Toxication

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Toxication

Toxication is the process of metabolism

Metabolism

Metabolism is the set of chemical reactions that occur in living organisms in order to maintain life. These processes allow organisms to grow and reproduce, maintain their structures, and respond to their environments....
in which the metabolite of a compound is more toxic than the parent drug

Medication

A pharmaceutical drug, also referred to as medicine or medicament, can be loosely defined as any substance intended for use in the diagnosis, cure, mitigation, treatment, or prevention of disease....
or chemical.

Toxication may involve:

While toxication is generally undesirable, in certain cases it is required for the in vivo
In vivo

In vivo 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 or a in vitro....
conversion of a prodrug

Prodrug

A prodrug is a Pharmacology substance that is administered in an inactive form. Once administered, the prodrug is drug metabolism in vivo into an active metabolite....
or chemical to a metabolite with desired pharmacological or toxicological activity. Codeine

Codeine

Codeine or methylmorphine is an opiate used for its analgesic, Cough medicine and Antidiarrhoeal properties. It is by far the most widely used opiate in the world and probably the most commonly used drug overall according to numerous reports over the years by organizations such as the World Health Organization and its League of Nations...
is an example of a prodrug, which is metabolized in the body to the opioid

Opioid

An opioid is a chemical substance that has a morphine-like action in the body. The main use is for analgesia. These agents work by binding to opioid receptors, which are found principally in the central nervous system and the gastrointestinal tract....
known as morphine

Morphine

Morphine is a highly potent opiate analgesic Medication, is the principal active agent in opium, and is considered to be the prototypical opioid....
.

Examples
The breakdown of methanol

Methanol

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Encyclopedia

Toxication is the process of metabolism

Metabolism

Medication

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

While toxication is generally undesirable, in certain cases it is required for the in vivo
In vivo

In vivo 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 or a in vitro....
conversion of a prodrug

Prodrug

Codeine

Opioid

Morphine

Morphine is a highly potent opiate analgesic Medication, is the principal active agent in opium, and is considered to be the prototypical opioid....
.

Examples

The breakdown of methanol

Methanol

Methanol, also known as methyl alcohol, carbinol, wood alcohol, wood naphtha or wood spirits, is a chemical compound with chemical formula carbonhydrogen3oxygenhydrogen ....
in the mammalian liver. Methanol in itself is toxic due to its CNS depressant properties, but acquires more dangerous toxicity through its metabolites formic acid

Formic acid

Formic acid is the simplest carboxylic acid. Its formula is hydrogencarbonoxygenOH or CH2O2. It is an important intermediate in chemical synthesis and occurs naturally, most notably in the venom of bee and ant stingers....
and formaldehyde

Formaldehyde

Formaldehyde is a chemical compound with the chemical formula H2CO. It is the simplest aldehyde. Formaldehyde exists in several forms aside from H2CO: the cyclic trimer trioxane and the polymer Polyoxymethylene....
, which can cause severe acidosis

Acidosis

Acidosis is an increased acidity . If not further qualified, it usually refers to acidity of the blood plasma.Acidosis is said to occur when arterial pH falls below 7.35, while its counterpart occurs at a pH over 7.45....
, damage to the optic nerve

Optic nerve

The optic nerve, also called cranial nerve II, transmits visual information from the retina to the brain....
, and other life-threatening complications.

The metabolism of paracetamol

Paracetamol

Paracetamol or acetaminophen is a widely used over-the-counter drug analgesic and antipyretic . It is commonly used for the relief of fever, headaches, and other minor aches and pains, and is a major ingredient in numerous common cold and Influenza remedies....
(acetaminophen) to the hepatotoxic

Hepatotoxicity

Hepatotoxicity implies chemical-driven liver damage. The liver plays a central role in transforming and clearing chemicals and is susceptible to the toxicity from these agents....
metabolite NAPQI

NAPQI

NAPQI is an acronym for the chemical N-acetyl-p-benzo-quinone imine. It is a toxic byproduct produced during the xenobiotic metabolism of the analgesic paracetamol ....
via the cytochrome P450 oxidase

Cytochrome P450 oxidase

Cytochrome P450 is a very large and diverse superfamily of hemoproteins found in all domains of life. Cytochromes P450 use a plethora of both exogenous and endogenous compounds as substrates in enzymatic reactions....
system.

Metabolic Activation of N-Hydroxy-2-aminofluorene and N-Hydroxy-2-acetylaminofluorene by Monomorphic N-Acetyltransferase (NAT1) and Polymorphic N-Acetyltransferase (NAT2)

Role of cytochrome P4501B1 in benzo[a]pyrene bio-activation to DNA-binding metabolites Evidence from 32p-postlabeling for formation of 3-hydroxybenzo[a]pyrene and benzo[a]pyrene-3,6-quinone as major proximate genotoxic intermediates