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First-generation antihistamines are widely available without a prescription and commonly used to treat allergic symptoms, including rhinitis, conjunctivitis, pruritus, eczema, urticaria, and anaphylactic reactions.

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(20) When introduced into the nose, histamine causes dilatation and leakage of blood vessels. 6 Antihistamine medications block or reduce histamine-mediated effects at one of four identified histamine receptors (see Table 1 below).These include the first-generation H1 antagonists, or sedating antihistamines (eg, diphenhydramine, chlorpheniramine), and second-generation H1 receptor blockers, or nonsedating antihistamines (eg, loratadine, cetirizine).In 2014 antihistamines such as desloratadine were found to be effective as adjuvants to standardized treatment of acne due to their anti-inflammatory properties and their ability to suppress sebum production.receptor and heightens the receptor's activity; the receptor antagonists work by binding to the receptor and blocking the activation of the receptor by histamine; by comparison, the inverse agonists bind to the receptor and reduce its activity, an effect which is opposite to histamine's.-antihistamines can also reduce inflammation, since the expression of NF-κB, the transcription factor the regulates inflammatory processes, is promoted by both the receptor's constitutive activity and agonist (i.e., histamine) binding at the H Second-generation antihistamines cross the blood–brain barrier to a much lower degree than the first-generation antihistamines.Tension headaches also can be triggered by external conditions such as stress, depression or anxiety.However, tension headache triggers are not limited to the previous list. So, how do you tell a tension headache apart from a migraine headache?Diphenhydramine (Benadryl) is the most common first-generation antihistamine found in OTC sleep aids, whether used alone or in combination with pain relievers, including acetaminophen (eg, Tylenol PM), ibuprofen (eg, Advil PM), and aspirin.Other sleep aids often contain the antihistamine doxylamine (eg, Unisom).Their main benefit is they primarily affect peripheral histamine receptors and therefore are less sedating.However, high doses can still induce the central nervous system drowsiness.Histamine produces increased vascular permeability, causing fluid to escape from capillaries into tissues, which leads to the classic symptoms of an allergic reaction — a runny nose and watery eyes. Antihistamines suppress the histamine-induced wheal response (swelling) and flare response (vasodilation) by blocking the binding of histamine to its receptors or reducing histamine receptor activity on nerves, vascular smooth muscle, glandular cells, endothelium, and mast cells.Itching, sneezing, and inflammatory responses are suppressed by antihistamines that act on H1-receptors.Histamine may also have a role in causing coughs, but this is less certain.There are two classes of antihistamines, the older ("first generation", "sedating") and the newer ("second generation", "non-sedating") classes.




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