Formation of nitroso compounds and mutagens from cinnarizine, ethambutol, piromidic acid, pyridinol carbamate and tiaramide by drug/nitrite interaction.

Abstract:

:The formation of nitroso compounds and mutagens from 5 nitrogen-containing drugs (cinnarizine, ethambutol, piromidic acid, pyridinol carbamate and tiaramide) by drug/nitrite interaction was examined. On the reaction of 50 micrometers drug and 500 micrometers nitrite at pH 3.0--3.4 and 37 degrees C for 4 h, the considerable formation of nitroso compounds was observed for ethambutol, cinnarizine and pyridinol carbamate. The reaction product of pyridinol carbamate and nitrite was remarkably mutagenic to Salmonella typhimurium TA100 in the absence of S-9 mix. Under conditions presumed to resemble those in the stomach after ingestion of a therapeutic dose of the drug, the formation of nitroso compounds was observed for ethambutol and significant mutagenicity was detected in the reaction product of pyridinol carbamate.

journal_name

Cancer Lett

journal_title

Cancer letters

authors

Takeda Y,Kanaya H

doi

10.1016/0304-3835(82)90075-1

subject

Has Abstract

pub_date

1982-01-01 00:00:00

pages

53-9

issue

1

eissn

0304-3835

issn

1872-7980

pii

0304-3835(82)90075-1

journal_volume

15

pub_type

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