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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 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 ...
Diphenylpyraline (DPP; sold as Allergen, Arbid, Belfene, Diafen, Hispril, Histyn, Lergobine, Lyssipol, Mepiben, Neargal) is a first-generation antihistamine with anticholinergic effects of the diphenyl piperidine class. [2] [3] [4] It is marketed in Europe for the treatment of allergies.
Diphenhydramine is a first-generation antihistamine used to treat several conditions including allergic symptoms and itchiness, the common cold, insomnia, motion sickness, and extrapyramidal symptoms. [19] [20] Diphenhydramine also has local anesthetic properties, and has been used as such in people allergic to common local anesthetics such as ...
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 ...
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]
Phenbenzamine, sold under the brand name Antergan and known by the former developmental code name RP-2339, is an antihistamine of the ethylenediamine class which also has anticholinergic properties. [ 1 ] [ 2 ] It was introduced in 1941 or 1942 and was the first antihistamine to be introduced for medical use.
As an antihistamine, doxylamine is an inverse agonist of the histamine H 1 receptor. As a first-generation antihistamine, it typically crosses the blood–brain barrier into the brain, thereby producing a suite of sedative and hypnotic effects that are mediated by the central nervous system. (N.b.: