Pharmacological teebmeem ntawm Aniracetam
Racitant-zoo li lub hlwb cell metabolizing tshuaj
Aniracetam, tseem hu ua aniracetam, belongs rau cov chav kawm racetam ntawm hlwb cell metabolizing tshuaj nrog rau piracetam thiab nafetilacetam. Cov chav kawm ntawm cov tshuaj no pab txhawb kev ua haujlwm ntawm neuronal intrasynaptic phospholipase thiab nce kev tsim thiab thauj ntawm ATP hauv lub hlwb, nce cov protein thiab RNA synthesis, txhawb nqa lub hlwb kev siv cov amino acids, phospholipids, qabzib thiab oxygen, thiab ua rau tus neeg mob muaj kev cuam tshuam, excitability thiab nco. . Aniracetam muaj cov teebmeem zoo dua li piracetam thiab cov teebmeem me me.
Pharmacological teebmeem
Aniracetam yog ib tug cyclized derivative ntawm -aminobutyric acid, uas yog ib lub hlwb kev ua hauj lwm tshuaj. Nws tuaj yeem xaiv ua haujlwm ntawm lub hauv nruab nrab paj hlwb los ntawm cov ntshav-hlwb barrier. Nws muaj cov nyhuv activating ntawm lub hlwb cell metabolism thiab tiv thaiv cov paj hlwb. Nws tseem tuaj yeem tsim cov txiaj ntsig kev txawj ntse los ntawm kev cuam tshuam rau glutamate receptor system. Nws kuj tseem txhim kho cortical tsis kam rau hypoxia thiab tiv thaiv kev kawm thiab kev nco tsis txaus los ntawm ntau yam tshuaj, hypercapnia, scopolamine lossis electroshock. Nws tsis muaj sedative lossis stimulant nyhuv, thiab tsis muaj vasodilator nyhuv. Tsiaj thwmsim tau ua pov thawj tias cov khoom no muaj kev txhawb nqa zoo ntawm cov txheej txheem kev tsim cov cim xeeb ntawm kev ntxub ntxaug kev kawm hauv cov nas ib txwm muaj, tuaj yeem tiv thaiv hypoxia vim tsis nco qab, thiab tuaj yeem txhim kho kev nco tsis zoo los ntawm qee yam laj thawj.
Cov lus qhia
Clinically siv rau kev kho mob ntawm me me thiab nruab nrab kev kawm, nco thiab kev txawj ntse dysfunction ntawm vascular dementia thiab Alzheimer's kab mob. Nws kuj tseem siv tau rau kev nco qab mob stroke, kev nco tsis zoo hauv cov neeg laus thiab cov neeg laus, thiab cov menyuam yaus uas muaj lub hlwb qeeb.
Pharmacokinetics
Cov ntaub ntawv qhia tias cov tshuaj tau nqus sai sai tom qab kev tswj hwm qhov ncauj hauv cov nas, nrog rau cov ntshav siab tshaj plaws hauv 20-40 feeb. Cov tshuaj feem ntau yog muab faib rau hauv plab hnyuv, raum, siab, hlwb thiab ntshav, thiab tom qab 24 teev, 77 feem pua -85 feem pua yog tawm hauv cov zis thiab 4 feem pua ntawm cov quav. Lub ntsiab metabolites hauv cov zis yog: Np-methoxybenzoylaminobutyric acid thiab 5-hydroxy-2-pyrrolidinone. Tib neeg: Tom qab nqus qhov ncauj, tshem tawm ib nrab-lub neej ntawm cov tshuaj qub hauv cov ntshav yog 20-30 feeb ntawm qhov nruab nrab, thiab cov ntshav siab yog qhov nyuaj rau ntsuas tom qab 2 teev.
Kev phiv tshuaj
Cov kev phiv tshuaj tsis tshua muaj tshwm sim, qee zaus lub qhov ncauj qhuav, anorexia, cem quav, kiv taub hau, tsaug zog, ploj tom qab tsis siv tshuaj.
Cov kev ceev faj
(1) Cov koob tshuaj yuav tsum tau hloov kho kom tsim nyog nyob rau hauv lub xub ntiag ntawm lub siab ua haujlwm txawv txav.
(2) Cov khoom no tuaj yeem ua rau cov tsos mob ntawm Huntington's chorea.
(3) Cov khoom no yog contraindicated nyob rau hauv cov neeg mob uas tsis haum rau nws los yog leej twg tsis tuaj yeem zam lwm yam tshuaj pyrrolidone.
(4) Kev pom zoo siv ntau yam kev nyab xeeb ntawm cov khoom no yog 0.3 ~ 1.8g / d.
Cov khoom siv tshuaj
Crystallized from ethanol, melting point 12l～122℃. Acute toxicity LD50 rats, mice (mg/kg): about 4500, >5000 lus.
Siv
Aniracetam yog ib tug derivative ntawm piracetam, uas yog ib tug -lactone Nws muaj peev xwm hla cov ntshav-hlwb barrier thiab ua xaiv ntawm lub hauv paus paj hlwb thiab lub paj hlwb cov ntaub so ntswg los txhim kho lub hlwb ua hauj lwm thiab nco, thiab muaj kev ua hauj lwm ntawm kev txhawb thiab txhawb kev nco. Piv nrog rau piracetam, nws muaj qhov zoo ntawm kev ua kom muaj zog, pib ua haujlwm sai thiab tsis muaj tshuaj lom. Tsiaj thwmsim tau ua pov thawj tias nws muaj kev txhawb nqa zoo ntawm cov txheej txheem kev tsim cov cim xeeb ntawm kev ntxub ntxaug hauv cov nas ib txwm muaj, tuaj yeem tiv thaiv kev nco tsis tau los ntawm hypoxia, thiab tuaj yeem txhim kho kev nco tsis zoo los ntawm qee yam laj thawj. Nws yog siv nyob rau hauv kev kho mob ntawm senile dementia, nco tsis tau tom qab cerebrovascular kab mob thiab nco poob nyob rau hauv nruab nrab thiab laus laus.
