Melasma – a difficult-to-treat pigmentation disorder that most commonly affects skin of III–VI Fitzpatrick types. The treatment of melasma is based on an integrated approach with the use of photoprotective agents, brightening preparations, as well as skin resurfacing procedures. New knowledge about the pathogenesis of melasma allows specialists to develop new effective methods of treating melasma, which replenish the arsenal of dermatologists and cosmetologists. This article estet-portal.com describes new topical and oral drugs for the treatment of melasma.
- Melasma pathogenesis and factors that increase the risk of pigmentation disorders
- Current approaches to the treatment of melasma
- New topical and oral drugs for the treatment of melasma
Melasma pathogenesis and factors that increase the risk of pigmentation disorders
Melasma – pigmentation disorders with complex pathogenesis. A number of pathways leading to the development of melasma have been established. etiological factors include:
- genetic predisposition;
- UV exposure;
- hormonal changes.
The affected areas of the skin are characterized by increased expression of stem cell growth factor, c-Kit and alpha-melanocyte-stimulating hormone. Markers indicate a high degree of oxidative stress, as well as a change in the Wnt signaling pathway and a violation of the barrier function of the skin. Melasma is also accompanied by solar elastosis, increased mast cells, vascular damage, impaired barrier function, and fatty acid abnormalities.
Current approaches to the treatment of melasma
For melasma commonly used:
- hydroquinone;
- azelaic acid;
- kojic acid;
- glycolic acid;
- salicylic acid;
- tretinoin.
The gold standard for treating melasma continues to be hydroquinone. Many studies show that combination formulas based on hydroquinone, retinoid and corticosteroid provide the best treatment results, the concentration of which can vary. After therapy the disease often recurs.
Melasma should be treated with a holistic approach that includes the use of sunscreens, antioxidants, brightening agents, exfoliants and, if necessary, resurfacing treatments.
Second line therapies such as chemical peels and laser resurfacing are effective in some patients, but they come with a risk of acute and long-term complications, especially in dark-skinned patients.
New topical and oral melasma treatments
Tranexamic acid
Tranexamic acid (TK) – a synthetic lysine derivative, a fibrinolytic agent that blocks the formation of plasmin from plasminogen and thus prevents the binding of plasminogen to keratinocytes.
TK also reduces:
- release of arachidonic acid;
- synthesis of prostaglandin and fibroblast growth factor, which stimulate the synthesis of melanin;
- number of mast cells;
- angiogenesis.
Photos before (A) and after (B) melasma treatment with 3% tranexamic acid and hydroquinone
TA preparations are available for oral, topical, intradermal, and microneedling delivery.
Oral tranexamic acid is prescribed at an average dose of 250 mg, taken twice a day.
Several studies confirm the effectiveness of TA in the treatment of melasma – decrease in MASI index and no serious adverse events.
The largest retrospective study on the treatment of melasma with tranexamic acid was conducted in Singapore. The authors analyzed data from 561 patients with melasma. Improvements after therapy with tranexamic acid occurred in 90% of them. Adverse events, mostly of moderate severity, occurred in 40 patients (7.1%).
TC is contraindicated in patients with a history of bleeding disorders and thromboembolism.
Possible adverse events after TA:
- moderate discomfort in the gastrointestinal tract;
- hypomenorrhea;
- allergic rash;
- alopecia;
- moderate elevation of alanine transaminase.
TA for oral administration is prescribed with caution, having previously studied the patient's history and eliminating the risk of complications.
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Studies compared topical TA (liposomal form, 5% concentration) and hydroquinone 4%, as well as TA suspension (3% concentration) and a preparation based on hydroquinone 2%, dexamethasone 0.01% and vitamin C) . The results demonstrated that the effectiveness of topical TA and hydroquinone is comparable.
Melatonin
The hormone melatonin – powerful antioxidant that stimulates superoxide dismutase, glutathione reductase and glutathione peroxidase. Melatonin also inhibits alpha-melanocyte-stimulating hormone receptors.
Topical and oral melatonin preparations were evaluated in 36 patients with melasma and 10 healthy controls. After 90 days of use, there was a significant decrease in the MASI index, as well as a decrease in the level of oxidative stress.
Read also: Cysteamine-based cream in the treatment of melasma: case studies
Glutathione
Glutathione – one of the most powerful endogenous antioxidants produced by the cells of the human body. Glutathione brightens the skin by inhibiting tyrosinase and inhibiting the synthesis of eumelanin and pheomelanin.
Research has shown that intravenous glutathione for skin lightening and treatment of melasma carries a risk of serious side effects such as Stevens-Johnson syndrome and anaphylaxis.
Glutathione for oral and topical application is well tolerated, does not cause serious side effects and, according to studies:
- 500 mg glutathione orally – moderate skin lightening in 90% of 30 patients after 8 weeks;
- topical application of glutathione suspension 2% – significant reduction in melanin index compared to placebo group after 10 weeks.
Cysteamine
Cysteamine Hydrochloride – degradation product of the amino acid L-cysteine, which is naturally produced in the human body. Cysteamine protects cells from the mutagenic and other lethal effects of ionizing radiation. Recent placebo-controlled studies support the efficacy of topical 5% cysteamine in the treatment of melasma.
Pigment Correcting Serum
The newly created pigment-correcting serum prevents:
- melatinocyte activation;
- melanos maturation;
- melanin synthesis;
- transportation by melanos;
- differentiation and desquamation of keratinocytes.
The composition of the serum includes TA, tetrapeptides, plankton extracts, niacinamide, phenylethyl resorcinol and undecylenoyl phenylalanine.
In a study of 43 patients, the serum showed efficacy in the treatment of post-inflammatory hyperpigmentation comparable to hydroquinone 4%.
Methimazole
Methimazole – an oral drug used to treat hyperthyroidism. When applied topically, the drug has a depigmenting effect. Methimazole – a powerful peroxidase inhibitor that blocks melanin synthesis. It has been used in patients with melasma and post-inflammatory hyperpigmentation.
Read also: Correction of hyperpigmentation: the choice of effective treatments for melasma
Topical methimazole 5%, has been shown to be detectable in serum in minimal amounts and does not cause thyroid dysfunction. The drug is well tolerated, causes minimal side effects on the skin. Significant changes in the levels of thyroid hormone, free thyroxine and free triiodothyronine were not recorded during the studies. It is recommended to apply only to melasma-affected areas of the skin.
Flutamide
The non-steroidal antiandrogen flutamide blocks the action of endogenous and exogenous testosterone by binding to androgen receptors.
Efficacy of flutamide 1% has been shown to be comparable to hydroquinone 4% in studies. However, satisfaction is higher in the flutamide group.
Melasma – a chronic condition that is difficult to treat and often recurs. Melasma is treated with a holistic approach that includes sunscreens, antioxidants, brightening agents, exfoliants, and resurfacing treatments. New drugs for oral and topical treatment of melasma allow expanding the arsenal of tools to combat this pigmentation disorder.
Adapted from International Journal of Women’s Dermatology.
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