Tibolon

Tibolon
(IUPAC) ime
	17-Hidroksi-7α-metil-19-nor-17α-pregn-5(10)-en-20-in-3-on
Klinički podaci
AHFS/Drugs.com	Internacionalno ime leka
Identifikatori
CAS broj	5630-53-5
ATC kod	G03CX01
PubChem	444008
ChemSpider	392038
UNII	FF9X0205V2
KEGG	D01639
ChEBI	CHEBI:32223
ChEMBL	CHEMBL1558898
Hemijski podaci
Formula	C21H28O2
Mol. masa	312,446 g/mol
SMILES	eMolekuli & PubHem
InChI
	InChI=1S/C21H28O2/c1-4-21(23)10-8-18-19-13(2)11-14-12-15(22)5-6-16(14)17(19)7-9-20(18,21)3/h1,13,17-19,23H,5-12H2,2-3H3/t13-,17-,18+,19-,20+,21+/m1/s1 ; Key: WZDGZWOAQTVYBX-XOINTXKNSA-N
Sinonimi	(7α,17β)-17-etinil-17-hidroksi-7-metilestr-5(10)-en-3-one
Farmakoinformacioni podaci
Trudnoća	?
Pravni status
Način primene	oralno

Tibolon je sintetički steroidni hormonski lek, koji je u znatnoj meri neselektivan. On deluje kao agonist na svih pet tipova Tipa I steroidnog hormonskog receptora.^[6] On se prvenstveno koristi za lečenje endometrioze,^[7] kao i u terapiji zamene hormona kod žena nakon menopauze. Tibolon ima sličnu ili veću efikasnost u odnosu na starije lekove za hormonsku zamenu, ali ima sličan profil nepoželjnih efekata.^[8]^[9]^[10] On je isto tako bio istraživan kao mogući tretman za seksualnu disfunkciju žena,^[11] mada nije jasno da li koristi takve primene opravdavaju izlaganje poznatim rizicima uporebe leka.

Nepoželjna dejstva

Tamoksifen, raloksifen, i tibolon korišteni za suzbijanje kancera dojke znatno redukuju invazivni kancer kor žena srednjeg i poznog doba. Međutim, oni isto tako povečavaju rizik od nepoželjnih nuspojava.^[12]

Reference

↑ Li Q, Cheng T, Wang Y, Bryant SH (2010). „PubChem as a public resource for drug discovery.”. Drug Discov Today 15 (23-24): 1052-7. DOI:10.1016/j.drudis.2010.10.003. PMID 20970519. edit
↑ Evan E. Bolton, Yanli Wang, Paul A. Thiessen, Stephen H. Bryant (2008). „Chapter 12 PubChem: Integrated Platform of Small Molecules and Biological Activities”. Annual Reports in Computational Chemistry 4: 217-241. DOI:10.1016/S1574-1400(08)00012-1.
↑ Hettne KM, Williams AJ, van Mulligen EM, Kleinjans J, Tkachenko V, Kors JA. (2010). „Automatic vs. manual curation of a multi-source chemical dictionary: the impact on text mining”. J Cheminform 2 (1): 3. DOI:10.1186/1758-2946-2-3. PMID 20331846. edit
↑ Joanne Wixon, Douglas Kell (2000). „Website Review: The Kyoto Encyclopedia of Genes and Genomes — KEGG”. Yeast 17 (1): 48–55. DOI:10.1002/(SICI)1097-0061(200004)17:1<48::AID-YEA2>3.0.CO;2-H.
↑ Gaulton A, Bellis LJ, Bento AP, Chambers J, Davies M, Hersey A, Light Y, McGlinchey S, Michalovich D, Al-Lazikani B, Overington JP. (2012). „ChEMBL: a large-scale bioactivity database for drug discovery”. Nucleic Acids Res 40 (Database issue): D1100-7. DOI:10.1093/nar/gkr777. PMID 21948594. edit
↑ Escande A, Servant N, Rabenoelina F, Auzou G, Kloosterboer H, Cavaillès V, Balaguer P, Maudelonde T (August 2009). „Regulation of activities of steroid hormone receptors by tibolone and its primary metabolites”. The Journal of Steroid Biochemistry and Molecular Biology 116 (1-2): 8–14. DOI:10.1016/j.jsbmb.2009.03.008. PMID 19464167.
↑ Al Kadri H, Hassan S, Al-Fozan HM, Hajeer A (2009). Al Kadri, Hanan. ur. „Hormone therapy for endometriosis and surgical menopause”. Cochrane Database of Systematic Reviews (Online) (1): CD005997. DOI:10.1002/14651858.CD005997.pub2. PMID 19160262.
↑ Lazovic G, Radivojevic U, Marinkovic J (April 2008). „Tibolone: the way to beat many a postmenopausal ailments”. Expert Opinion on Pharmacotherapy 9 (6): 1039–47. DOI:10.1517/14656566.9.6.1039. PMID 18377345.
↑ Garefalakis M, Hickey M (2008). „Role of androgens, progestins and tibolone in the treatment of menopausal symptoms: a review of the clinical evidence”. Clinical Interventions in Aging 3 (1): 1–8. PMC 2544356. PMID 18488873.
↑ Vavilis D, Zafrakas M, Goulis DG, Pantazis K, Agorastos T, Bontis JN (2009). „Hormone therapy for postmenopausal breast cancer survivors: a survey among obstetrician-gynaecologists”. European Journal of Gynaecological Oncology 30 (1): 82–4. PMID 19317264.
↑ Ziaei S, Moghasemi M, Faghihzadeh S. Comparative effects of conventional hormone replacement therapy and tibolone on climacteric symptoms and sexual dysfunction in postmenopausal women. Climacteric. 2009 Sep 1:1-10. PMID 19731119
↑ Medications Effective in Reducing Risk of Breast Cancer But Increase Risk of Adverse Effects Arhivirano 2012-09-21 na Wayback Machine-u, Приступљено 11. 4. 2013.

Spoljašnje veze

	Portal Medicina
	Portal Hemija

[1] Li Q, Cheng T, Wang Y, Bryant SH (2010). „PubChem as a public resource for drug discovery.”. Drug Discov Today 15 (23-24): 1052-7. DOI:10.1016/j.drudis.2010.10.003. PMID 20970519. edit

[2] Evan E. Bolton, Yanli Wang, Paul A. Thiessen, Stephen H. Bryant (2008). „Chapter 12 PubChem: Integrated Platform of Small Molecules and Biological Activities”. Annual Reports in Computational Chemistry 4: 217-241. DOI:10.1016/S1574-1400(08)00012-1.

[3] Hettne KM, Williams AJ, van Mulligen EM, Kleinjans J, Tkachenko V, Kors JA. (2010). „Automatic vs. manual curation of a multi-source chemical dictionary: the impact on text mining”. J Cheminform 2 (1): 3. DOI:10.1186/1758-2946-2-3. PMID 20331846. edit

[4] Joanne Wixon, Douglas Kell (2000). „Website Review: The Kyoto Encyclopedia of Genes and Genomes — KEGG”. Yeast 17 (1): 48–55. DOI:10.1002/(SICI)1097-0061(200004)17:1<48::AID-YEA2>3.0.CO;2-H.

[5] Gaulton A, Bellis LJ, Bento AP, Chambers J, Davies M, Hersey A, Light Y, McGlinchey S, Michalovich D, Al-Lazikani B, Overington JP. (2012). „ChEMBL: a large-scale bioactivity database for drug discovery”. Nucleic Acids Res 40 (Database issue): D1100-7. DOI:10.1093/nar/gkr777. PMID 21948594. edit

[pmid19464167-6] Escande A, Servant N, Rabenoelina F, Auzou G, Kloosterboer H, Cavaillès V, Balaguer P, Maudelonde T (August 2009). „Regulation of activities of steroid hormone receptors by tibolone and its primary metabolites”. The Journal of Steroid Biochemistry and Molecular Biology 116 (1-2): 8–14. DOI:10.1016/j.jsbmb.2009.03.008. PMID 19464167.

[pmid19160262-7] Al Kadri H, Hassan S, Al-Fozan HM, Hajeer A (2009). Al Kadri, Hanan. ur. „Hormone therapy for endometriosis and surgical menopause”. Cochrane Database of Systematic Reviews (Online) (1): CD005997. DOI:10.1002/14651858.CD005997.pub2. PMID 19160262.

[pmid18377345-8] Lazovic G, Radivojevic U, Marinkovic J (April 2008). „Tibolone: the way to beat many a postmenopausal ailments”. Expert Opinion on Pharmacotherapy 9 (6): 1039–47. DOI:10.1517/14656566.9.6.1039. PMID 18377345.

[pmid18488873-9] Garefalakis M, Hickey M (2008). „Role of androgens, progestins and tibolone in the treatment of menopausal symptoms: a review of the clinical evidence”. Clinical Interventions in Aging 3 (1): 1–8. PMC 2544356. PMID 18488873.

[pmid19317264-10] Vavilis D, Zafrakas M, Goulis DG, Pantazis K, Agorastos T, Bontis JN (2009). „Hormone therapy for postmenopausal breast cancer survivors: a survey among obstetrician-gynaecologists”. European Journal of Gynaecological Oncology 30 (1): 82–4. PMID 19317264.

[11] Ziaei S, Moghasemi M, Faghihzadeh S. Comparative effects of conventional hormone replacement therapy and tibolone on climacteric symptoms and sexual dysfunction in postmenopausal women. Climacteric. 2009 Sep 1:1-10. PMID 19731119

[12] Medications Effective in Reducing Risk of Breast Cancer But Increase Risk of Adverse Effects Arhivirano 2012-09-21 na Wayback Machine-u, Приступљено 11. 4. 2013.

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