Pharmacokinetics & Pharmacodynamics

Question 1

Apparent volume

Answer 1

Ratio of drug IN BODY: concentration of drug IN BLOOD

Question 2

Plasma protein: Albumin

Answer 2

High capacity with low affinity

Question 3

When is a drug considered protein bound?

Answer 3

90% or more

Question 4

What % of drug is responsible for the action of drug?

Answer 4

10%

Question 5

What is a partition coefficient?

Answer 5

how a substance distributes between 2 immiscible solvents

Question 6

Factors affecting drug distribution

Answer 6

lipid solubility (more = greater distribution)
drug protein binding
disease states
blood perfusion differences

Question 7

What is “F”

Answer 7

bioavailability

F= AUC PO/AUC IV

Question 8

Bioavailability

Answer 8

amount of drug that enters systemic circulation

Question 9

First pass effect

Answer 9

extent of bypassing the liver when delivering a drug

Question 10

high first pass effect

Answer 10

Bypass liver and high concentration able to go to target organ (IV)

Question 11

low first pass effect

Answer 11

Not being able to bypass liver and some of drug is metabolized and removed by liver (PO)

Question 12

First pass clearance

Answer 12

how much of a drug is removed by liver during first passage in the portal blood to systemic circulation

Question 13

high first pass clearance

Answer 13

bypassing portal vein of liver

Question 14

4 factors affecting diffusion rate (FMDM Diff)

Answer 14

formulation, molecule, drug solubility, membrane

Question 15

Rate of absorption

Answer 15

how quickly drug enters systemic circulation

Question 16

extent of absorption

Answer 16

amount of drug entering systemic circulation

Question 17

prodrug

Answer 17

an inactive precursor that is metabolized to active metabolites

Question 18

why are prodrugs used

Answer 18

improve how intended drug is ADME. usually improve solubility or absorption by improving interaction with cells

Question 19

Free drug

Answer 19

easily distributes to other tissues, not bound to protein and can display effect

Question 20

large therapeutic range

Answer 20

more room between max safe concentration and minimum effective concentration (harder to OD) = safer

Question 21

maximum safe concentration

Answer 21

Max amount of drug conc before adverse effects and toxicity

Question 22

minimum effective concentration

Answer 22

minimum concentration needed for therapeutic effect

Question 23

intensity

Answer 23

addresses efficacy

Question 24

therapeutic index

Answer 24

addresses safety

Question 25

one compartment model

Answer 25

rapidly equilibrate

Question 26

two compartment model

Answer 26

slowly equilibrate

Question 27

what compartment model are NMB and local anesthetics

Answer 27

2 compartment model

Question 28

where is central compartment in NMB drug

Answer 28

NMJ

Question 29

where is central compartment in local anesthetic

Answer 29

site of injection

Question 30

what needs to take place for most drugs to be eliminated

Answer 30

hepatic metabolism. drug turns more polar which makes it easier to be eliminated by kidneys

Question 31

2 categories of Hepatic reactions

Answer 31

phase 1 (non-synthetic preparatory) and phase 2 (synthetic)

Question 32

phase 1 hepatic reaction (OxSulfRedHydro) OSRH

Answer 32

Oxidation, Sulfoxidation, Reduction, Hydrolysis

Question 33

Phase 2 hepatic reaction (GlucMethAcetyl) GMA

Answer 33

Glucuronidation, Methylation, Acetylation

Question 34

Locations of biotransformation

Answer 34

liver mostly

Question 35

what happens during phase 1 metabolism

Answer 35

oxidation in hepatocytes by CYPs

Question 36

function of CYP enzyme

Answer 36

detoxification leading to drug metabolism

Question 37

clinical significance of CYP enzymes

Answer 37

can be inhibited/induced which effects metabolism of drugs

Question 38

inhibition of CYP

Answer 38

rapid onset, short DOA, more inhibitors in clinical practice

Question 39

induction of CYP

Answer 39

slow onset, long DOA, forms toxic metabolites, less inducers in clinical practice

Question 40

Bupivacaine vs. Ketamine (explain significance of enantiomers)

Answer 40

Enantiomers = mirror images with same chemical formation but different spatial arrangement aka different effects on body. LevoBUPIVACAINE = local anesthetic, Na+ channel blocker, levorotary (S, -) isomer, less cardiotoxic. DextroBUPIVACAINE (R, +) more potent blockade of Na+ channels. Available as racemic mixture. KETAMINE = administered as racemic mixture. S, - enantiomer is 2-3x more potent than R. Less hallucinations and adverse effects and less CV depression.

Question 41

stereoisomer

Answer 41

drugs with chiral carbon have same molecular formula but different structural formula

Question 42

in renal elimination, what is active transport

Answer 42

tubular secretion

Question 43

what is renal excretion

Answer 43

net of filtration, secretion, and absorption

Question 44

clearance formula

Answer 44

clearance = rate of elim/ concentration

Question 45

difference between clearance and elimination

Answer 45

clearance is volume of blood cleared of drug per unit of time. elimination is amount of drug cleared from blood per unit of time. CLEARANCE = blood cleared ELIMINATION = drug cleared

Question 46

Vd calculation

Answer 46

Vd = Dose * F * Salt factor / Cp (plasma conc)

Question 47

First order rate kinetics

Answer 47

linear graph, t1/2 = 0.693/Ke

Question 48

zero order kinetics

Answer 48

horizontal line

Question 49

Half life

Answer 49

dependent on elimination

Question 50

concentration dependent clearance

Answer 50

mixed order

Question 51

mixed order/MM

Answer 51

small dose = first order, large dose = zero order

Question 52

Vm

Answer 52

max amount of drug that can be eliminated

Question 53

Pharmacokinetic Triangle

Answer 53

rate of elimination, rate of elimination, and amount in body

Question 54

2 types of dose response relationships

Answer 54

``` graded = drug dose is related to an individual = maximal efficacy of a drug quantal = drug dose is related to response in a population = variability of responsiveness of drug ```

Question 55

potency

Answer 55

how much of drug is required to cause effect, look at ED50

Question 56

EC50

Answer 56

efficacy of drug

Question 57

efficacy

Answer 57

ability of a drug to produce a certain effect

Question 58

more potent

Answer 58

less drug needed to produce same effect. PO less potent than IM because first pass effect

Question 59

tachyphylaxis

Answer 59

acute tolerance, occurs rapidly after withdrawal of drug

Question 60

tolerance

Answer 60

hyperactivity resulting from chronic drug exposure

Question 61

full agonists

Answer 61

+ efficacy

Question 62

partial agonists

Answer 62

don't have same effect as full agonist even at max dose

Question 63

inverse agonists

Answer 63

- efficacy, make receptor inactive

Question 64

antagonists

Answer 64

0 efficacy, prevent agonists from binding to receptor