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Pharmacokinetics
By Dr. Hadley
15
Medical
Professional
04/24/2013

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Term
Drug transport types
Definition
1. passive diffusion: diffuses across membranes like gases and lipophiles
2. active transport: transport against concentration gradient with ATP (acid base excretion renal)
3. facilitated diffusion - only via concentration gradient (adenosine)
4. receptor mediated endocytosis: peptide hormones
Term
capillary fenestrations
Definition
mvmnt for water soluble drugs
-applies to fetus
-bbb stops water soluble drug entry (tight junctions)
Term
acid trap vs basic trap
Definition
acidification traps charged form weak bases!

alkalinization traps charged form weak acid
Term
active drug transporters
Definition
MDR expressed everywhere (organic cation)
Term
first pass effect
Definition
Much of the drug is absorbed and metabolized within stomach/liver before entering systemic circ.
Term
bioavailability
Definition
AUC oral/ AUC IV bolus
Term
drugs bound to serum proteins
Definition
1.albumin = warfarin
2. glycoprotein = lidocian
3. lipoproteins - propofol
Term
Vd
Definition
Volume distribution...larger means undergoes tissue binding
Term
zero order vs first order
Definition
zero = constant rate (sat receptor)
1st = proportional to concentation
(most drugs)
Term
phase one vs phase 2
Definition
phase 1 = oxidation by p450s
phase 2 = conjugation

t1/2 = .693/ke
Term
clearance
Definition
additive, used as measure of loss of particular concentration of fluid

C=ke * vd
Term
two compartment dist phase
Definition
I-injection co
II - entry tissues co
III - slow elimniztion
IV

distribution phase ends when periphral and circ enter equillibrium (III)
Term
when to use large dosing fraction and why
Definition
less frequent dosing...large theraputic window only

smaller f keeps concentration in smaller window but needs admin more often
Term
nonlinear dose dependant drugs
Definition
peak concentration changes non-proportionately to dose

occurs saturated kinetic process

may not reach steady state at higher doses
Term
partition coefficient
Definition
= drug plasma/drug alveolus

decreasing solubility = decreasing coefficient = equilibruim faster
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