Is tranexamic acid (TXA) available as a cream or serum?

Tranexamic Acid Formulations: Cream and Serum Availability

Yes, tranexamic acid is available in both cream and serum formulations for topical application, in addition to its more common oral and intravenous forms.

Available Formulations of Tranexamic Acid

Tranexamic acid (TXA) comes in multiple formulations:

• Topical formulations:

  • Cream: Used for dermatological conditions
  • Serum: Used for dermatological applications
  • Solution: Can be applied topically for various conditions

• Other formulations:

  • Oral tablets: For systemic administration 1
  • Intravenous solution: For acute bleeding management 1

Clinical Applications of Topical Tranexamic Acid

Dermatological Use

Topical TXA formulations (creams and serums) are primarily used for:

• Melasma and hyperpigmentation
• Post-inflammatory hyperpigmentation

Other Topical Applications

• Epistaxis (Nosebleeds): Topical TXA can be applied directly to control acute nosebleeds, showing higher rates of bleeding control compared to anterior nasal packing 1
• Surgical Applications: Topical application during surgery (as a solution) to reduce bleeding:
  • Can be applied by moistening wound surfaces (20 ml of 25 mg/ml solution)
  • Can be administered as a bolus into wound cavities (200 ml of 5 mg/ml solution) 2
• Ophthalmology: Eye drops (100 mg/ml solution) can be used to achieve therapeutic intraocular concentrations while minimizing systemic exposure 3

Pharmacokinetics of Topical Application

When applied topically, TXA demonstrates:

• Lower systemic absorption: Peak serum concentrations after topical application (4.9-5.2 μg/ml) are significantly lower than after intravenous administration (66.1 μg/ml) 2
• Delayed absorption: Peak concentrations occur 80-359 minutes after topical application versus 6 minutes after IV administration 2
• Higher local tissue concentrations: Topical application to the eye results in higher aqueous humor concentrations (15 μg/ml) compared to IV administration (9 μg/ml) 3

Safety Considerations

Topical TXA formulations generally have favorable safety profiles:

• Minimal systemic effects: Due to low serum concentrations after topical application 2
• Local side effects: May include:
  • Skin irritation
  • Dryness
  • Contact dermatitis

Clinical Pearls and Caveats

• Topical TXA is not FDA-approved for all applications where it's commonly used, particularly in dermatology
• For epistaxis, TXA can be applied using cotton soaked with the solution and inserted into the nose 1
• The method of topical application affects absorption:
  • Surface moistening provides more predictable absorption
  • Bolus administration into cavities results in more variable serum concentrations 2
• When using TXA for nosebleeds, it should be applied to the active bleeding site after proper anesthesia 1

Dosing for Topical Applications

• For epistaxis: Solution applied to cotton and inserted into the nose 1
• For surgical applications:
  • Surface moistening: 20 ml of 25 mg/ml solution
  • Cavity application: 200 ml of 5 mg/ml solution 2
• For ophthalmic use: One drop (0.05 mL) of 100 mg/mL solution every 8 hours 3

Topical TXA represents an effective local treatment option with minimal systemic exposure, making it particularly valuable for patients who may be at risk for systemic side effects from oral or IV administration.