NAISALLERG

Indications

• Allergic rhinitis
• Urticaria

Dosage

Children: Refer to BNF for Children for specific dosing recommendations.

Adults: 10 mg once daily.

Mechanism of action

Rupatadine is a dual antagonist of histamine H1 receptors and platelet activating factor (PAF) receptors. It prevents the effects of histamine and PAF, which are released during allergic responses, thereby alleviating symptoms like nasal congestion, rhinorrhea, itching, and swelling associated with allergies.

Pharmacodynamics

Rupatadine exhibits anti-allergenic properties, effectively reducing symptoms of allergies such as urticaria, rhinorrhea, sneezing, and itching. Its dual action on H1 and PAF receptors enhances its efficacy in managing allergic conditions.

Pharmacokinetics

Rupatadine is absorbed after oral administration and reaches peak plasma concentrations within a few hours. It has a prolonged duration of action, allowing for once-daily dosing. The drug undergoes hepatic metabolism and is eliminated through both renal and fecal pathways.

Contra-indications

• Hypersensitivity to rupatadine or any of its components
• Severe hepatic impairment

Adverse effects

• Drowsiness
• Headache
• Dry mouth
• Nausea
• Fatigue
• Palpitations
• QT interval prolongation
• Angioedema
• Seizures
• Tachycardia

Interactions

• Dronedarone (increases exposure)
• Grapefruit juice (increases exposure)
• Cobicistat (unknown increase in exposure)
• Crizotinib (unknown increase in exposure)
• Idelalisib (unknown increase in exposure)
• Imatinib (unknown increase in exposure)
• Letermovir (unknown increase in exposure)
• Nilotinib (unknown increase in exposure)

Precautions

• Caution in patients with a history of QT-interval prolongation
• Caution in patients with uncorrected hypokalaemia
• Drowsiness may affect driving or skilled tasks
• Use with caution in elderly patients due to limited information

Pregnancy

Most manufacturers advise avoiding use during pregnancy; however, there is no evidence of teratogenicity.

Breast-feeding

Most antihistamines are present in breast milk in varying amounts; although not known to be harmful, most manufacturers advise avoiding their use in breastfeeding mothers.

Storage

Store at room temperature, away from moisture and light.

Formulations

• 10 mg modified-release tablets
• Oral solution

Mechanism of action

Rupatadine is a dual histamine H1 receptor and platelet activating (PAF) receptor antagonist. During allergic response mast cells undergo degranulation, releasing histamine and other substances. Histamine acts on H1 receptors to produce symptoms of nasal blockage, rhinorhea, itching, and swelling. PAF is produced from phospholipids cleaved by phospholipase A2. It acts to produce vascular leakage which contributes to rhinorhea and nasal blockage. By blocking both the H1 receptor and PAF receptor, rupatidine prevents these mediators from exerting their effects and so reduces the severity of allergic symptoms.

Pharmacodynamics

Rupatadine is an anti allergenic and acts to reduce allergic symptoms like urticaria, rhinorrhea, sneezing and itching.