Pharmacokinetics of progestational compounds

Fotherby, K.

doi:10.1016/0378-5122(86)90019-8

Cited by 10 publications

(3 citation statements)

References 27 publications

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“…The group receiving estrogen monotherapy, furthermore, displayed physiological evidence of an estrogenic action on the endometrium. The estradiol and progestogen levels as well as the pharmacokinetic profile were comparable to those found in women receiving postmenopausal hormone replacement therapy (14,21). In the present study both the progestogens exerted significant effects on the endometrium, which implies that the doses given produced physiological effects.…”

Section: Discussionsupporting

confidence: 63%

Estrogen monotherapy and combined estrogen-progestogen replacement therapy attenuate aortic accumulation of cholesterol in ovariectomized cholesterol-fed rabbits.

Haarbo¹,

Leth-Espensen²,

Stender³

et al. 1991

J. Clin. Invest.

199

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Cardiovascular disease is currently the leading cause of death among women in the United States. To investigate the effect of postmenopausal hormone therapy on atherogenesis, we studied 75 cholesterol-fed female rabbits for 19 wk. The rabbits were randomly assigned to five groups. Four groups underwent bilateral ovariectomy followed by treatment with either 17 #l-estradiol, 17 f-estradiol plus norethisterone acetate, 17 ,-estradiol plus levonorgestrel, or placebo. The fifth group had a sham operation and received placebo. The hormone groups had only one-third of the aortic accumulation of cholesterol found in the placebo groups, a difference that was highly statistically significant (P < 0.0001). No significant differences in aortic accumulation of cholesterol were found in the hormone groups. This indicates that estrogen attenuates atherogenesis in cholesterolfed ovariectomized rabbits and that two commonly prescribed progestogens do not counteract the effect. The beneficial effect of estradiol could only partly be explained by its lowering effects on serum total cholesterol or VLDL cholesterol, which implies that estradiol possesses additional beneficial effects, possibly a direct action on the arterial wall. (J. Clin. Invest.

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Section: Discussionsupporting

confidence: 63%

Estrogen monotherapy and combined estrogen-progestogen replacement therapy attenuate aortic accumulation of cholesterol in ovariectomized cholesterol-fed rabbits.

Haarbo¹,

Leth-Espensen²,

Stender³

et al. 1991

J. Clin. Invest.

199

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“…The plasma elimination half-life of estradiol is approximately 1 hour, irrespective of the route of administration, and that of norethisterone is between 6 and 8 hours (Fotherby 1986;Nichols et al 1984).…”

Section: Metabolism and Eliminationmentioning

confidence: 99%

“…Four metabolites of norethisterone have been identified, the 5p,3a-hydroxy derivative being the most com-Drugs & Aging 4 (3) 1994 mon, which are predominantly excreted in urine and faeces as sulphate and glucuronide conjugates (Braselton et al 1979;Fotherby 1986;Stillwell et al 1972). Four metabolites of norethisterone have been identified, the 5p,3a-hydroxy derivative being the most com-Drugs & Aging 4 (3) 1994 mon, which are predominantly excreted in urine and faeces as sulphate and glucuronide conjugates (Braselton et al 1979;Fotherby 1986;Stillwell et al 1972).…”

Section: Metabolism and Eliminationmentioning

confidence: 99%

Transdermal Estradiol/Norethisterone

Wiseman¹,

McTavish²

1994

Drugs & Aging

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The combined transdermal estradiol/norethisterone therapeutic system is designed to deliver both estradiol and norethisterone into the systemic circulation at a constant rate for up to 4 days when affixed to the skin. Transdermal administration avoids hepatic first-pass metabolism, allowing therapeutic concentrations of the progestogen and estrogen to be maintained in postmenopausal women following low dose administration. Transdermal norethisterone does not appear to alter the potentially beneficial effects of transdermal estradiol on total cholesterol, low-density lipoprotein (LDL) or triglyceride levels, or metabolic parameters of bone resorption or vaginal cytology. Protection of the endometrium from the effects of unopposed estradiol is achieved by sequential treatment with transdermal estradiol/norethisterone for 2 weeks of each 28-day cycle, and the majority of patients experience a regular vaginal bleeding pattern with this treatment regimen. Menopausal symptoms are improved to a similar extent during the transdermal estradiol-only and combined estradiol/norethisterone treatment phases. The transdermal therapeutic system has been well accepted by patients in clinical trials. It is generally well tolerated, the most common adverse effect being local irritation at the site of application. Estrogen- and progestogen-related systemic adverse events are reported in a small proportion of patients. Thus, the combined estradiol/norethisterone transdermal delivery system offers a more convenient and consistent method of progestogen administration. Together with its therapeutic efficacy when administered at lower dosages than oral therapy, it is likely to further improve patient compliance during hormone replacement therapy.

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A Short Review on the Sources of Variability in Pharmacokinetic Parameters of Sex Steroids: Comment on the Paper by K. Fotherby

Hümpel¹

1994

Steroid Contraceptives and Women’s Response

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Pharmacokinetics of progestational compounds

Cited by 10 publications

References 27 publications

Estrogen monotherapy and combined estrogen-progestogen replacement therapy attenuate aortic accumulation of cholesterol in ovariectomized cholesterol-fed rabbits.

Estrogen monotherapy and combined estrogen-progestogen replacement therapy attenuate aortic accumulation of cholesterol in ovariectomized cholesterol-fed rabbits.

Transdermal Estradiol/Norethisterone

A Short Review on the Sources of Variability in Pharmacokinetic Parameters of Sex Steroids: Comment on the Paper by K. Fotherby

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