Effects of metronidazole and its metabolites on histamine immunosuppression activity.

Abstract:

:We have previously reported that metronidazole treatment increases human lymphocyte proliferation showing individual differences. This drug and its metabolites are imidazole compounds like histamine and cimetidine. The first is an endogenous amine that inhibits T-helper lymphocyte proliferation, and the second is a histamine antagonist. We presently report the in vitro effects of histamine, cimetidine, imidazole, metronidazole and its two principal metabolites (the acetic acid and hydroxy forms), on the mitogenic response to phytohemagglutinin (PHA) stimulation of human peripheral blood lymphocytes. Histamine decreased lymphocyte proliferation while (in order of potency) cimetidine, the hydroxy metabolite of metronidazole, imidazole and metronidazole, increased the mitogenic response to PHA in a dose-response fashion. The acetic acid metabolite lacked immunomodulatory effects. Competitive studies showed that cimetidine, metronidazole, and the hydroxy metabolite blocked the inhibitory effect of histamine on lymphocyte proliferation in a dose-related manner. This blockage was non-competitive, suggesting that the target of the imidazole compounds was not the active site of the H2 receptor.

journal_name

Life Sci

journal_title

Life sciences

authors

Elizondo G,Ostrosky-Wegman P

doi

10.1016/0024-3205(96)00297-4

subject

Has Abstract

pub_date

1996-01-01 00:00:00

pages

285-97

issue

4

eissn

0024-3205

issn

1879-0631

pii

0024320596002974

journal_volume

59

pub_type

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