaj opioid thiab difenoxate, uas tuaj yeem cuam tshuam kev ua haujlwm ntawm txoj hnyuv du thiab txo txoj hnyuv peristalsis. Nws tseem tuaj yeem txo qhov tso tawm ntawm acetylcholine los ntawm txoj hnyuv phab ntsa ntawm cov hlab ntsha thiab ncaj qha inhibit peristaltic reflex los ntawm kev sib cuam tshuam hauv zos ntawm cholinergic thiab non cholinergic neurons. Cov khoom no tuaj yeem ua rau lub sijhawm nyob ntawm cov zaub mov hauv cov hnyuv me, txhawb kev nqus dej, electrolytes, thiab qabzib, thiab cuam tshuam cov plab hnyuv siab los ntawm prostaglandins, cholera toxins, thiab lwm yam enterotoxins, tab sis cov tshuaj kho tsis cuam tshuam rau lub plab zom mov. secretion ntawm gastric acid. Cov khoom no tuaj yeem ua rau kom qhov nro ntawm qhov quav dilator cov leeg, yog li suppressing fecal incontinence thiab ceev ceev.

Pharmacokinetics: Cov khoom no tau yooj yim absorbed los ntawm lub plab hnyuv phab ntsa, thiab yuav luag tag nrho cov ntawm nws nkag mus rau lub siab metabolism. Vim nws cov affinity siab rau lub plab hnyuv phab ntsa thiab "thawj dhau metabolism", nws hardly nkag mus rau hauv cov hlab ntsha system. Cov ntshav concentration ntawm cov tshuaj tiv thaiv yog qis heev, thiab qhov siab tshaj plaws ntawm cov ntshav ntshav yog 5 teev tom qab kev tswj hwm qhov ncauj ntawm cov tshuaj ntsiav. Cov nyhuv kav ntev dua 24 teev. T1/2 yog 10.8h ntawm qhov nruab nrab. Cov protein khi tus nqi yog 97%. Excretion los ntawm bile thiab quav. Kev tso tawm hauv cov zis tso nyiaj txog li 5% - 10%.

1. Loperamide (Yimongting)
Mechanism ntawm kev ua:Loperamide feem ntau ua raws li tus neeg sawv cev tiv thaiv kab mob los ntawm kev khi rau txoj hnyuv opioid receptors, ua rau lub plab zom mov qeeb thiab ua kom lub sijhawm khaws cia ntawm cov hnyuv.
Kev ruaj ntseg:

• Ntawm cov koob tshuaj pom zoo, loperamide yog ib qho tshuaj tiv thaiv kab mob zoo.
• Txawm li cas los xij, ntau tshaj qhov pom zoo yuav ua rau muaj teeb meem loj, suav nrog arrhythmia hnyav thiab tuag. Tshwj xeeb tshaj yog nyob rau hauv cov xwm txheej ntawm txhob txwm yuam kev lossis tsim txom, qhov kev pheej hmoo siab dua.
• Loperamide kuj tseem tuaj yeem ua rau muaj kev cuam tshuam hauv nruab nrab xws li qaug zog, kiv taub hau, ua pa qeeb lossis ua pa sab nraud, nrog rau kev tsis zoo xws li cem quav.
• Kev siv ntev ntev yuav ua rau muaj kev vam khom.

teeb meem xav tau kev saib xyuas:

• Ua raws li cov lus qhia siv tshuaj nruj me ntsis ntawm daim ntawv xaj lossis cov lus qhia.
• Tsis txhob siv nws ua ke nrog lwm cov tshuaj uas yuav ua rau cem quav.
• Yog tias cov tsos mob hnyav xws li qaug zog, lub plawv dhia ceev, lossis lub plawv dhia tsis zoo, nrhiav kev kho mob tam sim ntawd.

2.Montmorillonite hmoov
Mechanism ntawm kev ua:Montmorillonite hmoov tsuas yog inhibits thiab tshem tawm cov kab mob, kab mob, thiab lawv cov co toxins los ntawm kev nkag mus rau hauv lub plab zom mov, thaum tiv thaiv lub plab hnyuv mucosa, ua tiav cov txiaj ntsig ntawm kev tso tseg raws plab.
Kev ruaj ntseg:

• Montmorillonite hmoov muaj cov txiaj ntsig zoo los tiv thaiv kev mob raws plab thiab qee qhov kev mob tshwm sim.
• Qhov tshwm sim tseem ceeb yog cem quav, tab sis feem ntau yog mob me.
• Montmorillonite hmoov tsis tshua nkag mus rau hauv cov hlab ntsha, yog li nws qhov cuam tshuam rau tag nrho lub cev kuj me me.

teeb meem xav tau kev saib xyuas:

• Ua raws li cov lus qhia tshuaj ntawm tus kws kho mob cov lus qhia lossis cov lus qhia.
• Thaum mob raws plab, kev noj zaub mov yuav tsum yog lub teeb kom tsis txhob muaj cov tsos mob raws plab.

3.kev sib piv

• Kev nyab xeeb:Raws li kev noj tshuaj kom raug, kev nyab xeeb ntawm montmorillonite hmoov yog qhov siab, nrog kev mob me me thiab tsis tshua muaj tshwm sim; Txawm hais tias loperamide muaj cov tshuaj tiv thaiv kab mob zoo, muaj kev pheej hmoo ntawm kev tsim txom uas yuav ua rau muaj kev phom sij loj.
• Cov pej xeem siv tau:montmorillonite hmoov yog tsim rau cov neeg mob uas muaj mob raws plab los ntawm txoj hnyuv microbiota; Loperamide yog qhov tsim nyog rau kev mob raws plab los ntawm mob hnyav thiab mob ntev.
• Cov lus qhia tshuaj:Thaum xaiv cov tshuaj tiv thaiv kab mob, kev xaiv yuav tsum ua raws li tus neeg mob qhov tshwj xeeb thiab tus kws kho mob cov lus qhia. Rau kev mob raws plab los ntawm kev cuam tshuam plab hnyuv microbiota, montmorillonite hmoov yuav tsim nyog dua; Rau kev mob raws plab los ntawm mob hnyav thiab mob ntev, loperamide tuaj yeem ua tau zoo dua. Txawm li cas los xij, tsis hais cov tshuaj twg yog siv, kev ua raws li cov lus qhia kho mob lossis cov lus qhia yuav tsum ua raws li kev noj qab haus huv ntawm cov tshuaj.

1.Txoj kev khaws cia thiab khaws cia

2.Lwm yam tshuaj ceev faj

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