Sublingual oral minoxidil: bioavailability and haemodynamic side effects

[JaneyElizabeth]

I really wanted oral minoxidil or sublingual minoxidil to work but unfortunately I think I cannot use them because of side effects.

I diluted 1ml of Foligain 5% topical solution with 19ml of ethanol, so I now presumably had 2.5mg of minoxidil in 1ml of my diluted solution.

First I tried swallowing 0.5ml of the solution, so 1.25mg minoxidil. 2 days ago I took this in the morning and then started to watch a movie, so I was really not focussing on side effects or maybe noceboing me. After 15 mins or so I started to feel chest pain, shortness of breath and general malaise. It was actually quite scary.

Yeasterday then I tried 1/4ml of my solution, so about 0.6mg minoxidil sublingually, so I kept it under my tongue for 1.5 minutes and then spit it out. Same side effects to a weaker extent. Not as scary as the day before but still not something I want to feel every day.

I had these side effects after years on topical minoxidil without any problems by the way. Sometimes even 10 % and 5 % together on beard and scalp.

As a last resort I ordered oral minoxidil tablets from alldaychemist now to see if I might tolerate them better...

Some of us older guys might have much more tolerance of such effects because we have used minoxidil for 30 years topically but I find drinking topical to energize my cocktail of meds which were already working.

 

[cetm-419]

Yeah but why do that instead of just drizzling it down the throat. SL is not precise and I think it might work better than topical or well with topical but not better than oral min after a liver pass. That's the whole point--avoid the bloodstream and have it processed via the liver. The stuff tastes nastier the long it's in your mouth but as they say, whatever floats your boat. It's all very interesting.

Best,
Janey

most likely some of the topical solution is destroyed in the GI tract.
the SULT1A1 sulfates minoxidil at the follicular level, and as the inactive form travels in the bloodstream after sublingual absorption, you minimize hemodynamic effects, allowing dose dependent response for people with low enzymatic activity.

also you have to think about the disadvantages of oral min (IF drinking minoxidil works, and that's a big if), as it is metabolized in the liver, the API (active pharmaceutical ingredient: minoxidil sulfate) is further metabolized by the kidney within 30 minutes, and withdrawn from the bloodstream. sublingual min travels in the bloodstream as its inactive form, allowing higher bioavailability. 90% of oral minoxidil is absorbed in the GI tract, but only 10% is metabolized into its API.

topical solution has an absorption rate of 3-5% when covering the entire scalp, now when applying sublingually, that absorption rate will go up. The oral mucosa is a tissue that allows diffusion of drugs (unlike the skin barrier), and leaving it for 5-10 minutes, you could estimate an absorption of 20%, being conservative.

conclusion, sublingual minoxidil is not only safer, but much more efficacious than drinking topical solution. And ongoing clinical trials for sublingual min will show how it's more efficacious than oral tablets.

you can see the results using .45-.90mg here: https://www.sinclairdermatology.com...a-retrospective-caseseries-of-64-patients.pdf

and if you watch the video at the start of the thread, you'll understand why sublingual is the way to go )

and we don't have taste buds in the sublingual region, if you let it sit there, it won't taste at all.

 

[cetm-419]

Okay, more research then but explain the process. Which enzyme does what and which works better. If you have found a way to exceed oral min that that's exciting but I don't know. Oral min by drizzling/drinking topical works and it is dirt cheap, say 10$ annually.

actually the genius is dr. Rodney Sinclair in Melbourne, Australia. the catch with sublingual is that minimizing of hemodynamic effects, thus, being able to use higher doses without risks (though it may be unnecessary due to the higher bioavailability of sublingual)

 

[LouisSarkozy]

actually the genius is dr. Rodney Sinclair in Melbourne, Australia. the catch with sublingual is that minimizing of hemodynamic effects, thus, being able to use higher doses without risks (though it may be unnecessary due to the higher bioavailability of sublingual)

thanks for your contribution man , do you think one could be able to avoid skin sides ( i got bad ones on topical and fucked up heart related sides using oral) using sublingual min or when i comes to skin sides it's all the same? btw do you think iit's safe to take long term and is tere any way for someone in france or europe to get his hands on sublingual min?

 

[JaneyElizabeth]

most likely some of the topical solution is destroyed in the GI tract.
the SULT1A1 sulfates minoxidil at the follicular level, and as the inactive form travels in the bloodstream after sublingual absorption, you minimize hemodynamic effects, allowing dose dependent response for people with low enzymatic activity.

also you have to think about the disadvantages of oral min (IF drinking minoxidil works, and that's a big if), as it is metabolized in the liver, the API (active pharmaceutical ingredient: minoxidil sulfate) is further metabolized by the kidney within 30 minutes, and withdrawn from the bloodstream. sublingual min travels in the bloodstream as its inactive form, allowing higher bioavailability. 90% of oral minoxidil is absorbed in the GI tract, but only 10% is metabolized into its API.

topical solution has an absorption rate of 3-5% when covering the entire scalp, now when applying sublingually, that absorption rate will go up. The oral mucosa is a tissue that allows diffusion of drugs (unlike the skin barrier), and leaving it for 5-10 minutes, you could estimate an absorption of 20%, being conservative.

conclusion, sublingual minoxidil is not only safer, but much more efficacious than drinking topical solution. And ongoing clinical trials for sublingual min will show how it's more efficacious than oral tablets.

you can see the results using .45-.90mg here: https://www.sinclairdermatology.com...a-retrospective-caseseries-of-64-patients.pdf

and if you watch the video at the start of the thread, you'll understand why sublingual is the way to go )

and we don't have taste buds in the sublingual region, if you let it sit there, it won't taste at all.

Trust me. Oral topical min makes it through the liver. I don't deny that small amounts might be lost but we are talking about something quite potent. I have been on very high levels of oral topical so maybe it is only half as potent or whatever but you know with this stuff if it is working because it took my slow steady HRT improvement which was going to work even without oral min but oral min just puts things into a frenzied growth state, for me anyway. Nothing ever worked for me as a male but maybe I should have tried Loniten before I jumped ship but honestly a couple of years ago when I wasn't so active, I had never heard of Loniten and I was afraid of peripheral hair growth but eh, that's
manageable. I don't even know how I would tell the difference plus are you saying the two types are equally viable?

 

[JaneyElizabeth]

actually the genius is dr. Rodney Sinclair in Melbourne, Australia. the catch with sublingual is that minimizing of hemodynamic effects, thus, being able to use higher doses without risks (though it may be unnecessary due to the higher bioavailability of sublingual)

You still have the blood pressure issue to do with but hey, it might be worth a try for people using lots like me and for people not responding to swallowing minoxidil. Pretty cool. I would like to see some non-affiliated data but then again we only have that for Loniten anyway. Most of the non-anti-androgens can carry heavy sides and long-term liver risk so yes, less garbage in, less garbage out. This includes finasteride and duta but I swear to Goddess that I take both daily and I have no idea that I am taking them. If a miss a few days since duta has a long half-life, I still don't feel any different.

Maybe I was made for hormonal medications and some think that minoxidil is also hormonal in nature ultimately.

 

[Moz5x]

You still have the blood pressure issue to do with but hey, it might be worth a try for people using lots like me and for people not responding to swallowing minoxidil. Pretty cool. I would like to see some non-affiliated data but then again we only have that for Loniten anyway. Most of the non-anti-androgens can carry heavy sides and long-term liver risk so yes, less garbage in, less garbage out. This includes finasteride and duta but I swear to Goddess that I take both daily and I have no idea that I am taking them. If a miss a few days since duta has a long half-life, I still don't feel any different.

Maybe I was made for hormonal medications and some think that minoxidil is also hormonal in nature ultimately.

Janey, how bad was the edema when you were at the highest doses of drinking liquid min? How did you manage it?

 

[JaneyElizabeth]

Janey, how bad was the edema when you were at the highest doses of drinking liquid min? How did you manage it?

It wasn't that long ago but I had had surgery under anesthesia and that might have affected. I lowered dosage mostly last week to 6.25mg twice daily and that seemed to work plus I dropped like ten pounds in a week which is impossible unless it is bloating. My under the eye issue has improved in just a few days and before they were pretty swollen when I woke. Somebody said that Prep-H is good for that.

It's good for me to use less and now I can play around with sublingual once daily. Some might consider my 12.5mg twice daily to be a mega-dosage but I think that is close to where the intolerable side-effects start. But when my feet and ankles were so swollen? I couldn't think of anything else to do.

I do take some risks because all of this is so thrilling to me; except bone, I have all but completely re-matrixed from head to toe. I have at least average breasts for a cis-female, i.e. C to D. My skin is much paler and tactile. My mind has been charged and it feels like I know what females and males both know, in terms of thoughts, emotions, aggression, risky behavior.

I get how I am supposed to be humiliated to enjoy or want this, but HRT removed really my ability to feel either shame or emotion. I am trying to novelize maybe a lot of my journey and the @bridgburn thread about just how much excitement there was when Bridge started growing long copious curls. I was on very weak HRT and slowly titrating bu i all went to tits and ***, so to speak. It's really hard for many to get facial or hair changes but I sure have and all of it over 55 pretty much in terms of when the big changes came and I was no longer just a guy in a dress. Androgyny creeps forward. I only need more length and just a tiny bit more in the hairline and then my lifetime goal of 36, an impossible goal, becomes reality.

Like Bridge, what do you do when you reach your goals? Pack up shop? Pretty soon all of this will just be par of my past and my new reality is one that is androgynous with really nice long hair. Anyway, since I was blessed, I have uploaded a huge representation of my hair and body journey. Trans people like to see body pics so I post some of those but also as a warning to people. I love how I look but I am pretty petite and soft and I can no longer hide my breast growth or my enormous nipples, when I wear white so eh, HRT and oral min can probably take a lot of people to the promised land but beware to all who enter the temple of Goddess:

"You can check out anytime that you want but you can never leave....."

 

[michel sapin]

left is from January, before minoxidil. right is current.

both pictures taken at the end of the day, when it starts looking bad, also same bathroom. (really harsh lightning)

man i have the exact same diffuse thinning as you! amazing result! did you use topical minoxidl previously? How long on oral minoxiidl to get those result? you used 5 mg ?
I used 1.25 mg for 3 month and only get huge hypertrichosis , like you for the face / upper cheek, etc. Do you also get arm/ leg/ body hypertrichosis?

 

[cetm-419]

thanks for your contribution man , do you think one could be able to avoid skin sides ( i got bad ones on topical and fucked up heart related sides using oral) using sublingual min or when i comes to skin sides it's all the same? btw do you think iit's safe to take long term and is tere any way for someone in france or europe to get his hands on sublingual min?

I haven't heard of any skin side effects using either oral min, but idk that much about topical minoxidil, I haven't used it. I don't know if sublingual/oral min are safe long term, future research is very much needed. but honestly and like most of us, I hate the way my hair feels and looks, I find it extremely annoying to live with. I wouldn't do any HRT as I think for males who don't want to transition, it's just solving one big problem with another big problem.

I'm really happy I'm getting any results this early on treatment, and I intervened early on; so I doubt I'll ever have to do anything extreme.

and unfortunately the only place you'll find minoxidil compounded for sublingual absorption Is Sinclair Dermatology. I'm using the topical solution applied under my tongue.

 

[cetm-419]

Trust me. Oral topical min makes it through the liver. I don't deny that small amounts might be lost but we are talking about something quite potent. I have been on very high levels of oral topical so maybe it is only half as potent or whatever but you know with this stuff if it is working because it took my slow steady HRT improvement which was going to work even without oral min but oral min just puts things into a frenzied growth state, for me anyway. Nothing ever worked for me as a male but maybe I should have tried Loniten before I jumped ship but honestly a couple of years ago when I wasn't so active, I had never heard of Loniten and I was afraid of peripheral hair growth but eh, that's
manageable. I don't even know how I would tell the difference plus are you saying the two types are equally viable?

the enzymatic activity is not only higher, but more homogeneous in the liver. but when comparing pros and cons of both routes of drug administration, I think sublingual is equivalent to oral minoxidil at least. maybe a superior treatment, so far studies show this, but unfortunately they are not top quality studies. most of them retrospective and/or letters to the editor (not peer reviewed).

and yes, i agree, topical solution should work to some extent, as there's been cases of 6-7 year olds drinking less than a teaspoon (aprox. 5 ml) and presenting serious hemodynamic effects. but I definitely think sublingual is the way to go when using topical solution.

 

[cetm-419]

You still have the blood pressure issue to do with but hey, it might be worth a try for people using lots like me and for people not responding to swallowing minoxidil. Pretty cool. I would like to see some non-affiliated data but then again we only have that for Loniten anyway. Most of the non-anti-androgens can carry heavy sides and long-term liver risk so yes, less garbage in, less garbage out. This includes finasteride and duta but I swear to Goddess that I take both daily and I have no idea that I am taking them. If a miss a few days since duta has a long half-life, I still don't feel any different.

Maybe I was made for hormonal medications and some think that minoxidil is also hormonal in nature ultimately.

any effect on blood pressure belongs to hemodynamic effects. that's why it's so promising.

and minoxidil is not hormonal, all scientific evidence point to it working through the wnt-beta-catenin pathway.

 

[cetm-419]

man i have the exact same diffuse thinning as you! amazing result! did you use topical minoxidl previously? How long on oral minoxiidl to get those result? you used 5 mg ?
I used 1.25 mg for 3 month and only get huge hypertrichosis , like you for the face / upper cheek, etc. Do you also get arm/ leg/ body hypertrichosis?

diffuse thinning sucks big time... though we can respond really good to treatments. I never applied the solution in my scalp.

I'm almost on month 5 and starting to notice improvement, specially in pictures, but it's only to the point where I know it's improving, but my hair still feels thin and has a poor aesthetic.

for me hypertrichosis has been fun tbh (and a sign I'm responding above average, hypertrichosis doesn't necessarily correlates with improvement in scalp hair, but scalp improvement does correlates with some degree of hypertrichosis).

yeah, I have small hairs on my shoulders, thicker hair on my arms and at the back of my neck. my legs where already hairy so I didn't notice any day and night difference, but they thickened for sure.

 

[bassie21]

so my take on the oral vs sublingual discussion: I could only find one study on sublingual use of minoxidil. sadly, they did not compare oral to sublingual administration. so, objectively speaking, there's no (scientific) way to know which one is better. hypothesizing either route is better than the other is just .... hypothesizing imo. I'm not saying it does not work - there's just been no study to investigate oral vs sublingual so your guess is as good as mine.

 

[cetm-419]

do you think topical solution would work sublingually?

 

[cetm-419]

so my take on the oral vs sublingual discussion: I could only find one study on sublingual use of minoxidil. sadly, they did not compare oral to sublingual administration. so, objectively speaking, there's no (scientific) way to know which one is better. hypothesizing either route is better than the other is just .... hypothesizing imo. I'm not saying it does not work - there's just been no study to investigate oral vs sublingual so your guess is as good as mine.

and yes, I agree with you, there isn't any scientific publication discussing oral vs sublingual. but with your knowledge being a chemist, how much do you think the topical solution would work sublingually? are there any compounding differences that could significantly affect absorption between the topical solution and a sublingual tablet?

 

[bassie21]

do you think topical solution would work sublingually?

yes it will, because it contains the same minoxidil molecule just as any other (DIY) minoxidil solution or Lonnoten would.

don't forget to dilute a 5% topical minoxidil solution 20x to get 2,5mg/ml concentration though! whether topical used sublingually is better or worse than topical used orally is anyones guess at this point.

also: when using a topical solution orally/sublingually, you're also ingesting delivery vehicle (water, ethanol, PG, .... ), possible impurities (different rules for topicals vs oral meds) and depending on exact formulation caffeine, retinol, azaleic acid or even added finasteride. So there's a risk you're getting more than you asked for.

 

[cetm-419]

yes it will, because it contains minoxidil just as any other (DIY) minoxidil solution would. don't forget to dilute a 5% minoxidil solution 20x to get 2,5mg/ml concentration though!

thanks! you were really helpful!!

 

[Moz5x]

yes it will, because it contains the same minoxidil molecule just as any other (DIY) minoxidil solution or Lonnoten would.

don't forget to dilute a 5% topical minoxidil solution 20x to get 2,5mg/ml concentration though! whether topical used sublingually is better or worse than topical used orally is anyones guess at this point.

also: when using a topical solution orally/sublingually, you're also ingesting delivery vehicle (water, ethanol, PG, .... ), possible impurities (different rules for topicals vs oral meds) and depending on exact formulation caffeine, retinol, azaleic acid or even added finasteride. So there's a risk you're getting more than you asked for.

bassie21, What are your thoughts about dissolving an oral min tablet under the tongue? Would it potentially be the same efficacy as swallowing the tablet?
Also, what are your thoughts on the video I posted in the original post of this thread?

I agree, without further research it’s all hypothesizing. My reason for posting that video was to hopefully get some discussion on Dr Bhoyrul’s claims. My interest in sublingual isn’t around the claim of higher efficacy of hair growth of sublingual vs topical vs oral per se but rather it’s potential to sidestep the uncomfortable and troublesome hemodynamic effects that make the drug intolerable as dosage increases.

 

[bassie21]

bassie21, What are your thoughts about dissolving an oral min tablet under the tongue? Would it potentially be the same efficacy as swallowing the tablet?
Also, what are your thoughts on the video I posted in the original post of this thread?

I agree, without further research it’s all hypothesizing. My reason for posting that video was to hopefully get some discussion on Dr Bhoyrul’s claims. My interest in sublingual isn’t around the claim of higher efficacy of hair growth of sublingual vs topical vs oral per se but rather it’s potential to sidestep the uncomfortable and troublesome hemodynamic effects that make the drug intolerable as dosage increases.

"What are your thoughts about dissolving an oral min tablet under the tongue?" --> should be perfectly fine (cut the pill into 5, 2.5 or 1.5 mg parts though!)

"Would it potentially be the same efficacy as swallowing the tablet?" --> that's the oral vs sublingual discussion, there's no scientific evidence yet one is better or worse than the other

"My interest in sublingual isn’t around the claim of higher efficacy of hair growth of sublingual vs topical vs oral per se but rather it’s potential to sidestep the uncomfortable and troublesome hemodynamic effects that make the drug intolerable as dosage increases." --> I would hypothesize that even if minoxidil gets into your bloodstream via the sublingual route, at least a part of it would also get into your liver sooner or later so it would be metabolized over there after all. I mean, what's the difference of chemicals getting into your bloodstream via the GI route vs the sublingual route, both routes result in the substance getting into your blood and therefore, sooner or later, in your liver.

Believing that using the sublingual route 100% of the minoxidil will be metabolized somewehere else than the liver so this magical route won't cause hemodynamic effects because 'sublingual you know, it does not reach the liver bc all is metabolized in your hair follicles' is just another hypothesis imho.