Effects of Tibolone on Serum Lipoprotein and Apolipoprotein Levels Compared With a Cyclical Estrogen/Progestogen Regimen

Farish, E; Barnes, Judith; Fletcher, Colin D.; Ekevall, K; Calder, Ann; Hart, D.M.

doi:10.1097/00042192-199906020-00005

Cited by 29 publications

(9 citation statements)

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“…These effects of tibolone and E2/NETA on lipids and lipoproteins are generally in accord with previous studies . In an earlier comprehensive evaluation of long‐term changes in lipid measures on tibolone, Farish and colleagues observed reductions in VLDL‐C and a small but significant increase in apo‐B on tibolone . We observed similar changes relative to baseline but relative to those taking placebo differences were not significant.…”

Section: Discussionsupporting

confidence: 91%

“…8,22 In an earlier comprehensive evaluation of long-term changes in lipid measures on tibolone, Farish and colleagues observed reductions in VLDL-C and a small but significant increase in apo-B on tibolone. 23 We observed similar changes relative to baseline but relative to those taking placebo differences were not significant. More in accord with previous studies, we observed that reductions in HDL-C concentrations with tibolone were primarily in the cholesterol-rich HDL 2 subfraction, which is the fraction of HDL on which hepatic lipase appears to act.…”

Section: Although Between-group Variation Insupporting

confidence: 62%

“…a Numbers of observations for VLDL were limited due to insufficient amounts of sample. At 6, 12 and 24 months numbers in tibolone, HRT and placebo groups were, respectively: VLDL-C26,27,23;27,26,24;and 27,27,27,22;24,25,24;26,26,27.…”

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confidence: 99%

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Effects of tibolone or continuous combined oestradiol and norethisterone acetate on lipids, high‐density lipoprotein subfractions and apolipoproteins in postmenopausal women in a two‐year, randomized, double‐blind, placebo‐controlled trial

Kotecha

Godsland

Crook

et al. 2020

Clinical Endocrinology

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Objective To compare the effects of (a) tibolone, (b) continuous combined oestrogen plus progestogen and (c) placebo on plasma lipid and lipoprotein markers of cardiovascular risk in healthy postmenopausal women. Study design Randomized, single‐centre, placebo‐controlled, double‐blind study. Patients One hundred and one postmenopausal women were randomized (1:1:1) into one of three groups taking daily 2.5 mg tibolone, continuous oral oestradiol‐17β 2 mg plus norethisterone acetate 1 mg daily (E2/NETA) or placebo. Main outcome measures Fasting serum lipid, lipoprotein and apolipoprotein concentrations measured at baseline and after 6, 12 and 24 months of treatment. Results Both tibolone and E2/NETA lowered plasma total cholesterol concentrations relative to placebo. With tibolone, high‐density lipoprotein cholesterol (HDL‐C) was reduced (−27% at 24 months, P < .001), the greatest effect being in the cholesterol‐enriched HDL2 subfraction (−40%, P < .001). Tibolone's effect on HDL concentrations was also apparent in the principal HDL protein component, apolipoprotein AI (−29% at 24 months, P < .001). However, there was no significant effect of tibolone on low‐density or very low‐density lipoprotein cholesterol (LDL‐C and VLDL‐C, respectively). By contrast, the greatest reduction in cholesterol with E2/NETA was in LDL‐C (−22% at 24 months, P = .008). E2/NETA reduced HDL‐C to a lesser extent than tibolone (−12% at 24 months, P < .001). Effects on HDL apolipoproteins were similarly diminished relative to tibolone. E2/NETA had no effect on VLDL‐C or on the protein component of LDL, apolipoprotein B. Conclusion Tibolone reduces serum HDL. E2/NETA reduces LDL cholesterol but not apolipoprotein B, suggesting decreased cholesterol loading of LDL. Any impact these changes may have on CVD risk needs further investigation.

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Section: Discussionsupporting

confidence: 91%

Section: Although Between-group Variation Insupporting

confidence: 62%

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Effects of tibolone or continuous combined oestradiol and norethisterone acetate on lipids, high‐density lipoprotein subfractions and apolipoproteins in postmenopausal women in a two‐year, randomized, double‐blind, placebo‐controlled trial

Kotecha

Godsland

Crook

et al. 2020

Clinical Endocrinology

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“…This was exemplified by the pronounced reduction in the serum levels of high density lipoprotein (HDL) cholesterol and sex hormone binding globulin (SHBG) 38,39 . Such an effect has previously been observed in women treated with oral contraceptives containing low-dose EE and high-dose levonorgestrel 40 , although the latter exerted only 12% of the androgenic potency of testosterone 41 .…”

Section: Surrogate Parametersmentioning

confidence: 99%

Can 19-nortestosterone derivatives be aromatized in the liver of adult humans? Are there clinical implications?

Kühl

Wiegratz

2007

Climacteric

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19-nortestosterone derivatives (norethisterone, norethynodrel, tibolone) can readily be aromatized in the adult human liver. This leads to the formation of the potent estrogens ethinylestradiol from norethisterone or norethynodrel and 7 alpha-methyl-ethinylestradiol from tibolone. This may have clinical consequences, e.g. the elevated risk of venous thromboembolic disease in premenopausal women treated with high doses of norethisterone for bleeding disorders, or the elevated risk of stroke or endometrial disease in postmenopausal women treated with tibolone.

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“…Beside this, its cardiovascular impact is still unclear. Tibolone induces mixed effect on lipid pattern by decreasing HDL but also VLDL and triglycerides [2][3][4][5]. It does not influence glucose tolerance but ameliorates insulin sensitivity [6,7].…”

Section: Introductionmentioning

confidence: 99%

Administration of tibolone decreases 24h heart rate but not blood pressure of post-menopausal women

et al. 2004

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Effects of Tibolone on Serum Lipoprotein and Apolipoprotein Levels Compared With a Cyclical Estrogen/Progestogen Regimen

Cited by 29 publications

References 0 publications

Effects of tibolone or continuous combined oestradiol and norethisterone acetate on lipids, high‐density lipoprotein subfractions and apolipoproteins in postmenopausal women in a two‐year, randomized, double‐blind, placebo‐controlled trial

Effects of tibolone or continuous combined oestradiol and norethisterone acetate on lipids, high‐density lipoprotein subfractions and apolipoproteins in postmenopausal women in a two‐year, randomized, double‐blind, placebo‐controlled trial

Can 19-nortestosterone derivatives be aromatized in the liver of adult humans? Are there clinical implications?

Administration of tibolone decreases 24h heart rate but not blood pressure of post-menopausal women

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