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World J Gastrointest Pharmacol Ther. May 6, 2014; 5(2): 57-62
Published online May 6, 2014. doi: 10.4292/wjgpt.v5.i2.57
Published online May 6, 2014. doi: 10.4292/wjgpt.v5.i2.57
Histamine2-receptor antagonists: Rapid development of tachyphylaxis with repeat dosing
Johnson W McRorie, Quantitative Sciences, Procter and Gamble, Mason, OH 45040, United States
James A Kirby, Corporate Pharmacy, The Kroger Company, Cincinnati, OH 45246, United States
Philip B Miner, President, Oklahoma Foundation for Digestive Research, Oklahoma City, OK 73104, United States
Author contributions: McRorie JW drafted the review; Kirby JA and Miner PB edited the review and provided important intellectual content.
Correspondence to: Johnson W McRorie, PhD, FACG, AGAF, Quantitative Sciences, Procter and Gamble, 8700 Mason-Montgomery Road, Mason, OH 45040, United States. mcrorie.jw@pg.com
Telephone: +1-513-6221423 Fax: +1-513-2777917
Received: October 22, 2013
Revised: January 10, 2014
Accepted: March 3, 2014
Published online: May 6, 2014
Revised: January 10, 2014
Accepted: March 3, 2014
Published online: May 6, 2014
Core Tip
Core tip: Histamine2-receptor antagonists (H2RAs) are available over-the-counter (OTC) for the treatment and prevention of heartburn, but recommendations for use should be limited to those with infrequent heartburn. A single dose of an H2RA can be effective for controlling gastric acid and preventing or relieving heartburn, but tolerance (tachyphylaxis) develops rapidly, and is evident by the second day/second dose. 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. For frequent heartburn (≥ 2 d/wk), an OTC proton pump inhibitor should be considered.