Unwanted side effects of sedating antihistamines

Currently the only FDA-approved histamine antagonist medications block the effects of histamine at H1 or H2 receptor sites. 6 Antihistamine medications block or reduce histamine-mediated effects at one of four identified histamine receptors (see Table 1 below).

These antihistamines have low receptor specificity and interact with both peripheral and central histamine receptors and readily cross the blood-brain barrier.Urinary retention and difficulty urinating can be particularly troublesome in male patients with enlarged prostates, and this retention can increase the risk of urinary tract infections, especially in women.4 The second-generation nonsedating antihistamines generally are considered as safer alternatives for use in older adults who require treatment for allergic rhinitis and other allergy symptoms.These antihistamines are more selective on peripheral H1 receptors and have a lower affinity for cholinergic and alpha-adrenergic receptor sites, which reduces the risk of anticholinergic and central nervous system side effects.Older adults are especially sensitive to the central nervous system- and anticholinergic-related side effects of sedating antihistamines because of decreased cholinergic neurons or receptors in the brain, reduced hepatic and renal function, and increased blood-brain permeability.These patients also often have coexisting conditions and often take multiple medications that increase the risk of drug-drug interactions and the potential for sedative adverse effects.

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