Pharmacodynamics

Question 1

Define pharmacodynamics

Answer 1

Study of what drugs do to the body

Question 2

Pharmacokinetics is

Answer 2

Question 3

Pharmacodynamics is

Answer 3

Question 4

A drug is a xenobiotic that induces an effect typically by interacting with an endogenous target molecule, also called a _____

Answer 4

Receptor

Question 5

The ____ can be an enzyme, nucleic acid, or a special membrane brown protein

Answer 5

Receptor

Question 6

A large class of drug receptors are ______ _____, a molecule produced by the body (endogenous). Examples include ligand gated ion channels, G protein coupled receptors

Answer 6

Physiological receptors

Question 7

The second largest class of drug targets are _____. Example is penicillin, ACE Inhibitors

Answer 7

Enzymes

Question 8

The third major class of drug receptors are _____.

Answer 8

Nucleic acids

Question 9

Drug dose response graph. The drug concentration is on the X axis and a _____ on the Y axis

Answer 9

Biological effect

Question 10

Fischer projection is a ___ and ____ model of thinking about enzyme and substrate interaction. This model has limitations

Answer 10

Lock and key

Question 11

_____ is the equilibrium dissociation constant of a drug-receptor complex. ______ is the reciprocal of kD. If affinity is high, the dissociation constant will be low.

Answer 11

kD
Affinity

Question 12

Low affinity requires a ____ concentration of molecules

Answer 12

Higher

Question 13

The _____ is the free drug concentration at which half of the receptors are drug bound

Answer 13

KD (similar to Km)

Question 14

Different drugs may possess distinct _____ for a common target (receptor)

Answer 14

Potencies

Drug A is more potent than drug B. It takes less concentration of drug A to reach the same effect

Question 15

A lower ED50 of a drug means the _____ the potency.

Answer 15

Higher

Question 16

The _____ opens the lock, the _____ does not open the lock. These two things can compete for each other.

Answer 16

Agonist
Antagonist

Question 17

Answer 17

Drug A is an agonist, Drug B is an antagonist

Question 18

_____ ____ can be overcome if sufficiently high concentration of agonist is present

Answer 18

Competitive antagonist

Question 19

____ _____ cannot be overcome even in the presence of extremely high agonist levels, sometimes considered insurmountable antagonist. Has no effect on the ED50

Answer 19

Non competitive antagonist

Question 20

_____ agonist, not able to produce the full effect as a full agonist.

Answer 20

Partial

In this picture, both drugs have identical potencies, meaning they reached half-maximal effect observed at identical doses

Question 21

Fentanyl is a ____ agonist, ibuprofen is a _____ agonist. Fentanyl is more _____.

Answer 21

Full
Partial
Efficacious

Question 22

Difference in drug efficacy will have different levels of _____ on a graph. Different drug potencies will effectually reach the same effect levels but at different ____ levels

Answer 22

Effect
Dose

Question 23

Answer 23

Fentanyl and buprenorphine are equally potent. Fentanyl and morphine are more efficacious than buprenorphine

Question 24

____ ____ ____ model replaced the lock and key model

Answer 24

Induced fit binding
(Conformational selection binding model)

Question 25

The ___ ____ model is the idea that the drug receptor can switch back and forth between the active and inactive state

Answer 25

Two State

Question 26

____ ____ ___ is how much activity does the receptor have in the absence of ligand

Answer 26

Constitutive Receptor Activation

Question 27

_____ receptor activity reduces the response in a system (inverse agonist). _____ receptor activity increases the level of response in a system (agonist). _____ receptor activity, the response remains the same (antagonist).

Answer 27

Diminished Enhanced Constitutive

Question 28

An agonist has a higher ___to bind to the active site in a receptor and shifts towards higher level of activity. An _____ agonist has a higher affinity to the inactive site of a receptor and diminishes the level of activity. A ____ has the same affinity for both the active and inactive sites on the receptor and has no effect of the levels of activity.

Answer 28

Affinity Inverse agonist Antagonist

Question 29

____ is the degree to which a drug binds to ONE receptor. Dopamine can interact with three different types of receptors.

Answer 29

Selectivity Dopamine is more selective for DA1

Question 30

______ dose response curve, when the dose of the drug is describe in terms of a percentage of the maximal response. _____ dose response is when a drug is described in terms of the cumulative percent of subject who exhibit an effect

Answer 30

Graded Quantal

Question 31

The range between the ED50 and LD50 (lethal dose) is the ____ ____

Answer 31

Therapeutic index

Question 32

Activation of cell surface receptor is associated with Intracellular production of ____ ____. This is the concept of signal transduction

Answer 32

Second messengers

Question 33

Second messengers can result in massive ____ of signaling

Answer 33

Amplification

Question 34

The largest class of receptors are ____ . They bind endogenous and therapeutic molecules

Answer 34

G protein

Question 35

Some important second messenger molecules include:

Answer 35

Ca++, cAMP, IP3, DAG, acetylcholine, nicotine, varenicline

Question 36

Receptor protein _____ ____ and _____ receptors are able to initiate a phosphorylation cascade. This is an example of a signal transduction pathway.

Answer 36

Tyrosine kinases Cytokine