Gene/Protein Disease Symptom Drug Enzyme Compound
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Query: UMLS:C0600142 (hot flushes)
 1,242 document(s) hit in 31,850,051 MEDLINE articles (0.00 seconds)

In an open prospective study with therapeutic monitoring, 34 women with climacteric symptoms, FSH > 40 IU/L and LH > 25 IU/L were treated for 12 months with an estradiol-depot-patch (Estraderm TTS) 50 micrograms twice a week and medroxyprogesterone acetate 10 mg tablets from 12th to 25th day of cycle. During the first months a significant improvement was seen in hot flushes and other climacteric inconveniences in terms of Kupperman's menopause index. During the study period FSH and LH were suppressed and the estrogen values were normalized. The fraction of free estradiol compared to protein bound estradiol remained unchanged during the whole treatment. The serum-lipids and serum-SHBG at inclusion were within normal limits and did not change during 12 months of treatment. Thus from these parameters no sign of any liver induction was seen. Ten patients had short term skin symptoms while four withdrew from the study because of persistent skin symptoms. Nine patients withdrew from the study, in five cases this was related to the therapy while in the other four it was due to other causes. Twenty-five (74%) women wished to continue the treatment after 12 months.
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PMID:Long-term treatment with transcutaneous estradiol and oral medroxyprogesterone acetate. 133 17

In an open-label, multicentric randomized trial the efficacy and tolerability of Estraderm TTS, a 17 beta-estradiol, and Premarin, consisting of conjugated estrogens, were compared in the treatment of the climacteric syndrome. 84 patients with manifest menopausal complaints were randomized into two groups of 42 women each. The duration of treatment was 11 weeks or 3 cycles, each with 3 weeks of estrogen treatment followed by a therapy-free week. Therapeutic efficacy was assessed with a questionnaire recording frequency and intensity of hot flushes and of sweating episodes during the night, changes in psychic well-being, frequency of micturition and dryness of the vagina. Systemic and local tolerability was also evaluated. Both substances proved almost equivalent in the treatment of menopausal complaints, although Estraderm TTS was markedly superior in suppressing vasomotor symptoms.
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PMID:[Treatment of climacteric syndrome using Estraderm TTS and premarin in a comparative study]. 133 8

The objective was to assess the efficacy and acceptability of a new transdermal norethisterone device as part of a hormone replacement therapy (HRT) regimen. The design was an open prospective clinical assessment for 6 months. The setting was the Academic Unit of Obstetrics and Gynaecology, Royal London Hospital, Whitechapel, London. Eighteen patients of confirmed menopausal status were recruited. Therapy consisted of continuous application of Estraderm TTS 50 (Ciba Laboratories) for a 28-day period, with the additional application of two norethisterone acetate patches in the last 12 days of this period. This schedule was repeated for six cycles. The main outcome measures were symptom and menstrual data--haematological indices, hepatic and renal function; lipid parameters; endometrial biopsy. The results showed a significant improvement in the patients' symptoms of hot flushes and sweating (P = 0.03). Of the 15 women who completed at least 6 months of medication, withdrawal vaginal bleeding was established at regular intervals in 9. One patient had a local irritant reaction to the patch. There were no significant changes observed in haematological indices, hepatic and renal function. There was a slight but not statistically significant decrease in the HDL cholesterol fraction when the patient was in the norethisterone phase of the cycle, but no change was observed between the beginning and end of the study. Histological examination of the endometrial biopsies showed features of secretory activity in 56% of samples after 6 months. There was no evidence of hyperplasia, pre-malignant or malignant changes in the remaining biopsies.(ABSTRACT TRUNCATED AT 250 WORDS)
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PMID:Hormone replacement therapy by the transdermal administration of oestradiol and norethisterone. 801 5

This randomized trial was designed to assess the efficacy, tolerability, and acceptability of two different transdermal estradiol replacement therapies: Cilag Estradiol-TTS (a matrix system) and Ciba-Geigy Estradiol-TTS (a reservoir system). Five hundred and fourteen patients were evaluable for efficacy, and all patients who had received the study medications were evaluated for safety (n = 530). Both treatments significantly improved systemic and urogenital symptoms as evidenced by a decrease in the number of hot flushes and the Kupperman Index score; there was no difference in effectiveness between the two treatments. Safety evaluation revealed a low incidence of adverse events, mainly compatible with exogenously administered estrogen and progestagen. Endometrial biopsies at the end of treatment were similar between groups and consistent with balanced hormone replacement therapy. Analyses of acceptability data revealed a low incidence of skin reactions and an added benefit with the Cilag-Estradiol-TTS patch in terms of convenience owing to the adhesiveness of the patch. In conclusion, both transdermal estradiol replacement therapies were effective and well tolerated in the treatment of postmenopausal estrogen deficiency symptoms, and the Cilag Estradiol-TTS patch had an advantage in terms of convenience and adhesiveness.
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PMID:A randomized study to compare the effectiveness, tolerability, and acceptability of two different transdermal estradiol replacement therapies. The Transdermal HRT Investigators Group. 848 12

Two-hundred and five (205) menopausal women with moderate to severe vasomotor symptoms, aged 39-64 years, were randomized from 20 clinical centers. After a 4-week treatment-free period, each woman received a cyclical regimen (25 days of a 4-week cycle) of Menorest 50, a new matrix-type transdermal estradiol system or Estraderm TTS 50, a marketed reservoir-type transdermal estradiol system twice weekly for 12 weeks. An oral progestin was also given for 10 days each cycle. The objectives were to compare local and systemic tolerability and efficacy in the treatment of menopausal symptoms. One-hundred and ninety-four [194] patients (96 and 98 patients in the Menorest 50 and the reservoir transdermal patch groups, respectively) were considered in the intent-to-treat population and 204 (102 in each group) in the safety population. The two treatment groups were comparable with regard to the demographic data and menopausal status. The primary efficacy criteria were the comparison between Menorest 50 and the reservoir transdermal patch in erythema and pruritus at application sites and the difference between the treatment groups in the mean number of hot flushes per day at week 12, adjusted for baseline. A statistically significant reduction in the mean number of hot flushes was observed in each group compared with baseline, with a decrease from 6.5 at baseline to 0.3 at 12 weeks and 6.4 to 0.4 in the Menorest 50 and reservoir transdermal patch groups respectively; there was no statistically significant difference between the two groups during the 12-week treatment. The severity score of menopausal symptoms was also dramatically improved in each of the two treatment groups. There were no statistically significant differences in the mean plasma estradiol concentrations and mean estradiol to estrone ratio (> 1.0) in both groups after 10 weeks of therapy. A similar number of adverse events was observed in both groups. Menorest 50 showed better local tolerability than the reservoir transdermal patch with a lower incidence of topical adverse events, erythema and pruritus. In summary, Menorest 50 was as effective as the reservoir transdermal patch in reducing the mean number of hot flushes, and improving the severity of other menopausal symptoms, including vasomotor, psychiatric and urogenital symptoms.
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PMID:Efficacy and tolerability of Menorest 50 compared with Estraderm TTS 50 in the treatment of postmenopausal symptoms. A randomized, multicenter, parallel group study. 874 78

This study was designed to compare the efficacy and safety of two sizes of Lyrelle, a new matrix design transdermal oestrogen patch, with Estraderm TTS 50, a reservoir system. Three hundred and ninety-four (394) hysterectomised postmenopausal women between 30 and 65 years of age participated in this open-label, randomised, multicentre clinical trial. The main efficacy criterion was the reduction in the mean number of hot flushes per day at six months. Secondary efficacy end points included other climacteric symptoms as well as various psychofunctional and genitourinary disorders. A significant decrease from baseline in the mean number of hot flushes/day was observed in all three groups from the end of cycle 1, reaching 90% at the end of cycle 7. there was no statistically significant difference between Lyrelle 50 and Estraderm at any time point for any parameter; however, between-group differences between Lyrelle 80 and Estraderm for various parameters were seen in the first three cycles in favour of Lyrelle 80. A similar impact on blood lipid levels was observed in all three groups, without significant between-group differences. We conclude that the new Lyrelle patch is a highly effective system for transdermal oestrogen replacement therapy that may enhance long-term patient compliance.
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PMID:A randomised study to compare the efficacy and safety of new 17 beta-oestradiol transdermal matrix patch with Estraderm TTS 50 in hysterectomised postmenopausal women. The Lyrelle Study Group. 915 67

The failure of follicular development that characterizes the menopause leads to a marked reduction in serum levels of estradiol and progesterone. As a result, the majority of women develop symptoms, including hot flushes, sleep disturbance, and vaginal dryness. Long-term consequences of ovarian insufficiency include genital atrophy, osteoporosis, and increased rates of myocardial infarction. Estradiol replacement (ERT) has proved effective in treating and preventing these problems. ERT has, however, led to increased risk of endometrial carcinoma. Consequently, treatment regimens now include progestins (HRT) to protect women who have a uterus. Progestins act by down-regulation of estradiol receptor activity, which is an advantage for preventing endometrial hyperstimulation, but a potential disadvantage when beneficial effects of estradiol are opposed. Current menopause health care includes assessment, treatment, and follow-up. Signs and symptoms of estradiol deficiency are evaluated during initial history-taking and physical examination. The MENSI (Menopause Symptom Index) has proved an efficient questionnaire for both initial assessment and monitoring of treatment effects. Vaginal cell maturation index (M.I.) can be helpful in determining need for hormonal treatment and for assessing response to treatment. A "therapeutic range" for ERT can be achieved with the availability of a variety of hormone preparations administered in different ways (oral, transdermal, skin gel, implants, etc.), thus avoiding the problems of both inadequate and excessive hormonal doses. This paper will describe a structured approach to the delivery of health care in the menopause.
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PMID:Hormone replacement therapy in the menopause. 916 Feb 17

The present studies evaluated the effect of estrogens and the selective estrogen receptor modulator (SERM) tamoxifen and raloxifene in a rat model for hot flush. In this model, ovariectomized rats were treated for 8 or 9 days either sc or po. Rats were dependent to morphine by implanting a morphine pellet (75 mg each) sc on days 3 and 5 of treatment. On the last day of treatment, a thermistor, connected to a data acquisition system, was placed on the tail of each animal and morphine addiction was withdrawn by naloxone injection (1.0 mg/kg, sc). Temperature measurements were taken for 1 h under ketamine (80 mg/kg, im) anesthesia. In general, vehicle treated rats showed a 5-6 degrees C elevation of their tail skin temperature with the peak occurring about 15 min after naloxone injection. 17 alpha-Ethinyl estradiol (EE) was evaluated both sc and po using a broad range of doses. The IC50 for inhibition of tail skin temperature rise was approximately 0.1 mg/kg, sc and 0.2 mg/kg, po. 17 beta-Estradiol and 17 alpha-estradiol were also active in this model whereas non-estrogenic steroids were inactive. Raloxifene and tamoxifen were tested for estrogen agonist and antagonist activity administered sc and po. Raloxifene did not demonstrate reproducible estrogen agonist activity at doses up to 10 mg/kg, whereas it demonstrated significant antagonistic activity at the 10 mg/kg dose regardless of the route of administration. Tamoxifen exhibited significant estrogen agonist activity at all doses tested (0.1-10.0 mg/kg) and was a significant antagonist of EE at the 1.0 mg/kg dose. Our results demonstrate the potential utility of this model to evaluate and discriminate among classes of compounds with varying degrees of estrogen agonist and antagonist activity.
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PMID:The effect of estrogens and antiestrogens in a rat model for hot flush. 988 31

Oestradiol, clonidine, tibolone and raloxifene were tested for their effects on the tail temperature of oestrogen deficient rats, a potential new model that can be used to test compounds that may be of use in the treatment of hot flushes in humans. Rats underwent ovariectomies or sham operations and their tail temperature and physical activity were measured telemetrically. Oestrogen depletion affected tail temperature in the rats' active, but not their resting phase. During the transition from the resting to the active phase, tail temperature in normal rats dropped by about 6 degrees C, but only by approximately 1 degrees C after ovariectomy. Treatment of the ovariectomised rats with oestrogen, clonidine or tibolone dose-dependently restored the drop in tail temperature. However, raloxifene did not change the tail temperature of ovariectomised rats. Thus, tibolone and raloxifene have different effects on the temperature regulation in the tail. This method of measuring tail temperature free of stress in ovariectomised rats may serve as a useful procedure for selecting compounds that are of potential use in the treatment of hot flushes.
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PMID:Effect of tibolone and raloxifene on the tail temperature of oestrogen-deficient rats. 1134 29

The purpose of the present study was to further evaluate the tail-temperature test as a tool to test potential steroidal and non-steroidal compounds for the treatment of hot flushes. Ovariectomized rats were implanted with a temperature sensitive probe. After a recovery period of 5 weeks, the effect of oestradiol (given via a silastic tube) and the 5-HT(2) receptor antagonist mirtazapine (10 mg/kg i.p.) on the tail-temperature in the active phase of the animals was measured. Oestradiol completely restored the disturbed tail temperature after 3 days. Treatment with mirtazapine also restored the oestrogen withdrawal-induced disturbed tail-temperature. The effect of mirtazapine was already seen on the first day of treatment. These experiments confirm and extend the idea that measuring the oestradiol withdrawal-induced disturbance of tail-temperature may be a useful tool to select compounds that might have beneficial effects in the treatment of hot flushes. Blockade of the 5-HT(2A) receptors prevented or reduced the ovariectomy-induced disturbance of the rat tail-temperature, which may validate this model to evaluate the effect of compounds on hot flushes.
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PMID:Oestradiol and mirtazapine restore the disturbed tail-temperature of oestrogen-deficient rats. 1466 40


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