Pharmacokinetics Flashcards
First order kinetics
Rate of abs or elimination is directly proportional to concentration
t1/2=.693/k
k and t1/2 DO NOT change with increased dosage
But, bc concentration declines, rate decreases as well
Zero order kinetics
rate is independent of dose
occurs in situations where the mechanism of elimination is saturated (i.e. enzyme), therefore elimination occurs at a constant rate
Examples: ETOH, ASA at high doses
Mass-law kinetics
a mixed order system
at low doses= first order kinetics
high doses=saturation of enzymes= zero-order
Volume of distribution
apparent volume of fluid in which drug is distributed
=loading dose/plasma concentration
Increased Vd= slower rate of elimination (drug is more spread out)
Vd>41 could indicated that much of the drug is sequestered in fat
total body clearance
volume of fluid from which drug is totally removed per unit time
describes efficiency of elimination pathways (metabolism and excretion)
Cl= Vd x Ke
peak concentration
proportional to dose (double dose = double peak)
duration of concentration in a single dose
only increases as function of half-life
duration increases by a single half-life as dose is doubled
Plateau Principle
Input= Constant rate (zero order)- i.e. give multiple doses
Output= exponential (first order)
Rate to plateau determined by Ke
Plateau reached by 5 elimination half-times
concentration at plateau is doubled when dose is doubled (still takes 5 half-times to get there)
bioavailability
(f)= fraction of the dose that is absorbed and reaches systemic circulation (i.e. w/o being destroyed in gut or liver)
= AUC oral/AUC IV