Literature DB >> 2908767

What are the differences between the H2-receptor antagonists?

W Schunack1.   

Abstract

The H2-receptor antagonists which are used for ulcer therapy fall into four main structural classes. Cimetidine is an imidazole derivative; ranitidine belongs to the basically substituted furans, famotidine is a member of the guanidinothiazole group; and roxatidine belongs to the aminoalkylphenoxy series. Famotidine is the most potent, selective H2-receptor antagonist yet available for ulcer therapy. On a weight basis, famotidine is approximately eight times more potent than ranitidine and 40 times more potent than cimetidine. Cimetidine, ranitidine and famotidine are competitive antagonists, while the long-acting H2-receptor antagonists, e.g. loxtidine and lamitidine, are insurmountable H2-receptor blockers. Famotidine has a longer duration of action than either ranitidine or cimetidine. Because famotidine does not interact with cytochrome P-450 of the hepatic enzyme system, it does not appear to affect the metabolism of drugs metabolized by this system. The overall number of side-effects of the H2-receptor antagonists is in the range of 2-3% and no irreversible adverse effects are known. Famotidine has been found to be generally well tolerated. In a first post-marketing study, the number of patients with side-effects was only 0.43%. Side-effects such as headache, dizziness, constipation and diarrhoea have been observed only occasionally. Thus, famotidine is a safe and potent H2-receptor blocker of acid secretion.

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Year:  1987        PMID: 2908767     DOI: 10.1111/j.1365-2036.1987.tb00658.x

Source DB:  PubMed          Journal:  Aliment Pharmacol Ther        ISSN: 0269-2813            Impact factor:   8.171


  6 in total

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2.  Characterization of histamine H2-receptors in human neutrophils with a series of guanidine analogues of impromidine. Are cell type-specific H2-receptors involved in the regulation of NADPH oxidase?

Authors:  R Burde; A Buschauer; R Seifert
Journal:  Naunyn Schmiedebergs Arch Pharmacol       Date:  1990-05       Impact factor: 3.000

Review 3.  Nephrotoxicity and hepatotoxicity of histamine H2 receptor antagonists.

Authors:  A A Fisher; D G Le Couteur
Journal:  Drug Saf       Date:  2001-01       Impact factor: 5.606

4.  RP-HPLC Method Development and Validation of Synthesized Codrug in Combination with Indomethacin, Paracetamol, and Famotidine.

Authors:  Mohyeddin Assali; Murad Abualhasan; Nihal Zohud; Noura Ghazal
Journal:  Int J Anal Chem       Date:  2020-07-01       Impact factor: 1.885

5.  Histamine inhibits activation of human neutrophils and HL-60 leukemic cells via H2-receptors.

Authors:  R Burde; R Seifert; A Buschauer; G Schultz
Journal:  Naunyn Schmiedebergs Arch Pharmacol       Date:  1989-12       Impact factor: 3.000

6.  Influence of histamine receptor antagonists on the dynamics of the cutaneous hypersensitivity reaction in patients infected with schistosoma haematobium.

Authors:  J R Snyman; D K Sommers; M D Gregorowski
Journal:  Eur J Clin Pharmacol       Date:  1993       Impact factor: 2.953

  6 in total

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