Substrates of Human CYP2D6
Shufeng Zhou in Cytochrome P450 2D6, 2018
Antihistamines are used in the treatment of allergies. First-generation histamine H1 receptor antagonists, such as diphenhydramine, chlorpheniramine (chlorphenamine), triprolidine, and hydroxyzine, frequently cause somnolence or other CNS adverse effects. Second-generation antihistamines such as terfenadine, astemizole, loratadine, and cetirizine, being more lipophobic, offer the advantages of a lack of CNS and cholinergic effects such as sedation and dry mouth (Oppenheimer and Casale 2002). However, terfenadine and astemizole have been withdrawn from the market because both drugs have shown rare but fatal cardiotoxic side effects (e.g., QT interval prolongation). The third-generation antihistamines, metabolites of the earlier drugs (e.g., fexofenadine, levocetirizine, and desloratadine), have demonstrated no cardiac effects of the parent drugs and are at least as potent as their parent molecules et al.
United Airways
Jonathan A. Bernstein, Mark L. Levy in Clinical Asthma, 2014
Antihistamines are useful for mild symptoms, either intermittent or persistent. In the latter case, regular daily use is advisable because when they are withdrawn the histamine receptor becomes more active and the symptoms can increase. Antihistamines are active against sneezing, rhinorrhea, and nasal itch, but are inferior to nasal corticosteroids in reducing nasal congestion. Most second-generation oral antihistamines (loratidine, cetirizine, fexofenadine, desloratidine, levocetirizine, misolastine, rupatadine) reduce symptoms within 1 hour and are used once daily. Acrivastine is an exception to this rule; it has a rapid onset of action, but lasts only 8 hours. Topical nasal antihistamines are available as azelastine and olopatadine, which have a 15-minute onset of action.
Interaction of Alcohol with Medications and Other Drugs
John Brick in Handbook of the Medical Consequences of Alcohol and Drug Abuse, 2012
Antihistamines (H1-antagonists) are the mainstay of symptomatic therapy for allergic disorders. Drugs such as diphenhydramine (Benadryl and others) are available without prescription to treat allergic symptoms. Others, such as hydroxyzine (Vistaril, Atarax), are used to treat anxiety and require a prescription. Many antihistamines cause drowsiness, which make them useful to treat insomnia, but potentially dangerous because they can impair skills necessary for safe motor vehicle operation or other complex divided attention tasks. Alcohol can substantially enhance the sedating effects of these agents and may further impair the ability to drive or operate other types of machinery (Ridout et al., 2003). Many common sedative antihistamines, such as chlorpheniramine and diphenhydramine, significantly impair psychomotor performance and significantly increase the deleterious effects of alcohol on reaction time, coordination, and related psychophysical tests (Burns, 1989; Burns and Mostowitz, 1980; Franks et al., 1979).
A primer on sleeping, dreaming, and psychoactive agents
Published in Journal of Social Work Practice in the Addictions, 2023
Antihistamines, first used therapeutically in the 1940s, constitute a diverse group of drugs that can inhibit histaminic actions in the body. They are structurally similar to histamine, a chemical found throughout the human body, and act to prevent histamine–receptor interaction through competition with histamine for histamine receptors. The primary function of antihistamines is to aid with allergies, excessive stomach acid, and motion sickness. Antihistamines can be used as sleep-inducing agents as they can produce sedation; however, they do not produce high-quality sleep. This leads to more time spent in stages one and two sleep and less in stage three. Older generation antihistamines also reduce REM sleep, impair learning, and reduce work efficiency (Church et al., 2010; Raman-Wilms, 2014).
A primer on sleeping, dreaming, and psychoactive agents
Published in Journal of Social Work Practice in the Addictions, 2023
Antihistamines, first used therapeutically in the 1940s, constitute a diverse group of drugs that can inhibit histaminic actions in the body. They are structurally similar to histamine, a chemical found throughout the human body, and act to prevent histamine-receptor interaction through competition with histamine for histamine receptors. The primary function of antihistamines is to aid with allergies, excessive stomach acid, and motion sickness. Antihistamines can be used as sleep-inducing agents as they can produce sedation; however, they do not produce high-quality sleep. This leads to more time spent in stages one and two sleep and less in stage three. Older generation antihistamines also reduce REM sleep, impair learning, and reduce work efficiency (Church et al., 2010; Raman-Wilms, 2014).
Efficiency and safety of desloratadine in combination with compound glycyrrhizin in the treatment of chronic urticaria: a meta-analysis and systematic review of randomised controlled trials
Published in Pharmaceutical Biology, 2021
Yulong Wen, Yidan Tang, Miaoyue Li, Yu Lai
According to most of the current hypotheses, CU is caused by the action of histamines and the H receptor involving the pathogenesis of autoimmunity (Su et al. 2020). Therefore, antihistamine drugs are widely applied in clinical treatment. Desloratadine, a second-generation H1 receptor antagonist, is highly selective for peripheral H1 receptors (Liang et al. 2014). In a related study, it was suggested that the efficacy and safety of desloratadine in the treatment of CU is obviously superior to that of other antihistamines, such as cetirizine, mizolastine, or loratadine. As a result, it is considered to have good efficacy and reliable safety in the treatment of urticaria (Lang et al. 2019). Nevertheless, the efficacy of desloratadine alone is limited, and the CU recurrence rate is relatively high (Maurer et al. 2013; Sui et al. 2018).
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