Flashcards in Pharmacogenics Deck (57)
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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
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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
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pharamcogenetics is the study or
clinical testing of genetic variation that gives rise to differing response to drugs
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codeine metabolism
require CYP2D6 gene to activate.
More copies makes you metabolize more
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normally metabolize ____% of codeine to morphine
10%
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once a drug is taken, the drug must:
1. reach its target
2. exert its effect
3. do the above before being inactivated/eliminated
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pharmacokinestics
describes absorption, distribution, metabolism and excretion of drugs (commonly referred to as ADME)
cytochrom p450, glyconyltransferase, thiopureine methyltransferase
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pharmacodynamics
describes the relationship between the concentration of a drug at its site of action and observed biological effects
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most major drugs are only effective in ___% of patients
25-60
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the CYP450 complex is
1. the gene products active in liver and intestinal epithelium
2. 3 main families: (CYP1, CYP2, CYP3)
3. CYP3A4
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the CYP1, CYP2, CYP3 have 6 main genes:
and phase I for ___% of common drugs
CYP1A1, CYP1A2, CYP2C9, CYP2C19, CYP2D6, CYP3A4
90%
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what gene accounts for 40% of all common drugs
CYP3A4
There is less genetic variation on CYP3A4 than other CYPs
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Most CYP's function to _____ drugs
inactivate.
But rarely they are needed to activate
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example of gene needed to activate a drug
CYP2D6
which converts codeine to morphine
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gene: CYP3A:
1. cyclosporine
2. ketoconanazole
2. rifampin
4. grapefruit juice
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CYP2D6 gene
codeine, this is needed to activate
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CYP2c9 + VKORC1
warfarin
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NAT
isoniazid
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TPMT
6-mercaptopurine/6-thiguanine and childhood
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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
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Pharmacokinestics is broken down farther into
two basic ways that drugs are metabolized through biotransformers
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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
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Frameshift -->
alter reading frame --> NO ACTIVITY
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splicing-->
skip exons and/or alter reading frame--> no activity
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missense -->
alter protein function--> usually REDUCED ACTIVITY
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