BILAXTEN

Indications

• Allergic rhinoconjunctivitis
• Urticaria

Dosage

Children: Child 6–11 years: 5 mg once daily; Child 12–17 years: 10 mg once daily.

Adults: 10 mg once daily, taken 1 hour before or 2 hours after food or fruit juice.

Mechanism of action

Bilastine exerts its effects by selectively antagonizing peripheral H1 receptors, thereby inhibiting the actions of histamine, which contributes to allergic symptoms.

Pharmacodynamics

Bilastine provides rapid onset of action with a duration of effect that allows for once-daily dosing. It has been shown to cause minimal sedation and psychomotor impairment.

Pharmacokinetics

Bilastine is rapidly absorbed after oral administration, with peak plasma concentrations occurring within 1-2 hours. It is not extensively metabolized in the liver and has a half-life of approximately 14 hours, allowing for once-daily dosing.

Contra-indications

• Acute porphyrias

Adverse effects

• Drowsiness
• Dry mouth
• Dizziness
• Rash
• Anxiety
• Appetite increased
• Asthenia
• Diarrhoea
• Dyspnoea
• Fever
• Gastritis
• Gastrointestinal discomfort
• Insomnia
• Nausea
• Oral herpes

Interactions

• Grapefruit juice may decrease exposure
• Rifampicin may decrease exposure

Precautions

• Patients should be advised that drowsiness can occur and may affect performance of skilled tasks (e.g. cycling or driving); alcohol should be avoided.

Pregnancy

Avoid-limited information available. Most manufacturers of antihistamines advise avoiding their use during pregnancy; however, there is no evidence of teratogenicity.

Breast-feeding

Avoid-no information available. Most antihistamines are present in breast milk in varying amounts; although not known to be harmful, most manufacturers advise avoiding their use in mothers who are breast-feeding.

Storage

Store below 25°C. Protect from light. Keep out of reach of children.

Formulations

• 8 mg oral tablets
• 18 mg capsules

Mechanism of action

Bilastine is a selective histamine H1 receptor antagonist (Ki = 64nM). During allergic response mast cells undergo degranulation which releases histamine and other subastances. By binding to and preventing activation of the H1 receptor, bilastine reduces the development of allergic symptoms due to the release of histamine from mast cells.

Pharmacodynamics

Bilastine is an antiallergenic and acts to reduce allergic symptoms such as nasal congestion and urticaria.