Ketoconazole shampoo is used topically to treat hair loss.
In this article, you’ll understand:
- the science behind ketoconazole;
- how your hormones impact the health of your hair;
- how ketoconazole shampoo can regrow your hair;
- and how it stands up to other hair loss treatments.
Ready to learn how ketoconazole shampoo can be your solution to getting healthy hair again? Just keep reading.
Quickly, make sure you take the free hair quiz later in this article.
What Is Ketoconazole?
Ketoconazole is an FDA-approved drug used to treat fungal infections. It also lowers testosterone as a side effect (1).
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Because of its mechanism of action, ketoconazole has recently been formulated to be used topically.
How Does Ketoconazole Work?
Before we get into exactly what ketoconazole does in the body, it’s important to understand how testosterone is made in the body. This is a complex process involving a ton of systems.
Sex Hormone Synthesis
Sex hormones like testosterone follow a specific biosynthesis, or creation pathway, in the body.
It starts like this: cholesterol is synthesized by the liver or obtained through diet. Then, it is absorbed into the bloodstream and transported to sites of sex hormone synthesis (e.g. cells in different tissue that contain the enzymes needed to create sex hormones).
These enzymes are called cytochrome P-450 enzymes (CYP-450).
There are many different kinds of CYP-450 enzymes and are involved in everything from vitamin D metabolism, detoxification, and drug metabolism. They can be found in both the mitochondria or endoplasmic reticulum (4).
In sex hormone biosynthesis, cholesterol is transported through the cell membrane, into the fluid of the cell, and then to mitochondria. Here, cholesterol interacts with a CYP-450 enzyme called CYP-17A1 and is converted to pregnenolone, the precursor to all sex hormones of the body (2).
After that, pregnenolone is transported to the endoplasmic reticulum, where it is converted by another CYP-450 enzyme into a hormone called DHEA.
Ketoconazole, Anti-Fungal Activity, and Testosterone
So, how are ketoconazole, sex hormone biosynthesis, and testosterone related?
Let’s break it down:
So, like we mentioned earlier, cholesterol is converted to pregnenolone by the CYP-17A1 enzyme. This is key in the production of androgens.
Well, ketoconazole downregulates CYP-17A1 enzymes, disrupting the production of androgens, and inherently lowering circulating testosterone.
It doesn’t interact with aromatase enzymes, meaning that testosterone is lowered but the activity of aromatase isn’t impacted.
Ketoconazole and Liver Injury
Another notable effect of oral ketoconazole is its inhibition of another CYP-450 enzyme called CYP-4A3, the main anti-fungal mechanism. It also does the same thing in humans.
This can be problematic considering this enzyme also helps detoxify foreign compounds and drugs in liver cells. When not detoxified, foreign compounds and drugs can damage liver cells, causing liver injury (6, 9).
For this reason, oral ketoconazole is no longer frequently prescribed for fungal infections.
Although oral ketoconazole isn’t regarded as safe, topical ketoconazole can be used safely and effectively (10).
This can be in the form of creams, gels, or even shampoos!
Ketoconazole and Hair Loss by Fungi
Trichomycosis, a fungal infection of the scalp, is a common cause of hair loss. It’s characterized by bald patches, inflammation, itching, and dry skin.
But, how do these tiny microscopic spores cause hair loss?
As fungi come in contact with the scalp, they can infiltrate the hair shaft and move into the follicle and surrounding skin. While some species don’t always incite the immune system, some do.
It’s important to recognize and get treatment for trichomycoses before they do too much damage, as hair loss can be permanent.
Ketoconazole shampoo can effectively treat trichomycoses, as it is an anti-fungal. In the case of trichomycoses, it acts as a hair loss prevention tool by killing fungi that can cause hair loss.
This means ketoconazole shampoo can help you achieve healthy, full hair again.
Ketoconazole and Hair Loss from Androgenetic Alopecia
Androgenetic alopecia is the result of high DHT levels in the scalp. As these levels increase, sebum output and scalp tension also increase (17).
Excess Sebum and Androgenetic Alopecia
Excess sebum on the scalp can be more than just an oily scalp. In fact, it’s a characteristic of androgenetic alopecia that may even contribute to hair loss (17).
Excess sebum on the scalp is food for bacteria like P. acnes on the scalp. As these bacteria consume more sebum, they multiply, secrete inflammatory substances, and can stimulate inflammation.
This can lead to scarring around the hair follicle, called perifollicular fibrosis, which can restrict the growth space of the follicle. As a result of this follicle miniaturization, hairs shrink and can cause baldness.
Scalp Tension and Androgenetic Alopecia
Scalp tension can cause and result from high androgen levels.
Confusing, I know. This catch-22 situation is complex and something that even the most well-versed scientists don’t fully understand.
But, here’s what we do know:
Androgens like testosterone and DHT are potent promoters of muscle growth. High DHT levels on the scalp may result in an overgrowth of the scalp muscle, leading to tension (17).
You know that feeling when you’re working out and your muscles are super sore? Well, that’s inflammation and the same exact thing happens when your scalp is under chronic tension.
This continual inflammation can stimulate scarring, just like excess sebum can, and contribute to perifollicular scarring.
Scalp tension coupled with inflammation also increases levels of a compound called TGF-β1. This substance can calcify blood vessels, reducing blood flow.
Proper blood flow is crucial for nutrient delivery to hair follicles. Without it, hair cannot receive the essential precursors it needs to grow. TGF-β1 also further contributes to scarring around the hair follicle.
Further exacerbating this whole issue is the hypothesis that scalp tension and inflammation also increase androgen production on the scalp. The androgen-mediated scalp tension is a vicious cycle that can frustrate hair loss sufferers.
How Ketoconazole Can Benefit Androgenetic Alopecia
Some of the factors in the development of androgenetic alopecia may be improved by ketoconazole shampoo.
Topical ketoconazole has demonstrated anti-inflammatory activity, which may be due to antibacterial properties (18).
If the main mechanism of ketoconazole’s anti-inflammatory action is truly through its ability to kill bacteria, it could, in theory, prevent hair loss. Considering one of the factors in androgenetic alopecia is excess sebum and the increased activity of P. acnes, the antibacterial action of ketoconazole could prevent inflammation associated with P. acnes overgrowth (18).
This means less inflammation and a healthier scalp!
Additionally, the testosterone-lowering properties of ketoconazole that we talked about earlier could prevent hair loss associated with androgenetic alopecia.
While the exact mechanism of this isn’t known, scientists seemed to have pinned some of ketoconazole shampoo’s efficacy down to its anti-androgenetic activity.
Other studies show evidence to support that ketoconazole can disrupt local testosterone to DHT conversion. By intervening in this process, a ketoconazole shampoo can boost the health of your hair, preventing powerful DHT from causing hair loss (19, 20).
However, this is complicated by the fact that ketoconazole seems to be effective even on androgen-insensitive hairs. This signals that ketoconazole may exert protective action against hair loss outside of factors related to androgens (16).
Although the exact mechanism of action is not fully known yet, ketoconazole shampoo has proven to significantly increase hair growth in androgenetic alopecia sufferers, both alone and in conjunction with other therapies. However, it has not been shown to increase the number of hair follicles that grow hair.
Ketoconazole Shampoo for Women
Ketoconazole in a shampoo equals lowered DHT, which means improved hair loss. Simple, right?
Well, not quite.
While high androgen levels are quite often seen in women with pattern hair loss, this isn’t always the case. If you suffer from pattern hair loss that isn’t a result of high DHT levels, ketoconazole might not work for you (23).
However, studies on ketoconazole shampoo demonstrate that it is effective at promoting hair growth in androgen-insensitive tissues (16).
So, will ketoconazole shampoo work for women? It’s hard to tell, as the scientific body of literature has limited studies on the efficacy of ketoconazole shampoo in women.
Before trying ketoconazole shampoo as a woman, it’s a good idea to have your androgen levels tested and discuss with your doctor.
How Ketoconazole Shampoo Stands Up to Other Hair Loss Treatments
To know if ketoconazole shampoo is for you, you have to compare it to some of the other options on the market. But, keep in mind that it doesn’t always have to be one or the other.
With your doctor’s approval, some of these treatments can be used in conjunction with topical ketoconazole.
Minoxidil, also known as Rogaine, is a widely used topical hair loss treatment. It relaxes the muscles of the scalp, reducing chronic scalp tension that can lead to hair loss (16).
However, in comparative studies minoxidil proves to be more effective than ketoconazole shampoo. This may be because minoxidil relieves more scalp tension compared to a ketoconazole shampoo.
Botulinum toxin is a poisonous, neurotoxic substance. It’s the main ingredient in Botox.
When injected into the scalp, it relaxes the muscles, allowing blood flow and oxygen into the hair follicles. In the presence of oxygen, more testosterone is aromatized into estrogen rather than DHT, meaning it can theoretically prevent androgenetic alopecia (21).
In one pilot study, the number of hair follicles in androgenetic alopecia scalps increased by 18 percent on average. While ketoconazole shampoo promotes hair thickness and density, it doesn’t demonstrate an ability to increase the number of hair follicles (13, 16).
The verdict? For treating hair loss and achieving healthier hair, botulinum toxin seems to win this one.
Scalp Tension Relief
There are various ways to relieve scalp tension.
Mechanical scalp tension relief can be achieved in the form of scalp massage or devices that relieve scalp tension. These are designed to restore blood flow to the scalp, reduce DHT production, and lower inflammation — all factors that cause hair loss.
The benefit of mechanical scalp tension relief is that it’s not super costly, unlike shampoos which require consistent purchase.
Best of all, it can be paired with any other treatment for a better overall effect with no worries about mixing ingredients!
Finasteride is an oral medication that inhibits the enzyme that converts testosterone to DHT. It was originally created as a prostate drug, however, scientists soon realized that it grew hair, too.
Studies on finasteride have shown mixed results. In women, high-quality studies show that finasteride is likely safe and effective (24).
In men, it seems to work much more effectively for regrowing hair (22).
Researchers hypothesize that finasteride and ketoconazole might be most effective when used together (19). As they both seemingly inhibit DHT production, using the two in combination may result in a better overall reduction in DHT on the scalp and reduced hair loss.
However, studies on these two therapies in conjunction have currently only been performed in men. Extrapolating these results to women, unfortunately, is difficult and doesn’t predict efficacy.
The Verdict: Does Ketoconazole Shampoo Work?
The answer is: it depends.
The human body is complex. What works for one person doesn’t always work for another. Further, the biological differences between men and women make it difficult to predict whether one hair loss therapy’s effectiveness will translate to the other sex.
It also depends on what exactly is causing your hair loss.
Ketoconazole shampoo can treat trichomycoses, fungal infections that can cause hair loss, and promotes hair growth in androgenetic alopecia scalps. However, the development of hair loss outside of these causes might not improve with ketoconazole shampoo.
The effectiveness of ketoconazole shampoo also doesn’t warrant tossing out a different hair loss therapy in exchange. Minoxidil still proves to be more effective along with botulinum toxin.
Although, ketoconazole shampoo can be used together with treatments like minoxidil, finasteride, and scalp tension relief tools for better overall hair health. As a precaution, though, you should always consult your doctor before using ketoconazole shampoo or conjunctive therapies.