As controversial as it is effective, the bleaching agent hydroquinone is the most commonly used tyrosinase inhibitor. Often used in the treatment room to prep for advanced exfoliating treatments, it’s also recommended for post-inflammatory pigment and melasma. In this episode of The Rogue Pharmacist, we sit down with Benjamin Knight Fuchs to discuss the effects of hydroquinone on melanin production and the dos and don’ts.
Associated Skin Care Professionals (ASCP) presents The Rogue Pharmacist with Benjamin Knight Fuchs, R.Ph. This podcast takes an enlightening approach to supporting licensed estheticians in their pursuit to achieve results-driven skin care treatments for their clients. You can always count on us to share professional skin care education, innovative techniques, and the latest in skin science.
Benjamin Knight Fuchs is a registered pharmacist, nutritionist, and skin care chemist with 35 years of experience developing pharmacy-potent skin health products for estheticians, dermatologists, and plastic surgeons. Ben’s expert advice gives licensed estheticians the education and skin science to better support the skin care services performed in the treatment room while sharing insights to enhance clients’ at-home skin care routines.
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0:00:55.4 MS: Welcome everybody to ASCP and The Rogue Pharmacist with Benjamin Knight Fuchs. In each episode, we will explore how ingredients chemicals and the environment can have a positive and negative effects on the skin. I'm Maggie Staszcuk, cosmetology education manager, speaking with Ben today about hydroquinone. Hey, Ben.
0:01:14.2 Benjamin Knight Fuchs: Hey, Maggie, good to see you.
0:01:16.0 MS: Good to see you. So hydroquinone I think is really commonly used, but it is maybe a little bit controversial. And sometimes the consumer as well as the esthetician doesn't quite know all the risks.
0:01:29.7 BF: Well, here's my take on hydroquinone...
0:01:33.0 MS: Tell us...
0:01:33.1 BF: Okay. In one word...
0:01:33.4 MS: Yeah...
0:01:33.7 BF: Yuck.
0:01:34.4 MS: Okay, why?
0:01:35.7 BF: It is a yucky yucky ingredient, because it's toxic.
0:01:39.4 MS: Okay.
0:01:40.0 BF: Now it's very effective, but it is toxic. I used to have to work with it in the pharmacy, I would have to make very high concentrations of hydroquinone. And I would wear a mask, it smells awful. It's carcinogenic. It's just a really yucky ingredient. However, it's also very effective. And so sometimes in skincare from a medicinal standpoint, you have to kind of compromise between yuck and effectiveness. It's unfortunate, but that's the way drugs work. And hydroquinone is a drug. Now, you can get it over the counter...
0:02:08.5 MS: Sure.
0:02:09.0 BF: Up to 2%. I think it's 2%. And then as a prescription, you can't get it more than 4%. And the reason that is is because, yuck. The chemical structure of hydroquinone is such that it's very reactive. It's particularly reactive when it comes to genetics. That's what accounts for its carcinogenicity. Now, I'm not gonna say low concentrations are carcinogenic, but you got to kind of think how much of a carcinogen is not gonna be a problem. There's really no answer for that the FDA limits over the counter preparations of hydroquinone to 2% and then prescription to 4%. Whether 2% is a problem or 3% is a problem or 4% is a problem and how often you use it etcetera those are all points that you have to take into account when it comes to the toxicity versus the benefit, the benefit to toxicity ratio. But it is very effective as far as skin lightening goes. However, in pharmacy school, we're taught and then pharmacists know that when you're on a hydroquinone preparation, you need to take time off.
0:03:12.0 MS: Right.
0:03:12.5 BF: Right.
0:03:12.9 MS: And I think that's what people don't always know.
0:03:15.6 BF: The time off part.
0:03:16.4 MS: The time off part. Yeah.
0:03:17.3 BF: Yes, because it can be toxic to melanocytes, melanocytes are the cells that make pigments and you can end up with permanent skin lightening, if you use hydroquinone for too long a period of time. So dermatologist should... Most dermatologists will tell you three months on three months off two months on two months off that kind of thing. So you got to kind of understand how to leverage the power of hydroquinone. Take advantage of the power of hydroquinone without going into toxicity. That being said, there's a lot of other skin lighteners that are not toxic that you can use and also, impressed most importantly, the skin lightening... I'm sorry, skin darkening or hyperpigmentation is a biochemical issue. It's not the sun's fault. And when you're a kid and you're out playing in the sun. What happens to your skin, you get tan, right?
0:04:03.1 MS: Right.
0:04:03.6 BF: You don't hyper pigment. Hyperpigmentation doesn't occur until your biochemistry starts to break down as you're an adult or as you're an older person. And usually it's related to the stress response. And interestingly, pigmentation is part of the systemic generic stress response. So when you're under stress, the body doesn't respond in just individual parts, the entire global system responds to stress and that could be stress from a credit card bill. It can be stress from a disease. It could be stress from the sun, it could be stress from chronic assaults from food or drugs or cigarette smoke. Anything that stresses the body is going to activate this stress response. And part of the stress response is pigmentation. In fact, melanin, the chemical name for pigment, melanin is very similar to stress chemicals that are made in the adrenal glands and as part of the stress biochemical pathway system. So when we're under stress as mediated by hormones, specifically cortisol, and believe it or not, you probably know this estrogen, you're in a pigment. And pigmentation should always be regarded as number one.
0:05:09.9 BF: I should say hyperpigmentation or melasma should always be regarded as a sign number one that the body is under some kind of duress. And number two, that there's some hormonal imbalances around estrogen, and around cortisol, which are very common. We have a chronically hyper cortisol population. That's why people can't sleep. This is why immune systems are suppressed. This is why people have skin problems. And this is why hyperpigmentation occurs. And women who have gone through pregnancy know about the mask of pregnancy, women who are on HRT, hormone replacement therapy, they know that they have a tendency to hyper pigment, women on the birth control pill sometimes will hyper pigment.
0:05:47.2 BF: So we know that estrogen is involved in the pigmentation... In stress response and then in pigmentation. So if you are hyperpigmentation, yeah, you can lighten the skin with hydroquinone and it is pretty effective. I'll tell you about some other ones that are just as effective or close to just as effective and non toxic, but it's gonna come back.
0:06:05.7 BF: If you don't take care of the problem. If you don't take care of the biochemical issues, the hormonal issues, the stress issues, it's just gonna come back. So really, what's the point? You may get some temporary relief. Yeah, hydroquinone can be effective, usually in the higher concentrations, but you're gonna be dealing with toxicity and you're not really addressing the problem.
0:06:24.4 MS: And toxicity in the sense that it is filtered by the liver, right?
0:06:27.9 BF: Yeah, it's a... It's a real... It's a powerful substance, hydroquinone. Now, it's found in nature, by the way, hydroquinone, it's a natural substance. The stuff that we use in skincare isn't necessarily natural. It's very... It's synthesized, but it is found in nature in very, very small quantities. So there are plants that will make hydroquinone, but in very, very, very trace amounts. There's a really interesting herb that grows up here in Boulder called Uva ursi. Have you heard of this?
0:06:56.4 MS: I have. Yeah.
0:06:57.6 BF: Yeah. Uva ursi has natural arbutin in it, which it can be broken down into hydroquinone and I actually use Uva ursi sometimes in my formulations, in my prescription formulation. So hydroquinone is a natural substance, it's found in very, very trace concentrations in plants. But the stuff that we get in products is 2%. That's a big dose, 4% is an even bigger dose. And by prescription, sometimes I would have to make a 10% or a 20% dose.
0:07:20.2 MS: Oh, wow.
0:07:21.5 BF: Concentration that's really high. And like I say, I would wear a mask. I'd work under the hood when I was making it, but it's effective and it will lighten the skin. Although as I say, the pigmentation will come back if you don't take care of the cause of the problem. The skin lightening has a cause. And while you can fix it, topically, if you don't address the cause, it's just gonna come back.
0:07:40.8 MS: You had a keyword there that stood out for me in that is that hydroquinone is a drug, I think, as aestheticians in the treatment room, they're not thinking in those terms. They're thinking this is a cosmetic that I'm applying topically.
0:07:52.0 BF: Yeah. Yeah. It's not a cosmetic, it's a medication and it's a drug. And even though in low concentrations, you can get it over the counter, in higher concentrations it requires a prescription and there is a limit on the over the... On even the drug preparations. And you have to have a compounding pharmacist like myself make higher concentrations. Interestingly, hydroquinone is very similar in chemical structure to parabens. It's very similar in chemical structure to salicylic acid and it's very similar in chemical structure to Resorcinol.
0:08:19.7 MS: Interesting.
0:08:21.3 BF: And it turns out that Resorcinol and salicylic acid also have skin lightning properties. And they're not as toxic as hydroquinone. Resorcinol is pretty toxic. I'd say Resorcinol has a close toxicity profile to hydroquinone. But salicylic acid is not as toxic and salicylic acid will give you anti-aging benefits. It will give you exfoliating benefits. It will give you collagen stimulating benefits. So if you really wanna use hydroquinone as a skin lightener you might wanna try salicylic acid. And salicylic acid, as I say will give you anti-aging benefits. In addition to lightning the skin, it's a great skin lightener on its own. And it's similar in chemical structure too, to hydroquinone.
0:09:00.5 MS: What about some of these other plant ingredients that you hear used for skin lightening like, licorice or Bearberry or things of that nature?
0:09:06.3 BF: Well, bearberries Uva ursi, that contains arbutin, which is broken down into hydroquinone... Not... I wouldn't... You're not gonna get much skin lighting just from Bearberry. It's more like a... I'm sorry, Bear claw, I think.
0:09:17.5 MS: Bear claw.
0:09:18.6 BF: Bear claw. Uva ursi is bear claw. I don't know about Bearberry if that has a skin lighting properties, does it?
0:09:22.5 MS: I think it does.
0:09:23.2 BF: It might. Okay. I don't know about Bearberry, but bear claw, Uva ursi but it's not in anywhere near in the same kind of potency as concentrated hydroquinone. Think about your... You're getting a super concentrated formulation when you get a 2%, 4%, or even a 10% product with hydroquinone in it. You're not gonna get that in nature. There is arbutin which as I say, is broken down into hydroquinone. Arbutin is really expensive and you don't get much hydroquinone out of arbutin. There is licorice, which works with the estrogenic system, helps stabilize estrogen. It has some mild skin lighting benefits, but it's not... These are mostly ancillary or like a extra that you could add into your hydroquinone formulation or your salicylic acid formulation, or to me, the best way to lighten the skin topically is with retinoic acid or retinol, both of which have skin lightening properties via their exfoliating benefits.
0:10:14.3 BF: They also made... I think they may be also, have an effect on the pigment making cells as well. And then you get all the wonderful anti-aging benefits of retinol and retinoic acid. So to me, I'm using, I recommend using retinol, retinoic acid, salicylic acid, and then interestingly, the pigment in your skin is made by the melanocytes and then it's injected into the keratinocytes. So you have your... Here's your skin. We can't see it, I guess. [laughter] So you have your skin and you have the skin cells, the keratinocytes in the bottom. And then you have your melanocytes that are located towards the bottom in the epidermis and the melanocytes are making pigment and then they do something really cool. They actually will inject the melanin into the keratinocytes as the keratinocytes is rising to the top. It's kind of like, you ever see how planes fuel in mid-air, like one plane will fly over and then it'll drop a little hose down to the other plane.
0:11:07.6 MS: Yeah.
0:11:07.9 BF: That's kind of what happens. And the reason this is relevant is because the keratinocytes is what's carrying the pigment and it's the keratinocytes which is darkening, the melanin in the keratinocytes is doing the darkening. And that means the keratinocytes is gonna rise up to the top and it's gonna contain the pigment, it sloughs off. So you can, by increasing sloughing via exfoliation techniques and peels, you can get rid of pigment. And so anything that peels the skin, exfoliates the skin, salicylic acid, retinol, glycolic acid, all these kinds of techniques, laser, TCA peels. They will have an anti pigment effect too, because they'll slough off the dead... The dead cells that contain the pigment. But there is, remember, this is part of the stress response, pigmentation.
0:11:51.4 BF: And one of the stresses that the skin undergoes is inflammation. So inflammation can also trigger pigmentation. That's called, I'm sure you know, post-inflammatory hyperpigmentation. And so while peels and exfoliating techniques can get rid of the pigment, they can also stimulate pigment. And that can be very troubling. If you go into an aesthetician and she peels you to get rid of pigment and you come back with more pigment, you're not gonna be very happy. And so post-inflammatory hyperpigmentation is a thing, a real thing. And so you want... This is why you want to control the pigmentation at the biochemical level, using hormonal strategies, using nutritional strategies, antioxidant strategies.
0:12:29.5 MS: I'm glad you're mentioning chemical peels, because I know there are a lot of estheticians that use a protocol incorporating hydroquinone leading up to the peel. And then...
0:12:40.2 BF: To prevent.
0:12:40.9 MS: To prevent it.
0:12:41.7 BF: Yes. Yes. Yes.
0:12:42.8 MS: Right. And then do the peel, especially with people that have darker Fitzpatrick.
0:12:46.0 BF: Yes, yes.
0:12:46.8 MS: So with...
0:12:46.8 BF: Middle Fitzpatrick, not that it's super dark, but towards the higher end, like the twos to fours, such kind of thing.
0:12:53.5 MS: Sure, sure. So my understanding with hydroquinone, and tell me if I'm wrong, but hydroquinone is targeting those melanocytes differently than an alternative ingredient, or even like if you're doing laser, where you're sloughing from the surface, it's actually blocking that melanocyte from transferring the pigment, is that correct?
0:13:10.7 BF: No, it's more like they inhibit the enzyme that makes melanin, tyrosinase, you've heard of it, I'm sure.
0:13:16.7 MS: Yeah, sure. Okay, got it.
0:13:17.1 BF: These are tyrosinase inhibitors. And by the way, I forgot one of my... Probably my favorite skin lightener is vitamin C, which is an antioxidant. And that protects melanin from oxidizing. The darkening of melanin is an oxidation reaction. So antioxidants will block that and vitamin C has a really, really nice skin lightening effect. And of course you get all the wonderful skin health and anti-aging benefits from vitamin C too. So hydroquinone, it's not a trans... There are some ingredients that are transfer blockers, that block that whole transfer process, but hydroquinone is mostly, it may have some transfer blocking effects, but it's mostly a tyrosinase inhibitor.
0:13:50.7 MS: Okay.
0:13:51.4 BF: And that's the main strategy for skin lightening. You've heard of kojic acid, right?
0:13:56.3 MS: Oh yeah.
0:13:57.2 BF: Yeah. I don't know what the big deal is with kojic acid, and I've been working with it for years, for decades. I have yet to see any skin lighting properties from kojic acid, but it is theoretically a tyrosinase inhibitor.
0:14:08.5 MS: Okay. So in terms of using hydroquinone and especially for people that are prescribing it for their clients for home use, really what is the best protocol?
0:14:18.9 BF: Two months on, two months off, every other day, every third day, three days on, two days off, make sure you give your skin a chance to recover, you don't bombard it with hydroquinone. And then you want to take a month or two months off completely. Otherwise you run the risk of permanent disabling of the melanocyte, which will give you a vitiligo like condition, skin whitening condition, which you don't want either. So you really want to take days off and then complete months off after you use it for two or three months.
0:14:46.8 MS: Okay. So really it's just temporary use and then you're done.
0:14:50.2 BF: Yeah. And then understand that the pigmentation is not a topical situation, even though it shows up in the skin as, and that's kind of like a general theme in skincare. Is it just 'cause something shows up on the skin, doesn't mean it's a skin problem. Things show up on the skin, but they are percolating and they're building up from biochemical breakdowns underneath and that's the most important. And to me as a pharmacist, it really is kind of... You ever hear that saying, when all you have is a hammer, everything looks like a nail, it's like that. We're trained as skincare professionals, we're trained in topical strategies and so that's all we do, but really the skin is the end result of what's happening inside the body with some exceptions. For the most part, if you have something on the skin, it's starting off inside the body, so we really have to address the biochemical dysfunction that's leading to the problem. So if you're gonna gonna use hydroquinone, make sure you're using cortisol stabling strategies, make sure you're using estrogen balancing strategies. Make sure you're staying away from inflammatory foods. Make sure you're staying away from sugar, make sure you're using essential fatty acids. There's all kinds of things that you can do. And that will not only take care of the pigmentation, really take care of the pigmentation, but it'll add years to your life and they'll reduce risks of further health challenges down the road.
0:16:03.2 MS: So you were telling us that the molecular structure of hydroquinone is a lot like salicylic acid or some of these other ingredients.
0:16:11.6 BF: Yeah.
0:16:12.3 MS: Is that really its ability to penetrate into the skin?
0:16:15.1 BF: Yeah. Hydroquinone is fat soluble... Well it's not really fat soluble, but it has a certain degree of fat solubility we'll say, but it's a small molecule. And so it does penetrate it pretty darn effectively, especially when it's used in vehicles like propylene, glycol or alcohol or an emulsion like in a cream, that will all increase its ability to penetrate. Hydroquinone is... As I'm sitting here thinking, it's pretty fat soluble, it's got a pretty good degree of fat solubility. So it will penetrate and it will get down to the melanocyte pretty effectively, which, penetration's a good thing, but then again, into the bloodstream and then into the liver's not a good thing because it is a really powerful drug. It's a powerful chemical. There's also something else I should tell you, there's a pigment that is not melanin, it's aging pigment.
0:17:04.6 MS: Oh, I haven't heard about it.
0:17:04.8 BF: Have you heard of this before?
0:17:06.2 MS: No.
0:17:06.3 BF: Yeah. You ever see older folks sometimes will have geographical things that looks like a map, like the map of France or something on their hands?
0:17:13.8 MS: Yeah.
0:17:14.4 BF: Or their legs, that's not melanin. That's aging pigment called lipofuscin. Have you heard of this?
0:17:19.8 MS: No, I've never heard that.
0:17:20.6 BF: Yeah. And there's a lot of confusion because people will see this pigment and they'll try to use hydroquinone or retinoic acid or peels or whatever and nothing happens, because it's not melanin and it's not located in the surface like most pigment is, it's located deeper down in the dermis and that is lipofuscin which is the pigment of aging. It's the end result of cells that are broken down and the waste products of these dead cells is not being cleaned out appropriately. It's a lymphatic problem, really.
0:17:48.2 MS: Interesting.
0:17:50.0 BF: Yeah. And lipofuscin happens in the eyes. Lipofuscin can happen in the brain and in the nervous system, and lipofuscin can happen in the skin. And it's very confusing because a lot of times people don't make this distinction between melanin and lipofuscin and they'll try to treat a lipofuscin condition with depigmentizing agents and nothing happens. So it could be very frustrating, if that occurs, you want to consider it to be a lymphatic issue, a sign that you're not detoxifying, which once again can lead to further problems. And by addressing your lipofuscin at the level of the lymphatic system, you can save yourself from health challenges down the road. Moving the body, slow deep breathing, hot cold plunges, dry brushing. These are all great strategies for removing the lymph, using nutrients like vitamin E, essential fatty acids. These can help drain out the lymph but you wanna make sure you're making a distinction as an aesthetician, or as a skincare professional, you wanna make sure that you're making a distinction between lipofuscin, L-I-P-O-F-U-S-C-I-N and pigment. And lipofuscin tends to be a little bit more brown than pigment. And you've probably... I'm sure you've seen it now that...
0:18:52.5 MS: Oh yeah. You see it on the hands of the elderly all the time.
0:18:55.4 BF: Yes. Yes. That's lipofuscin, and that's an aging pigment, it's a sign of a poor detoxification and lymphatic drainage.
0:19:01.3 MS: Interesting. Is that showing up on the skin on other parts of the body?
0:19:05.8 BF: Legs, it can show up in the torso.
0:19:07.1 MS: Interesting.
0:19:08.1 BF: Yeah. A lot of times on the hands though, that's what I know.
0:19:09.6 MS: Yeah. Yeah. The hands are so common. And I've always thought that that was like blood pooling.
0:19:14.5 BF: No.
0:19:15.0 MS: That's what it looks like to me.
0:19:15.9 BF: It's dead cells. Under ordinary circumstances when a cell dies, it's really interesting, there are components inside cells that are incinerated. Cells have little incinerators, little furnaces, and those furnaces are supposed to burn, literally break down those toxins. And then those toxins are... Not toxins but waste products, are then recycled. But as we get older, that doesn't happen as much, and then instead of getting recycled, they get dumped into the lymph system. And then instead of the lymph clearing them out like they should, they just accumulate, lymphatic stagnation, lymphatic clogging. So you wanna consider lipofuscin to be a problem with waste management, and that's why it only happens to older folks, but it's a sign that you're not clearing toxicity out as well as you should. And if you really resolve it at that level, you'll save yourself from health issues, further complications down the road.
0:20:04.5 MS: Yeah. That makes sense. I mean, everything slows down as we get older.
0:20:06.7 BF: Yes. Everything slows down as we get older.
0:20:08.7 MS: Any last comments Ben that you wanna share with us on hydroquinone?
0:20:12.2 BF: Use nutrition always. And if you are using hydroquinone, make sure you're using things like vitamin E and vitamin C and detoxification strategies to help your body clear out the hydroquinone. And if you are using hydroquinone, use vitamin C after or with your hydroquinone to help protect you from some of the untoward effects of the hydroquinone, and you'll also get extra skin lighting benefits too.
0:20:34.7 MS: That wraps our show today. And as always, if you're not an ASCP member, join today at ascpskincare.com/join. If you liked this episode, subscribe today so you never miss it. Details from what we discussed today will be in the show notes. If you just can't get enough of Ben Fuchs, The Rogue Pharmacist, you can listen to his syndicated radio program at brightsideben.com. Thanks everyone and have a great day.