Can Tranexamic Acid Help in Treating Melasma? Find Out the Truth! 

Melasma: A Brief Overview

Melasma, often referred to as chloasma, is a chronic skin disorder that presents itself as dark brown or grey hyperpigmented patches on the skin. The melasma symptoms commonly appear on the facial skin, usually on the cheeks, foreheads, the nose's bridge, the part above the upper lip, and the chin. Melasma can also occasionally develop non-facial body parts in some individuals, usually on the forearm and the neck. 

Why does Melasma occur?

The specific reason which causes melasma is yet to be discovered. However, after several studies, dermatologists have attributed various factors that can cause melasma over the years. Two of the most common causes among them are exposure to the sun and hormonal fluctuation.

1. Exposure to sun rays:  

The UV rays from the sun can over-stimulate the melanocytes or the pigment-producing cells of the skin in certain areas of your face and body on prolonged exposure. The aggravated melanocytes go on an overdrive and produce an increased amount of melanin and form dark, discolored patches and spots on the skin.

Smaller spots can fade on their own over time, but larger patches might require external aid to lighten. Sun-induced melasma can exacerbate during the summer months and can worsen the condition of healing lesions. Thus, it is essential to keep your skin protected from harmful sun rays.  

2. Fluctuation of Hormone Levels: 

Hormonal imbalance, too, can play a role in inducing the development of melasma. Women experience fluctuation in their hormonal levels during pregnancy, which can cause melasma. These lesions are also known as Chloasma or the 'Mask of pregnancy.' Hormonal Imbalance may also occur if the individual is under any hormonal medication such as contraceptive pills, hormone replacement therapy, etc.; such conditions might also induce the development of Melasma.

Facts about Melasma you should know:  

Melasma can also occur due to genetic disposition. It has been found that ethnicity plays a major role in the development of Melasma in an individual. According to epidemiological surveys, it was found that Latin/Hispanic, North American, African-American, Asian, Indian, Middle Eastern, and people of Mediterranean descent are more susceptible to developing melasma.

Apart from being more prevalent in darker-skinned individuals, it has been found that Melasma is more predominant in the female population. Though Melasma can occur in both males and females, on average, the female to male ratio is found to be 9:1.

However, epidemiological studies on Brazillian patients with melasma found the female to male ratio to be 34:1. Whereas another study done on melasma patients among the Indian population deduced the ratio to be 4:1.

Melasma is a relatively non-invasive type of skin disorder that has no harmful effect on the skin's health. However, blotchy discolored patches on the face can have a profound psychological impact on some individuals. Marks on the skin can lower their self-esteem and make them feel undesirable. Thus, the skincare industry has come up with several ingredients and products that can reduce melasma symptoms.

One such incredible ingredient that has risen to popularity for the treatment of melasma is Tranexamic Acid.

Scroll down to find out how tranexamic acid can help and what does science have to say about it.  

Tranexamic Acid: What is it? 

This acid was first formulated in 1962 by two Japanese researchers. Since then, this ingredient has been used to treat or prevent excessive blood loss from major trauma or postpartum bleeding, various surgeries, and heavy menstruation. Administered via the mouth or injected in the vein, Tranexamic acid has become one of the medical fields' major discoveries. It has been included in the World Health Organization's List of Essential Medicines.

Speaking of chemistry, Tranexamic acid, abbreviated as TXA, is trans-4-aminomethyl cyclohexane carboxylic acid. It is an antifibrinolytic agent that mimics the amino acid lysine and takes its place in the plasminogen molecules' lysine-binding site.

This, in turn, prevents the breakdown of the protein called fibrin, which is responsible for clotting of blood. This property of tranexamic acid to obstruct the process of fibrinolysis is a boon for people with genetic blood disorders such as hemophilia, who can bleed to death even from a small cut.

The property of tranexamic acid to prevent blood clots from breaking down also proves beneficial for women suffering from heavy postpartum bleeding or heavy menstrual bleeding. 

How Does Tranexamic Acid Work on Melasma? 

The use of Tranexamic acid or TXA for the treatment of Melasma is a recent recommendation. It is perhaps the first medication that can be taken orally for melasma. However, tranexamic acid can also be administered as topical or intralesional preparation.  

Did you Know?

Enjoy first reported the use of tranexamic acid for melasma in 1979. The beneficial effect of TXA on Melasma was discovered by accident when a patient with Melasma was also suffering from chronic urticaria and was prescribed TXA treatment.  

Let's talk science

Exposure of the skin to harsh sun rays causes the synthesis of plasmin activator, which leads to an increase in plasmin activity in the keratinocytes. The plasmin released induces the further release of Arachidonic acid via phospholipase A2. The Arachidonic acid/ AA can promote Prostaglandin E2 synthesis, which is responsible for enhancing melanogenesis.

Repeated exposure to the harmful UV rays also increases mast cell tryptase production, damaging the melanocytes' basement membrane. All these events together induce the development of melasma.

Ingesting hormone-regulating pills regularly or birth control pills can also increase serum plasminogen activator level, resulting in increased melanogenesis. A similar effect is also observed during pregnancy.

Tranexamic acid interferes with the plasminogen binding to the keratinocytes and thus prevents UV-induced pigmentation. This, in turn, reduces free Arachidonic acid and thereby decreases prostaglandins in the melanocytes.

For the treatment of Melasma, dermatologists have suggested oral administration of Tranexamic acid at a low dose of 250 mg two times a day. TXA is also available in 2% emulsion, 3% cream and is also prepared as a 5% solution. It can also be administered at a concentration of 4mg/ml as an intradermal injection.  

What does research have to say? 

A clinical study worth mentioning in this context is conducted by Wu et al. In the study, 74 women with Melasma were administered 250 mg TXA tablets twice daily for six months. At the end of the study, here's what was observed:  

• About 96% of the subjects showed significant improvement.  
  
• 5.4% of the subjects developed some gastrointestinal discomfort.  
  
• And about 8.1% of the subjects developed hypomenorrhea.  
  
• No severe adverse reactions were encountered.  
  

However, it was also noted that the administration of tranexamic acid showed no improvement in skin hyperpigmentation other than melasma, freckles, and lentigines.

Apart from this, several other clinical trials and literature reviews prove the efficacy of tranexamic acid in different forms for the treatment of Melasma.  

What Other Beneficial Effects Can You Expect from Tranexamic Acid?  

• Tranexamic acid can significantly reduce bleeding due to trauma and has proven to be a life-saving medication. It can show improvement in cerebral hemorrhages within three hours of ingestion and reduce death risk.
  
• Tranexamic acid is often used along with oxytocin to reduce postpartum bleeding and is among the essential drugs used during childbirth.
  
• The TXA preparation is also used in orthopedic surgery to reduce perioperative blood loss. It is also used in spinal surgeries or other surgical cases like craniosynostosis, coronary artery bypass surgery, etc., to prevent excessive blood loss. 
  
• Tranexamic acid is also used in dentistry as a 5% mouth rinse after tooth extraction or other dental surgeries to reduce blood loss. It is especially useful for patients with acquired or inherited bleeding disorders.  
  
• Tranexamic acid is also useful for nosebleeds, hemoptysis, hereditary angioedema, hereditary hemorrhagic telangiectasia, and various other bleeding disorders.   
  

Potential Side Effects of Tranexamic Acid: 

Usually, Tranexamic acid can cause minor side effects. As the body gets accustomed to the compound with regular use, the side effects might go away independently and do not require any medical attention. The common side effects include: 

• Nausea and vomiting 
  
• Gastrointestinal discomfort 
  
• Diarrhea 
  
• Chills and fever 
  
• Throbbing headache 
  
• Back and joint pain 
  
• Muscle pain and stiffness
  
• Difficulty in movement
  
• Runny or stuffy nose 
  

However, in some cases, certain individuals have experienced some adverse effects of a higher degree. Though rare, some people might experience anaphylactic shock with symptoms such as shortness of breath, fast heart rate, tightness in the chest, flushing in the face, skin rash and hives, swelling, itching.

Some other serious side effects include: 

• Severe Coughing  
  
• Anxiety and confusion 
  
• Unusual bleeding and bruising 
  
• Fatigue 
  
• Pallor 
  
• Changes in vision or other eye problems 
  

Are there any long-term side effects of Tranexamic Acid? 

Generally, tranexamic acid does not pose any long-term adverse reaction. Once the body gets used to the ingredient, TXA is well-tolerated.  

Does Tranexamic Acid Interact With Other Drugs?

Some drugs can react adversely with Tranexamic acid. Thus, if you are already under specific medication, it is recommended to consult with your doctor before using any TXA preparations. These are drugs that are not advised to take along with TXA medications: 

1. Hormonal Birth Control Devices and Drugs: 

Taking Tranexamic acid and using intrauterine devices, vaginal rings, or while consuming birth control pills can increase the risk of blood clots, stroke, and heart attacks. The risk is more if you smoke regularly.  

2. Anti-inhibitor Coagulant Complex 

This medication is prescribed to reduce excessive bleeding, and TXA is not recommended to take along with it.  

3. Chlorpromazine 

Chlorpromazine is an antipsychotic medicine. Taking TXA, along with it, might reduce its efficacy and also increase the risk of bleeding.

4. Tretinoin 

Tretinoin is a type of retinoid prescribed to treat acute promyelocytic leukemia, a type of cancer. If TXA is taken along with tretinoin, it might cause excessive bleeding.  

The Bottom Line 

Though a recent addition in the medical field, Tranexamic acid has proven to be of great benefit. Apart from its ability to reduce bleeding, tranexamic acid is said to improve melasma. Though some side effects have been reported, TXA preparation is an excellent solution for the undesirable melasma patches on your skin.