Tibolon

Tibolon
IUPAC ime
	17-Hidroksi-7α-metil-19-nor-17α-pregn-5(10)-en-20-in-3-on
Klinički podaci
Drugs.com	Internacionalno ime leka
Kategorija trudnoće	ADEC kategorija D;
Način primene	oralno
Identifikatori
CAS broj	5630-53-5
ATC kod	G03CX01 (WHO)
PubChem	CID 444008
ChemSpider	392038
UNII	FF9X0205V2
KEGG	D01639
ChEBI	CHEBI:32223
ChEMBL	CHEMBL1558898
Sinonimi	(7α,17β)-17-etinil-17-hidroksi-7-metilestr-5(10)-en-3-one
Hemijski podaci
Formula	C21H28O2
Molarna masa	312,446 g/mol
	SMILES O=C4CCC\1=C(\C[C@H]([C@@H]2[C@@H]/1CC[C@]3([C@H]2CC[C@]3(C#C)O)C)C)C4; ;
	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 ;

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.^[1] On se prvenstveno koristi za lečenje endometrioze,^[2] 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.^[3]^[4]^[5] On je isto tako bio istraživan kao mogući tretman za seksualnu disfunkciju žena,^[6] 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.^[7]

Reference

^ 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”. The Journal of Steroid Biochemistry and Molecular Biology. 116 (1-2): 8—14. PMID 19464167. doi:10.1016/j.jsbmb.2009.03.008.
^ Al Kadri H, Hassan S, Al-Fozan HM, Hajeer A (2009). Al Kadri, Hanan, ур. „Hormone therapy for endometriosis and surgical menopause”. Cochrane Database of Systematic Reviews (Online) (1): CD005997. PMID 19160262. doi:10.1002/14651858.CD005997.pub2.
^ Lazovic G, Radivojevic U, Marinkovic J (2008). „Tibolone: the way to beat many a postmenopausal ailments”. Expert Opinion on Pharmacotherapy. 9 (6): 1039—47. PMID 18377345. doi:10.1517/14656566.9.6.1039.
^ 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”. Архивирано из оригинала 21. 09. 2012. г. Приступљено 11. 4. 2013.

Spoljašnje veze

Molimo Vas, obratite pažnju na važno upozorenje
u vezi sa temama iz oblasti medicine (zdravlja).

[pmid19464167-1] 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”. The Journal of Steroid Biochemistry and Molecular Biology. 116 (1-2): 8—14. PMID 19464167. doi:10.1016/j.jsbmb.2009.03.008.

[pmid19160262-2] Al Kadri H, Hassan S, Al-Fozan HM, Hajeer A (2009). Al Kadri, Hanan, ур. „Hormone therapy for endometriosis and surgical menopause”. Cochrane Database of Systematic Reviews (Online) (1): CD005997. PMID 19160262. doi:10.1002/14651858.CD005997.pub2.

[pmid18377345-3] Lazovic G, Radivojevic U, Marinkovic J (2008). „Tibolone: the way to beat many a postmenopausal ailments”. Expert Opinion on Pharmacotherapy. 9 (6): 1039—47. PMID 18377345. doi:10.1517/14656566.9.6.1039.

[pmid18488873-4] 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.

[pmid19317264-5] 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.

[6] 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

[7] „Medications Effective in Reducing Risk of Breast Cancer But Increase Risk of Adverse Effects”. Архивирано из оригинала 21. 09. 2012. г. Приступљено 11. 4. 2013.

[1]

[2]

[3]

[4]

[5]

[6]

[7]