MPB and Finasteride (side effects/dosing theory)

[BillyJ03z]

If Finasteride has a cumulative effect then it wouldn't matter what dosage someone was taking as the finasteride would continue build up in the body to levels that would eventually cause side effects, it's just that a lower dose would take more time to achieve the negative side effects as opposed to larger doses which would be quicker to build levels that cause side effects...

My thinking is that any reduction in DHT would be an improvement than baseline for someone who is suffering MPB... I think if I could achieve no more than 25% DHT suppression that would at least slow down MPB.... Since finasteride has a half-life of 5-7 hours and takes approx 27-33 hours to clear the body/system, I'm think of taking 0.1 mg Finasteride 2x week (Mon and Thurs)... I believe that would be enough to induce a slight but beneficial decrease in DHT and it would in theory eliminate the cumulative dosing in the body.... as the key is to make sure the body has eliminated each finasteride dose before the next is administered. Possibly every 4 day dosing is probably the safest to ensure almost complete elimination of Fin in the body before next dose.
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[Cataceous]

I think a better approach is to take advantage of the newer research on micro-dosed topical finasteride, e.g. this. You do get less systemic DHT reduction and fairly decent results, albeit not as good as those from the full-dose oral treatment. Based on this and related work I've been using 0.2 mg/day finasteride topically with no apparent side effects. In contrast, 1 mg/day orally caused me a lot of problems.

 

[BillyJ03z]

I think a better approach is to take advantage of the newer research on micro-dosed topical finasteride, e.g. this. You do get less systemic DHT reduction and fairly decent results, albeit not as good as those from the full-dose oral treatment. Based on this and related work I've been using 0.2 mg/day finasteride topically with no apparent side effects. In contrast, 1 mg/day orally caused me a lot of problems.

I was considering going the topical route, but I am worried about transfer to my wife and kids after rubbing in... figured super low dose oral route would be the way to go... but regarding my theory you have to admit it does make sense considering all factors... I am almost 100% sure that ED use of finasteride regardless of dosage builds up cumulatively and crushes DHT production eventually.. I really believe spacing doses until the body clears the preceding dose is the way to go... However research has also said that the effects a single dose of fin can last up to 30 - 90 days to fully clear....

 

[Cataceous]

Your idea about the buildup isn't quite right. With a half-life of only six hours, finasteride will basically be at steady state in under two days. There's no additional buildup from daily dosing. The effect on DHT is more complicated. Its binding of the 5ar enzyme is pretty much irreversible. Thus the effects will depend on the dose and the creation rate of 5ar. Per Wiki it takes very little to get the maximum result: "An oral dosage of finasteride of only 0.2 mg/day has been found to achieve near-maximal suppression of DHT levels (68.6% for 0.2 mg/day relative to 72.2% for 5 mg/day). Finasteride does not completely suppress DHT production because it lacks significant inhibitory effects on the 5α-reductase type I isoenzyme, with more than 100-fold less inhibitory potency for type I as compared to type II ..."

 

[madman]

If Finasteride has a cumulative effect then it wouldn't matter what dosage someone was taking as the finasteride would continue build up in the body to levels that would eventually cause side effects, it's just that a lower dose would take more time to achieve the negative side effects as opposed to larger doses which would be quicker to build levels that cause side effects...

My thinking is that any reduction in DHT would be an improvement than baseline for someone who is suffering MPB... I think if I could achieve no more than 25% DHT suppression that would at least slow down MPB.... Since finasteride has a half-life of 5-7 hours and takes approx 27-33 hours to clear the body/system, I'm think of taking 0.1 mg Finasteride 2x week (Mon and Thurs)... I believe that would be enough to induce a slight but beneficial decrease in DHT and it would in theory eliminate the cumulative dosing in the body.... as the key is to make sure the body has eliminated each finasteride dose before the next is administered. Possibly every 4 day dosing is probably the safest to ensure almost complete elimination of Fin in the body before next dose.
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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!


*Considerable evidence exists in the contemporary literature regarding the physiological role of 5a-reductases in the peripheral tissues and CNS and the pathophysiological implication of inhibiting this family of enzymes and blunting biosynthesis of neurosteroids, which are critical biological mediators in the CNS, and contribute to altered mood, cognition, and libido (23–50). Also, significant pre-clinical evidence exists demonstrating that inhibition of 5a-RIs contributes to erectile dysfunction (16–22) and may also contribute to neurological symptoms (Fig. 4 (36).

Topical finasteride for male androgenetic alopecia

Abstract Background Oral finasteride is a well-established treatment for men with androgenetic alopecia (AGA), but long-term therapy is not always acceptable to patients. A topical finasteride formulation has been developed to minimize systemic exposure by acting specifically on hair follicles...

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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. 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. 14


PK and PD analyses Mean

Mean ± SD maximum plasma finasteride concentrations were 36.5 ± 45.9 pg/mL with topical finasteride and 7166 ± 12,744 pg/mL with oral finasteride at Week 12; and were 48.0 ± 87.2 pg/mL and 5029 ± 4182 pg/mL, respectively, at Week 24.

Mean serum DHT concentrations in the placebo group remained unaffected during the study (range: 38.5 to 39.8 ng/dL). 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). 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 ).

The lower impact of topical finasteride on DHT levels was not accompanied by any shift from normal to high plasma testosterone concentrations for patients in this group; this was also the case for the placebo group. In the oral finasteride group, this shift occurred in four (6.7%) patients




*Some patients treated with oral finasteride may experience adverse effects potentially related to the circulating plasma concentration of drug required to achieve effective concentrations at the scalp. 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 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). 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. 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 lower with topical than oral finasteride.




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. This result was achieved with markedly lower systemic exposure to finasteride and less impact on serum DHT concentrations compared with oral finasteride. 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. 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.

Finasteride for hair loss

Abstract Background and Objectives: Finasteride 1 mg/day is indicated for androgen-dependent conditions such as male androgenetic alopecia (AGA). Methods: The literature is comprehensively summarized on the pharmacodynamics, pharmacokinetics, mechanism of action, and metabolism of...

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4. Mechanism of action

Finasteride inhibits type II 5AR isoenzyme 100-fold more selectively over type I isoenzyme (7). 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 (7,23) (Figure 2). Therefore, this leads to a significant reduction in scalp and serum DHT levels (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). 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). 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).


6. Bioavailability

Propecia may be orally administered with or without meals as the bioavailability is not affected by food (7). 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). 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). Finasteride is absorbed completely in 6-8 hours post-administration (32). The circulating finasteride is bound to the plasma proteins (89.8-91.3%) and slowly accumulates after multiple doses (7,33).

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). Following oral administration of finasteride, it was reported that approximately 39% of the metabolites were excreted through urine and 57% excreted through feces (7).

 

[madman]

4. Impact of 5α-reductase inhibitors on sexual function


5-ARIs, mainly including finasteride and dutasteride, represent a class of drugs that competitively inhibit 5-alpha reductase isoenzymes (5-ARs). In humans, three types of 5-ARs have been described so far: type-1 is temporarily expressed in newborn skin and scalp and is permanently detectable in the skin after puberty onset; type-2 localizes predominately in fetal genital skin and male accessory glands including prostate [40]; type-3 is expressed both into androgen-dependent tissues (e.g. smooth muscle and prostate) and in the brain, heart, and other peripheral tissues [41].

In vitro experiments have shown a higher inhibitory activity of dutasteride on type 3 than type 2( 5-ARs). By contrast, these isoenzymes are similarly sensitive to finasteride [41]. Several mechanisms have to be considered when the impact of 5-ARIs on sexual function is considered.

*First of all, dihydrotestosterone (DHT) more effectively than T enhances nitric oxide (NO) availability in the endothelium [42]. Thus, 5-ARIs can indirectly reduce the peripheral amount of NO concentration and, consequently, have a negative impact on erection.

*The reduction in DHT explains the reduced volume of ejaculate experienced by treated patients and, in addition, these drugs are able to prevent the conversion of progesterone and deoxycorticosterone into neurosteroids, the latter playing a role in regulating mood, anxiety, sleep, and sexual function [43,44].

*Finally, finasteride can exert a central effect by crossing the blood-brain barrier and reducing the hormonal impregnation of the central nervous system [45,46].

 

[madman]

Sexual Problems in Men With Alopecia Treated With Oral Finasteride- Are Topical Solutions Better?

CONCLUSION AGA is a common situation that men are interested and seeking solutions. 5-ARIs—some of the FDA-approved medicines—have been increasingly used in this context in the treatment of AGA. However, 5-ARIs have well-defined side effects that can negatively affect sexual life. The real...

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Controversies in the treatment of androgenetic alopecia: The history of finasteride

2.3 | RECOMMENDATIONS All drugs carry a risk of adverse events. As clinicians, when prescribing drugs, we strike a balance between the risk of developing adverse events and the benefit of the treatment. While some drugs such as finasteride are effective in the treatment of the underlying...

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Efficacy of Topical Combination of 0.25% Finasteride and 3% Minoxidil Versus 3% Minoxidil Solution in Female Pattern Hair Loss:

Efficacy of Topical Combination of 0.25% Finasteride and 3% Minoxidil Versus 3% Minoxidil Solution in Female Pattern Hair Loss: A Randomized, Double‑Blind, Controlled Study Key Points The efficacy of oral finasteride in female pattern hair loss (FPHL) has been reported. Topical formulations of...

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Dutasteride vs Finasteride

Hi Is it true 0.25mg dutasteride is more powerful 5mg finasteride? Thanks

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Post-finasteride syndrome: a surmountable challenge for clinicians

Post-finasteride syndrome: a surmountable challenge for clinicians Abdulmaged M. Traish, Ph.D. Department of Urology, Boston University School of Medicine, Boston, Massachusetts Post-finasteride syndrome (PFS) is a constellation of serious adverse side effects manifested in clinical...

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Treatment review for male pattern hair-loss

ABSTRACT Introduction: Androgenetic alopecia is a common hair loss disorder affecting up to 80% of males by the age of 80. It is characterized by androgen-related progressive thinning of hair in a defined pattern. It results in diminished self-esteem, reduced confidence, and distress in...

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Health Risks Associated with Long-Term Finasteride and Dutasteride Use

https://wjmh.org/DOIx.php?id=10.5534/wjmh.200012 Health Risks Associated with Long-Term Finasteride and Dutasteride Use: It’s Time to Sound the Alarm 5α-dihydrotestosterone (5α-DHT) is the most potent natural androgen. 5α-DHT elicits a multitude of physiological actions, in a host of tissues...

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Finasteride (Propecia) Hair Lotion or Foam to Treat Hair Loss in Men and Women

Topical finasteride for the treatment of male androgenetic alopecia and female pattern hair loss: a review of the current literature ABSTRACT Background: Androgenetic alopecia (AGA) is a frequently encountered dermatological concern that impacts a patient’s self-esteem and quality of life...

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Finasteride (Propecia) for Scalp Hair Loss and Excess Facial Hair in Women: Safe and Effective?

The efficacy and use of finasteride in women: a systematic review Abstract Background Physicians are beginning to use finasteride as a treatment for hair loss, hirsutism, and various other dermatologic conditions in women. However, the reported efficacy and use of finasteride in the female...

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Finasteride: Suicidality and Psychological Adverse Events in Men Taking Propecia or Proscar

Investigation of Suicidality and Psychological Adverse Events in Patients Treated With Finasteride IMPORTANCE There is ongoing controversy about the adverse events of finasteride, a drug used in the management of alopecia and benign prostatic hyperplasia (BPH). In 2012, reports started...

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Efficacy and safety of dutasteride vs finasteride in treating males with BPH

Efficacy and safety of dutasteride compared with finasteride in treating males with benign prostatic hyperplasia: A meta‑analysis of randomized controlled trials Abstract The present study was an updated meta-analysis that aimed to confirm the efficacy and safety of dutasteride (0.5 mg) and...

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The clinical applications of 5ARi's

Introduction: Five-alpha reductase (5-AR) deficiency was first identified by Imperato-McGinley and Walsh as the cause of pseudohermaphroditism in two separate studies. The discoveries led to the development of finasteride (inhibitor of type 2 isoenzyme of 5-AR) and dutasteride (inhibitor of type...

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Effects of dutasteride on sex hormones and cerebrospinal steroids in patients treated for BPH

Abstract Purpose Neuroactive steroids may have a role in regulating sexual function. This case-control study assessed whether dutasteride, a 5α-reductase inhibitor used for the treatment of patients with benign prostate hyperplasia (BPH), impacts the levels of neuroactive steroids, leading to...

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Finasteride for hair loss

Abstract Background and Objectives: Finasteride 1 mg/day is indicated for androgen-dependent conditions such as male androgenetic alopecia (AGA). Methods: The literature is comprehensively summarized on the pharmacodynamics, pharmacokinetics, mechanism of action, and metabolism of...

www.excelmale.com

Clinical Patterns of Hair Loss in Men Is DHT the Only Culprit?

INTRODUCTION The pathophysiology of male androgenetic alopecia (AGA) has focused on the role of androgens, mainly dihydrotestosterone (DHT) and its production by 5a-reductase. Inhibitors of 5a-reductase have been developed and studied for male AGA including finasteride, which was approved by...

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The connection of 5AR inhibitors like finasteride to the development of depression

ABSTRACT Recent literature connects 5-alpha reductase inhibitors (5-ARIs) with neuropsychiatric adverse effects. Several clinical studies have indicated that former 5-ARIs users had a higher incidence of depressive symptoms and neuropsychiatric side effects than non-users. However, the...

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Post-Finasteride Syndrome

Endocrinologist Professor Michael Irwig shares his experiences seeing patients with persistent side effects from finasteride, a drug marketed to young men for male pattern baldness. Post-Finasteride Syndrome is the current term for a rare syndrome of devastating physical, neurological, and...

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Treatment options for androgenetic alopecia

Abstract Background: Androgenetic alopecia (AGA) is the most common form of hair loss consisting of a characteristic receding frontal hairline in men and diffuse hair thinning in women, with frontal hairline retention, and can impact an individual's quality of life. The condition is primarily...

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[madman]

I think a better approach is to take advantage of the newer research on micro-dosed topical finasteride, e.g. this. You do get less systemic DHT reduction and fairly decent results, albeit not as good as those from the full-dose oral treatment. Based on this and related work I've been using 0.2 mg/day finasteride topically with no apparent side effects. In contrast, 1 mg/day orally caused me a lot of problems.

Topical finasteride for male androgenetic alopecia

Abstract Background Oral finasteride is a well-established treatment for men with androgenetic alopecia (AGA), but long-term therapy is not always acceptable to patients. A topical finasteride formulation has been developed to minimize systemic exposure by acting specifically on hair follicles...

www.excelmale.com

 

[BillyJ03z]

I have scheduled an appt with a dermatologist to get a topical fin script but it's not until Feb 3rd.. UGH! I don't think I can afford to wait long....

Does anybody know of any peptide/research chem sites that sell liquid finasteride? I know of Minoxidil Max but I heard a bunch of shady things about them and it would take a few weeks to get here... I also know of a few peptide sites that sell Oral Finasteride but it is dosed at 5mg/ml in Polyethylene glycol (PEG)... assuming it's legit and properly dosed at exactly 5mg per ML then I could take just 1ml of fin and add 20 ml of liquified foam minox for a .05 topical... but it would be a waste of time if it wasn't real to begin with...

Any thoughts?????

 

[Cataceous]

Although it's not a good solution for you in particular, it is possible to get finasteride powder from thekaneshop.com. The problems: slow shipping—maybe international, minimum purchase is a gram for $100, and you need a decent milligram scale to measure doses.

 

[BillyJ03z]

Although it's not a good solution for you in particular, it is possible to get finasteride powder from thekaneshop.com. The problems: slow shipping—maybe international, minimum purchase is a gram for $100, and you need a decent milligram scale to measure doses.

Yeah, Finasteride is something I don't want to measure and dose it wrong... Ugh..

Sucks ass that I need to schedule an appt with a Dermatologist just to get a script for a finasteride topical... and I don't even know if he will prescribe what I want from Empower... smdh

 

[Systemlord]

I need to schedule an appt with a Dermatologist just to get a script for a finasteride topical... and I don't even know if he will prescribe what I want from Empower... smdh

My endo at Kaiser prescribed Empower T cream. I don't see why a doctor would reasonably refuse such a request when they regularly prescribe finasteride in pill form without much of a fight.

 

[BillyJ03z]

My endo at Kaiser prescribed Empower T cream. I don't see why a doctor would reasonably refuse such a request when they regularly prescribe finasteride in pill form without much of a fight.

So my GP prescribed Empower Pharmacy's Hair Restore LF Foam (lanatprost/finasteride)... Just started tonight... the LF foam (finasteride) is dosed at .1 mg/ml.... so I cut it with an additional 90 ml of melted Minoxidil foam..... so now I have a finasteride solution of .0125 per ml.... so I will see how this works and hopefully I don't get sides... so my nightly regimen is .0125 mg topical fin, additional 5% minox, nizoral 2% cream and 2% miconazole nitrate cream rubbed into scalp.....

 

[BillyJ03z]

Ok... so I have tried Empower Pharmacy's LF foam and Hair Restore Ultra.. My DHT starting point baseline in December 21' was 882 (ref range: 106.0 - 719.0 pg/mL). From December 21' to March 22', I was using LF foam @ .025/ML and in March my DHT lab came back at 412... but I also added 20-30mg Prog Cream to my scalp as well for about 2-3 weeks prior to testing. (During the 2-3 weeks that I added the Prog Cream my nipples became very soar and itchy, so the Prog cream could have possibly increased the DHT serum impact). So because it looked like LF foam was going systemic with DHT being cut by 50%, I switched to Empower Hair Restore Ultra @ .00625%. From March 22' to June 22', I was using Hair Restore Ultra @ .00625/ML (using 2 ML for total of .0125) and my lab test as of June 22' was 774, which is showing minimal/if none at all impact to serum DHT.

Results for hair during this time the following happened..... I had thinning in crown which was easily covered by Toppik, but after starting LF foam in Dec 21' the hair that I did have in my crown area seemed to fall out and I could no longer cover with toppik as their was no longer hair to hold onto (seemed to shed/fall out.) After I switched to Hair Restore Ultra in Mar 22', I noticed that in May 22' there seemed to hair regrowing in the crown area, which I attribute to being jumpstarted by LF foam, and I was able to use Toppik again as there was hair for the toppik to hold onto again. This is where I currently am presently. My only concern as of now is that the Hair Restore Ultra is not impacting my DHT serum, which should be a good thing, but it also makes me wonder if the Finasteride is doing anything or it's the minoxidil that is giving temporary appearance of hair growth.

The LF foam and Hair Restore Ultra come from Empower Pharmacy dosed at .1% and I cut it down with melted minoxidil foam. I find it hard to apply finasteride liquid as it runs down the scalp and it gets messy, so to get around the liquid mess, I put my dose of the liquid finasteride into a shot glass and then add a couple drops of pure Aloe Vera gel and mix together, which turns it into a thicker liquid substance which I can then scoop with my finger and put it directly onto my scalp without it running all over the place.