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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.
Chlorphenamine is an alkylamine and is a part of a series of antihistamines including pheniramine (Naphcon) and its halogenated derivatives including fluorpheniramine, dexchlorphenamine (Polaramine), brompheniramine (Dimetapp), dexbrompheniramine (Drixoral), deschlorpheniramine, and iodopheniramine.
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]
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]
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.
Cetirizine is a second-generation antihistamine used to treat allergic rhinitis (hay fever), dermatitis, and urticaria (hives). [5] It is taken by mouth. [6] Effects generally begin within thirty minutes and last for about a day. [6] The degree of benefit is similar to other antihistamines such as diphenhydramine, which is a first-generation ...
Pheniramine (trade name Avil among others) is an antihistamine with anticholinergic properties used to treat allergic conditions such as hay fever or urticaria.It has relatively strong sedative effects, and may sometimes be used off-label as an over-the-counter sleeping pill in a similar manner to other sedating antihistamines such as diphenhydramine.
It is a second-generation antihistamine and works by blocking the release of a number of inflammatory mediators including histamine. [7] [8] Azelastine was patented in 1971 and came into medical use in 1986. [10] It is available as a generic medication.