Abstract
H1-antihistamines are inverse agonists that combine with and stabilize inactive conformation of H1-receptors. Thus they interfere with actions of histamine at H1-receptors. They are widely used for treatment of allergic rhinitis, allergic conjunctivitis, urticaria, coughs, colds and insomnia. H1-antihistamines are classified as older ‘first generation’ and newer ‘second generation’. First generation H1-antihistamines have poor receptor H1-receptor selectivity, and cross blood-brain-barrier. They have a lot of adverse events such as anti-muscarinic, anti-α-adrenergic, anti-serotonin, and sedative effects. In contrast, second generation H1-antihistamines were highly selective for the histamine H1-receptor, do not cross the blood brain barrier, and have minimal adverse events. The risks of first-generation H1-antihistamines have been clearly underestimated, particularly when purchased as nonprescribed over the counter medications by public. This review summarizes curent literature to evaluate antihistamines including their mechanism, indications and side-effects.
Keywords: Adverse events, antihistamine(s), allergic rhinitis, atopic dermatitis, cardiotoxicity, histamine, pharmacology, receptor, sleep, urticaria
Anti-Inflammatory & Anti-Allergy Agents in Medicinal Chemistry
Title:Efficacy and Safety of H1-Antihistamines: An Update
Volume: 11 Issue: 3
Author(s): Fusun Kalpaklioglu and Ayse Baccioglu
Affiliation:
Keywords: Adverse events, antihistamine(s), allergic rhinitis, atopic dermatitis, cardiotoxicity, histamine, pharmacology, receptor, sleep, urticaria
Abstract: H1-antihistamines are inverse agonists that combine with and stabilize inactive conformation of H1-receptors. Thus they interfere with actions of histamine at H1-receptors. They are widely used for treatment of allergic rhinitis, allergic conjunctivitis, urticaria, coughs, colds and insomnia. H1-antihistamines are classified as older ‘first generation’ and newer ‘second generation’. First generation H1-antihistamines have poor receptor H1-receptor selectivity, and cross blood-brain-barrier. They have a lot of adverse events such as anti-muscarinic, anti-α-adrenergic, anti-serotonin, and sedative effects. In contrast, second generation H1-antihistamines were highly selective for the histamine H1-receptor, do not cross the blood brain barrier, and have minimal adverse events. The risks of first-generation H1-antihistamines have been clearly underestimated, particularly when purchased as nonprescribed over the counter medications by public. This review summarizes curent literature to evaluate antihistamines including their mechanism, indications and side-effects.
Export Options
About this article
Cite this article as:
Kalpaklioglu Fusun and Baccioglu Ayse, Efficacy and Safety of H1-Antihistamines: An Update, Anti-Inflammatory & Anti-Allergy Agents in Medicinal Chemistry 2012; 11 (3) . https://dx.doi.org/10.2174/1871523011202030230
DOI https://dx.doi.org/10.2174/1871523011202030230 |
Print ISSN 1871-5230 |
Publisher Name Bentham Science Publisher |
Online ISSN 1875-614X |
- Author Guidelines
- Graphical Abstracts
- Fabricating and Stating False Information
- Research Misconduct
- Post Publication Discussions and Corrections
- Publishing Ethics and Rectitude
- Increase Visibility of Your Article
- Archiving Policies
- Peer Review Workflow
- Order Your Article Before Print
- Promote Your Article
- Manuscript Transfer Facility
- Editorial Policies
- Allegations from Whistleblowers
Related Articles
-
Immunotherapy in Allergies: An Update
Inflammation & Allergy - Drug Targets (Discontinued) Provocation Tests in Diagnosing Drug Hypersensitivity
Current Pharmaceutical Design Immediate and Late Adverse Reactions to Iodinated Contrast Media: A Pharmacological Point of View
Anti-Inflammatory & Anti-Allergy Agents in Medicinal Chemistry Designed Multiple Ligands: Basic Research vs Clinical Outcomes
Current Medicinal Chemistry Inflammation and Coagulation in Urticaria and Angioedema
Current Vascular Pharmacology Reporting Rates of Yellow Fever Vaccine 17D or 17DD-Associated Serious Adverse Events in Pharmacovigilance Data Bases: Systematic Review
Current Drug Safety The Role of Immunosuppressive Medications in the Pathogenesis of Hypertension and Efficacy and Safety of Antihypertensive Agents in Kidney Transplant Recipients
Current Medicinal Chemistry Dipeptidyl Peptidase-4 Inhibitor Induced Angioedema – An Overlooked Adverse Drug Reaction?
Current Diabetes Reviews Life Threatening and Fatal Contrast Media Reactions: Pathomechanisms, Diagnosis, Prevention and Drug Management
Anti-Inflammatory & Anti-Allergy Agents in Medicinal Chemistry Interrelationships with Metabolic Syndrome, Obesity and Cardiovascular Risk
Current Vascular Pharmacology Pharmacogenomics of Asthma
Current Pharmaceutical Design What Does a Pediatrician Need to Know About Chronic Diarrhea?
Current Pediatric Reviews Conventional and Non-Conventional Targets of Natural Products in the Management of Diabetes Mellitus and Associated Complications
Current Medicinal Chemistry Unusual Food Allergy: AlioideaAllergic Reactions Overview
Recent Patents on Inflammation & Allergy Drug Discovery A Case of Pantoprazole Anaphylaxis with Cross Reactivity to All Proton Pump Inhibitors: Finding a Safe Alternative
Current Drug Safety “Something is Wrong in the Ras Kingdom” - Evidence for the Involvement of p21Ras/MAP Kinase in Autoimmune Diseases
Current Rheumatology Reviews New Insights on the Possible Role of Mast Cells in Aspirin-Induced Asthma
Current Molecular Pharmacology Prediction by Pharmacogenetics of Safety and Efficacy of Non-Steroidal Anti- Inflammatory Drugs: A Review
Current Drug Metabolism Perception of Symptoms in Hypertensive Patients and the Relevance to the Application of Anti- Hypertensive Drug Therapy
Current Pharmaceutical Design Plastid Molecular Pharming II. Production of Biopharmaceuticals by Plastid Transformation
Mini-Reviews in Medicinal Chemistry