Oral Minoxidil in the treatment of androgenetic alopecia

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The use of oral minoxidil (tablet) is one of the great innovations of recent years in the treatment of androgenetic alopecia both male and female.

In this article we will try to understand the benefits and side effects of this therapy.

Minoxidil: History

In our blog we have talked several times about the Minoxidil (brand name Rogaine). It is one of two drugs approved by the FDA (Food and Drugs Administration) to treat male androgenetic alopecia. The other drug approved for this purpose is the Finasteride..

Perhaps not everyone knows that Minoxidil was originally approved in 1979 as an oral drug under the trade name of Loniten for the treatment of hypertension (high blood pressure). The dosage that was recommended to patients was 10-40 mg per day.

It was observed over the years that a proportion of patients using Loniten therapy had a side effect that led to a significant improvement in the caliber of their hair. This side effect was studied at length with the goal of using the drug to improve hair density in patients suffering from androgenetic alopecia.

It was not until 1988 that Topical Minoxidil (lotion) was approved as a treatment for male pattern baldness while a version for women was approved in 1991.

Most men use Minoxidil 5% in a lotion or foam form applying 2 times a day. Those who experience side effects from the use of Minoxidil often reduce the application to once a day. Women tend to use a 2% topical formulation to promote regrowth of miniaturized hair.

As with the rest of the therapies for androgenetic alopecia, Minoxidil will produce effects for as long as it continues to be used, so it is a treatment that must be maintained over the long term.

Minoxidil: Mechanism of Action

The mechanism by which Minoxidil improves hair density and promotes the regrowth of new hair is still not entirely clear and there are many theories about it although some have received greater approval from the scientific community, among them we mention:

  • The increase generated by the use of Minoxidil of a substance stimulating hair regrowth called prostaglandin E2 (PGE2)
  • The fact that Minoxidil induces a prolongation of the anagen growth phase and a shortening of the telogen fall phase of the hair follicles
  • The vasodilating action of Minoxidil that allows to improve the blood supply to the follicles
  • The opening effect of the potassium channels

Oral Minoxidil: What dosage to take?

One of the problems encountered with topical Minoxidil is that it is often difficult to be consistent with the treatment because the application of the lotion is not very easy and often the hair is dirty or greasy after use. Other problems that are often encountered with the Minoxidil lotion refer to irritations of the scalp and dermatitis.

With the aim of improving therapeutic adherence since 2015 some doctors, including in particular it should be mentioned the Australian doctor Rodney Sinclair have begun to suggest to patients the use of minoxidil in oral form at doses obviously lower than those used for the treatment of arterial hypertension, with the aim of improving the trichological situation of the patient especially in terms of density and caliber of the hair but without compromising the arterial pressure.

Minoxidil in oral form is much more convenient for the patient as it is easier to take a tablet than to apply a lotion twice a day.

The posology of oral minoxidil for the treatment of alopecia depends on multiple factors, among which it is worth mentioning:

  • Sex of the patient
  • Type and degree of alopecia
  • Concurrent intake of other treatments for alopecia
  • Individual patient characteristics

It is therefore important to be followed by a dermatologist specialized in trichology who can recommend the best dosage of intake. Usually doses between 0.25-2mg per day in women and between 2.5-5mg per day in men are used. The effectiveness is greater as the dose increases but obviously the risk of incurring side effects is also increased.

Oral minoxidil: does it work?

The positive effects of therapy with oral Minoxidil begin to be observed from6 months of treatment and are maximized around one year of use.

In the first 3-4 months in 20-30% of patients you may experience an “induced fall” or shedding or an increase in hair loss. This is completely normal and should not be a cause for concern.

This increase in shedding occurs because one of the mechanisms of action of Minoxidil is replacing follicles in the telogen phase (thin and weak) with hair in the anagen phase (larger and healthier looking).

There are numerous studies that have demonstrated the effectiveness of oral Minoxidil even at low dosage in the treatment of androgenetic alopecia.

A study from 2019 showed that all male patients who were given Oral Minoxidil in doses between 2.5 and 5 mg had a noteworthy improvement and that for as many as 37.5% of them the improvement was particularly significant.

A study from 2020 showed that even very low doses of oral Minoxidil (1.25 mg of Loniten taken every night) could produce significant results in terms of hair regrowth and thickening as early as 3 months of use.

27-year-old female patient, improvement achieved with 1 mg of oral minoxidil for 6 months.
33-year-old woman improvement achieved with 1 mg oral minoxidil for 12 months
28-year-old man, improvement achieved after only 3 months of taking 5 mg of Minoxidil.

Oral minoxidil: mode of intake.

The use of Oral Minoxidil is currently “off label” meaning it is not approved for the treatment of baldness. This means that there is no medication with the correct dosage for the treatment of alopecia. You can find a version of Oral Minoxidil for the treatment of hypertension marketed as Loniten. in pharmacies.

These are 10 mg tablets that you will have to break into 2 or 4 fragments to get the 5 mg or 2.5 mg doses.

However, it is possible to have capsules with the correct dose of oral Minoxidil prepared in the pharmacy. It is obviously recommended to go to a pharmacy with proven experience in galenic and magistral preparation.

It is recommended to take Minoxidil Oral before going to bed, it is not necessary to take it on a full stomach and has no particular interactions with other drugs. It can be taken together with other drugs for the treatment of baldness such as Finasteride or Dutasteride.

It is not recommended for use in pregnant women while it is allowed, given the low dosages used in women, its use during the lactation period.

Oral minoxidil: What are the side effects?

The most frequent side effect resulting from the use of oral Minoxidil is the increase of hair in some areas of the body (hypertrichosis). This side effect is dose-related and appears iin less than 10% of patients taking a dose of 0.5 mg per day.

Several very recent studies have demonstrated the effectiveness of oral Minoxidil low dose as well as its safety, we cite two that see involved among others two Italian doctors as the Dr. Tosti and the Dr. Piraccini.

Usually the hair increases mainly in the area of the sideburns and temples. Fortunately, the intensity of hypertrichosis is in most cases mild and it is rarely necessary for the patient to abandon treatment because of this problem.

The rest of the side effects are very infrequent (less than 5% of users) and if they do occur they are reversible simply by reducing the dose of the drug.

These are mainly:

  • Bloating of legs and eyelids: is due to fluid retention caused by the vasodilator effect of oral Minoxidil. Many times this effect disappears without the need to reduce the dosage.
  • Decrease in blood pressure: Oral minoxidil, at the dosage used for the treatment of alopecia, does not usually cause a decrease in blood pressure. There are, however, patients with a higher sensitivity to the drug who may in some cases notice symptoms such as dizziness or palpitations during the initial intake of the drug. These side effects can be easily avoided by reducing the dose of oral Minoxidil.
  • Headsickness: Side effect also common to topical lotion, is believed to be due to the vasodilating action of Minoxidil.

Oral Minoxidil what happens in case of discontinuation of treatment

As with the rest of the treatments for alopecia the oral minoxidil is not a cure for baldness and thereforeits benefits will be maintained always and when the patient continues to use it over time.

The fact that the treatment must be used continuously does not mean that it must be taken every day.

In fact, many patients achieve stabilization by taking only 2-3 tablets of Minoxidil per week.

If you stop the treatment after using it for more than 2 months, the hair that has improved in size will return to the condition it was in before taking oral Minoxidil..

Fortunately, there is no risk that suspension of oral Minoxidil will plunge us into a worse situation than we were in before we started taking it, this is a false myth.

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