Tranexamic acid 250mg 60 capsules pigmentation/melasma treatment/ whitening

Description

Tranexamic Acid (TXA) for Pigmentation and Melasma

1. Overview:

Tranexamic acid is a synthetic derivative of the amino acid lysine. It primarily functions as an antifibrinolytic by inhibiting plasminogen activation. In dermatology, TXA is increasingly used for the treatment of melasma, post-inflammatory hyperpigmentation (PIH), and UV-induced pigmentation due to its ability to interfere with melanogenesis.

2. Mechanism of Action in Pigmentation Disorders:

• Inhibits melanocyte activation: TXA blocks the interaction between keratinocytes and melanocytes by inhibiting the plasminogen/plasmin system. This reduces the release of inflammatory mediators like arachidonic acid and prostaglandins that stimulate melanin synthesis.
• Vascular component: It reduces neovascularization in melasma by downregulating VEGF (vascular endothelial growth factor), which contributes to the improvement of dermal-type melasma.
• Reduces UV-induced pigmentation: By inhibiting plasmin, it reduces the production of melanocyte-stimulating factors after UV exposure.

3. Forms of TXA Used in Aesthetic Dermatology:

• Oral TXA:
  • Dose: 250 mg twice daily for 8–12 weeks (commonly used in Asian studies).
  • Often combined with topical or procedural therapies.
• Topical TXA:
  • Concentration: 2–5% cream or serum.
  • Often used in combination with other depigmenting agents such as niacinamide, kojic acid, or vitamin C.
• Injectable TXA (Mesotherapy or Microneedling):
  • Dose: 4–6 mg/ml, injected intradermally or used with microneedling in melasma-prone areas.

4. Indications in Dermatology:

• Melasma (epidermal, dermal, or mixed types)
• PIH (especially after acne, lasers, or trauma)
• UV-induced pigmentation
• Pigmentation associated with vascularity (telangiectasia in melasma)

5. Contraindications:

• Personal or family history of thromboembolic disorders (e.g., DVT, PE, stroke, MI)
• Use of combined oral contraceptive pills (COCPs) – increased risk of thrombosis
• Active intravascular clotting disorders
• Hypersensitivity to TXA
• Severe renal impairment (due to renal excretion of the drug)
• History of seizure disorders – TXA lowers seizure threshold, especially with IV use

6. Adverse Effects:

• Oral use:
  • Gastrointestinal upset (nausea, diarrhea, abdominal discomfort)
  • Headache
  • Menstrual irregularities
  • Risk of thrombosis (rare at low doses in healthy individuals)
• Topical use:
  • Mild skin irritation
  • Erythema or contact dermatitis (rare)
• Injectable use:
  • Mild local discomfort or erythema
  • Risk of bruising

7. Clinical Results & Duration:

• Visible improvement typically within 4–8 weeks
• Best results seen with combination therapy (e.g., TXA + sunscreen + topical depigmenting agents + procedural support like microneedling or laser)
• Relapse is common if sun protection and maintenance therapy are not continued

8. Drug Interactions & Precautions:

• Avoid concurrent use with estrogens (e.g., hormonal therapy, contraceptives)
• Caution with anticoagulants or patients at risk of bleeding/clotting disorders
• Routine blood tests are not required for low-dose oral TXA in healthy patients, but it may be advisable to assess coagulation profile in at-risk individuals before starting.

9. Patient Selection Tips:

• Best suited for refractory melasma or patients who have plateaued on topical treatments alone
• Ideal for those who can commit to strict photoprotection
• Caution in patients with vascular risk factors or on hormonal treatments

10. Summary Protocol Example (Melasma Management):

• Oral TXA: 250 mg BID for 12 weeks
• Topical TXA: 3% serum daily or BID
• Microneedling: With 5 mg/ml TXA solution monthly for 3 sessions
• Combine with:
  • SPF 50+ sunscreen daily
  • Depigmenting agents (e.g., 4% hydroquinone at night)
  • Antioxidants (vitamin C) in the morning
  • Monthly or bi-monthly maintenance treatments post-clearance