Introduction
Rupatadine is a dual histamine H1 receptor and platelet activating factor receptor antagonist that is used for symptomatic relief in seasonal and perennial rhinitis as well as chronic spontaneous urticaria. It was approved for marketing in Canada under the tradename Rupall and comes in tablet formulation for adult use and liquid formulation for pediatric use.
Uses
Rupatadine is a selective histamine H1 receptor antagonist and platelet activating factor (PAF) antagonist used to treat allergic rhinitis.
For the symptomatic relief of nasal and non-nasal symptoms of seasonal allergic rhinitis and perennial allergic rhinitis in patients 2 years of age and older . Also used for the symptomatic relief of chronic spontaneous urticaria in patients 2 years of age and older.
Associated Conditions
Pharmacodynamics
Rupatadine is an anti allergenic and acts to reduce allergic symptoms like urticaria, rhinorrhea, sneezing and itching .
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.
Absorption
Rupatidine is rapidly absorbed with a Tmax of 1 h . Administration with a high fat meal increases exposure by 23% and increases Tmax to 2 h.
Volume of Distribution
The apparent volume of distribution is 9799 L .
Protein Binding
Rupatidine is 98.5-99.0% bound to human plasma proteins .
Half Life
The half life of elimination is 15.9 h in children 2-5 years old, 12.3 h in children 6-11 years old, 5.9 h in adults, and 8.7 h in geriatric patients .
Clearance
Systemic clearance is 1556.2 L/h in young adults and 798.2 L/h in geriatric patients .
Food Interactions
- Avoid grapefruit products. Grapefruit inhibits CYP3A metabolism, which may increase the serum concentration of rupatadine.
- Take with or without food.
Dosage
Children aged 2 to 11 years:
- Children weighing 25 kg or more: 1 teaspoonful (5 ml) of the oral solution once daily with or without food.
- Children weighing equal or more than 10 kg to less than 25 kg: 1/2 teaspoonful (2.5 ml) oral solution once daily with or without food.
