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Testosterone Replacement, Low T, HCG, & Beyond
Testosterone Side Effect Management
Finasteride (Propecia) Hair Lotion or Foam to Treat Hair Loss in Men and Women
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<blockquote data-quote="madman" data-source="post: 181104" data-attributes="member: 13851"><p>Regardless of the duration, the dose used would be key to minimizing any impact on serum DHT levels.</p><p></p><p></p><p></p><p></p><p><strong>Pharmacology of topical finasteride </strong></p><p></p><p><span style="color: rgb(184, 49, 47)"><strong><em>The topical finasteride formulation aims to locally inhibit the 5α-reductase enzyme and decrease the production of DHT at the level of the hair follicle <u>with minimal disturbance of the serum DHT concentration</u>.</em></strong></span><em> <span style="color: rgb(44, 130, 201)"><strong>The finasteride plasma concentration in blood and the extent of absorption with the topical application are lower than that observed with oral administration.</strong></span> A preliminary clinical trial reported that serum finasteride concentrations after topical application of a combined 5% minoxidil and 0.1% finasteride lipid solution twice daily for 14 days were 10-fold lower than oral finasteride at a similar dosage (12). Another exploratory study reported very low concentrations of finasteride detected in 5 of 11 subjects after a single application of 0.25% topical finasteride; however, multiple applications of topical solution (twice daily for 7 days) resulted in small detectable finasteride plasma concentration in most subjects. Compared to oral tablets (1 mg twice daily for 7 days), the mean maximum finasteride concentration (Cmax) and area under the curve (AUC) of the topical formulation were 15 and 9 times lower, respectively; these were significantly different (13). The reduction in the scalp DHT levels from baseline was similar for 0.25% topical solution twice daily (47%) and oral finasteride 1 mg daily (51%), and significantly lower for daily application once (71%) (14).<span style="color: rgb(184, 49, 47)"> <strong>The suppression of serum DHT level was noted for both oral and topical administrations after 1-week of treatment. Although these confirm the similar inhibitory effects with multiple-dose treatment, </strong></span><span style="color: rgb(44, 130, 201)"><strong><u>the decline in DHT levels seems to be less pronounced with the use of lower-concentration topical formulations</u>.</strong></span> <strong><span style="color: rgb(184, 49, 47)">A study with an application of 0.005% topical solution<u> for 16 months did not observe any change in the serum DHT level </u>(15), while in another study, <u>applying 0.1% topical solution for 24 weeks resulted in no detection of finasteride in half of the blood samples </u>(16). Notably, all studies did not observe any significant difference in serum testosterone levels with topical application (13). </span></strong></em></p><p><em></em></p><p><em><span style="color: rgb(184, 49, 47)"><strong>A topical formulation with high skin penetration and deposition but low systemic absorption is preferable. <u>According to a study, the application of finasteride solution in doses of 100 and 200 μL once daily seems to be more efficacious than applying it twice daily</u>.</strong></span><span style="color: rgb(44, 130, 201)"><strong> On the other hand, increasing the dose up to 300 and 400 μL correlates with higher plasma finasteride concentrations and a possibility of systemic side effects (14).</strong></span> The drug-delivery system plays an important role in the efficacy of topical finasteride. Several compounds have been explored to provide appropriate drug delivery and for biomedical applications including topical solutions, gels, polymersomes, vesicular nanocarriers, vesicular ethosomal carriers, liposomes and niosomes, polymeric nanoparticles, and liquid crystalline nanoparticles (17-24). Among these, a finasteride liposomal gel system containing 2% methylcellulose and a gel system containing poloxamer P407 exhibited the highest skin penetration at the site of application; these may be the ideal future delivery systems for topical finasteride (17)</em></p></blockquote><p></p>
[QUOTE="madman, post: 181104, member: 13851"] Regardless of the duration, the dose used would be key to minimizing any impact on serum DHT levels. [B]Pharmacology of topical finasteride [/B] [COLOR=rgb(184, 49, 47)][B][I]The topical finasteride formulation aims to locally inhibit the 5α-reductase enzyme and decrease the production of DHT at the level of the hair follicle [U]with minimal disturbance of the serum DHT concentration[/U].[/I][/B][/COLOR][I] [COLOR=rgb(44, 130, 201)][B]The finasteride plasma concentration in blood and the extent of absorption with the topical application are lower than that observed with oral administration.[/B][/COLOR] A preliminary clinical trial reported that serum finasteride concentrations after topical application of a combined 5% minoxidil and 0.1% finasteride lipid solution twice daily for 14 days were 10-fold lower than oral finasteride at a similar dosage (12). Another exploratory study reported very low concentrations of finasteride detected in 5 of 11 subjects after a single application of 0.25% topical finasteride; however, multiple applications of topical solution (twice daily for 7 days) resulted in small detectable finasteride plasma concentration in most subjects. Compared to oral tablets (1 mg twice daily for 7 days), the mean maximum finasteride concentration (Cmax) and area under the curve (AUC) of the topical formulation were 15 and 9 times lower, respectively; these were significantly different (13). The reduction in the scalp DHT levels from baseline was similar for 0.25% topical solution twice daily (47%) and oral finasteride 1 mg daily (51%), and significantly lower for daily application once (71%) (14).[COLOR=rgb(184, 49, 47)] [B]The suppression of serum DHT level was noted for both oral and topical administrations after 1-week of treatment. Although these confirm the similar inhibitory effects with multiple-dose treatment, [/B][/COLOR][COLOR=rgb(44, 130, 201)][B][U]the decline in DHT levels seems to be less pronounced with the use of lower-concentration topical formulations[/U].[/B][/COLOR] [B][COLOR=rgb(184, 49, 47)]A study with an application of 0.005% topical solution[U] for 16 months did not observe any change in the serum DHT level [/U](15), while in another study, [U]applying 0.1% topical solution for 24 weeks resulted in no detection of finasteride in half of the blood samples [/U](16). Notably, all studies did not observe any significant difference in serum testosterone levels with topical application (13). [/COLOR][/B] [COLOR=rgb(184, 49, 47)][B]A topical formulation with high skin penetration and deposition but low systemic absorption is preferable. [U]According to a study, the application of finasteride solution in doses of 100 and 200 μL once daily seems to be more efficacious than applying it twice daily[/U].[/B][/COLOR][COLOR=rgb(44, 130, 201)][B] On the other hand, increasing the dose up to 300 and 400 μL correlates with higher plasma finasteride concentrations and a possibility of systemic side effects (14).[/B][/COLOR] The drug-delivery system plays an important role in the efficacy of topical finasteride. Several compounds have been explored to provide appropriate drug delivery and for biomedical applications including topical solutions, gels, polymersomes, vesicular nanocarriers, vesicular ethosomal carriers, liposomes and niosomes, polymeric nanoparticles, and liquid crystalline nanoparticles (17-24). Among these, a finasteride liposomal gel system containing 2% methylcellulose and a gel system containing poloxamer P407 exhibited the highest skin penetration at the site of application; these may be the ideal future delivery systems for topical finasteride (17)[/I] [/QUOTE]
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Testosterone Replacement, Low T, HCG, & Beyond
Testosterone Side Effect Management
Finasteride (Propecia) Hair Lotion or Foam to Treat Hair Loss in Men and Women
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