scholarly journals Achieving Physiologic 17-ẞ-Estradiol Levels in Transgender Females on Estradiol Transdermal Patches and Optimal Dosing

2021 ◽  
Vol 5 (Supplement_1) ◽  
pp. A787-A788
Author(s):  
Alexa Trovato ◽  
Matthew C Leinung ◽  
Jalaja Joseph ◽  
Son Nguyen

Abstract Purpose: Gender dysphoria is defined as a significant incongruence between an individual’s experienced gender and the gender assigned at birth, leading to persistent distress. Hormone therapy and gender affirmation surgery improve gender dysphoria by mitigating or completely removing undesirable primary/secondary sexual characteristics which would better align with one’s physical and psychological features. Maintaining cross-sex hormone levels in the physiologic range for the preferred gender is the basis of transgender hormonal therapy. For trans females (MTF), estradiol is most commonly administered orally, and studies have shown this route is often successful in achieving therapeutic hormone levels. However, there is wide individual variability in the dose response to oral estradiol, and approximately 25% of patients will not reach therapeutic goal on maximum oral estradiol. Furthermore, high dose oral estrogen has been associated with increased thrombotic risk, especially in older individuals. The efficacy or optimal dose of adding or switching to the transdermal route is not known. We investigated the efficacy of estradiol transdermal patches and the optimal dose to reach therapeutic goal. Methods: A chart review was conducted of all MTF patients who were treated with estradiol transdermal patches in our transgender clinic from 2006 through 2020. We looked at the success of achieving physiologic serum 17-β-estradiol levels (with and without antiandrogens spironolactone and finasteride) on various doses of estradiol transdermal patches. Target serum level for estradiol >100 pg/mL is recommended (but may be lower in certain clinical circumstances). Results: 371 MTF patients were identified, 41 received an estradiol transdermal patch. Of these 41 patients, 16 of them were placed on a transdermal patch due to failure to achieve target 17-β-estradiol levels on maximal oral therapy. We found that 9 of these 16 patients achieved goal estrogen levels, as well as one patient very near goal. Of the 7 who did not reach goal, only 2 were on patch doses >60 mcg/day. The majority who reached goal serum estradiol levels were taking a dose of 100 mcg/daily. When considering all MTF patients on the highest dose (100 mcg) of transdermal estrogen, 11 of 18 attained goal level, as well as one just under goal. Of the 41 MTF patients taking a transdermal patch, only 6 of them had serum estrogen levels lowered from being at goal on oral therapy. Thirteen patients had their estrogen levels improve to reach goal when placed on patch (4 as add-on therapy). Conclusions: Our study supports the findings that using an estradiol transdermal patch can help MTF patients achieve goal 17-β-estradiol levels. This delivery method can be useful for patients unable to reach goal on oral agents and for patients at higher thrombotic risk. The highest dose patch available is often needed to achieve therapeutic goal.

2021 ◽  
Vol 21 (1) ◽  
Author(s):  
Rong Lei ◽  
Yan Sun ◽  
Jiawen Liao ◽  
Yuan Yuan ◽  
Linlin Sun ◽  
...  

Abstract Background There are only a few studies on sex hormones in females of different ages suffering from depression, and their conclusions are not uniform until now. This study aimed to investigate the correlation between the severity of depression in females and factors such as sex hormones and differences in sex hormone levels in females of different ages, exploring variations after treatment. Methods A total of 169 females with depression were selected and divided into the first-episode (91 cases) and recurrent (78 cases) groups. Then, on the basis of their age, the first-episode patients were divided into the young (48 cases, age < 45 years), perimenopausal (20 cases, 45–55 years), and elderly groups (23 cases, age > 55 years); the patients with recurrent depression were classified into the young (37 cases, age < 45 years), perimenopausal (19 cases, 45–55 years), and elderly groups (22 cases, age > 55 years). The patients were assessed in accordance with the International Classification of Diseases of mental and behavioral disorders. The serum progesterone, prolactin, estradiol, and testosterone levels in the patients were measured, and differences in sex hormone levels of the groups were analyzed. Results The estradiol level was negatively correlated with age and the prolactin level was positively correlated with occupation. The severity of depression in females was found to be negatively correlated with age. The serum progesterone and estradiol levels in the young group were significantly higher than those in the elderly group, regardless of the first episode or recurrence. Estradiol levels in the perimenopausal and elderly groups with first-episode depression were significantly higher than those in the same group with recurrent depression. However, there was no significant difference in the serum progesterone, prolactin, estradiol, and testosterone levels in the recurrent group before and after treatment. Conclusions Sex hormone levels, especially estradiol, varied among females of different ages suffering from depression. Recurrent depression also has a certain effect on sex hormone levels in females. Not only should the age and relapse be considered when studying the sex hormone levels of females with depression, but also attention should be paid to whether the patients have used antidepressants before their sexual hormonal testing.


2021 ◽  
pp. 001857872098713
Author(s):  
Janna Afanasjeva ◽  
Michael Gabay ◽  
Thomas Poznanski ◽  
Stefanie Kerns

This is an update to the 2010 article published in Hospital Pharmacy on safety concerns involving transdermal patches and magnetic resonance imaging (MRI). Since publication of the original article, new brand and generic transdermal medications have become available and notable changes regarding the presence or absence of metallic content among existing transdermal formulations occurred. To update the tables within the article, Food and Drug Administration (FDA)-approved transdermal medications through October 2020 were researched in order to determine metallic content and procedures for reapplication after MRI, if applicable. Readers should consult the prescribing information or manufacturer for the most current information on use of transdermal medications in the MRI setting. Of note, manufacturers have not evaluated the use of transdermal products while patients undergo a MRI scan.


2020 ◽  
Author(s):  
Wen Wang ◽  
Lotte van Dammen ◽  
Shannin N. Moody ◽  
Jeff Kiesner ◽  
Jenae M. Neiderhiser ◽  
...  

Background. Saliva is a popular biospecimen for the measurement of hormones, yet fluctuations in hormone levels limit the extent to which saliva can address focusing on basal or long-term levels. Hair steroid assays return basal hormonal levels by collapsing across short-term hormonal variability, including menstrual cyclicity. Here we sought to validate a hair bioassay methodology that can capture stable estradiol levels from both human and monkey hair samples. Methods. Three projects were involved to examine hair-saliva correspondence and estradiol stability in hair. Project 1. Saliva samples were collected once per week for two cycles in 11 emerging adult women. Hair samples were collected at the end of each menstrual cycle and were segmented by 1 cm for the first 4 cm to reflect the past four serial months’ hormone levels. Project 2. Hair samples collected from 23 adolescent participants (Mage = 14.1, 56.5% female) were cut to three 1.5 cm segments from the scalp end. Project 3. Two hair samples were collected from two adjacent skin areas on each monkey (N = 8, 75% males). Whole hair samples were sheared and used for assay without segmentation. Hair biospecimens were processed using a double-extraction protocol validated in this study, then assayed using commercially-available enzyme-immuno-assays for estradiol. Results. Project 1. Hair estradiol concentrations were significantly associated with averaged saliva estradiol levels (r = 0.77, p&lt; .05). Estradiol levels in two consecutive segments were significantly associated (1st vs. 2nd: r = .63, p &lt; .01; 2nd vs. 3rd: r = .49, p &lt; .05; 3rd vs. 4th: r = .53, p &lt; .05). Project 2. Estradiol concentrations were significantly correlated between the first two successive hair segments from the scalp end (r = .69, p &lt; .01). Project 3. Estradiol levels in the two hair samples from each monkey were significantly correlated (r = .66, p &lt; .05).Discussion. Results suggest hair captures valid and reliable average estradiol concentrations using a double-extraction protocol that is applicable for both human and monkey hair. The measurement of hair provides valuable information on individual differences in average estradiol levels across months. Results also indicate that it is feasible and reliable to collect the first 2-3 centimeters of studies in which basal estradiol levels in the past 2 to 3 months are of interest as a stable hormonal index for different species.


2021 ◽  
Author(s):  
Maria Schroeder ◽  
Berfin Schaumburg ◽  
Zacharias Mueller ◽  
Ann Parplys ◽  
Dominik Jarczak ◽  
...  

Abstract BACKGROUNDMale sex was repeatedly identified as a risk factor for death and intensive care admission. However, it is yet unclear whether sex hormones are associated with disease severity in COVID-19 patients. We sought to characterize sex differences in hormone levels and cytokine responses in critically ill COVID-19 patients.METHODSWe performed a retrospective cohort study of critically ill COVID-19 patients. Males and females were compared. Multivariate regression was performed to assess the association between sex hormones, cytokine responses and the requirement for extracorporeal membrane oxygenation (ECMO) treatment.RESULTSWe analyzed sex hormone levels (estradiol and testosterone) of n=181 male and female individuals. These consisted of n=50 critically ill COVID-19 patients (n=39 males, n=11 females), n=42 critically ill non-COVID-19 patients (n=27 males, n=15 females), n=39 non-COVID-19 patients with coronary heart diseases (CHD) (n=25 males, n=14 females) and n=50 healthy individuals (n=30 males, n=20 females). We detected highest estradiol levels in critically ill male COVID-19 patients compared to non-COVID-19 patients (p=0.0123), patients with CHD (p=0.0002) or healthy individuals (p=0.0007). Lowest testosterone levels were detected in critically ill male COVID-19 patients compared to non-COVID-19 patients (p=0.0094), patients with CHD (p=0.0068) or healthy individuals (p<0.0001). No statistically significant differences in sex hormone levels were detected in critically ill female COVID-19 patients, albeit similar trends in estradiol levels were observed. In critically ill male COVID-19 patients, cytokine and chemokine responses (IFN-γ, p=0.0301; IL-1RA, p=0.0160; IL-6, p=0.0145; MCP-1, p=0.0052; MIP-1α, p=0.0134) were significantly elevated in those with higher Sequential Organ Failure Assessment (SOFA) scores (8-11). Linear regression analysis revealed that herein IFN-γ levels correlate with estradiol levels in male and female COVID-19 patients (R2=0.216, =0.0009). Male COVID-19 patients with elevated estradiol levels were more likely to receive ECMO treatment in the course of their ICU stay (p=0.0009). CONCLUSIONS We identified high estradiol and low testosterone levels as a hallmark of critically ill male COVID-19 patients. Elevated estradiol levels in critically ill male COVID-19 patients were positively associated with IFN-γ levels and increased risk for ECMO requirement.


2018 ◽  
Vol 2 (1) ◽  
pp. 01-03
Author(s):  
Luke Jackson ◽  
Jonathan Noah ◽  
Miguel Seth ◽  
Collin Jared

Background: Overactive bladder is an age-related urologic disease. An oxybutynin transdermal patch is used to treat overactive bladder; however, long-term use is not advised because of potential adverse reactions at the site of application. The present study aimed to investigate the advantages of administering a combination of heparinoid cream and oxybutynin transdermal patch treatment for overactive bladder in elderly patients. Methods: Eight patients (>65 years of age) with overactive bladder were included. The heparinoid cream was applied topically for 1 week, and skin hydration and transepidermal water loss were quantified before and after application. Thereafter, patients were treated with a combination of an oxybutynin transdermal patch and a heparinoid cream for 12 weeks, and the sites of application were monitored for adverse reactions. Clinical effects of the combinatorial treatment were assessed based on the overactive bladder symptom score. Results: Application of the heparinoid cream did not decrease transepidermal water loss, but increased skin hydration and improved dryness. Oxybutynin transdermal patch therapy was not interrupted because no skin irritation was observed at the site of application for 12 weeks, and the overactive bladder symptom score decreased significantly (p<0.05). Conclusions: Combination treatment with an oxybutynin transdermal patch and a heparinoid cream improved treatment outcomes, suggesting that skin hydration with heparinoid cream is a promising treatment method to ensure appropriate use of oxybutynin transdermal patches in elderly patients with overactive bladders.


2013 ◽  
Vol 32 (4) ◽  
pp. 308-313 ◽  
Author(s):  
Subham Banerjee ◽  
Pronobesh Chattopadhyay ◽  
Animesh Ghosh ◽  
Manash Pratim Pathak ◽  
Shweta Singh ◽  
...  

The skin irritating, sensitizing, and acute dermal toxicity potential of a novel combinational prophylactic transdermal patch, mainly composed of eserine and pralidoxime chloride as active pharmaceutical ingredients, against (±) anatoxin-a poisoning were investigated in rabbits, guinea pigs, and rats in compliance with the Organisation for Economic Cooperation and Development guidelines. In primary skin irritation test, rabbits were dermally attached with the therapeutically active transdermal patch or with a placebo patch for 72 hours. The transdermal patches did not induce any adverse reactions such as erythema and edema on intact skin sites. The active patch was classified as a practically nonirritating material based on the score in the primary irritation index. In the Buehler test, guinea pigs were sensitized by the active or placebo transdermal patches attached for 24 hours. The patches did not induce any sensitization reactions in contrast to a severe sensitization reaction that occurred in the positive control. Therefore, the active patch and placebo patch were both graded as weak in sensitization score and rate. Acute dermal toxicity test in rats did not produce any overt signs of toxicity following a 14-day treatment period. Taken together, these findings suggest that the transdermal patch does not cause skin irritation, skin sensitization, or dermal toxic effects following dermal application.


2021 ◽  
Vol 7 (1) ◽  
pp. 173-184
Author(s):  
Novia Novia ◽  
Noval Noval

The transdermal patch can deliver the active substance with good bioavailability, then made formulations of such preparations from dayak onion extract, which has a compound content of flavonoids, with a combination of polymer PVP K30 and ethyl cellulose to produce transdermal patches with good physical evaluation and penetration. The research aims to carry out the effect and ideal formulation of transdermal patches of dayak onion extract with a combination of polymers PVP K30 and ethyl cellulose based on physical evaluation and penetration—manufacture of transdermal patches using the solvent evaporation method. Physical evaluation includes organoleptic testing, weight uniformity, thickness, folding resistance, and moisture testing. Then evaluate the penetration of the active substance using Franz diffusion cells. Analyze data with One Way ANOVA. The physical evaluation results of weight uniformity, patch thickness, folding resistance, and moisture test of transdermal patches on F1, F2, F3, and F4 meet the requirements. As for the results of penetration tests, F1, F2, F3, and F4 can be penetrated from 120 minutes to 180 minutes with the concentration of active substances that are linearly penetrated. The combination of polymers PVP K30 and ethylcellulose has affected the physical evaluation of transdermal patches of dayak onion extract. Based on the physical evaluation and penetration test in vitro obtained, the most optimal formula results are F3 with comparison PVP K30 and ethyl cellulose (100:300).


2006 ◽  
Vol 24 (18_suppl) ◽  
pp. 8621-8621 ◽  
Author(s):  
M. Kirk ◽  
C. Hudis

8621 Background: Several studies have demonstrated suboptimal adherence to oral anticancer agents. Understanding barriers to treatment adherence is increasingly important with the growing number of oral agents available to treat BC. Gaining insights into the attitudes and behaviors of patients (pts) with BC regarding their prescribed treatment is necessary to identify and address factors responsible for poor adherence with oral medications. Methods: To identify barriers to adherence with oral hormonal medications, a self-reported, 30-question internet survey was posted on www.y-me.org from June 30 through October 31, 2005. Results: Of the 328 survey respondents, 65.9% were diagnosed with early BC and 53.3% were postmenopausal. Of the 60% of pts with BC who had been prescribed an oral therapy, 44.6% were prescribed tamoxifen, 31.8% anastrozole, and 7.9% letrozole. 88.6% of patients indicated that their healthcare provider discussed the importance of taking oral medications as directed. Only 44.2% reported receiving instruction on the importance of taking oral medications as directed at every office visit. For 33.3%, this topic was reportedly discussed only once, prior to treatment. 83.6% of patients indicated they were taking their oral therapy as directed, but only 57.4% rated their ability to adhere to therapy (not missing a single dose) as excellent. For 35.5%, knowing that adherence may improve clinical outcome would help them take their oral medication as directed. For 24.1%, better management of treatment-related side effects would improve their adherence to therapy. Conclusions: To improve adherence, the results of this survey suggest that healthcare professionals should discuss and emphasize 1) the importance of taking oral medications as directed and 2) the impact of adherence on clinical outcomes. Greater attention to managing treatment-related side effects may further enhance adherence to therapy. [Table: see text]


Pharmaceutics ◽  
2019 ◽  
Vol 11 (7) ◽  
pp. 359 ◽  
Author(s):  
Nair ◽  
Gupta ◽  
Al-Dhubiab ◽  
Jacob ◽  
Shinu ◽  
...  

The administration of pioglitazone as an oral therapy is restricted due to various challenges. The aim of the current investigation was to evaluate the suitability of pioglitazone in adhesive transdermal patch as an alternative delivery system, in order to improve therapeutic delivery. Drug in adhesive pioglitazone (2% w/w) transdermal patch were optimized for drug release, suitable adhesive, and skin permeation enhancer. The selected patch was examined for drug-loading capacity and the patch with greater pioglitazone (6% w/w) was evaluated in rat models. The release of pioglitazone was influenced by the tested adhesive and was shown to be significantly higher (p < 0.001) with patch, prepared using Duro-Tak 87-2516. The ex vivo permeation results substantiate the release data as a greater transdermal flux (15.67 ± 2.35 µg/cm2/h) was demonstrated in patch fabricated with Duro-Tak 87-2516. Skin penetration enhancers promoted the ex vivo transdermal delivery of pioglitazone, and was ~2 folds (p < 0.0001) higher with propylene glycol, as compared to patch without enhancer. The maximum solubility of pioglitazone in Duro-Tak 87-2516 was found to be 6% w/w. Increasing the drug content in patch enhanced the transdermal flux and was highest when the pioglitazone level was 6% w/w (72.68 ± 5.76 µg/cm2/h). In vivo pharmacokinetic data demonstrate that the AUC0-α in transdermal application (13,506.51 ± 1649.92 ng·h/mL) was ~2 times higher (p < 0.0001) as compared to oral dosage form. In conclusion, the promising results observed here signifies that developed patch could be a viable alternative for oral therapy of pioglitazone.


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