rupatadine fumarate: clinical use

Prescribing considerations

• Review concomitant CYP3A4 inhibitors and substrates before prescribing.
• Avoid grapefruit juice and assess medicines that may impair alertness.
• Use caution with known QT prolongation, uncorrected hypokalaemia, clinically significant bradycardia or acute myocardial ischaemia.
• Use tablets cautiously in older people because clinical experience is limited.
• Use is not recommended in renal or hepatic impairment because clinical experience is lacking.
• The oral solution is not recommended below 2 years; tablets are not recommended below 12 years.

Contraindications and cautions

• Hypersensitivity to rupatadine or any formulation excipient.
• Tablets should not be used in rare hereditary galactose intolerance, total lactase deficiency or glucose-galactose malabsorption.
• Oral solution should not be used in hereditary fructose intolerance, glucose-galactose malabsorption or sucrase-isomaltase insufficiency.

Monitoring

• No routine laboratory-monitoring programme is specified in the SmPC.
• Assess symptom control, somnolence and other adverse effects clinically.
• Consider cardiac risk factors and interacting medicines before and during treatment.
• The oral solution's propylene glycol content warrants particular review in young children and in renal or hepatic dysfunction.

Clinical pharmacology

Rupatadine is a long-acting second-generation peripheral H1-receptor antagonist. It is extensively metabolised, mainly through CYP3A4, and active metabolites including desloratadine contribute to overall antihistamine activity.

Formulation and product differences

• Tablets are licensed for adults and adolescents over 12 years and contain lactose.
• Oral solution is licensed for children aged 2 to 11 years and is supplied with a graduated oral syringe.
• The oral solution contains sucrose, methyl parahydroxybenzoate, propylene glycol and quinoline yellow; sucrose may harm teeth and methyl parahydroxybenzoate can cause delayed allergic reactions.
• The oral solution requires consideration of combined propylene glycol or alcohol exposure, particularly in children under 5 years.

Oral solution

Route: Oral

Strengths: 1 mg/mL

Tablet

Route: Oral

Strengths: 10 mg