Multicentre study of effects of Org OD 14 on endometrium, vaginal cytology and cervical mucus in post-menopausal and oophorectomized women

Punnonen, R.; Liukko, P.; Cortés-Prieto, J; F, Eydam; Milojevic, S Predrag; Trevoux, R.; Chryssikopoulos, E.; Franchi, F; Luisi, M; Kicovic, P.M.

doi:10.1016/0378-5122(84)90023-9

Cited by 61 publications

(14 citation statements)

References 6 publications

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“…This response is different from that in human females, in whom the hormonal profile of tibolone induces no or only weak endometrial stimulation, indicating that the estrogenic activity of tibolone on the endometrium is very weak. 42,43 The doses used are based on human and preclinical studies (see Methods). In rabbits, tibolone is rapidly metabolized to the same metabolites as in humans: the 3␣-and 3␤-hydroxy metabolites, both with estrogenic properties, and the ⌬4 keto isomer, with progestogenic/androgenic properties.…”

Section: Zandberg Et Almentioning

confidence: 99%

“…13,14,19 Tibolone (Org OD14), a synthetic steroid [(7␣,17␣)-17-hydroxy-7-methyl-19-norpregn-5(10)-en-20-yn-3-one] with a combination of estrogenic, androgenic, and progestogenic properties, is clinically effective for the treatment of climacteric symptoms 39,40 and the treatment and prevention of osteoporosis in postmenopausal women, 41 with no stimulatory effect on the endometrium. 42,43 The effect on the development of atherosclerosis is not known. It has been suggested that tibolone might have less atheroprotective effect than ERT because of its progestogenic/androgenic properties.…”

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confidence: 99%

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Tibolone Prevents Atherosclerotic Lesion Formation in Cholesterol-Fed, Ovariectomized Rabbits

Zandberg¹,

Peters²,

Demacker³

et al. 1998

ATVB

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Abstract-Tibolone (Org OD14), a synthetic steroid with estrogenic and progestogenic/androgenic properties, is clinically effective for the treatment of climacteric symptoms and the prevention and treatment of osteoporosis in postmenopausal women. The effect on atherogenesis, however, is not known. In the current study, we investigated the effect of tibolone in comparison with that of estradiol and norethisterone acetate on atherogenesis in 140 ovariectomized New Zealand White rabbits that had been induced by an atherogenic diet (0.4% cholesterol, 20 weeks). Tibolone at 18, 6, or 2 mg/d orally completely prevented cholesterol accumulation and fatty streak formation in the aorta; the impairment of endothelium-dependent smooth muscle relaxation of the aorta; and complex lesion formation after endothelial denudation in the carotid artery. Tibolone also reduced the increased postovariectomy plasma lipid concentrations. Analysis of the results, however, indicated that a substantial part of the strong, beneficial effects were plasma lipid independent. Compared with subcutaneous estradiol decanoate (150 g once weekly) and oral 17␤-estradiol (4 mg/d), the effects of tibolone were more pronounced at equipotent uterotropic activity. Norethisterone acetate (1 mg/d) did not affect atherosclerotic lesion formation. There are no indications that the progestogenic/androgenic properties of tibolone counteracted its atheroprotective effect on the vessel wall. Therefore, tibolone has the intrinsic potential to be a compound that protects the arterial vessel wall against atherosclerotic processes.

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Section: Zandberg Et Almentioning

confidence: 99%

mentioning

confidence: 99%

Tibolone Prevents Atherosclerotic Lesion Formation in Cholesterol-Fed, Ovariectomized Rabbits

Zandberg¹,

Peters²,

Demacker³

et al. 1998

ATVB

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“…The ␦-4 isomer, produced primarily within the endometrium, protects the endometrium from the agonist effects of the 2 estrogenic metabolites. 13,14 Tibolone treatment of postmenopausal women has some beneficial effects on plasma lipid/lipoprotein concentrations (reductions in plasma triglyceride 15,16 and lipoprotein[a] concentrations) 17 ; however, concern has arisen about its "cardiovascular safety" because of reductions in HDLC. 15,18 We have reported the long-term effects of tibolone on coronary artery atherosclerosis of surgically postmenopausal cynomolgus monkeys relative to the effects of conjugated equine estrogen (CEE) treatment and treatment with CEE plus medroxyprogesterone (MPA) administered continuously.…”

mentioning

confidence: 99%

Comparison of Tibolone and Conjugated Equine Estrogens Effects on Carotid Artery Atherosclerosis of Postmenopausal Monkeys

Clarkson

Anthony

Mikkola

et al. 2002

Stroke

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Background and Purpose-Tibolone is a tissue-specific compound that has favorable effects on bone and menopausal symptoms without stimulating endometrium or breast, but lowers concentrations of plasma high-density lipoprotein (HDL) cholesterol (HDLC). This study was designed to determine whether the HDL lowering with tibolone exacerbated common or internal carotid artery atherosclerosis and to evaluate tibolone treatment relative to conjugated equine estrogens (CEE) alone or in combination with medroxyprogesterone acetate (MPA). Methods-Carotid artery atherosclerosis was compared in groups of surgically postmenopausal cynomolgus monkeys treated with CEE, CEEϩMPA, or either of 2 doses of tibolone versus untreated monkeys. Results-Despite a 30% to 52% lowering of HDLC with tibolone, there was no significant effect on carotid artery atherosclerosis. CEE and CEEϩMPA, however, inhibited carotid artery atherosclerosis by Ϸ60%. Key Words: carotid atherosclerosis Ⅲ conjugated equine estrogens Ⅲ hormone replacement therapy Ⅲ tibolone Ⅲ monkeys I schemic stroke among middle-aged and older women is an important public health concern. 1 The exact pathogenesis of these events remains uncertain; however, positive associations with increasing atherosclerosis extent and inverse associations with concentrations of plasma high-density lipoprotein (HDL) cholesterol (HDLC) seem clear. [2][3][4] Although the effect of traditional hormone replacement therapy on stroke prevalence is controversial, [5][6][7][8] it is important to know whether newer menopausal therapies have either adverse or beneficial effects on atherosclerosis of common and internal carotid arteries. Conclusions-InTibolone, used widely in several countries for the treatment of menopausal symptoms 9,10 and for the prevention of postmenopausal osteoporosis, 11,12 is being considered for use in the United States. Tibolone is metabolized into 3 biologically active metabolites; the 3-␤ hydroxy metabolite and the 3-␣ hydroxy metabolite have estrogen agonist properties, whereas the ␦-4 ketoisomer has progestogenic and androgenic effects. The ␦-4 isomer, produced primarily within the endometrium, protects the endometrium from the agonist effects of the 2 estrogenic metabolites. 13,14 Tibolone treatment of postmenopausal women has some beneficial effects on plasma lipid/lipoprotein concentrations (reductions in plasma triglyceride 15,16 and lipoprotein[a] concentrations) 17 ; however, concern has arisen about its "cardiovascular safety" because of reductions in HDLC. 15,18 We have reported the long-term effects of tibolone on coronary artery atherosclerosis of surgically postmenopausal cynomolgus monkeys relative to the effects of conjugated equine estrogen (CEE) treatment and treatment with CEE plus medroxyprogesterone (MPA) administered continuously. 19 Reported herein are the common carotid and internal carotid artery atherosclerosis results from that long-term study. Specifically, we investigated whether the large decreases in HDLC associated with tibolone treatment would ...

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“…Gestajenifc özelliğinin yanında zayıf yanında androjenik, ve östrojenik özelliklere de sahip olan (97) ve endometriumda herhangi bir stimülasyon yapmayan (98,99) tibolon, sentetik bir steroidtir. Bu çalışmada tibolon tedavisinin aynı zamanda HDL-kolesterolde % 23, apolipoprotein A-I da % 14 düşüş, ve apolipoprotein Β de % 17 artışa neden olduğu bildirilmiştir.…”

Section: Hormonların Lp (A) üZerindeki Etkileriunclassified

Diyet, Farmakolojik Ajanlar ve Aferez Uygulamalarının Plasma Lipoprotein (a) Düzeyleri Üzerindeki Etkileri : The Effects of Diet, Pharmacological Agents and Apheresis Procedures on Plasma Levels of Li

Burat¹

1995

Ankara Universitesi Eczacilik Fakultesi Dergisi

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ÖZETYüksek plazma Lp (a) konsantrasyonu ile aterosklrıotik damar hastalıkları gelişimi arasındaki ilişkiyi gösteren epiderniyolojik kanıt lar ve yakın zamanda yapılan biyokimyasal çalışmalar, plazma Lp (a) konsantrasyonlarının düşürülmesinde büyük bir ilgi uyandırmıştır. Bu makalenin amacı, plazma Lp (a) konsantrasyonlarını güvenli düzeylere indirmede kullanılacak araçların tesbitiyle ilgili çalışmaları gözden geçirerek tartışmaktır.Anahtar kelimeler: Diyet, Farmakolojik ajanlar, Aferez, Lipopro tein (a) SUMMARY The epidemiological evidence and the recent biochemical studies which show association between elevated plasma concentrations of lipoprotein (a) (Lp (a)) and the development of atherosclerotic vascular disease, have stimulated a great deal of interest in lowering plasma Lp (a) concentrations. The aim of this paper is to rewiev and discuss the studies in identifying means for bringing plasma Lp (a) concentrations down to safe levels.

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Multicentre study of effects of Org OD 14 on endometrium, vaginal cytology and cervical mucus in post-menopausal and oophorectomized women

Cited by 61 publications

References 6 publications

Tibolone Prevents Atherosclerotic Lesion Formation in Cholesterol-Fed, Ovariectomized Rabbits

Tibolone Prevents Atherosclerotic Lesion Formation in Cholesterol-Fed, Ovariectomized Rabbits

Comparison of Tibolone and Conjugated Equine Estrogens Effects on Carotid Artery Atherosclerosis of Postmenopausal Monkeys

Diyet, Farmakolojik Ajanlar ve Aferez Uygulamalarının Plasma Lipoprotein (a) Düzeyleri Üzerindeki Etkileri : The Effects of Diet, Pharmacological Agents and Apheresis Procedures on Plasma Levels of Li

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