Main unwanted side effect of sedating antihistamines
Although some of these attributes may be predicted from preclinical and pharmacokinetic studies, it is only in the clinical environment that they may be definitively established.-receptors is determined in preclinical studies.
However, levocetirizine may cause somnolence in susceptible individuals while fexofenadine has a relatively short duration of action requiring twice daily administration for full all round daily protection.It is hardly surprising, therefore, that these first-generation antihistamines had poor receptor selectivity and significant unwanted side effects.During this time, knowledge of the nature and diversity of receptors was rudimentary to say the least and it was only several decades later that the existence of more than one species of histamine receptor was discovered.B, A surface view of an activated receptor with histamine linking domains III and V.
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C, A surface view of an inactive receptor with cetirizine linking domains IV and VI.-antihistamines, which are not structurally related to histamine, do not antagonize the binding of histamine but bind to different sites on the receptor to produce the opposite effect.It is not surprising then that antihistamines crossing the blood-brain barrier interfere with all of these processes.
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