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Brexanolone

Rating: Māhele:

Product Description

Nā ʻano kikoʻī

Product Name Brexanolone
Kāleka CAS 516-54-1
Ka Lā Molecular C21H34O2
Kaumaha Kaumaha 318.501
'O Synonyms Allopregnanolone

Brexanolone

516-54-1

ʻO Allotetrahydroprogesterone

Allopregnan-3alpha-ol-20-one

Keʻano ʻO ka pauma
Ka mālama a me ka lima lima Maloʻo, ʻeleʻele a ma 0 - 4 C no ka wā pōkole (mau lā a i mau pule) a -20 C no ka wā lōʻihi (mahina i mau makahiki) ..

 

Hōʻike Brexanolone

He ʻano ʻokoʻa ʻo Brexanolone, lawelawe intravenous, neuroactive steroidal antidepressant i hoʻohana ʻia i ka therapy of depressive postpartum moder-to-parah. I nā hoʻokolohua hoʻokolohua prelicensure, ʻaʻole pili ka brexanolone therapy me ka piʻi nui o nā kiʻekiʻe aminotransferase serum, a ʻaʻole i hoʻopili ʻia i nā hanana o ka hōʻeha ʻeha o ke ake maʻi.

ʻO Brexanolone kekahi 3-hydroxy-5alpha-pregnan-20-hoʻokahi kahi i loaʻa ai i ka hui hydroxy ma ke kūlana 3 ka alpha-configuration. He metabolite ia o ka progesterone hormone sex a hoʻohana ʻia no ka mālama ʻana i ke kaumaha postpartum i nā wahine. He kuleana kona e like me ka metabolite kanaka, kahi antidepressant, kahi modulator GABA, kahi anesthetic intravenous a me kahi mea hoʻohiamoe.

 

ʻO Brexanolone Hana Hana

ʻAʻoleʻike piha ʻia ka mīkini o ka hana o brexanolone. ʻO Brexanolone kahi hana aqueous o allopregnanolone. ʻO Allopregnanolone kahi metabolite nui o ka progesterone. Ke piʻi mau nei nā pae o ka allopregnanolone me ka progesterone i ka wā hāpai me ka kiʻekiʻe loa i ke kolu o ka trimester. ʻO Allopregnanolone kahi steroid neuroactive endogenous ikaika e hoʻololi i ka neuronal excitability ma o ka maikaʻi allosteric modulation ma ka synaptic a me extrasynaptic gamma-aminobutyric acid (GABA) type A mau mea loaʻa. ʻO ka extrasynaptic GABA type A nā mea loaʻa i waena i ka hoʻoliʻiliʻi tonic e hoʻohālikelike i ka hana a allopregnanolone ke hoʻohālikelike ʻia i nā benzodiazepines nāna e hoʻopili i ka pāpā phasic ma nā GABA type A ʻelima.

 

Noi Brexanolone

ʻO Brexanolone ka lāʻau mua i ʻae ʻia e ka US FDA kikoʻī no ka mālama ʻana i ke kaumaha postpartum (PPD) i nā wahine makua. ʻOiai ʻo PPD, e like me nā ʻano kaumaha ʻē aʻe, ʻike ʻia e nā manaʻo kaumaha, waiwai ʻole a hewa ʻole paha, hōʻino noʻonoʻo, a / a i ʻole manaʻo ideic suicidal, manaʻo ʻia he ola weliweli ia. No laila ua ʻike ʻia nā noiʻi ʻana he hiki i ka PPD ke loaʻa nā hopena maikaʻi ʻole i ka hoʻopaʻa makuahine a me ka ulu ʻana o ke keiki ma hope. ʻO ka hoʻomohala ʻana a me ka loaʻa o ka brexanolone no ka mālama ʻana o PPD i nā wahine makua a laila hāʻawi i kahi lāʻau hou a hoʻohiki hoʻi ma kahi o ka poʻe i noho ma mua. ʻO ka mea nui, ʻo ka hoʻohana ʻana o brexanolone i ka mālama ʻana iā PPD ua hoʻopuni ʻia me ka hoʻohiki no ka mea hana ia ma ke ʻāpana ma ke ʻano he supplement synthetic no nā hemahema i loko o ka brexanolone endogenous (allopregnanolone) i nā wahine postpartum maʻalahi i ka PPD akā ʻo ka nui o nā lāʻau anti-depressive i hoʻohana pinepine ʻia e hana i nā hana i hiki hoʻololi i ke alo a me ka hana o nā mea e like me serotonin, norepinephrine, a me / a i ʻole monoamine oxidase akā ʻaʻole e hoʻopili i nā hana e pili pono me PPD e like me nā fluctuations kūlohelohe i nā pae o nā endogenous neuroactive steroid e like me allopregnanolone. A ʻo ka mea hope loa, ʻoiai ʻo brexanolone paha e hoʻokolokolo ʻia nei i nā hoʻokolohua hoʻokolohua e noiʻi ai i kona mau hiki ke mālama i ka kūlana epilepticus kūlana kiʻekiʻe, ʻike ʻia ua kūleʻa ʻole kekahi mau ʻano ʻano e like me nā kikoʻī mua e hoʻohālikelike i ka kūleʻa o ka weaning o nā ʻaoʻao laina kolu a me ka hoʻonā ʻana o ka mea hiki. ke kūlana weliweli ola epilepticus me brexanolone vs. placebo ke hoʻohui ʻia i ka mālama maʻamau.

 

Nā hopena a me nā ʻōlelo aʻoaʻo a Brexanolone

Hoʻolaʻa nui ʻia ʻo Brexanolone e nā ala he nui a pēlā paha ʻaʻole e loaʻa nā launa lāʻau lāʻau nui. ʻO CYP2C9 wale nō ka enzyme cytochrome P450 i hōʻike ʻia e kāohi ʻia e ka brexanolone i nā noiʻi in vitro. ʻAʻole hiki i kahi noiʻi pili pilikino hōʻike e hōʻike i nā loli i ka pharmacokinetics ke coadministred ka brexanolone me phenytoin, kahi substrate CYP2C9. Hōʻike ʻia ka haʻahaʻa o ka hōʻino no ka haʻahaʻa, e like me ka hōʻike ʻole ʻia e nā ʻokoʻa i nā hōʻike kumumanaʻo i hoʻohālikelike ʻia me placebo. Ma nā ʻōlelo e pili ana i ka hopena o ka hōʻino hepatic a me ka hōʻino ma nā lāʻau lapaʻau, ʻaʻohe hoʻololi o ka hoʻomanawanui ʻana i nā mea maʻi me ka maʻi kaulike a koʻikoʻi i ka ate, a ʻaʻohe pono e hoʻoponopono ʻia no ka maʻi maʻi puʻuwai. Eia nō naʻe, hiki i ka ʻākena solubilizing SBECD ke hōʻiliʻili i nā mea maʻi me ka hōʻeha koʻikoʻi koʻikoʻi, a no laila ʻaʻole e hāʻawi ʻia ka brexanolone i nā mea maʻi me ka maʻi hōʻeha hope loa.

 

Reference

[1] Meltzer-Brody S, Colquhoun H, Riesenberg R, et al.: Brexanolone injection i loko o ke kaumaha post-partum: ʻelua multicentre, pālua makapō, hoʻokolohua ʻia, placebo-kāohi ʻia, pae hoʻāʻo 3. Lancet 2018; 392: 1058-1070 Crossref, Nānā ma Google.

[2] Luke DR, Tomaszewski K, Damle B, et al .: Nānā i ka lāʻau a me ka lāʻau lapaʻau o ka sulfobutylether-beta-cyclodextrin (SBECD). ʻO J Pharm Sci 2010; 99: 3291-3301 Crossref, Nānā ma Google.

[3] Brexanolone Injection, no ka Hoʻohana Intravenous: Palapala Hoʻolaha Hoʻolaha Kākoʻo. ʻO Cambridge, Mass, Sage Therapeutics, Kōmike Aʻoaʻo Hoʻohālikelike Laulaha Psychopharmacologic a me ka palekana palekana lāʻau a me ka palekana palekana a me ka hālāwai mālama palekana, Nov 2, 2018. Google Scholar.

[4] Luisi S, Petraglia F, Benedetto C, Nappi RE, Bernardi F, Fadalti M, Reis FM, Luisi M, Genazzani AR. Nā pae allopregnanolone serum i nā wahine hāpai: nā loli i ka wā hāpai, i ka wā hānau, a i nā mea maʻi hypertensive. ʻO J Clin Endocrinol Metab. 2000 Jul; 85 (7): 2429-33. [Hoʻokuʻuʻia].

[5] Paul SM, Purdy RH. ʻO nā steroid neuroactive. FASEB J. 1992 Mar; 6 (6): 2311-22. [PubMed].

[6] Farrant M, Nusser Z. Nā ʻano like ʻole ma ke kumumanaʻo kaohi: phasic a me ka tonic activation o GABA (A) mau mea loaʻa. Nat Rev Neurosci. 2005 Malaki; 6 (3): 215-29. [PubMed].

[7] ʻO Johannsen BM, Larsen JT, Laursen TM, Bergink V, Meltzer-Brody S, Munk-Olsen T. All-Cause Mortality ma nā Wahine Me nā maʻi psychiatric postpartum koʻikoʻi. ʻO Am J Psychiatry. 2016 Jun 01; 173 (6): 635-42. [PMC puke kūmole] [PubMed].

[8] Noorlander Y, Bergink V, van den Berg MP. ʻIke a nānā ʻia i ka pilina makuahine a me nā keiki i ka manawa o ka haukapila a hoʻokuʻu ʻia i ke kaumaha postpartum a me ka psychosis. ʻO Arch Womens Ment Health. 2008; 11 (1): 49-56. [PubMed].


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