Misoprostol, lub teeb daj kua nplaum, tuaj yeem ua rau miscible nrog ethanol, ether lossis chloroform, thiab nyuaj rau yaj hauv dej lossis n-hexane. Nws yog ib qho derivative ntawm prostaglandin E1, uas muaj zog ntawm inhibiting gastric acid secretion thiab contractile nyhuv ntawm cev xeeb tub lub tsev menyuam. Tsis tas li ntawd, misoprostol muaj cov tshuaj pharmacological ntawm e-prostaglandins, uas tuaj yeem ua rau lub ncauj tsev menyuam mos, txhim kho uterine tension thiab intrauterine siab. Tam sim no, daim ntawv thov ua ntu zus ntawm mifepristone los txhawb kev ua haujlwm tau dhau los ua ib txoj hauv kev tseem ceeb rau kev ua haujlwm nruab nrab ntawm kev ua haujlwm. Nws tuaj yeem hloov cov kev phais zoo dua xws li forceps curettage thiab amniocentesis. Qhov kev ua tiav ntawm kev rho menyuam yog li 96.1 feem pua. Nws yog ib txoj hauv kev nyab xeeb thiab siv tau zoo rau induction ntawm kev ua haujlwm. Misoprostol yog thawj qhov chaw kho mob PGE (prostaglandin E) derivative, uas muaj cov txiaj ntsig zoo rau ntau yam mob (tshwj tsis yog duodenal ulcer). Txawm li cas los xij, nws tus nqi kuj kim heev. Tam sim no, nws feem ntau yog siv los ua cov tshuaj thib ob rau kev kho mob ntawm cov kab mob, feem ntau yog rau refractory ulcers lossis recurrent ulcers.
Artificial synthesis ntawm misoprostol: noj azelaic acid ua raw khoom, react nrog diimidazolyl sulfoxide los tsim imidazole acylation khoom, uas muaj zog acylation kev ua si. Tom qab reacting nrog monomethyl malonate, nws yog acidified thiab decarboxylated los tsim 2-[8- (methoxycarbonyl) octyl] methyl acetate, ces hydrolyzed thiab decarboxylated los tsim 8-oxo decanoic acid, cyclized thiab decarboxylated nrog dimethyl oxalate los tsim 3- hloov cyclopentatrione, Ib pawg carbonyl tau xaiv hydrogenated rau hydroxyl, thiab tom qab ntawd txo mus rau 4-hydroxy-2- (methyl heptanate-7- yl) { {7}}, 3-cyclopentenone tom qab cov tshuaj tiv thaiv nrog acetone acetal. Thaum kawg, misoprostol tau txais los ntawm cov tshuaj tiv thaiv nrog cov organic aluminium reagent.
Nws yog tsuas yog siv los ua thawj chemically synthesized prostaglandin E1 anti ulcer tshuaj. Nws muaj cov txiaj ntsig zoo ntawm inhibiting gastric acid secretion thiab tiv thaiv kev tsim kab mob. Cov kua qaub hauv plab uas tuaj yeem tiv thaiv tau suav nrog basal gastric acid secretion thiab gastric acid secretion tshwm sim los ntawm histamine pentagastrin, zaub mov lossis kas fes stimulation, thiab tuaj yeem txo cov kua qaub hauv plab thaum hmo ntuj. Nws yog thawj cov tshuaj tiv thaiv kab mob peptic ulcer siv hauv tsev kho mob. Nws yog qhov zoo tshaj rau cov receptor antagonists nyob rau hauv lub sij hawm ntev ulcer recurrence, tab sis tsis tshua muaj txiaj ntsig los txo qhov mob peptic rwj dua li Island receptor antagonists. Rau plab hnyuv thiab duodenal rwj, tshwj xeeb tshaj yog rau cov neeg mob uas tsis tshua muaj prostaglandin.
Hais txog kev paub txog tshuaj kho mob ntawm misoprostol, prostaglandins thiab lawv cov derivatives yog ib chav kawm ntawm cov tshuaj tiv thaiv kab mob peptic uas tau pom nyob rau hauv 20 xyoo tsis ntev los no thiab tau txais kev nyiam ntau ntxiv. Cov khoom no yog thawj derivative ntawm hluavtaws prostaglandin I nkag mus rau hauv tsev kho mob. Nws tau raug pov thawj tias muaj cov txiaj ntsig zoo ntawm inhibiting gastric acid secretion hauv cov tsiaj thiab tib neeg. Tom qab kev tswj hwm, cov kua txiv hmab txiv ntoo tso tawm thiab kua qaub tawm los ntawm basal gastric acid, histamine, gastrin thiab zaub mov stimulation tau txo qis, thiab cov protease excretion kuj txo. Txawm li cas los xij, cov txheej txheem ntawm kev ua haujlwm tseem tsis tau qhia meej, uas tej zaum yuav cuam tshuam nrog cov txiaj ntsig ntawm adenylate cyclase kev ua haujlwm ntawm cAMP theem ntawm parietal hlwb. Cov kev sim tsiaj kuj tau ua pov thawj tias nws tuaj yeem tiv thaiv kev tsim cov kab mob. Yog li ntawd, nws tau txiav txim siab tias cov khoom no muaj zog tiv thaiv cell tiv thaiv ntxiv rau inhibiting gastric acid secretion. Tsis tas li ntawd, cov khoom no kuj muaj cov tshuaj pharmacological ntawm e-prostaglandins, uas tuaj yeem ua rau lub ncauj tsev menyuam mos, txhim kho lub tsev menyuam thiab lub siab hauv lub cev. Kev siv sib txuas nrog mifepristone tuaj yeem ua rau muaj kev nce ntxiv thiab ua rau muaj ntau zaus thiab qhov loj ntawm kev ua haujlwm ntawm lub tsev menyuam thaum cev xeeb tub, uas tuaj yeem siv los tiv thaiv kev xeeb tub thaum ntxov. Nws cov kev phiv tsis zoo yog me dua li cov thioprostone thiab carboprost methyl ester, thiab nws yooj yim siv. Qhov ncauj nqus tau zoo. Tom qab noj ib koob tshuaj, Tmax yog 0.5 teev thiab tshem tawm ib nrab-lub neej yog 20-40 feeb. Cov plasma protein khi tus nqi yog 80 ~ 90 feem pua. Cov tshuaj concentration hauv daim siab, raum, plab hnyuv, plab thiab lwm yam ntaub so ntswg yog siab dua li cov ntshav. Tom qab kev tswj hwm qhov ncauj, kwv yees li 75 feem pua ntawm cov khoom uas sau nrog cov khoom siv hluav taws xob yog tawm los ntawm cov zis, li 15 feem pua yog tawm ntawm cov quav, thiab 56 feem pua ntawm cov zis tawm hauv 8 teev.
Kev paub txog tshuaj pharmacokinetics: misoprostol yog nqus tau sai los ntawm kev tswj qhov ncauj, thiab tuaj yeem nqus tau tag nrho tom qab 1.5 teev. Tom qab 15 feeb ntawm kev tswj qhov ncauj, cov ntshav plasma nquag metabolite misoprotoic acid mus txog qhov kawg. Kev tswj qhov ncauj ib leeg 200 μ g. Qhov nruab nrab siab tshaj plasma concentration yog 0.309 μg / L. Lub plasma protein khi tus nqi ntawm misoprostol yog 80 feem pua ~ 90 feem pua. Cov tshuaj concentration hauv daim siab, raum, plab hnyuv, plab thiab lwm yam ntaub so ntswg yog siab dua li cov ntshav. Kev tshem tawm ib nrab-lub neej ntawm misoprostol yog 20 ~ 40min, thiab nws yuav tsum noj txhua 12 teev rau 400 μ G misoprostol tsis suav nrog hauv vivo. Kwv yees li 75 feem pua ntawm misoprostol tau tawm hauv cov zis los ntawm lub raum thiab li ntawm 15 feem pua ntawm cov quav tom qab kev tswj qhov ncauj; Cov zis tawm hauv 8 teev yog 56 feem pua.
Cov kws tshaj lij cuam tshuam tau soj ntsuam cov khoom no. Misoprostol yog ib qho derivative ntawm prostaglandin E1, uas muaj cov nyhuv muaj zog ntawm inhibiting gastric acid secretion thiab muaj cov nyhuv contractile ntawm cev xeeb tub. Tsis tas li ntawd, misoprostol muaj cov tshuaj pharmacological ntawm e-prostaglandins, uas tuaj yeem ua rau lub ncauj tsev menyuam mos, txhim kho uterine tension thiab intrauterine siab. Tam sim no, daim ntawv thov ua ntu zus ntawm mifepristone los txhawb kev ua haujlwm tau dhau los ua ib txoj hauv kev tseem ceeb rau kev ua haujlwm nruab nrab ntawm kev ua haujlwm. Nws tuaj yeem hloov cov kev phais zoo dua xws li forceps curettage thiab amniocentesis. Qhov kev ua tiav ntawm kev rho menyuam yog li 96.1 feem pua. Nws yog ib txoj hauv kev nyab xeeb thiab siv tau zoo rau induction ntawm kev ua haujlwm. Misoprostol yog thawj qhov chaw kho mob PGE (prostaglandin E) derivative, uas muaj cov txiaj ntsig zoo rau ntau yam mob (tshwj tsis yog duodenal ulcer). Txawm li cas los xij, nws tus nqi kuj kim heev. Tam sim no, nws feem ntau yog siv los ua cov tshuaj thib ob rau kev kho mob ntawm cov kab mob, feem ntau yog rau refractory ulcers lossis recurrent ulcers.