Pharmacology-Owen For Test 1

Front 1

Macromolecules that mediate biochemical and physiologic change in an organism (upon binding to a drug)

Back 1

Receptor

Front 2

Chemical compound that may be used on or administered to humans or animals as an aid in the diagnosis, treatment, or prevention of disease or other abnormal condition, for the relief of pain or suffering, or to control or improve any physiological or pathological condition

Back 2

Drugs

Front 3

Any substance that bring about a change in biological function through its chemical actions

Back 3

Drug

Front 4

Molecules that interact with specific molecular components of an organism

Back 4

Drug

Front 5

Value which measures the attraction of a drug for a receptor

Back 5

Affinity constant

Front 6

Tendency of a drug to complex with a receptor

Back 6

Affinity

Front 7

The drug must have a molecular conformation which permits binding with a particular receptor surface

Back 7

Drug selectivity

Front 8

Refers to the amount of drug necessary to elicit a response

Back 8

Potency

Front 9

Often expressed as the dose of a drug required to achieve 50% of the desired therapeutic effect

Back 9

Potency

Front 10

Drug that binds to and activates receptors and in turn, produces a biologic response

Back 10

Agonist

Front 11

Drug that binds to receptors to inhibit a biological response.

Back 11

Antagonist

Front 12

In the presence of __________, you require an increased concentration of agonist to produce the same effect as the agonist alone.

Back 12

Antagonist

Front 13

Compound that binds to a separate site on the receptor from which normally binds agonists

Back 13

Allosteric Modulators

Front 14

separate site on the receptor from which normally binds agonists

Back 14

Allosteric site

Front 15

Occupation of _______site can either increase or decrease the response to natural agonist, depending on whether it is a positive or negative modulator.

Back 15

Allosteric site

Front 16

Tendency of a drug to complex with a receptor

Back 16

Affinity

Front 17

What are the 4 major receptor families?

Back 17

1. ligand gated ion channels (eg. cholinergic nicotinic receptors)
2. G-protein coupled receptors (e.g.,alpha and beta adrenoreceptors)
3. enzyme linked receptors (e.g., Insulin receptor)
4. intracellular receptors (e.g., steroid receptors)

Front 18

What are the 5 types of chemical interactions involved in drug-receptor binding and which has the strongest bond strength?

Back 18

Covalent (strongest)
Ionic
Hydrogen
Hydophobic
van der Waals (weakest)

Front 19

Binds to receptor and activates it, like a key fits into a lock and turns it

Back 19

Agonist

Front 20

Activation of a receptor by this initiates conformational change in the receptor and activates one or more downstream signaling pathways

Back 20

Agonist

Front 21

These can fit the lock but can't open it

Back 21

Antagonists

Front 22

This inhibits activation by agonists

Back 22

Antagonists

Front 23

This curves shows and all-or-none response to a drug in a given population

Back 23

Quantal Dose Curve

Front 24

This curse shows a range of responses

Back 24

Graded Dose Curve

Front 25

Presence of ______ shifts the agonist concentration-effect curve to th left of the Kd for binding of agonist to receptor, and the degree of shift is proportional to the proportion of these

Back 25

spare receptors

Front 26

_____makes a tissue more sensitive to an agonist without changing its affinity for the receptor

Back 26

Spare receptors

Front 27

Ability of the agonist to cause the receptor to assume and active conformation

Back 27

Efficacy

Front 28

K3

Back 28

Efficacy

Front 29

Measure of drug safety

Back 29

Therapeutic Index

Front 30

LD50/ED50

Back 30

Therapeutic Index

Front 31

More realistic estimate of drug safety LD?/ED?

Back 31

LD1/ED99

Front 32

What does TD50/ED50 mean?

Back 32

Toxic dose in 50%/Effective dose in 50%

Front 33

What is the protective index?

Back 33

ED50(undesirable effect)/ED50 (desirable effect)

Front 34

Time before the therapeutic effect becomes the unwanted adverse effect

Back 34

Therapeutic Window

Front 35

Competes with agonist for the same binding site on a given receptor.

Back 35

Competitive antagonist

Front 36

This type of antagonist makes the agonist look less potent by shifting the dose-response curve to the ______. (left OR right?)

Back 36

Right

Front 37

Binds irreversibly to a different site than the agonist

Back 37

Noncompetitive antagonist

Front 38

This type of antagonist reduces the max response that an agonist can produce

Back 38

Noncompetitive antagonist

Front 39

Decreased ability of a receptor to respond to stimulation by a drug or ligand

Back 39

Desensitization

Front 40

Decreased response of a single class or receptor

Back 40

Homologous desensitization

Front 41

Decreased response of multiple classes of receptor

Back 41

Heterologous desensitization

Front 42

After chronic exposure of an agonist to a receptor ___________-regulation of the receptor occurs

Back 42

Down

Front 43

After chronic exposure of an agonist, this occurs, resulting in a decreased # of receptors present

Back 43

Down-regulation

Front 44

After chronic exposure of an antagonist to a receptor ___________-regulation of the receptor occurs

Back 44

Up-regulation

Front 45

After chronic exposure of an antagonist, this occurs, resulting in as increased # of receptors present

Back 45

Up-regulation

Front 46

List 2 classes of mechanisms which can confer selectivity of drug action

Back 46

1. Cell type specificity of receptor subtypes
2. Cell type specificity of receptor-effector coupling