Protein Name: | Cytochrome P450 2E1 (P05181) |
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Gene Name: | CYP2E1 |
Description: | |
PDB ID: | 3E4E |
Protein Family: | PF00067, PS00086 |
Protein Category: | Enzyme |
This panel provides drug-protein interaction and their ADRs along with references
Interacting Drugs | Toxicity | Mechanism | Reference |
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Acetaminophen | Hepatotoxicity | Particularly at high doses@ cytochrome P-450 enzymes--especially CYP1A2@ CYP2E1@ and isoforms of CYP3A--convert APAP to a reactive quinone form@ N-acetyl-p-benzoquinone imine (NAPQI)@that covalently binds to cellular macromolecules and also causes production of reactive oxygen species@ and leads to acetaminophen-induced hepatotoxicity [ ADR Type 1 ] | Toxicology Protecting liver from painkiller's lethal dose |
Acetaminophen | Sleepy | Isoniazid inhibits CYP2E1 activity@ thus it increases the level of acetaminophen in blood and increases acetaminophen toxicity [ ADR Type 4 ] | Acetaminophen hepatotoxicity: potentiation by isoniazid |
Clomipramine | Hepatitis | Clomipramine increases oxidative and nitrosative stress@ which triggers of reoccurrence of amineptine-induced hepatitis [ ADR Type 4 ] | CYP2E1 genotype and isoniazid-induced hepatotoxicity in patients treated for latent tuberculosis |
Dehydrated Alcohol | Apap Toxicity | APAP toxicity is increased in both humans and rodents by pretreatment with various inducers of CYP gene expression@ including ethanol@ an inducer of CYP2E and CYP3A isoforms (12@ 13)@ and phenobarbital (PB)@ a well-known inducer of CYP2B@ CYP3A@ and other isoforms. [ ADR Type 4 ] | Toxicology Protecting liver from painkiller's lethal dose |
Didanosine | Severe Hepatitis | Acetaminophen enhances impaired mitochondrial oxidative metabolism and alters mitchondrial ATPase activity@which may lead to severe hepatitis. [ ADR Type 4 ] | Toxic interaction of didanosine and acetaminophen leading to severe hepatitis and pancreatitis: a case report and review of the literature |
Didanosine | Severe Pancreatitis | Acetaminophen enhances impaired mitochondrial oxidative metabolism and alters mitchondrial ATPase activity@which may lead to severe pancreatitis [ ADR Type 4 ] | Toxic interaction of didanosine and acetaminophen leading to severe hepatitis and pancreatitis: a case report and review of the literature |
Halothane | Hepatotoxicity | Both P450 2E1 and P450 2A6 participate in human halothane metabolism@ and that P450 2E1 is the predominant catalytic isoform. [ ADR Type 2 ] | Cytochrome P450 2E1 is the principal catalyst of human oxidative halothane metabolism in vitro |
Methoxyflurane | Hepatotoxicity | Sevoflurane is metabolized by P-450 2E1@ so pathophysiologic factors and drug interactions altering P-450 2E1 activity will also influence sevoflurane metabolism (52) The extent of metabolism of sevoflurane@ 2% to 5%@ is less than that of all other volatile anesthetics except isoflurane and desflurane@ which might be associated with idiosyncratic hepatotoxicity [ ADR Type 2 ] | Biotransformation of sevoflurane |
Minocycline | Dangerous Side Effects | Theophylline inhibits CYP2E1 activity@ thus leads to reduction of minocylcine clearance and causes dangerous side effects. [ ADR Type 4 ] | Possible theophylline-minocycline interaction |
Theophylline | Dangerous Side Effects | Erythromycin inhibits CYP2E1 activity@thus increases the level of theophylline in blood and causes dangerous side effects [ ADR Type 4 ] | Acute drug prescribing to children on chronic antiepilepsy therapy and the potential for adverse drug interactions in primary care |
Valproic Acid | Hepatotoxicity | Associated with idiosyncratic hepatotoxicity [ ADR Type 2 ] | Identification and characterization of the glutathione and N-acetylcysteine conjugates of (E)-2-propyl-2,4-pentadienoic acid, a toxic metabolite of valproic acid, in rats and humans |
This panel provides information on drug category