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{{Drugbox|IUPAC_name=[(8''R'',9''S'',13''S'',14''S'',17''S'')-3-hydroxy-13-methyl-6,7,8,9,11,12,14,15,16,17-decahydrocyclopenta[''a'']phenanthren-17-yl] pentanoate|image=Estradiol valerate.svg|width=250px|image2=Estradiol valerate molecule ball.png|width2=250px
{{Drugbox|IUPAC_name=[(8''R'',9''S'',13''S'',14''S'',17''S'')-3-hydroxy-13-methyl-6,7,8,9,11,12,14,15,16,17-decahydrocyclopenta[''a'']phenanthren-17-yl] pentanoate|image=Estradiol valerate.svg|width=250px|image2=Estradiol valerate molecule ball.png|width2=250px


<!--Clinical data-->|tradename=Progynova, Delestrogen, Progynon Depot, dll.|pregnancy_AU=<!-- A / B1 / B2 / B3 / C / D / X -->|pregnancy_US=<!-- A / B / C / D / X -->|pregnancy_category=|legal_AU=<!-- Unscheduled / S2 / S3 / S4 / S5 / S6 / S7 / S8 / S9 -->|legal_CA=|legal_UK=|legal_US=|legal_status=Rx-only|routes_of_administration=Diminum, dihisap, injeksi intramuskular,<ref name="Zink1988">{{cite book | author = Christoph Zink | title = Dictionary of Obstetrics and Gynecology | url = https://books.google.com/books?id=EQlvzV9V7xIC&pg=PA86 | accessdate = 20 May 2012 | date = 1 January 1988 | publisher = Walter de Gruyter | isbn = 978-3-11-085727-6 | page = 86}}</ref> [[subkutan|injeksi subkutan]]|bioavailability=Oral: 3–5%<ref name="pmid7169965" /><ref name="pmid16112947" /><br />{{abbr|IM|Injeksi intramuskular}}: 100%<ref name="pmid7169965" />|protein_bound=Estradiol: ~98% ([[albumin serum manusia|albumin]] dan {{abbrlink|SHBG|globulin pengikat hormon seks}})<ref name="StanczykArcher2013">{{cite journal|last1=Stanczyk|first1=Frank Z.|last2=Archer|first2=David F.|last3=Bhavnani|first3=Bhagu R.|title=Ethinyl estradiol and 17β-estradiol in combined oral contraceptives: pharmacokinetics, pharmacodynamics and risk assessment|journal=Contraception|volume=87|issue=6|year=2013|pages=706–727|issn=0010-7824|doi=10.1016/j.contraception.2012.12.011|pmid=23375353}}</ref><ref name="FalconeHurd2007">{{cite book|author1=Tommaso Falcone|author2=William W. Hurd|title=Clinical Reproductive Medicine and Surgery|url=https://books.google.com/books?id=fOPtaEIKvcIC&pg=PA22|year=2007|publisher=Elsevier Health Sciences|isbn=978-0-323-03309-1|pages=22,362,388}}</ref>|elimination_half-life=Oral: 12–20 jam (sbg. {{abbrlink|E2|estradiol}})<ref name="pmid7169965" /><ref name="StanczykArcher2013">{{cite journal|last1=Stanczyk|first1=Frank Z.|last2=Archer|first2=David F.|last3=Bhavnani|first3=Bhagu R.|title=Ethinyl estradiol and 17β-estradiol in combined oral contraceptives: pharmacokinetics, pharmacodynamics and risk assessment|journal=Contraception|volume=87|issue=6|year=2013|pages=706–727|issn=0010-7824|doi=10.1016/j.contraception.2012.12.011|pmid=23375353}}</ref><br />{{abbr|IM|Injeksi intramuskular}}: 4–5 hari<ref name="pmid7169965" />|excretion=[[Urin]] (80%)<ref name="pmid7169965" />
<!--Clinical data-->|tradename=Progynova, Delestrogen, Progynon Depot, dll.|pregnancy_AU=<!-- A / B1 / B2 / B3 / C / D / X -->|pregnancy_US=<!-- A / B / C / D / X -->|pregnancy_category=|legal_AU=<!-- Unscheduled / S2 / S3 / S4 / S5 / S6 / S7 / S8 / S9 -->|legal_CA=|legal_UK=|legal_US=|legal_status=Rx-only|routes_of_administration=Diminum, dihisap, injeksi intramuskular,<ref name="Zink1988">{{cite book | author = Christoph Zink | title = Dictionary of Obstetrics and Gynecology | url = https://books.google.com/books?id=EQlvzV9V7xIC&pg=PA86 | date = 1988-01-01 | publisher = Walter de Gruyter | isbn = 978-3-11-085727-6 | page = 86}}</ref> [[subkutan|injeksi subkutan]]|bioavailability=Oral: 3–5%<ref name="pmid7169965" /><ref name="pmid16112947" /><br />{{abbr|IM|Injeksi intramuskular}}: 100%<ref name="pmid7169965" />|protein_bound=Estradiol: ~98% ([[albumin serum manusia|albumin]] dan {{abbrlink|SHBG|globulin pengikat hormon seks}})<ref name="StanczykArcher2013">{{cite journal|last1=Stanczyk|first1=Frank Z.|last2=Archer|first2=David F.|last3=Bhavnani|first3=Bhagu R.|title=Ethinyl estradiol and 17β-estradiol in combined oral contraceptives: pharmacokinetics, pharmacodynamics and risk assessment|journal=Contraception|volume=87|issue=6|year=2013|pages=706–727|issn=0010-7824|doi=10.1016/j.contraception.2012.12.011|pmid=23375353}}</ref><ref name="FalconeHurd2007">{{cite book|author1=Tommaso Falcone|author2=William W. Hurd|title=Clinical Reproductive Medicine and Surgery|url=https://books.google.com/books?id=fOPtaEIKvcIC&pg=PA22|year=2007|publisher=Elsevier Health Sciences|isbn=978-0-323-03309-1|pages=22,362,388}}</ref>|elimination_half-life=Oral: 12–20 jam (sbg. {{abbrlink|E2|estradiol}})<ref name="pmid7169965" /><ref name="StanczykArcher2013">{{cite journal|last1=Stanczyk|first1=Frank Z.|last2=Archer|first2=David F.|last3=Bhavnani|first3=Bhagu R.|title=Ethinyl estradiol and 17β-estradiol in combined oral contraceptives: pharmacokinetics, pharmacodynamics and risk assessment|journal=Contraception|volume=87|issue=6|year=2013|pages=706–727|issn=0010-7824|doi=10.1016/j.contraception.2012.12.011|pmid=23375353}}</ref><br />{{abbr|IM|Injeksi intramuskular}}: 4–5 hari<ref name="pmid7169965" />|excretion=[[Urin]] (80%)<ref name="pmid7169965" />


<!-- Identifiers -->|CAS_number_Ref=|CAS_number=979-32-8|CAS_supplemental=|ATC_prefix=G03|ATC_suffix=CA03|ATC_supplemental=|PubChem=13791|IUPHAR_ligand=|DrugBank=DB13956|ChemSpiderID_Ref=|ChemSpiderID=13194|UNII=OKG364O896|KEGG=D01413|ChEBI=31561|ChEMBL=1511|synonyms=EV; E2V; Oestradiol valerat; Estradiol pentanoat; Estradiol valerianat
<!-- Identifiers -->|CAS_number_Ref=|CAS_number=979-32-8|CAS_supplemental=|ATC_prefix=G03|ATC_suffix=CA03|ATC_supplemental=|PubChem=13791|IUPHAR_ligand=|DrugBank=DB13956|ChemSpiderID_Ref=|ChemSpiderID=13194|UNII=OKG364O896|KEGG=D01413|ChEBI=31561|ChEMBL=1511|synonyms=EV; E2V; Oestradiol valerat; Estradiol pentanoat; Estradiol valerianat
Baris 7: Baris 7:
<!--Chemical data-->|C=23|H=32|O=3|molecular_weight=356.498 g/mol|smiles=CCCCC(=O)O[C@H]1CC[C@@H]2[C@@]1(CC[C@H]3[C@H]2CCC4=C3C=CC(=C4)O)C|StdInChI_Ref=|StdInChI=1S/C23H32O3/c1-3-4-5-22(25)26-21-11-10-20-19-8-6-15-14-16(24)7-9-17(15)18(19)12-13-23(20,21)2/h7,9,14,18-21,24H,3-6,8,10-13H2,1-2H3/t18-,19-,20+,21+,23+/m1/s1|StdInChIKey_Ref=|StdInChIKey=RSEPBGGWRJCQGY-RBRWEJTLSA-N}}'''Estradiol valerat''' ('''EV'''), dikenal pula dengan nama antara lain '''Progynova''' (oral), '''Delestrogen''', atau '''Progynon Depot''' (injeksi) adalah suatu jenis [[Estrogen (obat)|estrogen]]. Estradiol valerat pada perempuan digunakan dalam [[terapi penyulihan hormon]] pada kasus [[menopause]] dan [[Hipoestrogen|kekurangan estrogen]], [[Terapi hormon feminin|terapi hormon]] bagi [[wanita transgender]], dan [[Kontrasepsi hormonal|obat kontrasepsi]] sementara pada laki-laki digunakan untuk pengobatan [[kanker prostat]].<ref name="pmid16112947">{{Cite journal|year=2005|title=Pharmacology of estrogens and progestogens: influence of different routes of administration|url=http://hormonebalance.org/images/documents/Kuhl%2005%20%20Pharm%20Estro%20Progest%20Climacteric_1313155660.pdf|journal=Climacteric|volume=8 Suppl 1|issue=|pages=3–63|doi=10.1080/13697130500148875|pmid=16112947}}</ref><ref name="pmid7169965">{{Cite journal|date=December 1982|title=Pharmacokinetic and pharmacological features of oestradiol valerate|url=|journal=Maturitas|volume=4|issue=4|pages=315–24|doi=10.1016/0378-5122(82)90064-0|pmid=7169965}}</ref><ref name="Delestrogen-Label">https://www.accessdata.fda.gov/drugsatfda_docs/label/2017/009402s052lbl.pdf</ref><ref name="Progynova-Label">[http://www.bayerresources.com.au/resources/uploads/pi/file9418.pdf PRODUCT INFORMATION PROGYNOVA®]</ref> Estradiol valerat dikonsumsi dengan cara diminum harian atau melalui injeksi intramuskular setiap beberapa minggu.<ref name="Delestrogen-Label" /><ref name="Progynova-Label" />
<!--Chemical data-->|C=23|H=32|O=3|molecular_weight=356.498 g/mol|smiles=CCCCC(=O)O[C@H]1CC[C@@H]2[C@@]1(CC[C@H]3[C@H]2CCC4=C3C=CC(=C4)O)C|StdInChI_Ref=|StdInChI=1S/C23H32O3/c1-3-4-5-22(25)26-21-11-10-20-19-8-6-15-14-16(24)7-9-17(15)18(19)12-13-23(20,21)2/h7,9,14,18-21,24H,3-6,8,10-13H2,1-2H3/t18-,19-,20+,21+,23+/m1/s1|StdInChIKey_Ref=|StdInChIKey=RSEPBGGWRJCQGY-RBRWEJTLSA-N}}'''Estradiol valerat''' ('''EV'''), dikenal pula dengan nama antara lain '''Progynova''' (oral), '''Delestrogen''', atau '''Progynon Depot''' (injeksi) adalah suatu jenis [[Estrogen (obat)|estrogen]]. Estradiol valerat pada perempuan digunakan dalam [[terapi penyulihan hormon]] pada kasus [[menopause]] dan [[Hipoestrogen|kekurangan estrogen]], [[Terapi hormon feminin|terapi hormon]] bagi [[wanita transgender]], dan [[Kontrasepsi hormonal|obat kontrasepsi]] sementara pada laki-laki digunakan untuk pengobatan [[kanker prostat]].<ref name="pmid16112947">{{Cite journal|year=2005|title=Pharmacology of estrogens and progestogens: influence of different routes of administration|url=http://hormonebalance.org/images/documents/Kuhl%2005%20%20Pharm%20Estro%20Progest%20Climacteric_1313155660.pdf|journal=Climacteric|volume=8 Suppl 1|issue=|pages=3–63|doi=10.1080/13697130500148875|pmid=16112947}}</ref><ref name="pmid7169965">{{Cite journal|date=December 1982|title=Pharmacokinetic and pharmacological features of oestradiol valerate|url=|journal=Maturitas|volume=4|issue=4|pages=315–24|doi=10.1016/0378-5122(82)90064-0|pmid=7169965}}</ref><ref name="Delestrogen-Label">https://www.accessdata.fda.gov/drugsatfda_docs/label/2017/009402s052lbl.pdf</ref><ref name="Progynova-Label">[http://www.bayerresources.com.au/resources/uploads/pi/file9418.pdf PRODUCT INFORMATION PROGYNOVA®]</ref> Estradiol valerat dikonsumsi dengan cara diminum harian atau melalui injeksi intramuskular setiap beberapa minggu.<ref name="Delestrogen-Label" /><ref name="Progynova-Label" />


Efek samping dari estradiol valerat di antaranya adalah [[Nyeri payudara|payudara yang nyeri]] atau [[Pertumbuhan payudara|membesar]], [[mual]], [[sakit kepala]], dan kesulitan buang air kecil.<ref name="Ghosh2010"/><ref name="Delestrogen-Label">https://www.accessdata.fda.gov/drugsatfda_docs/label/2017/009402s052lbl.pdf</ref><ref name="Progynova-Label"/> Estradiol valerat merupakan sebuah estrogen sintesis sehingga merupakan sebuah [[agonis]] [[Reseptor estrogen|reseptor estrogen—]]<nowiki/>target biologis dari hormon [[estrogen]] seperti [[estradiol]].<ref name="pmid16112947">{{Cite journal|year=2005|title=Pharmacology of estrogens and progestogens: influence of different routes of administration|url=http://hormonebalance.org/images/documents/Kuhl%2005%20%20Pharm%20Estro%20Progest%20Climacteric_1313155660.pdf|journal=Climacteric|volume=8 Suppl 1|issue=|pages=3–63|doi=10.1080/13697130500148875|pmid=16112947}}</ref><ref name="pmid7169965">{{Cite journal|date=December 1982|title=Pharmacokinetic and pharmacological features of oestradiol valerate|url=|journal=Maturitas|volume=4|issue=4|pages=315–24|doi=10.1016/0378-5122(82)90064-0|pmid=7169965}}</ref><ref name="OettelSchillinger2012" /> Obat ini juga merupakan ester estrogen serta [[bakal obat]] estradiol dalam tubuh.<ref name="OettelSchillinger2012" /><ref name="pmid16112947" /><ref name="pmid7169965" /> Karena itu, estradiol valerat dinilai sebagai sebuah bentuk [[Produk alami|natural]] dan bioidentik dari estrogen.<ref name="OettelSchillinger2012">{{Cite book|last=Michael Oettel|last2=Ekkehard Schillinger|title=Estrogens and Antiestrogens II: Pharmacology and Clinical Application of Estrogens and Antiestrogen|url=https://books.google.com/books?id=wBvyCAAAQBAJ&pg=PA261|date=6 December 2012|publisher=Springer Science & Business Media|isbn=978-3-642-60107-1|page=261|quote=Natural estrogens considered here include: [...] Esters of 17β-estradiol, such as estradiol valerate, estradiol benzoate and estradiol cypionate. Esterification aims at either better absorption after oral administration or a sustained release from the depot after intramuscular administration. During absorption, the esters are cleaved by endogenous esterases and the pharmacologically active 17β-estradiol is released; therefore, the esters are considered as natural estrogens.}}</ref><ref name="pmid17627398">{{Cite journal|date=June 2007|title=Bioidentical hormone therapy: a review of the evidence|url=|journal=J Womens Health (Larchmt)|volume=16|issue=5|pages=600–31|doi=10.1089/jwh.2006.0311|pmid=17627398}}</ref><ref name="pmid7169965" /><ref name="ArunNarendra2012">{{Cite book|last=Nagrath Arun|last2=Malhotra Narendra|last3=Seth Shikha|title=Progress in Obstetrics and Gynecology--3|url=https://books.google.com/books?id=AS3UBAAAQBAJ&pg=PA419|date=15 December 2012|publisher=Jaypee Brothers Medical Publishers Pvt. Ltd.|isbn=978-93-5090-575-3|pages=419–}}</ref>
Efek samping dari estradiol valerat di antaranya adalah [[Nyeri payudara|payudara yang nyeri]] atau [[Pertumbuhan payudara|membesar]], [[mual]], [[sakit kepala]], dan kesulitan buang air kecil.<ref name="Ghosh2010"/><ref name="Delestrogen-Label">https://www.accessdata.fda.gov/drugsatfda_docs/label/2017/009402s052lbl.pdf</ref><ref name="Progynova-Label"/> Estradiol valerat merupakan sebuah estrogen sintesis sehingga merupakan sebuah [[agonis]] [[Reseptor estrogen|reseptor estrogen—]]<nowiki/>target biologis dari hormon [[estrogen]] seperti [[estradiol]].<ref name="pmid16112947">{{Cite journal|year=2005|title=Pharmacology of estrogens and progestogens: influence of different routes of administration|url=http://hormonebalance.org/images/documents/Kuhl%2005%20%20Pharm%20Estro%20Progest%20Climacteric_1313155660.pdf|journal=Climacteric|volume=8 Suppl 1|issue=|pages=3–63|doi=10.1080/13697130500148875|pmid=16112947}}</ref><ref name="pmid7169965">{{Cite journal|date=December 1982|title=Pharmacokinetic and pharmacological features of oestradiol valerate|url=|journal=Maturitas|volume=4|issue=4|pages=315–24|doi=10.1016/0378-5122(82)90064-0|pmid=7169965}}</ref><ref name="OettelSchillinger2012" /> Obat ini juga merupakan ester estrogen serta [[bakal obat]] estradiol dalam tubuh.<ref name="OettelSchillinger2012" /><ref name="pmid16112947" /><ref name="pmid7169965" /> Karena itu, estradiol valerat dinilai sebagai sebuah bentuk [[Produk alami|natural]] dan bioidentik dari estrogen.<ref name="OettelSchillinger2012">{{Cite book|last=Michael Oettel|last2=Ekkehard Schillinger|title=Estrogens and Antiestrogens II: Pharmacology and Clinical Application of Estrogens and Antiestrogen|url=https://books.google.com/books?id=wBvyCAAAQBAJ&pg=PA261|date=2012|publisher=Springer Science & Business Media|isbn=978-3-642-60107-1|page=261|quote=Natural estrogens considered here include: [...] Esters of 17β-estradiol, such as estradiol valerate, estradiol benzoate and estradiol cypionate. Esterification aims at either better absorption after oral administration or a sustained release from the depot after intramuscular administration. During absorption, the esters are cleaved by endogenous esterases and the pharmacologically active 17β-estradiol is released; therefore, the esters are considered as natural estrogens.|first=|year=|location=}}</ref><ref name="pmid17627398">{{Cite journal|date=June 2007|title=Bioidentical hormone therapy: a review of the evidence|url=|journal=J Womens Health (Larchmt)|volume=16|issue=5|pages=600–31|doi=10.1089/jwh.2006.0311|pmid=17627398}}</ref><ref name="pmid7169965" /><ref name="ArunNarendra2012">{{Cite book|last=Nagrath Arun|last2=Malhotra Narendra|last3=Seth Shikha|title=Progress in Obstetrics and Gynecology--3|url=https://books.google.com/books?id=AS3UBAAAQBAJ&pg=PA419|date=2012|publisher=Jaypee Brothers Medical Publishers Pvt. Ltd.|isbn=978-93-5090-575-3|pages=419–|first=|year=|location=|page=}}</ref>


== Kegunaan medis ==
== Kegunaan medis ==
Estradiol valerat digunakan serupa dengan estradiol dan estrogen lainnya. Obat ini digunakan dalam terapi penyulihan hormon dan sebagai hormon kontrasepsi. Sebagai kontrasepsi, estradiol valerat tersedia dalam kombinasi dengan [[progestin]] ([[dienogest]]).<ref name="pmid21151673">{{Cite journal|year=2010|title=Review of the safety, efficacy and patient acceptability of the combined dienogest/estradiol valerate contraceptive pill|url=|journal=International Journal of Women's Health|volume=2|issue=|pages=279–90|doi=10.2147/IJWH.S6954|pmc=2990895|pmid=21151673}}</ref> Estradiol valerat bersama [[estradiol sipionat]], [[estradiol undesilat]],dan [[estradiol benzoat]] merupakan bentuk-bentuk estrogen yang digunakan dalam [[terapi hormon feminin]] bagi wanita transgender.<ref name="pmid28159148">{{Cite journal|date=March 2017|title=Hormonal and Surgical Treatment Options for Transgender Women and Transfeminine Spectrum Persons|url=|journal=Psychiatr. Clin. North Am.|volume=40|issue=1|pages=99–111|doi=10.1016/j.psc.2016.10.006|pmid=28159148}}</ref><ref name="pmid25220381">{{Cite journal|date=December 2014|title=Gonadal suppressive and cross-sex hormone therapy for gender dysphoria in adolescents and adults|url=|journal=Pharmacotherapy|volume=34|issue=12|pages=1282–97|doi=10.1002/phar.1487|pmid=25220381}}</ref><ref name="EttnerMonstrey2016">{{Cite book|last=Randi Ettner|last2=Stan Monstrey|last3=Eli Coleman|title=Principles of Transgender Medicine and Surgery|url=https://books.google.com/books?id=LwszDAAAQBAJ&pg=PA216|date=20 May 2016|publisher=Routledge|isbn=978-1-317-51460-2|pages=216–}}</ref><ref name="IsraelTarver2001">{{Cite book|last=Gianna E. Israel|last2=Donald E. Tarver|last3=Joy Diane Shaffer|title=Transgender Care: Recommended Guidelines, Practical Information, and Personal Accounts|url=https://books.google.com/books?id=IlPX6E5glDEC&pg=PA64|date=1 March 2001|publisher=Temple University Press|isbn=978-1-56639-852-7|pages=64–}}</ref> Obat ini juga digunakan dalam untuk pengobatan kanker prostat pada pria.<ref name="Delestrogen-Label">https://www.accessdata.fda.gov/drugsatfda_docs/label/2017/009402s052lbl.pdf</ref>
Estradiol valerat digunakan serupa dengan estradiol dan estrogen lainnya. Obat ini digunakan dalam terapi penyulihan hormon dan sebagai hormon kontrasepsi. Sebagai kontrasepsi, estradiol valerat tersedia dalam kombinasi dengan [[progestin]] ([[dienogest]]).<ref name="pmid21151673">{{Cite journal|year=2010|title=Review of the safety, efficacy and patient acceptability of the combined dienogest/estradiol valerate contraceptive pill|url=|journal=International Journal of Women's Health|volume=2|issue=|pages=279–90|doi=10.2147/IJWH.S6954|pmc=2990895|pmid=21151673}}</ref> Estradiol valerat bersama [[estradiol sipionat]], [[estradiol undesilat]],dan [[estradiol benzoat]] merupakan bentuk-bentuk estrogen yang digunakan dalam [[terapi hormon feminin]] bagi wanita transgender.<ref name="pmid28159148">{{Cite journal|last=|first=|date=2017|year=|title=Hormonal and Surgical Treatment Options for Transgender Women and Transfeminine Spectrum Persons|url=|journal=Psychiatr. Clin. North Am.|volume=40|issue=1|pages=99–111|doi=10.1016/j.psc.2016.10.006|pmid=28159148}}</ref><ref name="pmid25220381">{{Cite journal|last=|first=|date=2014|year=|title=Gonadal suppressive and cross-sex hormone therapy for gender dysphoria in adolescents and adults|url=|journal=Pharmacotherapy|volume=34|issue=12|pages=1282–97|doi=10.1002/phar.1487|pmid=25220381}}</ref><ref name="EttnerMonstrey2016">{{Cite book|last=Randi Ettner|last2=Stan Monstrey|last3=Eli Coleman|title=Principles of Transgender Medicine and Surgery|url=https://books.google.com/books?id=LwszDAAAQBAJ&pg=PA216|date=2016|publisher=Routledge|isbn=978-1-317-51460-2|pages=216–|first=|year=|location=|page=}}</ref><ref name="IsraelTarver2001">{{Cite book|last=Gianna E. Israel|last2=Donald E. Tarver|last3=Joy Diane Shaffer|title=Transgender Care: Recommended Guidelines, Practical Information, and Personal Accounts|url=https://books.google.com/books?id=IlPX6E5glDEC&pg=PA64|date=2001|publisher=Temple University Press|isbn=978-1-56639-852-7|pages=64–|first=|year=|location=|page=}}</ref> Obat ini juga digunakan dalam untuk pengobatan kanker prostat pada pria.<ref name="Delestrogen-Label">https://www.accessdata.fda.gov/drugsatfda_docs/label/2017/009402s052lbl.pdf</ref>


== Kontraindikasi ==
== Kontraindikasi ==

Revisi per 31 Juli 2019 11.55

Estradiol valerat
Nama sistematis (IUPAC)
[(8R,9S,13S,14S,17S)-3-hydroxy-13-methyl-6,7,8,9,11,12,14,15,16,17-decahydrocyclopenta[a]phenanthren-17-yl] pentanoate
Data klinis
Nama dagang Progynova, Delestrogen, Progynon Depot, dll.
Kat. kehamilan ?
Status hukum ℞ Preskripsi saja
Rute Diminum, dihisap, injeksi intramuskular,[1] injeksi subkutan
Data farmakokinetik
Bioavailabilitas Oral: 3–5%[2][3]
IM: 100%[2]
Ikatan protein Estradiol: ~98% (albumin dan SHBG)[4][5]
Waktu paruh Oral: 12–20 jam (sbg. E2)[2][4]
IM: 4–5 hari[2]
Ekskresi Urin (80%)[2]
Pengenal
Nomor CAS 979-32-8
Kode ATC G03CA03
PubChem CID 13791
DrugBank DB13956
ChemSpider 13194
UNII OKG364O896
KEGG D01413
ChEBI CHEBI:31561
ChEMBL CHEMBL1511
Sinonim EV; E2V; Oestradiol valerat; Estradiol pentanoat; Estradiol valerianat
Data kimia
Rumus C23H32O3 
Massa mol. 356.498 g/mol
SMILES eMolecules & PubChem

  • InChI=1S/C23H32O3/c1-3-4-5-22(25)26-21-11-10-20-19-8-6-15-14-16(24)7-9-17(15)18(19)12-13-23(20,21)2/h7,9,14,18-21,24H,3-6,8,10-13H2,1-2H3/t18-,19-,20+,21+,23+/m1/s1
    Key:RSEPBGGWRJCQGY-RBRWEJTLSA-N

Estradiol valerat (EV), dikenal pula dengan nama antara lain Progynova (oral), Delestrogen, atau Progynon Depot (injeksi) adalah suatu jenis estrogen. Estradiol valerat pada perempuan digunakan dalam terapi penyulihan hormon pada kasus menopause dan kekurangan estrogen, terapi hormon bagi wanita transgender, dan obat kontrasepsi sementara pada laki-laki digunakan untuk pengobatan kanker prostat.[3][2][6][7] Estradiol valerat dikonsumsi dengan cara diminum harian atau melalui injeksi intramuskular setiap beberapa minggu.[6][7]

Efek samping dari estradiol valerat di antaranya adalah payudara yang nyeri atau membesar, mual, sakit kepala, dan kesulitan buang air kecil.[8][6][7] Estradiol valerat merupakan sebuah estrogen sintesis sehingga merupakan sebuah agonis reseptor estrogen—target biologis dari hormon estrogen seperti estradiol.[3][2][9] Obat ini juga merupakan ester estrogen serta bakal obat estradiol dalam tubuh.[9][3][2] Karena itu, estradiol valerat dinilai sebagai sebuah bentuk natural dan bioidentik dari estrogen.[9][10][2][11]

Kegunaan medis

Estradiol valerat digunakan serupa dengan estradiol dan estrogen lainnya. Obat ini digunakan dalam terapi penyulihan hormon dan sebagai hormon kontrasepsi. Sebagai kontrasepsi, estradiol valerat tersedia dalam kombinasi dengan progestin (dienogest).[12] Estradiol valerat bersama estradiol sipionat, estradiol undesilat,dan estradiol benzoat merupakan bentuk-bentuk estrogen yang digunakan dalam terapi hormon feminin bagi wanita transgender.[13][14][15][16] Obat ini juga digunakan dalam untuk pengobatan kanker prostat pada pria.[6]

Kontraindikasi

Estradiol valerat memiliki kontraindikasi terhadap riwayat penggumpalan darah, penyakit kardiovaskular, penyakit hati, serta kanker sensitif hormon seperti kanker payudara dan kanker endometrium.[17][18][19][20]

Efek samping

Efek samping dari estradiol valerat umumnya sama dengan estradiol lainnya seperti payudara yang nyeri dan membesar, mual, edema, sakit kepala, dan melasma.[8][21] Terapi estrogen dosis tinggi melalui injeksi estradiol valerat dapat meningkatkan risiko trombosis vena, perubahan profil lipid darah, peningkatan resistensi insulin, serta peningkatan prolaktin.[21]

Referensi

  1. ^ Christoph Zink (1988-01-01). Dictionary of Obstetrics and Gynecology. Walter de Gruyter. hlm. 86. ISBN 978-3-11-085727-6. 
  2. ^ a b c d e f g h i "Pharmacokinetic and pharmacological features of oestradiol valerate". Maturitas. 4 (4): 315–24. December 1982. doi:10.1016/0378-5122(82)90064-0. PMID 7169965. 
  3. ^ a b c d "Pharmacology of estrogens and progestogens: influence of different routes of administration" (PDF). Climacteric. 8 Suppl 1: 3–63. 2005. doi:10.1080/13697130500148875. PMID 16112947. 
  4. ^ a b Stanczyk, Frank Z.; Archer, David F.; Bhavnani, Bhagu R. (2013). "Ethinyl estradiol and 17β-estradiol in combined oral contraceptives: pharmacokinetics, pharmacodynamics and risk assessment". Contraception. 87 (6): 706–727. doi:10.1016/j.contraception.2012.12.011. ISSN 0010-7824. PMID 23375353. 
  5. ^ Tommaso Falcone; William W. Hurd (2007). Clinical Reproductive Medicine and Surgery. Elsevier Health Sciences. hlm. 22,362,388. ISBN 978-0-323-03309-1. 
  6. ^ a b c d https://www.accessdata.fda.gov/drugsatfda_docs/label/2017/009402s052lbl.pdf
  7. ^ a b c PRODUCT INFORMATION PROGYNOVA®
  8. ^ a b Ghosh, Amit K. (2010). Mayo Clinic Internal Medicine Board Review. OUP USA. hlm. 222–. ISBN 978-0-19-975569-1. 
  9. ^ a b c Michael Oettel; Ekkehard Schillinger (2012). Estrogens and Antiestrogens II: Pharmacology and Clinical Application of Estrogens and Antiestrogen. Springer Science & Business Media. hlm. 261. ISBN 978-3-642-60107-1. Natural estrogens considered here include: [...] Esters of 17β-estradiol, such as estradiol valerate, estradiol benzoate and estradiol cypionate. Esterification aims at either better absorption after oral administration or a sustained release from the depot after intramuscular administration. During absorption, the esters are cleaved by endogenous esterases and the pharmacologically active 17β-estradiol is released; therefore, the esters are considered as natural estrogens. 
  10. ^ "Bioidentical hormone therapy: a review of the evidence". J Womens Health (Larchmt). 16 (5): 600–31. June 2007. doi:10.1089/jwh.2006.0311. PMID 17627398. 
  11. ^ Nagrath Arun; Malhotra Narendra; Seth Shikha (2012). Progress in Obstetrics and Gynecology--3. Jaypee Brothers Medical Publishers Pvt. Ltd. hlm. 419–. ISBN 978-93-5090-575-3. 
  12. ^ "Review of the safety, efficacy and patient acceptability of the combined dienogest/estradiol valerate contraceptive pill". International Journal of Women's Health. 2: 279–90. 2010. doi:10.2147/IJWH.S6954. PMC 2990895 alt=Dapat diakses gratis. PMID 21151673. 
  13. ^ "Hormonal and Surgical Treatment Options for Transgender Women and Transfeminine Spectrum Persons". Psychiatr. Clin. North Am. 40 (1): 99–111. 2017. doi:10.1016/j.psc.2016.10.006. PMID 28159148. 
  14. ^ "Gonadal suppressive and cross-sex hormone therapy for gender dysphoria in adolescents and adults". Pharmacotherapy. 34 (12): 1282–97. 2014. doi:10.1002/phar.1487. PMID 25220381. 
  15. ^ Randi Ettner; Stan Monstrey; Eli Coleman (2016). Principles of Transgender Medicine and Surgery. Routledge. hlm. 216–. ISBN 978-1-317-51460-2. 
  16. ^ Gianna E. Israel; Donald E. Tarver; Joy Diane Shaffer (2001). Transgender Care: Recommended Guidelines, Practical Information, and Personal Accounts. Temple University Press. hlm. 64–. ISBN 978-1-56639-852-7. 
  17. ^ "Clinical use of oestrogens and progestogens". Maturitas. 12 (3): 199–214. September 1990. doi:10.1016/0378-5122(90)90004-P. PMID 2215269. 
  18. ^ Christian Lauritzen; John W. W. Studd (22 June 2005). Current Management of the Menopause. CRC Press. hlm. 95–98,488. ISBN 978-0-203-48612-2. 
  19. ^ Laurtizen, Christian (2001). "Hormone Substitution Before, During and After Menopause" (PDF). Dalam Fisch. Menopause – Andropause: Hormone Replacement Therapy Through the Ages. Krause & Pachernegg: Gablitz. hlm. 67–88. ISBN 978-3-901299-34-6. 
  20. ^ Midwinter, Audrey (1976). "Contraindications to estrogen therapy and management of the menopausal syndrome in these cases". Dalam Campbell. The Management of the Menopause & Post-Menopausal Years: The Proceedings of the International Symposium held in London 24–26 November 1975 Arranged by the Institute of Obstetrics and Gynaecology, The University of London. MTP Press Limited. hlm. 377–382. doi:10.1007/978-94-011-6165-7_33. ISBN 978-94-011-6167-1. 
  21. ^ a b "Pharmacotherapy Considerations in the Management of Transgender Patients: A Brief Review". Pharmacotherapy. 35 (12): 1130–9. December 2015. doi:10.1002/phar.1668. PMID 26684553. 
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