PubMed · 8816638
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S L Corson. 1996. Assay variables.. https://doi.org/10.1016/s0015-0282(16)58589-6
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BACKGROUND: A long-acting parenteral depot estrogen, polyestradiol phosphate (PEP), which has been in clinical use for several years in combination therapy, has been reevaluated pharmacokinetically and clinically as a single treatment. The present report describes a model predicting the effect on testosterone flux achieved with this estrogen drug. METHODS: Data on serum levels of estradiol and testosterone from a single-dose study, in prostate cancer patients as well as data from injections of 240 or 320 mg PEP each fourth week, were used for pharmacokinetic/dynamic modeling. RESULTS: Serum concentrations of estradiol were governed by a flip-flop mechanism when administered as PEP. An indirect-response model fitted to individual data showed a value of about 500 pmol estradiol/l serum to get a 50% suppression of serum testosterone concentrations. CONCLUSIONS: This model could successfully predict the serum levels of estradiol and testosterone after repeated injections at different doses and was also used to simulate the testosterone suppressing effect of a new dose regimen.
HISTORY AND CLINICAL FINDINGS: A 51 year old female patient complained about marked pruritus of the whole integument. Since seven years she had been taking a two phase combination of estrogens and gestagen because of climacteric symptoms. 24 years ago severe pruritus occurred especially at the hands during the last trimenon of her first pregnancy whereas 7 years later during the subsequent pregnancy pruritus was absent. Physical examination revealed multiple excoriations over the whole body. No other relevant pathological findings were noted. INVESTIGATIONS: Laboratory findings, chest X-ray and abdominal sonography were normal. TREATMENT AND COURSE: Neither oral administration of an antihistaminic drug nor topical application of betamethasone improved the situation to a relevant extent. For 12 months the occurrence of pruritus had not been referred to hormonal treatment by the physicians in charge. Complete cessation of pruritus was seen within a few days after the patient had stopped hormonal medication on her own. CONCLUSION: Patients should be asked for pregnancy associated pruritus or jaundice before receiving drug combinations with estrogens and gestagens. In case of a positive history, the physician should inform them about possible side effects such as pruritus and icterus.
BACKGROUND: Estrogens have vascular effects through the activation of estrogen receptors (ERs). In addition to ERalpha, the first ER to be cloned, a second subtype called ERbeta has recently been discovered. METHODS AND RESULTS: Using a reverse-transcriptase polymerase chain reaction assay that employs the same primer pair to simultaneously amplify ERalpha and ERbeta transcripts, we found that ERbeta is the ER form that is predominantly expressed in human vascular smooth muscle, particularly in women. The transcriptional effects of the 2 ERs in transfected HeLa cells differed. In response to 17beta-estradiol, ERalpha is a stronger transactivator than ERbeta at low receptor concentrations. However, at higher receptor concentrations, ERalpha activity self-squelches, and ERbeta is a stronger transactivator. Tamoxifen has partial agonist effects with ERalpha but not with ERbeta. CONCLUSIONS: The protective effects of estrogens in the cardiovascular system of women may be due to the genomic effects of ERbeta in vascular tissue.