Dosage Forms
Excipient information presented when available (limited, particularly for generics); consult specific product labeling.
Solution, Ophthalmic, as besilate:
Bepreve: 1.5% (5 mL, 10 mL) [contains benzalkonium chloride]
Pharmacology
Mechanism of Action
Direct H1-receptor antagonist and inhibits release of histamine from mast cells
Pharmacokinetics/Pharmacodynamics
Absorption
Minimal systemic absorption
Metabolism
Minimal via CYP enzymes
Excretion
Urine (~75% to 90% unchanged)
Onset of Action
Within 3 minutes (Macejko 2010)
Time to Peak
Serum: 1 to 2 hours
Duration of Action
Up to 16 hours (Williams 2011)
Protein Binding
~55%
Use: Labeled Indications
Allergic conjunctivitis: Treatment of itching associated with allergic conjunctivitis
Contraindications
Hypersensitivity to bepotastine or any component of the formulation
Dosage and Administration
Dosing: Adult
Allergic conjunctivitis: Ophthalmic: Instill 1 drop into the affected eye(s) twice daily
Dosing: Geriatric
Refer to adult dosing.
Dosing: Pediatric
Allergic conjunctivitis: Ophthalmic: Children ≥2 years: Refer to adult dosing.
Administration
For topical ophthalmic use only. Contact lenses should be removed prior to application, may be inserted after 10 minutes. Do not insert contacts if eyes are red. Avoid contaminating the applicator tip.
Storage
Store at room temperature of 15°C to 25°C (59°F to 77°F).
Drug Interactions
There are no known significant interactions.
Adverse Reactions
>10%: Gastrointestinal: Dysgeusia (25%)
1% to 10%:
Central nervous system: Headache (2% to 5%)
Ophthalmic: Eye irritation (2% to 5%)
Respiratory: Nasopharyngitis (2% to 5%)
<1%, postmarketing, and/or case reports: Hypersensitivity reaction, pharyngeal edema, pruritus, skin rash, swelling of lips, swollen tongue
Warnings/Precautions
Special populations:
- Contact lens wearers: Contains benzalkonium chloride which may be absorbed by soft contact lenses; remove lens prior to administration and wait 10 minutes before reinserting.
Other warnings/precautions:
- Appropriate use: For topical ophthalmic use only. Not for the treatment of contact lens irritation; do not wear contact lenses if eye is red.
Pregnancy
Pregnancy Considerations
Adverse events were observed in some animal reproduction studies following oral administration. Plasma concentrations are below the limits of detection 24 hours after ophthalmic use. If ophthalmic agents are needed during pregnancy, the minimum effective dose should be used in combination with punctal occlusion to decrease potential exposure to the fetus (Samples 1988).
Patient Education
- Discuss specific use of drug and side effects with patient as it relates to treatment. (HCAHPS: During this hospital stay, were you given any medicine that you had not taken before? Before giving you any new medicine, how often did hospital staff tell you what the medicine was for? How often did hospital staff describe possible side effects in a way you could understand?)
- Patient may experience bad taste, headache, stuffy nose, or sore throat. Have patient report immediately to prescriber vision changes, eye pain, or severe eye irritation (HCAHPS).
- Educate patient about signs of a significant reaction (eg, wheezing; chest tightness; fever; itching; bad cough; blue skin color; seizures; or swelling of face, lips, tongue, or throat). Note: This is not a comprehensive list of all side effects. Patient should consult prescriber for additional questions.
Intended Use and Disclaimer: Should not be printed and given to patients. This information is intended to serve as a concise initial reference for health care professionals to use when discussing medications with a patient. You must ultimately rely on your own discretion, experience, and judgment in diagnosing, treating, and advising patients.
