تیبولون
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| داده‌های بالینی | |
|---|---|
| نام‌های تجاری | Livial, Tibella, Tibofem, others |
| نام‌های دیگر | TIB; ORG-OD-14; 7α-Methylnoretynodrel; 7α-Methyl-17α-ethynyl-19-nor-δ5(10)-testosterone; 17α-Ethynyl-7α-methylestr-5(10)-en-17β-ol-3-one; 7α-Methyl-19-nor-17α-pregn-5(10)-en-20-yn-17-ol-3-one |
| AHFS/Drugs.com | |
| رده‌بندی داروهای بارداری |
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| روش مصرف دارو | خوراکی[۱] |
| گروه دارویی | Progestogen; Progestin; Estrogen; آندروژن; استروئید آنابولیک |
| کد ATC | |
| وضعیت قانونی | |
| وضعیت قانونی | |
| داده‌های فارماکوکینتیک | |
| زیست فراهمی | ۹۲٪[۵] Its plasma protein binding is 96.3%.[۵] |
| پیوند پروتئینی | ۹۶٫۳٪ (به آلبومین، تمایل کم برای SHBG)[۵] |
| متابولیسم | کبد، لوله گوارش (هیدروکسیلاسیون، همپاری، conjugation)[۱][۶] |
| متابولیت‌ها | • Δ4-Tibolone[۷] • ۳α-Hydroxytibolone[۷] • ۳β-Hydroxytibolone[۷] • سولفات conjugates[۸] |
| نیمه‌عمر حذف | ۴۵ ساعت[۶] |
| دفع | ادرار: ۴۰٪[۵] مدفوع: ۶۰٪[۵] |
| شناسه‌ها | |
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| شمارهٔ سی‌ای‌اس | |
| پاب‌کم CID | |
| دراگ‌بنک | |
| کم‌اسپایدر | |
| UNII | |
| KEGG | |
| ChEBI | |
| ChEMBL | |
| CompTox Dashboard (EPA) | |
| ECHA InfoCard | 100.024.609 |
| داده‌های فیزیکی و شیمیایی | |
| فرمول شیمیایی | C21H28O۲ |
| جرم مولی | ۳۱۲٫۴۵۳ g·mol−1 |
| مدل سه بعدی (جی‌مول) | |
| |
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| (صحت‌سنجی) | |
تیبولون (به انگلیسی: Tibolone) که با نام تجاری Livial فروخته می‌شود، دارویی است که در هورمون درمانی یائسگی و در درمان پوکی استخوان و اندومتریوز پس از یائسگی استفاده می‌شود.[۹][۱۰][۱۱][۱۲] این دارو به تنهایی در دسترس است و به صورت ترکیب با سایر داروها استفاده نمی‌شود.[۱۳] این دارو به صورتخوراکی مصرف می‌شود.[۱]
عوارض جانبی تیبولون شامل آکنه و افزایش رشد مو و برخی دیگر از عوارض است. تیبولون یک استروئید سنتزی با فعالیت ضعیف استروژنی، پروژسترونیک و آندروژنی است و از این رو آگونیست گیرنده‌های استروژن، پروژسترون و آندروژن است.[۱۴][۱۵][۱۶] این ماده یک پیش دارو از چندین متابولیت است.[۱۷][۱۸][۱۹]
اثرات استروژنی تیبولون ممکن است انتخاب بافتی را در توزیع آن‌ها نشان دهد.[۲۰][۲۱][۲۲][۲۳]
تیبولون در دهه ۱۹۶۰ توسعه یافت و در سال ۱۹۸۸ برای استفاده پزشکی معرفی شد.[۲۴][۲۵] این دارو به طور گسترده در سراسر جهان به بازار عرضه می‌شود.[۱۳] با این حال در ایالات متحده موجود نیست.[۱۳]
منابع
- 1 2 3 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.
- ↑ خطای یادکرد: خطای یادکرد:برچسب
<ref> غیرمجاز؛ متنی برای یادکردهای با نامCDSA1996وارد نشده است. (صفحهٔ راهنما را مطالعه کنید.). - ↑ "Summary Basis of Decision (SBD) for Tibella". Health Canada. Retrieved 29 May 2022.
- ↑ "Livial 2.5mg tablets - Summary of Product Characteristics (SmPC)". (emc). 29 September 2020. Retrieved 8 November 2020.
- 1 2 3 4 5 "Tibolone 2.5 mg Tablets" (PDF). Public Assessment Report. United Kingdom Medicines and Healthcare products Regulatory Agency (MHRA). Archived from the original (PDF) on 25 April 2018. Retrieved 4 July 2022.
- 1 2 Albertazzi P, Di Micco R, Zanardi E (1998). "Tibolone: a review". Maturitas. 30 (3): 295–305. doi:10.1016/S0378-5122(98)00059-0. PMID 9881330.
- 1 2 3 خطای یادکرد: خطای یادکرد:برچسب
<ref> غیرمجاز؛ متنی برای یادکردهای با نامpmid 19464167وارد نشده است. (صفحهٔ راهنما را مطالعه کنید.). - ↑ خطای یادکرد: خطای یادکرد:برچسب
<ref> غیرمجاز؛ متنی برای یادکردهای با نامpmid 15145448وارد نشده است. (صفحهٔ راهنما را مطالعه کنید.). - ↑ 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. S2CID 24616324.
- ↑ Ganellin, C.R.; Triggle, David J. (21 November 1996). Dictionary of Pharmacological Agents. CRC Press. pp. 1974–. ISBN 978-0-412-46630-4.
- ↑ Morton, I.K.; Hall, Judith M. (6 December 2012). Concise Dictionary of Pharmacological Agents: Properties and Synonyms. Springer Science & Business Media. pp. 275–. ISBN 978-94-011-4439-1.
- ↑ "Tibolone". AdisInsight.
- 1 2 3 "Tibolone International". Drugs.com.
- ↑ Cano, Antonio (2 November 2017). Menopause: A Comprehensive Approach. Springer. pp. 103–. ISBN 978-3-319-59318-0.
- ↑ 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. S2CID 24616324.
- ↑ Escande A, Servant N, Rabenoelina F, Auzou G, Kloosterboer H, Cavaillès V, Balaguer P, Maudelonde T (2009). "Regulation of activities of steroid hormone receptors by tibolone and its primary metabolites". J. Steroid Biochem. Mol. Biol. 116 (1–2): 8–14. doi:10.1016/j.jsbmb.2009.03.008. PMID 19464167. S2CID 18346113.
- ↑ 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. S2CID 24616324.
- ↑ Cano, Antonio (2 November 2017). Menopause: A Comprehensive Approach. Springer. pp. 103–. ISBN 978-3-319-59318-0.
- ↑ Falcone, Tommaso; Hurd, William W. (14 June 2017). Clinical Reproductive Medicine and Surgery: A Practical Guide. Springer. pp. 182–. ISBN 978-3-319-52210-4.
- ↑ Cano, Antonio (2 November 2017). Menopause: A Comprehensive Approach. Springer. pp. 103–. ISBN 978-3-319-59318-0.
- ↑ Schneider, Hermann P.G.; Naftolin, Frederick (22 September 2004). Climacteric Medicine - Where Do We Go?: Proceedings of the 4th Workshop of the International Menopause Society. CRC Press. pp. 126–. ISBN 978-0-203-02496-6.
- ↑ Falcone, Tommaso; Hurd, William W. (14 June 2017). Clinical Reproductive Medicine and Surgery: A Practical Guide. Springer. pp. 182–. ISBN 978-3-319-52210-4.
- ↑ King, Tekoa; Brucker, Mary C. (25 October 2010). Pharmacology for Women's Health. Jones & Bartlett Learning. pp. 371–. ISBN 978-0-7637-5329-0.
- ↑ Fritz, Marc A.; Speroff, Leon (28 March 2012). Clinical Gynecologic Endocrinology and Infertility. Lippincott Williams & Wilkins. pp. 769–. ISBN 978-1-4511-4847-3.
- ↑ de Vries CS, Bromley SE, Thomas H, Farmer RD (2005). "Tibolone and endometrial cancer: a cohort and nested case-control study in the UK". Drug Safety. 28 (3): 241–9. doi:10.2165/00002018-200528030-00005. PMID 15733028. S2CID 19872216.
جهت مطالعه
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پیوند به بیرون
- "Tibolone". Drug Information Portal. U.S. National Library of Medicine.