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QUESTION OF THE WEEK


Switching from Topical to Oral Minoxidil - Is it Easy? How do we do it?

Switching from Topical to Oral Minoxidil has it’s Challenges

Topical minoxidil was FDA approved for treating male and female pattern hair loss several decades ago. Some astute clinicians and scientists realized in the 1970s that patients using oral minoxidil for treating high blood pressure grew more hair on the scalp (and more hair the body) - and this led to the development of topical minoxidil. Oral minoxidil slowly disappeared from mainstay treatments for blood pressure as better and better blood pressure treatments emerged in the market. Topical minoxidil became increasingly popular for hair loss.

About 10-15 years ago, pioneers like Dr Rod SInclair in Australia followed by others like Dr. Pathomvanich in Thailand started exploring the use of oral minoxidil to treat hair loss. Over the past 5 years, oral minoxidil has become increasingly popular and now has found itself as a mainstay treatment option for hair loss.

The benefit of oral minoxidil over topical minoxidil is several fold. First, the patient uses a pill and does not need to use something that potentially affects how the hair looks day to day. Some people find using oral medications easier than lotion. In addition, oral minoxidil does not need to be converted by the skin into minoxidil sulphate. It bypasses this critical step. This is why several people who don’t respond to topical minoxidil end up responding to oral minoxidil.

The down side of using oral minoxidil is that almost every cell in body sees it - it circulates in the blood stream. We don’t really need the pancreas, liver or heart to see oral minoxidil floating through the blood steam - but these organs do see it. Fortunately, the effects are minimal in most cases at the low doses we use.

Side Effects of Oral Minoxidil

There are more and more people using oral minoxidil for treating hair loss. I don’t think there is yet a full respect for the side effects of this drug and we’re still in what I call the prescribing excitement phase (PEP). Every new treatment for hair loss experiences this PEP. We see it with low dose naltrexone for treating some hair conditions (until physicians start realizing it can sometimes interfere with sleep and affect the thyroid function in those using thyroid medications) and we of course saw it with finasteride in the 1990s for treating male balding (until people started to wonder about long term effects) and we saw it with pioglitazone for treating LPP (until people started to realize it may not be a long term option due to bladder cancer risk). All new treatments come with a PEP.

And so we are in the excitement phase of using oral minoxidil.

Side effects of oral minoxdil depend on dose. In North America, the little minoxidil pills come in 2.5 mg strengths. In other parts of the world, they may come in 10 mg strengths. Some physicians prescribe a full 2.5 mg pill to start, some 1/2 pill (or 1.25 mg), some 1/4 pill (or 0.625 mg). Some don’t prescribe any bit of a pill and have a local compounding pharmacy make up special 0.25 mg pills.

Men tolerate higher doses than women.

Potential side effects include heartaches, dizziness, hair on the face, hair on the body, palpitations, fluid retention in the feet, fluid retention in the face, hives, and hair shedding. Of course, these are “potential” side effects - not the side effects that everyone gets. In addition, women can not use oral minoxidil or topical minoxidil if they are trying to become pregnant. Oral minoxidil can have devastating effects on a fetus.

My personal view is that oral minoxidil is fairly well tolerated at very low doses, but does not work as well at very low doses. Some women do respond to doses of 0.25 mg to 0.625 mg so it’s worth starting there for many patients. One small study suggested that for women, 1.25 mg was about equivalent to 5 % minoxidil lotion. Individuals using the 5 % lotion experienced more scalp itching, but those using the 1.25 mg pill experienced more hair on the face.

The tricky thing about using oral minoxidil is that some side effects develop quickly and some develop very slowly (more like …. S L O W L Y). If a patient is going to get dizzy on a certain dose or oral minoxidil, we’ll know in a week or two and maybe even sooner if they get dizzy. If they are going to get hair on the face or swelling in the feet or face, we won’t know for 3-5 months.

I see many female patients referred to me on 2.5 mg doses. These doses are often well tolerated in men but not as well tolerated in women. Of course, some women do tolerate these higher doses yes. Many female patents on 2.5 mg doses referred to me actually experience swelling in the feet or face. Some don’t know it. Some have had 3-5 pound (to 8 pound plus) weight gain that they did not know was from the minoxidil induced fluid retention. They thought it was from their diet or lack of exercise. In many cases - it’s from the minoxidil. Some female users of oral minoxidil are battling hair growth on the face. Many absolutely love the results for the hair but are troubled by what to do about the other side effects.

The answer, in my opinion, is to go slow on oral minoxidil dosing - especially for female patients.

There is nothing wrong with starting 0.25 mg or 0.625 mg (1/4 pill) and seeing how patients do over 3-6 months and then going up to 1/2 pill (1.25 mg). 1/2 pill is very helpful for many female patients. After that we might go up (after much discussion) to 1/2 pill alternating with 3/4 pill or 1/2 pill Monday to Friday and 3/4 pill on the weekends. Or…. we might not go up at all! Or…. we might go back down to 1/2 pill alternating with 1/4 pill.

The dose of oral minoxidil that we might start with depends on the health of the patient, and whether they are using any other blood pressure medications (including spironolactone in women), and whether they plan to use or overlap topical minoxidil).

We need to be aware that the dose we choose is ideally going to be the dose they stay on for life. If I prescribe 1.25 mg of minoxidil to any patient, male or female, I need to ask myself. Are they likely to tolerate this dose in 10 years? What about 20 years?

Switching from Topical to Oral Minoxidil

It’s really important to understand that switching from topical to oral minoxidil is not as easy as some think. If the topical minoxidil was not working at all and truly was useless, then it’s easy to switch. One simply needs to stop the topical minoxidil and start the oral minoxidil. . However, if the topical minoxidil was actually helping the hair and the patient wanted to switch because they did not like using it or had a reaction or wanted more improvement - then the switch becomes a bit more difficult.

Consider the 43 year old female on topical minoxidil who wants to switch. She thinks it was helping but hates the way topical minoxidil affected the hair. She is advised to stop topical minoxidil by her doctor and starts 0.625 mg of oral minoxidil. One month later she is experiencing lots of hair shedding. Her doctor advises her that shedding is common when minoxidil is started and so she continues. 3 months later she is back in the doctor’s office with concerns about shedding.

Why?

Well, the answer could be due to many reasons actually. But in this case the answer was simple - the scalp loved the 5 % topical minoxidil and when a switch was made to 0.625 mg the scalp was unhappy. It felt it was robbed of proper minoxidil amounts. It felt underdosed with minoxidil - and so shedding happened.

Let’s continue this example.

The patient has now increased from 0.625 mg (1/4 pill) to 1/2 pill on the advice of the doctor.. Shedding eventually stopped but she unfortunately she developed some hair on the face that she did not like. She had already spent $ 5800 in the past on laser hair removal and did not want to spend any more money on laser hair removal.

So what do we do?

Well, this is tricky. We can go back to topical minoxdil. We can go down to 0.625 mg alternating with 1.25 mg in hopes the hair growth stays okay. We can even go back on a bit of topical minoxidil (three times weekly) with a bit of oral minoxidil (0.625 mg daily). There are many options here.

Switching from Topical To Oral Minoxidil

Everyone who plans to switch from topical to oral minoxidil needs to have the situation reviewed on a case by case basis. Unfortunately, there is no formula or protocol that works with everyone.

I often continue topical minoxidil if possible and start low doses of oral minoxidil. After 3-5 months, I increase the oral minoxidil further with the hope that by month 6-9, I’ll be able to remove the topical minoxidil if that was the desired plan. Side effects are carefully monitored at each step.

So, can we use both oral and topical minoxidil overlapping like this? In a properly monitored patient - yes. A 2018 study by Tanaka and colleagues studied over 18,000 males receiving both topical 5 % minoxidil twice daily as well as 2.5 mg of oral minoxidil (along with other treatments). Side effects of the combination therapy were low. For example, swelling and dizziness were reported in 2 out of every 1000 patients.  

Conclusion and Summary

We are in the prescribing excitement phase of oral minoxidil. It’s being used around the world more and more often. Simply starting a 2.5 mg pill is not a reasonable option for all patients - especially female patients. Women tolerate lower doses than men. Some side effects are very delayed like hair on the and swelling in the feet, body or face. One needs to wait 3-4 months to get a good sense of how any dose truly affects the body. We do not start oral minoxidil on a Monday September 1 and phone the patient on Tuesday September 2 and ask “do you have swelling in your feet?” That side effects might not be fully realized until mid to late December. We might phone the patient on September 15 and ask do you have headaches or dizziness or any funny feelings. Those side effects appear early.

We need to be aware of the early and late side effects of oral minoxidil.

Switching from topical to oral minoxidil sure sounds easy. It sounds like all that one needs to do is to stop the topical minoxidil and start eating a pill. It’s not so simple. Sometimes it is simple of course and some patients do get it right and find the transition quite easy. Not everyone.

Starting slowly and staring low doses must be considered on a case by case basis and overlapping topical and oral minoxiil must also be factored into a long term treatment plan.

Reference

Tanaka Y, Aso T, Ono J, Hosoi R, Kaneko T. Androgenetic Alopecia Treatment in Asian Men. J Clin Aesthet Dermatol 2018;11:32-5.

Ramos PM et al. Minoxidil 1 mg oral versus minoxidil 5% topical solution for the treatment of female-pattern hair loss: A randomized clinical trial. .J Am Acad Dermatol. 2020 Jan;82(1):252-253. doi: 10.1016/j.jaad.201


This article was written by Dr. Jeff Donovan, a Canadian and US board certified dermatologist specializing exclusively in hair loss.



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