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Flashcards in Pharmacogenics Deck (57)
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1

Pharmacogenetics

the study of differences in drug response due to allelic variation in genes affecting drug metabolism, efficacy, and toxicity
variable response to individual gene

2

Pharamacogenomics

the genomic approach to the pharmacogenetics, is concerned with the assessment of common genetic variants in the aggregate for their impact on the outcome of drug therapy.
Variable response due to multiple loci across the genome

3

pharamcogenetics is the study or

clinical testing of genetic variation that gives rise to differing response to drugs

4

codeine metabolism

require CYP2D6 gene to activate.
More copies makes you metabolize more

5

normally metabolize ____% of codeine to morphine

10%

6

once a drug is taken, the drug must:

1. reach its target
2. exert its effect
3. do the above before being inactivated/eliminated

7

pharmacokinestics

describes absorption, distribution, metabolism and excretion of drugs (commonly referred to as ADME)
cytochrom p450, glyconyltransferase, thiopureine methyltransferase

8

pharmacodynamics

describes the relationship between the concentration of a drug at its site of action and observed biological effects

9

most major drugs are only effective in ___% of patients

25-60

10

the CYP450 complex is

1. the gene products active in liver and intestinal epithelium
2. 3 main families: (CYP1, CYP2, CYP3)
3. CYP3A4

11

the CYP1, CYP2, CYP3 have 6 main genes:
and phase I for ___% of common drugs

CYP1A1, CYP1A2, CYP2C9, CYP2C19, CYP2D6, CYP3A4

90%

12

what gene accounts for 40% of all common drugs

CYP3A4

There is less genetic variation on CYP3A4 than other CYPs

13

Most CYP's function to _____ drugs

inactivate.

But rarely they are needed to activate

14

example of gene needed to activate a drug

CYP2D6

which converts codeine to morphine

15

gene: CYP3A:

1. cyclosporine
2. ketoconanazole
2. rifampin
4. grapefruit juice

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CYP2D6 gene

codeine, this is needed to activate

17

CYP2c9 + VKORC1

warfarin

18

NAT

isoniazid

19

TPMT

6-mercaptopurine/6-thiguanine and childhood

20

G6PD

hemolytic anemia after sulfa drugs

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Pharmacokinetics:
• Genetic Examples:

Cytochrome P450, glucuronyltransferase, thiopurine methyltransferase

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Pharmacodynamics:
• Genetic Examples:

Glucose-6-phosphate dehydrogenase, vitamin K epoxide complex

23

Pharmacokinestics is broken down farther into

two basic ways that drugs are metabolized through biotransformers

24

pharmacokinestics phases

phase 1
phase 2

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phase 1 metabolism

attach a polar group onto the compound to make it more soluble; usually a hydroxylation step

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phase 2 metabolism

attach a sugar/acetyl group to detoxify the drug and make it easier to excrete

27

Frameshift -->

alter reading frame --> NO ACTIVITY

28

splicing-->

skip exons and/or alter reading frame--> no activity

29

missense -->

alter protein function--> usually REDUCED ACTIVITY

30

copy number alleles -->

increased gene copy alleles --> INCREASED (ULTRAFAST)