Besifloxacin

Approved Indications:

• Treatment of ocular itching associated with allergic conjunctivitis (seasonal and perennial).
• Relief of signs and symptoms of allergic conjunctivitis including redness, swelling, and irritation.

Clinically Accepted Off-Label Uses:

• Management of other allergic ocular conditions such as vernal conjunctivitis and atopic keratoconjunctivitis.
• Adjunctive treatment in allergic rhinitis with ocular symptoms.

Formulation and Route:

• Ophthalmic solution (eye drops).

Adults and Children ≥2 years:

• Instill one drop into the affected eye(s) twice daily (every 12 hours).

Pediatrics (<2 years):

• Safety and efficacy not established; use not recommended.

Elderly:

• No dosage adjustment required.

Special Populations:

• No specific dose adjustment necessary for renal or hepatic impairment.

Administration Notes:

• Wash hands before use.
• Avoid contact of the dropper tip with the eye or any surface to prevent contamination.
• Wait at least 5 minutes between administration of other ocular medications.

Bepotastine besilate is a selective histamine H1 receptor antagonist with mast cell stabilizing effects. It blocks histamine H1 receptors on conjunctival cells, preventing histamine-mediated itching, vasodilation, and increased vascular permeability. Additionally, it inhibits mast cell degranulation, reducing the release of inflammatory mediators and thereby alleviating ocular allergy symptoms.

• Absorption: Minimal systemic absorption after topical ocular administration.
• Distribution: Primarily localized in ocular tissues.
• Metabolism: Limited systemic metabolism due to low absorption.
• Elimination: Excreted renally; systemic exposure negligible.
• Onset of Action: Symptom relief typically begins within 15 minutes.
• Duration: Effect lasts approximately 8–12 hours, supporting twice-daily dosing.
• Half-life: Systemic half-life is clinically insignificant due to minimal absorption.

• Pregnancy: Limited data in humans. Use only if clearly needed and benefits outweigh risks.
• Lactation: Unknown if excreted in breast milk. Caution advised during breastfeeding.

• Primary Class: Antihistamine (H1 receptor antagonist)
• Subclass: Second-generation topical ocular antihistamine and mast cell stabilizer.

• Known hypersensitivity to bepotastine besilate or any formulation excipients.

• Use caution in patients with narrow-angle glaucoma or increased intraocular pressure.
• Remove contact lenses prior to administration and wait 15 minutes before reinsertion.
• Avoid contamination of the dropper tip.
• Discontinue if hypersensitivity or severe irritation develops.

Common:

• Mild burning or stinging on instillation
• Altered or bitter taste
• Headache

Less Common:

• Dry eyes
• Blurred vision
• Nasopharyngitis

Rare / Serious:

• Allergic reactions including conjunctival hyperemia, eyelid edema
• Severe ocular irritation (rare)

• No significant systemic drug interactions due to minimal systemic absorption.
• Separate administration from other ocular drugs by at least 5 minutes.
• Avoid concurrent use with ocular products containing irritating preservatives.

• Recommended as effective first-line treatment for ocular allergic symptoms with rapid onset and favorable safety profile.
• Emphasized in guidelines for its dual antihistamine and mast cell stabilizing action.
• Low sedation risk compared to systemic antihistamines.

• Store at 2°C to 30°C (36°F to 86°F).
• Protect from light and moisture.
• Keep the bottle tightly closed.
• Do not freeze.
• Keep out of reach of children.