Antihistamine
Mast Cell Stabilizer
Rx Required
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Ketotifen
:
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Ketotifen

.

Capsules, liquid, sublingual
$30-90/month typically
Compounded in USA

How it works

Prevents mast cells from releasing histamine and other inflammatory mediators, while also blocking H1 receptors.

Why compounded?

Oral ketotifen isn't commercially available in the US. Compounding pharmacies create custom formulations.

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What is

Ketotifen

?

Ketotifen fumarate is a benzocycloheptathiophene derivative that works through two mechanisms: it stabilizes mast cells (preventing degranulation and histamine release) and blocks H1 histamine receptors. This dual action makes it particularly useful for conditions involving mast cell activation.

While ketotifen eye drops (Zaditor, Alaway) are available over-the-counter in the US, oral ketotifen is not commercially manufactured domestically. Patients who need oral ketotifen must obtain it through a compounding pharmacy with a valid prescription.

How

Ketotifen

Works

Ketotifen acts on multiple pathways relevant to allergic and inflammatory conditions:

  • Mast cell stabilization β€” prevents release of histamine, leukotrienes, and other inflammatory mediators
  • H1 receptor antagonism β€” blocks histamine effects at target tissues
  • Eosinophil inhibition β€” reduces eosinophil accumulation in tissues
  • PAF antagonism β€” blocks platelet-activating factor

‍

Primary Uses

βœ“ Mast Cell Activation Syndrome (MCAS)

βœ“ Asthma prevention (prophylaxis)

βœ“ Allergic rhinitis & chronic urticaria

βœ“ Eosinophilic Esophagitis (EoE)

Other Applications

βœ“ Eosinophilic gastroenteritis

βœ“ Food allergy adjunct therapy

βœ“ Beta-2 receptor upregulation

βœ“ Interstitial cystitis (investigational)

‍

Dosing Information

⚠️ Note: Dosing should be determined by your prescriber. The information below is general guidance only.

Typical Adult Dosing

MCAS / Allergies

Starting: 0.5-1 mg at bedtime β†’ Target: 1-2 mg twice daily

Asthma prevention

Starting: 1 mg at bedtime β†’ Target: 1-2 mg twice daily

Pediatric

Starting: 0.5 mg at bedtime β†’ Target: 0.5-1 mg twice daily

Titration Tips

  1. Start low β€” drowsiness is common initially and dose-dependent
  2. Take at bedtime initially to manage sedation
  3. Increase by 0.5-1 mg every 5-7 days as tolerated
  4. Allow 2-4 weeks at target dose to assess efficacy

Available Forms

Compounding pharmacies typically prepare ketotifen as capsules (0.5 mg, 1 mg, 2 mg) or oral liquid (1 mg/mL is common). Liquid formulations allow more precise dosing and easier titration, especially for children or those who need very low starting doses.

Common (may improve over time)

  • Drowsiness/sedation β€” most common, usually decreases after 1-2 weeks
  • Increased appetite β€” can lead to weight gain
  • Dry mouth
  • Dizziness

Less Common

  • Headache
  • Nausea
  • Irritability (more common in children)
  • Insomnia (paradoxical)

Managing Side Effects

  • For drowsiness: Take dose at bedtime; start with lowest dose; give it 1-2 weeks to improve
  • For weight gain: Monitor appetite changes; maintain regular eating schedule
  • For dry mouth: Stay hydrated; sugar-free gum can help

Frequently Asked Questions

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