quantitative pharmacokinetics Flashcards
characteristics of a Compartment
-NOT a real anatomical region
-group of tissues w similar blood flow / drug affinity
-an open system (bc the drug can be eliminated from it)
-rapid mixing
-uniform distribution of drug within space
within a Compartment, the drug is _____ & _____
-uniformly distributed
-mixed rapidly & homogenously
what do rate constants represent in a Compartment
drug entry / exit from Compartment
what is 1CM
1-compartment model
what is 2CM
2-compartment model
factors of a 1CM
-single well-mixed container
-drug in blood is in rapid equilibrium w drug in extravascular tissues
-rapid mixing
-linear model- first order elimination
factors of a 2CM
-NO instantaneous distribution of drug within body
-has peripheral compartment
central compartment is comprised of _____
the vascular system (highly perfused tissues)
peripheral compartment is comprised of _____
poorly perfused tissues
the drug distributes to the peripheral compartment based on _____
the rate of transfer from the central compartment
what is zero-order kinetics
& example of drug(s)
a constant amount of drug is absorbed / eliminated per unit time
ethanol
what is an example of a zero-order process
a constant rate IV infusion
what is first-order kinetics
& example of drug(s)
a fraction of drug is absorbed / eliminated per unit time
most drugs
what is mixed-order kinetics
at low drug concentrations = first-order (dose-dependent)
at high drug concentrations = zero-order (dose-independent)
zero-order kinetics is dose-_____
independent
first-order kinetics is dose-_____
dependent
2 examples of drugs w mixed-order kinetics
phenytoin
&
salicylic acid (active metabolite of aspirin)
rate of change of amount of drug in the body is independent of _____
the quantity/concentration of drug in the body
why does drug concentration increase during the absorptive phase
bc rate of absorption is greater than rate of distribution / elimination
what happens at Cmax (drug concentration max)
rate of absorption falls
rate of distribution & elimination rises
-> and rate of absorption becomes = rate of elimination
what is peak concentration
the point where rate of absorption = rate of elimination
what is happening at stage 4 on the graph
there is a negative net balance & blood levels decline (bc very little drug is still available at the absorption site)
drug levels that fall into therapeutic window are considered _____
pharmacologically effective
what is true for drugs that fall in upper threshold of therapeutic window
they produce more side effects