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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]
Dexbrompheniramine is an antihistamine with anticholinergic properties [1] used to treat allergic conditions such as hay fever or urticaria. It is the pharmacologically active dextrorotatory isomer of brompheniramine. It was formerly marketed in combination with pseudoephedrine under the name Drixoral in the US and Canada. It is an alkylamine ...
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.
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 ]
Clinically, H 1-antihistamines are used to treat allergic reactions and mast cell-related disorders. Sedation is a common side effect of H 1-antihistamines that readily cross the blood–brain barrier; some of these drugs, such as diphenhydramine and doxylamine, may therefore be used to treat insomnia.
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 ...
Like the other first-generation drugs of its class, it is considered a sedating antihistamine. [2] It was patented in 1948 and came into medical use in 1955. [3] In 2022, the combination with dextromethorphan and pseudoephedrine was the 265th most commonly prescribed medication in the United States, with more than 1 million prescriptions. [4] [5]
Azatadine (Optimine) is a first-generation antihistamine and anticholinergic drug that was synthesized in 1963 by Schering-Plough, a former American pharmaceutical company. [ 1 ] [ 2 ] It was patented in 1967. [ 3 ]