Ocular itching associated with allergic conjunctivitis
1 drop in each affected eye BID, approximately 8 hours apart
Itch relief begins within 15 minutes of dosing and lasts about 8 hours.
Contraindications
None.
Available Forms
Ophthalmic solution, 0.24% (2.4 mg/mL), 5 mL fill in a 7.5 mL bottle, 7.5 mL fill in a 10 mL bottle, carton of 30 single-use 0.2 mL containers
Mechanism of Action
Topical histamine-1 (H1) receptor antagonist that blocks histamine-mediated ocular itching. In vitro binding shows no measurable affinity for receptors other than H1, with negligible anticholinergic and antiserotonergic activity in animal models.
Warnings & Precautions
Lens wear: Remove lenses before instillation and reinsert 10 minutes afterward; the benzalkonium chloride preservative may be absorbed by soft lenses. Lenses should not be worn while the eye is red.
Lens-related irritation: Not for treating eye irritation caused by contact lens wear.
Tip contamination: Avoid touching the eyelids or surrounding areas with the dropper tip or single-use container tip; keep the multi-dose bottle closed when not in use and discard each single-use container after dosing.
Common Side Effects
Ocular: Ocular hyperemia, instillation site pain and reduced visual acuity, each in approximately 1 to 7% of patients treated with either drug or vehicle across seven trials (cetirizine N=511, vehicle N=329).
Systemic: No systemic reactions listed; plasma Cmax 3.1 ng/mL after one week of BID dosing, roughly 100 times lower than levels after oral cetirizine 10 mg daily.
Pregnancy & Lactation
Pregnancy: No adequate, well-controlled studies in pregnant women; not teratogenic in mice, rats or rabbits at oral doses approximately 1,300 to 7,400 times the maximum recommended human ophthalmic dose. Use only if the potential benefit justifies the potential fetal risk.
Lactation: Oral cetirizine is excreted in human milk; whether topical ocular dosing produces detectable milk levels is unknown, and there are no data on effects on the breastfed infant or on milk production.
Pediatric Use
Safety and effectiveness established in patients 2 years and older.