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Ketotifen

  • Ophthalmic antiallergicsOphthalmic antiallergics

An antihistamine eye drop that also steadies mast cells. It relieves the itch of allergic conjunctivitis for several hours.

Updated

Quick facts

Group
Ophthalmic antiallergics
Target
Histamine H1 receptor (plus mast cell stabilisation)
Used for
Itching of allergic conjunctivitis
Key effects
Burning or stinging of the eye · Headache · Dry eye
Monitor
Relief of itching · Eye pain or vision change
ATC
S01GX08

No doses: the clinician sets them by the current guideline.

Mechanism of action

The figure shows desloratadine, another H1 antihistamine, in the human H1 receptor; ketotifen blocks the same receptor.

Target in 3D: Histamine H1 receptor (plus mast cell stabilisation). PDB structure 8X64 (RCSB PDB, public domain). View the structure at RCSB PDB

Ketotifen blocks histamine H1 receptors in the conjunctiva and reduces mediator release from mast cells. Blocking histamine relieves itching quickly; the mast cell action helps limit further allergic symptoms.

  1. Ketotifen blocks conjunctival H1 receptors
  2. It also lowers mast cell mediator release
  3. Itching eases within minutes

Indications

Adverse effects

Common

  • Burning or stinging of the eye
  • Headache, runny nose
  • Dry eye, eye discharge, light sensitivity
  • Blurred vision

Contraindications

  • Hypersensitivity to ketotifen or any component
  • Not for contact-lens irritation

Key interactions

Other eye drops
Spaced a few minutes apart so they are not washed out

What is monitored

  • Relief of itching
  • Eye pain or vision change

Administration and safety

  • Contact lenses come out before the drop and go back in at least 10 minutes later; no lenses while the eye is red.
  • The bottle tip should not touch any surface; the cap is replaced after use.
  • A solution that changes colour or turns cloudy is not used.
  • Oral ketotifen exists in some countries for other uses; the eye drop is a separate product.

Pregnancy and breastfeeding

Human data are limited; with little systemic absorption from the eye, it is used only if the benefit justifies the risk.

Nursing care

  • Confirm the problem is allergic itching, not pain or loss of vision.
  • Teach drop technique and lens removal.
  • Teach to seek review if itching worsens or lasts more than a few days.

Pharmacokinetics

Onset and duration
Relief within minutes, lasting several hours

Test yourself

Think of the answer, then tap the question to see it.

Which receptor does ketotifen block?

The histamine H1 receptor.

Besides H1 blockade, what else does it do?

It reduces mediator release from mast cells.

Should it be used for contact-lens irritation?

No; it treats allergic itching only.

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Connections

← Back to the class: Ophthalmic antiallergics

Educational content on how drugs work; not a prescribing guide and no substitute for a health professional's advice. No doses are given.

Sources: DailyMed - KETOTIFEN FUMARATE OPHTHALMIC SOLUTION- ketotifen fumarate solution/ drops (DailyMed (U.S. National Library of Medicine), 2026); Ketotifen Ophthalmic: MedlinePlus Drug Information (MedlinePlus (U.S. National Library of Medicine), 2026); ATCDDD - ATC/DDD Index (WHO Collaborating Centre for Drug Statistics Methodology, 2026); RCSB PDB - 8X64: CryoEM structure of the histamine H1 receptor-BRIL/Anti BRIL Fab complex with desloratadine (RCSB Protein Data Bank, 2026).

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Representative model, for educational purposes only.