Unwanted side effects of sedating antihistamines

Posted by / 10-Feb-2021 09:41

It is hardly surprising, therefore, that these first-generation antihistamines had poor receptor selectivity and significant unwanted side effects.

Candidate antihistaminic compounds were primarily modifications of those synthesized as cholinergic antagonists and are from diverse chemical entities, ethanolamines, ethylene diamines, alkylamines, piperazines, piperidines, and phenothiazines.Thus, the calculation of receptor occupancy after single oral doses of drug shows values of 95%, 90%, and 71% for fexofenadine, levocetirizine, and desloratadine, respectively, indicating that they are all very effective H-antihistamines.Although receptor occupancy for these drugs appears to correlate with pharmacodynamic activity in skin wheal and flare studies and with efficacy in allergen challenge chamber studies,[].While desloratadine is less efficacious, it has the advantages of rarely causing somnolence and having a long duration of action.Lastly, all H] and chlorpheniramine, brompheniramine, and promethazine later the same decade.

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For example, in inflammation the p H of the tissues is reduced[, histamine receptors are situated on the cellular membranes of cells, including vascular and airways smooth muscle, mucous glands, and sensory nerves, all of which are surrounded by the extracellular fluid.

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