GEN #30 & 31 Phase I Drug Metabolism

Pharmacogenomics allows for the individualization of drug treatment by assessing the potential that a drug agent will be efficacious due to ______ considerations and prevent toxicities due to _____ considerations

Biotransformation via the_______ represents one of the most common elimination mechanisms

15-30% of the most commonly used drugs are metabolized by the _______ isoform alone

Tamoxifen is metabolized by 9 CYP isoforms, as well as the ______________

_____________ reduces excess superoxide anion

Oxygen binds to CYP via a __________________________

________________ compares evolution of different families across species

What organ contains the most diverse array of CYP450 proteins

The CYP4B1 isoform is located in which tissue

In what tissue is the CYP4F8 isoform located

CYP11A, 11B1, 11B2 isoforms are found in the

The CYP24 isoform is located where

Which CYP isoform preferentially binds polar heterocyclic compounds and aryl amines

The majority of the CYPs expressed on the intestines & liver belong to which sub-family

Gene sequence changes shown in CYP450 genes that impact enzymatic activity

The phenotype that has no function alleles present

The phenotype that has either one funtionsl and one mutant/deficient allele or two partially active/deficient alleles present

The phenotype that has either 2 active alleles or a combination of one active and one partially active allele present

The phenotype that has 3 or more active alleles present

Which phenotypic metabolizer should be able to achieve therapeutic effects at normal dosing?
(I know this is poorly worded)

What non-CYP450 super family of phase I enzymes are expressed in the liver, intestines, and ER membranes

What is an alternative to genotyping CYP450 alleles

The assays for phenotyping are based on the ________ of substrate drugs that have been labeled with a stable or radioactive carbon

What substrate is used for a CYP3A4 breath test

What substrate is used for a CYP1A2 breath test

What substrate is used for a CYP2C19 breath test

erythromycin will undergo ____________ by CYP3A4

CYP1A2 is aslo known as

CYP2D6 aka

CYP2C19 aka

Smoking has what effect on CYP1A2

theophylline, clozapine, & olanzapine are metabolized by which CYP

clopidogrel, proton pump inhibitors, and phenytoin are metabolized by which CYP

phenytoin, warfarin, and sulfonylureas are metabolized by which CYP

bupropion, cyclophosphamide, methadone, & nevirapine are metabolized by which CYP

What is the most frequent allele of the CYP2B6 isoform

Mutant alleles generally have _________ catalytic activity of the expressed protein

Preferential substrates of CYP2C9 are _______ compounds having 1 or more ____________

Patients with the poor metabolizer alleles will show a 5X greater instance of _________ upon starting an oral sulfonylurea antihyperglycemic agent.

Ultra-rapid metabolizers will have _____________ levels of the oral sulfonylurea antihyperglycemic agents

The FDA recommends _____ & _____ genotyping for warfarin

CYP2C19 is also know as

Beta blockers are deactivated by CYP2D6 therefore which phenotype would result in a higher risk for therapeutic failure

Poor metaboliazer alleles for CYP2C19 are