I. PPT

Question 1

Determines the fraction of drug molecules charged (ionized) vs uncharged (non-ionized)

Answer 1

pH

Question 2

a neutral molecule that can reversibly dissociate into an anion and a proton

Answer 2

weak acid

Question 3

a neutral molecule that can form a cation by combining with a proton

Answer 3

weak bases

Question 4

(weak acids)

unprotonated form is more ____

Answer 4

water soluble

Question 5

(weak acids)

protonated is more ___

Answer 5

lipid soluble

Question 6

(weak acids)

better clearance

protonated/unprotonated

Answer 6

unprotonated

Question 7

(weak acids)

cross biological membrane easily

protonated/unprotonated

Answer 7

protonated

Question 8

(weak bases)

more lipid soluble, cross biological membrane easily

protonated/unprotonated

Answer 8

unprotonated

Question 9

(weak bases)

more water soluble, better clearance

protonated/unprotonated

Answer 9

protonated

Question 10

excretion of weak acid is accelerated by ___

Answer 10

alkalinizing the urine

Question 11

excretion of weak base is accelerated by ____

Answer 11

acidifying the urine

Question 12

the component of a cell or organism that interacts with a drug and initiates the chain of events leading to the drug’s observed effects

Answer 12

receptor

Question 13

responsible for selectivity of drug action

Answer 13

receptors

Question 14

largely determine the quantitative relations between dose or concentration of drug and pharmacologic effects

Answer 14

receptors

Question 15

mediate the actions of both pharmacologic agonists and antagonists

Answer 15

receptors

Question 16

receptors (3)

Answer 16

enzymes
transport proteins
structural proteins

Question 17

responses to low doses of a drug usually increase in ___ to dose

Answer 17

direct proportion

Question 18

as doses increase, the response increment __

Answer 18

diminishes

Question 19

the transduction process that links drug occupancy of receptors and pharmacologic response

Answer 19

coupling

Question 20

it is possible to elicit a maximal biologic response at a concentration of agonist that does not result in occupancy of all of the available receptors

Answer 20

spare receptors

Question 21

may be demonstrated by using irreversible antagonists to prevent binding of agonist to a proportion of available receptors and showing that high concentrations of agonist can still
produce an undiminished maximal response

Answer 21

spare receptors

Question 22

bind to receptors but do not activate them

Answer 22

antagonist

Question 23

prevents agonists from activating receptors

Answer 23

antagonist

Question 24

antagonists 2 types

Answer 24

competitive (reversible)
non-competitive (irreversible)

Question 25

___ agonist binds to receptors in a reversibleway

Answer 25

competetive

Question 26

the presence of antagonist increases the agonist concentration required for a given degree of response, and so the agonist concentration-effect curve is shifted to the ___

Answer 26

right

Question 27

the degree of inhibition produced by a competitive antagonist depends on the ____

Answer 27

concentration of antagonist

Question 28

cause downward shift of DRC

Answer 28

non competitive antagonist

Question 29

agonists 2 types

Answer 29

full a. partial a.

Question 30

capable of fully activating the effector system

Answer 30

full agonist

Question 31

high affinity for the activated receptor conformation

Answer 31

full agonist

Question 32

produce less than the full effect, even when it has saturated the receptors

Answer 32

partial agonist

Question 33

in the presence of an agonist, it acts as an inhibitor

Answer 33

partial agonist

Question 34

Interact directly with the drug being antagonized to remove it or to prevent it from reaching its target

Answer 34

Chemical antagonist

Question 35

Does not depend on the interaction with the agonist's receptor

Answer 35

Chemical antagonist

Question 36

Binds to a different receptor, producing an effect opposite to that produced by the drug it is antagonizing

Answer 36

Physiologic Antagonist

Question 37

Response of a particular receptor-effector system measured against increasing drug concentration

Answer 37

dose-response curve Emax, EC50

Question 38

Maximal effect an agonist can produce

Answer 38

Efficacy

Question 39

Determined mainly by the nature of the receptor and its associated effector system

Answer 39

Efficacy

Question 40

refers to the concentration (EC50) or dose (ED50) of a drug required to produce 50% of that drug's maximal effect

Answer 40

Potency

Question 41

Determined mainly by the affinity (Kd) of the receptor to the drug

Answer 41

Potency

Question 42

Minimum dose required to produce a specified response is determined in each member of a population

Answer 42

QUANTAL DOSE-EFFECT CURVES

Question 43

the measure of the ability of the body to eliminate the durg

Answer 43

clearance

Question 44

the factor that predicts the rate of elimination in relation to the drug concentration

Answer 44

clearance

Question 45

two major sites of drug elimination:

Answer 45

kidneys and liver

Question 46

clearance will vary depending on the concentration of drug that is achieved

Answer 46

capacity-limited elimination

Question 47

also known as saturable, dose- or concentration-dependent, nonlinear, and Michaelis-menten elimination

Answer 47

capacity-limited elimination

Question 48

drugs are cleared very readily by the organ of elimination, so that at any clinically realistic concentration of the drug, most of the drug in the blood perfusing the organ is eliminated on the first pass of the drug through it

Answer 48

flow-dependent elimination

Question 49

the elimination of these drugs will depend primarily on the rate of drug delivery to the organ of elimination

Answer 49

flow-dependent elimination

Question 50

is the time required to change the amount of drug in the body by one-half during elimination/ during constant infusion

Answer 50

half life

Question 51

indicates the time required to attain 50% of steady state

Answer 51

half time

Question 52

defined as the fraction of unchanged drug reaching the systemic circulation following administration by any route

Answer 52

bioavailability

Question 53

for a drug administered orally, bioavailability may be less than 100% for 2 reasons:

Answer 53

1. incomplete extent of absorption 2. first-pass elimination

Question 54

different routes of administration

Answer 54

IV IM SC PO Rectal Inhalation Transdermal

Question 55

following absorption across the gut wall, the portal blood delivers the drug to the liver prior to entry into the systemic circulation

Answer 55

first-pass elimination

Question 56

____ plays a pivotal role in terminating the biologic activity of some drugs

Answer 56

renal excretion

Question 57

converts the parent drug to a more polar or more reactive product by unmasking or inserting a polar functional group

Answer 57

PHASE 1

Question 58

phase 1 reactions examples

Answer 58

oxidation reduction deamination hydrolysis

Question 59

also called mixed-function oxidases

Answer 59

cytochrome P450

Question 60

Cytochrome P450 is found in the

Answer 60

SER of liver

Question 61

reactions that makes the drug more polar and less lipid-soluble

Answer 61

Phase II reactions

Question 62

Phase II reactions examples

Answer 62

glucoronidation acetylation glutathione conjugation glycine conjugation sulfation methylation

Question 63

metabolized to products that irreversibly inhibit the metabolizing enzymes

Answer 63

suicide inhibitors