ADME and Pharmacokinetics

Question 1

what is pharmacokinetics

Answer 1

how the body handles drugs- the process the drug is subject to once in the body

Question 2

what is pharmacodynamics

Answer 2

what the drug does to the body

Question 3

what processes are absorption

Answer 3

all processes from the site of administration to the site of measurement

Question 4

what is bioavailability relating to absorption

Answer 4

measure of the extent of absorption of unchanged administered compound

Question 5

what is distribution

Answer 5

reversible transfer of substance between site of measurement and other sites within the body

Question 6

distribution is _______ transfer

Answer 6

reversible

Question 7

define metabolism

Answer 7

irreversible loss of unchanged substance by chemical conversion- physiochemical properties of the drug are altered

Question 8

what can elimination and excretion be clumped together as?

Answer 8

disposition

Question 9

PK behaviour is a function of what 4 things?

Answer 9

Physicochemical and structural properties of drug
Dosage form
Route of drug administration
Physiology of the body

Question 10

poor PK properties may limit what? can lead to?

Answer 10

clinical application- ending in drug termination

Question 11

factors of a person that can influence the drugs PK

Answer 11

genetics, size, age, disease, co-administration of other drugs, environmental factors (smoking)

Question 12

3 types of PK models for the ADME process?

Answer 12

1. single equation: integrated or differential
2. kinetic compartmental models
3. physiologically based PK models

Question 13

explain what single equation PK model is?

Answer 13

integrated or differential

shows decline of drug concentration time

Question 14

which of the single equation PK models do we look at?

Answer 14

INTERGRATED

Question 15

integrated equation?

Answer 15

C= C0e^-kt

Question 16

what is the kinetic compartmental method used for?

Answer 16

to describe the data

number of compartments defined by the data

Question 17

what type of data is kinetic compartmental models used for?

Answer 17

for fitting of sparse clinical data- population PK modelling

Question 18

when are physiologically based PK models used?

Answer 18

at the end- give much more detail

Question 19

what is physiologically based PK models used for?

Answer 19

predicting in vivo pharmacokinetics from in vitro data

Question 20

off target effects of drugs are associated with?

Answer 20

minor toxicity or if too high then serious toxicity

Question 21

can you modify the PK properties of molecules?

Answer 21

yes

Question 22

what is the difference between physiologically based (PBPK) model and compartmental model?

Answer 22

has a mechanistic nature- equations can show exactly what happened

Question 23

drug independent physiological parameters?

PBPK model

Answer 23

tissue volumes and blood flow
tissue composition
intestinal pH and transit time
enzyme and transporter abundance

Question 24

population and external factors to consider with PBPK model?

Answer 24

age 
gender
race 
disease status 
genetics 
smoking and diet

Question 25

drug dependent factors for PBPK model

Answer 25

LogP, pKa, B/P, molecular weight 
permeability 
solubility 
particle size 
CLmax

Question 26

what can PBPK models allow simulations of?

Answer 26

drug plasma and tissue concentration time profiles after iv and oral administration