Pbda Exam 2

Front 1

Occupancy Theory

Back 1

Intensity of pharmacological effect is directly proportional to the number of receptors occupied

Front 2

NOAEL

Back 2

The maximum amount of compound administered without adverse reaction

Front 3

Toxicophore

Back 3

The part of the molecule that causes toxic effects

Front 4

ED50

Back 4

Dose amount that is maximum effective to 50% of test animals

Front 5

LD50

Back 5

Lethal dose for 50% of test animals

Front 6

Auxophore

Back 6

Part of the molecule that does not react with the receptor

Front 7

Pharmacophore

Back 7

Part of the molecule that reacts with the molecule

Front 8

SAR

Back 8

The relationship between the drug structure and it's effect on the body

Front 9

Lead Modification

Back 9

Modification of a molecule to fulfill required clinical usefulness

Front 10

Activity cliff

Back 10

Maximum modification of the molecule without loss of desired function

Front 11

Inverse Agonist

Back 11

Stimulates opposite response as agonist

Front 12

Agonist

Back 12

Stimulates response by receptor

Front 13

Antagonist

Back 13

Prevents receptor response

Front 14

Modified occupancy theory

Back 14

Accounts for partial agonists

Front 15

Efficacy

Back 15

Ability of a drug to produce maximum response

Front 16

4 major drug targets

Back 16

1. GPCR

2. Ion Channel

3. Nuclear Receptor

4. RTK

Front 17

2 Fundamental Characteristics of a Receptor

Back 17

1. Recognition Capacity

2. Initiation of Biological Response

Front 18

Kd

Back 18

Dissociation Constant,

Affinity of drug for receptor

Front 19

As a constant decreases, what happens to the Affinity of the drug for the receptor?

Back 19

The Affinity increases

Front 20

Intrinsic Sympathomimetic Activity

Back 20

The ability of a drug to activate adrenergic receptors that are similar to sympathetic nervous system stimulation

Front 21

Inverse Agonist drug

Back 21

Produces the opposite effect of the natural ligand

Front 22

Antagonist drug

Back 22

Blocks the response of a natural ligand

Front 23

Agonist drug

Back 23

Stimulates the response of a receptor

Front 24

Can agonists and antagonists bind the same site of a receptor?

Back 24

Yes

Front 25

Rate theory

Back 25

Activation of receptors is proportional to the total number of Encounters of a drug with its receptor per unit time

Front 26

Induced fit Theory

Back 26

Agonists induced conformational change antagonists do not induce conformational change

Front 27

Activation aggregation Theory

Back 27

The receptor is always in a state of dynamic equilibrium between activated form and inactivated form

Front 28

Back 28

Glycene

Front 29

Back 29

Serine

Front 30

Back 30

Threonine

Front 31

Back 31

Cysteine

Front 32

Back 32

Aspartic Acid

Front 33

Back 33

Glumatic Acid

Front 34

Back 34

Lysine

Front 35

Back 35

Histidine

Front 36

"Rate enhancement by proximity" is also known as:

Back 36

"Approximation"

Front 37

Which process is more simple: enzyme purification or receptor purification?

Back 37

Enzyme purification

Front 38

What is the symbol for "enzyme-substrate dissemination constant?

Back 38

Kd

Front 39

What is the symbol for a catalytic step?

Back 39

Kcat

Front 40

Is an ideal enzyme target include an enzyme essential for the patient?

Back 40

No

Front 41

What type of bond is associated with"irreversible inhibition"?

Back 41

Covalent

Front 42

What symbol represents concentration of 50% enzyme inhibition?

Back 42

IC50

Front 43

What is the effect on enzymes of E.I. formation?

Back 43

Prevents substrate binding

Front 44

What is the name of this equation?

Back 44

Michaelis-Menten Equation

Front 45

What is the symbol for substrate concentration at half-maximum velocity?

Back 45

Km

Front 46

What is the ratio of organisms that have mutations that offer drug resistance?

Back 46

1:10,000,000

Front 47

What is mechanism for bacterial transduction?

Back 47

Phage

Front 48

A chemical or drug that is metabolized after administration into an active drug

Back 48

Prodrug

Front 49

What is changed in bacteria with bactrim resistance?

Back 49

A single amino acid

Front 50

Which enzyme is involved in bactrim resistance?

Back 50

Dihydrofolate Reductace

Front 51

What in the bacteria is targeted by vancomycin?

Back 51

Peptidoglycan

Front 52

What bond is blocked with vancomycin resistance?

Back 52

Hydrogen bond

Front 53

How effective is vancomycin resistance?

Back 53

1000 fold

Front 54

What enzyme do bacteria produce to counter penicillin?

Back 54

Beta-lactimase

Front 55

What Secondary medicine is used to counter beta-lactamase?

Back 55

Clavulanic acid

Front 56

8 mechanisms of drug resistance

Back 56

1. Altered enzyme/receptor

2. Overproduction of enzyme/receptor

3. Overproduction of substrate/ligand

4. Increase drug-destroying mechanisms

5. Decreased prodrug activation

6. Activation of new pathways circumventing drug action

7. Reversal of drug action

8. Altered drug distribution to the site of action

Front 57

Homologation

Back 57

Increasing the length of a chain

Front 58

Ion Channel

Back 58

Transmembrane tissue composed of 3 elements

Front 59

What 3 elements is the ion Channel composed of?

Back 59

Pore: transit of ion and one or more gates

Gates: part of protein open and close in response to stimuli

Sensors: receives stimuli

Front 60

Nuclear receptors

Back 60

Ligands dependent transcription factors that sense steroid and thyroid hormones, bile acids, fatty acids, and certain vitamins and prostaglandin

Regulate gene expression

Front 61

What do Nuclear receptors control?

Back 61

Development

Differentiation

Metabolism

Reproduction of Organism

Front 62

What is the site of a drug action receptor

Back 62

Any biological molecule with which the drug interacts

Front 63

The site of a drug reaction is responsible for?

Back 63

The pharmaceutical effect-- pharmacodynamics

Front 64

Receptors discussed include 4 major drug targets

Back 64

GPCRS

Ion channels

Nuclear Receptors

Receptors tyrosine kinases

Front 65

What is the largest class of receptors known

Back 65

GPCRS about 800 different human genes, 4% of human genome

Front 66

What are RTKs (receptor tyrosine kinases)

Back 66

Subclass of cell-surface growth factor receptors having kinase activity

Front 67

RTKS kinase activity

Back 67

Catalyze and transfer of the y-phosphate group from donor which simulates a cascade of signaling pathways

Front 68

RTKS example of catalyze transfer

Back 68

ATP top hydroxyl groups of tyrosine residue of target proteins

Front 69

What controls the most fundamental cellular processes

Back 69

RTKS (receptor tyrosine kinases)

Front 70

What cellular processes do RTKs control

Back 70

Cell cycle

Cell migration

Cell metabolism

Survival

Carcinogenesis (cell proliferation and differentiation)

Front 71

Two fundamental characteristics of a receptor

Back 71

Recognition capacity

Amplification

Front 72

Recognition capacity

Back 72

Binding of molecules

Front 73

Amplification

Back 73

Initiation of biological response

Front 74

Forces in drug reaction complex

Back 74