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An Inexpensive and Effective Option for Removing Unwanted Pigment

Sun exposure, hormones, inflammation, pregnancy, acne, and certain medications all have something in common: they can lead to uneven and unwanted discoloration in the skin. This condition is often defined as hyperpigmentation, and occurs when a portion of the skin becomes darker than the skin surrounding it. Unfortunately, this condition can affect all skin types and is often the result of too much sun exposure. However, hyperpigmentation can also stem from other factors outside of our control. As a result, skin care professionals are often asked for inexpensive yet effective ways to reduce and prevent discoloration and thankfully, we have many great choices for doing so. Today, we are going to discuss one of the most widely used and cost-effective options called hydroquinone.


What is Hydroquinone?
Hydroquinone is a topical skin lightening agent. We call it a tyrosinase inhibitor as it hinders the enzyme tyrosinase from creating melanocytes in the skin. Melanocytes are the skin cells that make melanin which cause the skin to darken or pigment when exposed to sunlight. It’s this process that is responsible for what many define as a nice, healthy glow or tan. Sadly, it’s also responsible for creating freckles and age spots (3). Yes, you heard us correctly, even those cute little freckles you see on young children are signs of damage. Since use of hydroquinone acts as a buffer in the melanin making process, many have defined it as a bleaching agent. However, hydroquinone does not bleach the skin, it simply restores it to its natural (original) baseline color, even if years of unprotected sun exposure has us guessing what that color even is anymore (3,5). Hint: Look at areas typically unexposed or less exposed to the sun like the underarms, buttocks, or underside of the forearms.


What Hydroquinone is used For?
Hydroquinone can be used for a number of skin concerns including dark spots (aka age spots), freckles, melasma, and post inflammatory hyperpigmentation from acne. Keep in mind, hydroquinone helps to fade brown and red hyperpigmentation but will not be effective for correcting discoloration from active acne breakouts or deep cystic acne scars which are caused by damage to the dermis (4). In addition to being found in skin care products, hydroquinone is a unique molecule that occurs naturally in the environment and can also be found in plants and foods such as cranberries, blueberries, pears, coffee, tea, rice, onions, and wheat (2).


How to Use and Who Should Use Hydroquinone
For patients with moderate to severe hyperpigmentation, we suggest using prescription strength 4% hydroquinone twice daily. As a topical melanin suppressor, hydroquinone seems to work best when applied once every 12 hours. In the morning, we recommend using hydroquinone after cleansing, toning, and applying any serums, but before moisturizer and sunscreen. In the evenings, hydroquinone can be applied after cleansing and toning and any retinoid containing products but before heavier moisturizers. The lightening effects of prescription strength 4% hydroquinone are achieved with approximately four weeks of consistent, twice daily use. For those with mild hyperpigmentation, using once a day is typically enough to see results. We are often asked whether it is best to apply hydroquinone on just the dark spots someone desires to fade, and generally speaking, we suggest applying it to the entire face to ensure an even skin tone is achieved (3,5). However, when the product is being used off the face on a larger surface area, or if the skin is a bit more sensitive and thus prone to irritation, it is safe to spot treat. When only using once a day or spot treating, it may take a bit longer to see the effects of 4% hydroquinone. For patients who do not currently have unwanted pigment but are prone to pigment (pretty much anyone who is not diligent with sun protection), hydroquinone can be used as an excellent preventative agent. By blocking the melanin production in the skin, the spots have trouble forming to start with. Thus, this product is good for patients in their 20’s who still have fresh youthful skin, as well as those in their 60’s who are looking to erase the past. While many healthcare providers put patients on a pulse method where they are told to use their hydroquinone product(s) off and on for a period of time, we prefer patients to stick with them daily until they have gotten total or almost total correction. When correction is achieved, we prefer to decrease the dose to once a day or perhaps every other day to maintain. Alternatively, when ideal correction is achieved, we may suggest a milder tyrosinase inhibitor such as kojic acid. Providers who suggest the pulse method are doing so primarily to reduce the sting of rebound hyperpigmentation. This occurs because once hydroquinone containing products are stopped, tyrosinase is no longer inhibited, thus the pigment can return. Thus in theory, cycling the products off and on can make that process less dramatic. Another reason is to prevent ochronosis, a very rare issue that can occur in dark skinned patients and make the skin darker (as opposed to lighter which is the goal of hydroquinone). However, because the risk of ochronosis is so incredibly low in the United States, we do not think that warrants cycling for the vast majority of patients. In fact, the American Academy of Dermatology Association reported that as of 2006, there had been a grand total of only 15 ochronosis cases ever reported in the United States despite the product being used for over 40 plus years by tens of millions of patients (2). To this date, there is no clinical data available to support pulsing or cycling hydroquinone though most patients wind up doing so on their own over time regardless. Given that consistency is one of the greatest challenges when it comes to skin care regimens, we do not tend to fret on whether one should pulse or not.


Who Should NOT Use Hydroquinone:
Hydroquinone containing products are not recommended for those who are pregnant, nursing, or under 12 years of age.


Best Hydroquinone Containing Products
The best hydroquinone formulations are those available in a physician’s office as they contain 4% of the magic ingredient. There are less potent options available over the counter but they top out at concentrations of 2% and typically take considerably longer to see results. We tell patients there are products to save on and products to spend on, and prescription strength hydroquinone is definitely a product we suggest spending on as the results achieved with pharmaceutical grade potions are much faster and more effective.


Depending on your skin’s needs, and your commitment level, we have a variety of different skin care products to choose from:
Obagi Nuderm® is a complete topical system designed to treat severe hyperpigmentation such as melasma and dark spots. It has been on the market for years but has stood the test of time as the most transformational topical treatment option available. The full-size kit lasts approximately four months and costs $453. The trial size kit lasts for roughly six weeks and costs $245. While the full size kit is a much better deal on the surface, many patients like to do the travel size to start to see if they can maintain the required consistency with the products and/or simply to give their skin a jump-start.


The system comes in two formulations, one for normal/oily skin and one for normal/dry skin. With three to four daily doses of 4% hydroquinone, (depending on whether Sunfader® is added) this system packs the most comprehensive punch. The system consists of seven or eight steps (depending on whether retinoic acid is added) including a cleanser, toner, exfoliating agent, moisturizer, sunscreen, and two hydroquinone containing products.


Our patients who have used the system consistently are blown away by the results. The only negative feedback we hear is that the six to eight step system is too cumbersome for daily use and/or the initial irritation most patients experience is less than pleasant. However, in recent years, we have learned lots of tips and tricks to assist in getting patients adjusted to the system, therefore speeding up the period of time they need to fully acclimate to the active ingredients.


Obagi C®-Rx is a great option for those with mild to moderate hyperpigmentation that are still seeking a comprehensive skin care regimen. Similar to Nuderm®, the system comes in either a normal/oily ($348) or normal/dry ($374) formulation and has two daily doses of hydroquinone (one in the morning, and one in the evening). With only five products in the rotation (cleanser, toner (normal/oily only), Vitamin C/Hydroquinone Serum, day lotion (normal/dry only), and night lotion this system is a little easier to commit to for many folks. Therefore, it’s also suitable for patients with more severe hyperpigmentation who simply do not want to commit to the Nuderm® system.


For those who have reached a level of correction they are comfortable with, and just want to maintain, or who are not ready to commit to a system, the following stand-alone products are good choices:

• Obagi® C-Clarifying Serum ($135): One of our best sellers, this awesome antioxidant serum can be used in the morning after washing/toning. Since it contains Vitamin C, this product can save you a step in the morning. We love killing two birds with one stone! Helpful hint: Be sure to rub this product in completely. Do not let it sit on the top of the skin or it can resemble blackheads.

• Obagi Blender® ($113.50): This product is used at night in tandem with a retinoic acid. As the name implies, we like to “blend” the two to once more cut down on an extra step. However, if you prefer applying products sequentially, that is fine as well. This product is included in the Obagi Nuderm® system mentioned prior but can be purchased separately too.

• Obagi® Clear ($119): This product can be used morning and evening or one or the other (depending on the severity of discoloration). This product is also included in the Obagi Nuderm® system mentioned prior but can be purchased separately too.


Regardless of which option you choose, it is important to remember that hyperpigmentation is a chronic condition that many times cannot be cured but instead must be managed over time (1). It may take some trial and error to find the product(s) to fit your needs, but many find the results to be worth the effort.


Best Hydroquinone Free Products
For patients who do not like the feel, finish, or smell of hydroquinone (and yes, we do hear those complaints from time to time), or happen to have an allergy to products containing hydroquinone, there are other options available.


The two most popular hydroquinone free options are Lytera® 2.0 by SkinMedica® and Perle by Neocutis®.
Lytera® 2.0 ($154) is a hydroquinone-free, retinol-free, paraben-free, fragrance-free, non-comodogenic formulation that can be used on any skin tone or type including acne-prone skin. The key ingredients are: tranexamic acid, phenylethyl resorcinol, niacinamide & tetrapeptide-30, marine extract blend, and phytic acid. We still don’t suggest using this product if you are pregnant or breastfeeding but otherwise, it makes a great alternative for those who either cannot or do not want to use hydroquinone.


Neocutis® Perle ($115) is a skin brightening cream that utilizes Melaplex® to even out the appearance of uneven skin. It is gentle enough for everyday use and is safe on all skin types and tones providing results without irritation.
However, if you have excess or stubborn pigmentation, we do believe that the results of 4% hydroquinone are difficult to duplicate with hydroquinone free products so barring an allergy or contraindication previously listed, we generally suggest that you start there.


Products that Partner Well with Hydroquinone
We typically combine Hydroquinone with other skin brightening agents including Vitamin C, Retinoids, and of course Sunscreen! Hats, sunglasses, and protective clothing (we are liking Mott50) are great ideas too.


Safety Information and Potential Side Effects
Hydroquinone has been used safely for over 60 years by millions of patients worldwide and doctors across the country regard it as the gold-standard when it comes to topical treatment options for addressing pigment concerns. Over the years, there have been numerous clinical studies to demonstrate the safe and effective use of hydroquinone. We occasionally hear questions on whether hydroquinone causes cancer. The American Academy of Dermatology reports that any associations between hydroquinone and cancer in humans are completely unproven (2).
The most common side effects generally fade in a few days to a few weeks and include skin irritation such as dryness and redness and occasionally mild burning (4). Another side effect of hydroquinone is that it can make the skin more susceptible to UV damage since it disrupts the formation of melanin. Thus, it is important to use sunscreen all the time, but especially when using hydroquinone as any unprotected sun exposure sustains melanocytic activity, thus reducing results.


Finally, when the color of products containing hydroquinone has turned brown, that indicates the product has oxidized, and thus is no longer active. Oxidized products should be discarded.

Summary
1. Hydroquinone is an inexpensive and highly effective option for erasing and preventing uneven pigmentation.
2. Hydroquinone is an active ingredient found in many skin care products today that can be easily implemented in your current regimen to improve the overall look of your skin.
3. It should be used twice daily for best results and ideally in tandem with Vitamin C, Retinoids, and Sunscreen.
4. The FDA regards hydroquinone as a safe choice for treating hyperpigmentation.

REFERENCES
1. Allergan (2018). Get Even with Hyperpigmentation. Retrieved April 22, 2019 from https://www.skinmedica.com/get_even
2. American Academy of Dermatology Association (2006). Skin Bleaching Drug Products for Over-the-Counter Human Use; Proposed Rule.
3. Cerner Multrum. (2018, November 9). Hydroquinone Topical. Retrieved from https://www.everydayhealth.com/drugs/hydroquinone-topical
4. Drugs.com (2019). Hydroquinone. Retrieved April 22, 2019 from http://www.drugs.com/cdi/hydroquinone.html
5. Hydroquinone Skin Bleaching Cream. (2019). Retrieved from WebMD Web Site: https://www.webmd.com/drugs/2/drug-87530/hydroquinone-skin-bleaching-topical/details
6. Learn More About Hydroquinone. Retrieved from Science Direct Web Site: https://www.sciencedirect.com/topics/pharmacology-toxicology-and-pharmaceutical-science/hydroquinone

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