Pharmacology I

Question 1

define pharmacology

Answer 1

the branch of medicine concerned with the uses, effects and modes of action of drugs

Question 2

define pharmakinetics

Answer 2

the actions of the body on the drugs

Question 3

define pharmadynamics

Answer 3

the actions the drugs have on the body

Question 4

what does ADME mean?

Answer 4

A absorption
D distribution
M metabolism
E elimination

Question 5

Drug-receptor interactions:

Agonist

Answer 5

drug or natural ligand
activates the receptor
sometimes selective and sometimes not

Question 6

Drug-receptor interactions:

anatgonist

Answer 6

*bind to receptor but do not activate
interfere with agonist
typically shift dose-response to the right

Question 7

Drug-receptor interactions:

allosteric activator

Answer 7

postitive allosteric modulator
*binds to receptor site separate from agonist site
potentiates effects

Question 8

Drug-receptor interactions:

allosteric inhibitor

Answer 8

negative allosteric modulator
bind receptor site separate from agonist site
*noncompetitive
*actions often reversible

Question 9

in the absence of drugs, the two isoforms are in equilibrium and what is favored

Answer 9

receptor inactive

Question 10

what is a full agonists

Answer 10

has a much high affinity for the active receptor conformation and mass action thus favors the formation of the active receptor bound to the drug complex with a much larger observed effect**

Question 11

Partial agonists

Answer 11

produce lower response at receptor occupancy than full agonist

• intermediate affinity for both inactive and active receptor(less affinity than full agonist)
• does not stabilize active receptor-drug complex as well as a full.

Question 12

Inverse agonist

Answer 12

have a greater affinity for inactive receptor, reduce constitutive activity, and may produce a contrasting physiologic result

Question 13

conventional antagonist

Answer 13

equal affinity for the active and inactive receptor and thus no change in constitutive activity.
**flat line on graph

Question 14

what is the effective concentration 50?

Answer 14

drug concentration where effect is half the maximum

Question 15

what is the Kd?

Answer 15

drug concentration where receptor occupancy is half the maximum

Question 16

what causes a shift to the right in the EC50?

Answer 16

agonist and a competitive antagonist

Question 17

what causes a drop in the agonist effect?

Answer 17

agonist and a noncompetitive antagonist

**no shift in EC50

Question 18

what is the plateau?

Answer 18

the max effect of the agonist effect

Question 19

what is the threshold?

Answer 19

the lowest dose that causes a measurable effect

Question 20

receptors are spare for a given pharmacologic response if it is possible to do what?

Answer 20

elicit a maximal biologic response at a concentration of agonist that does not result in occupancy of the full complement of available receptors.
-so after one dose you can give another dose and get a maximal effect again due to spare receptors

Question 21

additive drug-receptor interactions

Answer 21

sum of the two drugs is equal to the two drugs

Question 22

synergistic drug-receptor interactions

Answer 22

the sum of the two drugs is greater than the sum of the two drugs

Question 23

antagonistic drug-receptor interactions

Answer 23

additive effect is less than the sum of the two drugs

eg. antidote

Question 24

chemical antagonist

Answer 24

does not involve receptor
eg. protein that is positively charged at physiologic pH counteracting the effects of a drug that is negatively charged by ionic binding that makes the other drug unavailable to interact

Question 25

physiological antagonist

Answer 25

involves endogenous regulatory pathways mediated by different receptors

Question 26

what does efficacy mean?

Answer 26

refers to the number of receptors that must be activated to yield a maximum response.

Question 27

A drug with high efficacy needs to stimulate only a small or large percentage of receptors?

Answer 27

small percentage **lower dosing needed vertical response

Question 28

a drug with a lesser efficacy (but still not considered to be a full agonist) has to activate a small or larger proportion of receptors?

Answer 28

larger percentage of receptors **higher dosing needed verticle response

Question 29

what does potency mean?

Answer 29

the relative concentrations of two or more drugs that produced the same drug effect. This effect is usually chosen is 50% of the maximal effect and the dose causing this effect is called the EC50

Question 30

is potency a vertical or horizontal relationship?

Answer 30

horizontal

Question 31

what is the therapeutic index?

Answer 31

toxic dose/effective dose | you want a wide range and a big number

Question 32

what is the therapeutic range?

Answer 32

the dose between toxicity and therapy

Question 33

what is margin of safety?

Answer 33

the amount of drug that is lethal to 1% divided by the amount of drug that causes beneficial effect in 99%

Question 34

a wide margin of safety means what?

Answer 34

a large difference between toxic dose and therapeutic dose

Question 35

what does parenteral mean?

Answer 35

not by way of intestine or GI tract

Question 36

intravenous

Answer 36

very rapid, easier to titrate avoids sub. cutaneous irritation, overdoses may have effects too immediate to reverse

Question 37

intramuscular

Answer 37

``` prompt absorption (5 minutes owing to blood flow) large volumes possible, sometimes painful ```

Question 38

subcutaneous

Answer 38

adsorption may be less rapid (i.e. 15 minutes) | smaller volumes than intramuscular, sometimes painful

Question 39

enteral

Answer 39

by way of the intestine or GI Buccal or sublingual oral rectal

Question 40

buccal or sublingual enteral

Answer 40

under tongue or incheek

Question 41

oral enteral

Answer 41

most common and convenient, onset of effects in 30 min. most unpredictable absorption via duodenum first pass metabolism

Question 42

rectal enteral

Answer 42

solution(enema) or suppository | less first pass than oral

Question 43

the initial distribution of drug into tissues is determined by what?

Answer 43

rate of blood flow

Question 44

the concentration of drug at a particular site is related to what?

Answer 44

affinity

Question 45

plasma binding proteins and gastric emptying time can play roles T/F

Answer 45

true

Question 46

what is the fastest way to deliver a drug?

Answer 46

inhalation

Question 47

topical delivery

Answer 47

applied to a surface

Question 48

transdermal delivery

Answer 48

onset of effect in 15 min slow and sustained nicotine patch

Question 49

what is a loading dose?

Answer 49

a boosted initial dose to get the concentration higher than the therapy level to start immediate effects

Question 50

what is a maintenance dose?

Answer 50

doses that keep the concentration in the therapy range or window