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First-generation antihistamines can easily cross the blood-brain barrier into the central nervous system to reach the H-1 receptors within, often causing drowsiness. [7] Second-generation antihistamines selectively bind to the peripheral H-1 receptors outside the blood-brain barrier, therefore they are less likely to cause sedation.
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 ...
H 1-antihistamines work by binding to histamine H 1 receptors in mast cells, smooth muscle, and endothelium in the body as well as in the tuberomammillary nucleus in the brain. Antihistamines that target the histamine H 1 -receptor are used to treat allergic reactions in the nose (e.g., itching, runny nose, and sneezing).
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]
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.
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 .
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.:
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 ...