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Final Exam 2021
Terms in this set (82)
a transporter protein that moves drugs out of cells
Placenta= maternal blood
Brain= blood, limit access to brain
Polar molecules- no charge
Ions- have charge, cant cross membranes, need to be nonionized (no charge)
pH partitioning/ion trapping
acidic drugs go to alkaline side
basic drugs go to acidic side
acidic drugs ionize in alkaline media (and vise versa)
Biotransformation (drug metabolism)
enzyme alters drug structure usually in liver by P450 system
(CYP 1, CYP 2, CYP 3, etc.)
P450 enzyme inducers
P450 enzyme inhibitors
drugs metabolized by P450.
Inducers- increase liver enzyme activity, increase drug metabolism, less active drugs/cant achieve therapeutive effect.
Inhibitors- inhibit liver, slow metabolism, increased active drugs/toxicity and increased adverse effects
Infant liver not fully developed until?
Decreased drug metabolism.
Elderly ability to metabolize drug?
decreased drug metabolism==> toxicity.
Reduce drug dose to prevent.
First pass effect
Drug is completely inactivated on it's first pass through liver.
(For PO drugs that go through GI tract)
Newborn Kidney Function
not fully developed
Elderly kidney function
organ degeneration, decreased excretion of drugs.
Renal dosing, lower dose.
Minimum effective concentration
Drug Half life calculation
minimum plasma drug lvl for therapeutic range
Toxic- too high plasma lvl
Half life= 4.5-5 have lives for drug to reach steady state
Affinity and intrinsic activity
affinity- strength of attraction
Intrinsic activity- activates receptor when binding
-competitive and noncompetitive
agonist- activates receptors, high affinity and high intrinsic activity
antagonist- prevent receptor activation. high affinity but no intrinsic activity
noncompetitive- irreversible binding, reduce max response.
competitive- reversible, equal affinity, whichever drug there is more of will win and bind more receptors (compete with agonists)
moderate intrinsic activity
both agonist and antagonist effects
continuous exposure to agonist
Desensitized or refractory
(less sensitive to effects)
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