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Rupatadine

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Rupatadine
File:Rupatadine.png
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
Clinical data
Trade names Rupafin, Alergoliber, Rinialer, Pafinur, Rupax, Ralif
AHFS/Drugs.com International Drug Names
  • Prescription drug
Oral
Pharmacokinetic data
Protein binding 98–99%
Metabolism Hepatic, CYP-mediated
Half-life 5.9 hours
Excretion 34.6% urine, 60.9% faeces
Identifiers
158876-82-5 7pxN (free base)
182349-12-8 (fumarate)
R06AX28
PubChem CID 133017
ChemSpider 117388 7pxY
UNII 2AE8M83G3E 7pxY
ChEMBL CHEMBL91397 7pxY
Chemical data
Formula C26H26ClN3
415.958 g/mol
 14pxN (what is this?)  (verify)

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.

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.

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.

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.

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]

Pharmacokinetics

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

History

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.

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]

References

  1. Patents: EP 577957 , US 5407941 , US 5476856 
  2. Merlos, M.; Giral, M.; Balsa, D.; Ferrando, R.; Queralt, M.; Puigdemont, A.; García-Rafanell, J.; Forn, J. (1997). "Rupatadine, a new potent, orally active dual antagonist of histamine and platelet-activating factor (PAF)". The Journal of Pharmacology and Experimental Therapeutics 280 (1): 114–121. PMID 8996188.  edit
  3. 3.0 3.1 Picado, C. S. (2006). "Rupatadine: Pharmacological profile and its use in the treatment of allergic disorders". Expert Opinion on Pharmacotherapy 7 (14): 1989–2001. PMID 17020424. doi:10.1517/14656566.7.14.1989.  edit
  4. Keam, S. J.; Plosker, G. L. (2007). "Rupatadine: A review of its use in the management of allergic disorders". Drugs 67 (3): 457–474. PMID 17335300. doi:10.2165/00003495-200767030-00008.  edit
  5. Mullol, J.; Bousquet, J.; Bachert, C.; Canonica, W. G.; Gimenez-Arnau, A.; Kowalski, M. L.; Martí-Guadaño, E.; Maurer, M.; Picado, C.; Scadding, G.; Van Cauwenberge, P. (2008). "Rupatadine in allergic rhinitis and chronic urticaria". Allergy 63: 5–28. PMID 18339040. doi:10.1111/j.1398-9995.2008.01640.x.  edit