Hydroquinone Skin Lightening Creams: Answers

Hydroquinone Skin Lightening Creams and Hyperpigmentation: What You Need to Know

Hydroquinone is considered the “gold standard” for treatment of dark spots and other hyperpigmentation problems. It is present in a variety of nonprescription skin lightening creams and in skin lightening ointments and creams that require a doctor’s prescription. Hydroquinone can be found in a number of over-the-counter products like Nadinola, Dr. Palmers, Porcelana fade cream.  Dermatologists office and medical spas may also offer nonprescription Hydroquinone creams at higher percentages and with formulations that are advertised to be better for skin (Musely, Obaji).

Hydroquinone Strengths

Most of these products contain small percentages of the compound (2% Hydroquinone).  There are higher percentages available which are stronger, but they require a prescription.  We’ve encountered concentrations as high as 20% Hydroquinone offered online.    It turns out that there is only one cream containing Hydroquinone is actually approved for use by the FDA.  It is called Tri-Luma.  It is approved specifically for the treatment of moderate-to-severe melasma, a hormone induced or aging-induced pigmentation problem, most common in women.  Tri=Luma is intended for short-term use only.  This skin lightening cream for melasma contains 4% Hydroquinone plus fluocinolone acetonide (a corticosteroid) and a retinoid (retin-A/tretinoin/retinoic acid).  The combination of the Tyrosinase enzyme inhibitor (Hydroquinone), with a steroid lowering inflammation and suppressing melanocyte activity, and a retinoid reagent which speeds up skin cell turnover is effective for some people with hyperpigmentation like melasma.  Long-term effects of steroids on the skin and retinoids are unclear.  So, its use is time-limited to avoid side-effects including damaging the skin, it is not useful or approved for other types of skin lightening for dark skin, or as a dark spot remover or hyperpigmentation improvement.

Why Hydroquinone?

Hydroquinone, the skin lightening was one of the earliest chemical compounds found to be able to improve the appearance of hyperpigmentation, which is the only reason it is the gold standard.   One of the clues that Hydroquinone could prove helpful and beneficial in fighting pigmentation problems was the finding that photographers who used hydroquinone solution as a developer in the black-and-white photography process, sometimes developed lightening of the hands when they used the chemical solution without using gloves.  It made sense that skin conditions that over produced melanin could be treated with Hydroquinone, or a pigmentation blocker derivative, so long as it was safe.

We now know that Hydroquinone is one of many substances that is able to produce a reduction in pigmentation.  Many of the compounds which inhibit melanin production share similarity in their chemical structure.  Arbutin (a sugar derivative of hydroquinone) and kojic acid are examples of structure homologues which are used in skin lightening products.  The substitution of chemical groups to basic structure of Hydroquinone may block melanin production to a greater or lesser degree than Hydroquinone.  In the case of Arbutin and Kojic Acid, they are weaker than hydroquinone, but they avoid some of the systemic problems that are typical of hydroquinone.  Naturally occurring derivatives of Hydroquinone or artificial derivatives synthesized by chemists have permitted the identification of thousands of derivatives which can be tested for strength in inhibiting melanin production.  And from those, the ones which through further testing reveal better safety and performance profile can be adapted for use in the cosmetic and medical treatment of hyperpigmentation disorders.

 

Finding better alternatives to Hydroquinone for hyperpigmentation involved uncovering a way to test the derivatives in a way that would not harm human subjects.

Hydroquinone Blocks Tyrosinase

The target of Hydroquinone is an enzyme in skin cells which produce melanin.   That enzyme is called tyrosinase.  It turns out that human version of this enzyme is structurally and functionally similar to the version of tyrosinase that is present within mushroom species.   And these species generally turn out to be a great testing model for pigmentation blockers like Hydroquinone derivatives.

When isolated apart from Human cells or mushroom sources, tyrosinase catalyzes the chemical reaction that takes the dietary amino acid TYROSINE and converts it to a similar molecule called DOPA.  The process is an oxidation reaction, where oxygen present in the solution is used to form Hydroxyl groups or “Oxide groups”.  The reaction is possible due the presence of two Copper metal ions (cofactor) embedded in the enzyme active site (where the chemical bonds are broken and re-arranged).  The copper ions are capable of changing their oxidation state (similar to the way Iron ions experience the ability to rust) which allows the corresponding change on the substrate molecule (tyrosine) structure.

As for the tyrosinase enzyme in human cells, the process is a bit more complicated.  Tyrosine substrates are converted through the enzyme reaction to DOPA.  The DOPA substance is converted by the same enzyme to DOPAquinone.  And a cascade of reactions occurs using DOPAquinone is able to form long crosslinked 3-dimensional chains which result in the different forms of melanin.

The mushroom tyrosinase reactions can approximate the behavior of human tyrosinase in some cases. But in other cases, the response to blockers related to Hydroquinone are completely different.  So, experiments with tyrosinase in human cells had to be done to determine effectiveness and power.  In so doing, there are great alternatives to Hydroquinone skin lightening products that are stronger and avoid the untoward effects.  They can be used in high doses and for longer periods of time.

With Hydroquinone, More is NOT Better

Naturally, there are people who formulate skin lightening creams, skin lightening lotions containing percentages of Hydroquinone exceeding what the FDA deems as reasonably safe.  As stated previously, there are 10% Hydroquinone skin lightening creams and 20% Hydroquinone creams being sold over the internet by vendors both in the US and Internationally.   Prescription strengths begin at 4% Hydroquinone.  In special cases, doctors may order stronger concentrations than 4% Hydroquinone lotions and creams through special pharmacies called “Compounding Pharmacies”.  This is done in cases where individualized treatment is necessary, recognizing that consequences are complications may occur.  This is the best reason nontraditional doses of hydroquinone need to be done under the direction supervision of a physician who can stop the treatment if systemic problems develop that could endanger the health of the patient.

Problems with Hydroquinone Use

Problems from using Hydroquinone skin lightening creams and lotions for extended periods of time are clear.   Prolonged use can lead to darkening of fingernails, which could take months to reverse.

 

Similar, a rebound hyperpigmentation or darkening of the skin can occur after prolonged use of hydroquinone or high percentages.  This phenomenon of overuse of Hydroquinone skin lightening creams is called Ochronosis.  This rebound darkening is most likely to occur after 6 months of continuous use.  It is seen frequently in Brazil where high doses and percentages can be obtained easily without a prescription.

Unfortunately, there is no convincing evidence that raising the level of Hydroquinone to beyond 10% is helpful or better than the prescription levels. Not only can the skin be affected, but other areas including the whites (Sclera) of the eyes, the ear drum, the cartilage of joint surfaces and even heart valve.  Ochronosis due to Hydroquinone-containing skin lightening cream and lotion can occur with percentages of Hydroquinone as low as 2%.   The fact that 2% Hydroquinone skin lightening cream is over the counter does not mean you will be protected.

There are even reports of using Hydroquinone skin lightening creams as being responsible for skin cancers.  In the final analysis, it may not be worth the risks when there are alternative and better skin lightening products for Black skin and dark spot remover for Black skin and all other skin types that are safer.

 

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