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The newer, second-generation H 1-antihistamines are far more selective for peripheral histamine H 1-receptors and have a better tolerability profile compared to the first-generation agents. The most common adverse effects noted for second-generation agents include drowsiness, fatigue, headache, nausea and dry mouth. [4]
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]
Diphenhydramine, sold under the brand name Benadryl among others, is an antihistamine and sedative. It is a first-generation H 1-antihistamine and it works by blocking certain effects of histamine, which produces its antihistamine and sedative effects. [11] [2] Diphenhydramine is also a potent anticholinergic. [12]
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]
Cyproheptadine, sold under the brand name Periactin among others, is a first-generation antihistamine with additional anticholinergic, antiserotonergic, and local anesthetic properties. It was patented in 1959 and came into medical use in 1961. [ 5 ]
The same goes for mental health conditions like generalized anxiety disorder (also known as GAD or just anxiety) and depression (or major depressive disorder). Drugs known as antidepressants are ...
Doxylamine and other first-generation antihistamines are the most widely used sleep medications in the world. [6] Typical side effects of doxylamine (at recommended doses) include dizziness, drowsiness, grogginess, and dry mouth, among others. [7] [4] As an antihistamine, doxylamine is an inverse agonist of the histamine H 1 receptor.
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