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Tranexamic Acid

A twice-daily capsule for melasma. Tranexamic acid quiets a signal that tells pigment cells to make more pigment, which can lighten melasma that creams alone haven’t cleared. It’s taken twice a day, usually alongside a lightening cream and daily sunscreen, and prescribed off-label for melasma, compounded at a low dose in the strength your provider sets.

  • Compounded low-dose capsules, 120 per bottle
  • Twice a day, alongside your cream and sunscreen
  • Off-label for melasma, after a check of your clot risk

Twice-daily capsule · from $150/2 months. Prices are preliminary.

How to use it

  1. Take one capsule twice a day, about 12 hours apart, with or without food.
  2. Wear a broad-spectrum sunscreen every day, and keep using your lightening cream if you have one.
  3. Stop and get emergency care for pain or swelling in one leg, chest pain or sudden shortness of breath, signs of a stroke, or any change in your vision.
Form
Capsule, 120 per bottle, about 2 months
Strength
Low dose, usually 250 mg; your provider sets it
Typical use
One capsule twice a day, for at least 3 months
Who it’s for
Adults with melasma who don’t have a raised risk of blood clots, if a provider decides it’s right for them

One active, at a low dose.

  • Tranexamic acid (Low dose, usually 250 mg): Blocks plasmin, a signal that skin cells and sunlight use to push pigment cells to make more melanin. At far higher doses it’s an FDA-approved treatment for heavy periods.

What the research does and doesn’t show

In a placebo-controlled trial, women taking 250 mg twice a day for 3 months saw their melasma improve by about half, against about a fifth on placebo; 3 months after stopping, much of that gain had faded. In a records study of 561 people, about 9 in 10 improved, and about 1 in 4 relapsed. In pooled trials, adding tranexamic acid to a lightening cream gave better results and fewer relapses than the cream alone.

So it helps most people with melasma while they take it, alongside a cream and daily sunscreen, and it’s an off-label use.

Studies: Del Rosario et al., J Am Acad Dermatol 2018 (44 women, 250 mg twice daily vs placebo for 3 months; mMASI −49% vs −18%; PMID 28987494); Lee et al., J Am Acad Dermatol 2016 (561 patients; PMID 27206758); meta-analysis of oral tranexamic acid added to triple-combination cream, 4 trials, 490 patients (PMID 38848545); tranexamic acid tablets prescribing information (DailyMed).

What to expect

Weeks 4–8
Melasma often starts to lighten within the first 2 months. Side effects are usually mild: an upset stomach, a headache, or lighter periods.
Month 3
In a placebo-controlled trial, melasma improved by about half after 3 months, against about a fifth on placebo.
After you stop
Melasma often comes back, especially with sun: in that trial much of the gain faded within 3 months of stopping. Your provider plans how long to continue and how to keep your results.

Important safety information

Before you start

Your provider reviews your health history, medicines and allergies before prescribing, and prescribes only if it’s right for you. Tell your care team about any side effect, and get emergency care for chest pain, trouble breathing, or swelling of the face, lips or throat.

Side effects, and when to get help

Usually mild: an upset stomach or bloating, a headache, and lighter or irregular periods. Get emergency care for pain or swelling in one leg, chest pain, sudden shortness of breath or coughing up blood, a drooping face, arm weakness, trouble speaking or a sudden severe headache, throat tightness or trouble breathing. Stop the capsules and get care for any change in your vision.

Rules that keep it safe

Don’t take it with birth control that contains estrogen (most pills, the patch or the ring), if you’re pregnant, or if you’ve ever had a blood clot, a stroke or a blocked blood vessel in the eye, or have a clotting disorder. Tell your clinician if you smoke, have kidney disease, take any other estrogen, or have surgery or a long flight or drive coming up. Wear sunscreen every day.

Is it FDA-approved?

No. These capsules are compounded: prepared by a licensed pharmacy for you, and not reviewed by the FDA for safety, effectiveness or quality. Tranexamic acid tablets are FDA-approved only for heavy menstrual bleeding, at much higher doses, so using it for melasma is off-label.

About Tranexamic Acid

Why a capsule if I already use a cream?

Melasma has several causes, and creams work on the pigment in the skin. Tranexamic acid works on one of the signals that drive it. In pooled studies, adding it to a lightening cream gave better results and fewer relapses than the cream alone.

What about blood clots?

That’s the main safety question, because tranexamic acid helps blood clot. At the low doses used for melasma, studies haven’t shown a clear rise in clots, but people with a history of clots, a clotting disorder, or estrogen birth control were left out, so they shouldn’t take it. Your provider checks your risk first.

How long do I take it?

Usually at least 3 months, then your provider reviews how it’s going and plans how long to continue.

Will my melasma come back?

It often does, especially with sun. Daily sunscreen and a lightening cream help keep results, and your provider can plan a maintenance course.

Can I take it with my birth control?

Not with methods that contain estrogen: most pills, the patch and the ring. If you use one of those, your provider can talk through other options.

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