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Rupatadine
Systematic (IUPAC) name
8-Chloro-6,11-dihydro-11-[1-[(5-methyl-3-pyridinyl)methyl]-4-piperidinylidene]-5H-benzo[5,6]cyclohepta[1,2-b]pyridine fumarate
Identifiers
CAS number 158876-82-5 (free base)
182349-12-8 (fumarate)
ATC code R06AX28
PubChem 6449107
Chemical data
Formula C 26H26ClN3  
Mol. mass 415.958 g/mol
Pharmacokinetic data
Bioavailability  ?
Protein binding 98-99%
Metabolism Hepatic, CYP-mediated
Half life 5.9 hours
Excretion (34.6% urine, 60.9% faeces)
Therapeutic considerations
Pregnancy cat.  ?
Legal status Prescription drug
Routes Oral

Rupatadine is a second generation antihistamine and PAF antagonist used to treat allergies. It was discovered and developed by J. Uriach y Cia, S. A.[1] and is marketed under several trade names such as Rupafin, Alergoliber, Rinialer, Pafinur, Rupax and Ralif.

Contents

Available form

Rupatadine is available as round, light salmon coloured tablets containing 10 mg of rupatadine (as fumarate) to be administered orally, once a day.

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.[2]

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 TNF in human mast cells and monocytes.[3]

History and formulations

Rupatadine discovery, pre-clinical and clinical development was performed by J. Uriach y Cia, S. A., a Spanish pharmaceutical company. It was launched in 2003 in Spain by J. Uriach y Cia, S. A., with the brand name of Rupafin. The registration of the product is approved in 23 countries from the EU, 8 Central American countries, Brazil, Argentina, Chile, Turkey and 14 African countries.

Therapeutic indications approved

Rupatadine fumarate has been approved for the treatment of allergic rhinitis and chronic urticaria in adults and children over 12 years. The Defined Daily Dose (DDD) is 10 mg orally.

Efficacy in humans

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.[3][4][5]

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.

References

  1. ^ Patents: EP 577957, US 5407941, US 5476856
  2. ^ Merlos M, Giral M, Balsa D et al. Rupatadine, a new potent, orally active dual antagonist of histamine and platelet-activating factor (PAF).J Pharmacol Exp Ther 1997; 280 (1): 114-121.
  3. ^ a b Picado C. Rupatadine: pharmacological profile and its use in the treatment of allergic disorders. Expert Opin Pharmacother. (2006) 7: 1989-2001.
  4. ^ Kean SJ; Plosker GL. “Rupatadine: A review of its use in the management of allergic disorders. Drugs 2007: 67(3).
  5. ^ J. Mullol, J. Bousquet, C. Bachert et al. Rupatadine in allergic rhinitis and chronic urticaria. Allergy 2008: 63 (Suppl.87): 5-28.
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