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Toxication
From Wikipedia, the free encyclopedia
Toxication is the process of drug metabolism in which the metabolite of a compound is more toxic than the parent drug or chemical.
Toxication may involve: 1. Changing the physicochemical properties to cause a change in the microenvironment 2. Increasing the potency of a compound 3. Conversion of the compound into: (a) Electrophile (b) Free radical (c) Nucleophile (d) Redox-active reactant
An example of toxication is the breakdown of methanol in the mammalian liver. While methanol itself is intoxicating, it is not directly poisonous. However, its metabolites are formic acid and formaldehyde, which can cause severe acidosis, damage to the optic nerve, and other life-threatening complications.
Another example of toxication is the metabolism of paracetamol (acetaminophen) to the hepatotoxic metabolite NAPQI via the cytochrome P450 oxidase system.
While toxication is generally undesirable, in certain cases it is required for the in vivo conversion of a prodrug or chemical to a metabolite with desired pharmacological or toxicological activity. Codeine is an example of a prodrug, which is metabolized in the body to the opioid known as morphine.
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