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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]
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 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]
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 ...
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 ...
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.
For children suffering from allergies, Reigart says saline nose drops or first generation antihistamines such as Benadryl can be beneficial for congestion. But oftentimes, you can skip the meds.
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]