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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.
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]
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]
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 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 ...
Mepyramine, also known as pyrilamine, is a first-generation antihistamine, targeting the H 1 receptor as an inverse agonist. [1] Mepyramine rapidly permeates the brain, often causing drowsiness. [2] It is often sold as a maleate salt, pyrilamine maleate.