Spironolakton: Perbedaan antara revisi
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| bioavailability = 60–90%<ref name="Sica2005" >{{cite journal|last1=Sica|first1=Domenic A.|title=Pharmacokinetics and Pharmacodynamics of Mineralocorticoid Blocking Agents and their Effects on Potassium Homeostasis|journal=Heart Failure Reviews|volume=10|issue=1|year=2005|pages=23–29|issn=1382-4147|doi=10.1007/s10741-005-2345-1|pmid=15947888}}</ref><ref name="pmid18729003">{{cite journal | vauthors = Maron BA, Leopold JA | title = Mineralocorticoid receptor antagonists and endothelial function | journal = Curr Opin Investig Drugs | volume = 9 | issue = 9 | pages = 963–9 | year = 2008 | pmid = 18729003 | pmc = 2967484 | doi = | url = }}</ref><ref name="CaroneOxberry2017">{{cite journal|last1=Carone|first1=Laura|last2=Oxberry|first2=Stephen G.|last3=Twycross|first3=Robert|last4=Charlesworth|first4=Sarah|last5=Mihalyo|first5=Mary|last6=Wilcock|first6=Andrew|title=Spironolactone|journal=Journal of Pain and Symptom Management|volume=53|issue=2|year=2017|pages=288–292|issn=0885-3924|doi=10.1016/j.jpainsymman.2016.12.320|pmid=28024992}}</ref>
| protein_bound = Spironolactone: 88% (pada [[human serum albumin|albumin]] dan {{abbrlink|AGP|alpha-1-acid glycoprotein}})<ref name="TakamuraMaruyama1997" >{{cite journal|last1=Takamura|first1=Norito|last2=Maruyama|first2=Toru|last3=Ahmed|first3=Shamim|last4=Suenaga|first4=Ayaka|last5=Otagiri|first5=Masaki |title=Interactions of Aldosterone Antagonist Diuretics with Human Serum Proteins |journal=Pharmaceutical Research|volume=14|issue=4|year=1997|pages=522–526|issn=0724-8741 |doi=10.1023/A:1012168020545|pmid=9144743}}</ref><br />Canrenone: 99.2% (pada albumin)<ref name="TakamuraMaruyama1997" />
| metabolism = [[Liver]], lainnya:<br />• [[Deacetylation]] via {{abbrlink|CES|carboxylesterase}}<br />• ''S''-[[Oxidation|Oxygenation]] via {{abbrlink|FOM|flavin-containing monooxygenase}}<br />• ''S''-[[Methylation]] via {{abbrlink|TMT|thiol S-methyltransferase}}<br />• [[Dethioacetylation]]<br />• [[Hydroxylation]] via [[CYP3A4]]<br />• [[Lactone]] [[hydrolysis]] via [[PON3]])<ref name="Sica2005" /><ref name="pmid18729003" /><ref name="Parkinson2001">{{cite book|author=Andrew Parkinson|title=Biotransformation of Xenobiotics|url=https://books.google.com/books?id=pAovcgAACAAJ|year=2001|publisher=McGraw-Hill|pages=137–138, 169, 171, 180, 195, 208}}</ref><ref name="Klaassen2007">{{cite book|author=Curtis D. Klaassen|title=Casarett & Doull's Toxicology: The Basic Science of Poisons, Seventh Edition|url=https://books.google.com/books?id=4yi7-j48uhIC|date=11 December 2007|publisher=McGraw Hill Professional|isbn=978-0-07-159351-9|page=173|quote=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).}}</ref><ref name="pmid7895608">{{cite journal | vauthors = Los LE, Pitzenberger SM, Ramjit HG, Coddington AB, Colby HD | title = Hepatic metabolism of spironolactone. Production of 3-hydroxy-thiomethyl metabolites | journal = Drug Metab. Dispos. | volume = 22 | issue = 6 | pages = 903–8 | date = 1994 | pmid = 7895608 | doi = | url = http://dmd.aspetjournals.org/content/22/6/903}}</ref><ref name="BlackElliott2006">{{cite book|author1=Henry R. Black|author2=William Elliott|title=Hypertension: A Companion to Braunwald's Heart Disease|url=https://books.google.com/books?id=42Fcmne6_w8C&pg=PA295|date=28 December 2006|publisher=Elsevier Health Sciences|isbn=978-1-4377-1078-6|pages=295–}}</ref>
| metabolites = {{abbrlink|7α-TS|7α-Thiospironolactone}}, {{abbrlink|7α-TMS|7α-thiomethylspironolactone}}, {{abbrlink|6β-OH-7α-TMS|6β-hydroxy-7α-thiomethylspironolactone}}, [[canrenone]], lainnya<ref name="Sica2005" /><ref name="pmid18729003" /><ref name="SzaszBudvari-Barany1990" /><br />(All three active)<ref name="McDonaghGardner2011">{{cite book|author1=Theresa A. McDonagh|author2=Roy S. Gardner|author3=Andrew L. Clark|author4=Henry Dargie|title=Oxford Textbook of Heart Failure|url=https://books.google.com/books?id=KDDCiTQyGLsC&pg=PA403|date=14 July 2011|publisher=OUP Oxford|isbn=978-0-19-957772-9|pages=403–|url-status=live|archiveurl=https://web.archive.org/web/20170327090209/https://books.google.com/books?id=KDDCiTQyGLsC&pg=PA403|archivedate=27 March 2017}}</ref>
| elimination_half-life = Spironolactone: 1.4 jam<ref name="Sica2005" /><br />{{abbrlink|7α-TMS|7α-thiomethylspironolactone}}: 13.8 jam<ref name="Sica2005" /><br />{{abbrlink|6β-OH-7α-TMS|6β-hydroxy-7α-thiomethylspironolactone}}: 15.0 jam<ref name="Sica2005" /><br />[[Canrenone]]: 16.5 jam<ref name="Sica2005" />
Baris 66:
| melting_high = 135
}}
'''Spironolakton''', dijual dengan merk dagang '''Aldactone''', adalah obat yang digunakan untuk menangani [[sembap]] atau edema akibat [[gagal jantung]], [[sirosis hati]], atau [[penyakit ginjal]].<ref name=AHFS2015>{{cite web|title=Spironolactone|url=https://www.drugs.com/monograph/spironolactone.html|publisher=The American Society of Health-System Pharmacists|accessdate=Oct 24, 2015|url-status=live|archiveurl=https://web.archive.org/web/20151116054857/http://www.drugs.com/monograph/spironolactone.html|archivedate=2015-11-16}}</ref> Obat ini juga dipakai untuk menangani [[hipertensi]] ([[tekanan darah]] tinggi), [[hipokalemia|kadar kalium yang rendah dalam darah]] dan tak kunjung membaik walau sudah mengonsumsi suplemen, pubertas dini pada laki-laki, jerawat, dan pertumbuhan rambut yang berlebihan pada wanita. Spironolakton bahkan juga dapat dimanfaatkan untuk [[terapi hormon feminin]] untuk [[wanita transgender]].<ref name=AHFS2015/><ref>{{cite journal|first1=Adam J.|last1=Friedman|title=Spironolactone for Adult Female Acne|journal=Cutis|date=1 October 2015|issn=2326-6929|pages=216–217|volume=96|issue=4|pmid=27141564}}</ref><ref>{{cite book|last1=Maizes|first1=Victoria|title=Integrative Women's Health|date=2015|isbn=9780190214807|page=746|edition=2|url=https://books.google.com/books?id=uveJCgAAQBAJ&pg=PA746|df=}}</ref> Spironolakton dikonsumsi lewat mulut.<ref name=AHFS2015/>
== Kontraindikasi ==
Efek samping yang dapat muncul jika mengonsumsi obat ini meliputi [[abnormalitas elektrolit]] (khususnya [[hiperkalemia|kadar kalium dalam darah yang terlalu tinggi]]), mual, muntah, sakit kepala, bercak, dan berkurangnya nafsu seks.<ref name=AHFS2015/> Mereka yang mengalami gangguan hati atau ginjal harus berhati-hati dalam mengonsumsi obat ini.<ref name=AHFS2015/> Belum ada cukup penelitian yang mengkaji konsumsi spironolakton pada ibu hamil, sehingga obat ini sebaiknya tidak diberikan untuk menangani [[penyakit kehamilan hipertensi]].<ref name="Drugs.com pregnancy">{{cite web|title=Spironolactone Pregnancy and Breastfeeding Warnings|url=https://www.drugs.com/pregnancy/spironolactone.html|accessdate=29 November 2015|url-status=live|archiveurl=https://web.archive.org/web/20151202081203/http://www.drugs.com/pregnancy/spironolactone.html|archivedate=2 December 2015}}</ref> Obat ini sendiri adalah [[steroid]] yang menghambat efek hormon [[aldosteron]] dan [[testosteron]] dan memiliki efek yang seperti [[estrogen]].<ref name=AHFS2015/><ref name="Deedwania2014">{{cite book|author=Prakash C Deedwania|title=Drug & Device Selection in Heart Failure|url=https://books.google.com/books?id=k8bUAgAAQBAJ&pg=PA47|date=30 January 2014|publisher=JP Medical Ltd|isbn=978-93-5090-723-8|pages=47–}}</ref> Spironolakton tergolong ke dalam golongan obat-obatan yang disebut ''[[potassium-sparing diuretic]]''.<ref name=AHFS2015/>▼
Tentunya, tidak semua orang boleh mengonsumsi obat ini. Terdapat beberapa kondisi di mana sebaiknya pasien menghindari obat ini seperti:
* Pasien dengan penyakit Addison
Spironolakton pertama kali ditemukan pada tahun 1957 dan diperkenalkan kepada umum pada tahun 1959.<ref name="OttowWeinmann2008">{{cite book | author1 = Eckhard Ottow | author2 = Hilmar Weinmann | title = Nuclear Receptors As Drug Targets | url = https://books.google.com/books?id=iATfLbPgRugC&pg=PA410 | accessdate = 28 May 2012 | date = 9 July 2008 | publisher = John Wiley & Sons | isbn = 978-3-527-62330-3 | page = 410 | url-status = live | archiveurl = https://web.archive.org/web/20130621121614/http://books.google.com/books?id=iATfLbPgRugC&pg=PA410 | archivedate = 21 June 2013 }}</ref><ref name="Wermuth2008">{{cite book | author = Camille Georges Wermuth | title = The Practice of Medicinal Chemistry | url = https://books.google.com/books?id=Qmt1_DQkCpEC&pg=PA34 | accessdate = 27 May 2012 | date = 24 July 2008 | publisher = Academic Press | isbn = 978-0-12-374194-3 | page = 34 | url-status = live | archiveurl = https://web.archive.org/web/20130621115634/http://books.google.com/books?id=Qmt1_DQkCpEC&pg=PA34 | archivedate = 21 June 2013 | author-link = Camille Georges Wermuth }}</ref><ref name="Sittig1988">{{cite book | author = Marshall Sittig | title = Pharmaceutical Manufacturing Encyclopedia | url = https://books.google.com/books?id=XCsJgUnclbcC&pg=PA1385 | accessdate = 27 May 2012 | year = 1988 | publisher = William Andrew | isbn = 978-0-8155-1144-1 | page = 1385 | url-status = live | archiveurl = https://web.archive.org/web/20130620225714/http://books.google.com/books?id=XCsJgUnclbcC&pg=PA1385 | archivedate = 20 June 2013 }}</ref> Obat ini termasuk ke dalam daftar [[Obat Esensial Organisasi Kesehatan Dunia]].<ref name="WHO21st">{{cite book | vauthors = ((World Health Organization)) | title = World Health Organization model list of essential medicines: 21st list 2019 | year = 2019 | hdl = 10665/325771 | author-link = World Health Organization | publisher = World Health Organization | location = Geneva | id = WHO/MVP/EMP/IAU/2019.06. License: CC BY-NC-SA 3.0 IGO }}</ref> Spironolakton tersedia dalam bentuk generik.<ref name=AHFS2015/> Harga grosiran obat ini di negara berkembang pada tahun 2014 berkisar antara {{US$}}0,02 hingga {{US$}}0,12 per hari.<ref>{{cite web|title=Spironolactone|url=http://mshpriceguide.org/en/single-drug-information/?DMFId=731&searchYear=2014|website=International Drug Price Indicator Guide|accessdate=29 November 2015}}</ref> Di Amerika Serikat harganya dapat mencapai {{US$}}0,50 per hari.<ref name=AHFS2015/>▼
* Pasien dengan hiperkalemia
* Pasien yang tidak dapat buang air kecil
* Pasien yang hipersensitif terhadap kandungan bahan aktif maupun komponen lain dalam obat ini<ref name="Informasi Kesehatan">{{Cite web|url=https://doktersehat.com/obat-spironolakton/|website=www.doktersehat.com|title=Spironolactone: Manfaat, Dosis, dan Efek Samping|language=id|access-date=2020-07-14|archive-date=2020-07-16|archive-url=https://web.archive.org/web/20200716174343/https://doktersehat.com/obat-spironolakton/|dead-url=yes}}</ref>
== Efek Samping ==
▲Efek samping yang dapat muncul jika mengonsumsi obat ini meliputi [[abnormalitas elektrolit]] (khususnya [[hiperkalemia|kadar kalium dalam darah yang terlalu tinggi]]), mual, muntah, [[sakit kepala]], bercak, dan berkurangnya nafsu seks.<ref name=AHFS2015/> Mereka yang mengalami gangguan hati atau ginjal harus berhati-hati dalam mengonsumsi obat ini.<ref name=AHFS2015/> Belum ada cukup penelitian yang mengkaji konsumsi spironolakton pada ibu hamil, sehingga obat ini sebaiknya tidak diberikan untuk menangani [[penyakit kehamilan hipertensi]].<ref name="Drugs.com pregnancy">{{cite web|title=Spironolactone Pregnancy and Breastfeeding Warnings|url=https://www.drugs.com/pregnancy/spironolactone.html|accessdate=29 November 2015|url-status=live|archiveurl=https://web.archive.org/web/20151202081203/http://www.drugs.com/pregnancy/spironolactone.html|archivedate=2 December 2015}}</ref> Obat ini sendiri adalah [[steroid]] yang menghambat efek hormon [[aldosteron]] dan [[testosteron]] dan memiliki efek yang seperti [[estrogen]].<ref name=AHFS2015/><ref name="Deedwania2014">{{cite book|author=Prakash C Deedwania|title=Drug & Device Selection in Heart Failure|url=https://books.google.com/books?id=k8bUAgAAQBAJ&pg=PA47|date=30 January 2014|publisher=JP Medical Ltd|isbn=978-93-5090-723-8|pages=47–}}</ref> Spironolakton tergolong ke dalam golongan obat-obatan yang disebut ''[[potassium-sparing diuretic]]''.<ref name=AHFS2015/>
== Sejarah ==
▲Spironolakton pertama kali ditemukan pada tahun 1957 dan diperkenalkan kepada umum pada tahun 1959.<ref name="OttowWeinmann2008">{{cite book | author1 = Eckhard Ottow | author2 = Hilmar Weinmann | title = Nuclear Receptors As Drug Targets | url = https://books.google.com/books?id=iATfLbPgRugC&pg=PA410 | accessdate = 28 May 2012 | date = 9 July 2008 | publisher = John Wiley & Sons | isbn = 978-3-527-62330-3 | page = 410 | url-status = live | archiveurl = https://web.archive.org/web/20130621121614/http://books.google.com/books?id=iATfLbPgRugC&pg=PA410 | archivedate = 21 June 2013 }}</ref><ref name="Wermuth2008">{{cite book | author = Camille Georges Wermuth | title = The Practice of Medicinal Chemistry | url = https://books.google.com/books?id=Qmt1_DQkCpEC&pg=PA34 | accessdate = 27 May 2012 | date = 24 July 2008 | publisher = Academic Press | isbn = 978-0-12-374194-3 | page = 34 | url-status = live | archiveurl = https://web.archive.org/web/20130621115634/http://books.google.com/books?id=Qmt1_DQkCpEC&pg=PA34 | archivedate = 21 June 2013 | author-link = Camille Georges Wermuth }}</ref><ref name="Sittig1988">{{cite book | author = Marshall Sittig | title = Pharmaceutical Manufacturing Encyclopedia | url = https://books.google.com/books?id=XCsJgUnclbcC&pg=PA1385 | accessdate = 27 May 2012 | year = 1988 | publisher = William Andrew | isbn = 978-0-8155-1144-1 | page = 1385 | url-status = live | archiveurl = https://web.archive.org/web/20130620225714/http://books.google.com/books?id=XCsJgUnclbcC&pg=PA1385 | archivedate = 20 June 2013 }}</ref> Obat ini termasuk ke dalam daftar [[Obat Esensial Organisasi Kesehatan Dunia]].<ref name="WHO21st">{{cite book | vauthors = ((World Health Organization)) | title = World Health Organization model list of essential medicines: 21st list 2019 | year = 2019 | hdl = 10665/325771 | author-link = World Health Organization | publisher = World Health Organization | location = Geneva | id = WHO/MVP/EMP/IAU/2019.06. License: CC BY-NC-SA 3.0 IGO }}</ref> Spironolakton tersedia dalam bentuk generik.<ref name=AHFS2015/> Harga grosiran obat ini di [[negara berkembang]] pada tahun 2014 berkisar antara {{US$}}0,02 hingga {{US$}}0,12 per hari.<ref>{{cite web|title=Spironolactone|url=http://mshpriceguide.org/en/single-drug-information/?DMFId=731&searchYear=2014|website=International Drug Price Indicator Guide|accessdate=29 November 2015}}</ref> Di Amerika Serikat harganya dapat mencapai {{US$}}0,50 per hari.<ref name=AHFS2015/>
== Referensi ==
{{reflist}}
[[Kategori:Spironolakton| ]]
[[Kategori:Obat Esensial Organisasi Kesehatan Dunia]]
[[Kategori:Obat Esensial Nasional Indonesia]]
[[Kategori:Diuretik]]
[[Kategori:Penghambat sintase aldosteron]]
[[Kategori:Antihipertensi]]
[[Kategori:Antiedema]]
[[Kategori:Penghambat 3β-HSD]]
[[Kategori:Penghambat 5α-reduktase]]
[[Kategori:Penghambat CYP11B1]]
[[Kategori:Penghambat 17β-HSD]]
[[Kategori:Penghambat CYP21A2]]
[[Kategori:Penghambat CYP17A1]]
[[Kategori:Penghambat CYP11A1]]
[[Kategori:antagonis reseptor mineralokortikoid]]
[[Kategori:Bakal obat]]
[[Kategori:Agonis NR1I2]]
[[Kategori:Progestogen]]
[[Kategori:Modulator reseptor estrogen selektif]]
[[Kategori:Spirolakton]]
[[Kategori:Ester asetat]]
[[Kategori:Tioester]]
[[Kategori:Diuretik hemat kalium]]
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