Rupatadine is a second generation

antihistamine Antihistamines are drugs which treat allergic rhinitis, common cold, influenza, and other allergies. Typically, people take antihistamines as an inexpensive, generic (not patented) drug that can be bought without a prescription and provides ...

and

platelet-activating factor Platelet-activating factor, also known as PAF, PAF-acether or AGEPC (acetyl-glyceryl-ether-phosphorylcholine), is a potent phospholipid activator and mediator of many leukocyte functions, platelet aggregation and degranulation, inflammation, and an ...

antagonist used to treat allergies. It was discovered and developed by and is marketed as Rupafin and under several other trade names.

Medical uses

Rupatadine fumarate has been approved for the treatment of

allergic rhinitis Allergic rhinitis, of which the seasonal type is called hay fever, is a type of inflammation in the nose that occurs when the immune system overreacts to allergens in the air. It is classified as a type I hypersensitivity reaction. Signs a ...

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 Somnolence (alternatively sleepiness or drowsiness) is a state of strong desire for sleep, or sleeping for unusually long periods (compare hypersomnia). It has distinct meanings and causes. It can refer to the usual state preceding falling aslee ...

headache A headache, also known as cephalalgia, is the symptom of pain in the face, head, or neck. It can occur as a migraine, tension-type headache, or cluster headache. There is an increased risk of Depression (mood), depression in those with severe ...

s and

fatigue Fatigue is a state of tiredness (which is not sleepiness), exhaustion or loss of energy. It is a signs and symptoms, symptom of any of various diseases; it is not a disease in itself. Fatigue (in the medical sense) is sometimes associated wit ...

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 Degranulation is a cellular process that releases antimicrobial, cytotoxic, or other molecules from secretory vesicles called granules found inside some cells. It is used by several different cells involved in the immune system, including gran ...

mast cell A mast cell (also known as a mastocyte or a labrocyte) is a resident cell of connective tissue that contains many granules rich in histamine and heparin. Specifically, it is a type of granulocyte derived from the myeloid stem cell that is a p ...

s induced by immunological and non-immunological stimuli, and inhibition of the release of

cytokine Cytokines () are a broad and loose category of small proteins (~5–25 kDa) important in cell signaling. Cytokines are produced by a broad range of cells, including immune cells like macrophages, B cell, B lymphocytes, T cell, T lymphocytes ...

s, particularly of the

tumor necrosis factors The tumor necrosis factor (TNF) superfamily is a protein superfamily of transmembrane protein#Classification by topology, type II transmembrane proteins containing TNF homology domain and forming Protein trimer, trimers. Members of this superfa ...

(TNF) in human mast cells and

monocyte Monocytes are a type of leukocyte or white blood cell. They are the largest type of leukocyte in blood and can differentiate into macrophages and monocyte-derived dendritic cells. As a part of the vertebrate innate immune system monocytes also ...

Pharmacokinetics

Rupatadine has several

active metabolite An active metabolite, or pharmacologically active metabolite is a biologically active metabolite of a xenobiotic substance, such as a drug or environmental chemical. Active metabolites may produce therapeutic effects, as well as harmful effects. ...

s such as

desloratadine Desloratadine sold under the brand name Aerius among others, is a tricyclic H1 antagonist, H1 inverse agonist that is used to treat allergy, allergies. It is an active metabolite of loratadine. It was patented in 1984 and came into medical u ...

, 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.: Rupatadine.

References

{{Portal bar , Medicine H1 receptor antagonists Disubstituted pyridines Piperidines Chloroarenes Benzocycloheptapyridines Peripherally selective drugs