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Information about Toxication

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:
  • Changing the physicochemical properties to cause a change in the microenvironment
  • Increasing the potency of a compound
  • Conversion of the compound into:
    • Electrophile
    • Free radical
    • Nucleophile
    • 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.
Drug metabolism is the metabolism of drugs, their biochemical modification or degradation, usually through specialized enzymatic systems. Drug metabolism often converts lipophilic chemical compounds into more readily excreted polar products.
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A medication, medicine or drug is any substance or combination of substances administered to human beings or animals to treat or prevent disease; alternatively to assist in medical diagnosis.
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Methanol, also known as methyl alcohol, carbinol, wood alcohol, wood naptha or wood spirits, is a chemical compound with chemical formula CH3OH.
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Formic acid (systematically called methanoic acid) is the simplest carboxylic acid. Its formula is HCOOH or CH2O2. It is an important intermediate in chemical synthesis and occurs naturally, most famously in the venom of bee and ant stings.
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Formaldehyde (methanal) is the chemical compound with the formula H2CO. The simplest aldehyde, it was first synthesized by the Russian chemist Aleksandr Butlerov but was conclusively identified by August Wilhelm von Hofmann.
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MeSH D000138
For acidosis referring to acidity of the urine, see renal tubular acidosis.
Acidosis is an increased acidity (i.e. an increased hydrogen ion concentration). If not further qualified, it refers to acidity of the blood plasma.
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Optic Nerve may be a reference to:
  • Optic nerve, the anatomical structure;
  • Optic Nerve (comic), the comic book series;
  • Optic Nerve (1998), the seminal release from the Irish hip hop act known as Exile Eye; or

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Paracetamol (INN) (IPA: /ˌpærəˈsiːtəmɒl, -ˈsɛtə-/) or acetaminophen (USAN), is the active metabolite of phenacetin, a so-called coal tar analgesic.
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<noinclude> </noinclude> Hepatotoxicity (from hepatic toxicity) implies chemical-driven liver damage. Liver plays central role in transformation and clearance of most chemicals and is susceptible to the toxicity from these agents.
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NAPQI is an acronym for the chemical N-acetyl-p-benzo-quinone imine. It is a toxic byproduct produced during the metabolism of paracetamol (also called acetaminophen). It is normally produced only in small amounts, and then almost immediately detoxified in the liver.
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Cytochrome P450 (abbreviated CYP, P450, infrequently CYP450) is a very large and diverse superfamily of hemoproteins found in bacteria, archaea and eukaryotes.[1] They are so named because of their properties i.e.
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In vivo (Latin: (with)in the living) means that which takes place inside an organism. In science, in vivo refers to experimentation done in or on the living tissue of a whole, living organism as opposed to a partial or dead one.
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A prodrug is a pharmacological substance (drug) which is administered in an inactive (or significantly less active) form. Once administered, the prodrug is metabolised in vivo into the active compound.
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This article is about the drug. For the band, see Codeine (band).
Codeine (INN) or methylmorphine is an opiate used for its analgesic, antitussive and antidiarrheal properties.
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An opioid is a chemical substance that has a morphine-like action in the body. The main use is for pain relief. These agents work by binding to opioid receptors, which are found principally in the central nervous system and the gastrointestinal tract.
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Morphine (INN) (IPA: [ˈmɔ(ɹ)fin]) is a highly potent opiate analgesic drug and is the principal active agent in opium and the prototypical opioid. Like other opiates, e.g.
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