Weißmacher-Rohstoff Tranexamsäure
As the saying goes, “a white cover a hundred ugly”, today and everyone talk about sweeping red and black, let you white to light the messenger – spread bright acid. Tranexamic acid, the scientific name of tranexamic acid, also known as coagulation acid and hemostatic cyclic acid, is a highly efficient and safe medicinal ingredient. It is a synthetic lysine analogue that can be absorbed through the skin and is stable to light. It is not as easily oxidized as vitamin C, nor as irritating as A alcohol, nor as accidentally leaving permanent white spots as hydroquinone.
Tranexamic acid was found
In 1962, Japanese female doctor Okamoto published her findings, the initial purpose of the drug was mainly to prevent postpartum bleeding, but because of the unequal attitude toward professional women in Japan, Okamoto was never able to successfully persuade the obstetrician of the hospital where she worked to try this drug. At the time, the BBC reported the wording of the story: If this long-discovered drug could be taken seriously and given to trauma patients with severe blood loss, at least 100,000 lives could be saved every year. Later, people noticed that it also has an interesting “side effect”, when using this drug to stop bleeding, it was accidentally found that the patient’s skin turned white, and the color spots also subsided. The discovery has given it a place in the cosmetics world. Gold will always shine, with the deepening of observation and research, the current tranamine acid in the field of whitening and tender skin, especially in the prevention and control of melasma and inflammatory pigmentation is famous.
The star course of transbright acid from doubt to wide application
Names like tranexamic acid, thrombotic acid, and tranexamic acid have always raised some doubts:
It’s acid. Does it irritate the skin?
Is it really safe? Does it affect blood clotting?
Does it really work? Why does a clotting drug have a whitening effect?
Which of the several ways it is administered works best?
1. As an artificial amino acid, tranamine acid is neutral and does not irritate skin for external use;
2. It reduces the breakdown of blood clots and reduces post-traumatic bleeding by inhibiting the activity of plasminase. Prevents the clots that have formed and blocked the opening of the blood from being dissolved. However, it does not change the activity of thrombin in the body, so for normal people without blood clots in the blood vessels, it is unlikely to lead to a hypercoagulable state of blood. As long as there’s no blood clots, you can eat almost anything. In this way, dermatologists are crazy about it: efficient whitening, high safety.
3. Doctors first recommended oral pharmic acid at a dose of 500 mg/day for patients with pigmentation, but soon found that if used alone, the effect is not particularly ideal, but also needs to be combined with other systemic treatment drugs such as vitamin C, glutathione, etc., and the taking cycle is longer, compliance is poor, and there are side effects such as retches, gastrointestinal discomfort, and less monthly passing. And problems with drug withdrawal and relapse. In order to become white, some desperate people tried intravenous injection, “whitening needle” was once popular in Hong Kong and Taiwan, and stars flocked to it, but the accumulation of PIH of the needle eye was faster than the speed of white. Probably because it’s systemic, the dose reaching the skin is too small. This is when the water needle enters the public’s field of vision, and for sensitive skin, this operation is too irritating, lasting skin flushing and itching and PIH may occur after surgery. Followed by the use of microneedle beauty plastic and various penetration promotion technologies, came into being.
The medical Tranexamic acid whitening has been deeply explored
1. For the mechanism of vasodilation and hyperplasia
The number and volume of blood vessels in the lesion area of melasma increased significantly, and the increase of blood vessels was more significant, and was positively correlated with pigmentation. Plasminase plays an important role in the angiogenesis process, which can convert extracellular matrix binding vascular endothelial growth factor (VEGF) into soluble, thus promoting angiogenesis. Tranatemic acid is a plasminase inhibitor that directly or indirectly inhibits angiogenesis. Clinical studies have shown that after topical treatment of chloasma with 2% tranatemic acid for 12 weeks, epidermal melanin particles are significantly reduced, the number of CD31-positive blood vessels and VEGF expression are decreased, and the expression of endothelin 1 is also significantly decreased, which confirms that tranatemic acid can inhibit the formation of blood vessels and suppress erythema.
2. Tranexamic acid targeting mast cell mechanism:
Elastic fibrosis and mast cell infiltration were found in the lesion area of melasma, suggesting that photoaging caused by ultraviolet light may be involved in the pathogenesis of melasma, in which inflammatory cells, especially mast cells, play an important role. Mast cell activation can be prevented by inhibitors of aprotinin and plasminase. Tranmitic acid is a plasminase inhibitor. Studies have confirmed that tranmitic acid can inhibit the proliferation and activity of mast cells, which may be one of the mechanisms of its treatment of melasma, but the specific mechanism needs to be further studied and confirmed.
3. Tranexamic acid for basement membrane belt:
In patients with melasma, the basal membrane zone is damaged, and UV irradiation can activate matrix metalloproteinase (MMP) or cause mast cells to release trypsin, which is involved in extracellular matrix injury and basement membrane zone destruction. The treatment of tranmin acid on the basal membrane band of melasma lesions may be related to the inhibition of plasminase, MMP and trypsin.
4. Tranexamic acid prevents melanin production through multiple pathways:
The activity of melanocyte in the epidermis of melasma lesion was enhanced, and the synthesis of melanin was increased. Studies have shown that tranminic acid can prevent the conversion of plasminogen to plasminase, reduce the release of arachidonic acid and prostaglandin E2, and inhibit melanin production. The structure of transom acid is similar to that of tyrosine, which can competitively inhibit tyrosinase activity and reduce melanin synthesis. It can also inhibit melanin synthesis by activating extracellular signaling to regulate the kinase pathway and down-regulate the expression of microphthalmia related transcription factor protein. The pigmentation of melasma is not only related to melanin synthesis, but also to melanin transport. Transom acid is also a serine protease inhibitor, and it is speculated that transom acid may inhibit melanin transport through protease-activated receptor 2 signaling pathway.
5. Tranexamic acid targets the epidermal barrier:
Lipid content in the stratum corneum plays a key role in maintaining the homeostasis of the skin barrier. However, most lipid metabolity-related genes in melasma lesions are down-regulated, and the recovery rate of damaged barrier in the skin lesions is slow, suggesting that there is epidermal barrier dysfunction in melasma. Studies have shown that Tranexamic acid can significantly increase the expression of skin occlusion protein and promote skin barrier repair, which may be one of the important mechanisms of its treatment of melasma.
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