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Minoxidil: Revived hopes for balding people

Posted on2021-05-03 by
Love0

What is Minoxidil? How did it appear on the baldness market? What is the mechanism of its action and effect on hair growth? You will find answers to these and many other questions on this page of the site.

History of the invention of minoxidil

For many years, Minoxidil has remained the only medicine with confidence by doctors as a hair regrowth remedy. The honor of discovering Minoxidil belongs to the American physician Alfred Kligman, who in 1982 discovered its stimulating effect on hair growth. Currently, the most famous (and most expensive) versions of the drug using Minoxidil are manufactured by Pfizer. It was she who, as a result of numerous mergers and acquisitions, inherited the invention of Pharmacy and Upjohn. So that you can imagine the seriousness of the scientific potential inherent in this drug, we would like to inform you that at one time Pharmacy and Upjohn was one of the largest companies in the world (like Pfizer today). In terms of production, Pharmacy and Upjohn was one of the 5 largest pharmaceutical companies in Europe and among the 15 largest pharmaceutical companies in the world.

In Europe, Minoxidil is distributed by Pfizer under the brand name Regaine, in the United States and some other countries - under the brand name Rogaine. The Rogaine company ranks as one of its most significant achievements. Its effectiveness in the fight against baldness contributed to the increased promotion of the drug in the US market, and then in Europe and many countries of the world.

The history of the emergence of drugs based on minoxidil is very interesting. Here's how Rogaine came into being.

Rogaine - one of the first drugs based on minoxidil

Rogaine is one of the first drugs based on minoxidil

No patented baldness remedy has revived so many dying hopes, so many Rogaine (outside the US - Regaine) registered by Upjohn in 1996 Perhaps the reason for the consumer enthusiasm was that Rogaine became the first officially approved "hair growing agent" in the United States, after a long ban, that could be bought without a prescription and applied on its own. The fact is that just 5 years earlier, in 1990, the US Food and Drug Administration (Food and Drug Administration - FDA) banned the sale of such products, arguing that hair loss is a serious matter and requires treatment. It is clear to everyone that the word "treatment" includes a visit to a doctor, a medical examination and medications. No miraculous lotions! So the FDA directive limited the tasks of cosmetics and left them only to improve the appearance of the hair, protect it from adverse effects, visually increase the volume of the hairstyle, and so on.

It is difficult for a person to live without hope, and it is not so easy to take it away from him. People who are losing hair do not consider themselves sick, are reluctant to go to the doctor and are ready to try anything that can be bought without a prescription. Hope creates demand, and new cosmetics are on the market to stimulate growth, strengthen roots and restore the vitality of weakened hair. Promises to regain hair or at least stop hair loss are also heard from the side of alternative medicine, to which all hopeless ones turn.

Still, when it comes to combating baldness, the FDA recently it was adamant - only a medicine and only a prescription. And so, the situation began to change. The fact is that Rogaine clearly occupies an intermediate position between cosmetics and medicines - from the official point of view, it is a medicine, however, an over-the-counter dispensing, and from the point of view of consumers, it is no different from a cosmetic product. Indeed, you can prescribe Rogaine yourself and apply for as long as you like, since it has no side effects and is not toxic. Rogaine is colorless, odorless, absorbs quickly, so you can apply it to your hair right before you leave the house. It looks like a liquid lotion in pretty bottles, very easy to use.

Phases of hair growth and development.

Structural formula of minoxidil (2D model and 3D model)

And, nevertheless, under the brand name Rogaine the real medicine is hidden - Minoxidil - a powerful antihypertensive agent. When taken internally, Minoxidil is not as harmless as when used externally. In any case, cardiologists, knowing about the side effects of Minoxidil, use it only in cases of severe hypertension, when all other drugs are powerless. When taking Minoxidil by mouth, swelling, tachycardia, headache, congestive circulatory failure, myocardial infarction and ... increased hair growth throughout the body (hypertrichosis) may occur.

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The pathogenesis of hemodynamic disturbances when taking Minoxidil inside was not a problem. Everything was clear here - both the reasons and the mechanism. Hypertrichosis made scientists think about it. The result of this thought was the idea to try Minoxidil topically and use it to treat hair loss. The idea turned out to be successful, since when applied topically, all the side effects of Minoxidil disappeared, and the effect on hair growth, on the contrary, became more pronounced.

Tailless macaques, which are a good model of human androgenic alopecia, were the first to try the new drug. On such a model, the results can be assessed using a biopsy and without any subjectivity on the part of the subjects. Microscopic analysis of hair follicles showed that under the influence of 2% and 5% solutions of Minoxidil:

  1. vellus hair follicles are enlarged to the state of medium or even terminal follicles (effect of enhancing hair growth);
  2. the growth phase of terminal follicles is prolonged (slowing down baldness).

The most sensitive to Minoxidil were juvenile macaques in the early stages of baldness, and hair regrowth was worst in older macaques with long-standing baldness. Cancellation of the drug caused a fairly rapid degradation of the follicles. When the treatment was resumed, follicular growth began again. Additional in vitro studies have shown that the growth of follicles under the influence of Minoxidil is accompanied by an increase in DNA synthesis, which indicates a direct effect of Minoxidil on proliferation processes. I must say that none of the previously existing baldness remedies directly affected the follicles. Even antiandrogens such as finasteride (Propecia) were more likely to stop baldness by protecting the hair follicles from the effects of DHT than to stimulate new hair.

The results obtained on monkeys were very encouraging for the researchers. Since the end of the 80s, a wave of clinical trials of a new drug begins, which are carried out in many countries of the world (in the USA, Europe, China and Australia, etc.). The bulk of the research is carried out by scientists from the Upjohn Company, which has the honor of creating the drug Rogaine. Clinical trials with minoxidil have yielded almost the same results as those in monkeys.

The large number of clinical trials of Minoxidil led to some conclusions.

  1. Minoxidil can be used to restore hair growth in androgenic and alopecia areata.
  2. Treatment with Minoxidil gives first results after four months and stabilization of hair growth after 12 months.
  3. Hair growth is maintained as long as the patient is using Minoxidil. When Minoxidil is canceled baldness starts again.
  4. Early stages of baldness are better treated than long-lasting smooth baldness.
  5. Minoxidil applied topically is safe and does not cause systemic effects even with prolonged use. Skin reactions such as dry skin and irritation are rare and resolve quickly.

So, almost 10 years of clinical trials have confirmed the efficacy of Minoxidil. However, the mechanism of action of Minoxidil is still not fully understood.

The first hypotheses linked the effect of Minoxidil on hair with its vasodilating effect. It was assumed that the increase in hair growth is caused by the expansion of blood vessels that feed the hair root. However, this effect, although undoubtedly significant, could not explain the full range of effects of minoxidil on hair. Then scientists tried to find a connection between the mechanism of vasodilation and hair growth. And such a connection was found. It turned out that both vascular tone and the change in hair growth phases are controlled by potassium channels. The potassium channel is a protein that is responsible for the transport of K + ions across the cell membrane. A change in the flux of potassium ions changes the membrane potential (charge), which leads to a change in the flux of other ions, in particular, calcium. In the vessels, a change in the concentration of intracellular calcium serves as a signal for the synthesis of nitric oxide, an endogenous vasodilator. Minoxidil opens potassium channels, activating the flow of potassium and calcium into the cell, followed by the release of nitric oxide, the appearance of which causes vasodilation.

Thus, Minoxidil causes an increase in the concentration of nitric oxide similar to the famous Viagra. By the way, even before the appearance of Viagra, applications of Minoxidil were used to treat impotence, and there were much fewer side effects.

To date, there is a lot of experimental evidence that the activation of potassium channels causes an extension of the phase of hair growth. It is not yet clear whether NO is involved in this process or other mechanisms are at work here. One thing is certain - agents that can change the permeability of the cell membrane for potassium ions will also affect hair growth. The proof is that the analogs of Minoxidil, the hypotensive effect of which is based on the activation of potassium channels, are pinacidil, diazoxide, cromakalim, nicorandil - also cause prolongation of the growth phase of the hair follicle.

The cyclical nature of hair growth is both a cause of baldness and a source of hope for balding people. Each follicle can be in three different phases of the life cycle: anagen, catagen, and telogen. Anagen is the time when the hair follicle produces hair. In the anagen stage, which lasts for several years, 85% of the hair follicles are usually found. Catagen is the time of follicle degradation. Hair growth stops and the hair root takes on the characteristic bulb shape. This phase lasts several weeks. In the telogen, the hair is detached from the root and slowly moves towards the surface of the skin.

The telogen stage is about 15% of the hair. It is this hair that is combed out with a comb and gets stuck in the gutter when shampooing. Normal hair loss is 70-80 hairs per day. With androgenic alopecia, the duration of the growth phase is shortened. The follicles do not reach their maximum size and therefore begin to produce thin and weak hair. The shortening of the growth phase leads to the fact that the percentage of hairs in this stage decreases, and the number of follicles in the telogen phase increases. Microscopic examination reveals miniaturized, atrophic follicles that are characteristic of androgenetic alopecia.

Minoxidil, which lengthens the hair growth phase, allows the follicle to enlarge enough to begin producing normal hair. Since it takes time for a significant number of hairs to be in the growth phase, the effect of Minoxidil is noticeable only months after the start of using the drug. After 12 months, the number of hairs entering the growth phase no longer increases, and the effect is stabilized. Cancellation of Minoxidil turns off the mechanism that activates potassium channels. This is similar to the effect of a window that suddenly slams shut in a poorly ventilated room. Deprived of the potassium flow, the cells of the hair follicle are again exposed to all those factors that caused the reduction of the hair growth phase. As a result, baldness resumes.

No medicine can promise 100% healing, and Minoxidil is no exception. He helps someone, but not to someone. At times, Minoxidil causes a light cannon to appear on bald areas instead of cosmetically acceptable hair growth. It helps women better than men, and balding people better than completely bald ones. And yet, if we are talking about female androgenic alopecia, which is accompanied by thinning and thinning of the hair, or about the initial stages of male androgenic alopecia, which began with thinning hair at the crown, it is worth trying, since the chances of success are very high.

Learn More About Minoxidil

In the beginning, the drug was dispensed only by prescription. In February 1996, FDA - U.S. The Food and Drug Administration in order to make the drug more affordable, allowed (only for American companies) the production of identical to Regaine generic versions of the drug. The word "generic" in medicine has the meaning of "clone", that is, a drug produced using a similar or exactly the same technology, from the same raw materials, but produced not under a trademark, but under the name of the active chemical principle.

With the passage of time, when the safety of Minoxidil has received large-scale statistically verified confirmation, 2% Minoxidil Solution has been dispensed without a doctor's prescription. Gradually, many well-known pharmaceutical companies in the world began to produce minoxidil under their own brands, or simply as generic minoxidil. Again, this is an exact copy of Regaine (Rogaine) in terms of its composition, manufacturing technology and, in some cases, even the components coming from the same manufacturer. Generic drugs are of the same quality, have the same therapeutic effect, but are cheaper, since it eliminates the costs associated with the use of brands. It should be remembered that the price of a "promoted" brand includes huge expenses for advertising and product promotion on the market.

Among the manufacturers of generic minoxidil, the most famous are such large pharmaceutical companies as Alpharma, Kirkland Signature (brand of Costco), Copley Pharmaceutical, TEVA Pharmaceutical, Pierre Phabre and others.

If you are already familiar with Rogaine or Regaine, you can now use cheaper generic versions of these drugs as there is no longer any need to pay for a brand name. Many preparations based on minoxidil are similar to Regaine not only in composition, but even in the form of packaging and principles of use.

References on minoxidil

  1. "Clinical Pharmacology" / Ed. Kukesa V.G., M .: Publishing house of the Moscow Medical Academy, 1991, P. 444.

  2. Uno H, Cappas A, Brigham P. "Action of topical minoxidil in the bald stump-tailed macaque". J Am Acad Dermatol 1987; 16(3 Pt 2): 657-668.

  3. Jacobs JP.Szpunar CA, Wamer ML. "Use of topical minoxidil therapy for androgenetic alopecia in women". Int J Dermatol 1993; 32(10): 758-762.

  4. Headington JT. "Hair follicle biology and topical minoxidil: possible mechanisms of action". Dermatologica 1987; 175 Suppl2:19-22.

  5. Orias M. [Blood pressure regulation by potassium channels]. [Article in Spanish]. Medicina (B Aires) 1998; 58(4): 429-432.

  6. Schultheiss D, Stief CG, Truss MC, Jonas U. [Pharmacological therapy in erectile dysfunction — current standards and new viewpoint]. [Article in German] Wien Med Wochenschr 1997; 147(4-5): 102-104.

  7. Buhl AE, Waldon DJ, Conrad SJ, Mulholland MJ, Shull KL, Kubicek MF, Johnson GA, Brunden MN, Stefanski KJ, Stehle RG, et al. "Potassium channel conductance: a mechanism affecting hair growth both in vitro and in vivo". J Invest Dermatol 1992; 98(3):315-319.

  8. Callan AW, Montalto J. "Female androgenetic alopecia: an update". Australas J Dermatol 1995; 36(2): 51-57.

  9. Savin RC, Atton AV "Minoxidil: Update on its clinical role". Dermatol Clin 1993:11(1): 55-64.

Regaine® is a registered trademark of Pharmacia and Upjohn, Inc.
Rogaine® is a registered trademark of Pharmacia and Upjohn, Inc.

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