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Genetic polymorphisms can cause a decrease in drug metabolizing enzyme function in the following three ways....
1. decrease enzyme efficiency or activity
2. decrease affinity of enzyme for substrate
3. inactavation of enzymes
Decrease DME function affects the following how
1. CL
2. drug plasma conc
3. half life
1. decreased CL
2. increases conc
3. increases T 1/2
Increasing DME function affects the following how
1. CL
2. drug plasma conc
3. half life
1. increases CL
2. decreases conc
3. decreases T 1/2
Genetic polymorphisms can cause an increase in drug metabolizing enzyme function in the following two ways....
1. increase about of metabolizing enzymes
2. increase in metabolizing enzme function

These changes are usually a result of gene duplications
If yo decrease enzyme activity and your drug is a pro drug what happens?
failure of efficacy
What drugs are substrates of CYP 2DC (6)
Codeine
Tamoxifen
Antidepressants
Antipsychotics
Antiarrhythmics
Beta Blockers
Do CYP 2D6 allel frequencies differ by race?
YES,
CYP2D6*5-->NO enzyme is more common in white population
What are the CYP2D6 metabolism phenotypes
Ultrarapid metabolizer
Extensive "
Intermediate "
Poor "
CYP2D6 ultrarapid metabolizers have
1__________ metabolism
2_________ drug plasma conc
3_____effect on drug response
1. increased metabolism
2. decreased plasma conc
3. decreased drug response
CYP2D6 extensive metabolizers have
1__________ metabolism
2_________ drug plasma conc
3_____effect on drug response
1. expected metabolism
2. expected plasma conc
3. expected drug response
CYP2D6 intermediate metabolizers have
1__________ metabolism
2_________ drug plasma conc
3_____effect on drug response
1. decreased metabolism
2. increased plasma conc
3. increased drug response increased side effects
CYP2D6 poor metabolizers have
1__________ metabolism
2_________ drug plasma conc
3_____effect on drug response
1. decreased metabolism
2. increased plasma conc
3. large increase in drug response and large increase in side effects
Atomoxetine is metabolized by what enzyme?
CYP2D6
What does Atomoxetine treat?
ADHD
What are the the side effects of atomoxetine? Does it have active metabolites?
Few active metabolites
Insomnia, tachycardia, increased BP, irritability, nervousness, nausea
Atomoxetine what is the difference between EM and PM
1. oral CL
2. T 1/2
3. AUC
4 CMAX
PMs have
1. lower CL
2. much longer T1/2 (5 vs 20hr)
3. 10 times higher AUC
4. 5 fold higher CMAX
How do CYP2D6 PMs tollerate adverse effect compared to EMs when taking Atomoxetine (strattera)?
more PMs have to dc therapy because of adverse affects compared to EMs
What drugs are substrates of CYP 2DC (6)
Codeine
Tamoxifen
Antidepressants
Antipsychotics
Antiarrhythmics
Beta Blockers
Do CYP 2D6 allel frequencies differ by race?
YES,
CYP2D6*5-->NO enzyme is more common in white population
What warning does the FDA give to nursing mothers about the use of codeine?
Infants may be at increased risk of morphine OD if their mothers are taking codeine and are ultra rapid metabolizers?

Known UM should not take codeine. If they do they should watch their innfants for excessive drowsiness, difficulty breathing, and poor feeding.
How is codeine metabolized
small but most active metabilite is morphine (CYP2D6)

also norcodeine (3A4) and codiene glucuronide (UGT2B7)
What are the effects if UR takes codeine?
greater analgesic effect and increased risk of adverse events
What are the effects if PM takes codeine?
decreased analgesic effect/lack of efficacy
Tamoxifen is metabolized by what enzyme?
CYP2D6
What does Tamoxifen treat?
Selective Estrogen Receptor that is used to treat/prevent breast cancer
What are the metabolites of tamoxifen?
N desmethyl tamoxifen

4 hydroxy tamoxifen

endoxifen(this is the secondary metabolite that has the greatest affinity for the receptor)
What metabolite of tamoxifen that has the greatest efficacy (affinity for receptor)?
endoxifen
What makes someone an ER of tamoxifen? How does having this phenotype chang drug concentrations?
*1/*1 (EM)
conc of 80 (highest conc)
What makes someone an IM of tamoxifen? How does having this phenotype chang drug concentrations?
*1 plus 1 variant allele (IM)
conc of 40(conc cut in half)
What makes someone a PM of tamoxifen? How does having this phenotype chang drug concentrations?
2 variant alleles (PM)
conc of 20 (nc cut in fourth)
A breast cancer patient being treated with tamoxifen is most likely to have a relapse if they are what kind of metabolizer?
PMs