Sedative effects of antihistamines
Abstract
The central effects of a newly developed, long-acting H1 antihistamine, loratadine (10 and 40 mg), were compared with those of a standard H1 antihistamine, diphenhydramine (50 mg three times a day) with measures of performance and daytime sleepiness (multiple sleep latency test). Sixteen healthy adults (six women and 10 men), 19 to 35 years of age, received each of the drugs and placebo for 2 days, separated by 5 days at home. Each day, the drug or placebo was administered at 8 A.M. and 12 and 4 P.M. Diphenhydramine was administered in three equal doses (50 mg), and loratadine was administered in a single dose followed by two placebo doses. Mean latency to sleep on tests done at 9 and 11 A.M. and 1, 3, and 5 P.M. was reduced significantly with diphenhydramine compared to placebo, whereas neither loratadine dose reduced sleep latency. Performance measured at 9:30 P.M. and 1:30 P.M. with a battery of tests, including reaction time, vigilance, digit symbol substitution, and symbol copying tasks demonstrated a significant reduction in symbols copied and digits substituted after diphenhydramine compared to both loratadine doses. These results demonstrate that loratadine (10 and 40 mg doses) did not have clinically significant central nervous system activity, whereas diphenhydramine increases sleepiness and disrupts performance efficiency.
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The DSST could statistically significantly distinguish the cognitive effect of the H1 antagonist diphenhydramine from placebo with an effect size of 0.28.
“The authors demonstrated that the DSST could statistically significantly distinguish the cognitive effect of the H1 antagonist diphenhydramine from placebo with an effect size of 0.28 (calculated from the published statistics).”
From Digit Symbol Substitution Test: The Case for Sensitivity Over Specificity in Neuropsychological Testing (2018) · cites this paper as [32]
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- Authors
- Roth, T., Roehrs, T., Koshorek, G., Sicklesteel, J., & Zorick, F.
- ORCID
- Venue
- Journal of Allergy and Clinical Immunology
- Publisher
- Elsevier BV
- Published
- 1987-07
- Volume
- 80
- Issue
- 1
- Pages
- 94-98
- ISSN
- 0091-6749 (ISSN-L)
- OpenAlex
- W2012513486
- Semantic Scholar
- 95f3254ac3e2a3785305a180748e3b4965485bc0
- Cited by
- 151
- References
- 11
- Citations by year
- 2026: 3 · 2025: 3 · 2024: 1 · 2023: 3 · 2022: 1 · 2021: 4 · 2020: 2 · 2019: 2 · 2018: 2 · 2017: 1 · 2016: 4 · 2015: 2 · 2014: 2
- FWCI
- 1.82
- Type
- journal article
- Language
- en
- Open access
- closed
- Locations
- Journal of Allergy and Clinical Immunology (publishedVersion)
- PubMed (publishedVersion)
- Topics
- Life Sciences › Immunology and Microbiology › Immunology › Mast cells and histamine
- Social Sciences › Psychology › Experimental and Cognitive Psychology › Sleep and Work-Related Fatigue
- Health Sciences › Medicine › Immunology and Allergy › Allergic Rhinitis and Sensitization
- Keywords
- loratadine, diphenhydramine, histamine H1 receptor antagonists, sedative effects, daytime sleepiness, sleep latency, central nervous system effects, cognitive performance, reaction time, sustained attention
- MeSH terms
- Adult, Cyproheptadine, Diphenhydramine, Female, Histamine H1 Antagonists, Humans, Hypnotics and Sedatives, Male, Sleep, Loratadine
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