CYP2E1

Cytochrome P450 2E1 (abbreviated CYP2E1, ), a member of the cytochrome P450 mixed-function oxidase system, is involved in the metabolism of xenobiotic

Xenobiotic

A xenobiotic is a chemical which is found in an organism but which is not normally produced or expected to be present in it. It can also cover substances which are present in much higher concentrations than are usual...

s in the body. While it is involved only in the oxidative metabolism of a small range of substrates (mostly small polar molecules), there are many important drug interactions mediated by CYP2E1.


Within one day of birth, the rat hepatic CYP2E1 gene is activated transcriptionally.

Cytochrome P450 2E1 (abbreviated CYP2E1, ), a member of the cytochrome P450 mixed-function oxidase system, is involved in the metabolism of xenobiotic

Xenobiotic

A xenobiotic is a chemical which is found in an organism but which is not normally produced or expected to be present in it. It can also cover substances which are present in much higher concentrations than are usual...

s in the body. While it is involved only in the oxidative metabolism of a small range of substrates (mostly small polar molecules), there are many important drug interactions mediated by CYP2E1.

CYP2E1 Ligands

Selected inducers, inhibitors and substrates of CYP2E1

Substrates	Inhibitors	Inducers
Often mentioned: anaesthetics halothane Halothane Halothane vapour is an inhalational general anaesthetic. Its IUPAC name is 2-bromo-2-chloro-1,1,1-trifluoroethane. It is the only inhalational anaesthetic agent containing a bromine atom; there are several other halogenated anesthesia agents which lack the bromine atom and do contain the fluorine... isoflurane Isoflurane Isoflurane is a halogenated ether used for inhalational anesthesia. Together with enflurane and halothane, it replaced the flammable ethers used in the pioneer days of surgery. Its use in human medicine is now starting to decline, being replaced with sevoflurane, desflurane and the intravenous... enflurane Enflurane Enflurane is a halogenated ether that was commonly used for inhalational anesthesia during the 1970s and 1980s. Developed by Ross Terrell in 1963, it was first used clinically in 1966.... paracetamol Paracetamol Paracetamol or acetaminophen is a widely used over-the-counter 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 cold and flu remedies...  (analgesic Analgesic An analgesic is any member of the diverse group of drugs used to relieve pain . The word analgesic derives from Greek an- and algos... , antipyretic Antipyretic Antipyretics are drugs that reduce body temperature in situations such as fever. However, they will not affect the normal body temperature if one does not have a fever.... ) Other: dapsone Dapsone Dapsone is a pharmacological medication most commonly used in combination with rifampicin and clofazimine as multidrug therapy for the treatment of Mycobacterium leprae infections . It is also used to treat Pneumocystis carinii pneumonia caused by Pneumocystis jiroveci...  (antibiotic Antibiotic In common usage, an antibiotic is a substance or compound that kills or inhibits the growth of bacteria... ) theophylline Theophylline Theophylline, also known as dimethylxanthine, is a methylxanthine drug used in therapy for respiratory diseases such as COPD or asthma under a variety of brand names. Due to its numerous side-effects, these drugs are now rarely administered for clinical use. As a member of the xanthine family, it...  (stimulant Stimulant Stimulants, also sometimes called psychostimulants, are psychoactive drugs which induce temporary improvements in either mental or physical function or both. Examples of these kinds of effects may include enhanced alertness, wakefulness, and locomotion, among others... ) ethanol Ethanol Ethanol, also called ethyl alcohol, pure alcohol, grain alcohol, or drinking alcohol, is a volatile, flammable, colorless liquid. It is a psychoactive drug, best known as the type of alcohol found in alcoholic beverages and in modern thermometers. Ethanol is one of the oldest recreational drugs...  (psychoactive) chlorzoxazone Chlorzoxazone Chlorzoxazone is a centrally acting muscle relaxant used to treat muscle spasm and the resulting pain or discomfort. It acts on the spinal cord by depressing reflexes. It is sold as Muscol or Parafon Forte, a combination of chlorzoxazone and acetaminophen. Possible side effects include...  (muscle relaxant Muscle relaxant A muscle relaxant is a drug which affects skeletal muscle function and decreases the muscle tone. It may be used to alleviate symptoms such as muscle spasms, pain, and hyperreflexia. The term "muscle relaxant" is used to refer to two major therapeutic groups: neuromuscular blockers and spasmolytics... ) toluene Toluene Toluene, also known as methylbenzene, or Toluol, is a clear water-insoluble liquid with the typical smell of paint thinners, reminiscent of the related compound benzene. It is an aromatic hydrocarbon that is widely used as an industrial feedstock and as a solvent...  (solvent Solvent A solvent is a liquid, solid, or gas that dissolves another solid, liquid, or gaseous solute, resulting in a solution.The most common solvent in everyday life is water. Most other commonly-used solvents are organic chemicals. These are called organic solvents... ) - primarily	Strong: diethyldithiocarbamate (in cancer Cancer Cancer is a class of diseases in which a group of cells display uncontrolled growth , invasion , and sometimes metastasis... ) unspecified: cimetidine Cimetidine Cimetidine is a histamine H2-receptor antagonist that inhibits the production of acid in the stomach. It is largely used in the treatment of heartburn and peptic ulcers...  (H2-receptor antagonist H2-receptor antagonist The H2-receptor antagonists are a class of drugs used to block the action of histamine on parietal cells in the stomach, decreasing the production of acid by these cells... ) disulfiram Disulfiram Disulfiram is a drug used to support the treatment of chronic alcoholism by producing an acute sensitivity to alcohol. Trade names for disulfiram in different countries are Antabuse and Antabus manufactured by Odyssey Pharmaceuticals...  (in alcoholism Alcoholism Alcoholism is a term with multiple and sometimes conflicting definitions. In common and historic usage, alcoholism is any condition that results in the continued consumption of alcoholic beverages, despite health problems and negative social consequences... )	acetone Acetone Acetone is the organic compound with the formula OC2. This colorless, mobile, flammable liquid is the simplest example of the ketones. Owing to the fact that acetone is miscible with water it serves as an important solvent in its own right, typically as the solvent of choice for...  (cleaning fluid) ethanol Ethanol Ethanol, also called ethyl alcohol, pure alcohol, grain alcohol, or drinking alcohol, is a volatile, flammable, colorless liquid. It is a psychoactive drug, best known as the type of alcohol found in alcoholic beverages and in modern thermometers. Ethanol is one of the oldest recreational drugs...  (psychoactive) isoniazid Isoniazid Isoniazid is an organic compound that is the first-line antituberculosis medication in prevention and treatment. First discovered in 1912 as an inhibitor of the MAO enzyme, it was first used as an antidepressant, but discontinued due to side effects...  (in tuberculosis Tuberculosis Tuberculosis is a common and often deadly infectious disease caused by mycobacteria... )

Regulation of CYP2E1

Within one day of birth, the rat hepatic CYP2E1 gene is activated transcriptionally. CYP2E1 expression is easily inducible. It seems that there exist two stages of induction, a posttranslational mechanism for increased protein stability at low levels of ethanol, and an additional transcriptional induction at high levels of ethanol

Further reading