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Oxatomide, is a sedating H1-antihistamine, having mast-cell stabilising properties perhaps by a calcium-channel antagonist effect , without anticholinergic effect.It is used in treatment of chronic urticaria, atopic dermatitis and dermographisms. Doxylamine is a sedating antihistamine also used as an hypnotic.The drug to use in severe situations is adrenaline The early H1-antihistamines usually induce drowsiness and their prescription to patients with an activity requiring a normal vigilance, like control of a vehicle, is contra-indicated.By their alpha-adrenolytic effect especially when they are given by parenteral route, they could reduce the vasoconstrictive effect of adrenaline, administered for example in case of anaphylactic shock.In addition to this antihistamine effect, they can have parallel pharmacological properties, for example antimuscarinic and adrenolytic effects which must be considered.It is usual to classify H1-antihistamines into two classes: old ones, called first-generation agents, which are sedating and recent ones, called second-generation agents which have slight or no sedating effects because they do not cross the blood-brain barrier.New H1-antihistamines, terfenadine and astemizole, which were associated with cardiac adverse effects, prolongation of QT interval, torsades de pointes by inhibition of potassium channels, are no longer approved for use. Other adverse effects of H1-antihistamines have been reported, in particular allergic reactions.
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Loratadine acts mainly via one of its metabolites, decarboethoxyloratadine, also called desloratadine, which is also marketed.New H1-antihistamines induce only exceptionally drowsiness. This possibility, even rare, must however be taken into account, particularly at time of a first prescription.
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