What is ketotifen?
Ketotifen is an antihistaminic agent of the first generation with a unique double effect: it blocks H1 histamine receptors and at the same time stabilizes mast cells so that less histamine is released. This makes it not only symptomatic, but also preventive.
Ketotifen is used orally as tablets or syrup and topically as eye drops. The eye drops (e.g. Zaditen® ophtha) are particularly popular with allergic conjunctivitis (binding skin inflammation) and can be used both acutely and prophylactically.
Oral form is used in allergic asthma, allergic rhinitis and allergic skin diseases. Ketotifen has a slow dosage and requires a few weeks to develop its full mast cell stabilizing effect.
Active Ingredients & Mechanism of Action
Active ingredient: Ketotifenfumarat
Ketotifen has a dual effect:
1. Antihistamines effect:
- Blocking of H1 histamine receptors
- Immediate relief from itching, sneezing, tear flow
- Works on eyes, nose and skin
**2. Mast cell stabilization:* *
- inhibits degranulation of mast cells
- Less histamine and other inflammatory mediators are released
- Preventive effect with regular application
- This effect only starts after 2–4 weeks
More properties:
- inhibits phosphodiesterase (inflammatory)
- Reduces the eosinophilic activation
- Works bronchodilatatorically on allergic asthma
Initiation of action:
- Antihistamines effect: within 1–2 hours
- Mast cell stabilization: After 2–4 weeks of regular intake
Who is it suitable for?
Ketotifen is suitable for:
Oral:
- Prophylaxis and treatment of allergic diseases
- Allergic asthma bronchiale (prophylactic)
- Allergic rhinitis and conjunctivitis
- Allergic skin diseases
Augen drop:
- Allergic conjunctivitis
- Seasonal and perennial eye symptoms
- Adults and children from 3 years
Especially recommended at:
- Patients who have both eye and nose symptoms
- Prophylactic treatment before pollen season
- Allergic asthma as an additional therapy
Not suitable:
- Oral form: Not first choice for sedation
- Not for acute treatment of asthma attacks
Available Dosages
Oral – Adults:
- initial dose: 1 mg in the evening (slowly dosed)
- Maintenance dose: 1 mg in the morning and 1 mg in the evening
- Maximum dose: 2 mg twice a day
Oral – Children (6 months to 3 years):
- 0.5 mg (0.25 ml syrup) twice a day
Augen drop (Zaditen® ophtha):
- 1 drop twice a day in each affected eye
- Morning and evening
Available dosage forms:
- 1 mg capsules / tablets
- 1 mg/5 ml syrup
- 0.25 mg/ml eye drops
Application duration:
- Oral: minimum 2–3 months for full effect
- Eye drops: throughout the allergy season
How to Take
Oral intake:
- Start in the evening (due to fatigue in the initial phase)
- Slowly increase over 1–2 weeks to full dose
- With or without food
- Don't suddenly drop (slow)
Augen drop:
- Wash hands before application
- Remove contact lenses before (15 minutes wait for typing)
- Add drops to the conjunctive bag
- Keep an eye close
- Tear point 1 minute easy to press
Important notes:
- The oral form makes especially initial tired – start taking in the evening
- Full mast cell stabilizing effect only after 2–4 weeks
- Not suitable for acute treatment of asthma attacks
- Do not drop existing asthma medication
Contraindications
**Ketotifen may not be taken at:* *
- hypersensitivity to ketotifen or other components
- Acute asthma attacks (oral – not effective in case of acute)
Preview at:
- Epilepsy (oral – ketotifen can lower the cramping threshold)
- Simultaneous intake of antidiabetics (oral form can trigger thrombocyte-like states)
- liver or kidney malfunction
pregnant and breastfeeding: There are no sufficient data for oral form. Eye drops: Low systemic intake, however recommended medical consultation. Ketotifen goes to breast milk.
Augen drop:
- Preservant can discolor contact lenses
- Do not apply to eye infections without medical clarification
Possible Side Effects
Oral – Frequently (1–10 %):
- fatigue and sedation (especially at the beginning, often after 1–2 weeks)
- Mouth dryness
- Squeeze
- Weight gain (for long-term use)
- Increased appetite
Oral – Occasionally:
- Headaches
- nausea
- Nervosity (in children)
- Sleep disorders
Augendriving – Frequently:
- Easy to burn when dripping
- Eye irritation
- Obscured vision (surrounding)
Augendriving – Occasionally:
- Condensation
- Eye dryness
- Headaches
** Oral fatigue is the main disadvantage of ketotifen. It leaves in most patients after 1–2 weeks. The eye drops have a much better compatibility profile.
Interactions
Oral intake:
- Alcohol and CNS Damping Substances: Enhanced Sedation
- Oral antidiabetics: Possible reversible thrombocytopenia (same)
- Antihistamines: Additive effect
- Sedativa, sleeping pills: reinforced sedation
Augen drop:
- Hard systemic interactions due to low exposure
- Keep your eye drops 5 minutes away
** In the case of oral administration, the sedative action in combination with alcohol or other sedative drugs is particularly relevant. Clinically relevant interactions are rare in the eye drops.
Frequently Asked Questions
Similar Medications
Is ketotifen right for you?
A licensed doctor will review your information and issue a prescription if suitable. Discreet and secure.
Important Notice
This information does not replace medical advice. If you have questions about your health or the suitability of this medication, please consult a doctor. Read the package leaflet before use.





