CYP450 Paper INTRO INFO
Endanur INFO ONTRO
Today, the P450 field has made tremendous contributions in numerous areas. The understanding of P450s has revolutionized aspects of drug development and agriculture. We now understand genetic diseases in endocrinology, and P450 played a leading role in fields as diverse as pharmacogenetics, chemical carcinogenesis, molecular epidemiology, bioremediation, plant breeding, and insect control.
---Recognizing whether the drugs involved act as enzyme substrates, inducers, or inhibitors can prevent clinically significant interactions from occurring. Avoiding coadministration or anticipating potential problems and adjusting a patient's drug regimen early in the course of therapy can provide optimal response with minimal adverse effects.
Drug metabolism via the cytochrome P450 system has emerged as an important determinant in the occurrence of several drug-drug interactions. A greater degree of interaction predictability has been achieved through the identification of P450 isozymes and some of the drugs that share them. Six different P450 isozymes—CYP1A2, CYP2C19, CYP2C9, CYP2D6, CYP2E1, and CYP3A4—that play important roles in drug metabolism have been identified (1, 2). Of these 6 isozymes, shared metabolism by the CYP3A4 isozyme has resulted in several clinically significant drug-drug interactions. More information about the effects of certain drugs on enzyme-mediated biotransformation has led to identification of enzyme inducers and inhibitors, providing even greater insight into the nature of the interactions.
Cytochrome P450 represents a family of isozymes responsible for biotransformation of many drugs via oxidation. The enzymes are heme-containing membrane proteins, which are located in the smooth endoplasmic reticulum of several tissues. Although a majority of the isozymes are located in the liver, extrahepatic metabolism also occurs in the kidneys, skin, gastrointestinal tract, and lungs. Significant inactivation of some orally administered
Today, the P450 field has made tremendous contributions in numerous areas. The understanding of P450s has revolutionized aspects of drug development and agriculture. We now understand genetic diseases in endocrinology, and P450 played a leading role in fields as diverse as pharmacogenetics, chemical carcinogenesis, molecular epidemiology, bioremediation, plant breeding, and insect control.
---Recognizing whether the drugs involved act as enzyme substrates, inducers, or inhibitors can prevent clinically significant interactions from occurring. Avoiding coadministration or anticipating potential problems and adjusting a patient's drug regimen early in the course of therapy can provide optimal response with minimal adverse effects.
Drug metabolism via the cytochrome P450 system has emerged as an important determinant in the occurrence of several drug-drug interactions. A greater degree of interaction predictability has been achieved through the identification of P450 isozymes and some of the drugs that share them. Six different P450 isozymes—CYP1A2, CYP2C19, CYP2C9, CYP2D6, CYP2E1, and CYP3A4—that play important roles in drug metabolism have been identified (1, 2). Of these 6 isozymes, shared metabolism by the CYP3A4 isozyme has resulted in several clinically significant drug-drug interactions. More information about the effects of certain drugs on enzyme-mediated biotransformation has led to identification of enzyme inducers and inhibitors, providing even greater insight into the nature of the interactions.
Cytochrome P450 represents a family of isozymes responsible for biotransformation of many drugs via oxidation. The enzymes are heme-containing membrane proteins, which are located in the smooth endoplasmic reticulum of several tissues. Although a majority of the isozymes are located in the liver, extrahepatic metabolism also occurs in the kidneys, skin, gastrointestinal tract, and lungs. Significant inactivation of some orally administered