ଆଲୋପ୍ରେଗନାନୋଲୋନ

ଆଲୋପ୍ରେଗନାନୋଲୋନ
Clinical data
Trade names	Zulresso
Synonyms	Brexanolone; Allo; AlloP; SAGE-547; SGE-102; 5α-Pregnan-3α-ol-20-one; 5α-Pregnane-3α-ol-20-one; 3α-Hydroxy-5α-pregnan-20-one; 3α,5α-Tetrahydroprogesterone; 3α,5α-THP
AHFS/Drugs.com	monograph
MedlinePlus	a619037
data	US DailyMed: Brexanolone;
Pregnancy; category	US: N (Not classified yet) ; ;
Routes of; administration	Intravenous infusion
Legal status
Legal status	US: Schedule IV ;
Pharmacokinetic data
Bioavailability	Oral: <5%
Protein binding	>99%
Metabolism	Non-CYP450 (keto-reduction via aldo-keto reductases (AKR), glucuronidation via glucuronosyltransferases (UGT), sulfation via sulfotransferases (SULT))
Elimination half-life	9 hours
Excretion	Feces: 47%; Urine: 42%
Identifiers
	IUPAC name 1-[(3R,5S,8R,9S,10S,13S,14S,17S)-3-hydroxy-10,13-dimethyl-2,3,4,5,6,7,8,9,11,12,14,15,16,17-tetradecahydro-1H-cyclopenta[a]phenanthren-17-yl]ethanone;
Chemical and physical data
Formula	C21H34O2
Molar mass	୩୧୮.୫0 g·mol−1
3D model (JSmol)	Interactive image;
	SMILES CC(=O)[C@H]1CC[C@@H]2[C@@]1(CC[C@H]3[C@H]2CC[C@@H]4[C@@]3(CC[C@H](C4)O)C)C;
	InChI InChI=1S/C21H34O2/c1-13(22)17-6-7-18-16-5-4-14-12-15(23)8-10-20(14,2)19(16)9-11-21(17,18)3/h14-19,23H,4-12H2,1-3H3/t14-,15+,16-,17+,18-,19-,20-,21+/m0/s1; Key:AURFZBICLPNKBZ-SYBPFIFISA-N;

ଆଲୋପ୍ରେଗନାନୋଲୋନ ଏକ ପ୍ରାକୃତିକ ଭାବରେ ଘଟୁଥିବା ହରମୋନ୍ ଯାହା ଏକ ଔଷଧ ଭାବରେ ମଧ୍ୟ ବ୍ୟବହୃତ ହୁଏ । ^[୯] ^[୧] ଏକ ଔଷଧ ଭାବରେ ଏହା ବ୍ରେକ୍ସାନୋଲୋନ୍ ଭାବରେ ଜଣାଶୁଣା, ଜୁଲେସୋ ନାମରେ ବିକ୍ରି ହୁଏ ଏବଂ ପ୍ରସବ ପରବର୍ତ୍ତୀ ଅବସାଦର ଚିକିତ୍ସା ପାଇଁ ବ୍ୟବହୃତ ହୁଏ । ^[୧] ଡାକ୍ତରୀ ତତ୍ତ୍ୱାବଧାନରେ ୬୦ ଘଣ୍ଟା ମଧ୍ୟରେ ଏହା ଏକ ଶିରାରେ ଇଞ୍ଜେକ୍ସନ ଆକାରରେ ଦିଆଯାଏ । ^[୧]

ସାଧାରଣ ପାର୍ଶ୍ୱ ପ୍ରତିକ୍ରିୟାରେ ନିଦ୍ରାଳୁ ଭାବ, ଶୁଖିଲା ପାଟି, ଗରମ ଚମକ ଏବଂ ଅଚେତନ ହୋଇପାରେ । ^[୧] ଅନ୍ୟ ପାର୍ଶ୍ୱ ପ୍ରତିକ୍ରିୟାରେ ଆତ୍ମହତ୍ୟା ଚିନ୍ତାଧାରା ହୋଇପାରେ। ^[୧] ଗର୍ଭାବସ୍ଥାରେ ବ୍ୟବହାର ଶିଶୁର କ୍ଷତି କରିପାରେ । ^[୧] ଏହା ଏକ ନ୍ୟୁରୋଷ୍ଟେରଏଡ୍ ଏବଂ ଜିଏବିଏ<sub id="mwTQ">ଏ</sub> (GABA <sub id="mwTQ">A)</sub> ରିସେପ୍ଟରର ଏକ ସକରାତ୍ମକ ଆଲୋଷ୍ଟେରିକ୍ ମୋଡ୍ୟୁଲେଟର ଭାବରେ କାର୍ଯ୍ୟ କରେ । ^[୧]

୨୦୧୯ ମସିହାରେ ଯୁକ୍ତରାଷ୍ଟ୍ରରେ ଚିକିତ୍ସା ବ୍ୟବହାର ପାଇଁ ବ୍ରେକ୍ସାନୋଲୋନ ଅନୁମୋଦିତ ହୋଇଥିଲା । ^[୧] ^[୧୦] ୟୁରୋପ କିମ୍ବା ବ୍ରିଟେନରେ ଏହା ୨୦୨୨ ସୁଦ୍ଧା ଅନୁମୋଦିତ ନୁହେଁ। ଯୁକ୍ତରାଷ୍ଟ୍ରରେ ୨୦୧୯ ସୁଦ୍ଧା ଗୋଟିଏ ଚିକିତ୍ସା କ୍ରମରେ ଔଷଧର ମୂଲ୍ୟ ୩୪,୦୦୦ ଡଲାର ଅଟେ । ^[୧୧] ଦୀର୍ଘ ପ୍ରଶାସନର ସମୟ, ମୂଲ୍ୟ, ଏବଂ ଡାକ୍ତରଖାନାରେ ଭର୍ତ୍ତି ହେବାର ଆବଶ୍ୟକତା, ଉପଲବ୍ଧତା ବିଷୟ ଚିନ୍ତା ଜନ‌କ ହୋଇଛି । ^[୧୧]

ଆଧାର

↑ ^୧.୦୦ ^୧.୦୧ ^୧.୦୨ ^୧.୦୩ ^୧.୦୪ ^୧.୦୫ ^୧.୦୬ ^୧.୦୭ ^୧.୦୮ ^୧.୦୯ ^୧.୧୦ ^୧.୧୧ ^୧.୧୨ ^୧.୧୩ ^୧.୧୪ "Zulresso- brexanolone injection, solution". DailyMed. 18 November 2019. Archived from the original on 2 July 2019. Retrieved 23 November 2019.
↑ Krieger NR, Mok WM, Herschkowitz S (September 1990). "5α-Pregnane-3α-ol-20-one Identified as an Active Molecular Species of Steroid Anesthetic in Brain". Anesthesiology. 73. doi:10.1097/00000542-199009001-00702.
↑ Yagen B, Gallili GE, Mateles RI (August 1978). "Progesterone biotransformation by plant cell suspension cultures". Applied and Environmental Microbiology. 36 (2): 213–6. Bibcode:1978ApEnM..36..213Y. doi:10.1128/AEM.36.2.213-216.1978. PMC 291203. PMID 697360.
↑ Meyer HH, Jewgenow K, Hodges JK (February 1997). "Binding activity of 5alpha-reduced gestagens to the progestin receptor from African elephant (Loxodonta africana)". General and Comparative Endocrinology. 105 (2): 164–7. doi:10.1006/gcen.1996.6813. PMID 9038248.
↑ Frye C, Seliga A (May 2002). "Olanzapine and progesterone have dose-dependent and additive effects to enhance lordosis and progestin concentrations of rats". Physiology & Behavior. 76 (1): 151–8. doi:10.1016/s0031-9384(02)00689-3. PMID 12175598. S2CID 38249308.
↑ Mahendroo M, Wilson JD, Richardson JA, Auchus RJ (July 2004). "Steroid 5alpha-reductase 1 promotes 5alpha-androstane-3alpha,17beta-diol synthesis in immature mouse testes by two pathways". Molecular and Cellular Endocrinology. 222 (1–2): 113–20. doi:10.1016/j.mce.2004.04.009. PMID 15249131. S2CID 54297812.
↑ "DEA Schedules Postpartum Depression Treatment Zulresso". Monthly Prescribing Reference. 17 June 2019. Archived from the original on 3 September 2019. Retrieved 24 November 2019.
↑ ^୮.୦ ^୮.୧ ^୮.୨ ^୮.୩ ^୮.୪ ^୮.୫ Scott LJ (May 2019). "Brexanolone: First Global Approval". Drugs. 79 (7): 779–783. doi:10.1007/s40265-019-01121-0. PMID 31006078. S2CID 123095177.
↑ Reddy DS (2010). Neurosteroids: endogenous role in the human brain and therapeutic potentials. Progress in Brain Research. Vol. 186. pp. 113–37. doi:10.1016/B978-0-444-53630-3.00008-7. ISBN 9780444536303. PMC 3139029. PMID 21094889. {{cite book}}: |work= ignored (help)
↑ "Brexanolone". SPS - Specialist Pharmacy Service. 21 January 2016. Archived from the original on 1 November 2019. Retrieved 11 January 2022.
↑ ^୧୧.୦ ^୧୧.୧ "New Postpartum Depression Drug Could Be Hard To Access For Moms Most In Need". NPR. 21 March 2019. Archived from the original on 21 March 2019. Retrieved 22 March 2019.

[PI2022-1] ୧.୦୦ ^୧.୦୧ ^୧.୦୨ ^୧.୦୩ ^୧.୦୪ ^୧.୦୫ ^୧.୦୬ ^୧.୦୭ ^୧.୦୮ ^୧.୦୯ ^୧.୧୦ ^୧.୧୧ ^୧.୧୨ ^୧.୧୩ ^୧.୧୪ "Zulresso- brexanolone injection, solution". DailyMed. 18 November 2019. Archived from the original on 2 July 2019. Retrieved 23 November 2019.

[doi1010970000054219900900100702-2] Krieger NR, Mok WM, Herschkowitz S (September 1990). "5α-Pregnane-3α-ol-20-one Identified as an Active Molecular Species of Steroid Anesthetic in Brain". Anesthesiology. 73. doi:10.1097/00000542-199009001-00702.

[pmid697360-3] Yagen B, Gallili GE, Mateles RI (August 1978). "Progesterone biotransformation by plant cell suspension cultures". Applied and Environmental Microbiology. 36 (2): 213–6. Bibcode:1978ApEnM..36..213Y. doi:10.1128/AEM.36.2.213-216.1978. PMC 291203. PMID 697360.

[pmid9038248-4] Meyer HH, Jewgenow K, Hodges JK (February 1997). "Binding activity of 5alpha-reduced gestagens to the progestin receptor from African elephant (Loxodonta africana)". General and Comparative Endocrinology. 105 (2): 164–7. doi:10.1006/gcen.1996.6813. PMID 9038248.

[pmid12175598-5] Frye C, Seliga A (May 2002). "Olanzapine and progesterone have dose-dependent and additive effects to enhance lordosis and progestin concentrations of rats". Physiology & Behavior. 76 (1): 151–8. doi:10.1016/s0031-9384(02)00689-3. PMID 12175598. S2CID 38249308.

[pmid15249131-6] Mahendroo M, Wilson JD, Richardson JA, Auchus RJ (July 2004). "Steroid 5alpha-reductase 1 promotes 5alpha-androstane-3alpha,17beta-diol synthesis in immature mouse testes by two pathways". Molecular and Cellular Endocrinology. 222 (1–2): 113–20. doi:10.1016/j.mce.2004.04.009. PMID 15249131. S2CID 54297812.

[MPR-7] "DEA Schedules Postpartum Depression Treatment Zulresso". Monthly Prescribing Reference. 17 June 2019. Archived from the original on 3 September 2019. Retrieved 24 November 2019.

[Scott2019-8] ୮.୦ ^୮.୧ ^୮.୨ ^୮.୩ ^୮.୪ ^୮.୫ Scott LJ (May 2019). "Brexanolone: First Global Approval". Drugs. 79 (7): 779–783. doi:10.1007/s40265-019-01121-0. PMID 31006078. S2CID 123095177.

[Doo2010-9] Reddy DS (2010). Neurosteroids: endogenous role in the human brain and therapeutic potentials. Progress in Brain Research. Vol. 186. pp. 113–37. doi:10.1016/B978-0-444-53630-3.00008-7. ISBN 9780444536303. PMC 3139029. PMID 21094889. {{cite book}}: |work= ignored (help)

[SP2022-10] "Brexanolone". SPS - Specialist Pharmacy Service. 21 January 2016. Archived from the original on 1 November 2019. Retrieved 11 January 2022.

[NPR2019-11] ୧୧.୦ ^୧୧.୧ "New Postpartum Depression Drug Could Be Hard To Access For Moms Most In Need". NPR. 21 March 2019. Archived from the original on 21 March 2019. Retrieved 22 March 2019.

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