What is a CYP3A substrate?
What is a CYP3A substrate?
CYP3A is responsible for the metabolism of more drugs than any other P450 enzyme. Other CYP3A substrates (dextromethorphan N-demethylation, nelfinavir, indinavir) have also been studied during pregnancy. N-demethylation of oral dextromethorphan was increased by 35–38% during pregnancy [27].
What does CYP3A4 substrate mean?
Drugs metabolized by CYP3A4 are called CYP3A4 substrates. Keep in mind that many drugs are metabolized by more than one CYP450 enzyme, and CYP3A4 may represent only one pathway.
What drugs are CYP3A4 substrates?
Cytochrome P450 enzymes metabolize approximately 60% of prescribed drugs, with CYP3A4 responsible for about half of this metabolism; substrates include acetaminophen, codeine, ciclosporin (cyclosporin), diazepam, and erythromycin. The enzyme also metabolizes some steroids and carcinogens.
What are CYP3A inducers?
An antibiotic used to treat several types of mycobacterial infections including Mycobacterium avium complex, leprosy, and in combination with other antibacterials to treat latent or active tuberculosis.
What is the difference between CYP3A4 and CYP3A?
CYP3A5 is 83% homologous to CYP3A4, is expressed at a much lower level than CYP3A4 in the liver, but is the main CYP3A isoform in the kidney. CYP3A7 is the major CYP isoform detected in human embryonic, fetal and newborn liver, but is also detected in adult liver, although at a much lower level than CYP3A4.
What is a P450 substrate?
Definitions. substrates are drugs or other substances (xenobiotics) which are metabolized by cytochrome enzymes including 1. pharmacologically active drugs which require metabolism to inactive form for clearance from the body. metabolically activated drugs (prodrugs) which require conversion to active drug.
What is cyp450 substrate?
What is cyp450 3A4 substrate?
Human cytochrome P450 (CYP) 3A4 is the most abundant hepatic and intestinal phase I enzyme that metabolizes approximately 50% marketed drugs. A number of important drugs have been identified as substrates, inducers and/or inhibitors of CYP3A4.
What are drug substrates?
substrates are drugs or other substances (xenobiotics) which are metabolized by cytochrome enzymes including 1. pharmacologically active drugs which require metabolism to inactive form for clearance from the body.
Is acetaminophen a CYP3A4 inhibitor?
High concentrations of APAP inhibited CYP3A4 activity. At lower concentrations, APAP produced a dose-dependent increase in CYP3A4 activity and content.
What is a cytochrome P450 substrate?
substrates are drugs or other substances (xenobiotics) which are metabolized by cytochrome enzymes including 1. pharmacologically active drugs which require metabolism to inactive form for clearance from the body. metabolically activated drugs (prodrugs) which require conversion to active drug.
What does CYP3A stand for?
Cytochrome P450
Cytochrome P450, family 3, subfamily A, also known as CYP3A, is a human gene locus. A homologous locus is found in mice. The CYP3A locus includes all the known members of the 3A subfamily of the cytochrome P450 superfamily of genes.
