Second-generation antihistamines: a study of poisoning in children
Eva Verdu, Ingrid Blanc-Brisset, Géraldine Meyer, Gaël Le Roux, Chloé Bruneau & Marie Deguigne
Received 21 Feb 2019, Accepted 08 Jun 2019, Published online: 04 Jul 2019
Download citation https://doi.org/10.1080/15563650.2019.1634812
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Abstract
Background and objectives: The toxicity of second-generation antihistamines after an overdose by a child is still unknown. The objective of this study is to use data from Poisons Centres in France to describe the toxicity profile of second-generation antihistamines for children and to compare the severity of poisoning observed from these with a first-generation antihistamine.
Method: This was a retrospective, multi-centre and observational study focusing on human cases of single-substance exposure to a second-generation antihistamine and to mequitazine, reported between 1 January 2001 and 31 December 2016 in Poisons Centres in France.
Results: From a total of 9403 children included, 5980 were exposed to a second-generation antihistamine and 3423 were exposed to mequitazine. The severity of exposure to second-generation antihistamines in children is low: among the children followed until a known outcome, 9% of children were symptomatic and in 97% of cases, the symptoms shown were of a minor-level severity (primarily drowsiness or restlessness). Depending on the substance, children who ingested doses 16 to 69 times the maximum recommended therapeutic dose remained asymptomatic. No deaths or severe symptoms were observed. No cases of lengthening of the QT interval or arrhythmias were identified. Mequitazine led to more symptoms than other substances (14.8% symptomatic children vs. 7.5%, Odd ratio (OR): 2.3 (2.0–2.6), p < 0.0001), more symptoms of moderate intensity (1.4 vs. 0.2%, OR: 8.3 (4.1–18.5), p < 0.0001) and more hospitalisation (19.1 vs. 8.7%, OR: 2.5, 95% CI: (2.2–2.8), p < 0.0001).
Conclusion: The severity of poisoning from second-generation antihistamines appears to be low among children and considerably lower than poisoning caused by mequitazine.
Key Words: Anti-allergic agents, histamine H1 antagonists, drug overdose, pediatrics
Second-generation antihistamines: a comparative review.
Slater JW1, Zechnich AD, Haxby DG.
Author information
1
College of Pharmacy, Oregon State University, Portland, USA.
Abstract
Second-generation histamine H1 receptor antagonists (antihistamines) have been developed to reduce or eliminate the sedation and anticholinergic adverse effects that occur with older H1 receptor antagonists. This article evaluates second-generation antihistamines, including acrivastine, astemizole, azelastine, cetirizine, ebastine, fexofenadine, ketotifen, loratadine, mizolastine and terfenadine, for significant features that affect choice. In addition to their primary mechanism of antagonising histamine at the H1 receptor, these agents may act on other mediators of the allergic reaction. However, the clinical significance of activity beyond that mediated by histamine H1 receptor antagonism has yet to be demonstrated. Most of the agents reviewed are metabolised by the liver to active metabolites that play a significant role in their effect. Conditions that result in accumulation of astemizole, ebastine and terfenadine may prolong the QT interval and result in torsade de pointes. The remaining agents reviewed do not appear to have this risk. For allergic rhinitis, all agents are effective and the choice should be based on other factors. For urticaria, cetirizine and mizolastine demonstrate superior suppression of wheal and flare at the dosages recommended by the manufacturer. For atopic dermatitis, as adjunctive therapy to reduce pruritus, cetirizine, ketotifen and loratadine demonstrate efficacy. Although current evidence does not suggest a primary role for these agents in the management of asthma, it does support their use for asthmatic patients when there is coexisting allergic rhinitis, dermatitis or urticaria.
Comment in
Cardiotoxicity of second-generation antihistamines.
PMID: 9951950 DOI: 10.2165/00003495-199957010-00004
Eva Verdu, Ingrid Blanc-Brisset, Géraldine Meyer, Gaël Le Roux, Chloé Bruneau & Marie Deguigne
Received 21 Feb 2019, Accepted 08 Jun 2019, Published online: 04 Jul 2019
Download citation https://doi.org/10.1080/15563650.2019.1634812
Select Language▼
Translator disclaimer
Abstract
Background and objectives: The toxicity of second-generation antihistamines after an overdose by a child is still unknown. The objective of this study is to use data from Poisons Centres in France to describe the toxicity profile of second-generation antihistamines for children and to compare the severity of poisoning observed from these with a first-generation antihistamine.
Method: This was a retrospective, multi-centre and observational study focusing on human cases of single-substance exposure to a second-generation antihistamine and to mequitazine, reported between 1 January 2001 and 31 December 2016 in Poisons Centres in France.
Results: From a total of 9403 children included, 5980 were exposed to a second-generation antihistamine and 3423 were exposed to mequitazine. The severity of exposure to second-generation antihistamines in children is low: among the children followed until a known outcome, 9% of children were symptomatic and in 97% of cases, the symptoms shown were of a minor-level severity (primarily drowsiness or restlessness). Depending on the substance, children who ingested doses 16 to 69 times the maximum recommended therapeutic dose remained asymptomatic. No deaths or severe symptoms were observed. No cases of lengthening of the QT interval or arrhythmias were identified. Mequitazine led to more symptoms than other substances (14.8% symptomatic children vs. 7.5%, Odd ratio (OR): 2.3 (2.0–2.6), p < 0.0001), more symptoms of moderate intensity (1.4 vs. 0.2%, OR: 8.3 (4.1–18.5), p < 0.0001) and more hospitalisation (19.1 vs. 8.7%, OR: 2.5, 95% CI: (2.2–2.8), p < 0.0001).
Conclusion: The severity of poisoning from second-generation antihistamines appears to be low among children and considerably lower than poisoning caused by mequitazine.
Key Words: Anti-allergic agents, histamine H1 antagonists, drug overdose, pediatrics
Second-generation antihistamines: a comparative review.
Slater JW1, Zechnich AD, Haxby DG.
Author information
1
College of Pharmacy, Oregon State University, Portland, USA.
Abstract
Second-generation histamine H1 receptor antagonists (antihistamines) have been developed to reduce or eliminate the sedation and anticholinergic adverse effects that occur with older H1 receptor antagonists. This article evaluates second-generation antihistamines, including acrivastine, astemizole, azelastine, cetirizine, ebastine, fexofenadine, ketotifen, loratadine, mizolastine and terfenadine, for significant features that affect choice. In addition to their primary mechanism of antagonising histamine at the H1 receptor, these agents may act on other mediators of the allergic reaction. However, the clinical significance of activity beyond that mediated by histamine H1 receptor antagonism has yet to be demonstrated. Most of the agents reviewed are metabolised by the liver to active metabolites that play a significant role in their effect. Conditions that result in accumulation of astemizole, ebastine and terfenadine may prolong the QT interval and result in torsade de pointes. The remaining agents reviewed do not appear to have this risk. For allergic rhinitis, all agents are effective and the choice should be based on other factors. For urticaria, cetirizine and mizolastine demonstrate superior suppression of wheal and flare at the dosages recommended by the manufacturer. For atopic dermatitis, as adjunctive therapy to reduce pruritus, cetirizine, ketotifen and loratadine demonstrate efficacy. Although current evidence does not suggest a primary role for these agents in the management of asthma, it does support their use for asthmatic patients when there is coexisting allergic rhinitis, dermatitis or urticaria.
Comment in
Cardiotoxicity of second-generation antihistamines.
PMID: 9951950 DOI: 10.2165/00003495-199957010-00004
Antihistamines, 2nd Generation
- Alavert
- Allegra
- Allegra Allergy 12 Hour
- Allegra Allergy 24 Hour
- Aller-Tec
- cetirizine
- Children's Allegra Allergy
- Children's Zyrtec Allergy
- Children's Zyrtec Hives Relief
- Clarinex
- Clarinex RediTabs
- Claritin
- Claritin RediTabs
- desloratadine
- fexofenadine
- levocetirizine
- loratadine
- Mucinex Allergy
- PediaCare Children's 24 Hour Allergy
- QlearQuil All Day & All Night 24 Hour Allergy Relief
- Wal-Zyr
- Xyzal
- Xyzal Allergy 24HR Oral Solution
- Xyzal Allergy 24HR Tablets
- Zyrtec
- Zyrtec Allergy
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