Test 1

Question 1

Receptor

Answer 1

A protein or other substance that binds to an endogenous chemical or drug. They are sensitive, selective, and specific.

Question 2

Signal transduction

Answer 2

A process by which a cell converts one kind of signal or stimulus into another.

Question 3

Competitive antagonist

Answer 3

Has a weak affinity for the same receptor protein and may be displaced by an agonist.

Question 4

Non-competitive antagonist

Answer 4

has a strong affinity for the receptor protein and cannot be displaced by an agonist.

Question 5

Physiologic antagonism

Answer 5

Two agonist drugs that bind to different receptors. They bind to specific unrelated receptor proteins and elicit individual tissue responses. Responses generate opposing forces.

Question 6

Chemical antagonism

Answer 6

When a drug action is blocked and no receptor is activated.

Question 7

Down-regulation

Answer 7

Continued stimulation of cells with agonists generally results in a state of desensitization.

Question 8

Pharmacokinetics

Answer 8

Quantitative state of absorption, metabolism, distribution, and excretion of injected and inhaled drugs.
“What the body does to the drug”

Question 9

Pharmacodynamics

Answer 9

Quantitative study of the body’s response to a drug.

“What the drug does to the body”.

Question 10

Efficacy

Answer 10

Is a measure of the intrinsic ability of a drug to produce a given physiologic or clinical effect.

Question 11

ED50

Answer 11

The dose of drug required to produce a specific desired effect in 50% of individuals receiving the drug

Question 12

LD50

Answer 12

The dose of drug required to produce death in 50% of patients.

Question 13

Therapeutic index

Answer 13

the ratio between LD50 and ED50. the larger the therapeutic range, the safer the drug.

Question 14

Stereochemistry

Answer 14

Study of how molecules are structured in three-dimension.

Question 15

Chiral

Answer 15

A molecule that has a center (or centers) of 3D asymmetry

Question 16

Enantiomers

Answer 16

A pair of molecules existing in two forms that are mirror images of each other but cannot be superimposed.

Question 17

Clearance (Cl)

Answer 17

Clearance (Cl)= k (rate constante) X V (Volume of distribution)

Question 18

Central compartment

Answer 18

Elements of the body that dilute the drug within the first minute after injection:

1) venous blood volume of the arm
2) the volume of great vessels, the heart, the lungs, and upper aorta
3) whatever uptake of drugs occurs in the first passage through the lungs.

Question 19

Vessel rich group

Answer 19

Tissues that received the bulk of arterial blood flow: the brain, heart, lungs, kidneys, and liver

Question 20

Intrinsic clearance

Answer 20

The ability of the liver to remove a drug from the blood in the absence of any limitation imposed by blood flow or drug binding

Question 21

First-order kinetics

Answer 21

A constant fraction of the drug is removed during a finite period of time regardless of the drug amount or concentration.

Question 22

Half-lives

Answer 22

The time required for the concentration to change by a factor of 2.

Question 23

Elimination clearance

Answer 23

Theoretical volume of blood from which the drug is completely and irreversibly removed in a unit of time.

Question 24

Elimination half-time

Answer 24

The time during which the amount of drug in the body decreases by 50%

Question 25

Two compartment model

Answer 25

1) Rapid decrease in concentration (due to passage of drug from plasma to tissue) 2) Drug distribution within the central compartment is instantaneous.

Question 26

Minimum effective concentration (MEC)

Answer 26

The minimum concentration of drug plasma required to produce the therapeutic effect

Question 27

Minimum toxic concentration (MTC)

Answer 27

Minimum concentration in which toxicity usually occurs

Question 28

pKa

Answer 28

A pH in which a drug is 50% ionized

Question 29

Zero-order kinetics

Answer 29

A constant amount of drug is eliminated per unit time

Question 30

Volume of distribution

Answer 30

Amount of drug administered/initial drug plasma concentration

Question 31

Partial agonist

Answer 31

A drug that is NOT capable of producing the maximal effect even at a very high concentration

Question 32

Potency

Answer 32

The dose required to produce a given effect

Question 33

Content-sensitive half time

Answer 33

The time required by the drug concentration of the plasma to decrease by 50%

Question 34

Steady state

Answer 34

A stable plasma concentration of a drug is achieved

Question 35

Pharmacogenetics

Answer 35

Study of variations in human genes that are responsible for different responses to drug therapy

Question 36

Polymorphism

Answer 36

Variations in the DNA sequence that occur at 1% of the population

Question 37

Types of receptors

Answer 37

1) Ion channel-gated receptors * Ligand-gated receptors * Voltage-gated receptors 2) G-protein coupled receptors (GPCRs) 3) Intrinsic enzyme-linked receptors * Tyrosine kinase 4) Intracellular receptors

Question 38

Alpha 1 receptors

Answer 38

Increases IP3 + DAG via activation of phospholipase. Found: POST-SYNAPTIC in peripheral tissues (vascular smooth muscle, glands) *Causes increased systemic arterial BP, mydriasis, hyperglycemia, bronchoconstriction, GI relaxation

Question 39

Alpha 2 Receptors

Answer 39

Inhibits adenylyl cyclase, thus decreasing cAMP. Found: PRE-SYNAPTIC nerve terminals of sympathetic postganglionic neurons POST-SYNAPTIC membranes in the brainstem and peripheral tissues *Causes inhibition of NE synthesis and release (presynaptic), sedation, analgesia, decreased insulin secretion