Chapter 5 - Distribution Flashcards
true or false
if a drug is highly protein bound, the half life will be short
false - prolonged
if a drug is highly protein bound, is this linear or nonlinear pharmacokinetics
nonlinear
as free drug is excreted and leaves circulation, what happens to protein bound drug?
the bound drug will release from its protein and go into circulation to maintain equilibrium
true or false
a drug can bind to proteins not only in the plasma, but in the tissue as well
true
but more focused on plasma proteins
true or false
both free and bound drug can be distributed and eliminated
false - only free drug
are we able to measure the amount of FREE DRUG in a patient
no – just the total amount
measuring just free drug is too much $$
how much plasma is in an average 70kg male
3L
3 areas that drug can be distributed
plasma
other body areas (adipose tissue, protein, bone, etc)
plasma proteins
name 3 plasma proteins
albumin, alpha glycoprotein, lipoprotein
ACIDIC DRUGS principally bind to what plasma protein
albumin
BASIC DRUGS primarily bind to what plasma protein
all 3 - albumin, lipoprotein, and alpha glycoprotein
minimum VD in an average person
3L
true or false
in a normal person, the concentration of plasma proteins usually fluctuates
FALSE - usually constant
if a patient has a certain disease state - changes
what will happen if a patient has NO plasma proteins
the entire dose will be free
true or false
high plasma protein binding = linear kinetics
FALSE - nonlinear
*just an important note
ONLY FREE DRUG CAN HAVE THERAPEUTIC EFFECT!!!!!
What is a disadvantage of drug being distributed to other tissues (aside from the target tissue)
side effects
formula to determine the fraction of free drug (a)
a = Cfree/C bound + Cfree
as alpha decreases, what happens
the amount of free drug increases significantly - need to reduce dose
true or false
if the alpha value decreases, we need to increase the dose of the drug
FALSE
there will be more free drug, so need to decrease the dose
after the drug molecules have entered the bloodstream, the pattern of DISTRIBUTION is determined by what
PERFUSION to each tissue
4 factors that affect drug distribution
-rate of flow of blood
-partition characteristics of the drug between plasma and tissue
-partition coefficient of drug into various tissues
-volume or mass of the tissue
if Vd is low, where will the drug remain
drug remains in the plasma and keeps circulating
rate of renal plasma flow
this is also known as the rate of…
590-695mL/min
rate of filtration