Sedating antihistamines and


10-Nov-2018 03:43

Antihistamines are a class of agents that block histamine release from histamine-1 receptors and are mostly used to treat allergies or cold and flu symptoms, although some first-generation antihistamines may also be used for other conditions.

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Second generation antihistamines were developed in the 1980s and are much less sedating than first-generation antihistamines.

They act on histamine-1 receptors in the periphery and are unlikely to penetrate the brain, so are less likely to cause side effects or interact with drugs.

Most second-generation antihistamines do not cause drowsiness, although some (such as cetirizine and fexofenadine), may be more likely to do so at higher dosages.

The dichotomy between 1st and 2nd generation antihistamines was introduced in 1983 at about the time of the European registration of two drugs: terfenadine and astemizole.

The distinction was drawn by the drugs' manufactures to indicate a major pharmacological difference between these drugs and their predecessors.

The 2nd generation antihistamines were less soluble in lipid and thus less readily penetrated the blood brain barrier.



Antihistamines are classified into two groups – the first-generation “sedatingand second-generation “non-sedating”. Sedating antihistamines cause sedation as they are highly lipid soluble and readily cross the blood brain barrier. This sedating activity is sometimes used in managing conditions such as eczema where.… continue reading »


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CLASSIFICATION OF SEDATING ANTIHISTAMINES. TASK. To examine the safety of sedating antihistamines and produce a report suggesting the most appropriate schedule for both combination and single ingredient formulations of sedating antihistamines marketed in NZ. BACKGROUND. Allergic conditions affect about.… continue reading »


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Jan 10, 2018. Side effects might include daytime drowsiness, dry mouth and dizziness. Also, diphenhydramine and doxylamine — sedating antihistamines found in various over-the-counter sleep aids — aren't recommended for people who have closed-angle glaucoma, asthma, chronic obstructive pulmonary disease or.… continue reading »


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This page includes the following topics and synonyms Sedating Antihistamine, First Generation Antihistamine, Antihistamine, Chlorpheniramine, Bromopheniramine, Cyproheptadine, Hydroxyzine, Periactin, Atarax, Vistaril.… continue reading »


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They act as inverse agonists rather than antagonists of histamine H1-receptors which are members of the G-protein family. The older first generation H1-antihistamines penetrate readily into the brain to cause sedation, drowsiness, fatigue and impaired concentration and memory causing detrimental effects on learning and.… continue reading »


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Although the second generation antihistamines are known to all have similar efficacy, the extent of their sedative effects is not well established. To further examine the sedative effects of four commonly prescribed antihistamines—loratadine, cetirizine, fexofenadine, and acrivastine—we analysed the results of four.… continue reading »


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