Pharmacodynamics

Question 1

Adverse effects

Answer 1

unintended

Question 2

What is the study of adverse effects called

Answer 2

pharmacovigilance

Question 3

What are physical interactions on targets for drug action

Answer 3

osmotic diuretics
antacids
radioactive iodine

Question 4

Osmotic diuretics

Answer 4

molecules move through the body dragging water via osmosis until secreted

Question 5

Antacids

Answer 5

directly interact with acid in GI, physiologic antagonism

Question 6

Radioactive Iodine

Answer 6

actively concentrated in thyroid and radiation will destroy tissue 2-3 mm causing focal controlled destruction

Question 7

Ionotropic receptors

Answer 7

proteins in cell membrane that make a pore/tunnel. Usually ligand gated, something binds to them causing a change in shape allowing a large influx in ions (think neurotransmission).
Drugs can activate of prevent opening.

Question 8

Metabotropic Receptors

Answer 8

G-protein/7TM
Transduce extracellular signal to intracellular by activating G protein messenger system
Drug binds to receptor outside the cell caause G proteins inside the cell to bind to the receptor and take up GTP which gives them enough energy to move to a target enzyme or channel to cause an action
(Common in smooth muscle functions)

Question 9

Side effects

Answer 9

secondary to intended effect, can be good or bad

Question 10

Kinase-coupled receptors

Answer 10

Transmembrane proteins with and extracellular and intracellular portion that has enzymatic activity.
Phosphorylation and activation of proteins which activate effectors.
Insulin receptors are this type

Question 11

Nuclear Receptors (Transcription Factor Receptors)

Answer 11

Located in the cytoplasm but after ligand binds translocate to nucleus and bind to a response element within DNA to initiate specific gene transcription.
Ex- steroid and thyroid hormones

Question 12

Up regulation

Answer 12

increase in # of receptors and increase of effect of drug

Question 13

Down regulation

Answer 13

reduction of effect

May be part of normal cell metabolism or tolerance or tachyphylaxis

Question 14

How can drugs affect Voltage gated ion channels?

Answer 14

physical obstruction

modulate opening or closing of channel

Question 15

How can drugs affect enzymes?

Answer 15

Can be analogs
Prodrugs
False substrates leading to formation of abnormal metabolites

Question 16

How can drugs alter carrier proteins?

Answer 16

Preventing uptake

Preventing output

Question 17

Ligand

Answer 17

anything that binds to a recognition site

Question 18

Agonist

Answer 18

mimics the effect of endogenous ligand

Question 19

Full agonist

Answer 19

binds to receptor for maximal response

Question 20

Partial agonist

Answer 20

not as much effect as full agaonist but prevents anything else from binding

Question 21

Reverse agonist

Answer 21

binds to the receptor and causes opposite effect

Question 22

Antagonist

Answer 22

Binds to receptor and does nothing but block the receptor

Question 23

Competitive antagonism

Answer 23

binds and releases as long as its present. If agonist is present they will compete, who binds more often is determined by concentration and affinity. Can be reversible or irreversible.

Question 24

Efficacy

Answer 24

the maximal effect a drug can have (e=1 is full effect)

Question 25

Potency

Answer 25

Comparison of the concentration of two drugs needed to induce the same magnitude effect

Question 26

EC50

Answer 26

Effective Concentration 50%, concentration at which the drug produces 50% of its maximal effect. Applies only in vitro.

Question 27

ED50

Answer 27

Dose that produces a result in 50% of the animals. In vitro.

Question 28

Therapeutic Index

Answer 28

LD50/ED50

Question 29

Do you want a high or low therapeutic index?

Answer 29

High, low indicates a more dangerous drug.

Question 30

Onset of action

Answer 30

The time required after drug administration for a response to be observed

Question 31

Duration of action

Answer 31

length of time that a drug is effective