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Vol 6, No 2 (2021)
Review article
Published online: 2021-03-29
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Tibolone among drugs in the therapy of postmenopausal women

Adrianna Nieciecka1, Kornelia Kędziora-Kornatowska1, Marta Janiszewska1
·
Medical Research Journal 2021;6(2):140-146.
Affiliations
  1. Collegium Medicum in Bydgoszcz, Nicolaus Copernicus University in Toruń, ul. Jagiellońska 13-15, Bydgoszcz, Poland

open access

Vol 6, No 2 (2021)
REVIEW ARTICLES
Published online: 2021-03-29

Abstract

The ageing of society is undoubtedly a success, but also a challenge of modern medicine. Postmenopausal women struggle with many health problems, and their treatment recommended so far is often associated with many side effects such as the increased risk of hormone-dependent tumours or thromboembolism. The purpose of this article is to discuss the effects of a relatively new drug called tibolone against the currently recommended treatment. The unique mechanism of estrogenic, progestogenic, and androgenic action of tibolone is due to the breakdown of the parent compound into 3 active metabolites, each selectively acting on different tissues differently. Tibolone is approved for the relief of menopausal symptoms and its effectiveness is similar to that of hormone replacement therapy and the prevention of osteoporosis. The article will also discuss the results of various studies on the risk of cancer during treatment with tibolone, especially in comparison to hormone replacement therapy. Tibolone affects also the cardiovascular system, including reducing the level of lipoprotein a, total cholesterol, triglycerides, and HDL. Tibolone also has a neuroprotective effect and improves mood and libido. Like all medicines, tibolone is not free from side effects such as weight gain, vaginal bleeding, hirsutism, and inflammation of the reproductive organs, so the benefits and risks of therapy should always be considered. There are still no clear conclusions regarding many aspects of the influence of tibolone on the patient’s body, therefore large studies are needed to assess the effectiveness and safety of tibolone.

Abstract

The ageing of society is undoubtedly a success, but also a challenge of modern medicine. Postmenopausal women struggle with many health problems, and their treatment recommended so far is often associated with many side effects such as the increased risk of hormone-dependent tumours or thromboembolism. The purpose of this article is to discuss the effects of a relatively new drug called tibolone against the currently recommended treatment. The unique mechanism of estrogenic, progestogenic, and androgenic action of tibolone is due to the breakdown of the parent compound into 3 active metabolites, each selectively acting on different tissues differently. Tibolone is approved for the relief of menopausal symptoms and its effectiveness is similar to that of hormone replacement therapy and the prevention of osteoporosis. The article will also discuss the results of various studies on the risk of cancer during treatment with tibolone, especially in comparison to hormone replacement therapy. Tibolone affects also the cardiovascular system, including reducing the level of lipoprotein a, total cholesterol, triglycerides, and HDL. Tibolone also has a neuroprotective effect and improves mood and libido. Like all medicines, tibolone is not free from side effects such as weight gain, vaginal bleeding, hirsutism, and inflammation of the reproductive organs, so the benefits and risks of therapy should always be considered. There are still no clear conclusions regarding many aspects of the influence of tibolone on the patient’s body, therefore large studies are needed to assess the effectiveness and safety of tibolone.

Get Citation

Keywords

tibolone, menopause, hormone replacement therapy, neoplasms, osteoporosis

About this article
Title

Tibolone among drugs in the therapy of postmenopausal women

Journal

Medical Research Journal

Issue

Vol 6, No 2 (2021)

Article type

Review article

Pages

140-146

Published online

2021-03-29

Page views

1450

Article views/downloads

2674

DOI

10.5603/MRJ.a2021.0014

Bibliographic record

Medical Research Journal 2021;6(2):140-146.

Keywords

tibolone
menopause
hormone replacement therapy
neoplasms
osteoporosis

Authors

Adrianna Nieciecka
Kornelia Kędziora-Kornatowska
Marta Janiszewska

References (49)
  1. Zalega T. Proces starzenia się społeczeństwa-wybrane aspekty. Zarządzanie Innowacyjne w Gospodarce i Biznesie. 2018; 1(26): 121–139.
  2. Zdziebło K. Współczesne zjawiska demograficzne a problemy zdrowotne starzejącego się społeczeństwa. Studia medyczne. 2008; 9: 63–69.
  3. Kloosterboer HJ. Historical milestones in the development of tibolone (Livial®). Climacteric. 2011; 14(6): 609–621.
  4. Swegle JM, Kelly MW. Tibolone: a unique version of hormone replacement therapy. Ann Pharmacother. 2004; 38(5): 874–881.
  5. Dębski R, Kotarski J, Paszkowski T, et al. Stanowisko Zespołu Ekspertów Polskiego Towarzystwa Ginekologicznego na temat zastosowania tibolonu w ramach menopauzalnej terapii hormonalnej. Menopause Review/Przegląd Menopauzalny. 2009; 8(1): 1–5.
  6. Kenemans P, Speroff L. International Tibolone Consensus Group. Tibolone: clinical recommendations and practical guidelines. A report of the International Tibolone Consensus Group. Maturitas. 2005; 51(1): 21–28.
  7. Santoro N. Perimenopause: From Research to Practice. J Womens Health (Larchmt). 2016; 25(4): 332–339.
  8. Johnson A, Roberts L, Elkins G. Complementary and Alternative Medicine for Menopause. J Evid Based Integr Med. 2019; 24: 2515690X19829380.
  9. Baranowski W, Debski R, Paszkowski T, et al. Rekomendacje Polskiego Towarzystwa Menopauzy i Andropauzy dotyczące stosowania lokalnej terapii hormonalnej u kobiet w okresie menopauzy. Przegląd Menopauzalny. 2011; 15(4): 263.
  10. Fait T. Menopause hormone therapy: latest developments and clinical practice. Drugs Context. 2019; 8: 212551.
  11. Umland EM, Falconieri L. Treatment options for vasomotor symptoms in menopause: focus on desvenlafaxine. Int J Womens Health. 2012; 4: 305–319.
  12. Kim HK, Jeon SH, Ryu KiJ, et al. Comparison of the Efficacy of Tibolone and Transdermal Estrogen in Treating Menopausal Symptoms in Postmenopausal Women. J Menopausal Med. 2019; 25(3): 123–129.
  13. Ito K. Hormone replacement therapy and cancers: the biological roles of estrogen and progestin in tumorigenesis are different between the endometrium and breast. Tohoku J Exp Med. 2007; 212(1): 1–12.
  14. Løkkegaard EC, Mørch LS. Tibolone and risk of gynecological hormone sensitive cancer. Int J Cancer. 2018; 142(12): 2435–2440.
  15. Szlendak-Sauer K, Wierzba W, Radowicki S. Wpływ stosowania tibolonu na obraz endometrium u kobiet po menopauzie. Ginekologia Polska, 2008; 79. ; 11: 758–761.
  16. de Vries CS, Bromley SE, Thomas H, et al. Tibolone and endometrial cancer: a cohort and nested case-control study in the UK. Drug Saf. 2005; 28(3): 241–249.
  17. Gemmell LC, Webster KE, Kirtley S, et al. The management of menopause in women with a history of endometriosis: a systematic review. Hum Reprod Update. 2017; 23(4): 481–500.
  18. Husejko J, Porada M, Bieniek D, et al. Breast cancer as a significant social problem. J Educ Health Sport. 2019; 9(8): 412–423.
  19. Wang PH, Cheng MH, Chao HT, et al. Effects of tibolone on the breast of postmenopausal women. Taiwan J Obstet Gynecol. 2007; 46(2): 121–126.
  20. Green J, Reeves GK, Floud S, et al. Million Women Study Collaborators, Million Women Study Collaborators, Million Women Study Collaborators, Million Women Study Collaborators, Million Women Study Collaborators, Million Women Study Collaborators, Million Women Study Collaborators, Million Women Study Collaborators, Million Women Study Collaborators, Million Women Study Collaborators. Breast cancer and hormone-replacement therapy in the Million Women Study. Lancet. 2003; 362(9382): 419–427.
  21. Vitale C, Mammi C, Gambacciani M, et al. Effect of hormone replacement therapy with the anti-mineralocorticoid progestin Drospirenone compared to tibolone on endothelial function and central haemodynamics in post-menopausal women. Int J Cardiol. 2017; 227: 217–221.
  22. Henderson VW, Lobo RA. Hormone therapy and the risk of stroke: perspectives 10 years after the Women's Health Initiative trials. Climacteric. 2012; 15(3): 229–234.
  23. Anagnostis P, Bitzer J, Cano A, et al. Menopause symptom management in women with dyslipidemias: An EMAS clinical guide. Maturitas. 2020; 135: 82–88.
  24. Kotani K, Sahebkar A, Serban C, et al. Lipid and Blood Pressure Meta-analysis Collaboration (LBPMC) Group. Tibolone decreases Lipoprotein(a) levels in postmenopausal women: A systematic review and meta-analysis of 12 studies with 1009 patients. Atherosclerosis. 2015; 242(1): 87–96.
  25. Anagnostis P, Galanis P, Chatzistergiou V, et al. The effect of hormone replacement therapy and tibolone on lipoprotein (a) concentrations in postmenopausal women: A systematic review and meta-analysis. Maturitas. 2017; 99: 27–36.
  26. Lloyd G, McGing E, Cooper A, et al. A randomised placebo controlled trial of the effects of tibolone on blood pressure and lipids in hypertensive women. J Hum Hypertens. 2000; 14(2): 99–104.
  27. Bała M, Sahebkar A, Ursoniu S, et al. Lipid Blood Pressure Meta-Analysis Collaboration Group. Effects of tibolone on fibrinogen and antithrombin III: A systematic review and meta-analysis of controlled trials. Pharmacol Res. 2017; 124: 64–73.
  28. Skalska A. Efekt działania tybolonu u kobiet w starszym wieku w okresie pomenopauzalnym. Gerontologia Polska, 2008, tom 16, nr. ; 3: 183.
  29. Smektała A, Dobosz A. Osteoporoza – patofizjologia, objawy, profilaktyka i leczenie. Farmacja Polska. 2020; 6: 344.
  30. Notelovitz M. Postmenopausal tibolone therapy: biologic principles and applied clinical practice. MedGenMed. 2007; 9(1): 2.
  31. Gambacciani M, Cagnacci A, Lello S, et al. Italian Menopause Society (SIM), International Menopause Society, International Menopause Society Writing Group, International Menopause Society Expert Workshop, Executive Committee of the International Menopause Society. The osteoporosis dilemma. Gynecol Endocrinol. 2004; 18(2): 59–61.
  32. Gambacciani M, Ciaponi M, Cappagli B, et al. A longitudinal evaluation of the effect of two doses of tibolone on bone density and metabolism in early postmenopausal women. Gynecol Endocrinol. 2004; 18(1): 9–16.
  33. Cummings SR, Ettinger B, Delmas PD, et al. LIFT Trial Investigators. The effects of tibolone in older postmenopausal women. N Engl J Med. 2008; 359(7): 697–708.
  34. Eastell R, Rosen CJ, Black DM, et al. Pharmacological Management of Osteoporosis in Postmenopausal Women: An Endocrine Society* Clinical Practice Guideline. J Clin Endocrinol Metab. 2019; 104(5): 1595–1622.
  35. Karsdal MA, Byrjalsen I, Leeming DJ, et al. Tibolone inhibits bone resorption without secondary positive effects on cartilage degradation. BMC Musculoskelet Disord. 2008; 9: 153.
  36. Laçin S, Oruç S, Karaca S, et al. Assessment of the effectiveness of postmenopausal tibolone therapy on neural functions by measuring visual evoked potentials: a placebo-controlled study. Eur J Obstet Gynecol Reprod Biol. 2001; 98(1): 72–76.
  37. Henderson VW. Progesterone and human cognition. Climacteric. 2018; 21(4): 333–340.
  38. Pinto-Almazán R, Segura-Uribe JJ, Farfán-García ED, et al. Effects of Tibolone on the Central Nervous System: Clinical and Experimental Approaches. Biomed Res Int. 2017; 2017: 8630764.
  39. Genazzani AR, Pluchino N, Bernardi F, et al. Beneficial effect of tibolone on mood, cognition, well-being, and sexuality in menopausal women. Neuropsychiatr Dis Treat. 2006; 2(3): 299–307.
  40. Martin-Jiménez C, Gaitán-Vaca DM, Areiza N, et al. Astrocytes Mediate Protective Actions of Estrogenic Compounds after Traumatic Brain Injury. Neuroendocrinology. 2019; 108(2): 142–160.
  41. Hidalgo-Lanussa O, Baez-Jurado E, Echeverria V, et al. Lipotoxicity, neuroinflammation, glial cells and oestrogenic compounds. J Neuroendocrinol. 2020; 32(1): e12776.
  42. Crespo-Castrillo A, Garcia-Segura LM, Arevalo MA. The synthetic steroid tibolone exerts sex-specific regulation of astrocyte phagocytosis under basal conditions and after an inflammatory challenge. J Neuroinflammation. 2020; 17(1): 37.
  43. Davis SR. The effects of tibolone on mood and libido. Menopause. 2002; 9(3): 162–170.
  44. Genazzani AR, Bernardi F, Pluchino N, et al. Effect of tibolone administration on central and peripheral levels of allopregnanolone and beta-endorphin in female rats. Menopause. 2006; 13(1): 57–64.
  45. Gupta B, Mittal P, Khuteta R, et al. A Comparative Study of CEE, Tibolone, and DHEA as Hormone Replacement Therapy for Surgical Menopause. J Obstet Gynaecol India. 2013; 63(3): 194–198.
  46. LiverTox: Clinical and Research Information on Drug-Induced Liver Injury [Internet]. Bethesda (MD): National Institute of Diabetes and Digestive and Kidney Diseases; 2012-. Tibolone. [Updated 2020 Sep 2]. https://www.ncbi.nlm.nih.gov/books/NBK548180/.
  47. Formoso G, Perrone E, Maltoni S, et al. Short and long term effects of tibolone in postmenopausal women. Cochrane Database Syst Rev. 2012(2): CD008536.
  48. Staples L, Milder T, Choi PYI. Polycythaemia Secondary to Hormone Replacement Therapy with Tibolone. Case Rep Hematol. 2017; 2017: 3476349.
  49. González-Arenas A, De la Fuente-Granada M, Camacho-Arroyo I, et al. Tibolone Effects on Human Glioblastoma Cell Lines. Arch Med Res. 2019; 50(4): 187–196.

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