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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 ...
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 ...
Hydroxyzine works by blocking the effects of histamine. [9] 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]
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]
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.
Promethazine, sold under the brand name Phenergan among others, is a first-generation antihistamine, sedative, and antiemetic used to treat allergies, insomnia, and nausea. It may also help with some symptoms associated with the common cold [ 4 ] and may also be used for sedating people who are agitated or anxious, an effect that has led to ...
Brompheniramine, sold under the brand name Dimetapp among others, is a first-generation antihistamine drug of the propylamine (alkylamine) class. [2] It is indicated for the treatment of the symptoms of the common cold and allergic rhinitis, such as runny nose, itchy eyes, watery eyes, and sneezing.