Histamine2-receptor antagonists: Rapid development of tachyphylaxis with repeat dosing

• Published in: World journal of gastrointestinal pharmacology and therapeutics 2014-05, Vol.5 (2), p.57-62
• Main Authors: McRorie, Johnson W, Kirby, James A, Miner, Philip B
• Format: Article
• Language: English
• Subjects: antagonist; Tachyphylaxis; Tolerance; Gastric; Histamine2-receptor; Review
• ISSN: 2150-5349; 2150-5349
• DOI: 10.4292/wjgpt.v5.i2.57

Histamine2-receptor antagonists（H2RAs） are availableover-the-counter （OTC） for the treatment and prevention of heartburn, but more than occasional, singledose use can lead to rapid development of tachyphylaxis. The aim of this review is to assess the publishedevidence regarding the development of tachyphylaxiswith repeat usage of H2RAs. PubMed and SCOPUS were searched across all years to identify clinical studies thatexamined the development of tachyphylaxis with repeated dosing of H2RAs. Although a single （first） doseof an H2RA can be effective for controlling gastric acidand preventing or relieving food-related heartburn, numerous studies confirm that tachyphylaxis, also knownas tolerance, is consistently detected at the first timepoint assessed after the first dose, including the second day and/or second dose. Even if symptom relief isachieved with an H2RA, it may be due to desensitizationof the esophagus to acid exposure, potentially providingsymptom relief without significantly decreasing esophageal acid exposure. When recommending OTC drugsfor treatment of frequent heartburn, clinicians shouldbe aware of the potential for rapid development oftachyphylaxis in patients who use H2RAs for 2 or more consecutive days. Even if symptom relief is achieved, it may be due to desensitization of the esophagus to acid by the H2RA, potentially providing symptom relief without significantly decreasing esophageal acid exposure. Other strategies, such as an OTC proton pump inhibitor, may be needed to optimize management of frequent heartburn.