Pharmacology Basics

Question 1

actions of the biological system on the drug
What the body does to the drug

Answer 1

Pharmacokinetics

Question 2

Pharmacokinetics describes:

Answer 2

What the body does to the drug

Question 3

study of the undesired effects of chemicals on biological systems

Answer 3

Toxicology

Question 4

action of drugs on the biological system
What the drug does to the body

Answer 4

Pharmacodynamics

Question 5

Pharmacodynamics describes:

Answer 5

What the drug does to the body

Question 6

Molecules whose interaction with receptor causes cellular responses

Answer 6

Agonists

Question 7

Molecules whose interaction with receptor does not cause cellular response

Answer 7

Antagonists
But can prevent action of an agonist

Question 8

Difference between agonists and antagonists

Answer 8

Agonists cause cellular responses; antagonists do not

Question 9

Type of drug-target binding that is rare for drug-receptor interactions and irreversible

Answer 9

Covalent bonds

Question 10

Drug-target binding for aspirin

Answer 10

Aspirin forms covalent (irreversible) bond with cyclooxygenase

Question 11

Aspirin forms this type of bond with cyclooxygenase

Answer 11

Covalent (irreversible)

Question 12

Aspirin forms covalent (irreversible) bond with this

Answer 12

Cyclooxygenase

Question 13

Type of drug-target binding that is the primary electrostatic attractor

Answer 13

Ionic bond

Question 14

Type of drug-target binding that is the secondary attractor; increased influence with better “fit”

Answer 14

Hydrogen and/or Van der Waals bonds

Question 15

Opiate stereoisomers that are analgesic

Answer 15

L opiates
(D opiates are not)

Question 16

Opiate stereoisomers that are antitussive

Answer 16

Both L and D opiates

Question 17

Do stereoisomers require a symmetric or asymmetric center?

Answer 17

Asymmetric

Question 18

proteins that bind with specificity and selectivity but are not receptors
No activity change with binding

Answer 18

Acceptors

Question 19

Is there activity change with binding of acceptors?

Answer 19

No

Question 20

Acceptors can affect pharmacodynamics by binding the drug and preventing:

Answer 20

Prevent drug interaction with the receptor

Question 21

Drugs binding to acceptors is also referred to as this

Answer 21

Nonspecific protein binding

Question 22

Nonspecific protein binding refers to this

Answer 22

Drugs binding to acceptors

Question 23

Part of the dose response curve that is a measure of drug effectiveness or efficacy

Answer 23

Emax or the ceiling

Question 24

Part of the dose response curve that is an indicator of binding affinity (strength) for the drug

Answer 24

Steepness of curve

Question 25

Part of the dose response curve that is a measure of drug potency

Answer 25

Dose at 50% = effective dose 50% (ED50)

Question 26

Emax or the ceiling of the dose response curve is a measure of this

Answer 26

Drug effectiveness / efficacy

Question 27

Steepness of the dose response curve is an indicator of this

Answer 27

Binding affinity (strength) for the drug

Question 28

Effective dose 50% (ED50; dose at 50% response) is a measure of this

Answer 28

Drug potency

Question 29

Comparison of dose at a single level of effect Does not allow comparison of effectiveness, merely dose at each drug’s half maximal response

Answer 29

Potency

Question 30

Potency is this

Answer 30

Comparison of dose at a single level of effect (dose at each drug's half maximal response)

Question 31

Does potency increase or decrease as the dose response curve shifts left?

Answer 31

Increases

Question 32

Measure of maximal response effect Does not compare dose at maximal effect NOT a dose

Answer 32

Efficacy (aka intrinsic activity)

Question 33

Efficacy (intrinsic activity) measures this

Answer 33

Maximal response effect

Question 34

Does efficacy increase or decrease as dose response curve shifts down?

Answer 34

Decreases

Question 35

Does potency or efficacy measure dose?

Answer 35

Potency

Question 36

Intrinsic activity is also referred to as this

Answer 36

Efficacy

Question 37

Efficacy is also referred to as this

Answer 37

Intrinsic activity

Question 38

Describes when fewer than the total number of receptors are required to be occupied to achieve a maximal response

Answer 38

Receptor reserve ("spare receptors")

Question 39

Receptor reserve ("spare receptors") describes when:

Answer 39

Fewer than the total number of receptors are required to be occupied to achieve a maximal response

Question 40

Type of antagonism that binds the receptor but does not activate Prevents other molecules from binding the receptor

Answer 40

Receptor antagonism

Question 41

Type of antagonism that is a direct chemical interaction between agonist and antagonist, that renders agonist inactive

Answer 41

Chemical antagonism

Question 42

Type of antagonism that involves two agonists with opposing effects

Answer 42

Functional antagonism

Question 43

A receptor antagonist does this

Answer 43

Binds receptor but does not activate Prevents other molecules from binding the receptor

Question 44

A chemical antagonist does this

Answer 44

Directly chemically interacts with agonist and renders it inactive

Question 45

Functional antagonism involves this

Answer 45

2 agonists with opposing effects

Question 46

Type of antagonism where the agonist and inhibitor compete for access to binding site Maximal effect maintained; potency reduced

Answer 46

Competitive

Question 47

Type of antagonism with two major types: irreversible (covalent binding) and allosteric antagonists Reduces efficacy

Answer 47

Noncompetitive antagonism

Question 48

Competitive antagonism reduces this

Answer 48

Potency

Question 49

Competitive antagonism has no effect on this

Answer 49

Maximal effect / efficacy

Question 50

Noncompetitive antagonism reduces this

Answer 50

Efficacy

Question 51

Allosteric antagonists mimic the dose response curve of this

Answer 51

Noncompetitive antagonism

Question 52

Allosteric ______ enhance effect of primary receptor activation

Answer 52

Allosteric agonists

Question 53

Allosteric _____ reduce the effect of primary receptor activation

Answer 53

Allosteric antagonists

Question 54

Allosteric agonists has this affect on dose response curve

Answer 54

Opposite of competitive = increase potency, shift left

Question 55

Allosteric antagonist has this affect on dose response curve

Answer 55

Mimic non-competitive = lower curve

Question 56

Type of agonists that when added to a full agonist, may reduce the maximal activity achieved with only the full agonist by blocking the full agonist’s access to the active receptor

Answer 56

Partial agonists

Question 57

Type of agonists that have intrinsic activity opposing agonist activity Some receptors are normally ‘active’ and require an agonist to turm them “off”

Answer 57

Inverse agonists

Question 58

Type of agonist that lowers the activity from that of full agonist, but still remains more active that constitutive activity

Answer 58

Partial agonist

Question 59

Type of agonist that decrease activity below that of the constitutive activity level

Answer 59

Inverse agonist

Question 60

state of decreased responsiveness to a drug (describes loss of response to drugs)

Answer 60

Desensitization

Question 61

rapid desensitization due to repeated exposure to the same drug concentration

Answer 61

Tachyphylaxis

Question 62

Desensitization that is rapid and receptors are usually retained

Answer 62

Tachyphylaxis

Question 63

Type of desensitization that is not dose dependent

Answer 63

Tachyphylaxis

Question 64

Tachyphylaxis describes this

Answer 64

rapid desensitization due to repeated exposure to the same drug concentration

Question 65

reduced response to drug exposure over a long time frame, usually involving reduced receptor numbers

Answer 65

Tolerance

Question 66

Type of desensitization involving changes in receptor number and/or function due to drug exposure

Answer 66

Tolerance

Question 67

4 mechanisms of desensitization

Answer 67

Uncoupling of the receptor from downstream signaling Endocytosis Degradation Down regulation

Question 68

Uncoupling of the receptor, endocytosis, degradation, and down regulation are mechanisms of this

Answer 68

Desensitization

Question 69

processes that reduce the number of receptor in a cell membrane Occurs following continuous exposure to agonist or endogenous ligand, dictated at least in part by negative feedback Mechanisms may include decreased gene transcription or increased mRNA degradation

Answer 69

Down regulation

Question 70

2 mechanisms of down regulation

Answer 70

Decreased gene transcription Increase mRNA degradation

Question 71

Occurs when: The cell is continuously exposed to an antagonist, decreasing exposure to agonist, Disease reduces concentration or availability of endogenous ligand Genetic amplification

Answer 71

Up regulation

Question 72

Drug that induces up-regulation of opioid receptors

Answer 72

Naloxone

Question 73

exaggerated receptor response resulting from chronic reduction of receptor stimulation Usually due to prolonged lack of exposure

Answer 73

Supersensitivity

Question 74

Supersensitivity describes this:

Answer 74

Exaggerated receptor response resulting from chronic reduction of receptor stimulation