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Histamine2-receptor antagonists: Rapid development of tachyphylaxis with repeat dosing
Johnson W McRorie1, James A Kirby1, Philip B Miner1
1Johnson W McRorie, Quantitative Sciences, Procter and Gamble, Mason, OH 45040, United States.
Summary
Histamine2-receptor antagonists (H2RAs) lose effectiveness rapidly with repeat use, leading to tachyphylaxis. This tolerance can occur by the second day, potentially masking symptoms without reducing acid exposure.
Area of Science:
- Gastroenterology
- Pharmacology
Background:
- Over-the-counter (OTC) Histamine2-receptor antagonists (H2RAs) are commonly used for heartburn relief.
- However, frequent or repeated use can lead to tachyphylaxis, diminishing their effectiveness.
Purpose of the Study:
- To review existing evidence on the development of tachyphylaxis with repeated H2RA usage.
- To inform clinical recommendations for managing frequent heartburn.
Main Methods:
- A systematic literature search of PubMed and SCOPUS was conducted.
- Studies examining tachyphylaxis development with repeated H2RA dosing were included.
Main Results:
- Tachyphylaxis, or tolerance, to H2RAs can develop rapidly, often by the second day or second dose.
- Symptom relief may occur due to esophageal desensitization, not necessarily reduced acid exposure.
- This tolerance impacts the efficacy of H2RAs for frequent heartburn management.
Conclusions:
- Clinicians must recognize the potential for rapid H2RA tachyphylaxis in patients using them for 2+ consecutive days.
- Alternative treatments, like OTC proton pump inhibitors, may be necessary for optimal frequent heartburn management.
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