The Laryngoscope · 2025
Histamine 2-Receptor Antagonists Tachyphylaxis: A Scoping Review.
СтатьяScoping ReviewНазвание и аннотация: Перевод пока не подготовлен
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Clark James H, Hussain Zilla, Akst Lee, Marks Stanley L, Belafsky Peter C
Аннотация
OBJECTIVE: Histamine 2-receptor antagonists (H2RAs) commonly treat gastroesophageal reflux disease (GERD). However, tachyphylaxis, defined as the rapid reduction of efficacy, is frequently reported and remains poorly understood. This investigation performed a scoping review on the decrease in H2RA efficacy with repeat dosing.
DATA SOURCE: Following PRISMA-ScR guidelines, we systematically searched PubMed, Embase, Scopus, Web of Science, and the Cochrane Database through August 27, 2025.
REVIEW METHOD: Two reviewers independently screened studies and extracted data on mechanisms, impact, and management strategies.
RESULTS: While H2RAs effectively reduce gastric acid secretion, continuous dosing leads to tachyphylaxis of unclear etiology. Initial H2RA treatment increases the percentage of time intragastric pH is > 4, from 8% to 38%. Tachyphylaxis begins by the second dose, 2, with an 11.2% reduction in efficacy by day 3. By day 15, tachyphylaxis results in a 13.0%-27.5% (mean: 20.3%) decrease in efficacy, after which no further reduction in effectiveness occurs. In comparison, once-daily proton pump inhibitors maintain a daily intragastric pH of 63% above 4, with no tachyphylaxis observed after 14 days.
CONCLUSION: Tachyphylaxis is a well-documented, diminished treatment effect observed across the entire class of H2RAs. It typically begins by day 2 and plateaus quickly, resulting in up to a quarter decrease in absolute efficacy. The precise mechanisms underlying H2RA tachyphylaxis remain uncertain. H2RAs should not be prescribed as first-line agents for the management of frequent GERD or routinely added in cases of incomplete response to PPIs.
DATA SOURCE: Following PRISMA-ScR guidelines, we systematically searched PubMed, Embase, Scopus, Web of Science, and the Cochrane Database through August 27, 2025.
REVIEW METHOD: Two reviewers independently screened studies and extracted data on mechanisms, impact, and management strategies.
RESULTS: While H2RAs effectively reduce gastric acid secretion, continuous dosing leads to tachyphylaxis of unclear etiology. Initial H2RA treatment increases the percentage of time intragastric pH is > 4, from 8% to 38%. Tachyphylaxis begins by the second dose, 2, with an 11.2% reduction in efficacy by day 3. By day 15, tachyphylaxis results in a 13.0%-27.5% (mean: 20.3%) decrease in efficacy, after which no further reduction in effectiveness occurs. In comparison, once-daily proton pump inhibitors maintain a daily intragastric pH of 63% above 4, with no tachyphylaxis observed after 14 days.
CONCLUSION: Tachyphylaxis is a well-documented, diminished treatment effect observed across the entire class of H2RAs. It typically begins by day 2 and plateaus quickly, resulting in up to a quarter decrease in absolute efficacy. The precise mechanisms underlying H2RA tachyphylaxis remain uncertain. H2RAs should not be prescribed as first-line agents for the management of frequent GERD or routinely added in cases of incomplete response to PPIs.