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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 ...
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.
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 ]
Piperoxan was discovered in 1933 and was the first compound with antihistamine effects to be identified. [22] Piperoxan and its analogues were too toxic to be used in humans. [22] Phenbenzamine (Antergan) was the first clinically useful antihistamine and was introduced for medical use in 1942. [22]
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]
Chlorcyclizine (Di-Paralene, Mantadil, Pruresidine, Trihistan) is a first-generation antihistamine of the diphenylmethylpiperazine group marketed in the United States and certain other countries. [ 1 ] [ 2 ] [ 3 ] It is used primarily to treat allergy symptoms such as rhinitis , urticaria , and pruritus , and may also be used as an antiemetic .
Clemastine, also known as meclastin, is a first-generation H1 histamine antagonist (antihistamine) with anticholinergic properties (drying) and sedative side effects. [1] Like all first-generation antihistamines, it is sedating. [2] [3] Patented in 1960, it came into medical use in 1967. [4]