Pharmacokinetics and pharmacodynamics of transdermal dosage forms of 17β-estradiol: Comparison with conventional oral estrogens used for hormone replacement

Powers, Marilou S.; Schenkel, L.; Darley, Paul E.; Good, William R.; Balestra, Joanne C.; Place, Virgil A.

doi:10.1016/0002-9378(85)90569-1

Cited by 279 publications

(91 citation statements)

References 12 publications

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“…13,15 Fluctuation in levels with marked peak and trough levels was apparent in all ¢ve of the longer-term studies after several patch applications. 12,13,15,21,23 The di¡erence between peak and trough levels varied from 1¢3 to 1¢7 in two studies using the twice weekly 0 ¢ 05 mg/day patch (see Table 3) 13,21 but was much higher (ratio 10 ¢ 0 after 19 days) in the study by Jarvinen et al 24 In the latter study this ratio was achieved by both higher peak and lower trough oestradiol levels compared with the other two studies. In the 3-week study published by Powers and co-workers for women using the 0¢05 mg/day twice weekly Estraderm 2 patch, trough levels after the sixth patch application represented 71% of the average level achieved during use of six patches.…”

Section: Comparison Of Oestradiol Pharmacokinetic Data From Seven Pubmentioning

confidence: 91%

Hormone replacement therapy (oestradiol-only preparations): can the laboratory recommend a concentration of plasma oestradiol to protect against osteoporosis?

Armston¹,

Wood²

2002

Ann Clin Biochem

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Target concentrations of plasma oestradiol to protect against osteoporosis have now been published in at least one textbook 1 and are increasingly discussed by clinicians. A survey of the literature revealed that many reports do not give details of oestradiol assay methods, despite the fact that there is a wide range of biases. Plasma oestradiol measurements made after ingestion of equine oestrogen preparations are not valid, and for oral oestradiol and oestradiol valerate preparations a single untimed sample does not give a reliable estimate of the average exposure over 24 h. Oestradiol measurements in plasma from women using patch, gel or implant preparations could be useful provided that consideration is given to the time of sampling and to the assay method used, although target levels have not been established. Further studies are required in this area.

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Section: Comparison Of Oestradiol Pharmacokinetic Data From Seven Pubmentioning

confidence: 91%

Hormone replacement therapy (oestradiol-only preparations): can the laboratory recommend a concentration of plasma oestradiol to protect against osteoporosis?

Armston¹,

Wood²

2002

Ann Clin Biochem

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“…In other words, a more physiological estradiol/estrone ratio (approximately 1) exists. When estrogen is administered orally, this ratio is 0.2, and therefore is not in accordance with the physiological values (32). Transdermal estrodiol valerate (Estraderm, CIBA Pharmaceutical Co.; Summit, NJ, USA) plasters are applied on the lower abdominal region, whereby between day 1 and 6 of the cycle, plasters are applied as a dose of 50 micrograms once every three days; between day 7 and 9, one plaster of 100 micrograms; on days 10 and 11, a 200 microgram plaster; and between day 12 and 14, four plasters, each of 100 micrograms (400 micrograms total) are used.…”

Section: Artificial Endometrium Preparation By the Exogenous Administmentioning

confidence: 95%

Methods for endometrial preparation in frozen-thawed embryo transfer cycles

Kalem

Gürgan

2016

J Turkish German Gynecol Assoc

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Review 168 IntroductionFrozen-thawed (FT) embryo transfer is a procedure used for the storage and transfer of excess embryos obtained during in vitro fertilization (IVF)-intracytoplasmic sperm injection (ICSI) cycles. In recent years, improvements in laboratory conditions and limitations on the number of embryos to be transferred have led to a progressive increase in FT embryo transfer cycles. Another preferred practice to prevent multiple pregnancies in IVF cycles is to transfer a single embryo and freeze all surplus embryos (1). However, the best solution for endometrial preparation in these cycles is still a matter of debate (2). Frozen-thawed embryo transfer prevents embryo waste and increases the probability of pregnancy in a single stimulated cycle. Protocols applied in FT cycles aim for endometrial preparation only and are therefore simpler than complicated protocols that aim to develop many follicles. As the treatment for subfertility increases, so does the importance of FT embryo transfer; however, there is no consensus about which method is the best (3, 4). Pregnancy rates following FT embryo transfer have been found to be higher than those following fresh embryo transfer (5). Further, FT embryo transfer increases the cumulative pregnancy rate and decreases the cost; in addition, it is easy to perform and can be applied in a shorter time duration when compared to repetitive fresh embryo transfers (5). Using frozen excess embryos obtained as a result of the time-totime implementation of in vitro maturation (IVM) in patients with polycystic ovaries, successful pregnancies have been achieved (6). Therefore, studies have concentrated on factors affecting the success rate of FT embryo transfer cycles.Various cycle protocols are used for the preparation of the endometrium in an FT embryo transfer cycle. In one of these procedures, the transfer time is determined either by the natural course of a cycle [i.e., in an ovulatory patient exhibiting a natural (spontaneous) cycle] or by inducing ovulation during the course of a natural cycle. The second procedure involves the artificial preparation of the endometrium through the administration of exogenous estrogen and progesterone, which can be performed with or without the association of a gonadotropin-releasing hormone agonist. In the third procedure, the cycle is stimulated by gonadotropins and ovulation is induced by recombinant-human chorionic gonadotropin (rHcg) or hCG; however, this practice is no longer applied (7,8). Embryo transfer in a natural (spontaneous) cycleBoth embryo and endometrial development have to be synchronized in FT embryo transfer cycles in order to maximize the pregnancy rate (9). This synchronization can be achieved in several ways. The easiest is the endocrinological preparation of the endometrium during the natural cycle using the patient's own follicular sex steroids. In this application, the timing for embryo transfer (ET) is determined by either investigating the spontaneous luteinizing hormone (LH) surge or by the administration o...

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“…(Pan CC, 1985) Following oral intake of CEEs, mean serum estrone levels (152 pg/mL) are far higher than estradiol levels (31 pg/mL). (Powers MS et al 1985) However, the estrone component is largely inactive because it is albumin-bound. The clinical response to CEE is hypothesized to be mediated through a mechanism involving conversion of circulating, bound estrone to E2 in the liver.…”

Section: Types and Routes Of Administration Of Postmenopausal Estrogementioning

confidence: 99%

Sex Hormones and Vascular Function

Bowling¹,

Oparil²,

Hage³

et al. 2012

Sex Hormones

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Pharmacokinetics and pharmacodynamics of transdermal dosage forms of 17β-estradiol: Comparison with conventional oral estrogens used for hormone replacement

Cited by 279 publications

References 12 publications

Hormone replacement therapy (oestradiol-only preparations): can the laboratory recommend a concentration of plasma oestradiol to protect against osteoporosis?

Hormone replacement therapy (oestradiol-only preparations): can the laboratory recommend a concentration of plasma oestradiol to protect against osteoporosis?

Methods for endometrial preparation in frozen-thawed embryo transfer cycles

Sex Hormones and Vascular Function

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