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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).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.Because delirium and hallucinations can result from the use of anticholinergics including sedating antihistamines, patients receiving these medications are at risk of being prescribed antipsychotic medications.Cognitive decline, falls, and behaviors such as hallucinations, delirium, and agitated aggressive behaviors may result in affected patients being hospitalized or admitted to long term care facilities.Regardless of practice setting, healthcare professionals should take steps to increase the awareness of side effects associated with first-generation antihistamines.Educating older patients and their caregivers is especially important because of the widespread OTC availability of these antihistamines.H3 receptor antagonists could provide new treatment options for sleep disorders, weight loss, neuropathic pain, obesity, movement disorders, schizophrenia, attention deficit disorders, and Alzheimer’s dementia, while the development of antagonists for H4 receptors may lead to new treatment options for autoimmune inflammatory diseases.1,2 The first H1 sedating antihistamines have been available for more than 60 years and were synthesized based on a chemical structure similar to that used to develop cholinergic muscarinic antagonists, tranquilizers, and antihypertensive agents.These antihistamines have low receptor specificity and interact with both peripheral and central histamine receptors and readily cross the blood-brain barrier.
Topical antihistamine creams may be used to relieve pain and itching due to insect bites, minor cuts and burns, and to resolve rashes due to an allergy or plants such as poison ivy, poison oak, or poison sumac. Currently the only FDA-approved histamine antagonist medications block the effects of histamine at H1 or H2 receptor sites. 6 Antihistamine medications block or reduce histamine-mediated effects at one of four identified histamine receptors (see Table 1 below).Other sleep aids often contain the antihistamine doxylamine (eg, Unisom).H2 blockers (eg, ranitidine, famotidine) commonly are used for the treatment of heartburn and gastroesophageal reflux disease.