Pharmacogenics Flashcards
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
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
pharamcogenetics is the study or
clinical testing of genetic variation that gives rise to differing response to drugs
codeine metabolism
require CYP2D6 gene to activate.
More copies makes you metabolize more
normally metabolize ____% of codeine to morphine
10%
once a drug is taken, the drug must:
- reach its target
- exert its effect
- do the above before being inactivated/eliminated
pharmacokinestics
describes absorption, distribution, metabolism and excretion of drugs (commonly referred to as ADME)
cytochrom p450, glyconyltransferase, thiopureine methyltransferase
pharmacodynamics
describes the relationship between the concentration of a drug at its site of action and observed biological effects
most major drugs are only effective in ___% of patients
25-60
the CYP450 complex is
- the gene products active in liver and intestinal epithelium
- 3 main families: (CYP1, CYP2, CYP3)
- CYP3A4
the CYP1, CYP2, CYP3 have 6 main genes:
and phase I for ___% of common drugs
CYP1A1, CYP1A2, CYP2C9, CYP2C19, CYP2D6, CYP3A4
90%
what gene accounts for 40% of all common drugs
CYP3A4
There is less genetic variation on CYP3A4 than other CYPs
Most CYP’s function to _____ drugs
inactivate.
But rarely they are needed to activate
example of gene needed to activate a drug
CYP2D6
which converts codeine to morphine
gene: CYP3A:
- cyclosporine
- ketoconanazole
- rifampin
- grapefruit juice
CYP2D6 gene
codeine, this is needed to activate
CYP2c9 + VKORC1
warfarin
NAT
isoniazid
TPMT
6-mercaptopurine/6-thiguanine and childhood
G6PD
hemolytic anemia after sulfa drugs
Pharmacokinetics:
• Genetic Examples:
Cytochrome P450, glucuronyltransferase, thiopurine methyltransferase
Pharmacodynamics:
• Genetic Examples:
Glucose-6-phosphate dehydrogenase, vitamin K epoxide complex