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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]
It is a first-generation antihistamine in the piperazine family of chemicals. [8] [4] Common side effects include sleepiness, headache, and dry mouth. [8] [9] Serious side effects may include QT prolongation. [9] It is unclear if use during pregnancy or breastfeeding is safe. [8]
The first-generation sedating antihistamines diphenhydramine, doxepin, doxylamine, and pyrilamine are the most widely used medications in the world for preventing and treating insomnia. [6] As of 2004, doxylamine and diphenhydramine, which are both over-the-counter medications, were the agents most commonly used to treat short-term insomnia. [11]
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The introduction of the first-generation antihistamines marked the beginning of medical treatment of nasal allergies. [28] Research into these drugs led to the discovery that they were H 1 receptor antagonists and also to the development of H 2 receptor antagonists , where H 1 -antihistamines affected the nose and the H 2 -antihistamines ...
It is a first-generation antihistamine and works by blocking the histamine H 1 receptor. [2] Common side effects include sleepiness, restlessness, and weakness. Other side effects may include dry mouth and wheeziness. [2] Chlorpheniramine was patented in 1948 and came into medical use in 1949. [3] It is available as a generic medication and ...
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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]