Rupatadine

Medical uses

Rupatadine fumarate has been approved for the treatment of allergic rhinitis and chronic urticaria in adults and children over 12 years. It is available as round, light salmon coloured tablets containing 10 mg of rupatadine (as fumarate) to be administered orally, once a day.

The efficacy of rupatadine as treatment for allergic rhinitis (AR) and chronic idiopathic urticaria (CIU) has been investigated in adults and adolescents (aged over 12 years) in several controlled studies, showing a rapid onset of action and a good safety profile even in prolonged treatment periods of a year.

Side effects

Rupatadine is a non-sedating antihistamine. However, as in other non sedating second-generation antihistamines, the most common side effects in controlled clinical studies were somnolence, headaches and fatigue.

Pharmacology

Mechanism of action

Rupatadine is a second generation, non-sedating, long-acting histamine antagonist with selective peripheral H1 receptor antagonist activity. It further blocks the receptors of the platelet-activating factor (PAF) according to in vitro and in vivo studies.

Rupatadine possesses anti-allergic properties such as the inhibition of the degranulation of mast cells induced by immunological and non-immunological stimuli, and inhibition of the release of cytokines, particularly of the tumor necrosis factors (TNF) in human mast cells and monocytes.

Pharmacokinetics

Rupatadine has several active metabolites such as desloratadine, 3-hydroxydesloratadine, 5-hydroxydesloratadine and 6-hydroxydesloratadine.

History

Rupatadine discovery, pre-clinical and clinical development was performed by Uriach, a Spanish pharmaceutical company. It was launched in 2003 in Spain under the brand name of Rupafin. It was launched in Canada under the name Rupall.

Brand names

Brand names include Rupafin, Rupall, Rupanase, Rinialer, Pafinur, Rupax, Urtimed, Wystamm and Ralif, Rupita (EURO Pharma Ltd.)among others.

References

References

1. (14 March 2017). "Health Canada New Drug Authorizations: 2016 Highlights".
2. (2 September 2021). "Active Substance: rupatadine". European Medicines Agency.
3. Patents: {{Patent. EP. 577957, {{Patent. US. 5407941, {{Patent. US. 5476856
4. link. (2018-02-10 .)
5. (2007). "Rupatadine: a review of its use in the management of allergic disorders". Drugs.
6. (April 2008). "Rupatadine in allergic rhinitis and chronic urticaria". Allergy.
7. (January 1997). "Rupatadine, a new potent, orally active dual antagonist of histamine and platelet-activating factor (PAF)". The Journal of Pharmacology and Experimental Therapeutics.
8. (October 2006). "Rupatadine: pharmacological profile and its use in the treatment of allergic disorders". Expert Opinion on Pharmacotherapy.
9. (May 2007). "Influence of food on the oral bioavailability of rupatadine tablets in healthy volunteers: a single-dose, randomized, open-label, two-way crossover study". Clinical Therapeutics.
10. (January 2020). "Structural and clinical impact of anti-allergy agents: An overview". Bioorganic Chemistry.
11. (January 25, 2017). "Pediapharm Announces the Commercial Launch of Rupall (rupatadine) in Canada". Pediapharm.
12. {{drugs.com. international. rupatadine: Rupatadine.