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The most common adverse effects noted for second-generation agents include drowsiness, fatigue, headache, nausea and dry mouth. [4] Continuous and/or cumulative use of anticholinergic medications, including first-generation antihistamines, is associated with higher risk for cognitive decline and dementia in older people. [8] [9]
It is used in the treatment of itchiness, anxiety, insomnia, and nausea (including that due to motion sickness). [8] It is used either by mouth or injection into a muscle. [8] Hydroxyzine works by blocking the effects of histamine. [9] It is a first-generation antihistamine in the piperazine family of chemicals.
The first tricyclic antidepressant, imipramine, was originally developed and studied to be an antihistamine alongside other first-generation antihistamines of the time, such as promethazine. [7] TCAs can increase the level of norepinephrine and serotonin by inhibiting their reuptake transport proteins. [ 8 ]
It is classified as a second-generation antihistamine because it is less able to pass the blood–brain barrier and cause sedation, compared to first-generation antihistamines. [12] [13] It was patented in 1979 and came into medical use in 1996. [14] It is on the World Health Organization's List of Essential Medicines. [15]
Second-generation antihistamines selectively bind to the peripheral H-1 receptors outside the blood-brain barrier, therefore they are less likely to cause sedation. First-generation antihistamines usually last around 4–6 hours whilst second-generation antihistamines work for 12–24 hours. [7]
Diphenhydramine is a first-generation antihistamine used to treat several conditions including allergic symptoms and itchiness, the common cold, insomnia, motion sickness, and extrapyramidal symptoms. [19] [20] Diphenhydramine also has local anesthetic properties, and has been used as such in people allergic to common local anesthetics such as ...
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Cetirizine is a second-generation antihistamine used to treat allergic rhinitis (hay fever), dermatitis, and urticaria (hives). [5] It is taken by mouth. [6] Effects generally begin within thirty minutes and last for about a day. [6] The degree of benefit is similar to other antihistamines such as diphenhydramine, which is a first-generation ...