Methylergonovine Malaste ntsevyog ib qho orgaline alkaline compound nrog molecular mis c20h24n2O2 B4H6O4, CAS 57432-61-8. Nws yog cov hmoov dawb lossis zoo sib xws dawb crystalline, thiab nws daim ntawv ua lead ua feem ntau prismatic lossis kem. Nws yog insoluble nyob rau hauv dej thiab yooj yim soluble hauv cov kuab tshuaj muaj kuab yam xws li ethanol, chloroform, benethen, thiab ether. Kev txiav txim siab tshwm sim ntawm kev kub, thiab cov khoom tseem ceeb suav nrog nitrogen, carbon monoxide, carbon dioxide, thiab dej. Nws yog ib qho isomer muab rho tawm cov noob ntawm cov genus datura Stramonium thiab muaj ntau roj ntsha, xws li analgesic, anti ntxhov siab, thiab kev ntxhov siab tiv thaiv, thiab kev ntxhov siab tiv thaiv, thiab kev ntxhov siab rau kev ntxhov siab. Nws yog Ergot alkaloid, ib qho metabolite nquag ntawm cov methyl ergot alkaloid, nrog vasoconsliction thiab Uterine feem cuam tshuam. Methyl malate yog qhov tsim nyog xaiv 5-HT Receptor kev thaiv kev thaiv kev thaiv nrog qhov ncauj ua si thiab PA2 tus nqi ntawm 9.6. Methylergudrine morate muaj anti migraine thiab dopaminerity kev ua si, uas tuaj yeem siv los tiv thaiv thiab tswj cov hemorrhatum.
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Tshuaj Cov Qauv |
C24H29N3O6 |
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Muaj pes tsawg leej |
455 |
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Molecular hnyav |
455 |
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m/z |
455 (100.0%), 456 (26.0%), 457 (2.7%), 457 |
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Kev Ntsuam Xyuas |
C, 63.28; H, 6.42; N, 9.23; O, 21.07 |
Cov hauv qab no yog cov khoom tsom ntaub ntawv:
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Methylergudrine mantice, raws li ib qho kev siv tshuaj alkaloids, tau dhau los ua nws lub ntsej muag tshwj xeeb, thiab kev qhia dav dav vim nws tau tshwm sim thaum nws rov tshwm sim hauv nruab nrab-20th caug xyoo. Nws ncaj qha txhim kho Uterine Fwv dej los ntawm kev txhawb nqa alpha adculatory thiab serotoninestion du leeg, thiab vascular system.
1. Kev Tiv Thaiv thiab Kev Kho Mob Tom Qab Kev Kawm Ntawv Hnem
Tom qab hemorum yog qhov ua rau muaj kev ua kom tuag ntawm niam txiv neej ntiaj teb thoob ntiaj teb, nrog kwv yees li 80% tshwm sim los ntawm uterine atony. Methylergline Marate ncaj qha ua rau uterine du cov leeg nqaij, ua rau cov hlab ntshav maj mam txav ntawm cov hlab ntshav ntawm cov hlab ntsha.
Kev tiv thaiv kev tiv thaiv: txhaj tshuaj tiv thaiv 0.2mg intramuscularly tam sim ntawd tom qab kev xa khoom me me tuaj yeem txo cov oxytocin ib leeg), thiab tsis muaj qhov sib txawv ntawm qhov tshwm sim ntawm cov xwm txheej tsis zoo.
Kho siv tshuaj: Rau kev tawm tsam tawv ncauj uas tsis muaj txiaj ntsig nrog oxytocin, dilutedous thiab maj mam thawb) tuaj yeem siv sijhawm li 30 feeb thiab ntev li 45 feeb. Yog tias tsim nyog, rov hais dua txhua 2-4 teev, txog 5 zaug.
XIM: Tsis txhob siv ua ntej xa cov me nyuam hauv plab, txwv tsis pub nws yuav ua rau uterine rigidity thiab condaction, ua rau mob plab hypoxia lossis intracranial hemorrhage.
2. Ua tsis tiav uterine involution tom qab kev nchuav menyuam
Tom qab kev rho menyuam tawm lossis kev rho menyuam tawm, cov kev mob plab tsis muaj zog yuav ua rau cov nqaij uas tsis tshua muaj ntshav cia thiab ntshav. Methyllolesgoline malaste txhawb kev mob plab thiab ua kom nrawm nrawm ntawm cov ntsiab lus uterine.
Txoj kev tshawb fawb nrog 300 tus neeg mob uas muaj kev nchuav menyuam thaum ntxov ntawm kev tawm tsam ntawm Uterine los ntawm 65%, thaum txo lub sijhawm ntawm qhov chaw mos los los ntawm qhov nruab nrab ntawm 2.3 hnub.
4. Kev kho mob rau kev coj khaub ncaws ntau dhau
Rau cov neeg mob uas antovulatory dysfunctional uterine los ntshav (dub), utterometrine maleas tuaj yeem txo cov kev tswj hwm ntawm kev tswj hwm Uterine du cov leeg. Kev tswj hwm ntawm qhov ncauj ntawm 0.2mg ob zaug hauv ib hnub rau 5 hnub sib law liag tuaj yeem ua rau muaj kev sib law los ntawm 40% -50%, tshwj xeeb yog rau kev kho mob hauv kev kho hormone.
Kev Kho Mob Tshwj Xeeb: Hla rau kev rau txim thov los ntawm Migraine kom cov plab muaj kev tsis sib haum xeeb
1. Mob raum kho mob ntawm migraine
Methylergonovine Malaste ntsevMalaste xaiv tau 5-hydroxyptamine 2a receptors ntawm intracranial leeg leeg hlwb, ua rau vasoconscular thiab undeviating migraine cov tsos mob tshwm sim los ntawm kev nce intracranial siab. Nws cov kev ua tau zoo yog qhov tseem ceeb tshaj plaws hauv cov neeg mob migraine nrog aura: cov kev tswj hwm kev txhaj tshuaj ntawm 0.2%, ntau dua li cov pab pawg placebo (35%).
CEEV FAJ: Kev siv ntev yuav ua rau tshuaj noj mob taub hau (moh), thiab nws raug nquahu kom siv ntau tshaj 9 hnub hauv ib hlis.
2.Qhov kev ua kom muaj kev kub ntxhov
Cov tshuaj no ua rau cov roj ntsha ua kom muaj zog los ntawm kev ua haujlwm zoo ntawm acetylipe ntawm cov leeg plab zom mov
Kev phais mob ncej puab tes tuag taw tes dag zog: peb zaug ib hnub twg yuav tsum tau phais mob plab (rau nruab nrab 1.5 hnub dhau los) thiab txo qhov muaj kev cuam tshuam ntawm txoj hnyuv.
Ntshav qab zib Gastroparesis: ua ke nrog domperidone, lub sij hawm pas lub plab zom mov tuaj yeem ua kom luv los ntawm 120 feeb, txhim kho cov tsos mob ntawm lub xeev siab thiab ntuav.
Mechanism: los ntawm kev txhawb nqa dopamine receptors hauv nruab nrab lub paj hlwb, nws tsis ncaj inhibits vagal laus.
3. Kev pab ntawm kev mob siab
Methyllolesgoline malate tuaj yeem ua ncaj qha rau ntawm 5-hydroxyptamine receptors nyob rau saum npoo ntawm cov leeg nqaij hlwb, inhibit calcium ion Incium, thiab txo cov kev ua kom zoo nkauj. Rau ureteral spasms tshwm sim los ntawm lub raum pob zeb, intramuscular txhaj tshuaj ntawm 0.2mg tuaj yeem txo cov qhab nia muaj mob (vas) los ntawm 8 txog rau 3 teev. Cov nyhuv yog piv rau cov phloroglucinol tab sis siv cov nyhuv sai.
1. Synergistic nyhuv nrog oxytocin
Hauv kev kho mob ntawm tus menyuam kawm ntawv hemorrhats, kev sib xyaw ntawm 0.2 mg intramuscular txhaj tshuaj ntawm oxytocin tuaj yeem tsim cov txiaj ntsig kev sib xyaw ua ke. Kev kawm multicenter qhia tau hais tias kev sib xyaw ua ke pab pawg muaj 29% txo qis hauv Postpartum 24-teev los tiv thaiv rau Oxytocin Group ib leeg (P<0.01), and the hysterectomy rate decreased from 1.2% to 0.3%.
Mechanism: Oxytocin feem ntau ua rau lub cev lub cev, thaum Ergometrine Marets muaj qhov muaj zog zuj zus ntawm lub tsev menyuam yaus, thiab ob qho kev sib txuam kom npog tag nrho cov meterus.
2. Kev ceev faj kev kho nrog cov tshuaj prostaglandin
Txog kev ua yeeb yam tom tsev kawm ntawv Postpartum Txawm li cas los xij, nws yuav tsum tau sau tseg tias:
Both have strong vasoconstrictive effects and may cause severe hypertension (systolic blood pressure>180mmhg), yuav tsum tau saib xyuas cov ntshav siab.
Thaum siv ua ke, koob tshuaj ntawm ergergometrine malate yuav tsum tau halved (0.1mg intramuscular txhaj tshuaj) kom txo qis kev pheej hmoo ntawm cov xwm txheej plawv.
3. Kev cuam tshuam nrog tshuaj tua kab mob antihpertive
Alpha adrenergic recenter agonistic nyhuv ntawm ugharety malate tej zaum yuav ua rau muaj kev sib xyaw nrog cov tshuaj tua kab mob xws li antihervertensive thiab labetalol thiab labetalol thiab labetalol thiab Labetalol thiab Labetalol thiab Labetalol thiab Labetalol. Piv txwv li, hauv kev kho mob ntawm kev kawm ntawv hemorrhats hauv herpertensive niam, yog tias siv ntawm nifedipine yuav tsum tau suav los ntawm 30mg / hnub, thiab ntshav siab yuav tsum tau saib xyuas txhua 30 feeb.
Kev npaj ntawm cov khoom lag luam:
Weigh og ntawm crude methylergudrine malatee, 25g ntawm ethanol mus rau 250ml cov koob tshuaj tiv thaiv cab, thiab ua kom sov}℃c rau kev sib cais; Ntxiv 0.5 g ntawm cov av nplaum kom tau ua kom muaj 30 feeb, ua kom cov methees ua kom txias rau 5 xyoos, thiab qhuav} g, tawm los 73%.
Npaj ntawm methylegretrine maraeate compound:
Hnyav ibog me me Methylergine MarEmol thiab 450g ntawm ethanol mus rau 1000} Whe} lawv mus txog 70℃C txog rau kev sib cais; Ntxiv 2G ntawm cov av nplaum uas muaj cov av nplaum, do rau 30}}℃rau qhov ua kom txias rau {} g, tawm los 69%.
Npaj ntawm methylegretrine maraeate compound:
Hnyav ibog me me Methylergine methanol thiab 175g ntawm ethanol mus rau 250ml cov tshuaj tiv thaiv flask, thiab ua kom sov} kev ua kom sov rau 650℃c rau kev sib cais; Ntxiv 0. 75 g ntawm cov av nplaum ua kom txias, do lub lim kom txias rau 0 degree.
Synthesis txoj kev ntawmMethylergonovine Malaste ntsevyog raws li nram no:
Ua ntej tshaj, ergolometrine thiab methyl metacrylate tau siv tau estrenified nyob rau hauv catalyy cawv thiab alkali kom tau txais methylpropenyfration erryonretrine.
6-methyl-8-bromoergonamine tau los ntawm reacting methyloplep decate nrog txhuas trichloride hauv dichhlorometide hauv Dichhloromshane.
Cov tshuaj tiv thaiv ntawm 6-methyl-8-bromoergotine thiab ethyl acetate hauv sodium aqueque aquee daws 6-methyl-8-ethyl acetate ethroty uretate ergotine.
6-methyl-8-phenol repometrine tau npaj los ntawm reergting 6-methyl-8-ethyl acetate apium hydrocide aque kua.
6-Methyl-8-Phenol Errylate tau npaj los ntawm reacting 6-Methyl-8-phenol Ergesine nrog Acrylic Anhydride hauv acetone.
Cov tshuaj tiv thaiv ntawm 6-methyl-8-phenol ergotamine acrylate acrylate thiab ergot acid hauv ethanol kom tau txais methylergotamine Andronate.
Qhov no yog cov xwm txheej yooj yim ntawm methylergotamine Andronate, tej zaum yuav muaj ntau cov kev coj ua ntau yam los yog cov tshuaj tiv thaiv saum toj no yuav raug hloov kho.
Ib txoj kev rau kev npaj methylergotamine milate compound yog tus cwj pwm hauv qab no: cua sov cov kuab tshuaj ua rau hauv qab no: nplawm, nplawm, thiab lim; Qhov filtrate yog txias thiab crystallized, sib cais, thiab ziab, thiab ziab kom tau txais cov crystal daim me me ntawm methylergotamine milate.
Npaj ntawm nws compound:
Hnyav ibog ntawm crude methylergudrine malatee, 30g ntawm ethanol mus rau 250ml kev soj ntsuam flakk nyob rau hauv lem, thiab ua kom sov lawv mus rau 60℃C txog rau kev sib nrauj; Ntxiv iG cov av nplaum, do rau 30 feeb, siv cov lim dej kom txias rau (TC kom qhuav, thiab muab cov metyl
Cov khoom plig ntawmMethylergonovine Malaste ntsev:
Thermal Stability:
Mega muaj qhov zoo thermal stability nyob rau hauv cov xwm txheej qhuav, tab sis nws yooj yim rau decompose hauv qab huab cua.
Acid - Base Stability:
MamquagonandronandronAronate yog qhov sib luag nyob rau hauv acidic thiab nruab nrab kev mob, tab sis nws yooj yim rau decompose hauv qab cov kev mob alkaline muaj zog.
Photostility:
Mam medhageergonandronArronate tsis ruaj khov rau lub teeb thiab yooj yim rau photodegrade.
Oxidation -}} Cov cuab yeej kom txo qis:
Meth -MandronArronArronate yog Redox rhiab rhiab compound, uas yog yooj yim cuam tshuam los ntawm redox cov tshuaj tiv thaiv.
Nws yog cov tshuaj feem ntau siv los kho tus cwj pwm tom qab yug menyuam thiab cov uterine dystrophy. Cov hauv qab no yog nws cov tshuaj lom neeg:
Dissociability:
Methylergotamine thiab Androgenic acid tuaj yeem sib cais rau hauv methylergiatamine thiab Androgenic acid hauv dej.
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Carboxylic Acid Rauv:
Methylergotamine Andronate muaj cov pab pawg carboxyl, uas tuaj yeem siv qhov kev tawm tsam esterification, acidolysis tiv thaiv, thiab lwm yam.
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Electrophilic hloov cov cai lij choj:
Muaj ib tug ortho hydrogen atom rau ntawm phenylpropyl amino pab pawg hauv methylergotamine andronate hloov cov tshuaj tiv thaiv, xws li alkylation thiab arylation.
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Txo cov tshuaj tiv thaiv:
Methylergotamine tuaj yeem txo rau methylergotamine los ntawm kev tawm tsam txo.
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Nws yog cov tshuaj feem ntau siv los kho tus cwj pwm tom qab yug menyuam thiab cov uterine dystrophy. Hauv qab no yog nws cov yam ntxwv pharmaciinetic:
Kev nqus:
Tom qab cov thawj coj ntawm qhov ncauj, methylenergotandronate tuaj yeem nqus tau nyob rau hauv lub plab zom mov, nrog cov xyoob ntoo, nrog cov xyoob ntoo muaj txiaj ntsig ntawm 60-70%. Kev nqus tau tus nqi nqus yuav nrawm dua thaum siv tshuaj los ntawm lwm txoj kev (xws li kev txhaj tshuaj tsis zoo nkauj).
01
Faib:
Meth -MonArdronArronArronArronate tuaj yeem dhau los ntawm cov txheej txheem ntawm kev placental, tab sis kev faib tawm hauv cov mis nyuj yog tseem tsis meej. Cov tshuaj feem ntau yog muab faib rau daim siab, mob ntsws, raum thiab tsev menyuam.
02
Metabolism:
Methylergotandronate Undergoes Hydroxylation thiab demethylation nyob rau hauv daim siab, thiab nws cov metabolation yog feem ntau methylergotamine thiab methylergotamine thiab methylergotamine.
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Excretion:
Methylergotandronate yog feem ntau yog excreted los ntawm daim siab thiab lub raum, thiab lub ntsiab metabolites raug ua tiav los ntawm lub raum yog hydroxymethyllolamine thiab hydroxymethylabotamotamotamine.
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Pharmacyamics:
Mam li cas meantabgonandronAronate feem ntau ua tau kev pab ua haujlwm thiab cov menyuam yaus ntawm lub hom phiaj ntawm kev kho cov leeg nqaij daim tawv nqaij ntawm kev kho mob tom qab yug menyuam.
05
Methylergonovine Malaste ntsevyog ib semi - cua phryetic ergonovine analogue, txhim kho lub hom phiaj ntawm kev kho mob plab, yog li ua kom tiav lub hom phiaj ntawm kev kho mob tom qab kev hem lub ntsej muag thiab uterine dystrophy. Hauv qab no yog nws cov yam ntxwv ntawm cov tshuaj paporological:
1. Mechanism ntawm Kev Ua: MinequaronArdronate Ua rau ntawm uterine du cov leeg thiab 5-hydrourgic recenor thiab 5-hydrourgic recenor thiab 5-hydrourgic cov hlab ntshav, yog li txo cov ntshav siab tom qab.
2. Kws muag tshuaj: Mega tuaj yeem nce cov nro thiab qhov ntau ntawm uterine du leeg, yog li txo tus mob tom qab. Ntawm cov poj niam tau dhau los ntawm cov chaw ua noj Cesarean, Mega tuaj yeem txo qhov tshwm sim los ntshav, tshwj xeeb tshaj yog thaum poj niam muaj kev pheej hmoo, xws li muaj mob, Etratraurine, thiab lwm yam.
3. Pharmacokinetics: Tom qab cov thawj coj ntawm qhov ncauj, methylergotandronate tuaj yeem nqus tau nyob rau hauv lub plab zom mov, nrog cov kab mob ntawm 60-70%. Kev nqus tau tus nqi nqus yuav nrawm dua thaum siv tshuaj los ntawm lwm txoj kev (xws li kev txhaj tshuaj tsis zoo nkauj). Cov tshuaj feem ntau yog muab faib rau daim siab, mob ntsws, lub raum, tsev menyuam thiab lwm cov ntaub so ntswg hauv lub cev, thiab yog feem ntau yog ua rau lub siab thiab lub raum.
4. Cov tshuaj tiv thaiv zoo no: MamthergonArdronate tuaj yeem ua rau cov ntshav siab xws li arhythmia, thiab kev lom zem Epidermal Necroly (kaum), mob ntsws.
Cim npe nrov: Methylergonovine Malaste ntsev CAS 57432-61-8, cov neeg muag khoom, chaw tsim khoom, chaw tsim khoom, yuav khoom, khoom, rau muag