Efficacy, acceptability, and metabolic effects of transdermal estradiol in the management of postmenopausal women

Padwick, Malcolm; Endacott, J.; Whitehead, M. I.

doi:10.1016/0002-9378(85)90567-8

Cited by 108 publications

(18 citation statements)

References 10 publications

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“…The TTS patch, one of the most recent developments, has advantages over older delivery methods [9], however, the problem of allergic skin reac tions in about a third of our patients cannot be ignored. This study agrees with Padwick et al [ 15] In conclusion, a good start has been made with use of HRT in Kuwait. Women with vasomotor symptoms had significant allevia tion of their symptoms.…”

Section: Resultssupporting

confidence: 82%

One-Year Follow-Up of Postmenopausal Women on Hormone Replacement Therapy in Kuwait

Omu¹,

Al-Qattan²

1994

Med Princ Pract

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The objective of this study was to evaluate the effect of hormone replacement therapy in 261 postmenopausal women in Kuwait 1 year after starting treatment. The investigations were carried out from June 1992 to June 1994. Combined estrogen and progesterone were used by 50.6% of the women while estrogen implants were used by 18%, transdermal therapeutic system (TTS) patches by 10.3%, natural estrogen by 10.0%, Livial by 6.1%, and estrogen cream by 5.0%. The side effects of HRT were few and mild. Nine of the 27 patients on TTS patch had allergic skin reactions. Significant reduction in the vasomotor symptoms of hot flushes, night sweats and palpitations was achieved in 80-90% of the patients; 31-37% experiencing total elimination of symptoms. Although there was appreciable reduction in the musculoskeletal, psychological and sexual dysfunction symptoms, relief was significantly better for the vasomotor symptoms (p < 0.01). There was a significant reduction in the levels of FSH and LH, and an increase in estrogen levels (p < 0.001), but no significant change was recorded in the lipoprotein profile (p > 0.05). In conclusion, hormone replacement therapy has a significant place in the alleviation of climacteric symptoms in this community.

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Section: Resultssupporting

confidence: 82%

One-Year Follow-Up of Postmenopausal Women on Hormone Replacement Therapy in Kuwait

Omu¹,

Al-Qattan²

1994

Med Princ Pract

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“…10 When the transdermal route is used, induction of hepatic first-pass metabolism can be avoided, and a more physiological estrone/estradiol ratio is achieved. 11 Mainly based on animal studies 12,13 or the use of pharmacological doses of estrogen in prostate cancer, 14 the explanation for the LDL cholesterol-lowering effect of estrogens has been the enhanced LDL receptor activity in the liver. The present study was designed to investigate whether the commonly used doses of estrogen in replacement therapy might also affect LDL clearance.…”

mentioning

confidence: 99%

Mechanisms Regulating LDL Metabolism in Subjects on Peroral and Transdermal Estrogen Replacement Therapy

Karjalainen

Heikkinen

Savolainen

et al. 2000

ATVB

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Abstract-To study the mechanisms of low density lipoprotein (LDL) cholesterol lowering by peroral and transdermal estrogen replacement therapy (ERT), 79 hysterectomized postmenopausal women aged 48 to 62 years were randomized in a double-blind double-dummy trial to receive either peroral estradiol valerate (2 mg/d) or transdermal estradiol gel (1 mg/d) for 6 months. Plasma LDL cholesterol decreased from 4.19Ϯ0.83 (meanϮSD) to 3.39Ϯ0.78 mmol/L (PϽ0.001) in the peroral group and from 4.11Ϯ0.86 to 3.72Ϯ0.78 mmol/L (PϽ0.001) in the transdermal estrogen group. Peroral estrogen did, but transdermal treatment did not, enhance the fractional catabolic rate (FCR) and production of LDL apolipoprotein B (apoB). However, the decrease of LDL cholesterol was related to an increase in FCR for LDL apoB on both peroral and transdermal ERT (rϭϪ0.645, PϽ0.001 and rϭϪ0.627, PϽ0.001, respectively). These changes were associated with changes in the serum estrogen level. Both therapies reduced absorption of dietary cholesterol by 6% to 10% (PϽ0.05). The effects of estrogen were not modified by the polymorphisms of apoE and apoB or cholesterol 7␣-hydroxylase. In conclusion, the ERT-induced LDL cholesterollowering effect is related to changes in estrogen level, which presumably enhance LDL receptor activity, which is manifested as an increase in FCR for LDL apoB. The small decrease in the absorption efficiency of dietary cholesterol does not seem to contribute largely to the cholesterol lowering on either transdermal or peroral ERT. Key Words: estrogen replacement therapy Ⅲ LDL cholesterol Ⅲ menopause Ⅲ lipids A ccording to observational studies, up to 50% of cardiovascular mortality in postmenopausal women could be prevented by postmenopausal hormone replacement therapy (HRT). 1,2 However, a recent randomized secondary prevention study was not able to confirm these results. 3 At any rate, menopause is related to unfavorable alterations in lipids and lipoproteins. 4,5 The beneficial changes in lipids and lipoproteins observed during HRT in several previous studies have been assumed to explain 25% to 50% of the reduced cardiovascular risk. 1 Peroral estrogens decrease total and LDL cholesterol and Lp(a) and increase HDL cholesterol but also triglycerides, whereas less marked reduction in total and LDL cholesterol and no change in Lp(a), HDL cholesterol, and triglyceride levels have been observed during transdermal estrogen treatments. 6,7 The underlying mechanisms of action of estrogen administered via various routes are poorly known. The serum estrogen level is varied by the estrogen regimen and the route of estrogen administration. 8,9 After peroral administration, high levels of estradiol are catabolized into estrone, which induces protein synthesis in the liver. 10 When the transdermal route is used, induction of hepatic first-pass metabolism can be avoided, and a more physiological estrone/estradiol ratio is achieved. 11 Mainly based on animal studies 12,13 or the use of pharmacological doses of estrogen in prostate cancer, 14 the ...

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“…Topical irritation (mainly transient erythema) was reported in 20% of patients (Place et al 1985). Laufer (1983), Padwick et al (1985) and Whitehead et al (1985) in smaller. uncontrolled studies also concluded that use of the oestradiol transdermal drug delivery system leads to significant improvement in symptoms and that the patches are well tolerated,…”

Section: Oestradiolmentioning

confidence: 95%

Pharmacokinetic Considerations in the Use of Newer Transdermal Formulations

Ridout

Santus

Guy

1988

Clinical Pharmacokinetics

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This review addresses the pharmacokinetics and pharmacodynamics of transdermally delivered drugs. The systemic input of drugs via the skin has attracted considerable interest over the past 15 years. The early promise of the administration route has, to some extent, been realised with the approval and successful launching of transdermal formulations of hyoscine (scopolamine), glyceryl trinitrate (nitroglycerin), clonidine and oestradiol. The further application of transdermal delivery, however, will require additional effort. While other molecules (e.g. testosterone, fentanyl, nicotine) may ultimately be administered in this way, important questions pertaining to pharmacology (tolerance), toxicity (irritation, sensitisation) and dose sufficiency (penetration enhancement) remain. These problems are illustrated using information which has been published in the literature. Overall, while the enthusiasm for attraction and benefits of transdermal delivery remain evident, it is clear that future successes will demand a heightened level of commitment and skill from the pharmaceutical scientist.

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Efficacy, acceptability, and metabolic effects of transdermal estradiol in the management of postmenopausal women

Cited by 108 publications

References 10 publications

One-Year Follow-Up of Postmenopausal Women on Hormone Replacement Therapy in Kuwait

One-Year Follow-Up of Postmenopausal Women on Hormone Replacement Therapy in Kuwait

Mechanisms Regulating LDL Metabolism in Subjects on Peroral and Transdermal Estrogen Replacement Therapy

Pharmacokinetic Considerations in the Use of Newer Transdermal Formulations

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