Oral TXA (the clinical trial registration number DH-4243) has been shown to be effective against melasma and has been available in Japan as an over-the-counter treatment for melasma since 2007. Despite the important role of mast cells and histamine in the pathogenesis of melasma, anti-histamines have failed to show a benefit in the treatment of this condition. Mast cells may produce vascular endothelial growth factor (VEGF), transforming growth factor-β (TGF-β), and basic fibroblast growth factor (bFGF), all of which promote vascular growth and therefore contribute to the development of melasma. Increased numbers of mast cells have been observed in the skin at the site of melasma lesions. Melasma is a common hyperpigmentation disorder, especially in women of reproductive age who are pregnant or using oral contraceptives. TXA is available as a pharmaceutical cosmetic (quasi-drug containing TXA) that is effective against freckles and other pigment spots, and women with freckles can easily use it as part of their skin-lightening skincare regimen. In addition to inhibiting plasmin, TXA has recently been shown to readily compete with tyrosinase activity and can inhibit hyperpigmentation by decreasing melanin synthesis. In the field of dermatology, TXA at 750–2000 mg per day in 3–4 divided doses have been used in the treatment of skin diseases such as eczema and related conditions, urticaria, drug eruptions, and toxic reactions, and its effects on itching, swelling, erythema, and other symptoms have been established. ![]() Tranexamic acid (trans-4-aminomethylcyclohexanecarboxylic acid TXA, Figure 1) is a drug with approximately 10-fold the anti-plasmin action exhibited by ε-aminocaproic acid and has been used for more than 30 years to treat bleeding tendency and abnormal bleeding potentially related to increased fibrinolysis. To date, approximately 20 quasi-drug whitening active ingredients have been developed for use in Japan.
0 Comments
Leave a Reply. |