Ocustin

Approved Indications:

• Treatment of allergic conjunctivitis, including seasonal and perennial types
• Relief of ocular itching associated with allergic conjunctivitis

Clinically Accepted Off-Label Uses:

• Management of other ocular allergic conditions such as vernal conjunctivitis and atopic keratoconjunctivitis
• Adjunct therapy for allergic rhinitis with ocular symptoms (topical ocular use)

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 dosage adjustment recommended for renal or hepatic impairment due to minimal systemic exposure with topical ocular use

Administration Notes:

• Wash hands before administration
• Avoid touching the dropper tip to the eye or any surface
• Wait at least 5 minutes before instilling other eye medications

Bepotastine besilate is a selective histamine H1 receptor antagonist with additional mast cell-stabilizing properties. By blocking H1 receptors on conjunctival and ocular tissue cells, it prevents histamine-induced itching, vasodilation, and increased vascular permeability. Its mast cell stabilization inhibits release of inflammatory mediators, reducing ocular redness, swelling, and itching associated with allergic conjunctivitis.

• Absorption: Minimal systemic absorption after ocular administration
• Distribution: Primarily localized in ocular tissues with low systemic exposure
• Metabolism: Limited systemic metabolism due to topical administration
• Elimination: Systemic clearance occurs mainly via renal excretion; however, systemic levels are negligible
• Onset of Action: Symptom relief generally occurs within 15 minutes after administration
• Duration: Effect lasts approximately 8 to 12 hours, supporting twice-daily dosing
• Half-life: Systemic half-life is not clinically significant due to low absorption

• Pregnancy: No adequate well-controlled studies in pregnant women. Use only if potential benefit justifies potential risk.
• Lactation: It is unknown whether bepotastine is excreted in human milk. Caution is advised; avoid ocular administration during breastfeeding or consult a healthcare provider.

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

• Known hypersensitivity to bepotastine besilate or any components of the formulation
• History of hypersensitivity reactions to other H1-antihistamines

• Use with caution in patients with narrow-angle glaucoma or increased intraocular pressure
• Contact lens wearers should remove lenses prior to administration and wait 15 minutes before reinsertion
• Avoid contamination of the dropper tip to prevent ocular infections
• Discontinue use if eye irritation or hypersensitivity reactions occur
• Not intended for systemic use

Common:

• Mild eye irritation or burning upon instillation
• Headache
• Taste alteration (bitter or unpleasant taste)

Less Common:

• Dry eyes
• Blurred vision
• Nasopharyngitis

Rare / Serious:

• Hypersensitivity reactions such as conjunctival hyperemia, edema, or eyelid swelling
• Severe allergic reactions are rare

• No significant drug interactions are expected due to minimal systemic absorption
• Concomitant use with other topical ocular medications is generally safe but separate administration by at least 5 minutes is recommended
• Avoid concurrent use with eye drops containing preservatives that may cause irritation

• Recognized as an effective and well-tolerated topical treatment for allergic conjunctivitis with rapid onset of symptom relief
• Guidelines support its use as first-line therapy for ocular itching and redness related to allergic conjunctivitis
• Emphasis on favorable safety profile and 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 when not in use
• Do not freeze
• Keep out of reach of children