The Ultimate Hydroquinone FAQ
What is hyperpigmentation?
As it pertains to hydroquinone, hyperpigmentation is best described as the darkening of a certain area of the skin or even the nails brought about by an increase in the production of melanin, a substance that is responsible for giving the skin its darker hue. Highly specialized cells in the skin, called melanocytes, produce melanin by oxidizing tyrosine and polymerizing it to form its final pigment molecule.
Excessive exposure to UV radiation can lead to oxidative stress, freeing free radicals into the circulation and substantially increasing the production of melanin. The presence of inflammatory substances can also facilitate the abnormal production of melanin. Other factors that can increase melanin production include antibiotics, birth control pills, diabetes, tissue injury, and hormonal changes, among others. Heredity can also play a role in the overproduction of melanin leading to hyperpigmentation or increased darkness of the skin tone.
Hyperpigmentation has also been associated with many health conditions such as Addison’s disease, melisma, linea nigra, Cushing’s disease, Grave’s disease, and tinea infections to name a few. It has also been known to be brought by dermatological laser procedures secondary to the microscopic burn injuries that occur at the tissue level.
What are the common forms of hyperpigmentation?
There are different forms or types of hyperpigmentation. Two of the most common forms are skin tanning and solar lentigines. Everyone knows that skin tanning is the purposeful darkening of the skin accomplished either through exposure to direct sunlight or through the use of special tanning equipment.
Solar lentigines, on the other hand, are also the direct result of overexposure to the sun’s rays, although these are also associated with advancing age. Solar lentigines are also known as liver spots, old age spots, solar lentigo, senile freckle, or simply age spot. The hyperpigmentation is not purposeful and can range from light brown to reddish brown to black in color. These are also found mostly on the skin of body parts that are frequently exposed to UV radiation such as the hands, arms, shoulders, face, and the forehead. Liver spots or solar lentigines typically occur among middle-aged individuals beginning at the age of 40 because of the reduced ability of skin cells to regenerate fast enough.
Acanthosis nigricans is another form of hyperpigmentation that is mostly confined in body folds such as the region between the neck and the torso, the armpits, the navel, and the groin. This form of hyperpigmentation is mostly seen in obese individuals, although persons with endocrine abnormalities or cancer can also present with such hyperpigmentation. Individuals taking growth hormones, glucocorticoids, nicotinic acid, or oral contraceptive pills are also more prone to develop acanthosis nigricans. The hyperpigmented area of the skin takes on an unusually dark color, usually dark brown to black, and comes with very poorly defined borders.
melanin at a particular site in the skin that gives it its characteristic darker-than-normal skin tone. Examples of conditions that can cause post-inflammatory hyperpigmentation include acne, atopic dermatitis, contact dermatitis, and the use of abrasive chemical peels.
Melisma typically occurs among pregnant women and is also known as the mask of pregnancy or chloasma face. However, almost anybody can have melisma especially those that are genetically predisposed to such a form of hyperpigmentation. Individuals with thyroid disorders are also at an increased risk of developing melasma. Certain medications and cosmetics are also known to produce an allergic reaction whereby melisma is one of the presenting signs.
What’s the difference between skin whitening, skin lightening, and skin brightening?
There really are no significant differences between skin whitening, skin brightening, and skin lightening other than as a marketing ploy to appeal to a certain demographic. Skin lightening and skin brightening are terms that are often used to describe products that aim to correct hyperpigmentation sold in Western markets. Eastern markets, on the other hand, are more familiar with skin whitening products. They may have different marketing terms, but the technology inherent in these products is essentially the same.
What is hydroquinone?
During its heyday, hydroquinone was used by dermatologists to treat localized hyperpigmentation such as liver spots or age spots and other forms of hyperpigmentation that don’t require whole-body lightening or brightening.
Hydroquinone typically comes in a cream formulation, containing about 2 to 4 percent of the active ingredient. The base of the hydroquinone cream typically includes a blend of glyceryl monostearate, PEG-25 propylene glycol stearate, purified water, mineral oil, polyoxl 40 stearate, stearic acid, squalene, propylene glycol, sodium metabisulfite, and propylparaben.
Hydroquinone is not necessarily a synthetic compound designed in a laboratory setting. It is actually found in nature. A wide variety of foods and drinks are known to contain hydroquinone. Examples of these include red wine, coffee, tea, berries, onions, broccoli, and wheat as well as any others.
What is the principal indication of hydroquinone?
Hydroquinone is indicated in the management of acne scars, freckles, age spots or liver spots, and chloasma or melasma. It is indicated in the gradual lightening or brightening of localized hyperpigmentation. As such, if one is looking for quick skin lightening results, hydroquinone may not be the correct answer for such a need.
Is hydroquinone effective in the management of hyperpigmentation?
Hydroquinone has been around for several decades. And while it was initially used in the development of black-and-white still images since the early 19thcentury, its use as skin depigmentation has been lauded by many as a breakthrough in the ongoing search for the more effective management of hyperpigmentation. In the 1970s hydroquinone was available only with a prescription. In 1982, the US FDA classified it as generally recognized as safe and effective.
Ever since its introduction in the market as a skin de-pigmenter, millions of individuals have already used a variety of products that come with hydroquinone as one of its ingredients. Even pure hydroquinone formulations of 2% are made available to everyone as an over-the-counter drug. The more concentrated formulation at 4% can only be obtained with a prescription.
This underscores the effectiveness of hydroquinone in the management of hyperpigmentation. Unfortunately, serious issues have been raised related to its potentially-carcinogenic and genotoxic effects.
How does hydroquinone work in the management of hyperpigmentation?
Hydroquinone works by inhibiting the oxidation of tyrosine by enzymes. This helps prevent the conversion of tyrosine to 3,4-dihydroxyphenylalanine or levodopa. L-tyrosine, L-phenylalanine, and levodopa are known to be precursors to the formation of melanin. Since hydroquinone effectively prevents tyrosinase from catalyzing the conversion of l-tyrosine to l-dopa, two of the fundamental precursors of melanin production is inhibited.
In addition to the effects of hydroquinone on the enzyme tyrosinase, it also works to suppress the other metabolic processes inherent in melanocytes, the special cells the produce melanin. Specifically, it increases the rate of decomposition of melanosomes, the pigment granules found in melanin. Together, these two mechanisms of action of hydroquinone lead to the normalization of skin pigmentation.
Are the effects of hydroquinone permanent?
Since the mechanism of action of hydroquinone is related to the inhibition of the action of the enzyme tyrosinase, once hydroquinone has been discontinued there is no longer a mechanism that will prevent the integration of tyrosine, phenylalanine, and levodopa in the synthesis or production of melanin. That being said, if one discontinues the use of hydroquinone, the increased production of melanin, hence hyperpigmentation will reoccur. As such, the effects of hydroquinone are not permanent.
Are there risks involved in the use of hydroquinone?
The major issue with hydroquinone, as underscored in the revocation of its FDA approval in 2006, is that it has the potential to cause cancer. This was largely based on the observation that hydroquinone is rapidly absorbed through the human skin. While this does not clearly point out to the possibility of a carcinogenic effect, laboratory tests revealed that laboratory animals applied with hydroquinone showed an increased risk of developing neoplastic growths including anisokaryosis, cellular adenomas of the liver, follicular cell hyperplasia of the thyroid glands, and cellular adenomas of the renal tubules. Again, there is no conclusive evidence showing the relationship between hydroquinone and the formation of these cancers in humans. However, there are also no clear-cut studies showing that there’s no relationship at all. Nonetheless, the risk is ever-present.
Another major risk that is associated with hydroquinone use is the development of exogenous ochronosis, a type of disorder in which there is further deterioration of the hyperpigmentation often coming in the form of blue-black pigmentations on the skin. These observations were more prevalent on oral formulations of hydroquinone, however, rather than the topical application. Nevertheless, it should still pose a great concern especially if the product that one is using happens to include Resorcinol.
Studies show that the combination of resorcinol, a disinfectant and antiseptic, and hydroquinone increases the risk and severity of ochronosis. Additionally, the chronic use of hydroquinone, as well as the use of greater than 4% concentrations of the formulation, can also contribute to the worsening of ochronosis.
There is also the risk of developing skin sensitivity which can expose the skin to other more serious problems in the future. It is also for this reason that hydroquinone is often used in combination with an appropriate sunscreen, preferably with a high persistent pigment darkening or PPD rating, especially when going outside. Protecting the body parts that are applied with hydroquinone can also help minimize skin sensitivity.
Are there contraindications to the use of hydroquinone?
One of the most important contraindications to the use of hydroquinone is a known allergy or hypersensitivity to the substance or other ingredients of the formulation. Under no circumstance that hydroquinone should be used on individuals with known hypersensitivity to phenols or benzenes.
For individuals who are not sure if they are sensitive to hydroquinone, skin testing the product prior to application on target areas is recommended. This means one needs to apply a very small amount of hydroquinone on a part of the skin that is typically hidden from public view. This site should be encircled with a permanent marker or even a ball pen to help establish the borders of the application. After 24 hours, the site should be inspected and see if there is redness in the area. If there is, then there is a high chance that one is sensitive to hydroquinone.
Currently, hydroquinone has not been studied on pregnant and lactating women. As such these life stages are not really considered as absolute contraindications to its use, but rather more as a precaution. The same is true with children below the age of 12 years.
What are the most common side effects associated with hydroquinone use?
Signs of an allergic reaction always require immediate medical attention. As such, if one observes difficulty breathing, the development of hives, or even swelling in the throat, face, lips, and tongue, then there is a chance that one is experiencing a severe allergic reaction from hydroquinone.
In the 1980s, hydroquinone was deemed generally safe and effective. Unfortunately, succeeding studies by the National Toxicology Program concluded that hydroquinone poses a risk of genotoxic and carcinogenic effects.
Among the most commonly-reported side effects of hydroquinone include mild itching, irritation, or redness at the site of application as well as a sensation of mild burning or stinging. Other possible side effects include localized contact dermatitis. The rare disorder exogenous ochronosis has been documented 22 times in the past 50 years. And while this is a very rare side effect, there is still a possibility of its development.
Other side effects may be present, but most of these are brushed off by individuals who are more concerned about the skin lightening effects of hydroquinone rather than its side effects.
Are there serious adverse reactions to the use of hydroquinone?
Animal studies show that hydroquinone has serious clastogenic and carcinogenic effects. This means that it has the ability to disrupt or damage chromosomes. This can lead to chromosomal aberrations such as chromosomal deletions, reassortment, or even additions. The ability to cause certain cancers of the thyroid, liver, and kidneys has also been documented in animal studies. However, whether or not these risks extend well into human populations is still debatable. The key is our <2% dosage which makes it safe for use.
Some of the more immediate serious adverse reactions that one can experience with the use of hydroquinone include severe skin redness, severe stinging or burning sensation, the presence of oozing or blistering, severe skin dryness that can lead to cracking, blue-black discoloration, and bleeding. If you see any of these signs, it is imperative that you seek medical attention at once.
How should hydroquinone be used?
The topical application of hydroquinone should not be started unless a test dose has been administered. You can apply a small amount of hydroquinone to a healthy part of the skin, preferably one that is typically hidden. Leave this for 24 hours and take note of any redness that may occur at the site of application after 24 hours. If there’s only minor redness you can proceed with the application of hydroquinone on the target site. It is important to perform a test dose or a skin test to make sure that you are not allergic or sensitive to hydroquinone or any of the formulation’s ingredients. If there is itching, blistering, or puffiness in the area of application, then it is possible that you’re allergic to it.
Always wash your hands thoroughly before and after the application of the cream. Prepare the area that needs to be treated with the formulation. Clean, wash, rinse, and dry it thoroughly so that debris and other skin surface contaminants will be prevented from affecting the action of hydroquinone.
Make sure to apply it only to the affected area and never to stray into the surrounding skin. Make sure to rub the cream well into the skin. However, care should also be taken so that it will not be applied to other parts of the body especially the eyes, mouth, or even nose. In cases where the medication has been inadvertently applied to these body parts, you should flush these with copious amounts of water.
If you have to use sunscreen, non-medicated cosmetics, or even moisturizers, it is imperative that you apply hydroquinone first before these products. It is also important that you allow the hydroquinone to sit on the surface of the skin for several minutes before topping it with a layer of other topical preparations.
In using hydroquinone with other medicated products, it is important to consult your dermatologist or doctor about potential drug interactions. Hydroquinone can react adversely with peroxide products so you might need the opinion of your doctor before applying any of these products on the same area as the hydroquinone targeted site. Peroxide products are known to cause staining on the skin which can be an entirely different set of problems to deal with.
How often should I use hydroquinone?
The current recommendation is to apply hydroquinone onto affected areas of the skin twice a day or as deemed necessary by your dermatologist. When administered twice a day, one should be applied in the morning and the other just before going to bed. It is also highly advisable that you apply it at exactly the same time every day so you don’t run the risk of missing a dose.
Is it safe to use hydroquinone if I am pregnant?
The effects of hydroquinone on pregnant humans have never been studied. As such, its effects on fetal development are not known or whether it has an adverse effect on the reproductive capacity of women who are using hydroquinone to treat a variety of localized hyperpigmentation problems. The prevailing theory is that hydroquinone is absorbed through the skin and reaches the bloodstream. And since blood also circulates to the developing fetus, then there is the possibility of an interaction between hydroquinone molecules and the cells and tissues of the developing fetus.
What is understood is that animal studies show hydroquinone can largely affect chromosomes which are essential in cellular division and propagation. It is for this reason that pregnant women who choose to use hydroquinone should only do so under the strict guidance of a medical practitioner and only when there is a clear indication for it that outweighs the risks.
Is it safe to use hydroquinone if I am breastfeeding?
Just as the effects of hydroquinone on pregnant women have never been established nor studied, the same can be said of lactating or nursing mothers. It is generally not known whether the substance can be excreted in human breast milk. However, since there are a large number of medications that are excreted in breast milk, it is also possible that even topical hydroquinone can be found in breast milk. Again, caution should be observed when giving hydroquinone to a woman who is currently breastfeeding.
Is it safe to use hydroquinone on children?
Currently, there is no conclusive evidence to show that using hydroquinone on children below the age of 12 is safe. However, there are also no studies saying that it is not safe. As always, caution should be exercised when giving this medication to members of the pediatric population.
What are the things I need to avoid when using hydroquinone?
One of the things that can occur with the use of hydroquinone is the development of increased skin sensitivity. It should be understood that melanin actually has a protective function in the skin. Melanin can dissipate as much as 99.9% of UV radiation to the surrounding tissues, saving the skin from tissue injury. This is one of the reasons why certain types of skin cancers are more prevalent among fair, or light-skinned people because they have less melanin. That being said, you should always avoid exposing the hydroquinone-treated areas of the skin to direct sunlight as you will easily get sunburn. While some hydroquinone products already contain sunscreen, it is equally important to look at the label so that it should contain at least an SPF 30 rating.
Because of increased skin sensitivity, you may also experience a variety of skin reactions to weather extremes. Weather extremes like too hot or too cold can irritate the hydroquinone-treated skin leading to inflammation and possibly secondary bacterial or fungal infections. Since it is virtually impossible to avoid weather extremes, you can nevertheless protect yourself by wearing appropriate clothing. You can also apply moisturizing lotion to help keep your skin from drying.
It is also important to avoid using hydroquinone with peroxide products such as hydrogen peroxide and benzoyl peroxide, among others. It has been shown that hydroquinone reacts with these compounds to produce a different kind of stain on the skin. The good news, nonetheless, is that this stain is easily removed with plain water and soap.
Do not use skin care products that contain harsh chemicals as they can severely damage the skin because of the removal of melanin underneath. Harsh soaps, skin cleansers, shampoos, hair waxes, hair coloring, and hair removers should be avoided at all cost. Skin care products that contain astringents, alcohol, lime, or spices, as well as many others, should also be avoided.
Do not allow hydroquinone to get anywhere near the eyes as this can lead to permanent corneal damage. This can result in visual problems.
Is it possible to overdose hydroquinone?
Topical hydroquinone works as a local application. The side effects that have been observed are, thus, mostly local reactions. Overdosing is not really a major issue, although some adverse reactions can be exceptional causes of concern. Transient skin redness and a stinging or burning sensation are the most common complaints associated with its use.
However, if hydroquinone is swallowed especially by children it is possible that gastric upset can occur, often depending on the amount of the drug that was ingested. The individual should also be brought to the nearest emergency medical facility so that the necessary treatments can be initiated.
How long does it take for hydroquinone to work?
Individuals who are using hydroquinone typically notice improvements in their hyperpigmentation after about 4 weeks of continuous treatment. However, the noticeable improvements can also occur at a much later time. The current convention is that if there are no improvements in the hyperpigmentation after 2 months of continuous application, it is imperative to inform your doctor about it. In many cases, your doctor might recommend extending the treatment for another month. If after 3 months of continued use, no improvements are noticeable, the application of hydroquinone should be discontinued and another skin lightening product should be considered.
What can I do to improve the skin lightening effects of hydroquinone?
Protecting hydroquinone-treated skin from the harmful rays of the sun is a must if one desires to leverage on the skin lightening benefits of hydroquinone. Since hydroquinone effectively strips the skin of its protective mechanism – melanin – which normally protects it against excessive UV radiation, applying sunscreen with a minimum sun protection rating of SPF 30 should help enhance the skin lightening effects of the medication.
Wearing appropriate clothing to help minimize skin sensitivity can also help improve the skin lightening effects of hydroquinone. It is important to realize that melanin generally serves a protective purpose. Removing it from the skin exposes this part of the body to a variety of insults which can lead to other health problems.
Using only skin care products that are made of safe, natural, and mild ingredients can also help. Skin care products that contain harsh chemicals or ingredients can seriously damage the already-sensitive skin brought about by the removal of melanin secondary to the administration of hydroquinone.
Should I wear a sunscreen when I am indoors and currently receiving hydroquinone?
Hydroquinone makes your skin extra sensitive. That is why it is important to protect the hydroquinone-treated skin with sunscreen or some other means. However, if one is staying indoors where UV radiation is very minimal, there is no need to wear sunscreen. What one needs to wear, nonetheless, is appropriate clothing since extremes in temperature can also damage hydroquinone-induced sensitive skin.
What should I do in case I develop hypersensitivity reactions to hydroquinone?
Any form of allergic or hypersensitivity reaction, be it from hydroquinone or some other substance, require immediate medical attention. It is imperative that one is vigilant about the signs of an allergic reaction such as hives, facial or airway swelling, and difficulty breathing. This is to help make sure that prompt and appropriate treatment will be made available.
Can I avoid hypersensitivity reactions to hydroquinone?
It is easy to avoid hypersensitivity reactions to hydroquinone. One only needs to perform a skin test or a test dose on a part of the skin that doesn’t have any hyperpigmentation. This is the ‘test site’. Preferably, choose an area that is hidden from view so that even if a reaction takes place it will not be readily visible to others. A small amount of hydroquinone is applied to the chosen ‘test area’ of the skin and left there for 24 hours. Once the 24-hour period has elapsed, the ‘test area’ should be examined carefully. If you notice nothing but a very mild redness on the area, then it is a good sign that you are not hypersensitive to hydroquinone. However, if the area becomes itchy, has turned bright red or shows diffuse redness, or is showing beginning signs of blister formation, then you can consider these as indications of a possible allergic or hypersensitivity reaction to hydroquinone.
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