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What are the differences between the H2-receptor antagonists?

W Schunack1

  • 1Institute of Pharmacy, Free University of Berlin, FRG.

Alimentary Pharmacology & Therapeutics
|January 1, 1987
PubMed
Summary
This summary is machine-generated.

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Famotidine is a potent H2-receptor antagonist for ulcer therapy, showing greater efficacy and longer action than older drugs. It is well-tolerated with minimal side effects, making it a safe choice for acid secretion blockade.

Area of Science:

  • Pharmacology
  • Gastroenterology

Background:

  • H2-receptor antagonists are crucial for ulcer therapy.
  • Four main structural classes exist: imidazole, furan, guanidinothiazole, and aminoalkylphenoxy derivatives.

Purpose of the Study:

  • To evaluate famotidine as a potent and selective H2-receptor antagonist.
  • To compare famotidine's efficacy and safety with other H2-receptor antagonists.

Main Methods:

  • Comparative analysis of H2-receptor antagonist potency and selectivity.
  • Assessment of duration of action and drug interaction profiles.
  • Review of post-marketing safety data and side-effect incidence.

Main Results:

  • Famotidine is the most potent and selective H2-receptor antagonist available.

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  • On a weight basis, famotidine is 8x more potent than ranitidine and 40x more potent than cimetidine.
  • Famotidine exhibits a longer duration of action and does not inhibit cytochrome P-450, avoiding drug metabolism interactions.

    • Conclusions:

    • Famotidine is a highly effective and safe H2-receptor blocker for acid secretion.
    • Its favorable safety profile, with a low incidence of side effects (0.43% in post-marketing studies), makes it well-tolerated.
    • Famotidine represents a significant advancement in ulcer therapy due to its potency, selectivity, and safety.