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PubMed1994

Self-administered Nicotine-Dependence Scale (SANDS): item selection, reliability estimation, and initial validation.

The Self-Administered Nicotine-Dependence Scale (SANDS) is a questionnaire to assist in the determination of the most appropriate intervention for the nicotine-dependent individual. Six content domains included are: (1) self-efficacy; (2) social skills deficit; (3) loss of control; (4) consequences of use; (5) social support for smoking; and (6) concern for healthy life-style. A preliminary set of 79 items was reduced to a 32-item scale, which, in turn, was divided into two non-overlapping subscales of 16 items each. Logistic regression analyses of an additional sample of subjects indicated that the SANDS added predictive power to knowledge of sex and transdermal-patch status for predictions of smoking status 6 months later.

Adult↗
PubMed2004

Scopolamine for preventing and treating motion sickness.

BACKGROUND: Motion sickness - the discomfort experienced when perceived motion disturbs the organs of balance - may include symptoms such as nausea, vomiting, pallor, cold sweats, hypersalivation, hyperventilation and headaches. The control and prevention of these symptoms have included pharmacological, behavioural and complementary therapies. Although scopolamine has been used in the treatment and prevention of motion sickness for decades, there have been no systematic reviews of its effectiveness. OBJECTIVES: To assess the effectiveness of scopolamine versus no therapy, placebo, other drugs, behavioural and complementary therapy or two or more of the above therapies in combination for motion sickness in persons (both adults and children) without known vestibular, visual or central nervous system pathology. SEARCH STRATEGY: The Cochrane Ear, Nose and Throat Disorders Group Specialised Register, the Cochrane Central Register of Controlled Trials (The Cochrane Library, Issue 4, 2003), MEDLINE (OVID, 1966 to March Week 1 2004), EMBASE (1974 to 2004) CINAHL (Ovid, 1982 to March Week 1 2004) and reference lists of retrieved studies were searched for relevant studies. No language restrictions were applied. SELECTION CRITERIA: All parallel-arm, randomised controlled trials (RCTs) focusing on scopolamine versus no therapy, placebo, other drugs, behavioural and complementary therapy or two or more of the above therapies in combination were included. Outcomes relating to the prevention of onset or treatment of clinically-defined motion sickness, task ability and psychological tests, changes in physiological parameters and adverse effects were considered. DATA COLLECTION AND ANALYSIS: Data from the studies were extracted independently by two authors using standardised forms. Study quality was assessed. Dichotomous data were expressed as odds ratio (OR) and a pooled OR was calculated using the random effects model. MAIN RESULTS: Of 27 studies considered potentially relevant, 12 studies enrolling 901 subjects met the entry criteria. Scopolamine was administered via transdermal patches, tablets or capsules, oral solutions or intravenously. Scopolamine was compared against placebo, calcium channel antagonists, antihistamine, meth-scopolamine or a combination of scopolamine and ephedrine. Studies were generally small in size and of varying quality. Scopolamine was more effective than placebo in the prevention of symptoms. Comparisons between scopolamine and other agents were few and suggested that scopolamine was superior (versus meth-scopolamine) or equivalent (versus antihistamines) as a preventative agent. Evidence comparing scopolamine to cinnarizine or combinations of scopolamine and ephedrine is equivocal or minimal. Although sample sizes were small, scopolamine was no more likely to induce drowsiness, blurring of vision or dizziness compared to other agents. Dry mouth was more likely with scopolamine than with meth-scopolamine or cinnarizine. No studies were available relating to the therapeutic effectiveness of scopolamine in the management of established symptoms of motion sickness. REVIEWERS' CONCLUSIONS: The use of scopolamine versus placebo in preventing motion sickness has been shown to be effective. No conclusions can be made on the comparative effectiveness of scopolamine and other agents such as antihistamines and calcium channel antagonists. In addition, no randomised controlled trials were identified that examined the effectiveness of scopolamine in the treatment of established symptoms of motion sickness.

Humans↗
PubMed1999

Worsening of motor performance in patients with Parkinson's disease following transdermal nicotine administration.

Nicotine has been reported to have positive effects on motor performance in patients with Parkinson's disease. In this study, motor performance was evaluated in 16 patients with idiopathic Parkinson's disease during a practical off-period using the motor part of the Unified Parkinson's Disease Rating Scale after 12 hours' exposure to a transdermal patch containing 35 mg nicotine or placebo. The study was performed using a double-blind crossover design. In contrast to previous reports, nicotine exposure was followed by a worsening of symptoms compared with placebo. A negative response to subthreshold dopaminergic stimulation, resulting from an inhibitory effect of low striatal dopamine concentrations acting on a subset of dopamine receptors, might possibly account for this finding.

Administration, Cutaneous↗
PubMedDate not supplied

Testosterone release from a subcutaneous, biodegradable microcapsule formulation (Viatrel) in hypogonadal men.

Men with hypogonadism require testosterone replacement for optimal health. In the United States, testosterone is currently administered by daily transdermal patches, topical gels or intramuscular injections every 1-3 weeks. Biodegradable polylactide-co-glycolide microcapsules are currently used for long-term drug delivery in humans. Such microcapsules that contain testosterone could provide a better means of long-term testosterone therapy. We therefore studied the pharmacokinetics and pharmacodynamics of testosterone release from testosterone microcapsules in men with hypogonadism. Fourteen men who had been treated previously with testosterone were enrolled in an open-label, prospective study of testosterone microcapsule administration. Subjects were enrolled if 2 consecutive serum total testosterone levels were lower than 8.7 nmol/L after a 4-week washout from testosterone therapy. Subjects were injected with a single dose of either 267 mg (n = 7) or 534 mg (n = 7) of (Viatrel) testosterone microcapsule, and serum total testosterone, dihydrotestosterone, estradiol, sex-hormone binding globulin, luteinizing hormone, and follicle-stimulating hormone levels were determined at days -14, -7, and 0 before the injection; at days 1, 2, and 7 after the injection; and then weekly thereafter for 8-12 weeks. Mean serum total testosterone levels peaked immediately following injection on day 1 at 25.2 +/- 2.6 nmol/L in the 267 mg group and 34.7 +/- 2.4 nmol/L in the 534 mg group. Total serum testosterone levels declined gradually and fell below 8.7 nmol/L at 42 days after injection in the 267 mg group, and 70 days after injection in the 534 mg group. Estradiol and dihydrotestosterone levels followed a similar pattern. Mean serum free testosterone also peaked immediately following injection on day 1 at 0.51 +/- 0.05 nmol/L in the 267 mg group and 0.97 +/- 0.08 nmol/L in the 534 mg group. No significant adverse reactions were seen, although 2 subjects complained of transient tenderness and fullness at their injection sites. We conclude that a single injection of 534 mg of testosterone microcapsules to men with hypogonadism normalizes serum hormone levels for up to 10-11 weeks, albeit with a pronounced early peak and a relatively long period of low-normal serum total testosterone. Subcutaneously administered testosterone microcapsules may provide a safe and convenient method for the long-term treatment of male hypogonadism or testosterone replacement in male contraceptive regimens.

Affect↗
PubMed2005

Rheology and NMR self-diffusion experiments as well as skin permeation of diclofenac-sodium and cyproterone acetate of new gel preparations.

The viscoelastic properties of two transparent semisolid preparations, one consisting of surfactant, paraffin oil, and water (BAS), and the other consisting of surfactant, cetylstearyl-2-ethylhexanoate, and water (CUBO), were characterized by oscillatory measurements. In (1)H-NMR diffusion experiments it was confirmed that the formulations are O/W systems, and the three-dimensional packing of the closed globular aggregates form a cubic structure. Moreover, standard diffusion experiments with porcine skin using Franz cells were performed with incorporated diclofenac-sodium and cyproterone acetate, respectively. The cumulative amount released after 48 h of diclofenac-sodium were excellent with 665.28 microg/cm(2) and with 36.7 microg/cm(2) for cyproterone acetate. The new drug-containing formulations were also prepared as transdermal patches by using carrageenan as a matrix. In diffusion studies zero-order kinetics was found for both drugs, but with a higher lag time for cyproterone acetate. The total work of adhesion was analyzed by tensile studies on porcine skin and found to be very good. The presented cubic gels as well as mixtures with carrageenan are promising alternative drug carrier systems for topical pharmaceutical as well as cosmetics.

Animals↗
PubMed1995

Permeability of pure enantiomers of ketorolac through human cadaver skin.

The permeability of pure enantiomers of ketorolac acid, a potent non-narcotic analgesic, through human cadaver skin was evaluated. The melting temperature of each enantiomer was 20 degrees C higher than that of the racemic compound. As expected, the solubility of the racemic compound in water and isopropyl alcohol/water/isopropyl myristate (IPA/water/IPM, 50:50:1.5) was roughly 2 times higher than that of the enantiomers. The permeability of the enantiomers through poly(ethylenevinyl acetate) (EVA) synthetic membrane and human cadaver skin was determined with a side-by-side diffusion cell. The skin flux of the racemic compound was about 1.5 times higher than those of the enantiomers. On the other hand, no significant differences in the intrinsic permeability coefficient of the racemic compound and the enantiomers in the EVA membrane and human cadaver skin was observed. An excellent agreement between the predicted and experimental flux ratio of the racemic compound and enantiomer in the EVA membrane and cadaver skin was observed. The IPA/water/IPM (50:50:1.5) provided the highest in vitro skin flux of the S enantiomer among the three vehicle formulations studied. The skin flux of the active pure S enantiomer was ca. 34% higher than that of the impure S enantiomer in the racemic mixture. Furthermore, about 14% intersubject variability in the in vitro skin flux of the S enantiomer was observed. The required skin flux of the S enantiomer as calculated from the pharmacokinetic parameters was about 32 micrograms/cm2/h from a 25 cm2 transdermal patch, which was readily achievable from the IPA/water/IPM (50:50:1.5) ternary vehicle system.

Anti-Inflammatory Agents, Non-Steroidal↗
PubMed2006

Minimal clinically important change in urinary incontinence detected by a quality of life assessment tool in overactive bladder syndrome with urge incontinence.

AIMS: The objective of this research was to detect a minimal clinically important change (MCIC) in frequency of incontinence episodes in Japanese patients with overactive bladder syndrome (OAB) based on the change in domain scores of health-related quality of life (HRQoL). METHODS: The patients (n = 659) enrolled for the 8 weeks, randomized, double-blind, placebo-controlled study of an oxybutynin transdermal patch were used for the analysis. The endpoints of the study were the change in frequency of incontinence episodes and the domain scores of King's health questionnaire (KHQ) from baseline to the end of treatment. To search a threshold of the change of incontinence frequency that apparently improves patient's quality of life (QOL), we calculated mean changes of selected five KHQ domain scores for nine patient groups divided by the amount of change of incontinence frequency. A minimum value of the change of incontinence frequency in the groups with apparent improvement in the QOL scores was defined as an MCIC of incontinence frequency. RESULTS: The apparent improvement of KHQ domain scores was seen in the patient groups whose incontinence episodes decreased more than three times per week (/w) after treatment. This result was common in almost all domain scores, but more relevant for the domains related to patients' life limitations. CONCLUSION: Japanese OAB patients can feel their QOL improved if their incontinence episodes decrease more than 3 times/w. This suggests that the reduction of '3 times /w' is an MCIC of incontinence frequency for Japanese OAB patients.

Administration, Cutaneous↗
PubMed1997

Protein delivery with infusion pumps.

When a therapeutic effect is optimized by precise control of specific temporal patterns of plasma levels, infusion offers distinct advantages over oral administration, bolus injection, or depot delivery of polypeptides. The limitations of oral delivery are well known, and although research is under way into development of carrier systems that prevent degradation of labile agents, it is unlikely that the variances in absorption will meet the need for precise control. Depot delivery from subcutaneous or intramuscular implants presents a difficult situation when local tissue reactions to the agent sometimes occur. Removal of a depot system in the event of adverse reactions presents additional difficulties. Bolus injections are unable to sustain constant plasma levels unless the drug half-life is long or the injections are frequently administered. Insulin injections, for example, would be required every 30-60 minutes to approximate the plasma levels provided by a continuous infusion; such frequent injections would not be practical on a 24-hour basis. For the developer of new polypeptides, parenteral administration offers the most direct route to the marketplace. The step from periodic injections to tightly controlled infusion is a logical progression as compared with modification of the molecules or vehicles to obtain equivalent profiles. In Table II several different types of devices that can be used for infusion of proteins are compared. Microelectronics have played a major role in the miniaturization of infusion devices and undoubtedly will continue to do so. Micromachining, a spin-off technology of integrated circuit manufacture, will also find application in small infusion devices. In the future, we will have cost-effective disposable devices (Saaman et al., 1994) built on this technology that are programmable and thus can be adapted to meet each individual therapeutic need (Horres, 1994). We can also expect to see more closed-loop drug delivery systems where biosensors and infusion devices are combined to optimize a particular therapy. Recent positive results obtained in diabetics by a decade on tight glucose control may forecast a resurgence of popularity of insulin pumps. At the other end of the spectrum, low-cost, small, and simple-to-use osmotically powered systems are close to being marketed; these systems will make infusion almost as convenient as transdermal patches. We will also see major advances in how drugs and devices are interfaced. Prefilled and ready-to-use drug cartridges have proven to be efficient in surgical and emergency medicine and can greatly improve most infusion applications. It is anticipated that coded, prefilled cartridges or pouches will be automatically, recognized by preprogrammed pumps to reduce operator labor and entry error.

Animals↗
PubMed1996

The anti-ulcer drug sucralfate does not affect gastric nicotine levels.

OBJECTIVE: It has been claimed that sucralfate can overcome the negative effects of nicotine in patients with peptic ulcer disease, although the possible mechanism being unknown. This study was performed in order to test whether sucralfate was capable of binding intragastric nicotine, thus making it impossible for the substance to exert effect. METHOD: Nicotine was administered via transdermal patches or as capsules yielding gastric concentrations of 40-2980 ng.ml-1. Gastric juice aspirates (n = 9) were incubated with sucralfate, which was then separated by centrifugation, and the nicotine concentration was compared in incubated and non-incubated samples. RESULTS: A median decrease of 13% (range 0-27%) in nicotine concentration was seen after incubation with sucralfate (P = 0.01). CONCLUSION: The binding of nicotine to the precipitating agent sucralfate is not sufficient effectively to remove nicotine from the gastric juice.

Administration, Cutaneous↗
PubMed1995

Effects of transderman nicotine on mood and sleep in nonsmoking major depressed patients.

The role of nicotine as an indirect cholinergic agent in sleep has been studied in normal subjects. There are no studies of its effects on sleep in depressed patients. Nicotine transdermal patches (17.5 mg), were studied in eight depressed patients (DSM-III-R) and eight normal volunteers. Subjects wore placebo and nicotine patches for 24 h. Depressed patients showed increased REM sleep without changes in other sleep variables. They also showed a short term improvement of mood. Normal volunteers had sleep fragmentation, and reduction of REM sleep time. No major side effects were reported in either group.

Adult↗
PubMed1998

Estrogen replacement therapy modulates spontaneous GH secretion but does not affect GH-RH-induced GH response and low T3 syndrome in women with hypothalamic amenorrhea associated to weight-loss.

Severe dieting and negative energy balance usually lead to the occurrence of amenorrhea together with several endocrine disturbances such as the "low T3 syndrome" and an abnormal GH secretion. To evaluate whether estrogen replacement therapy (ERT) affects thyroid hormones and GH secretion, two groups of patients affected by weight-loss-related amenorrhea and with low plasma T3 levels were treated with two different schedules of ERT using 50 or 100 micrograms estradiol transdermal patches twice a week (Dermestril, Rottapharm, Monza, Italy). Before and after 5 weeks of therapy in each patient thyroid hormones, spontaneous GH secretion and GH-RH-induced GH release were evaluated. After ERT, plasma GH and IGF-1 levels increased in both groups and a consistent change in GH spontaneous release was observed. Conversely the low T3 plasma levels and GH-RH-induced GH response were not modified by ERT. Our present data suggest that in amenorrhea related to weight-loss, hormonal abnormalities are only in part dependent from the hypoestrogenic condition.

Administration, Cutaneous↗
PubMed1997

Scopolamine increases prehensile force during object manipulation by reducing palmar sweating and decreasing skin friction.

The aim of this study was to determine whether relatively long-term changes in skin friction induced by a pharmacological blockade of sweat excretion would alter the grip forces applied to objects of a variety of different surface textures and frictions. Five men and three women were asked to lift the vertically mounted armature of a linear motor between the thumb and index finger and to hold it against an opposing force for 2 s. A 1.0-kHz tone indicated to the subject that the manipulandum had been correctly positioned between the upper and lower position limits. The linear motor generated a 2.5-N force tangential to the skin surface simulating an object weighing approximately 250 g. Three different polyamide plastic surfaces (either smooth or etched with 1.0 mm high Braille beads evenly spaced at 2- or 3-mm intervals) contacted the fingers in these experiments. Subjects lifted and held in a precision grip one of the three surfaces for blocks of ten consecutive trials, but the order of presentation of the three different textures was varied to offset the effect of expectancy. On a second block of ten trials the subjects were requested to release the object slowly to measure the ratio of the grip force normal to the grasped surface to the tangential load force at the moment of slip. This ratio or its inverse provided the coefficient of friction or the slip ratio for a particular subject and surface condition. Twelve hours prior to a second recording session all subjects placed transdermal patches of 1.5 mg scopolamine behind each ear to reduce palmar sweating by blocking the muscarinic receptors of exocrine sweat glands. The subjects were re-tested following procedures that were identical to the first session. Scopolamine significantly reduced the friction of the skin on the smooth and 2-mm beaded surfaces, but the friction of the 3-mm beaded texture was unaffected. Scopolamine also caused subjects to increase both the peak and static grip forces for all the textures including the 3-mm beaded surface, suggesting that for two of the three surfaces they were responding to the increased slipperiness of the skin due to reduced sweat production.

Adult↗
PubMed2001

Withdrawal of hormone replacement therapy is associated with significant vertebral bone loss in postmenopausal women.

This study aimed to assess the changes in vertebral bone mineral density (BMD) after cessation of hormone replacement therapy (HRT) in postmenopausal women who had been treated on a long-term basis. Fifty healthy postmenopausal women who had been followed both during the course of HRT and after cessation of treatment in our menopause clinic were included in this study. All women had started HRT within the first 3 years after the postmenopause and had received HRT (either 1.5 mg/day of 17 beta-estradiol given percutaneously or 50 micrograms/day of 17 beta-estradiol given as a transdermal patch, combined in all women with natural progesterone or a 19-norprogesterone derivative) for a mean 5 +/- 2.4 years. In all women, vertebral BMD was assessed during the course of HRT up to the last 6 months before estrogen withdrawal, then at least once within the first 18 months after cessation of treatment. Of the initial population, 30 women were additionally reviewed later on and up to 8 years after cessation of treatment (mean duration of follow-up for the whole population: 3.9 +/- 1.7 years). Rates of changes in vertebral BMD were compared with those determined in a group of healthy untreated women who had been followed within the first years of postmenopause during the same time period as the study population. In the study group, bone loss was found to accelerate within the first 2 years after HRT withdrawal and the annual rate of loss was identical to that which occurs within the first 2 years of postmenopause in untreated women (-1.64% +/- 1.3% vs -1.52 +/- 0.9%, NS). Beyond this first 2-year time period, the annual rate of bone loss decreased as a function of time following cessation of treatment, as was observed following the menopause in untreated women (between 3 and 5 years: -0.83% + 1.35% in the study group vs -0.70% +/- 0.8% in the control group, NS). On average, 3 years after cessation of HRT mean vertebral BMD when expressed as a Z-score was significantly higher (-0.13 vs -0.89, p < 0.01) than at baseline, before HRT was started, which suggested a lasting beneficial effect on bone mass. However, even though our findings do not support the hypothesis that bone loss might continue to be accelerated several years after cessation of treatment we cannot fully address the question as to whether any residual benefit on bone mass over a longer period of time may be observed. In conclusion, the pattern of bone loss observed after cessation of estrogen therapy was found to be comparable to that which occurs in younger women within the first years after the menopause. Such a pattern needs to be kept in mind when the decision to stop HRT is taken, especially in women who were given HRT to prevent osteoporosis. The issue of assessing their risk of fracture several years after cessation of treatment thus needs to be addressed.

Bone Density↗
PubMed2001

Effects of transdermal nicotine on attention and memory in healthy elderly non-smokers.

RATIONALE: Nicotine has been found to improve cognitive functions in patients with Alzheimer's disease, but little is known about its effects in the healthy non-smoking elderly. OBJECTIVES: This study aimed to investigate the effects of nicotine on cognitive function in healthy non-smoking or nicotine-naïve elderly subjects. METHODS: A transdermal patch containing either 5 mg nicotine or placebo was applied on the back of 63 healthy nicotine-naïve or non-smoking elderly Koreans. Cognitive functions were evaluated with the Short Blessed Test, Rey-Kim Memory Test, and digit span test of the Korean-WAIS, both before and 5.5 h after nicotine administration. The plasma level of nicotine after testing was measured using gas chromatography. RESULTS: The subjects' memory functions in trial 5 of the Rey-Kim Memory Tests improved significantly. Furthermore, the effect on memory slope was significantly correlated with the higher plasma level of nicotine. However, the other tests did not reveal any correlation to a significant degree. CONCLUSIONS: These results suggest that nicotine of lower plasma level can improve short-term verbal memory functions in non-smoking or nicotine-naïve healthy elderly people and that some effects are dependent on nicotine plasma levels.

Administration, Cutaneous↗
PubMed2006

The ORTHO BC-SAT--a satisfaction questionnaire for women using hormonal contraceptives.

OBJECTIVE: To assess the reliability and validity of the ORTHO Birth Control Satisfaction Assessment Tool (ORTHO BC-SAT). DESIGN: 339 women using 1 of 4 hormonal birth control methods (oral contraceptives, transdermal patch, vaginal ring, injections), completed the questionnaire 1-2 times. MATERIALS AND METHODS: The questionnaire was developed based on findings from the literature, focus groups, and interviews. Internal consistency reliability, test-retest reliability, construct validity, and known groups validity were evaluated. RESULTS: Based on variable clustering, 8 domains were identified (Ease of Use/Convenience, Compliance, Lifestyle Impact, Symptom/Side Effect Bother, Menstrual Impact, Future Fertility Concerns, Assurance/Confidence, Overall Satisfaction). Internal consistency reliability was demonstrated with Cronbach's alpha values ranging from 0.70 to 0.89. All multi-item scales reported acceptable test-retest reliability (0.79-0.87). Construct validity was demonstrated by support of a hypothesized pattern of correlations. Known groups validity was confirmed by examining scale scores of women categorized by levels of symptom bother. As expected, women with the least amount of bother reported higher scores on all satisfaction scales than those with higher bother (p < 0.0001), except on Future Fertility Concerns (p = 0.27). CONCLUSION: Our results support the reliability and validity of the ORTHO BC-SAT. It may be used in future studies to evaluate satisfaction among hormonal contraceptive users.

Adult↗
PubMed1987

Pharmacology and pharmacokinetics of estrogens.

The primary source of estrogen, ovarian 17 beta-estradiol, is normally converted to estrone and estriol, both of which are metabolized to their sulfate and glucuronide forms, as well as oxidated to nonestrogens. In postmenopausal women, the primary sources of estrogen are nonovarian, including the production of androstenedione from the adrenal cortex and its metabolism to estrone by the liver, adipose tissue, skeletal muscle, kidney, brain, and hair follicles. Estrogen circulates bound to sex hormone-binding globulin and albumin. The sulfate form may be a storage form of this hormone and is freely converted back to estrone and estriol. The glucuronide and sulfate forms have limited cell penetration; they are excreted mainly in the kidney, with little tubular reabsorption. Several theories have been advanced to explain the effects of estrogens on the basis of their receptors. A consideration of pharmacologic and pharmacokinetic characteristics reveals specific advantages and disadvantages of the preparations currently available for estrogen replacement therapy. Oral agents have the disadvantage of being subject to a considerable first-pass hepatic effect, resulting in their conversion to estriol, oxidation to nonestrogens, and conjugation to sulfate and glucuronide salts. These preparations can also be associated with poor patient compliance, as can injectable, topical, or suppository preparations. On the other hand, transdermal patches are not subject to a first-pass hepatic effect, provide relatively uniform serum levels, and may help alleviate the problem of noncompliance.

Estradiol↗
PubMed1988

A randomized comparison of nonoral estradiol delivery in postmenopausal women.

We compared the transdermal and subdermal routes of estrogen administration with respect to the constancy of estrogen delivery and metabolic effects. Twenty postmenopausal women were randomized to receive either two 25 mg estradiol pellets subdermally (n = 10) or a 0.1 mg estradiol transdermal patch twice weekly (n = 10). Blood was sampled at 0, 2, 4, 6, 8, 12, 24, and 72 hours and 1, 2, 4, 8, 12, 16, 20, and 24 weeks (fasting samples at 0, 12, and 24 weeks), and a fasting urine was obtained after diuresis at 0, 12, and 24 weeks. In a 72-hour profile, serum estradiol levels (mean +/- SE) were highest at 24 hours (179 +/- 20 pg/ml) and fell to 139 +/- 16 pg/ml at 72 hours in the pellet group. In the patch group, estradiol levels rose rapidly to 152 +/- 33 pg/ml at 4 hours, remained relatively constant over 8 hours, and fell to 46 +/- 10 pg/ml at 72 hours. At 1 week, estradiol levels in the pellet group were 113 +/- 12 pg/ml and remained relatively constant for 24 weeks. In contrast, estradiol levels in the patch group were 52 +/- 11 pg/ml at 1 week and then varied widely until 24 weeks, when the levels were 89 +/- 26 pg/ml. The mean estradiol/estrone ratio ranged between 1 and 2.5 in both groups but fluctuated widely in the patch group. Follicle-stimulating hormone was suppressed in both groups; however, the decrement in the pellet group was greater (p less than 0.002). There was a significant increase in high-density lipoprotein cholesterol and a decrease in total cholesterol/high-density lipoprotein cholesterol at 12 weeks with the pellet but only at 24 weeks with the patch. The urinary calcium/creatinine ratio was reduced more consistently with the pellet than with the patch. Hot flushes were eliminated in all subjects.

Administration, Cutaneous↗
PubMed1995

Estrogen augments serotonergic activity in postmenopausal women.

To investigate the influence of estrogen replacement on serotonergic activity in postmenopausal women, the serotonin agonist meta-chlorophenylpiperazine (m-CPP) (0.5 mg/kg) was given orally to 18 normal postmenopausal women, 11 of whom were also tested following 30 days' treatment with estrogen transdermal patches (estraderm 0.1 mg). Fifteen normal, healthy women of reproductive status served as a control group. Cortisol and prolactin responses to m-CPP were measured. Without estrogen, the prolactin and cortisol responses of postmenopausal women to m-CPP were blunted compared to those of reproductive women. Estrogen replacement increased the hormonal responses. It is suggested that decreased serotonergic activity in postmenopausal women might contribute to their vulnerability to affective disorders. Estrogen replacement therapy might decrease this vulnerability and might add to the efficacy of serotonergic antidepressants when warranted.

Administration, Cutaneous↗