Etinilestradiol
senyawa kimia
Etinilestradiol (EE) adalah obat estrogen yang digunakan secara luas dalam pil kontrasepsi, dalam campuran dengan progestin..[10][11] Sebelumnya, EE digunakan untuk berbagai indikasi, seperti pengobatan gejala menopause, kelainan ginekologi, serta kanker sensitif hormon tertentu. Obat ini biasanya diminum tetapi kadang juga dihantarkan melalui kulit dengan pelekat transdermal, atau melalui gelang vaginal.[10][12]
Nama sistematis (IUPAC) | |
---|---|
(8R,9S,13S,14S,17R)-17-ethynyl-13-methyl-7,8,9,11,12,14,15,16-octahydro-6H-cyclopenta[a]phenanthrene-3,17-diol | |
Data klinis | |
Nama dagang | Numerous |
AHFS/Drugs.com | International Drug Names |
MedlinePlus | a604032 |
Data lisensi | EMA:pranala |
Kat. kehamilan | X (USA) |
Status hukum | ℞ Preskripsi saja |
Rute | • By mouth (tablet) • Transdermal (patch) • Vaginal (ring) |
Data farmakokinetik | |
Bioavailabilitas | 38–48%[1][2][3] |
Ikatan protein | 97–98% (to albumin;[4] is not bound to SHBG)[5] |
Metabolisme | Liver (primarily CYP3A4)[6] |
Waktu paruh | 7–36 hours[1][6][7][8] |
Ekskresi | Feces: 62%[7] Urine: 38%[7] |
Pengenal | |
Nomor CAS | 57-63-6 |
Kode ATC | G03CA01 L02AA03 |
PubChem | CID 5991 |
Ligan IUPHAR | 7071 |
DrugBank | DB00977 |
ChemSpider | 5770 |
UNII | 423D2T571U |
KEGG | D00554 |
ChEBI | CHEBI:4903 |
ChEMBL | CHEMBL691 |
Sinonim | Ethynylestradiol; Ethinyl estradiol; Ethinyl oestradiol; EE; EE2; 17α-Ethynylestradiol; 17α-Ethynylestra-1,3,5(10)-triene-3,17β-diol; NSC-10973[9] |
Data kimia | |
Rumus | C20H24O2 |
| |
Data fisik | |
Titik lebur | 182–184 °C (360–363 °F) |
Referensi
sunting- ^ a b Goldzieher JW, Brody SA (1990). "Pharmacokinetics of ethinyl estradiol and mestranol". American Journal of Obstetrics and Gynecology. 163 (6 Pt 2): 2114–9. doi:10.1016/0002-9378(90)90550-Q. PMID 2256522.
- ^ Fruzzetti F, Trémollieres F, Bitzer J (2012). "An overview of the development of combined oral contraceptives containing estradiol: focus on estradiol valerate/dienogest". Gynecological Endocrinology. 28 (5): 400–8. doi:10.3109/09513590.2012.662547. PMC 3399636 . PMID 22468839.
- ^ Fotherby K (August 1996). "Bioavailability of orally administered sex steroids used in oral contraception and hormone replacement therapy". Contraception. 54 (2): 59–69. doi:10.1016/0010-7824(96)00136-9. PMID 8842581.
- ^ Facts and Comparisons (Firm); Ovid Technologies, Inc (2005). Drug Facts and Comparisons 2005: Pocket Version. Facts and Comparisons. hlm. 121. ISBN 978-1-57439-179-4.
- ^ Micromedex (1 January 2003). USP DI 2003: Drug Information for Healthcare Professionals. Thomson Micromedex. hlm. 1253, 1258, 1266. ISBN 978-1-56363-429-1.
- ^ a b Claude L Hughes; Michael D. Waters (23 March 2016). Translational Toxicology: Defining a New Therapeutic Discipline. Humana Press. hlm. 73–. ISBN 978-3-319-27449-2.
- ^ a b c Kesalahan pengutipan: Tag
<ref>
tidak sah; tidak ditemukan teks untuk ref bernamapmid23375353
- ^ Kesalahan pengutipan: Tag
<ref>
tidak sah; tidak ditemukan teks untuk ref bernamaShellenberger1986
- ^ Kesalahan pengutipan: Tag
<ref>
tidak sah; tidak ditemukan teks untuk ref bernamaElks2014
- ^ a b Kuhl H (2005). "Pharmacology of estrogens and progestogens: influence of different routes of administration" (PDF). Climacteric. 8 Suppl 1: 3–63. doi:10.1080/13697130500148875. PMID 16112947.
- ^ Michael Oettel; Ekkehard Schillinger (6 December 2012). Estrogens and Antiestrogens II: Pharmacology and Clinical Application of Estrogens and Antiestrogen. Springer Science & Business Media. hlm. 4,10,15,165,247–248,276–291,363–408,424,514,540,543,581. ISBN 978-3-642-60107-1.
The binding affinity of EE2 for the estrogen receptor is similar to that of estradiol. [...] During daily intake, the EE2 levels increase up to a steady state which is reached after about 1 week.
- ^ Kesalahan pengutipan: Tag
<ref>
tidak sah; tidak ditemukan teks untuk ref bernamaDrugs@FDA