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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]
Therapeutically, fexofenadine is a selective peripheral H 1 blocker. 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]
Rupatadine is a second generation, non-sedating, long-acting histamine antagonist with selective peripheral H 1 receptor antagonist activity. It further blocks the receptors of the platelet-activating factor (PAF) according to in vitro and in vivo studies.
It is classified as a second-generation antihistamine and works by blocking histamine H 1-receptors. [6] [3] Levocetirizine was approved for medical use in the United States in 2007, [3] and is available as a generic medication. [4] In 2022, it was the 152nd most commonly prescribed medication in the United States, with more than 3 million ...
Among second-generation antihistamines, cetirizine is more likely than fexofenadine and loratadine to cause drowsiness. [8] Use in pregnancy appears safe, but use during breastfeeding is not recommended. [9] The medication works by blocking histamine H 1 receptors, mostly outside the brain. [6] Cetirizine can be used for paediatric patients.
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).
Bilastine is an antihistamine medication used to treat hives (), allergic rhinitis and itchy inflamed eyes (allergic conjunctivitis) caused by an allergy. [6] It is a second-generation antihistamine and takes effect by selectively inhibiting the histamine H 1 receptor, preventing these allergic reactions. [7]
Ebastine is a second-generation H1 receptor antagonist that is indicated mainly for allergic rhinitis and chronic idiopathic urticaria. [5] It is available in 10 and 20 mg tablets [6] and as fast-dissolving tablets, [7] as well as in pediatric syrup. It has a recommended flexible daily dose of 10 or 20 mg, depending on disease severity.