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
-
Novel Agents Aiming at Specific Molecular Targets Increase Chemosensitivity and Overcome Chemoresistance in Hematopoietic Malignancies
Current Pharmaceutical Design Genetic Predictors of Drug Hypersensitivity
Current Pharmaceutical Design Dipeptidyl Peptidase-4 Inhibition: Linking Chemical Properties to Clinical Safety
Current Medicinal Chemistry Editorial [Hot Topic: Antihistamines (Guest Editor: Esen Ozkaya)]
Current Medicinal Chemistry - Anti-Inflammatory & Anti-Allergy Agents Macrolides Allergy
Current Pharmaceutical Design A New Binding Site Involving the C-terminal Domain to Design Specific Inhibitors of PepX
Protein & Peptide Letters A Brief Review of Cardiovascular Diseases, Associated Risk Factors and Current Treatment Regimes
Current Pharmaceutical Design The Role of Inflammation and Allergy in Acute Coronary Syndromes
Inflammation & Allergy - Drug Targets (Discontinued) Could Additional Inhibitors of the Renin -Angiotensin System be Clinically Useful?
Current Hypertension Reviews Drugs in Pediatric Ischemic Stroke
Current Drug Targets Efalizumab
Anti-Inflammatory & Anti-Allergy Agents in Medicinal Chemistry Classic Histamine H1 Receptor Antagonists: A Critical Review of their Metabolic and Pharmacokinetic Fate from a Birds Eye View
Current Drug Metabolism Complement System in SLE as a Target for Antibodies
Current Rheumatology Reviews Kinin Receptors in Vascular Biology and Pathology
Current Vascular Pharmacology Editorial [Hot Topic: An Update on the Diagnosis of Allergic and Non-Allergic Drug Hypersensitivity (Executive Editors: M.T. Ventura and A. Romano) ]
Current Pharmaceutical Design Chemistry and Pharmacology of Angiotensin-Converting Enzyme Inhibitors
Current Pharmaceutical Design A Closer Look to Polyesters: Properties, Synthesis, Characterization, and Particle Drug Delivery Applications
Nanoscience & Nanotechnology-Asia Discovery of Highly Potent Small Molecule Kallikrein Inhibitors
Medicinal Chemistry Editorial: (New Drug (LCZ696) for the Treatment of Heart Failure with Reduced Ejection Fraction After 10 Years. Can One Study Change the Guidelines?)
Current Vascular Pharmacology Inflammation-Mediating Proteases: Structure, Function in (Patho) Physiology and Inhibition
Protein & Peptide Letters