Exam 2 Material

Question 1

Science of interactions of chemical compounds with biological systems, how and where drugs act

Answer 1

Pharmacology

Question 2

Study of biochemical and physiological effects of drugs and the mechanisms of their actions, including the correlation of their actions and effects with their chemical structure

Answer 2

Pharmacodynamics

Question 3

The study of absorption, distribution, biotransformation, and elimination of xenobiotics

Answer 3

Pharmacokinetics

Question 4

Characteristics of drugs

Answer 4

Defined by actions, most act on receptors

Question 5

Endogenous drugs

Answer 5

foreign to the body, include toxins/poisons

Question 6

Where endogenous ligands bind

Answer 6

orthosteric site

Question 7

Receptor where gastric acid is neutralized by antacids

Answer 7

Extracellular receptor

Question 8

Receptor used to treat infections, cancer therapy, hormones like estrogen

Answer 8

Intracellular receptor

Question 9

Receptor of acetylcholine, muscarinic, nicotinic, GF receptors

Answer 9

Cell surface receptor

Question 10

Drug that binds to a receptor and stimulates a biological response

Answer 10

Agonist

Question 11

Drug that binds to a receptor without altering receptor function, alters interaction of receptor with another drug

Answer 11

Antagonist

Question 12

Drug must achieve adequate concentrations at site of action to produce characteristic effect

Answer 12

Purpose of drug therapy

Question 13

T/F No drug has a single effect

Answer 13

True

Question 14

KD measures

Answer 14

Affinity, determines potency

Question 15

Lower KD means

Answer 15

Higher affinity

Question 16

Cheng Prusoff

Answer 16

Ki = IC50/[1+L/KD]

Question 17

Total number of receptors on given cell or tissue

Answer 17

Bmax

Question 18

Affinity of ligand for the receptor identified at 1/2 Bmax

Answer 18

KD

Question 19

DOR,KOR,MOR question

Answer 19

Most selective for DOR - low ki value for DOR, high for MOR and KOR
Least selective - close values of ki for DOR, MOR, and KOR

Question 20

Binding of an agonist results in

Answer 20

induced fit that activates the receptor

Question 21

Binding of an antagonist results in

Answer 21

An induced fit that does not activate the receptor

Question 22

Dose response curve for agonist

Answer 22

Highest

Question 23

Dose response curve for antagonist

Answer 23

Zero

Question 24

Dose response curve for inverse agonist

Answer 24

negative

Question 25

Potency on graph

Answer 25

Farthest left on graph

Question 26

Efficacy on graph

Answer 26

Height on graph, limited by toxicity

Question 27

Produces a reduced response even at full receptor occupancy, can't produce same effect as full agonist regardless of concentration

Answer 27

Partial agonist

Question 28

Inverse agonist binds to

Answer 28

Orthosteric site

Question 29

Competitive antagonism on graph

Answer 29

Lines same shape spaced apart

Question 30

How to reverse competitive antagonism

Answer 30

Increase dose

Question 31

Schild plot determines

Answer 31

Affinity of agonist or receptor

Question 32

Non competitive agonist on graph

Answer 32

Lines different heights same starting point

Question 33

Non competitive agonist increases ____ an decreases ___

Answer 33

KD, Emax

Question 34

When the max response can be elicited by an agonist that does not result in 100% occupancy

Answer 34

Spare receptor

Question 35

Functional antagonism

Answer 35

Two drugs influence a physiological system in opposite directions ex - histamine and epinephrine

Question 36

Chemical antagonism

Answer 36

Chemical reaction between agonist and antagonist that forms inactive product

Question 37

Allosteric ligand benefit in therapy

Answer 37

ceiling effect, increased specificity for receptors with similar orthosteric binding sites

Question 38

Ki value table problems

Answer 38

Ki = 50% occupied Divide by 10 is 10% occupancy multiply by 10 is 90% occupancy

Question 39

Men who studied GPCRs

Answer 39

Lefkowits and Brian kobilka

Question 40

G protein effectors

Answer 40

Channels, enzymes, regulatory proteins

Question 41

G protein subtypes/second messengers

Answer 41

Cyclic AMP, Ca2+, Phosphoisinotides

Question 42

Quantal log dose response

Answer 42

All or none, increasing curve, ED50, LD50, or TD50

Question 43

Graded log dose response

Answer 43

Increases with increasing concentration, progressive increase, ED50 or TD50, S shaped with center symmetry Allows comparison of drugs with similar properties

Question 44

Calculate therapeutic indec

Answer 44

LD50/ED50, larger ratio= greater safety

Question 45

Drug tolerance

Answer 45

Decreased responsiveness to a drug

Question 46

Cross tolerance

Answer 46

Tolerance develops to one drug seen with drugs belonging to the same class

Question 47

Tachyphylaxis

Answer 47

Acute development of tolerance following rapid or repeated administration, can't overcome with increased dose

Question 48

Behavioral sensitization

Answer 48

Increased effect of drug the more times its administered

Question 49

Idiosyncratic reaction

Answer 49

Genetically determined abnormal reactivity to a drug, sensitive to low doses or not sensitive to high doses

Question 50

Physiological variables

Answer 50

Age, Gender, Pregnancy, Food, Circadian Clock

Question 51

Pathological factors

Answer 51

Liver disease, Renal disease, Malnutrition

Question 52

Genetic factors

Answer 52

Pseudocholinesterase deficiency, malignant hyperthermia