Minoxidil - Sublingual

[Approach]

I currently take 2.5 oral Minoxidil once/day.

Today my doctor prescribed 2.5 mg/ml sublingual Minoxidil liquid drops, to be filled at my local compound pharmacy.  I anticipated I would start at a lower dose, but maybe she made it 2.5 since my body is used to taking Minoxidil pills?  (I will call her for further clarification as to whether this is too high of a starting dose.)

My question is:  Generally speaking, is sublingual Minoxidil typically taken twice/day?   (I'm asking b/c I've been taking the pill-form once/day.)  From what you're hearing from others, is twice/day sublingual typical? 

This is what she looked at right before prescribing it to me: https://www.bayviewrx.com/formulas/Minoxidil-2-5-mg-ml-Oral-Sublingual-Solution-Alopecia-Hypertension-Androgenic-Alopecia-Telogen-Effluvium-Hypotrichosis-

I plan to follow up with her to address these concerns.  In-the-mean-time, do you guys have any personal opinions about my question above, or any general opinions about this oral solution?  Thanks guys.

PS) Admittedly, I believe I should have a dermatologist evaluate me / prescribe this.  But, frankly-  my pcp makes herself available to me at times that fit my schedule better, etc.  

Edited June 19 by Approach

[Eli_Avdikian]

I don't think it matters much how many times you take it a day, as long as you stick with a certain dose. If you take the 2.5 mg dose twice a day, you'ill end up ingesting 5 mg of minoxidil daily, which is a very standard dose 

[Viney]

Once a day should be fine. I only take it once a day.

Some docs will recommend taking it before bed to prevent feeling potential side effects such as dizziness. I take it in the morning as it suits my routine more.

2.5mg is a pretty strong starting dose for SM in my opinion. I started at 0.9mg and slowly worked my way up to 2.7mg. But since you're already taking oral min your body should hopefully be used to it.

Edited June 19 by Viney

[arthurSam]

I saw in another post related to sublingual  minox  that it can reduce sides ... I am curious how sublingual oral minoxidil can reduce sides compared to oral minox... can someone explain me ? I have sides with oral so I'm interested

Edited June 19 by arthurSam

[Viney]

8 minutes ago, arthurSam said:

I saw in another post related to sublingual  minox  that it can reduce sides ... I am curious how sublingual oral minoxidil can reduce sides compared to oral minox... can someone explain me ? I have sides with oral so I'm interested

Quoting a paper online:

As sublingual dosing bypasses hepatic first-pass metabolism, sublingual minoxidil (SM) would be anticipated to increase follicular minoxidil sulfate bioavailability and consequently hair growth. As hepatic sulfation of minoxidil enhances the haemodynamic effect, SM would also be anticipated to reduce haemodynamic side effects and consequently improve safety. 

[arthurSam]

3 minutes ago, Viney said:

Quoting a paper online:

As sublingual dosing bypasses hepatic first-pass metabolism, sublingual minoxidil (SM) would be anticipated to increase follicular minoxidil sulfate bioavailability and consequently hair growth. As hepatic sulfation of minoxidil enhances the haemodynamic effect, SM would also be anticipated to reduce haemodynamic side effects and consequently improve safety. 

Thanks I will try to find SM in my country

[Approach]

I really appreciate it guys.  You've given me some feedback to think about.  I'll verify all this with my doctor next time I see her.

[Approach]

38 minutes ago, arthurSam said:

I saw in another post related to sublingual  minox  that it can reduce sides ... I am curious how sublingual oral minoxidil can reduce sides compared to oral minox... can someone explain me ? I have sides with oral so I'm interested

"Part" of the reason I'm going the SM route is to hopefully reduce my side effect from the Minoxidil pill.  Bypassing hepatic first-pass metabolism....might be the trick for me.  Stay in touch, I'll let you know.

[arthurSam]

Hello,

Thanks you for your answers.

I've done some research on sublingual minoxidil and I found very interesting things :

• Equivalent for efficacy of 5mg oral minox is about 1,5 -2 mg sublingual with a high reduction in serum level (more than 80%) and so also in sides.
• 4mg sublingual is 2,5x better in efficacy than 5mg minox, with about same serum level than 2.5mg oral and so less sides than 5 mg

 

There are some data I found : (approximatly)

For peak serum level at t+30min:

 

For hair count (Hair count: +Frontal / +Vertex)

PS1 : Not sure about +27 hairs on vertex area for topical minox

 

From paper :

Oral Minoxidil is potent vasodilator used to treat hypertension.

It is a pro-drug, activated by hepatic dehydroepiandosterone sulfotransferase (SULT2A1) to minoxidil sulfate.

Minoxidil Lotion is also a pro-drug converted in hair bulbs by thermostable phenol sulfotransferase SULT1A1 to minoxidil sulfate.

Low SULT1A1 predicts weak hair regrowth with both ML and OM.

Weak hair growth due to low follicular SULT1A1 can be overcome with Oral Minoxidil  through dose escalation, but cannot be overcome with Minoxidil Lotion due to low solubility and saturation absorption kinetics.

As sublingual dosing bypasses hepatic first-pass metabolism, Sublingual Minoxidil would be anticipated to increase follicular minoxidil sulfate bioavailability and consequently hair growth.

As hepatic sulfation of minoxidil enhances the haemodynamic effect, Sublingual Minoxidil would also be anticipated to reduce haemodynamic side effects and consequently improve safety.

 

Sources:

Treatment of male and female pattern hair loss with sublingual minoxidil: a retrospective case-series of 64 patients

Sublingual minoxidil for the treatment of male and female pattern hair loss: a randomized, double-blind, placebo-controlled, phase 1B clinical trial

https://www.anzctr.org.au/Trial/Registration/TrialReview.aspx?id=374567

Clinical efficacy and safety of low-dose oral minoxidil versus topical solution in the improvement of androgenetic alopecia: A randomized controlled trial

Edited June 25 by arthurSam

[Approach]

3 hours ago, arthurSam said:

Hello,

Thanks you for your answers.

I've done some research on sublingual minoxidil and I found very interesting things :

• Equivalent for efficacy of 5mg oral minox is about 1,5 -2 mg sublingual with a high reduction in serum level (more than 80%) and so also in sides.
• 4mg sublingual is 2,5x better in efficacy than 5mg minox, with about same serum level than 2.5mg oral and so less sides than 5 mg

 

There are some data I found : (approximatly)

For peak serum level at t+30min:

 

For hair count (Hair count: +Frontal / +Vertex)

PS1 : Not sure about +27 hairs on vertex area for topical minox

 

From paper :

Oral Minoxidil is potent vasodilator used to treat hypertension.

It is a pro-drug, activated by hepatic dehydroepiandosterone sulfotransferase (SULT2A1) to minoxidil sulfate.

Minoxidil Lotion is also a pro-drug converted in hair bulbs by thermostable phenol sulfotransferase SULT1A1 to minoxidil sulfate.

Low SULT1A1 predicts weak hair regrowth with both ML and OM.

Weak hair growth due to low follicular SULT1A1 can be overcome with Oral Minoxidil  through dose escalation, but cannot be overcome with Minoxidil Lotion due to low solubility and saturation absorption kinetics.

As sublingual dosing bypasses hepatic first-pass metabolism, Sublingual Minoxidil would be anticipated to increase follicular minoxidil sulfate bioavailability and consequently hair growth.

As hepatic sulfation of minoxidil enhances the haemodynamic effect, Sublingual Minoxidil would also be anticipated to reduce haemodynamic side effects and consequently improve safety.

 

Sources:

Treatment of male and female pattern hair loss with sublingual minoxidil: a retrospective case-series of 64 patients

Sublingual minoxidil for the treatment of male and female pattern hair loss: a randomized, double-blind, placebo-controlled, phase 1B clinical trial

Clinical efficacy and safety of low-dose oral minoxidil versus topical solution in the improvement of androgenetic alopecia: A randomized controlled trial

Thank you for your research!