Our library of drug research abstracts drawn from the medical literature is updated on a regular schedule, and you can be assured that new estraderm research articles will be listed here shortly after becoming available to us.
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Medical research on estraderm
J Obstet Gynaecol. 1998 Nov; 18(6): 575-80
Bowen A, John VA, Ramirez ME, Good WR
This open-label, randomised, two-way crossover study compared the steady-state bioavailability of oestradiol administered by way of a new oestradiol matrix transdermal delivery system (Alora 0.1 mg/day) with that of Estraderm (0.1 mg/day) in 24 subjects. Serum oestradiol, oestrone and oestrone sulphate concentrations were determined by measurement of blood samples. Mean SD pre-dosing, nonadjusted oestradiol levels for Alora (71.9 27.0 pg/ml) were substantially higher than those for Estraderm (26.7 9.7 pg/ml), while peak oestradiol concentrations were comparable. Consequently, fluctuations in steady-state levels were substantially smaller for Alora than for Estraderm; the fluctuation index values (\[C- C ])/ max min C ) were significantly lower for Alora (0.97 0.23) than av for Estraderm (1.68 0.45). Oestradiol levels remained constant over the dosing interval with Alora but decreased significantly after 48 hours with Estraderm. The bioavailability of oestradiol with Alora was 127 56% that of Estraderm. Oestrone and oestrone sulphate data showed the same qualitative and quantitative differences between the two systems. Both systems were well tolerated. In summary, Alora delivered more oestradiol to the systemic circulation with greater consistency and over a longer time than did Estraderm.
Clin Endocrinol (Oxf). 2003 Dec; 59(6): 690-8
Nugent AG, Leung KC, Sullivan D, Reutens AT, Ho KK
OBJECTIVE: Oral but not transdermal oestrogen administration reduces IGF-I, and increases GH binding protein (GHBP) reflecting effects on hepatic endocrine function in postmenopausal women. As progestogens attenuate the effects of oestrogen on circulating lipid levels according to their androgenic properties, we have investigated the impact of progestogen types on the hepatic endocrine effects of oestrogen. DESIGN: Four progestogens differing in androgenicity were co-administered in a monthly cyclical regimen in random order to postmenopausal women receiving either oral (n = 9, premarin 1.25 mg) or transdermal (n = 10, Estraderm 100 microg patches twice weekly). The four progestogens were cyproterone acetate (CA 5 mg, antiandrogenic), dydrogesterone (20 mg, neutral), medroxyprogesterone acetate (MPA 10 mg, mildly androgenic), norethisterone (2.5 mg, androgenic). PATIENTS: Nineteen postmenopausal women (age 57 +/- 3 years, mean +/- SE) were studied. MEASUREMENTS: The effects of oestrogen alone and the combined effects with each progestogen type on IGF-I, GHBP, SHBG, cholesterol, triglycerides and lipoprotein(a) were investigated. RESULTS: Mean IGF-I fell while GHBP and SHBG levels increased with oral (P < 0.01) but not transdermal oestrogen administration. When the combined effects were examined, progestogens did not affect IGF-I, GHBP and SHBG during oral oestrogen treatment, while they significantly increased (P < 0.01) mean IGF-I levels during transdermal therapy. Among the progestogen types, only norethisterone prevented the fall in IGF-I induced by oral oestrogen. During transdermal therapy, MPA and norethisterone but not CA or dydrogesterone significantly increased (P < 0.005) IGF-I. The rise in GHBP induced by oral oestrogens tended to be lower during co-administration of MPA and norethisterone. The increase in SHBG induced by oral oestrogen was attenuated (P < 0.05) by norethisterone which was the only progestogen that lowered SHBG (P < 0.05) during transdermal oestrogen treatment. Mean IGF-I was higher (P < 0.001), GHBP and SHBG lower during co-administration of androgenic progestogens (MPA and norethisterone). CONCLUSIONS: Oestrogen effects on IGF-I, GHBP and SHBG are dependent on the route of administration with progestogens having variable effects. Among the progestogen types, norethisterone, the most androgenic, had the greatest effect, particularly on IGF-I. Progestogens modulate the effects of oestrogen on hepatic endocrine function in relation to their intrinsic androgenic properties. The modulatory effects of progestogens on IGF-I during oestrogen therapy may have long-term implications for lean body mass.
Drug Dev Ind Pharm. 2002 Nov; 28(10): 1251-9
Fauth C, Wiedersberg S, Neubert RH, Dittgen M
Standard tensile strength and peel adhesion tests were carried out to investigate interactions of pressure-sensitive adhesives (PSAs) with several backing foils used for transdermal patches. Seven branded transdermal patches (Alora, Cutanum, Estraderm MX 50, Estraderm TTS 50, Fem7 -50 micrograms, Menorest, Oesclim) were included in the investigation. Their skin adhesion measured in several clinical trials was compared with the results of the laboratory measurements according to PSTC-1 (Peel Adhesion for Single Coated Tapes 180 degrees Angle, Pressure Sensitive Tape Council, Illinois, 1996), such as Young's modulus at 3% elongation and peel adhesion to stainless steel. Data obtained for the PSA-coated backings (laminates) show increasing elasticity with increasing PSA thickness. Interactions of PSAs with backing foil became evident in significant changes in Young's modulus by low PSA thickness, as seen for the silicone adhesive. The Young's moduli of the laminates were found to be influenced not only by the elasticity of the backing foil but also by the chemical structure of the PSA. There was no correlation between the elasticity and peel adhesion of both the laminates and the branded patches. Likewise, for the branded patches the peel adhesion to stainless steel does not correlate with skin adhesion values obtained from clinical trials. The Young's modulus of the branded patches was between 4 N/mm2 (Oesclim) and 501 N/mm2 (Fem7). For the branded transdermal patches no correlation was found between Young's modulus and both the peel force on stainless steel and the skin adhesion reported in studies.
Acute effects of transdermal 17beta-estradiol on hemostatic variables after 24-hour treatment.
Clin Appl Thromb Hemost. 2002 Jul; 8(3): 239-43
Hognert H, Ghanoum B, Gustafsson H, Milsom I, Manhem K
The aim of this study was to investigate the acute effects of transdermal 17beta-estradiol (Estraderm) on plasma levels of coagulatory and fibrinolytic factors in postmenopausal normotensive and hypertensive women. Eleven normotensive and 13 hypertensive women were included in this placebo-controlled crossover study. In a randomized order each subject was treated with a patch of 100 microg 17beta-estradiol or placebo for 24 hours. Serum levels of tissue type plasminogen activator (tPA) activity, plasminogen activator inhibitor-I (PAI-1) activity, tPA antigen, PAI-I antigen, FVII, FX, and fibrinogen were assayed after both treatments. There was no significant difference in serum levels of hemostatic variables after treatment with estrogen compared to levels after placebo treatment in either of the groups. Nor was there any measurable difference when comparing hypertensive and normotensive subjects.
Eur J Obstet Gynecol Reprod Biol. 2002 Jun 10; 103(1): 43-7
Banz C, Katalinic A, Al-Hasani S, Seelig AS, Weiss JM, Diedrich K, Ludwig M
Supernumary pronucleated stage oocytes (PN) can be cryopreserved and later transferred in spontaneous, stimulated or artificial cycles. In this study, we re-evaluated 342 artificial cycles with a transdermal estradiol release system (Estraderm TTS 100) in combination with a vaginal progesterone delivery system (Crinone 8%). Endometrial thickness and serum estradiol on day 14 were correlated with clinical and ongoing pregnancy rates. Endometrial thickness between 7 and 15 mm did not relate to significantly different pregnancy rates. The estradiol serum level did not predict success. In conclusion, this method of endometrial preparation is comfortable for patients and monitoring is unnecessary.
Arch Gynecol Obstet. 2002 Jan; 266(1): 38-43
Sendag F, Karadadas N, Ozsener S, Bilgin O
The aim of this study was to compare the effects of sequential combined transdermal and oral postmenopausal hormone replacement therapies on serum lipid-lipoprotein profiles risk markers for cardiovascular disease. A prospective randomize study was designed: Ninety-six healthy nonhysterectomised postmenopausal women were randomized to receive either transdermal continuous 17beta-estradiol, 0.05 mg/d (Estraderm TTS, Novartis, Basel, Switzerland), with transdermal sequential norethisterone acetate, 0.25 mg/d (Estragest TTS, Novartis, Basel, Switzerland), or oral continuous conjugated equine estrogens, 0.625 mg/d (Premarin 0.625 mg, Wyeth, Philadelphia, U.S.A.), with oral sequential medroxyprogesterone acetate, 10 mg/d (Farlutal 5 mg, Deva, Istanbul, Turkey). 84 women completed the trial, 42 in oral and 42 in the transdermal group. The serum levels of total cholesterol, LDL-cholesterol, HDL-cholesterol, triglycerides, apolipoproteins AI and apolipoproteins B at 6 months after starting treatment were compared with baseline values for both therapies. Both oral and transdermal therapies significantly reduced serum levels of total cholesterol (208-190 mg/dL and 216-199 mg/dL, respectively, p=0.0001) and LDL-cholesterol (128-112 mg/dL and 140-127 mg/dL, respectively, p=0.001). The serum levels of triglycerides did not show any significant change with oral therapy, whereas this lipid fell (128-101 mg/dL, p=0.0001) significantly with transdermal therapy. We found significant decrease in HDL-cholesterol with transdermal therapy while there was no significant change with oral therapy. Apolipoproteins AI, the major protein component of HDL2 subfraction, was increased by oral therapy and lowered by transdermal therapy. As a conclusion, we have found that serum total cholesterol and LDL-cholesterol were lowered by both therapies, with no significant differences between treatments, whereas there were significant differences between treatments according to effects on serum triglycerides and apolipoproteins AI.
Climacteric. 2000 Sep; 3(3): 168-75
Reginster JY, Donazzolo Y, Brion N, Lins R
OBJECTIVE: A new matrix 17 beta-estradiol transdermal patch incorporating lauric acid to improve estradiol skin absorption has been designed for hormone replacement therapy. Estradiol pharmacokinetics obtained with the prototype, its industrial counterpart, a matrix-type, System 50, and a reservoir-type, Estraderm TTS 50, transdermal patch have been compared. Each device delivers 50 micrograms estradiol daily. METHODS: Twenty postmenopausal women received each of the four formulations for 3 days in a Latin-square design and with a minimum 4-day wash-out period between treatments. Estradiol plasma concentrations were measured by radioimmunoassay at 6, 12, 24, 48 and 72 h after application. RESULTS: The prototype patch and its industrial counterpart showed no significant difference in estradiol delivery, with 72-h systemic exposure to estradiol similar to that of the reservoir patch but greater than that of the reference matrix formulation, with average baseline-corrected concentrations (SEM) of 35 (4), 32 (3), 32 (2) and 19 (1.8) pg/ml, respectively. In addition, they ensured more stable delivery, with coefficients of variation of plasma estradiol concentrations (12-72 h) of 29, 41, 63 and 84%, respectively. All matrix patches demonstrated the same patients to be poor estradiol absorbers, different from those encountered with the reservoir patch type, despite an improved estradiol bioavailability with the lauric acid-containing matrix patch. CONCLUSION: Matrix patches incorporating lauric acid led to estradiol plasma levels more stable than with the reference matrix and reservoir patches, and greater than those with the reference matrix patch.
Influence of exogenous estrogen administration on serum CA-125 originating from the endometrium.
Int J Gynaecol Obstet. 2002 Feb; 76(2): 169-72
Karabacak O, Ilgin N, Tiras B, Gursoy R, Himmetoglu O
OBJECTIVES: The purpose of the study is to assess the endometrial contribution of serum CA-125 using exogenous estrogen administration by ruling out ovarian activity. A randomized, controlled, prospective study was designed to assess the endometrial contribution of serum CA-125 and its influence from estrogen administration in menopausal women. METHODS: Twenty menopausal women with intact uterus and ovaries (study group) and 10 cases with previous total hysterectomy with intact ovaries (control group) were included in the study. The mean age of subjects in the study and control groups were similar at 53 +/- 1.9 (S.D.) and 51 +/- 2.7 years. The length of menopause in the study and control groups were also similar at 61.0 +/- 18 and 52.6 +/- 26.5 months, respectively. Group 1 consisted of 10 randomly selected cases and five controls who received 15 days of 50 microg/day transdermal 17beta-estradiol (TE). Group 2 consisted of the next randomly selected 10 cases and five controls who had 15 days of transdermal 100 microg/day 17beta-estradiol (Estraderm-Ciba) administration. Serum CA-125 and estradiol were measured at day 0, 15 by radioimmunoassay (RIA). RESULTS: Serum mean CA-125 levels increased significantly in endometrium intact menopausal women from day 0 to 15 of TE administration in group 2 and 1, 70% and 6%, respectively (P=0.03 and P=0.05, respectively). Interestingly, the increase in serum estradiol levels accompanied this change only in group 2. CONCLUSIONS: These results suggest that endometrial CA-125 secretion to serum is dependent on the dose of administered exogenous estrogen.
Maturitas. 2001 Dec 14; 40(3): 203-9
Paoletti AM, Pilia I, Nannipieri F, Bigini C, Melis GB
OBJECTIVES: to compare the patterns of a 17 beta-estradiol (E(2)) gel containing 0.6 mg/g (1.5 mg E(2) per day, Gelestra); with the transdermal delivery system (Estraderm TTS 50) applied every 3 days over a 14-day period to women in spontaneous or surgical menopause. METHODS: a single centre, open, randomised, parallel-group study was conducted. A total number of 33 postmenopausal women were enrolled. In 23 of them the menopause occurred spontaneously, while 10 women were bilaterally ovariectomized. Randomly, the subjects were treated with Estraderm TTS 50 (no. 8) or with Gelestra (no. 14). The pharmacokinetic study of the drugs was performed at the seventh, ninth and 14th day in Gelestra treated women and at the first, third and second day in Estraderm TTS 50 treated women. In fact, the seventh, ninth and 14th day of percutaneous treatment corresponds to the first, third and second day of application of the transdermal system application. Blood samples were taken by each subject at baseline and 1, 2, 3, 4, 8, 12 and 24 h after the gel or transdermal system application. In almost all samples the level of E(2) and estrone (E(1)) were evaluated. Statistical analysis was performed by comparing the two groups of treatment. The following parameters were assessed: mean E(2) and E(1) concentrations, E(2) peak serum concentration within interval from 0 to 72 h (C(max)), E(2) trough concentration within interval from 0 to 72 h (C(min)), area under the E(2) time concentration curve in the interval from 0 to 72 h (AUC((0-72))), the average E(2) concentration during the measurement interval, calculated by dividing AUC((0-72)) by 72 h (C(av)), E(1)/E(2) ratio, and percentage fluctuation (%Fluct) which is equal to 100 (C(max)-C(min)/C(max)). RESULTS: there was no significant difference in E(2) C(av) between the two treatments. However, significant differences in favour to the gel on the first day (first h) and on third day (72nd h) and in favour to the patch at the second day (48th h) were detected. C(max), E(1)/E(2) ratio and AUC((0-72)) were not statistically different, while a significantly higher C(min) for the gel was observed. Furthermore, the 90% confidence interval for AUC((0-72)) ratio (0.83-1.10) was within the commonly applied bioequivalence acceptance range (0.80-1.25). The %Fluct was significantly lower for Gelestra than for Estraderm TTS 50. CONCLUSIONS: although the mean E(2) and E(1)concentrations, C(max), E(1)/E(2) ratio and the AUC((0-72)) did not differ between the two E(2) treatments, the Gelestra treatment showed a lower day-to-day variation over the three day application, than the Estraderm TTS 50.
The influence of hormone replacement therapy on skin ageing: a pilot study.
Maturitas. 2001 Jul 25; 39(1): 43-55
Sator PG, Schmidt JB, Sator MO, Huber JC, Hönigsmann H
OBJECTIVES: We studied the effect of hormonal treatment on skin ageing in menopausal women. METHODS: Twenty-four patients (45-68 years; mean age, 54.9 years) without hormone treatment for at least 6 months were included. Patients were assigned to three therapy groups: 1, oestrogen only (Estraderm TTS 50) (n=6); 2, transdermal oestrogen and progesterone (Estraderm TTS 50 and 0.4 mg progesterone vaginal suppository) (n=7); and 3, oral oestrogen and progesterone (2 mg Progynova and 0.4 mg progesterone vaginal suppository) (n=8). One group without therapy was included as a control group (n=3). Treatment was continued for 6 months. Three patients, one from group 2 and two from group 3, discontinued therapy before the study endpoint. The following skin parameters were measured at monthly intervals during treatment: skin surface lipids, epidermal skin hydration, skin elasticity and skin thickness. Concomitant clinical evaluation included a subjective clinical evaluation form, a patient questionnaire and laboratory tests for oestradiol, progesterone and follicle stimulating hormone. RESULTS: Mean levels of epidermal skin moisture, elasticity and skin thickness were improved at the end of treatment based on both subjective and objective evaluation in patients with hormone replacement therapy (HRT). Skin surface lipids were increased during combined HRT, which may reflect stimulatory effects of the progestagen component on sebaceous gland activity, while oestrogen alone has a sebum-suppressive action. In the HRT groups, the questionnaire for climacteric complaints demonstrated significant improvements, while laboratory tests showed increases in oestradiol and progesterone and decreases in FSH. CONCLUSIONS: HRT with the mentioned regimes significantly improved parameters of skin ageing.