ATC Class:S01GX08
VA Class:OP900
Ketotifen fumarate is a relatively selective histamine H1-receptor antagonist and mast-cell stabilizer.1
Ketotifen is used for self-medication for the temporary relief of ocular itching associated with allergic conjunctivitis (i.e., conjunctivitis due to pollen, grass, ragweed or animal hair or dander).6, 7 Efficacy for the prevention of such ocular itching was demonstrated in controlled conjunctival allergen challenge studies.1 The onset of action for ketotifen is rapid, with an effect occurring within minutes after ocular administration.1
Avoidance of allergen and other triggering factors (e.g., irritants) and application of cold compresses and lubricating eye drops are the initial means of managing allergic conjunctivitis.2, 3, 4, 5 Drug therapy generally is reserved for use when such avoidance is not possible or is ineffective and can include both prophylactic (e.g., mast-cell stabilizers) and symptomatic (e.g., topical and/or systemic antihistamines, topical vasoconstrictors, topical steroidal and nonsteroidal anti-inflammatory agents [NSAIAs]) therapy.2, 3, 4, 5 The specific therapy(ies) employed will depend on the characteristics and severity of the allergic conjunctivitis.2, 3, 4, 5 For patients with seasonal allergic conjunctivitis, prophylaxis with a mast-cell stabilizer often is initiated before and maintained throughout the pollen season, and symptomatic therapy with other agents (e.g., topical antihistamines, topical NSAIAs) generally is initiated as necessary to provide acute relief.2, 3, 4, 5 Topical corticosteroids usually are reserved for short-term use in patients with moderate to severe symptoms of allergic conjunctivitis.2, 3, 4, 5
Ketotifen fumarate is applied topically to the eye as an ophthalmic solution.6, 7 Care should be taken to avoid contamination of the solution container.6, 7
The manufacturer states that ketotifen fumarate ophthalmic solution should not be used for the symptomatic management of contact lens-related irritation.6, 7 Patients should be advised to remove their contact lenses prior to administration of each dose of ketotifen fumarate ophthalmic solution because the solution contains benzalkonium chloride, which may be absorbed by some soft contact lenses.1, 6, 7 Patients may reinsert contact lenses 10 minutes following administration of the ophthalmic solution.6, 7
Dosage of ketotifen fumarate is expressed in terms of ketotifen.6, 7
The recommended dosage of ketotifen for the temporary relief of ocular itching associated with allergic conjunctivitis in adults and children 3 years of age and older is 1 drop of a 0.025% solution in the affected eye(s) twice daily at an interval of 8-12 hours.6, 7 The drug should not be administered more frequently than twice daily.6, 7
Known hypersensitivity to ketotifen or any ingredient in the formulation.6, 7
For topical ophthalmic use only.6, 7 This preparation should not be used if the solution changes color or becomes cloudy.6, 7
Category C. (See Users Guide.)1
Ketotifen is distributed into milk in rats following oral administration.1 It is not known if topical ocular administration could result in sufficient systemic absorption to produce detectable distribution in breast milk; therefore, caution should be exercised when ocular ketotifen is administered to a nursing woman.1
Safety and efficacy not established in children younger than 3 years of age.6, 7 Ketotifen fumarate ophthalmic solution should not be used in children younger than 3 years of age unless otherwise directed by a clinician.6, 7
Conjunctival injection, headaches, and rhinitis occur in 10-25% of patients.1 Some events may be related to the underlying ocular disease rather than ketotifen.1
Minimally absorbed following topical application to the eye.1
Within minutes after topical application to the eye.1
Ketotifen fumarate is a relatively selective histamine H1-receptor antagonist and mast-cell stabilizer.1 Ketotifen suppresses the release of mediators from cells involved in hypersensitivity reactions and decreases chemotaxis and activation of eosinophils.1
Importance of learning and adhering to proper administration techniques to avoid contamination of the product.6, 7
Importance of delaying insertion of contact lenses for at least 10 minutes after ketotifen instillation, since benzalkonium chloride preservative may be absorbed by soft lenses.1, 6, 7
Not indicated for contact lens-related ocular irritation.6, 7
Emphasis on the need to report new-onset eye pain/discomfort, visual disturbances, eye redness, worsening of itching, or itching lasting for longer than 72 hours.6, 7
Importance of seeking prompt medical attention if preparation is ingested orally.6, 7
Importance of women informing clinicians if they are or plan to become pregnant or plan to breast-feed.1
Importance of informing clinicians of existing or contemplated concomitant therapy, including prescription and OTC drugs, as well as any concomitant illnesses.6, 7
Importance of informing patients of other important precautionary information.6, 7 (See Cautions.)
Additional Information
Overview (see Users Guide). For additional information until a more detailed monograph is developed and published, the manufacturer's labeling should be consulted. It is essential that the manufacturer's labeling be consulted for more detailed information on usual cautions, precautions, contraindications, potential drug interactions, laboratory test interferences, and acute toxicity.
Excipients in commercially available drug preparations may have clinically important effects in some individuals; consult specific product labeling for details.
Please refer to the ASHP Drug Shortages Resource Center for information on shortages of one or more of these preparations.
Routes | Dosage Forms | Strengths | Brand Names | Manufacturer |
|---|---|---|---|---|
Ophthalmic | Solution | 0.025% (of ketotifen) | Alaway® | Bausch & Lomb |
Zaditor® | Novartis |
AHFS® Drug Information. © Copyright, 1959-2025, Selected Revisions July 1, 2009. American Society of Health-System Pharmacists, Inc., 4500 East-West Highway, Suite 900, Bethesda, MD 20814.
1. Novartis Ophthalmics. Zaditor® (ketotifen fumarate) ophthalmic solution prescribing information. Duluth, GA; 2002 Oct (draft).
2. Ciprandi G, Buscaglia S, Cerqueti PM et al. Drug treatment of allergic conjunctivitis: a review of the evidence. Drugs . 1992; 43:154-76. [PubMed 1372215]
3. Morrow GL, Abbott RL. Conjunctivitis. Am Fam Physician . 1998; 57:735-46. [PubMed 9490996]
4. Titi MJ. A critical look at ocular allergy drugs. Am Fam Physician . 1996; 53:2637-42. [PubMed 8644576]
5. Galindez OA, Kaufman HE. Coping with the itchy-burnies: the management of allergic conjunctivitis. Ophthalmology . 1996; 103:1335-6. [PubMed 8841290]
6. Novartis. Zaditor® (ketotifen fumarate) drug facts. 2007. From Zaditor website ([Web]). Accessed 2007 Sep 26.
7. Bausch & Lomb. Alaway® (ketotifen fumarate) ophthalmic solution 0.025%: antihistamine eye drops. From Bausch & Lomb website ([Web]). Accessed 2007 Sep 27.