Effectiveness of Oral Tranexamic Acid in the Treatment of Melasma: A Systematic Review
Abstract
Melasma is a skin condition characterized by hyperpigmented patches, generally appearing on facial areas such as the cheeks, forehead, and upper lip. This condition is more common in women, especially during pregnancy or when using hormonal contraceptives. The factors that cause melasma include sun exposure, hormonal changes, and genetic factors. The purpose of this study is to examine the effectiveness and safety of the use of oral Tranexamic acid (TXA) in the treatment of melasma based on recent studies. The method used by literature search in journals published between 2022–2024 used keywords related to oral TXA and melasma. Studies that met the inclusion criteria were evaluated to compare the outcomes of oral TXA therapy based on dose, duration, and side effects. The results showed that oral TXA was proven to be effective in reducing the Melasma Area Severity Index (MASI) score with a dose of 500–1500 mg/day for 8–12 weeks. A significant decrease in MASI scores was achieved at week 12, showing consistent results across multiple studies. The most commonly reported side effects are gastrointestinal disorders, such as nausea and abdominal pain. Oral TXA does not cause serious side effects at doses up to 4 g/day. Tranexamic acid (TXA) in oral form is an effective and safe therapy in managing melasma. However, further research is needed to determine the ideal duration of treatment and strategies in preventing melasma recurrence.
References
AbdElrahman, S. E. A., Mohamed, M., Farag, M., Ali, A., Abdallah, E., Moussa, H. M., & Mohamed, A. (2023). Clinical and dermoscopic evaluation of the efficacy of melasma treatment with oral tranexamic acid. NILES Journal for Geriatric and Gerontology, 6(2), 517–545.
Adebusoye, O. C., & Srivastava, G. (2025). Clinical approaches in vogue for combination therapies for acne and post-inflammatory hyperpigmentation–A comprehensive review. Cosmoderma, 5. https://doi.org/10.1016/j.jaad.2017.01.036
Agrawal, M., Varma, K., Kumar, U., Bhargava, S., Mahadik, A., & Agrawal, V. (2023). Comparison of oral versus topical tranexamic acid for treatment of melasma. Age (Years), 30, 28. http://dx.doi.org/10.18231/j.ijced.2023.015
Akl, E. M. (2022). Liposomal azelaic acid 20% cream vs hydroquinone 4% cream as adjuvant to oral tranexamic acid in melasma: A comparative study. Journal of Dermatological Treatment, 33(4), 2008–2013. https://doi.org/10.1080/09546634.2021.1905765
Ankad, B. S., Nikam, B. P., Drago, N., & Narkhede, N. (2021). Hyperpigmentary disorders. Dermoscopy-Histopathology Correlation: A Conspectus in the Skin of colour, 145-183. http://dx.doi.org/10.1007/978-981-33-4638-3_6
Asditya, A., & Sukanto, H. (2017). Studi retrospektif: Profil pasien melasma (Profile of melasma patients: A retrospective study). Laser, 1, 2.
Bala, H. R., Lee, S., Wong, C., Pandya, A. G., & Rodrigues, M. (2018). Oral tranexamic acid for the treatment of melasma: a review. Dermatologic Surgery, 44(6), 814-825. https://doi.org/10.1097/dss.0000000000001518
Batra, J., Brar, B. K., Kumar, S., & Arora, H. (2022). Tranexamic acid in melasma: Comparative evaluation of therapeutic efficacy of oral tranexamic acid versus its transepidermal administration. Journal of Cutaneous and Aesthetic Surgery, 15(4), 394–399. https://doi.org/10.4103/jcas.jcas_237_20
Botsali, A., Esme, P., Erbil, H., & Caliskan, E. (2022). Comparison of fractional erbium: YAG laserassisted tranexamic acid delivery alone and in combination with oral tranexamic acid in melasma. Lasers in Medical Science, 37(7), 2823–2830. https://doi.org/10.1007/s10103-022-03547-7
Cassiano, D. P., Espósito, A. C. C., Hassun, K. M., de Andrade Lima, M. M. D., de Andrade Lima, E. V., Miot, L. D. B., Miot, H. A., & Bagatin, E. (2022). Histological changes in facial melasma after treatment with triple combination cream with or without oral tranexamic acid and/or microneedling: A randomised clinical trial. Indian Journal of Dermatology, Venereology and Leprology, 88(6), 761–770. https://doi.org/10.25259/ijdvl_126_2021
Cassiano, D. P., Espósito, A. C. C., Hassun, K. M., de Andrade Lima, M. M. D., de Andrade Lima, E. V., Miot, L. D. B., ... & Bagatin, E. (2022). Histological changes in facial melasma after treatment with triple combination cream with or without oral tranexamic acid and/or microneedling: A randomised clinical trial. Indian Journal of Dermatology, Venereology and Leprology, 88(6), 761-770. http://dx.doi.org/10.25259/IJDVL_126_2021
Chatterjee, M., & Vasudevan, B. (2014). Recent advances in melasma. Pigment International, 1(2), 70-80. http://dx.doi.org/10.4103/2349-5847.147044
Das, P. C., & Akhtar, D. (2023). Hyperpigmented macules and patches: Localized. In Atlas of Clinical Dermatology in Coloured Skin (pp. 19-38). CRC Press.
Davis, E. C., & Callender, V. D. (2010). Postinflammatory hyperpigmentation: a review of the epidemiology, clinical features, and treatment options in skin of color. The Journal of clinical and aesthetic dermatology, 3(7), 20.
Fijen, L. M., Bork, K., & Cohn, D. M. (2021). Current and prospective targets of pharmacologic treatment of hereditary angioedema types 1 and 2. Clinical Reviews in Allergy & Immunology, 61(1), 66-76. https://doi.org/10.1007/s12016-021-08832-x
Guo, L., Liu, X., Liu, Q., Xie, X., & Jiang, X. (2024). Treatment of melasma with tranexamic acid essence combined with iontophoresis: A randomized, double-blind, placebo-controlled clinical trial. Drug Design, Development and Therapy, 3659–3666. https://doi.org/10.2147/dddt.s472922
Gupta, A., Sharma, V., & Verma, R. (2022). Epidemiology and pathogenesis of melasma. Journal of Dermatology.
Kim, H. J., Moon, S. H., Cho, S. H., Lee, J. D., & Kim, H. S. (2017). Efficacy and safety of tranexamic acid in melasma: a meta-analysis and systematic review. Acta Dermato-Venereologica, 97(7), 776-781.. https://doi.org/10.2340/00015555-2668
Latha, S. (2019). Comparative Study of Efficacy and Safety of Oral Tranexamic Acid with Topical Triple Combination Cream Containing Fluticasone Propionate 0.05%, Tretinoin 0.025% and Hydroquinone 2% Versus Topical Triple Combination Alone in the Treatment of Melasma (Doctoral dissertation, Rajiv Gandhi University of Health Sciences (India)).
Li, T. J., & Tan, C. (2023). Hyperpigmentation Coexisted with Hypopigmentation. In Atlas of Pigmentary Skin Disorders (pp. 411-434). Singapore: Springer Nature Singapore. http://dx.doi.org/10.1007/978-981-19-5634-8_17
Liu, L.-X., Liao, Z.-K., Dong, B.-Q., Jiang, S., & Lei, T.-C. (2024). Tranexamic acid ameliorates skin hyperpigmentation by downregulating endothelin-1 expression in dermal microvascular endothelial cells. Annals of Dermatology, 36(3), 151. https://doi.org/10.5021/ad.23.108
Maeda, K. (2022). Timeline of the development of skin-lightening active ingredients in Japan. Molecules, 27(15), 4774. https://doi.org/10.3390/molecules27154774
Mushtaq, F., Marwat, R. K., Saleem, M., Khan, A., Khan, S., & Imran, H. (2024). Comparison of efficacy of 5% tranexamic acid vs 20% azelaic acid in patients with melasma. Journal of Health and Rehabilitation Research, 4(1), 591–595. https://doi.org/10.61919/jhrr.v4i1.465
Mustofa, A., Hapsari, A. N., Nabiila, A., Putri, A. K., Nurissyita, A. M., & Catur, E. (2021). Faktor risiko depresi pasca persalinan di negara-negara Asia Tenggara. Medica Arter, 3(2), 62–67. https://doi.org/10.26714/medart.3.2.2021.62-67
Nautiyal, A., & Wairkar, S. (2021). Management of hyperpigmentation: Current treatments and emerging therapies. Pigment cell & melanoma research, 34(6), 1000-1014. https://doi.org/10.1111/pcmr.12986
Prathyoosha, S., Ananditha, K., Rao, T. N., Gopal, K. V. T., & Raju, P. V. K. (2024). A randomized study to evaluate the efficacy of oral tranexamic acid, modified Kligman’s formula, and placebo cream in melasma. Indian Dermatology Online Journal, 15(5), 787–793. https://doi.org/10.4103/idoj.idoj_797_23
Rao, S. K., Rajashekar, T. S., & Ashraf, A. (2022). Efficacy of intralesional tranexamic acid in melasma: Assessment with melasma area severity index and dermatology quality of life index. Turkderm-Turk Arch Dermatol Venereol, 56, 58–63. http://dx.doi.org/10.4274/turkderm.galenos.2022.42709
Raza, M. H., Iftikhar, N., Anwar, A., Mashhood, A. A., Tariq, S., & Hamid, M. A. B. (2022). Split-face comparative analysis of micro-needling with tranexamic acid vs vitamin c serum in melasma. Journal of Ayub Medical College Abbottabad, 34(1), 169-172. https://doi.org/10.55519/jamc-01-9840
Sandhu, S., Neema, S., & Radhakrishnan, S. (2021). Dermoscopy of disorders of hyperpigmentation. Pigment International, 8(1), 14-24. http://dx.doi.org/10.4103/Pigmentinternational_40_20
Santos, L. C., Lana, G. L., Santos, G. S., Visoni, S. B. C., Brigagão, R. J., Santos, N., ... & Lana, J. F. (2024). The biological role of platelet derivatives in regenerative aesthetics. International Journal of Molecular Sciences, 25(11), 5604. https://doi.org/10.3390/ijms25115604
Sarwar, U., Munir, A., Ashraf, A., Khan, I. H., Tariq, H., Rashid, S., & Bokhari, M. A. (2023). Efficacy of oral tranexamic acid in patients with melasma. Journal of Pakistan Association of Dermatologists, 33(2), 519–524.
Tawanwongsri, W., Siri-Archawawat, D., Sindhusen, S., & Eden, C. (2024). Therapeutic efficiency and safety assessment of intradermal platelet-rich plasma combined with oral tranexamic acid in patients with facial melasma. Advances in Clinical and Experimental Medicine: Official Organ Wroclaw Medical University. https://doi.org/10.17219/acem/187874
Triyanti, M. N. (2022). Tinjauan Atas Efikasi Asam Traneksamat Oral untuk Terapi Melasma. Cermin Dunia Kedokteran, 49(8), 465-468. http://dx.doi.org/10.55175/cdk.v49i8.290
Verma, P., & Yadav, K. S. (2023). Novel formulations for topical delivery of tranexamic acid: assessing the need of epidermal targeting for hyperpigmentation disorders. Expert Opinion on Drug Delivery, 20(6), 773-783. https://doi.org/10.1080/17425247.2023.2206645
Wang, Y., Zhao, J., Jiang, L., & Mu, Y. (2021). The application of skin care product in melasma treatment. Clinical, Cosmetic and Investigational Dermatology, 1165-1171. https://doi.org/10.2147/ccid.s323748
Widgerow, A., Wang, J., Ziegler, M., Fabi, S., Garruto, J., Robinson, D., & Bell, M. (2022). Advances in Pigmentation Management: A Multipronged Approach. Journal of Drugs in Dermatology, 21(11), 1206-1220. https://doi.org/10.36849/jdd.7013
Wikurendra, E. A. (2018). Pengaruh penyuluhan cuci tangan pakai sabun terhadap sikap mencuci tangan siswa. Jurnal Ilmiah Kesehatan Media Husada, 7(2), 64–69. https://doi.org/10.33475/jikmh.v7i2.21
Wulandari, P. (2021). Asam traneksamat oral sebagai terapi melasma. Cermin Dunia Kedokteran, 48(4), 255–260. https://doi.org/10.55175/cdk.v48i4.69
Zhang, C., Wu, T., & Shen, N. (2022). Effect of platelet-rich plasma combined with tranexamic acid in the treatment of melasma and its effect on the serum levels of vascular endothelial growth factor, endothelin-1, and melatonin. Pakistan Journal of Medical Sciences, 38(8), 2163. https://doi.org/10.12669/pjms.38.8.6786
Zuniarto, A. A., TW, S. P., & Kinanti, V. P. (2025). Effectiveness of Oral Tranexamic Acid in the Treatment of Melasma: A Systematic Review. Journal La Medihealtico, 6(2), 326-337. https://doi.org/10.37899/journallamedihealtico.v6i2.1929
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