lecture 3 stuff Flashcards
what are the 3 excretion steps (renal)
glomerular filtration
tubular reabsorption
tubular secretion
what enzyme are most drugs metabolized by
CYP 3A4/5
what is the importance of induction
allows enzyme to change in response to foreign substance
what are the effects of induction
increased clearance
decreased half life
decreased response
what factors other than drugs can cause induction
environment
smoking increases metabolism
herbal and nutritional supplements
what does a drug that is an enzyme inducer do
drug increases amount of enzyme for metabolism
what does a drug that is and enzyme inhibitor do
drug blocks metabolism of another drug
what are the effects of an enzyme inhibitor
increased response
increase half life
immediate effects
what does aspirin and warfarin cause
hemmorage
what does erythromycin and seldane cause
fatal arythmia
what does 2 CNS depressants cause
respiratory depression
what does viagra and nitro cause
hypotension
what does ACE inhibitors and potassium sparing diuretics cause
hyperkalemia
if a drug is an inhibitor what are the PK effects
decreased clearance
increased half life
if a drug is an inhibitor what are the PD effects
increased response
increased duration
in what ways does the CYP gene family vary
expression level
enzyme activity
enzyme induction
what type of metabolizer are most drugs made for
extensive metabolizer
what are poor metabolizers more prone to
increased risk of toxicity
what are people who are ultraextensive metabolizers more prone to
reduced response
how many CYP2D6 alleles are there? how many copies can it have
43 alleles
1-5, or 13 copies
how does the copies of CYP2D6 alleles affect metabolism
more copies = more metabolism
what would happen if you had 0 copies of the CYP2D6 allelle?
1-3?
13
0 - no metabolism may be toxic
1-3 adequate response
13 rapid metabolism overdose?
what do you do to a drug dose if someone has impaired organ that functions in metabolism or excretion
adjust dose
what are 3 outcomes of drug metabolism
inactivity
toxicity
water solubility