Is Sublingual Minoxidil the game-changer we were waiting for?


Oral Finasteride & Topical Minoxidil that allow the battle against hair loss to be fought simultaneously on 2 fronts, are the established, scientifically proven, uncontested, present day Gold Standard for medical treatment of androgenic alopecia.

Though the widely accepted Gold standard, this combination has never been the popular flavour of the month. To rational, intelligent minds medical consensus carries more weight than the endless speculations, constant ramblings, and misplaced opinion of trolls & cyber-stalkers without medical credentials on various hair loss forums

“Since when have facts come in the way of business interests?”- you may interject!

Companies will continue to reinvent the wheel, put old wine in new bottles for profit. Vested interests in this billion dollar hair loss treatment industry will continue to confuse, confound and slander cheap and effective cures for baldness.

A drug that works through oral route is being denigrated in favour of topical form, a drug that works and is USFDA approved for use in topical form is being castigated and it’s oral form which even though toxic is being eulogised and being universally promoted.

Can anyone figure out what’s happening?

Aren’t we relentlessly flogging a dead horse in an attempt to perfect something that is old, something that was scientifically dismissed a long time before?

There are simpler solutions that need to be perfected. Just a simple example is the 5 strategies video which I published a few years back where I have explained how even microdoses of a drug like Finasteride can be optimally utilised to give the same benefits the full dose would. All in an effort to minimise side effects in those susceptible. The video on 5 Strategies for using Oral Finasteride.

On the flip side it isn’t a hidden fact any more that in hair loss research, that because of duress and miscellaneous compulsions companies and individual researchers have fallen into the trap of jumping onto the next big thing that promises profit. They are busy all the time since so many years. The ‘Hamster Wheel’ comes to mind. An activity that involves someone being busy all the time but never achieving anything important or reaching the end of a task. Effort going in vain due to needless not well thought of pursuits.

How can we reverse this mindset and get integrity back into medical research in hair loss.

It is easy to dismiss an old treatment on flimsy logic and calculations.

Drug companies will not allocate funds for clinical trials for something that will not bring in huge profits. Research into Oral Minoxidil will never make a company richer since it is an old drug.

Are we not aware that many things that we consume are killers at high doses but safe and efficacious at low doses?

Alcohol that most drink routinely, can kill you at high doses but we are unmindful and do enjoy it often.

All said, evidence is starting to build in favour of oral Minoxidil, a heretofore obscure treatment for hair loss, being a far better choice over the topical form when used in low dosage.

To summarise use of Minoxidil for hair loss, Minoxidil is an approved medication for severe hypertension since it is a potent vasodilator, and its side effect includes the salubrious effect it has on hair loss due to androgenetic alopecia.  Minoxidil is a pro-drug, activated by hepatic dehydroepiandrosterone sulfotransferase (SULT2A1) to minoxidil sulfate the active principle form. OM doses of 2.5 and 5 mg produced peak plasma concentrations of 16.8 and 37.2 ng/mL within 30 min post-dose. Side-effects include hypertrichosis, lower limb oedema, postural hypotension and tachycardia. Topical Minoxidil lotion is approved by USFDA for the treatment of hair loss. It is also a prodrug converted in hair bulbs by thermostable phenol sulfotransferase (SULT1A1) to minoxidil sulphate. There is a considerable inter subject variability in levels of both hepatic SULT2A1 and follicular SULT1A1. Low SULT1A1 predicts weak hair regrowth with both TM and OM. Weak hair growth due to low follicular SULT1A1 can be overcome with OM through dose escalation but cannot be overcome with TM due to low solubility and saturation absorption kinetics.

Low-dose 0.25 mg a day oral minoxidil has been proven to have virtue when treating FPHL in combination with spironolactone. On the other hand, oral minoxidil 2’5-5 mg daily has many votaries on forums and in the medical fraternity support is building up for use in MPB.

Sublingual minoxidil is the same as oral minoxidil. The only difference is the process of their going systemic. Sublingual versions of drugs in common use abound.- like Zofran, Ambien, Claritin, and a whole lot more. And the most well known being NTG.

Systemic minoxidil does seem to be better but has greater propensity for ill effects, howsoever low in incidence.

The side effects we read about happen at very high doses due to which initially this route was dismissed many years ago for treating hair loss.

So, a little about Minoxidil. It is a pre-drug that neds to be converted to its active form Minoxidil Sulphate by the enzyme Sulphotransferase. Whether we are deficient in this enzyme cannot be predicted without checking for SULT1A1 gene if we wish to know about conversion of topical Minoxidil and the SULT1A2 for the systemic version.

The best absorption happens when we take sublingual Minoxidil since it does not pass through our liver. Minoxidil gets round the first pass metabolism in the liver to get converted to the active form Minoxidil Sulphate in the hair follicle.

Why would anyone prefer oral to topical if there are more risks with the oral? Only if there are also more benefits.

Several renowned physicians have said that oral Minoxidil works better than topical for hair growth.
Dr Rodney Sinclair’s experience with sublingual form and that of Dr Pathamvonich with the oral form have been encouraging.

Oral and Sublingual Minoxidil are emerging as popular treatments for hair loss in low doses. It may soon prove to be a game changer. Also because this is a cheaper medicine the cost of which can be covered in medical benefits.

I have myself been using oral Minoxidil on my patients for some time now.

Why is this shift taking place. For 5 reasons:

1. Topical form does not work for everyone
2. Topical form gives most folks dry dandruff
3. Topical form cannot be used in skin disease like psoriasis, dermatitis
4. Non responders to Topical Minoxidil. For topical form to work you need to have the enzyme SULT1A1 in the scalp
5. Topical form is messy to apply and makes hair look dry, rough and unkempt

Low-dose oral minoxidil (OM) is fast becoming a mainstay in the therapeutic ladder for male and female pattern hair loss.

In my practice, I still recommend topical minoxidil as the first-line therapy given its well-established safety and efficacy profile. In non-responders, sulphotransferase activity can be increased in the scalp through judicious use of 0.1% Tretinoin which turns non-responders to responders.

I consider low-dose oral minoxidil 0.625mg, 1.25 mg, 2.5 mg and even 5 mg if there is a poor response after 6 to 9 months of diligent use of topical Minoxidil.

As minoxidil is a pro-drug, it needs to be activated through the enzyme sulfotransferase to the principle form minoxidil sulphate. This can happen either in the hair follicle or it can happen in the liver.

Sublingual Minoxidil, if Rodney Sinclair is to be believed, seems to have a better bioavailability and also fewer cardiovascular hemodynamic effects since it avoids the first-pass liver metabolism.

So, will sublingual minoxidil be a game changer?

Time will prove this!

Though Rodney Sinclair is making a good case for use of sublingual minoxidil and he has the patent for it, it needs to be seen if it will displace the much more affordable, generic oral minoxidil which is also covered by medical benefits.

However, the sample size is negligible and the study is not prospective and it was lacking a control group.

As of today it is unclear how the 2 will compete in the years to come.

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