Emerging safety issues regarding long-term usage of H₁-receptor antagonists

Abstract

The second generation histamine H₁-receptor antagonists are important therapeutic tools in the treatment of atopic disease and may also have a place as an adjunct therapy for those patients whose allergic asthma coexists with allergic rhinitis. They are amongst the most widely prescribed and safest drugs in the world. However, as second generation H₁-receptor antagonists are used to treat non-life threatening conditions, the risk of adverse effects is of vital importance. For many, the potential for sedation by some of the newer antihistamines still remains an issue, while there have recently been widespread concerns regarding the potential for cardiotoxicity and the impact of drug–drug interactions associated with some second generation H₁-receptor antagonists. Consequently, progress with this class of drugs should involve not only increased efficacy but also improvements in their safety and specificity. Moreover, there is a trend towards using second generation H₁-receptor antagonists as long-term therapy rather than confining their use to treating the short-term manifestations of allergic disease. To this end, a number of novel, potent and safe antihistamines have been developed which are either metabolites of active drugs or enantiomers. This review will examine some of the safety issues associated with established and newer second generation drugs particularly in relation to their long-term usage in adults and children.

• antihistamines
• antihistamine metabolites
• enantiomers
• safety