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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.
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 ]
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]
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]
Doxylamine and other first-generation antihistamines are the most widely used sleep medications in the world. [6] Typical side effects of doxylamine (at recommended doses) include dizziness, drowsiness, grogginess, and dry mouth, among others. [7] [4] As an antihistamine, doxylamine is an inverse agonist of the histamine H 1 receptor.
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]
Diphenhydramine, sold under the brand name Benadryl among others, is an antihistamine and sedative. It is a first-generation H 1-antihistamine and it works by blocking certain effects of histamine, which produces its antihistamine and sedative effects. [11] [2] Diphenhydramine is also a potent anticholinergic. [12]
It is a first-generation antihistamine and works by blocking the histamine H 1 receptor. [2] Common side effects include sleepiness, restlessness, and weakness. Other side effects may include dry mouth and wheeziness. [2] Chlorpheniramine was patented in 1948 and came into medical use in 1949. [3] It is available as a generic medication and ...
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