Brexanolone (516-54-1) foda - Maƙerin Maƙerin Masana'antu
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Brexanolone

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Samfur Description

Abubuwa Na Asali

Product Name Brexanolone
CAS Number 516-54-1
kwayoyin Formula C21H34O2
Formula Weight 318.501
nufin abu ɗaya ne Allopregnanolone

Brexanolone

516-54-1

Allotetrahydroprogesterone

Allopregnan-3alpha-ol-20-daya

Appearance White foda
Ajiye da kulawa Dry, duhu kuma a 0 - 4 C don gajere (kwanaki zuwa makonni) ko -20 C na dogon lokaci (watanni zuwa shekaru) ..

 

Bayanin Brexanolone

Brexanolone na musamman ne, ana gudanar da shi ta hanyar intanet, wanda ake amfani da shi a cikin cututtukan steroidal wanda ake amfani dashi a cikin maganin matsanancin matsanancin halin haihuwa. A cikin gwajin gwaji na asibiti, maganin brexanolone ba shi da alaƙa da haɓakar haɓakar magani aminotransferase, kuma ba a haɗa shi da lokuttan cutar hanta mai saurin bayyana ba.

Brexanolone kuma shine 3-hydroxy-5alpha-pregnan-20-daya wanda rukunin hydroxy a matsayi na 3 yake da tsarin alpha. Amfani ne na homonin jima'i na progesterone kuma ana amfani dashi don maganin baƙin ciki na haihuwa bayan mata. Yana da rawa azaman motsa jiki na mutum, mai kwantar da hankali, mai ba da damar GABA, mai maganin sa cikin ciki da na kwantar da hankali.

 

Tsarin Brexanolone na Aiki

Hanyar aiwatar da brexanolone ba ta da cikakkiyar masaniya. Brexanolone sigar mai ruwa-ruwa ne na allopregnanolone. Allopregnanolone shine babban maye gurbin progesterone. Matakan allopregnanolone na ci gaba da tashi tare da progesterone yayin daukar ciki tare da mafi girma a cikin watanni uku. Allopregnanolone mai ƙarfi ne, mai cike da ƙwayoyin cuta wanda ke canza haɓakar neuronal ta hanyar haɓakar allo mai kyau akan synaptic da extrasynaptic gamma-aminobutyric acid (GABA) nau'in masu karɓar A. Masu karɓar nau'ikan GABA mai ɗauke da ƙwayar cuta suna ƙaddamar da haɓaka tonic wanda ya sa tsarin allopregnanolone ya zama na musamman idan aka kwatanta shi da benzodiazepines waɗanda ke yin sulhu kan ɓarkewar ƙwayar cuta a GABA type A receptors.

 

Brexanolone Aikace-aikace

Brexanolone shine magani na farko da FDA ta Amurka ta taɓa yarda dashi musamman don maganin baƙin ciki bayan haihuwa (PPD) a cikin matan da suka manyanta. Tunda PPD, kamar sauran nau'o'in baƙin ciki, yana tattare da baƙin ciki, rashin amfani ko laifi, raunin hankali, da / ko yuwuwar kashe kansa, ana ɗaukarsa halin haɗari na rai. Karatuttuka sun gano cewa PPD na iya haifar da tasirin gaske game da alaƙar jarirai da kuma ci gaban jarirai daga baya. Haɓakawa da wadatar brexanolone don kula da PPD a cikin matan da suka girma daga baya ya ba da sabon magani mai fa'ida inda ƙalilan suka kasance a da. Musamman, yin amfani da brexanolone wajen magance PPD yana kewaye da alƙawari saboda yana aiki a wani ɓangare azaman ƙarin haɗin roba don yiwuwar rashi a cikin ƙyamar brexanolone (allopregnanolone) a cikin matan da suka haihu mai saukin kamuwa da PPD yayin da yawancin magungunan da ake amfani da su don magance cututtukan ciki suna nuna ayyukan da zasu iya tsara kasancewar da ayyukan abubuwa kamar serotonin, norepinephrine, da / ko monoamine oxidase amma kada ku sasanta ayyukan da suka shafi kai tsaye tare da PPD kamar sauye-sauyen yanayi a cikin matakan cututtukan cututtukan ƙwayoyin cuta marasa ƙarfi kamar allopregnanolone. Kuma a ƙarshe, kodayake brexanolone na iya fuskantar gwaji na asibiti don bincika iyawarta don magance matsanancin hali na rashin lafiya, ya bayyana cewa wasu irin waɗannan karatun sun kasa cimma matsaya na farko waɗanda ke kwatanta nasara a cikin yaye wakilan jamiái na uku da ƙudurin yiwuwar Matsayi mai barazanar rai tare da brexanolone vs. placebo lokacin da aka kara shi zuwa daidaitaccen kulawa.

 

Brexanolone Side Gurbin & Gargadi

Brexanolone yana haɓaka ta hanyoyi da yawa don haka yana da wuya ya sami mahimman hulɗar miyagun ƙwayoyi da miyagun ƙwayoyi. CYP2C9 shine kawai enzyme cytochrome P450 wanda ya nuna cewa an hana shi ta hanyar brexanolone a cikin nazarin in vitro. Nazarin hulɗar hulɗar asibiti ya kasa nuna kowane canje-canje a cikin ilimin kimiyyar magani lokacin da aka haɗa brexanolone tare da phenytoin, samfurin CYP2C9. Hakanan an nuna yiwuwar cin zarafin ya zama ƙarami, kamar yadda yake bayyane ta hanyar babu bambance-bambance a cikin rahotanni na kai tsaye idan aka kwatanta da placebo. Dangane da tasirin cututtukan hanta da na koda a kan magunguna, babu canje-canje a cikin haƙuri a cikin marasa lafiya da ke fama da cutar hanta mai matsakaici zuwa mai tsanani, kuma babu wani gyare-gyaren kashi da ya zama dole don cutar koda mai tsanani. Koyaya, wakilin warware matsalar SBECD na iya tarawa a cikin marasa lafiya mai fama da larurar koda, saboda haka bai kamata a ba brexanolone ga marasa lafiya masu fama da cutar koda ta ƙarshe ba.

 

reference

[1] Meltzer-Brody S, Colquhoun H, Riesenberg R, et al.: Allurar Brexanolone a cikin damuwar bayan-bangare: biyu da yawa, makafi biyu, bazuwar, sarrafa wuribo, gwaji na 3 lokaci. Lancet 2018; 392: 1058-1070 Crossref, Google masani.

[2] Luke DR, Tomaszewski K, Damle B, et al.: Bincike na asali da kuma maganin asibiti na sulfobutylether-beta-cyclodextrin (SBECD). J Pharm Sci 2010; 99: 3291-3301 Crossref, Google masani.

[3] Allurar Brexanolone, don Amfani da Hanji: Takardar Takaitaccen Taimako. Cambridge, Mass, Sage Therapeutics, Psychopharmacologic Kwamitin Ba da Shawara kan Magunguna da Tsaro na Lafiya da Tsaro da Haɗarin Haɗarin Hadarin, Nov 2, 2018. Google masani.

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[6] Farrant M, Nusser Z. Bambancin akan maudu'in hanawa: juyawa da kunnawa na masu karɓar GABA (A). Nat Rev Neurosci. 2005 Mar; 6 (3): 215-29. [PubMed].

[7] Johannsen BM, Larsen JT, Laursen TM, Bergink V, Meltzer-Brody S, Munk-Olsen T. Dukan-Dalilin Mutuwar Mata a cikin Matsanancin Matsanancin Rashin Lafiya na Haifa. Am J Zuciyar. 2016 Jun 01; 173 (6): 635-42. [Labarin PMC kyauta] [PubMed].

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