Ketotifen is a second-generation antihistamine and mast cell stabilizer used primarily for the prophylactic management of allergic conditions, including allergic conjunctivitis, allergic rhinitis, and certain forms of asthma and urticaria. It functions by inhibiting the release of inflammatory mediators from mast cells, thereby reducing hypersensitivity reactions. Its dual mechanism offers both immediate and long-term control, making it a cornerstone in allergy management protocols. Available in oral and ophthalmic formulations, it is valued for its efficacy and favorable safety profile in both adult and pediatric populations.

Features

• Contains ketotifen fumarate as the active pharmaceutical ingredient
• Available in oral syrup, tablet, and ophthalmic solution formulations
• Exhibits both potent H1-antihistamine and mast cell-stabilizing properties
• Rapid onset of action with sustained prophylactic effects
• Suitable for long-term use with minimal risk of tolerance
• Compatible with a wide range of patient demographics, including children over 3 years

Benefits

• Provides effective prevention and reduction of allergic symptoms such as itching, redness, sneezing, and rhinorrhea
• Reduces frequency and severity of asthma exacerbations in allergic asthma patients
• Minimizes reliance on rescue medications like short-acting bronchodilators or topical steroids
• Offers convenient once or twice-daily dosing depending on formulation, supporting adherence
• Demonstrates a well-established safety profile with extensive clinical use worldwide
• Improves quality of life by enabling better control over chronic allergic conditions

Common use

Ketotifen is commonly prescribed for the prophylaxis and treatment of allergic disorders. Its primary indications include allergic conjunctivitis (via ophthalmic solution), allergic rhinitis, and mild to moderate allergic asthma. It is also used off-label in conditions such as chronic urticaria, atopic dermatitis, and mast cell activation syndrome. In pediatric populations, it is often selected for its safety and palatable syrup formulation. Clinical use emphasizes preventive administration rather than acute symptom relief.

Dosage and direction

Oral administration (tablets/syrup):
Adults and children over 3 years: 1 mg twice daily. May be increased to 2 mg twice daily in adults under medical supervision.
Ophthalmic solution:
Adults and children over 3 years: One drop in each affected eye twice daily, approximately 8–12 hours apart.

Administration should begin prior to anticipated allergen exposure for optimal prophylactic effect. Oral doses may be taken with or without food. Patients should not wear contact lenses while using ophthalmic formulations. Dosage adjustments may be necessary in hepatic impairment.

Precautions

Use with caution in patients with hepatic impairment, renal dysfunction, or a history of seizures. Sedation may occur, particularly at therapy initiation; patients should avoid driving or operating machinery until individual response is ascertained. Periodic liver function tests may be advised during long-term therapy. Pregnancy Category C: use only if potential benefit justifies potential risk. Excretion in breast milk is probable; caution advised during lactation.

Contraindications

Hypersensitivity to ketotifen or any component of the formulation. Contraindicated in patients with acute asthma attacks or status asthmaticus. Not recommended in children under 3 years of age. Avoid use in patients with angle-closure glaucoma when using ophthalmic solution.

Possible side effect

Common: drowsiness, dry mouth, mild dizziness, irritability (in children), weight gain.
Less common: headache, nausea, rhinitis, pharyngitis.
Rare: thrombocytopenia, hepatitis, seizures, anaphylaxis.
Ophthalmic: burning/stinging upon instillation, conjunctival hyperemia, corneal erosion.

Drug interaction

Potentiated sedation with CNS depressants (alcohol, benzodiazepines, opioids). Ketotifen may enhance effects of anticholinergic drugs. Concurrent use with MAO inhibitors is not recommended. No clinically significant interactions with theophylline or inhaled corticosteroids have been reported.

Missed dose

If a dose is missed, take it as soon as remembered unless it is nearly time for the next dose. Do not double the dose. Resume regular dosing schedule.

Overdose

Symptoms may include severe drowsiness, disorientation, tachycardia, and hypotension. Gastric lavage and symptomatic supportive care are recommended. There is no specific antidote. Hemodialysis is not effective due to high protein binding.

Storage

Store at room temperature (15–30°C). Protect from light and moisture. Keep oral formulations in tightly closed containers. Do not freeze. Keep out of reach of children.

Disclaimer

This information is for educational purposes and does not replace professional medical advice. Always consult a healthcare provider for diagnosis, treatment decisions, and personalized dosage recommendations. Do not initiate or discontinue therapy without medical supervision.

Reviews

“Ketotifen has significantly reduced my perennial allergic conjunctivitis symptoms. The twice-daily drops are easy to use and provide sustained relief without rebound redness.” – Maria L., 42
“As a pediatric allergist, I find ketotifen syrup invaluable for young patients with multi-system allergies. It’s effective and well-tolerated, with fewer behavioral side effects than some alternatives.” – Dr. A. Reynolds, MD
“After years of seasonal asthma exacerbations, starting ketotifen prophylactically has cut my rescue inhaler use by over 70%. Life-changing preventive care.” – James K., 51