Lecture 1.5: Uptake and Distribution

Question 1

What form of drug will have an effect on the brain?

Answer 1

non ionized, lipophilic

Question 2

What form of drug will be excreted by kidneys?

Answer 2

ionized

Question 3

What is happening in the liver?

Answer 3

non ionized to ionized, lipophilic to hydrophilic

Question 4

Degree of ionization depends on:

Answer 4

dissociation constant and pt’s pH

Question 5

Give acidic drug to acidic pt:

Answer 5

give lower dose

Question 6

Give basic drug to acidic pt:

Answer 6

give higher dose

Question 7

Ion trapping example

Answer 7

give basic drug to alkalemic mother - nonionized drug passes to fetus
fetus pH is acidic - ionizes drug, can’t pass back to mother

Question 8

Difference in pH of mother/fetus

Answer 8

fetus more acidic than mother

Question 9

Protein binding trends

Answer 9

acids bind to albumin (main one)

bases bind to alpha 1 glycoproteins

Question 10

Drugs that are highly protein bound:

Answer 10

warfarin, propranolol, phenytoin, diazepam

Question 11

What is clearance

Answer 11

the volume of plasma cleared by metabolism and excretion

Question 12

What is first order kinetics

Answer 12

drug cleared at rate proportional to amount in plasma

Question 13

What is zero order kinetics

Answer 13

drug cleared at constant rate per unit of TIME

Eg: ASA, Dilantin, ETOH

Question 14

Hepatic clearance

Answer 14

if hepatic extraction is > 0.7, depends on hepatic blood flow
(perfusion dependent elimination)

Question 15

If hepatic extraction ration < 0.3

Answer 15

hepatic clearance depends on enzyme activity

capacity dependent elimination

Question 16

Renal clearance

Answer 16

most important organ for eliminating ionized drugs

Question 17

Renal clearance of lipophilic drugs

Answer 17

little to no excretion

Question 18

Metabolism definition

Answer 18

converting lipid soluble to water soluble

usually become inactive (midazolam is example of exception)

Question 19

Phase I metabolism

Answer 19

oxidation-reduction or hydrolysis

Question 20

Phase II metabolism

Answer 20

parent or metabolite reacts to something in liver to form water soluble conjugate

Question 21

Sites of metabolism

Answer 21

liver, plasma, kidney, lungs, GI tract

Question 22

What is CP-450

Answer 22

enzymes in hepatic smooth endoplasmic reticulum

Question 23

Enzyme induction

Answer 23

drugs can stimulate and increase enzymes

Eg chronic alcohol use

Question 24

Enzyme induction drug example

Answer 24

phenobarbital (other anti seizure meds) will induce liver enzymes, will need to shorten dose intervals for anesthetics

Question 25

Non enzyme metabolism forms and drug examples

Answer 25

conjugation, hydrolysis in liver mostly, do not undergo enzyme induction determined genetically Eg: succhs, esmolol

Question 26

How does pharmacodynamics mainly work?

Answer 26

through Mu receptors, also kappa and delta receptors

Question 27

Concentration of receptors

Answer 27

up-regulation and down-regulation in response to stimuli

Question 28

Concentration of receptor example

Answer 28

stopping beta blocker abruptly - hypertensive crisis due to up-regulated receptors

Question 29

State of receptor activation theory

Answer 29

non-activated receptors that are converted to active by the drug

Question 30

Receptor occupancy theory

Answer 30

More receptors occupied by drug, more effective the drug

Question 31

Non-receptor drug action example

Answer 31

antacids

Question 32

Most antagonist drugs are what kind?

Answer 32

competitive antagonists (Narcan)

Question 33

What kind of mixture do our drugs tend to come in?

Answer 33

racemic mixture

Question 34

What is Efficacy?

Answer 34

Ability of drug to produce desired effect

Question 35

What is Potency?

Answer 35

Relationship between therapeutic effect and dose necessary to achieve effect Lower dose, higher effect, higher potency

Question 36

Therapeutic index equation

Answer 36

LD50 / ED50

Question 37

Hyper-reactive effect

Answer 37

unusually low dose produces effect

Question 38

Hyper-sensitivity effect

Answer 38

Allergy

Question 39

Additive effect and example

Answer 39

1+1=2 | Eg: Fentanyl and Propofol

Question 40

Synergetic effect and example

Answer 40

1+1=3 | Eg: Fentanyl and Midazolam