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EspañolRetinoids: Uses, common brands, and safety info
Most people who have searched for skincare products to improve the health or appearance of their skin have come across products that contain retinoids. Retinoids are drugs derived from vitamin A and are the most used and studied anti-aging compounds. They are used to reduce wrinkles, lighten dark spots, reduce acne, and treat many skin conditions. Retinoids are an attractive option for the young and the old, as they improve skin health in many different ways. In this article, we will review different kinds of retinoid products, including how they work, what conditions they can treat, many brand names, and their cost, side effects, and safe use.
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List of retinoids
Other retinoids
Targretin gel (bexarotene)
Retinol (OTC)
Retinol esters (OTC)
Retinaldehyde (OTC)
What are retinoids?
Retinoids are a class of drugs that are derived from vitamin A (retinol) that promote healthy skin. They are available over-the-counter and by prescription and are used for various dermatologic conditions. Retinoids are one of the most common forms of treatment of acne. Their comedolytic properties make them highly effective at preventing clogged pores, so they are commonly sold in health and beauty stores to promote clear skin. According to the American Family Physician Foundation, retinoids are the most effective agents at preventing blocked pores, which is a reason they have been used for over thirty years. Retinoids are available in multiple forms, including gels, creams, ointments, lotions, foams, liquids, and capsules.
How do retinoids work?
Skin afflicted with acne is characterized by skin cells that have slow turnover. Dead cells are not removed quickly enough and build up, blocking pores in the skin. Retinoids bind to retinoic acid receptors (RAR) inside cells, where it activates the expression of specific genes that control the function of skin cells. One result of this gene expression is faster skin cell turnover and faster removal of dead skin cells (exfoliation). By accelerating skin turnover, retinoids also reduce pigmentation (darkening of skin) which effectively lightens dark spots. Retinoids can prevent new dark spots by stopping the transfer of melanosomes to the skin surface. Melanosomes are structures that carry molecules called melanin, which are dark brown or black pigments that darken the skin.
Retinoids also prevent abnormal skin growth by slowing down the formation (proliferation) and growth of new skin cells when they are being produced too quickly (hyperproliferation), as in the case of psoriasis. They also promote collagen growth beneath the skin, improving skin elasticity. They also fight wrinkles and sun damage through their antioxidant activity.
Retinoids block multiple inflammatory pathways that contribute to the inflammatory lesions that are common in acne. They reduce inflammation by inhibiting inflammatory molecules called cytokines. Examples of cytokines inhibited by retinoids include tumor necrosis factor alpha (TNF-a), interleukin-6, and interferon gamma (IFN-γ).
Types of retinoids
First generation retinoids
First generation retinoids are natural and have the closest structure and function to vitamin A. These include retinol, retinal, tretinoin (retinoic acid), isotretinoin, and alitretinoin. While naturally occurring, their use as therapeutic agents are associated with the most toxic effects compared to newer generations, which have been modified to increase their tolerability.
Second generation retinoids
Second generation retinoids are synthetic (man-made) and have similar chemical structure to first generation retinoids. These include etretinate and its metabolite acitretin. These activate all types of retinoic acid receptors but bind poorly to them and are more easily eliminated from the body than first generation retinoids, making them more tolerable.
Third generation retinoids
Third generation retinoids are structurally designed to bind more specifically and effectively with certain retinoic acid receptors (such as retinoid x receptors) and include adapalene, bexarotene, and tazarotene. By targeting specific types of retinoic acid receptors, these have useful clinical applications in cutaneous T-cell lymphoma and psoriasis, among other dermatologic conditions.
Fourth generation retinoids
Most recently, a fourth generation retinoid called Trifarotene was designed to be even more potent and selective for particular kinds of retinoic acid receptors, which makes it more effective with decreased skin irritation and a more tolerable safety profile overall compared to previous generations.
What are retinoids used for?
Retinoids have a broad range of uses related to promoting healthier skin. While many over-the-counter forms of retinoids may be incorporated into cosmetics that improve skin health and appearance (i.e. reducing wrinkles, aging of skin due to UV exposure, etc), this article deals mainly with their medical use in treating dermatological conditions. These include:
Hyperpigmentation
Kaposi's sarcoma
Cutaneous T-cell lymphoma
Post inflammatory hyperpigmentation
Cutaneous lupus erythematosus
Chronic hand eczema
Melasma
Actinic lentigines
Warts
Scalp folliculitis
Who can take retinoids?
Patients of all ages and genders can take retinoids so long as they are not pregnant, breastfeeding (certain retinoids can be used while pregnant breastfeeding), and do not fall into additional categories that disqualify them from specific products. For example, Soriatane (acitretin) cannot be used in patients who have liver damage. Additionally, patients may have to follow certain requirements while taking retinoids to use them safely. Alcohol must be avoided during and after treatment with certain retinoids such as Soriatane.
Before using any retinoid products, tell your doctor about your medical conditions and history and any medications you take, including prescription drugs, OTC medicines, and vitamins or supplements. Having an accurate and complete medical history will ensure that your provider can make the best treatment decision for you.
Can men take retinoids?
Men can take retinoids provided they do not have a hypersensitivity to any of the product components and do not fall into a restricted category for the particular retinoid. Men taking any generic or brand version of isotretinoin must adhere to the iPLEDGE drug safety program requirements to obtain the medication from a participating pharmacy. While the program requirements are fewer for men, they still need to register and participate in the online screening program before each refill of isotretinoin. Men who take any isotretinoin product must not donate blood during and for at least one month following therapy. Men who take Soriatane (acitretin) must not donate blood during and for at least three years following therapy.
Can women take retinoids?
Women can take retinoids as long as they are not pregnant or breastfeeding. Many retinoids must be avoided by pregnant women. Isotretinoin requires strict adherence to the iPLEDGE drug safety program requirements to obtain the medication from participating pharmacies. The primary purpose of this program is to prevent pregnancies in females of childbearing age who are taking retinoids that can cause birth defects. Additionally, the program ensures that patients are aware of mental health problems that isotretinoin may precipitate, such as depression, psychosis, or suicide.
Female patients of childbearing age must agree to use two methods of birth control one month before, while taking, and for one month after taking isotretinoin. They must have two negative pregnancy tests before receiving the first month's supply of isotretinoin. The first pregnancy test will be done by a doctor before the patient is accepted into the program. After, the patient must test each month using a certified laboratory.
Women need a negative pregnancy test before getting each refill, and another test a month after stopping isotretinoin. They must also pick up the prescription within seven days of testing. If a female patient can't get her prescription within this window, she must do another pregnancy test, and answer questions in the iPLEDGE system again.
While isotretinoin is the only retinoid that has a designated computer-based risk management program, other retinoids have similar requirements. For example, Soriatane (acitretin) requires women to do monthly pregnancy tests before, during, and after treatment, and prohibits blood donation during treatment and for three years after treatment.
Can seniors take retinoids?
Generally, older adults can take retinoids as long as they do not have a history of hypersensitivity to the drug, do not fall into a restricted category for the particular retinoid product, and are using them for appropriate conditions. There may be an increased risk of side effects due to slower elimination of drugs in the elderly population.
Are retinoids safe?
Recalls
Akorn, Inc. voluntary recall of Myorisan (isotretinoin) 20 mg capsules due to a package mislabeling (carton labeled 20 mg capsules contain 40 mg capsules in addition 20 20 mg capsules) (January 6, 2020). Affected lots expired in January 2021.
Amneal Pharmaceutical, Inc. voluntary recall of isotretinoin 10 mg capsules due to tretinoin levels above specification limits (October 16, 2019). All affected lots have since expired.
Restrictions
Soriatane (acitretin) and isotretinoin products carry a black box warning stating that they must not be used in female patients who are or may become pregnant. There is an extremely high birth defect risk if pregnancy occurs while using isotretinoin even for a short period of time, during any stage of pregnancy. Birth defects include abnormalities of the face, eyes, ears, skull, central nervous system, cardiovascular system, thymus gland, and parathyroid gland. In addition to these abnormalities, there exists risk for spontaneous abortion, premature birth, and developmental issues such as low IQ score.
Do not take retinoid products if you have a history of a hypersensitivity reaction to its active ingredient or any other components of the product. If you have a history of an allergic reaction to any retinoid products, ask your doctor before using any other retinoid products.
Can you take retinoids while pregnant or breastfeeding?
Oral retinoid products should not be used during pregnancy or while breastfeeding due to their known teratogenic effects. All patients using oral retinoids must participate in a REMS safety program as mandated by the FDA, to assure that risks are properly averted.
Topical retinoids applied to the skins are less likely to harm the unborn child. However, as a precaution, they are still not recommended for use during pregnancy, mainly due to inadequate data regarding their potential to cause fetal harm.
Topical retinoids should generally be avoided while breastfeeding when possible and should be used minimally and with caution due to lack of data regarding infant risk. This means using the retinoid for the shortest time needed and applying to the smallest area of skin as possible. Some topical retinoids such as Renova or OTC products such as Differin may be used while breastfeeding.
Are retinoids controlled substances?
No, retinoids are not controlled substances.
Common retinoids side effects
Retinoid drugs do not come without side effects. Many adverse effects can be reduced or prevented through additional skin care measures, such as using sun protection like a hat or sunscreen, and a moisturizer. The most common side effects of retinoid products include:
Skin dryness
Scaling of the skin
Pruritus (itching)
Less common side effects include:
Skin discoloration
Light sensitivity
Sensitive skin
Initial acne flare-up
Eczema flare-up
Swelling of the skin
Blistering and stinging
This is not a comprehensive list of all possible side effects of retinoid products. Speak with a dermatologist or pharmacist to get a complete list of side effects and to determine whether taking retinoids is appropriate for you.
How much do retinoids cost?
Retinoids vary greatly in price. Most retinoids are available in a generic formulation, with a few exceptions such as Panretin and Aklief. Some brand name retinoids can cost thousands of dollars for a single tube. Fortunately, costs can be drastically reduced by using SingleCare. Soriatane costs over $1500 but you can pay less than $150 by using a free coupon or discount card.
Most Medicare plans cover certain types of retinoids products, at least in their generic form. For example, 99% of Medicare drug plans cover tretinoin, and many cover isotretinoin, tazarotene, acitretin, and bexarotene. Whether you are uninsured or have prescription drug coverage, check out SingleCare for discounts on retinoids—your out-of-pocket costs may be less with a SingleCare coupon even if you have insurance.