Melatonin

What is the summary?

• Melatonin is a naturally occurring hormone 
• It can be marginally effective for melasma pigmentation
• Melatonin is less effective than conventional medical therapy for melasma
• It can be considered as adjunctive therapy 
• Oral supplementation is better than creams
• Melatonin dose ranges between 3 to 5 mg taken at night

How good is it for melasma pigment?

Melatonin is one of the less powerful pigment correctors for melasma pigmentation, however it can be considered if you are into alternative natural remedies, or if your melasma is resistant to conventional therapies. 

Melatonin is not considered a mainstream treatment for melasma as it serves as a useful adjunctive option. 

What is the best way to take melatonin?

Tablets over fluffy creams is the best method. The dose ranges between 3 to 5 mg melatonin taken orally at night. Though it can be used as a cream, the greatest level of evidence for melasma is oral supplementation. Read more to understand the brands that are available in Australia.

How long before I see results?

Improvement in melasma pigment is seen within 4 to 12 weeks (depending on the papers you read). Melatonin is best used with other medical therapy & of course, sunscreen. 

Obviously melatonin will not work on all cases of melasma pigmentation as the results of any melasma treatment (creams, lasers, peels, oral supplementation etc) is determined on a bell curve response.

What brands of melatonin do we recommend?

2 ways to take this; firstly as prescriptive medication for 5 mg melatonin tablets, or secondly as over the counter melatonin tablets. OTC comes in 2 mg tablets. The dose is 4-5 mg nightly. 

Circadin 2 mg tablets cost $35 for 30 tablets (more expensive option). 

Wagner Health 2mg melatonin tablets $44 for 60 tablets (better option). 

You can buy this from most leading pharmacies in Australia. 

Does melatonin have any side effects?

Melatonin is generally considered safe when used short-term, but it can have side effects in some individuals, they include –

Drowsiness: As melatonin is primarily used to regulate sleep, its most common side effect is daytime drowsiness or grogginess, especially if taken in excessive doses. Fix? Take it earlier than your normal bedtime, eg. 630-730 pm. Still drowsy? Half the dose. 

Headaches: Some users report mild to moderate headaches after taking melatonin, it is usually transient & short lived, so don’t stress. 

Dizziness: Light-headedness or dizziness can occur in some individuals.

Nausea: Melatonin can sometimes cause gastrointestinal issues like nausea or an upset stomach. Solution? Take it with food (eg. dinner). 

What is an example of a skin care routine using melatonin for treating melasma?

A simple melasma skincare routine is as follows: 

AM: Ascorbic acid, ferulic acid, SPF

Midday: Sunscreen reapplication, lotion, stick or spray.

PM: Melatonin supplementation before bedtime, 5 mg. Azelaic acid – arbutin – cysteamine- thiamidol – kojic acid – HQ – retinoid compounded topical cream. 

In the context of melatonin creams, there are no robust studies, hence our recommendation is oral supplementation. If your Google research thesis study has suggested otherwise, knock yourself out on eBay or Amazon.  

Note: The greatest traction of any melasma skincare routine is the correct application of sunscreen. This has a much greater impact on melasma than any marketing objective of any skin care ingredient. 

How good is melatonin for dermal melasma?

Dermal melasma is hard to treat. There are no universally accepted treatments for this condition, however we do combine melatonin with pico lasers & other medical therapies. 

Can I use melatonin long term?

Unlike hydroquinone, melatonin can be used long term without any complications. 

Is melatonin natural?

Yes, melatonin is a natural hormone produced by the pineal gland in the brain. Melatonin is also found in certain foods like tart cherries, grapes, tomatoes, and some grains, and it can be synthesized and made available in supplement form for therapeutic use.

Melatonin’s natural production in the body is influenced by light exposure, with higher levels produced during the night to promote sleep.

Can melatonin be used in pregnancy?

Yes, it can be done safely. Studies have supported melatonin’s use in pregnancy as a sleep regulator. Some studies have suggested that it reduces preeclampsia in pregnancy. 

As of 2025, there are no studies regarding the effectiveness of oral melatonin in pregnant melasma patients. 

What are other supplements that can be used to treat melasma pigmentation?

We do not routinely prescribe supplements for straight forward melasma, primarily because medical therapy has a higher hit rate. Supplementation can be considered in two scenarios-

1. For greenies who elect to have ‘natural treatments for melasma’, namely those who seek alternative, less effective therapies. 
2. For resistant melasma (mixed, genetic driven, deep dermal melasma). In this group we throw in the kitchen skin of melasma supplementation. It goes like this-

• Polypodium leucotomos extract. Dose is 480 g twice daily.
• Melatonin 3-5 mg supplements. 
• Ascorbic acid supplement (not fluff creams but oral supplements). 
• Glutathione orally.  Dose is 500 mg twice daily.

What is the science behind melatonin for melasma pigmentation?

Several studies have explored the potential of melatonin in treating melasma due to its antioxidant and anti-inflammatory properties:

Melatonin for UV-induced Pigmentation: One study demonstrated that topical melatonin could reduce UV-induced pigmentation by neutralizing oxidative stress in skin cells. This is particularly relevant for melasma, as UV exposure is a major trigger for the condition. The study showed that melatonin application reduced the formation of melanin by inhibiting tyrosinase, a key enzyme in melanin synthesis .

Melatonin Combined with Other Ingredients: A clinical trial involving a topical product containing melatonin, vitamin C, and other antioxidants showed improvement in melasma severity. The combination reduced hyperpigmentation while also providing anti-inflammatory effects, helping prevent further darkening caused by UV exposure and oxidative damage .

Melatonin’s Role in Skin Barrier Repair: Another study investigated the role of melatonin in strengthening the skin barrier, which can be compromised in patients with melasma. By enhancing skin barrier function, melatonin can help protect against external triggers like UV rays and pollutants, which exacerbate pigmentation issues  .

These studies suggest that melatonin can be a beneficial adjunct in melasma treatment, especially when combined with other skin-brightening and antioxidant ingredients.

Outcomes of Treatment With Oral Melatonin in Patients With Recalcitrant Melasma

Published: International Journal of Dermatology

In a study by Sarkar et al., the effectiveness of oral melatonin for treating persistent melasma was explored. In the trial, seven patients received 3 mg of melatonin along with broad-spectrum sunscreen for 12 weeks, resulting in a reduction in the modified Melasma Area and Severity Index (mMASI) scores in all participants by the end of the treatment period. Melatonin, produced by the pineal gland, is well-known for regulating sleep cycles, but research has shown it also has roles in managing oxidative stress, melanin production, and immune responses.

Other studies have supported the use of both topical & oral melatonin in managing melasma. Recent research has demonstrated improved efficacy when melatonin is combined with tranexamic acid compared to tranexamic acid alone. Given the small sample size in Sarkar et al.’s trial and similar studies, there is a need for larger, well-structured randomized trials to evaluate both the short- and long-term safety and effectiveness of melatonin as a melasma treatment.

References

1. Kim TK, Lin Z, Tidwell WJ, et al. Melatonin and Its Metabolites Accumulate in the Human Epidermis In Vivo and Inhibit Proliferation and Tyrosinase Activity in Epidermal Melanocytes In Vitro. Mol Cell Endocrinol. 2015;404:1–8. https://www.sciencedirect.com/science/article/abs/pii/S0303720714002469?via%3Dihub
2. Sarkar R, Devadasan S, Choubey V, et al. Melatonin and Oxidative Stress in Melasma — An Unexplored Territory; A Prospective Study. Int J Dermatol. 2020;59(5):572–575. https://onlinelibrary.wiley.com/doi/10.1111/ijd.14827
3. Malankar TE, Thomas M, Gangawane AA, et al. Melatonin: A Paradigm Shift in the Management of Melasma. The American Journal of Cosmetic Surgery. 2023 Dec 11. Online ahead of print. doi: 10.1177/07488068231213416. https://journals.sagepub.com/doi/abs/10.1177/07488068231213416

Publication

Efficacy of oral 5 mg melatonin in the treatment of facial melasma in women: A double-blind, randomized, placebo-controlled clinical trial.

Ingrid Rocha Meireles Holanda et al, January 2024

Journal of The European Academy of Dermatology and Venereology

Results: The study investigated the efficacy of 5 mg oral melatonin in treating facial melasma in women. It was a double-blind, randomized, placebo-controlled clinical trial approved by the FMB-Unesp Institutional Review Board.

Publication

Melatonin and oxidative stress in melasma – an unexplored territory; a prospective study.Rashmi Sarkar. Mar 2020

International Journal of Dermatology.

Results: Melatonin levels are lower in melasma patients, indicating a potential role in oxidative stress. Further research is needed to explore this relationship and potential therapeutic interventions.

What exactly is melatonin (in depth not fluffy explanation)?

Melatonin is a hormone naturally produced by the pineal gland in the brain, primarily responsible for regulating the body’s sleep-wake cycle or circadian rhythm. Its production increases in response to darkness, helping to promote sleep, & decreases during daylight hours. 

Melatonin plays a key role in influencing melasma pigmentation, largely due to its antioxidant properties and its regulation of melanin production. This is the in depth explanation. 

Melatonin inhibits melanin synthesis by reducing tyrosinase activity, a critical enzyme in melanin production, and by downregulating melanogenesis-related genes such as MITF, TYR, TYRP1, and DCT. It also helps limit UVB-induced melanin synthesis by regulating the p53-TYR pathway, thereby reducing premature aging and melanin production in melanocytes.

Furthermore, melatonin protects melanocytes from UVB-induced oxidative stress and DNA damage by activating NRF2-dependent pathways, boosting antioxidative enzymes, and promoting DNA repair. It also reduces reactive oxygen species (ROS) and stimulates ROS scavenging enzyme production. Its antioxidant, anti-inflammatory, and melanin-inhibiting effects position melatonin as a promising treatment option for melasma.