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Hydroquinone: Over-the-Counter and Prescription Forms

Hydroquinone: Over-the-Counter and Prescription Forms

While relatively unknown to many, the CARES Act included a provision that restricted the sale of hydroquinone products over-the-counter. The debate over when to ban OTC hydroquinone products has been going on for many years but it was not until the CARES Act that it was actually enacted. The smaller legislation was given the opportunity to be enacted by including it along with the larger bill. The main concern with OTC hydroquinone was that it was being overused and misused by patients who were using it unmonitored by a healthcare provider.

How Does Hydroquinone Work?

Hydroquinone decreases the production of pigment in the skin, which can be useful for treating melasma and other types of dark spots and hyperpigmentation. It is often used in combination with retinoic acid and hydrocortisone. Often treatment takes many weeks or even months for results to be noticed. For sensitive skin, hydroquinone may be irritating however it is typically well tolerated. Changing the frequency of application may help reduce irritation. Sunscreen use is essential as skin may become more sensitive to UV radiation. In addition you do not want to create more hyperpigmentation when you are trying to treat it.

The mechanism of hydroquinone’s action is that it inhibits tyrosinase, which is an enzyme related to the production of melanin. It will reduce hyperpigmentation in the epidermis (top layer of skin) but not in the dermis (deeper layer of skin). The change in pigmentation that is made by hydroquinone is reversible and not a permanent alteration in the skin. If you suffer from  melasma and stop hydroquinone treatment, it is possible for your melasma to flare up again.

What Happened to Hydroquinone OTC?

Hydroquinone can be toxic when used inappropriately. The main concern is exogenous ochronosis, which can occur with overuse of hydroquinone. This condition causes the skin’s pigmentation to turn blue-black. There are various stages of severity ranging from mild, which may be confused with melasma, to more severe which includes nodules/cysts. Exogenous ochronosis is challenging to treat with few available options. In some cases chemical peels or lasers may be used. Misuse of hydroquinone, or use of hydroquinone in certain skin types, is the leading cause of exogenous ochronosis. If there are any signs that the condition is developing treatment with hydroquinone must be discontinued.

The issue with OTC hydroquinone according to the FDA is that its use is not monitored by a healthcare provider and it is in the non-GRASE category (discussed more below). The effects of hydroquinone – whether it is working and if it is causing any side effects – are not always noticeable to someone without training in treating skin conditions. Especially when it comes to managing one’s appearance, some individuals may go overboard with the hydroquinone use hoping that its effects will work faster or be more significant. However treatment with hydroquinone takes time and is often done in treatment courses with breaks in between.

The CARES Act did not specifically mention that hydroquinone should not be an OTC product. Instead it changed the way that OTCs in general are regulated. Some drug products that were on the market prior to the act did not have final monographs but were available under a category called “not-GRASE” or not generally recognized as safe and effective. These products were commercially available until the FDA was able to determine an official monograph. However the CARES Act makes it so that these not-GRASE products must be removed from the market until there is an FDA approved monograph. Hydroquinone was entered into the non-GRASE category due to concerns about its cancer risk as demonstrated in studies on rats. No evidence or association with cancer has been shown in its many years of human use. However the FDA determined the evidence was insufficient and therefore there could not be a definitive conclusion.

Prior to the ban on OTC hydroquinone, numerous formulations were available online from a variety of skincare retailers as well as sites like Amazon. All of them have now been removed. A review article with affiliate links on the top OTC hydroquinone products shows this with a top ten list of links to Amazon — all with pages that have been removed. This change in policy means that any patient looking for a hydroquinone product must consult a dermatologist and that the formulations with hydroquinone can only be obtained from a compounding pharmacy.

Prescription vs. OTC

The main difference between prescription and OTC hydroquinone (when it was available) was the strength of the active ingredient. OTC formulations typically included up to 2% hydroquinone. Prescription formulations can be 4% or higher. Compounded formulations sometimes include 6, 8, or even 10% hydroquinone. Hydroquinone in both prescription and OTC formulations has been used without serious adverse effects for many years in the United States. A compounding pharmacy can also make hydroquinone in combination with other ingredients like retinoic acid and kojic acid.

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