What are the side effects and contraindications of Bepirex (bepotastine) eye drops?

Side Effects and Contraindications of Bepirex (Bepotastine) Eye Drops

Bepirex (bepotastine besilate) ophthalmic solution is contraindicated in patients with a history of hypersensitivity reactions to bepotastine or any of the other ingredients in the formulation. 1

Common Side Effects

Bepotastine besilate ophthalmic solution has a generally favorable side effect profile, with the following common adverse reactions:

• Mild taste following instillation (occurs in approximately 25% of patients)
• Eye irritation (occurs in 2-5% of patients)
• Headache (occurs in 2-5% of patients)
• Nasopharyngitis (occurs in 2-5% of patients) 1

Rare Side Effects

Post-marketing surveillance has identified rare hypersensitivity reactions, which may include:

• Itching
• Body rash
• Swelling of lips, tongue, and/or throat 1

Contraindications

The only absolute contraindication for bepotastine besilate ophthalmic solution is:

• History of hypersensitivity reactions to bepotastine or any other ingredients in the formulation 1

Special Considerations and Precautions

Contact Lens Wear

• Bepotastine should not be used to treat contact lens-related irritation
• Contact lenses should be removed prior to instillation
• Benzalkonium chloride (preservative) may be absorbed by soft contact lenses
• Lenses may be reinserted 10 minutes following administration 1

Contamination Prevention

• Patients should avoid touching the dropper tip to eyelids or surrounding areas
• Keep the bottle tightly closed when not in use to minimize contamination 1

Pregnancy Considerations

• No available human data for use during pregnancy
• Animal studies did not show adverse embryofetal effects at clinically relevant exposures
• The background risk of major birth defects in the general U.S. population is 2-4% 1

Proper Administration

For optimal therapeutic effect and to minimize side effects:

1. Instill one drop into the affected eye(s) twice a day
2. Remove contact lenses prior to instillation
3. Wait 10 minutes before reinserting contact lenses 1

Pharmacological Properties

Bepotastine besilate is a second-generation H1-antihistamine with:

• Selective histamine H1-receptor antagonist activity
• Mast cell stabilizing properties
• Anti-inflammatory effects
• Inhibitory effects on eosinophilic activity 2, 3

These properties contribute to its effectiveness in treating ocular itching associated with allergic conjunctivitis, with onset of action within 15 minutes and duration of action of at least 8 hours after administration 4, 5.

Unlike some older antihistamines, bepotastine has negligible affinity for receptors associated with undesirable adverse effects, including histamine H3, adrenergic, serotonin, muscarinic, and benzodiazepine receptors, which contributes to its favorable side effect profile 3.

Clinical Pearls

• Bepotastine besilate ophthalmic solution has been shown to reduce not only ocular symptoms but also some nonocular symptoms of allergic conjunctivitis, such as nasal congestion and rhinorrhea 6
• If artificial tears are needed more than four times per day in patients with concurrent dry eye, non-preserved tears should be used to avoid preservative toxicity 7
• When managing allergic eye conditions, bepotastine can be considered as part of a comprehensive treatment approach that may include lid hygiene and other measures depending on severity 7