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
MPB and Finasteride (side effects/dosing theory)
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="madman" data-source="post: 215046" data-attributes="member: 13851"><p>I know you have been struggling on trt especially when it comes to mood/overall well-being.</p><p></p><p>I would think twice before jumping on the oral route.</p><p></p><p>Seems more sensible to give the topical a go first!</p><p></p><p></p><p><strong><em>*Considerable evidence exists in the contemporary literature regarding the <u>physiological role of 5a-reductases in the peripheral tissues and CNS</u> and the pathophysiological implication of inhibiting this family of enzymes and blunting biosynthesis of <u>neurosteroids, which are critical biological mediators in the CNS, and contribute to altered mood, cognition, and libido </u>(23–50). <u>Also, significant pre-clinical evidence exists demonstrating that inhibition of 5a-RIs contributes to erectile dysfunction</u> (16–22) <u>and may also contribute to neurological symptoms</u> (Fig. 4 (36).</em></strong></p><p></p><p></p><p></p><p></p><p></p><p>[URL unfurl="true"]https://www.excelmale.com/forum/threads/topical-finasteride-for-male-androgenetic-alopecia.24239/[/URL]</p><p></p><p><em><strong>Although oral finasteride is generally well tolerated, 5 in some patients 5α -reductase inhibition is associated with sexual adverse effects (erectile dysfunction, ejaculation problems, decreased libido),11 and increased risk of depression,12 prompting health authorities in some countries to include warnings in the product labeling. 13.</strong> <strong><u>Topical administration of finasteride offers the potential to reduce systemic effects related to its mechanism of action by preferentially inhibiting 5 -α reductase in the scalp, as has been suggested in recent years</u>. 14</strong></em></p><p></p><p></p><p><strong>PK and PD analyses Mean</strong></p><p><strong></strong></p><p><strong><em>Mean ± SD maximum plasma finasteride concentrations were 36.5 ± 45.9 pg/mL with topical finasteride</em> </strong><em>and 7166 ± 12,744 pg/mL with oral finasteride at Week<strong> 12</strong>; and were </em><strong><em>48.0 ± 87.2 pg/mL</em></strong><em> and 5029 ± 4182 pg/mL, respectively, at Week <strong>24</strong>.</em></p><p><em></em></p><p><em>Mean serum DHT concentrations in the placebo group remained unaffected during the study (range: 38.5 to 39.8 ng/dL).<strong> <u>Mean serum DHT concentrations at Week 24 were 34.6% lower than at baseline in the topical finasteride group (25.75 vs. 39.32 ng/dL, respectively), and were 55.6% lower than at baseline in the oral finasteride group (15.75 vs. 35.50 ng/d L, respectively)</u>. The adjusted mean difference in the change from baseline in serum DHT concentrations was statistically significant between topical finasteride and placebo (p < 0.05), and between topical finasteride and oral finasteride (p < 0.05), at each of Weeks 4, 8, 12, and 24 (Figure 5 ).</strong></em></p><p><em></em></p><p><strong><em>The <u>lower impact of topical finasteride on DHT levels</u> was not accompanied by any shift from normal to high plasma testosterone concentrations for patients in this group;</em></strong><em> this was also the case for the placebo group. In the oral finasteride group, this shift occurred in four (6.7%) patients</em></p><p><em></em></p><p><em></em></p><p><em></em></p><p><em></em></p><p><strong><em>*Some patients treated with oral finasteride may experience adverse effects potentially related to the <u>circulating plasma concentration of drug required to achieve effective concentrations at the scalp</u>.</em></strong><em> There is an ongoing debate whether, in some cases, the use of oral finasteride 1 mg/day to treat male pattern hair loss may be associated with irreversible sexual dysfunction and severe depression. 26-29 <strong><u>As demonstrated in the current study, maximum mean plasma finasteride concentrations were more than 100 -fold lower with the topical versus oral formulation, and the impact on serum DHT concentrations after 24 weeks’ treatment was statistically significantly lower with topical versus oral finasteride (reductions of 34.6% and 55.6%, respectively)</u>. <u>While this does not exclude the possibility of systemic adverse events related to decreased DHT in both groups, the probability is lower with topical than oral finasteride</u>. A trend was evident for fewer treatment-related sexual adverse events, and associated treatment discontinuations, in the topical versus oral finasteride group</strong></em></p><p><em><strong></strong></em></p><p><em><strong></strong></em></p><p><em><strong>*While this does not exclude the possibility of systemic adverse events related to decreased DHT in both groups, the probability is <u>lower with topical than oral finasteride</u></strong></em><strong><em>.</em></strong></p><p></p><p></p><p></p><p></p><p><em><strong><u>The main finding of the study was that the change from baseline in hair count was significantly greater with topical finasteride than placebo and similar to that observed with oral finasteride</u>. <u>This result was achieved with markedly lower systemic exposure to finasteride and less impact on serum DHT concentrations compared with oral finasteride</u>. Topical finasteride was well tolerated and had a safety profile not meaningfully different from that of placebo. As such, topical finasteride appears to be a useful option for the treatment of AGA in men.</strong> Further studies would be useful to demonstrate the long-term efficacy of topical finasteride. Understanding the reasons for the relatively high number of treatment discontinuations and negligible changes from baseline to end of treatment in certain subjective measures such as patient-assessed MHGQ score for ‘overall assessment’ and blinded -assessor evaluation of patient hair growth/loss may assist in designing future studies.</em></p><p></p><p></p><p></p><p></p><p>[URL unfurl="true"]https://www.excelmale.com/forum/threads/finasteride-for-hair-loss.23828/[/URL]</p><p></p><p><strong>4. Mechanism of action</strong></p><p></p><p><em><strong>Finasteride inhibits type II 5AR isoenzyme 100-fold more selectively over type I isoenzyme (7). <u>The NAPDH-mediated irreversible inhibition leads to finasteride being reduced to dihydrofinasteride, thereby blocking the peripheral conversion of testosterone to DHT at the dermal papillae level </u>(7,23) (Figure 2). <u>Therefore, this leads to a significant reduction in scalp and serum DHT levels</u> (7).</strong></em></p><p><em><strong></strong></em></p><p><em><strong>Finasteride reduces serum DHT levels by about 70% after administration of a single oral dose (24). Preliminary studies showed that finasteride 5 mg/day suppressed scalp DHT concentrations significantly compared to placebo (25). <u>Thereafter, in a scalp DHT dose-ranging study (5, 1, 0.2 mg/day finasteride) demonstrated a reduction in scalp DHT levels by about 65% at doses ≥ 0.5 mg/day after 6 weeks of treatment (25,26)</u>. DHT levels are not reduced completely due to the residual conversion of testosterone through type I 5AR (4,7). DHT levels are shown to return to normal within 2 weeks of treatment discontinuation (27).</strong></em></p><p></p><p></p><p><strong>6. Bioavailability</strong></p><p></p><p><em>Propecia may be orally administered with or without meals as the bioavailability is not affected by food (7). <strong>The mean bioavailability of finasteride 1mg tablets is 65% (range: 26-170%) in a study conducted in 15 healthy young male volunteers (7). Multiple studies have calculated the percentage bioavailability of finasteride between 63% to 80% (29,31). <u>Finasteride reaches a steady state in plasma within 2 hours of administration, with a peak concentration of 9.2 ng/mL (range: 4.9-13.7 ng/mL) (7)</u>. <u>Finasteride is absorbed completely in 6-8 hours post-administration (32)</u>. <u>The circulating finasteride is bound to the plasma proteins (89.8-91.3%) and slowly accumulates after multiple doses (7,33)</u>.</strong></em></p><p><em><strong></strong></em></p><p><em><strong>The mean terminal half-life of finasteride is 5-6 hours in men 18-60 years age and approximately 8 hours in mean aged 70 years and above (7)</strong>. Following oral administration of finasteride, it was reported that approximately 39% of the metabolites were excreted through urine and 57% excreted through feces (7).</em></p></blockquote><p></p>
[QUOTE="madman, post: 215046, member: 13851"] I know you have been struggling on trt especially when it comes to mood/overall well-being. I would think twice before jumping on the oral route. Seems more sensible to give the topical a go first! [B][I]*Considerable evidence exists in the contemporary literature regarding the [U]physiological role of 5a-reductases in the peripheral tissues and CNS[/U] and the pathophysiological implication of inhibiting this family of enzymes and blunting biosynthesis of [U]neurosteroids, which are critical biological mediators in the CNS, and contribute to altered mood, cognition, and libido [/U](23–50). [U]Also, significant pre-clinical evidence exists demonstrating that inhibition of 5a-RIs contributes to erectile dysfunction[/U] (16–22) [U]and may also contribute to neurological symptoms[/U] (Fig. 4 (36).[/I][/B] [URL unfurl="true"]https://www.excelmale.com/forum/threads/topical-finasteride-for-male-androgenetic-alopecia.24239/[/URL] [I][B]Although oral finasteride is generally well tolerated, 5 in some patients 5α -reductase inhibition is associated with sexual adverse effects (erectile dysfunction, ejaculation problems, decreased libido),11 and increased risk of depression,12 prompting health authorities in some countries to include warnings in the product labeling. 13.[/B] [B][U]Topical administration of finasteride offers the potential to reduce systemic effects related to its mechanism of action by preferentially inhibiting 5 -α reductase in the scalp, as has been suggested in recent years[/U]. 14[/B][/I] [B]PK and PD analyses Mean [I]Mean ± SD maximum plasma finasteride concentrations were 36.5 ± 45.9 pg/mL with topical finasteride[/I] [/B][I]and 7166 ± 12,744 pg/mL with oral finasteride at Week[B] 12[/B]; and were [/I][B][I]48.0 ± 87.2 pg/mL[/I][/B][I] and 5029 ± 4182 pg/mL, respectively, at Week [B]24[/B]. Mean serum DHT concentrations in the placebo group remained unaffected during the study (range: 38.5 to 39.8 ng/dL).[B] [U]Mean serum DHT concentrations at Week 24 were 34.6% lower than at baseline in the topical finasteride group (25.75 vs. 39.32 ng/dL, respectively), and were 55.6% lower than at baseline in the oral finasteride group (15.75 vs. 35.50 ng/d L, respectively)[/U]. The adjusted mean difference in the change from baseline in serum DHT concentrations was statistically significant between topical finasteride and placebo (p < 0.05), and between topical finasteride and oral finasteride (p < 0.05), at each of Weeks 4, 8, 12, and 24 (Figure 5 ).[/B] [/I] [B][I]The [U]lower impact of topical finasteride on DHT levels[/U] was not accompanied by any shift from normal to high plasma testosterone concentrations for patients in this group;[/I][/B][I] this was also the case for the placebo group. In the oral finasteride group, this shift occurred in four (6.7%) patients [/I] [B][I]*Some patients treated with oral finasteride may experience adverse effects potentially related to the [U]circulating plasma concentration of drug required to achieve effective concentrations at the scalp[/U].[/I][/B][I] There is an ongoing debate whether, in some cases, the use of oral finasteride 1 mg/day to treat male pattern hair loss may be associated with irreversible sexual dysfunction and severe depression. 26-29 [B][U]As demonstrated in the current study, maximum mean plasma finasteride concentrations were more than 100 -fold lower with the topical versus oral formulation, and the impact on serum DHT concentrations after 24 weeks’ treatment was statistically significantly lower with topical versus oral finasteride (reductions of 34.6% and 55.6%, respectively)[/U]. [U]While this does not exclude the possibility of systemic adverse events related to decreased DHT in both groups, the probability is lower with topical than oral finasteride[/U]. A trend was evident for fewer treatment-related sexual adverse events, and associated treatment discontinuations, in the topical versus oral finasteride group *While this does not exclude the possibility of systemic adverse events related to decreased DHT in both groups, the probability is [U]lower with topical than oral finasteride[/U][/B][/I][B][I].[/I][/B] [I][B][U]The main finding of the study was that the change from baseline in hair count was significantly greater with topical finasteride than placebo and similar to that observed with oral finasteride[/U]. [U]This result was achieved with markedly lower systemic exposure to finasteride and less impact on serum DHT concentrations compared with oral finasteride[/U]. Topical finasteride was well tolerated and had a safety profile not meaningfully different from that of placebo. As such, topical finasteride appears to be a useful option for the treatment of AGA in men.[/B] Further studies would be useful to demonstrate the long-term efficacy of topical finasteride. Understanding the reasons for the relatively high number of treatment discontinuations and negligible changes from baseline to end of treatment in certain subjective measures such as patient-assessed MHGQ score for ‘overall assessment’ and blinded -assessor evaluation of patient hair growth/loss may assist in designing future studies.[/I] [URL unfurl="true"]https://www.excelmale.com/forum/threads/finasteride-for-hair-loss.23828/[/URL] [B]4. Mechanism of action[/B] [I][B]Finasteride inhibits type II 5AR isoenzyme 100-fold more selectively over type I isoenzyme (7). [U]The NAPDH-mediated irreversible inhibition leads to finasteride being reduced to dihydrofinasteride, thereby blocking the peripheral conversion of testosterone to DHT at the dermal papillae level [/U](7,23) (Figure 2). [U]Therefore, this leads to a significant reduction in scalp and serum DHT levels[/U] (7). Finasteride reduces serum DHT levels by about 70% after administration of a single oral dose (24). Preliminary studies showed that finasteride 5 mg/day suppressed scalp DHT concentrations significantly compared to placebo (25). [U]Thereafter, in a scalp DHT dose-ranging study (5, 1, 0.2 mg/day finasteride) demonstrated a reduction in scalp DHT levels by about 65% at doses ≥ 0.5 mg/day after 6 weeks of treatment (25,26)[/U]. DHT levels are not reduced completely due to the residual conversion of testosterone through type I 5AR (4,7). DHT levels are shown to return to normal within 2 weeks of treatment discontinuation (27).[/B][/I] [B]6. Bioavailability[/B] [I]Propecia may be orally administered with or without meals as the bioavailability is not affected by food (7). [B]The mean bioavailability of finasteride 1mg tablets is 65% (range: 26-170%) in a study conducted in 15 healthy young male volunteers (7). Multiple studies have calculated the percentage bioavailability of finasteride between 63% to 80% (29,31). [U]Finasteride reaches a steady state in plasma within 2 hours of administration, with a peak concentration of 9.2 ng/mL (range: 4.9-13.7 ng/mL) (7)[/U]. [U]Finasteride is absorbed completely in 6-8 hours post-administration (32)[/U]. [U]The circulating finasteride is bound to the plasma proteins (89.8-91.3%) and slowly accumulates after multiple doses (7,33)[/U]. The mean terminal half-life of finasteride is 5-6 hours in men 18-60 years age and approximately 8 hours in mean aged 70 years and above (7)[/B]. Following oral administration of finasteride, it was reported that approximately 39% of the metabolites were excreted through urine and 57% excreted through feces (7).[/I] [/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
MPB and Finasteride (side effects/dosing theory)
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