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Xenobiotica
the fate of foreign compounds in biological systems
Volume 20, 1990 - Issue 2
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Research Article

Aspirin acetylates the tricyclic antidepressant amoxapine spontaneously to N-acetylamoxapine in vitro and in vivo

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Pages 169-176 | Received 21 Mar 1989, Accepted 10 Sep 1989, Published online: 22 Sep 2008
 

Abstract

1. N-Acetylamoxapine is formed nonenzymically in vitro, and in mice, from amoxapine, a tricyclic antidepressant, and aspirin.

2. Formation of acetylamoxapine from amoxapine and aspirin in vitro was maximal at pH5.0 since this pH optimized reactant solubilities as well as decreasing aspirin hydrolysis.

3. Formation of acetylamoxapine from amoxapine and aspirin in mouse stomachs was rapid, and the pH study indicates that the intestinal pH would favour formation even more.

4. Acetylamoxapine administered to mice produced the same CNS-related signs, leading to death, as with amoxapine, but much larger doses and longer time periods were required to elicit these effects. As brain and liver levels of amoxapine in animals dying from acetylamoxapine administration were less than half those found in animals given lethal doses of amoxapine, the toxicity in mice of acetylamoxapine may not be due solely to deacetylation of acetylamoxapine to the parent compound.

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