Non Linear PK

Question 1

what is saturation

Answer 1

when all protein binding sites are occupied

Question 2

when is non linear PK observed

Answer 2

when saturation occurs at therapeutic levels (not above them)

Question 3

absorption

Answer 3

when uptake transporters are saturated, bioavailability decreases at higher concentrations
when efflux transporters are saturated, more drug is absorbed so bioavailability increases at higher doses

Question 4

distribution

Answer 4

higher free fraction when plasma proteins are saturated at higher doses
when uptake transporters are saturated, there are lower tissue concentrations
when efflux transporters are saturated, there is higher tissue concentrations at higher doses

Question 5

metabolism

Answer 5

when hepatic enzymes are saturated, there is lower clearance at higher doses

Question 6

excretion

Answer 6

uptake transporters are saturated, lower clearance at higher doses
efflux transporters are saturated, lower clearance at higher doses

Question 7

non linear renal excretion

Answer 7

neither glomerular filtrtion rate nor passive re-absorption are saturable
active secretion and reabsorption are saturable