N301 Q#1 Pharmacology Foundation Principles

Question 1

____: any fxnl macromolecule in or on a cell to which a drug binds to produce it’s effects.

Answer 1

Receptor

Question 2

Pharmacodynamics begins where?

Answer 2

at binding site or site of action

Question 3

Binding of a drug to its receptor is usually ____. The receptor must be ___ to influence cellular fxn.
Receptor activity is regulated by ____ compounds.

Answer 3

1. reversible
2. on
3. endogenous

Question 4

Endogenous compounds are?

Answer 4

neurotransmitters, hormones and other regulatory mlcls.

Question 5

Drugs either ___ or block the action of the body’s own regulatory molecules. Drugs produce therapeutic effects by helping the body use it’s pre-existing ___.

Answer 5

Mimic

capacities

Question 6

What are the 4 types of receptor families?

Answer 6

1. cell membrane-embedded enzymes
2. ligand-gated ion channels
3. G Protein-coupled receptor systems
4. transcription factors

Question 7

____: receptors located on the cells surface, binding of an ___ activates the enzyme resulting in rapid ___. Provide an example.

Answer 7

Cell membrane embedded enzymes
agonist
response
Insulin

Question 8

_____: receptors that span the cell membrane and regulate the flow in and out of cells. Each one is for a specific ___. Several neurotransmitters including ___ and ____ act thru this type of receptor.

Answer 8

ligand-gated ion channels
ion
ACH and GABA

Question 9

G-protein coupled receptor systems bind an agonist drug that activates the ____ which activates ___ which then activates its effector. rapid response results. Which ligands act through these receptors?

Answer 9

receptor
G-protein
NE, serotonin, histamine

Question 10

_____: are receptors that are found within the cell (not on the surface). They have ____ response. An agonist drug activates the receptor by stimulating ___ which spurs protein synthesis. What hormone acts through this receptor type?

Answer 10

Transcription factors
delayed
mRNA
Thyroid hormone

Question 11

True or False: the more selective a drug the greater the side effects.
Selectivity does not guarantee ____.

Answer 11

False. less side effects

safety

Question 12

simple occupancy theory is a drug-receptor ____. The ___ of the response to the drug is proportional to the number of receptors occupied by that drug. A maximal response will occur when all available receptors have been ____.

Answer 12

interaction
intensity
occupied

Question 13

____ occupancy theory explains why simple occupancy doesn’t work. Because of ___ and Intrinsic activity

Answer 13

Modified

affinity

Question 14

___: the strength of the attraction b/w a drug and its receptor. High affinity drugs have a ___ attraction for receptor sites, they are also very ___. Drugs with low affinity have to be present in high ____ to elicit a response and are therefore ___ potent.

Answer 14

Affinity
strong
potent
concentrations
less

Question 15

____: the ability of a drug to activate a receptor on binding. High IA have high maximal ___ and produce an ___ response b/c they cause intense receptor ____.

Answer 15

Intrinsic Activity
efficacy
intense
activation

Question 16

Intrinsic activity of a drug is reflected by its maximal _____. IA only applies to ____.

Answer 16

efficacy

agonists

Question 17

True or False: affinity applies to both agonists and antagonists while intrinsic affinity only applies to agonists.

Answer 17

True

Question 18

The intensity of response is still related to the number of ___ but the intensity is also related to the ability of the drug to ___ receptors once binding has occurred.

Answer 18

receptors

activate

Question 19

antagonists have ___ for a receptor but have no intrinsic activity. Affinity permits receptor binding and lack of IA prevents receptor ___.

Answer 19

affinity

activation

Question 20

Define Noncompetitive antagonists

Answer 20

bind irreversibly to receptors reducing the total number of receptors available to an agonist.

Question 21

noncompetitive antagonists bind irreversibly, will this last indefinitely?

Answer 21

No, it will only last for the life of the receptor which is usually only a few days.

Question 22

Competitive antagonist bind ____. If an agonist and antagonist have equal ___ for a receptor, then the receptor will be occupied by whichever agent is present in highest ____.

Answer 22

reversibly
affinity
concentration

Question 23

A partial agonist has moderate ____. Therefore maximal effect is lower than a full agonist. Partial agonists can act as agonists if no full agonist is present OR as an _____ if a full agonist is present.

Answer 23

intrinsic activity

antagonist

Question 24

If you introduce a full agonist while a partial agonist is on board, will you get a response? Example: if you prescribe pentazocine (partial agonist) and don’t d/c the pentazocine before starting morphine, the patient will or will not get the full affect of the morphine?

Answer 24

NO, the partial agonist will act as an antagonist

Will not, the pentazocine is occupying the opioid receptors.

Question 25

_____ results from continuous exposure of cell receptors to an agonist. ____ results from continuous exposure of a cell receptors to an antagonist.

Answer 25

Desensitization | Hypersensitivity

Question 26

What do antacids, antiseptics, saline laxatives and chelating agents have in common?

Answer 26

They do not act via receptors.

Question 27

ED50?

Answer 27

The average effective dose for 50% of the population. The remaining 50% will be under or over treated with the initial dose.

Question 28

Define the following pregnancy categories: | A, B, C, D and X

Answer 28

A: 100% safe B: remote risk C: wild card, wasn't tested D and X: BAD proven risk

Question 29

Based on research for teratogenic effects on the fetus, up to 60 days after ____ adverse effects will result in gross malformations. Exposure later in pregnancy results in _____ impairment or cognitive defects. Within week 1 or 2 fetus will either die from exposure or will survive. all or nothing.

Answer 29

implantation | functional

Question 30

Pediatrics are more sensitive to drug therapy due to organ system ____ while elderly are sensitive due to organ system ____.

Answer 30

immaturity | degeneration

Question 31

Peds have differences in ____ and distribution. They have a higher ___ content, immature ____ and limited ____ capacity.

Answer 31

absorption water blood-brain barrier protein binding

Question 32

Peds also have lower drug ____ capacity because the ____ is immature. Adult ____ levels are acheived by age one.

Answer 32

metabolism liver excretion