Lidocaine Hmoov Rau Kev Tshuaj Ntsuam Xyuas Cas: 137-58-6

Nws yog dab tsi: The Crystalline Core

Lidocaine Hmoov tsis yog tsuas yog "av -}} dua lidocaine"; Nws yog lub huv, synthesized cov khoom xyaw ntawm cov tshuaj (API) hauv nws daim ntawv. Nws zoo nkaus li ib tug dawb kom tawm ntawm- dawb, tsw, crystalline hmoov. Qhov tseem ceeb, nws muaj nyob rau hauv nws daim foos freebase, txawv ntawm cov ntsev hydrochloride (Lidocaine HCl) feem ntau siv hauv kev txhaj tshuaj aqueous. Daim foos FreeBase yog:

● Lipophilic:Ntxim siab heev hauv lipids thiab cov kuab tshuaj organic, tab sis tsis zoo soluble hauv dej. Cov cuab yeej no yog qhov tseem ceeb rau nws lub peev xwm mus rau kev nkag mus rau hauv cov leeg.

● Lub hauv paus tsis muaj zog:Muaj pka nyob ib ncig ntawm 7.9. Qhov no sau tseg nws lub xeev ionization (thiab yog li nws lub peev xwm los thaiv cov ntsev sodium raws) raws li cov ntaub so ntswg.

● Polymorphic Muaj Peev Xwm:Zoo li ntau ntau cov khib nyiab crystalline, Lidocaine lub hauv paus tuaj yeem muaj nyob hauv kev sib txawv crystal kev sib txawv (polymorphs zoo} Kev ruaj khov thiab cov khoom muaj peev xwm tiv thaiv tau tuaj yeem cuam tshuam los ntawm polymorphism.

Hygroscopic:Nws muaj lub siab nyiam nqus noo ntawm huab cua, uas tuaj yeem cuam tshuam kev sib tua, kev ruaj khov, thiab sib sau ua ke. Txoj kev tswj hwm nruj ib puag ncig yog qhov tseem ceeb thaum lub sijhawm cia thiab ua.

 

 

Cov hmoov daim foos muaj cov cwj pwm tshwj xeeb thiab xav tau kev tuav ntaub ntawv tshwj xeeb:

● Cov ntsiab lus tsis zoo:Sawv cev cov ntshiab kom edthetic molecule ntawm siab tshaj plaws kev pom, ua rau muaj kev yoog tau yooj yim.

● Tsim Kom yooj yim:Lub pob zeb rau compound rau cov kws muag tshuaj thiab cov chaw tsim tshuaj lag luam. Nws tuaj yeem yaj nyob rau ntau cov kuab tshuaj (roj, dej cawv, glycerin) los tsim cov kev daws teeb meem customized, cov kua nplaum, tshuaj pleev, cov khoom noj. Nws yog qhov pib cov khoom rau kev tsim cov kev daws teeb meem (qhov chaw uas hloov pauv mus rau cov kua txiv ntoo rau cov dej solubility), tshuaj tsuag, thaj ua rau thaj, thiab ntsiav tshuaj, thiab ntsiav tshuaj.

● Muaj peev xwm (thaum daws tau zoo):Nyob rau hauv nws cov ntshiab, qhuav, crystalline lub xeev, tiv thaiv los ntawm lub teeb, thiab ntau dhau ntawm cov khoom siv tau zoo heev, feem ntau dhau ntawm cov khoom lag luam.

Rightling rhiab heev:Nws hygroscopic xwm yuav tsum tau ceevfulous fandling nyob rau hauv qis {{}} Cov hnab av noo) thaum lub sijhawm noo noo chaw lossis sib xyaw kom tiv thaiv kom tsis txhob muaj qhov hnyav, thiab tsis muaj peev xwm. Kev hu ncaj qha rau cov tawv nqaij yuav tsum zam.

● Lub luag haujlwm tseem ceeb hauv Ph Hloov Kho:Thaum tsim aqueous {{}}} based cov khoom zoo li gels me me ntawm cov kua qaub (xws li HCl) rau ib nrab hloov nws mus rau soluble hydrochloride ntsevnyob rau hauv situ, ua tiav qhov xav tau PHEM NTH (feem ntau 5.0 - 7.0) rau ob qho tib si ruaj ntseg thiab ua tau zoo. This careful balance optimizes the proportion of unionized (membrane-penetrating) and ionized (channel-blocking) forms.

Lidocaine ua haujlwm nyob rau theem siab tshaj plaws ntawm neuronal kos npe: Voltage {{mate} gated sodium channel (VGSC). Nws ua raws li asiv -} kavlossisXeev -} kavKev thaiv.

In Unional Unional Penetation:Hauv nws daim ntawv teev npe (feem ntau ntawm lub physiological PH), lipophilic lidocaine thov kev hloov los ntawm cov hlab ntaws ntawm cov hlab ntaws ntawm cov hlab ntaws.

● ● ionized blockade:Sab hauv ntawm tes, ntawm qhov qis me ntsis intracellular ph, feem tseem ceeb ua ionized (zoo them). Daim ntawv cationic no khi nrog high affinity rau ib tug tshwj xeeb receptor chawnyob hauvVGSC thaum cov channel nyob rau hauv nws qhib lossis inactivated xeev (piv txwv li, thaum lub sijhawm ua haujlwm).

Filling Jam:Qhov no khi lub cev thaiv cov channel pore, tiv thaiv kev kub ntawm sodium ntawm sodium ntawm theem (na) uas yog qhov muaj peev xwm.

Dais Halt:Yog tias tsis muaj txaus na + influx, qhov kev txiav txim siab yuav tsis propagate raws cov leeg fiber ntau. Qhov kev txwv no tau thim rov qab thiab nyiam me me, tsis muaj ntsej muag ({{{{4} Lub cev muaj zog), piav qhia cov xwm txheej ntawm kev xav ntawm cov kev ploj (mob ua ntej, ces kov, ces kev muaj nuj nqi).

Thaum cov hnub nyoog hauv Hidocaine HCL yog iconic, hmoov versatility ua rau ntau cov ntaub ntawv ntawm cov ntawv thov:

● Cov kev daws teeb meem (ntawm cov ntsev tsim):Thawj qhov kev siv. Hmoov yog yaj thiab reased nrog hydrochloric acid los ua lub ruaj khov, thiab ntim rau infiltration, cov pob zeb, cov kab mob epidural, thiab lwm yam.

Lum suav cov ntsiab lus npaj tseg:

○ High -}}} concent concent concent concent concent concent concent concent concent concent concent (OG, 5-10%):Txog kev mob mucosal loj (qhov ncauj qhov ncauj, cov tshuaj esophagitis), shingles (phn), lossis raws li cov txheej txheem pretreatment rau cov txheej txheem rab koob.

○ Cov tsheb coj mus kuaj:DUAB nyob rau hauv lipophilic bases (roj av) rau lub tsho luv luv lossis tshwj xeeb (piv txwv li, urethalstalce).

Muchodhesive Tsim Qauv:Rau lub caij nyoog ntev hauv zos ntawm qhov ncauj, chaw mos, lossis lub ntsuas hluav taws.

○ Spyarary Daim Ntawv Thov:Cov qauv kev cai rau cov tawv nqaij, pob ntseg, lossis cov txheej txheem kev xav tau hauv cov tsiaj.

Chaw Tsim Tshuaj Topicals:Hmoov yog tus API qhov chaw rau cov tshuaj pleev ua lag luam / piv txwv (piv txwv li, 5%), thaj ua rau thaj (lidoderm, tshuaj tsuag, thiab cov kev daws teeb meem.

● Npaj hniav:Siv nyob rau hauv cov kev tsim cov tshuaj loog rau kev ua kom zoo nkauj rau gingiva thiab muaj cov txheej txheem kho hniav.

● Cov kev daws teeb meem ophthalmic (cov tshuaj tsis tshua muaj):Rau cov txheej txheem me me hauv pob kws lossis tshuaj loog ntev (yuav tsum muaj kev ua kom muaj zog thiab tsis muaj tub txuv).

● Muaj cov ntawv thov:Siv me me ua ib qho anti - arrhythmic nyob rau hauv cov kev ua haujlwm IV (txawm tias siv rau kev tshawb fawb), thiab siv tshwj xeeb rau kev tshawb fawb.

Lidocaine lub dominance stems los ntawm cov khoom haum zoo tsim tau ntau xyoo lawm:

● Ceev xwm ceev:Ua tau zoo lub hlab ntsha javade nrawm nrawm piv rau cov laus zoo li propaine.

● Nruab Nrab Nruab Nrab Duration:Muab cov sijhawm txaus (1-2 teev rau infiltration, ntev dua rau cov hlab ntsha nrog Vasoconstrictor) rau ntau cov txheej txheem tsis muaj ntau dhau heev.

● Versatility:Zoo los ntawm yuav luag txhua txoj kev (infiltration, leeg thaiv, epidural, txha caj qaum, cov txuj ci, IV). (* Cov qauv tshwj xeeb / lub hom phiaj).

● Kev txhim khu kev muaj kev nyab xeeb txog kev nyab xeeb (thaum siv kom tsim nyog):Cov kev paub match thiab zoo {- sotioning toxicology (feem ntau cns thiab flasiovascular).

● Vasodilatory cov khoom:Kev nqus dej me me vasodation ids systemic kev nqus tab sis kuj tseem siv tau} Cov thawj coj}}} kev nqus kom haum nyob rau hauv ntau cov xwm txheej.

Assetial Methabolic Zoo Tshaj:Feem ntau metabolized hepatically los ntawm cyp1a2 thiab cyp3A4 kom nquag plias (megx) thiab tsis muaj zog ntxiv) ua rau cov neeg mob atypical pseudocholinesterase.

Tus nqi - ua tau zoo:Kuj pheej yig pheej yig los tsim cov nplai.

● Kev siv tshuaj (kev xav tseem ceeb rau cov hmoov): Lidocaine hmoov tsis tau muab ncaj qha rau cov neeg mob.Noj tshuaj yog ib txwm txiav txim siabtom qabNws tau raug hnyav thiab koom nrog rau qhov tshwj xeeb, qauv qauv. Kev noj tshuaj nyob ntawm:

Formal kawg:Kev txhaj tshuaj (mg / kg, nrog max koob), cov ntsiab lus (% concentration, cheeb tsam / sijhawm), thaj (mg / thaj).

○ Txoj Kev Tswj Xyuas:Infiltration Vs. Epidgural thiab cov ntsiab lus.

Tus Neeg Mob Lub Siab:Qhov hnyav, hnub nyoog, hepatic / renal muaj nuj nqi, comorbidities (piv txwv, lub plawv tsis ua haujlwm), tib cov tshuaj tsis ua haujlwm), tib cov tshuaj tsis ua haujlwm), tib cov tshuaj tsis ua haujlwm), tib cov tshuaj tsis ua haujlwm), thooj txhij cov tshuaj tsis ua haujlwm), thooj txhij cov tshuaj tsis ua haujlwm), tib cov tshuaj tsis ua haujlwm), thooj txhij txhua yam tshuaj.

○ Muaj cov vasoconstrictor:Epinephrine tau txo qis cov kev nqus cov kab ke, tso cai rau cov koob tshuaj zoo dua hauv zos.

Qhov kev xav tau zoo tshaj plaws koob tshuaj (MRD):Txoj kev txwv nruj ib txwm muaj (piv txwv li, 4.5 mg / kg nrog EPI rau kev noj qab haus huv cov neeg laus} Tab sis yeej ib txwm sab cov lus qhia tam sim no / cov txheej txheem tshiab).Kev sib xyaw ua ke los ntawm cov hmoov tsis yog - kev sib ceg rau tus neeg mob kev nyab xeeb.

Er "voj voog" tswvyim:Lidocaine nws tus kheej tsis yog feem ntau "cycled" zoo li kev ua haujlwm -} kev txhim kho yeeb tshuaj. Nws cov kev cuam tshuam yog kev hloov pauv thiab cov txheej txheem - nyob. Txawm li cas los xij, hauv cov ntsiab lus li tswj hwm mob Lo lus tsis yog tshuaj yuav cuam tshuam rau lidocaine thawj qhov kev ua kom loog.

Ib nrab - lub neej (try):Hais txog kev tshem tawm ib nrab - lub neej los ntawm cov kev ncigtom qabkev nqus.

Ot ○ Lub davhlau ya nres ib nrab - lub neej:Kwv yees li 1.5 txog 2 teev rau cov neeg laus uas muaj kev ua haujlwm hepatic qub.

Cov ntsiab lus cuam tshuam ib nrab - lub neej:

◇ Cov Ntshav Ntshav Hepatic Flow & Ua Haujlwm:Txoj kev loj ntawm cov metabolism (CYP450). Txo cov dej ntws (piv txwv li, lub plawv tsis ua hauj lwm) lossis tsis muaj zog (piv txwv li, kev sib tw ntawm kev phom sij try thiab nce kev phom sij. Megx, ib qho kev nquag siv metabolite, tseem muaj CNS teebmeem thiab nrawm dua T½ (~ 2-3 teev).

Protein khi:Lidocaine yog cov protein me ntsis - bars (60-80%, feem ntau yog rau AAG). Kev hloov pauv ntawm kev khi (piv txwv li cov av nplaum tsawg, siab AAG hauv kev ntxhov siab) cuam tshuam rau kev siv tshuaj dawb, muaj feem xyuam tshuaj.

Subletion:Tsuas yog kwv yees li 10% ntawm kev hloov pauv Lidocaine thiab 80% ntawm cov metabolites yog excreted renally. Kev puas siab txog kev tsis pom kev tsis pom kev zoo ib txwm muaj rau cov metabolite ntxiv (txawm tias tsawg dua li qhov tsis txaus siab hepatic tsis zoo).

◇ Kev Sib Tham Yeeb Tshuaj:CYP1A2 / 3A4 inibitors (piv txwv li, Cimetidine, fluVoxine, qee cov beta- blockers) nce lidocaine qib. Taw qhia tej zaum yuav txo qib. Beta - blockers kuj txo cov ntshav hepatic.

Tus thawj cov kev pheej hmoo kav los ntawmSystemic nqus tau tshaj lithabolic muaj peev xwm, ua rau cov ntshav siab ntshav siab. Kev lom zem Kev lom neeg manifests ua ntu zus:

1.Centtral Nervous system (Cns):Thaum Ntxov Cov Yeeb Yam Thaum Ntxov - Lub teb chaws} Kev txiav txim siab ntawm lub ntsej muag, tinnitus, ligredusness, tsaug zog. Kev nce qib rau kev ntxhov siab, cov leeg mus sib tw, tshee, ntxhov siab, ntxhov siab, tsis meej pem hais lus. Kev lom zem heev ua rau qaug txeeb, fa, ua pa kev kev txom nyem / raug ntes.

2.Cardiovascular system (CVS):Pib kev txaus siab (kev kub siab, tachycardia - Feem ntau npog tau los ntawm Epi). Tom qab ntawd, kev nyuaj siab ncaj qha Dominction Dominates: Bradycardia, Conduction qeeb (PR / QRS lub caij nyoog), vt, vf), asystole. Lidocaine suppresses tsis siv neeg thiab qeeb qeeb.

Tshuaj lom neeg:Kev nqus tau cov hmoov tuaj yeem ua rau ua pa pheeb suab. Daim tawv nqaij tiv tauj, tshwj xeeb tshaj yog lub sijhawm ntev los yog nrog tawv nqaij pom, tuaj yeem ua rau muaj kev nqus tau zoo thiab muaj kev cuam tshuam hauv zos (loog). Kev noj khoom yog qhov txaus ntshai heev.

Compounding tsis raug:Qhov tsis muaj tseeb (vim yog hygroscopicity lossis tib neeg yuam kev) tuaj yeem ua rau dastically dhau {{{{{concentrated formulations, ua rau muaj kev lom zem lossis kho tsis tau. Cov menyuam cev ua txhaum cai thaum lub sijhawm sib xyaw rau cov tshuaj tiv thaiv tau tuaj yeem ua rau kis tau tus mob.

● Tawm ntawm - daim ntawv lo / undonupvised siv:Muaj peev xwm rau kev siv tsis ncaj vim siv tau (tab sis tswj hwm), ua rau LDL hnyav, nce qib siab, muaj ntau yam) roj (zoo) cov roj (zoo)

Kev Lag Luam Npe	Lidocaine, xylocaine, ztlido, lignocaine
Cas	137-58-6
Tus hniav loj	234.343
Cov lus ntawm ib txoj kab ke	C14H22N2O
Kev coj dawb huv	Saum toj no 98%
Kev tsim nyog	Dawb crystalline hmoov

 

 

Kev xav tau, thov hu rau peb

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Lidocaine hmoov dhau deb tshaj li ib qho tseem ceeb; Nws yog qhov tseem ceeb crystalline corestalline enterabling cov hluav taws xob kho hluav taws xob ntawm lidocaine. Nws lipophilic freebase spine qhia nws cov tshuab ntawm kev ua thiab tsim nyog ua tib zoo ua yeeb yam los ntawm nws cov txiaj ntsig kev nyab xeeb. Nws lub luag haujlwm hauv compounding tso cai rau cov tshuaj kho tus kheej, sib sau cov khoob hauv cov khoom lag luam muaj. Txawm li cas los xij, nws cov kev xav tau zoo heev. Meticulous kov cov qauv, cov qauv sib xyaw ua ke, nruj dua cov lus qhia yog tsis tiv thaiv cov kev mob phem. Los ntawm kev tsim khoom cog rau cov lab, Lidocaine hmoov tseem muaj qhov tseem ceeb, cov cuab yeej muaj zog heev rau ntau lab tus lej ua haujlwm thaum daws nws cov lus txib. Nws txoj kev ua txhaum cai qub txeeg qub teg yog ua rau lub hauv paus ntawm kev ua kom nkag siab ntawm cov tshuaj thiab tsis muaj kev cog lus rau kev nyab xeeb.

Cim npe nrov: Lidocaine Hmoov Rau Kev Tshuaj Ntsuam Rau Kev Tshuaj Ntsuam Xyuas Cas: 137-58-6, Tuam Tshoj Lidocaine Hmoov Rau Anesthetics Cas: 137-58-6 Cov Chaw Tsim Tshuaj, Chaw Tsim Tshuaj, Hoobkas