Biltin

• Approved Indications:
• Treatment of seasonal allergic rhinitis (hay fever) in adults and children aged 12 years and older.
• Treatment of chronic spontaneous urticaria (chronic hives) in adults and adolescents aged 12 years and older.
• Off-label / Clinically Accepted Uses:
• Relief of other allergic conditions such as perennial allergic rhinitis (persistent year-round allergies) in some regions.
• Sometimes used off-label for other histamine-mediated allergic conditions where second-generation antihistamines are appropriate.

• Route: Oral
• Adult and Adolescents (≥12 years):
• 20 mg once daily, taken on an empty stomach (at least 1 hour before or 2 hours after food or fruit juice to optimize absorption).
• Pediatrics (<12 years):
• Safety and efficacy not established; not recommended for children under 12.
• Elderly:
• No dosage adjustment required.
• Renal/Hepatic Impairment:
• No dosage adjustment required for mild to moderate impairment.
• Limited data in severe impairment; use with caution.
• Duration:
• As prescribed; symptom relief typically observed within 1 hour, lasting 24 hours.
• Use for the duration of allergen exposure or until symptom resolution.

Bilastine is a selective peripheral H1 histamine receptor antagonist that competitively inhibits histamine binding to H1 receptors on effector cells in the respiratory tract, skin, and other tissues. By blocking these receptors, bilastine prevents histamine-mediated allergic symptoms such as vasodilation, increased vascular permeability, edema, pruritus, and bronchoconstriction. It does not cross the blood-brain barrier significantly, resulting in minimal sedation.

• Absorption: Rapidly absorbed orally; peak plasma concentrations reached within approximately 1 hour post-dose.
• Bioavailability: Approximately 60%; reduced by food and fruit juices; therefore recommended to take on an empty stomach.
• Distribution: Low volume of distribution (~1.3 L/kg); high plasma protein binding (~84–90%).
• Metabolism: Minimal hepatic metabolism; largely excreted unchanged.
• Elimination: Primarily excreted unchanged via feces (~67%) and urine (~33%).
• Half-life: Approximately 14.5 hours, supporting once-daily dosing.
• Steady State: Achieved within 3 days of repeated dosing.

• Pregnancy: No adequate human studies; animal studies show no direct teratogenic effects. Use only if clearly needed after risk-benefit assessment.
• Lactation: Unknown if excreted in human milk; caution advised. Avoid breastfeeding or discontinue drug if necessary.

• Primary Class: Antihistamine
• Subclass: Second-generation H1 receptor antagonist (non-sedating)

• Known hypersensitivity to bilastine or any of its excipients.
• Concomitant use with fruit juices (grapefruit, orange, apple) should be avoided due to reduced absorption.

• Use caution in patients with renal impairment; although no dose adjustment is required, monitor clinical response.
• Bilastine has minimal sedative effects but caution advised when driving or operating machinery until individual response is known.
• Avoid alcohol consumption with bilastine due to possible additive sedative effects.
• Not established for use in children under 12 years.
• No significant cardiac safety concerns at recommended doses.

• Common (>1%):
• Headache
• Drowsiness (less frequent than first-generation antihistamines)
• Fatigue
• Dry mouth
• Gastrointestinal discomfort (nausea, abdominal pain)
• Rare/Serious:
• Hypersensitivity reactions (rash, angioedema)
• Palpitations (rare)
• Elevated liver enzymes (rare)
• Side effects are generally mild, transient, and dose-independent.

• Fruit juices (grapefruit, orange, apple): Reduce bilastine absorption; avoid concurrent intake or separate by at least 2 hours.
• P-glycoprotein inhibitors (e.g., ciclosporin): May increase bilastine plasma levels; monitor for enhanced effects.
• No significant interactions with CYP450 enzyme inhibitors or inducers.
• No known interactions with alcohol, but concurrent use may increase sedation.

• Current allergy management guidelines (ARIA, EAACI) recognize bilastine as an effective, well-tolerated second-generation antihistamine option.
• No major recent changes in approved indications or dosing.
• Emphasis on avoidance of fruit juices to optimize bioavailability has been reinforced.
• Recognized for minimal sedation and favorable safety profile compared to older antihistamines.

• Store at 20°C to 25°C (68°F to 77°F).
• Protect from moisture and light.
• Keep in original packaging until use.
• Do not freeze.
• Keep out of reach of children.