2014•Russian Journal of AllergyOpen access

Polyfunctional antiallergic potencies of Д-antihistamine levocetirizine

Igor S. Gushchin

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Abstract

The burden of allergic diseases worldwide is such that it represents a serious public health problem that attracts considerable efforts to identify effective and safe therapies. Antihistamines are an important part of the therapeutic options for allergic diseases. Levocetirizine is the R-enantiomer of cetirizine with pharmacokinetically and pharmacodynamically favourable characteristics. It is a potent inverse agonist of H 1-receptors with anti-inflammatory/anti-allergic properties. It appears to have grater in vivo H 1-receptor occupancy comparatively with other 2 nd generation H 1-antihistamines. This may confer an advantageous efficacy and safety profile. clinical trials indicate that it is safe and effective for the treatment of allergic rhinitis, chronic urticaria and some other allergic conditions in adults and children with a minimal number of untoward reactions. It is also becoming clearer that, in addition to its being a potent antihistamine, levocetirizine has several anti-inflammatory/anti-allergic effects that are observed at clinically relevant concentrations that may enhance its therapeutic benefit.

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What this paper is about

The burden of allergic diseases worldwide is such that it represents a serious public health problem that attracts considerable efforts to identify effective and safe therapies. Antihistamines are an important part of the therapeutic options for allergic diseases. Levocetirizine is the R-enantiomer of cetirizine with pharmacokinetically and pharmacodynamically favourable characteristics. It is a potent inverse agonist of H 1-receptors with anti-inflammatory/anti-allergic properties. It appears to have grater in vivo H 1-receptor occupancy comparatively with other 2 nd generation H 1-antihistamines. This may confer an advantageous efficacy and safety profile. clinical trials indicate that it is safe and effective for the treatment of allergic rhinitis, chronic urticaria and some other allergic conditions in adults and children with a minimal number of untoward reactions. It is also becoming clearer that, in addition to its being a potent antihistamine, levocetirizine has several anti-inflammatory/anti-allergic effects that are observed at clinically relevant concentrations that may enhance its therapeutic benefit.

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Available abstract

The burden of allergic diseases worldwide is such that it represents a serious public health problem that attracts considerable efforts to identify effective and safe therapies. Antihistamines are an important part of the therapeutic options for allergic diseases. Levocetirizine is the R-enantiomer of cetirizine with pharmacokinetically and pharmacodynamically favourable characteristics. It is a potent inverse agonist of H 1-receptors with anti-inflammatory/anti-allergic properties. It appears to have grater in vivo H 1-receptor occupancy comparatively with other 2 nd generation H 1-antihistamines. This may confer an advantageous efficacy and safety profile. clinical trials indicate that it is safe and effective for the treatment of allergic rhinitis, chronic urticaria and some other allergic conditions in adults and children with a minimal number of untoward reactions. It is also becoming clearer that, in addition to its being a potent antihistamine, levocetirizine has several anti-inflammatory/anti-allergic effects that are observed at clinically relevant concentrations that may enhance its therapeutic benefit.

Key concepts: Levocetirizine, Antihistamine, Cetirizine, Medicine, Pharmacology, Immunology

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