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| Data klinis | |
|---|---|
| Nama dagang | Androcur, Androcur Depot, Cyprostat, Siterone, dll |
| Nama lain | SH-80714; SH-714; NSC-81430; 1α,2α-Metilena-6-kloro-17α-hidroksi-δ6-progesteron asetate; 1α,2α-Metilena-6-kloro-17α-hidroksipregna-4,6-diena-3,20-diona asetat |
| AHFS/Drugs.com | Micromedex Detailed Consumer Information |
| Kategori kehamilan |
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| Rute pemberian | Oral, intramuskular |
| Kelas obat | Steroidal antiandrogen; Progestin; Progestogen ester; Antigonadotropin |
| Kode ATC | |
| Status hukum | |
| Status hukum |
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| Data farmakokinetika | |
| Bioavailabilitas | Oral: 68–100%[1][2] |
| Pengikatan protein | Albumin: 93% Bebas: 7%[3][4][5][6] |
| Metabolisme | Hati (CYP3A4)[11][12] |
| Metabolit | • 15β-OH-CPA (major)[1][7] • Cyproterone (minor)[8] • Acetic acid (minor)[8] |
| Waktu paruh eliminasi | Oral: 1,6–4,3 hari[8][9][10] IM: 3–4,3 hari[2][8][10] |
| Ekskresi | Feses: 70%[8] Urin: 30%[8] |
| Pengenal | |
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| Nomor CAS |
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| PubChem CID | |
| IUPHAR/BPS | |
| DrugBank | |
| ChemSpider | |
| UNII | |
| KEGG | |
| ChEBI | |
| ChEMBL | |
| CompTox Dashboard (EPA) | |
| ECHA InfoCard | 100.006.409 |
| Data sifat kimia dan fisik | |
| Rumus | C24H29ClO4 |
| Massa molar | 416,94 g·mol−1 |
| Model 3D (JSmol) | |
| Titik leleh | 200 hingga 201 °C (392 hingga 394 °F) |
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Siproteron asetat (bahasa Inggris: Cyproterone acetate, disingkat CPA), dijual sendiri dengan merek Androcur atau bersama dengan etinilestradiol dengan merek Diane atau Diane-35, adalah obat antiandrogen dan progestin yang digunakan dalam pengobatan kondisi yang bergantung pada androgen seperti jerawat, hirsutisme, pubertas dini, dan kanker prostat, serta sebagai komponen Terapi hormon feminin untuk individu transgender, dan dalam pil KB.[1][9][13][14][15] Obat ini diformulasikan dan digunakan baik sendiri maupun dalam kombinasi dengan estrogen. CPA diminum satu hingga tiga kali sehari.
Referensi
sunting- ^ a b c Kuhl H (2005). "Pharmacology of estrogens and progestogens: influence of different routes of administration". Climacteric. 8 (Suppl 1): 3–63. doi:10.1080/13697130500148875. PMID 16112947. S2CID 24616324.
- ^ a b Huber J, Zeillinger R, Schmidt J, Täuber U, Kuhnz W, Spona J (November 1988). "Pharmacokinetics of cyproterone acetate and its main metabolite 15 beta-hydroxy-cyproterone acetate in young healthy women". International Journal of Clinical Pharmacology, Therapy, and Toxicology. 26 (11): 555–561. PMID 2977383.
- ^ Bińkowska M, Woroń J (June 2015). "Progestogens in menopausal hormone therapy". Przeglad Menopauzalny = Menopause Review. 14 (2): 134–143. doi:10.5114/pm.2015.52154. PMC 4498031. PMID 26327902.
- ^ Schindler AE, Campagnoli C, Druckmann R, Huber J, Pasqualini JR, Schweppe KW, Thijssen JH (December 2003). "Classification and pharmacology of progestins". Maturitas. 46 Suppl 1 (Suppl 1): S7 – S16. doi:10.1016/j.maturitas.2003.09.014. PMID 14670641.
Since there is no binding of CPA to SHBG and CBG in the serum, 93% of the compound is bound to serum albumin.
- ^ Wakelin SH, Maibach HI, Archer CB (1 June 2002). Systemic Drug Treatment in Dermatology: A Handbook. CRC Press. hlm. 32–. ISBN 978-1-84076-013-2. Diarsipkan dari versi aslinya tanggal 14 January 2023. Diakses tanggal 27 September 2016.
It is almost exclusively bound to plasma albumin.
- ^ Hammond GL, Lähteenmäki PL, Lähteenmäki P, Luukkainen T (October 1982). "Distribution and percentages of non-protein bound contraceptive steroids in human serum". Journal of Steroid Biochemistry. 17 (4): 375–380. doi:10.1016/0022-4731(82)90629-X. PMID 6215538.
- ^ Frith RG, Phillipou G (February 1985). "15-Hydroxycyproterone acetate and cyproterone acetate levels in plasma and urine". Journal of Chromatography. 338 (1): 179–186. doi:10.1016/0378-4347(85)80082-7. PMID 3160716.
- ^ a b c d e f Weber GF (22 July 2015). Molecular Therapies of Cancer. Springer. hlm. 316–. ISBN 978-3-319-13278-5.
The terminal half-life is about 38 h. A portion of the drug is metabolized by hydrolysis to cyproterone and acetic acid. However, in contrast to many other steroid esters hydrolysis is not extensive, and much of the pharmacological activity is exerted by the acetate form. Excretion is about 70% in the feces, mainly in the form of glucuronidated metabolites, and about 30% in the urine, predominantly as non-conjugated metabolites.
- ^ a b Barradell LB, Faulds D (July 1994). "Cyproterone. A review of its pharmacology and therapeutic efficacy in prostate cancer". Drugs Aging. 5 (1): 59–80. doi:10.2165/00002512-199405010-00006. PMID 7919640. S2CID 260845477.
- ^ a b AAPL Newsletter (PDF). The Academy. 1998. Diarsipkan (PDF) dari versi aslinya tanggal 30 August 2017. Diakses tanggal 16 August 2016.
CPA is 100% bioavailable when taken orally with a half life of 38 hours. The injectable form reaches maximum plasma levels in 82 hours and has a half life of about 72 hours.
- ^ Dickman A (27 September 2012). Drugs in Palliative Care. OUP Oxford. hlm. 137–138. ISBN 978-0-19-966039-1.
- ^ Boarder M, Newby D, Navti P (25 March 2010). Pharmacology for Pharmacy and the Health Sciences: A Patient-centred Approach. OUP Oxford. hlm. 632–. ISBN 978-0-19-955982-4. Diarsipkan dari versi aslinya tanggal 6 July 2024. Diakses tanggal 27 September 2016.
- ^ Neumann F (1994). "The antiandrogen cyproterone acetate: discovery, chemistry, basic pharmacology, clinical use and tool in basic research". Exp. Clin. Endocrinol. 102 (1): 1–32. doi:10.1055/s-0029-1211261. PMID 8005205.
- ^ Neumann F (January 1977). "Pharmacology and potential use of cyproterone acetate". Horm. Metab. Res. 9 (1): 1–13. doi:10.1055/s-0028-1093574. PMID 66176. S2CID 7224893.
- ^ Neumann F, Töpert M (November 1986). "Pharmacology of antiandrogens". Journal of Steroid Biochemistry. 25 (5B): 885–95. doi:10.1016/0022-4731(86)90320-1. PMID 2949114.
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