스피로놀락톤

스피로놀락톤
體系的名稱 ( IUPAC 命名法 )
	S -[(7 R ,8 R ,9 S ,10 R ,13 S ,14 S ,17 R )-10,13-Dimethyl-3,5'-dioxospiro[2,6,7,8,9,11,12,14,15,16-decahydro-1 H -cyclopenta[ a ]phenanthrene-17,2'-oxolane]-7-yl] ethanethioate
識別情報
CAS 登錄番號	52-01-7
ATC 코드	C03 DA01
PubChem	5833
드러그뱅크	DB00421
ChemSpider	5628
化學的性質
化學式	C 24 H 32 O 4 S
分子量	416.574 g/mol
類義語	SC-9420; NSC-150339; 7α-Acetylthiospirolactone; 7α-Acetylthio-17α-hydroxy-3-oxopregn-4-ene-21-carboxylic acid γ-lactone
物理的性質
녹는點	134?135 °C (273?275 °F)
藥東學情報
生體適合性	60?90%
蛋白質結合	Spironolactone: 88% (to albumin and AGP ) ; Canrenone: 99.2% (to albumin)
同等生物醫藥品	?
藥물 大使	Liver , others: ; ? Deacetylation via CES ; ? S - Oxygenation via FOM ; ? S - Methylation via TMT ; ? Dethioacetylation ; ? Hydroxylation via CYP3A4 ; ? Lactone hydrolysis via PON3 )
生物學的半減期	Spironolactone: 1.4 hrs ; 7α-TMS : 13.8 hours ; 6β-OH-7α-TMS : 15.0 hrs ; Canrenone : 16.5 hours
排出	Urine , bile
處方注意事項
妊婦投與安全性	B3 ( 오스트레일리아 ) C ( 美國 )
法的狀態	UK : POM (Prescription only) ; US : ?-only ;
投與方法	By mouth , topical

스피로놀락톤 ( 英語 : spironolactone )은 港알도스테론第, 칼륨 保存性利尿劑 , 스피로 化合物中의 하나로, 體內 알도스테론 과 그의 受容體끼리의 結合을 抑制하여 體內 칼륨 이온을 保存하는 利尿作用을 나타낸다. 主로 心不全, 肝硬變性復讐, 高血壓治療劑에 使用되며, 低칼륨血症 에 對한 補助的인 治療藥으로도 活用된다. 男性 호르몬 을 抑制하는 副作用으로 인해 女性型乳房 , 乳房痛, 皮膚發疹等을 일으키나 이것을 應用해 女性 에게 發病되는 男性型脫毛症 과 여드름 治療劑로 利用하기도 한다. 또한 트랜스젠더의 女性化 호르몬 治療 에도 利用된다.

같이 보기 [ 編輯 ]

락톤

各州 [ 編輯 ]

↑ ^가 ^나 ^다 ^라 ^마 ^바 Sica, Domenic A. (2005). “Pharmacokinetics and Pharmacodynamics of Mineralocorticoid Blocking Agents and their Effects on Potassium Homeostasis”. 《Heart Failure Reviews》 10 (1): 23?29. doi : 10.1007/s10741-005-2345-1 . ISSN 1382-4147 . PMID 15947888 .
↑ ^가 ^나 ^다 Maron BA, Leopold JA (2008). “Mineralocorticoid receptor antagonists and endothelial function” . 《Curr Opin Investig Drugs》 9 (9): 963?9. PMC 2967484 . PMID 18729003 .
↑ Carone, Laura; Oxberry, Stephen G.; Twycross, Robert; Charlesworth, Sarah; Mihalyo, Mary; Wilcock, Andrew (2017). “Spironolactone”. 《Journal of Pain and Symptom Management》 53 (2): 288?292. doi : 10.1016/j.jpainsymman.2016.12.320 . ISSN 0885-3924 . PMID 28024992 .
↑ ^가 ^나 Takamura, Norito; Maruyama, Toru; Ahmed, Shamim; Suenaga, Ayaka; Otagiri, Masaki (1997). “Interactions of Aldosterone Antagonist Diuretics with Human Serum Proteins”. 《Pharmaceutical Research》 14 (4): 522?526. doi : 10.1023/A:1012168020545 . ISSN 0724-8741 .
↑ Andrew Parkinson (2001). 《Biotransformation of Xenobiotics》 . McGraw-Hill. 137?138,169,171,180,195,208쪽.
↑ Curtis D. Klaassen (2007年 12月 11日). 《Casarett & Doull's Toxicology: The Basic Science of Poisons, Seventh Edition》 . McGraw Hill Professional. 173쪽. ISBN 978-0-07-159351-9 . Some P450 enzymes (such as the rate enzyme CYP2A1) preferentially catalyze the 6α-hydroxylation reaction, whereas other P450 enzymes (such as the CYP3A enzymes in all mammalian species) preferentially catalyze the 6β-hydroxylation reaction (which is a major route of hepatic steroid biotransformation).
↑ Los LE, Pitzenberger SM, Ramjit HG, Coddington AB, Colby HD (1994). “Hepatic metabolism of spironolactone. Production of 3-hydroxy-thiomethyl metabolites” . 《Drug Metab. Dispos.》 22 (6): 903?8. PMID 7895608 .
↑ Henry R. Black; William Elliott (2006年 12月 28日). 《Hypertension: A Companion to Braunwald's Heart Disease》 . Elsevier Health Sciences. 295?쪽. ISBN 978-1-4377-1078-6 .
↑ Draganov DI, La Du BN (January 2004). “Pharmacogenetics of paraoxonases: a brief review”. 《Naunyn Schmiedebergs Arch. Pharmacol.》 369 (1): 78?88. doi : 10.1007/s00210-003-0833-1 . PMID 14579013 .
↑ “Spironolactone” . The American Society of Health-System Pharmacists. 2015年 11月 16日에 原本文書 에서 保存된 文書 . Oct 24, 2015에 確認함 .
↑ NADIR R. FARID; Evanthia Diamanti-Kandarakis (2009年 2月 27日). 《Diagnosis and Management of Polycystic Ovary Syndrome》 . Springer Science & Business Media. 235?쪽. ISBN 978-0-387-09718-3 .

[Sica2005-1] 가 ^나 ^다 ^라 ^마 ^바 Sica, Domenic A. (2005). “Pharmacokinetics and Pharmacodynamics of Mineralocorticoid Blocking Agents and their Effects on Potassium Homeostasis”. 《Heart Failure Reviews》 10 (1): 23?29. doi : 10.1007/s10741-005-2345-1 . ISSN 1382-4147 . PMID 15947888 .

[pmid18729003-2] 가 ^나 ^다 Maron BA, Leopold JA (2008). “Mineralocorticoid receptor antagonists and endothelial function” . 《Curr Opin Investig Drugs》 9 (9): 963?9. PMC 2967484 . PMID 18729003 .

[CaroneOxberry2017-3] Carone, Laura; Oxberry, Stephen G.; Twycross, Robert; Charlesworth, Sarah; Mihalyo, Mary; Wilcock, Andrew (2017). “Spironolactone”. 《Journal of Pain and Symptom Management》 53 (2): 288?292. doi : 10.1016/j.jpainsymman.2016.12.320 . ISSN 0885-3924 . PMID 28024992 .

[TakamuraMaruyama1997-4] 가 ^나 Takamura, Norito; Maruyama, Toru; Ahmed, Shamim; Suenaga, Ayaka; Otagiri, Masaki (1997). “Interactions of Aldosterone Antagonist Diuretics with Human Serum Proteins”. 《Pharmaceutical Research》 14 (4): 522?526. doi : 10.1023/A:1012168020545 . ISSN 0724-8741 .

[Parkinson2001-5] Andrew Parkinson (2001). 《Biotransformation of Xenobiotics》 . McGraw-Hill. 137?138,169,171,180,195,208쪽.

[Klaassen2007-6] Curtis D. Klaassen (2007年 12月 11日). 《Casarett & Doull's Toxicology: The Basic Science of Poisons, Seventh Edition》 . McGraw Hill Professional. 173쪽. ISBN 978-0-07-159351-9 . Some P450 enzymes (such as the rate enzyme CYP2A1) preferentially catalyze the 6α-hydroxylation reaction, whereas other P450 enzymes (such as the CYP3A enzymes in all mammalian species) preferentially catalyze the 6β-hydroxylation reaction (which is a major route of hepatic steroid biotransformation).

[pmid7895608-7] Los LE, Pitzenberger SM, Ramjit HG, Coddington AB, Colby HD (1994). “Hepatic metabolism of spironolactone. Production of 3-hydroxy-thiomethyl metabolites” . 《Drug Metab. Dispos.》 22 (6): 903?8. PMID 7895608 .

[BlackElliott2006-8] Henry R. Black; William Elliott (2006年 12月 28日). 《Hypertension: A Companion to Braunwald's Heart Disease》 . Elsevier Health Sciences. 295?쪽. ISBN 978-1-4377-1078-6 .

[pmid14579013-9] Draganov DI, La Du BN (January 2004). “Pharmacogenetics of paraoxonases: a brief review”. 《Naunyn Schmiedebergs Arch. Pharmacol.》 369 (1): 78?88. doi : 10.1007/s00210-003-0833-1 . PMID 14579013 .

[AHFS2015-10] “Spironolactone” . The American Society of Health-System Pharmacists. 2015年 11月 16日에 原本文書 에서 保存된 文書 . Oct 24, 2015에 確認함 .

[FARIDDiamanti-Kandarakis2009-11] NADIR R. FARID; Evanthia Diamanti-Kandarakis (2009年 2月 27日). 《Diagnosis and Management of Polycystic Ovary Syndrome》 . Springer Science & Business Media. 235?쪽. ISBN 978-0-387-09718-3 .

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