ExcelMale
Menu
Home
What's new
Latest activity
Forums
New posts
Search forums
What's new
New posts
Latest activity
Videos
Lab Tests
Doctor Finder
Buy Books
About Us
Men’s Health Coaching
Log in
Register
What's new
Search
Search
Search titles only
By:
New posts
Search forums
Menu
Log in
Register
Navigation
Install the app
Install
More options
Contact us
Close Menu
Forums
Testosterone Replacement, Low T, HCG, & Beyond
Testosterone Side Effect Management
Tamoxifen (Nolvadex) Nipple Cream for Gynecomastia Now Available at Empower Pharmacy
JavaScript is disabled. For a better experience, please enable JavaScript in your browser before proceeding.
You are using an out of date browser. It may not display this or other websites correctly.
You should upgrade or use an
alternative browser
.
Reply to thread
Message
<blockquote data-quote="Sides" data-source="post: 153008" data-attributes="member: 31749"><p>As the article mentioned above states, transdermal tamoxifen cream applied locally to the breast shouldn't work, as tamoxifen is a pro-drug and it's beneficial effects depend on conversion in the liver into it's active metabolites like 4-OHT. However, if someone were to make a transdermal cream containing 4-OHT, that has been shown to work locally on the breast while avoiding the systemic effects of tamoxifen. I wish someone had a transdermal 4-OHT cream available.</p><p></p><p>"Tamoxifen is a pro-drug, requiring conversion by the phase I drug metabolizing cytochrome P450 enzymes, predominantly CYP2D6 but also CYP3A4/5 among others, to its major anti-estrogenic metabolites [<a href="https://www.ncbi.nlm.nih.gov/pmc/articles/PMC4053098/#B52" target="_blank">52</a>]. Toxicity can result from systemic administration, due to the activity of tamoxifen in non-breast tissues.</p><p>Transdermal delivery has long been recognized as an effective alternative to conventional systemic therapy, including oral administration. When delivered transdermally, a drug is characterized by distinct pharmacokinetics, with longer retention in the local tissue. However, due to the effectiveness of the barrier function of the stratum corneum, only a relatively small number of lipophilic drugs with low molecular weights (< 500 Da) have been successfully formulated for these purposes. </p><p>Since tamoxifen is a pro-drug requiring hepatic activation, the transdermal approach may not be suitable <em>per se</em>. A more reasonable approach is to utilize its more active metabolites. Mauvais-Jarvis and colleagues [<a href="https://www.ncbi.nlm.nih.gov/pmc/articles/PMC4053098/#B58" target="_blank">58</a>] determined that the tamoxifen metabolite 4-OHT, like progesterone, could be concentrated directly in the breast tissue.</p><p>Following transdermal application of 4-OHT in the studies conducted so far, very low plasma concentrations of the drug have been observed. These low plasma levels in the setting of a topical approach that bypasses first-pass metabolism in the liver suggest that there should be a reduction in systemic toxicity [<a href="https://www.ncbi.nlm.nih.gov/pmc/articles/PMC4053098/#B58" target="_blank">58</a>,<a href="https://www.ncbi.nlm.nih.gov/pmc/articles/PMC4053098/#B59" target="_blank">59</a>,<a href="https://www.ncbi.nlm.nih.gov/pmc/articles/PMC4053098/#B65" target="_blank">65</a>,<a href="https://www.ncbi.nlm.nih.gov/pmc/articles/PMC4053098/#B78" target="_blank">78</a>,<a href="https://www.ncbi.nlm.nih.gov/pmc/articles/PMC4053098/#B79" target="_blank">79</a>]."</p><p></p><p><a href="https://www.ncbi.nlm.nih.gov/pmc/articles/PMC4053098/#!po=0.500000" target="_blank">Oral low dose and topical tamoxifen for breast cancer prevention: modern approaches for an old drug</a></p></blockquote><p></p>
[QUOTE="Sides, post: 153008, member: 31749"] As the article mentioned above states, transdermal tamoxifen cream applied locally to the breast shouldn't work, as tamoxifen is a pro-drug and it's beneficial effects depend on conversion in the liver into it's active metabolites like 4-OHT. However, if someone were to make a transdermal cream containing 4-OHT, that has been shown to work locally on the breast while avoiding the systemic effects of tamoxifen. I wish someone had a transdermal 4-OHT cream available. "Tamoxifen is a pro-drug, requiring conversion by the phase I drug metabolizing cytochrome P450 enzymes, predominantly CYP2D6 but also CYP3A4/5 among others, to its major anti-estrogenic metabolites [[URL='https://www.ncbi.nlm.nih.gov/pmc/articles/PMC4053098/#B52']52[/URL]]. Toxicity can result from systemic administration, due to the activity of tamoxifen in non-breast tissues. Transdermal delivery has long been recognized as an effective alternative to conventional systemic therapy, including oral administration. When delivered transdermally, a drug is characterized by distinct pharmacokinetics, with longer retention in the local tissue. However, due to the effectiveness of the barrier function of the stratum corneum, only a relatively small number of lipophilic drugs with low molecular weights (< 500 Da) have been successfully formulated for these purposes. Since tamoxifen is a pro-drug requiring hepatic activation, the transdermal approach may not be suitable [I]per se[/I]. A more reasonable approach is to utilize its more active metabolites. Mauvais-Jarvis and colleagues [[URL='https://www.ncbi.nlm.nih.gov/pmc/articles/PMC4053098/#B58']58[/URL]] determined that the tamoxifen metabolite 4-OHT, like progesterone, could be concentrated directly in the breast tissue. Following transdermal application of 4-OHT in the studies conducted so far, very low plasma concentrations of the drug have been observed. These low plasma levels in the setting of a topical approach that bypasses first-pass metabolism in the liver suggest that there should be a reduction in systemic toxicity [[URL='https://www.ncbi.nlm.nih.gov/pmc/articles/PMC4053098/#B58']58[/URL],[URL='https://www.ncbi.nlm.nih.gov/pmc/articles/PMC4053098/#B59']59[/URL],[URL='https://www.ncbi.nlm.nih.gov/pmc/articles/PMC4053098/#B65']65[/URL],[URL='https://www.ncbi.nlm.nih.gov/pmc/articles/PMC4053098/#B78']78[/URL],[URL='https://www.ncbi.nlm.nih.gov/pmc/articles/PMC4053098/#B79']79[/URL]]." [URL="https://www.ncbi.nlm.nih.gov/pmc/articles/PMC4053098/#!po=0.500000"]Oral low dose and topical tamoxifen for breast cancer prevention: modern approaches for an old drug[/URL] [/QUOTE]
Insert quotes…
Verification
Post reply
Share this page
Facebook
Twitter
Reddit
Pinterest
Tumblr
WhatsApp
Email
Share
Link
Sponsors
Forums
Testosterone Replacement, Low T, HCG, & Beyond
Testosterone Side Effect Management
Tamoxifen (Nolvadex) Nipple Cream for Gynecomastia Now Available at Empower Pharmacy
This site uses cookies to help personalise content, tailor your experience and to keep you logged in if you register.
By continuing to use this site, you are consenting to our use of cookies.
Accept
Learn more…
Top