Basic Principles

Question 1

Action of the body on the drug

Answer 1

Pharmacokinetics

Question 2

Action of the drug on the body

Answer 2

Pharmacodynamics

Question 3

Physiologic mechanisms by which a drug produces its adverse effects

Answer 3

Pharmacotoxicology

Question 4

______________ provides the link between pharmacokinetics and pharmacodynamics and is the focus of the target concentration approach to rational dosing

Answer 4

Concentration

Question 5

The 3 primary processes of pharmacokinetics are _________, __________ and _________.

Answer 5

input

distribution

elimination

Question 6

Drugs that produce an effect similar to the natural effect of hormones, neurotransmitters, and other substances

Answer 6

Agonists

Question 7

Drugs that block the natural effects of hormones, neurotransmitters or other drugs

Answer 7

Antagonists

Question 8

What type of agonist:

Shift the majority of available receptors into action

Answer 8

Full agonist

Question 9

What type of agonist:

DO NOT evoke as great a response no matter how high the concentration

Answer 9

Partial agonist

Question 10

What type of agonist:

Drug will reduce any constitutive activity, thus resulting in effects that are the opposite of the effects produced by conventional agonists at that receptor

Answer 10

Inverse agonist

Question 11

(T/F) Sufficiently high concentrations of agonists can exceed the effect of a given antagonist

Answer 11

True

Question 12

Can an antagonist reduce constitutive activity?

Answer 12

No, will only bring receptor effects down to constitutive (basal) activity. Cannot decrease effects lower than this constitutive (basal) level.

Question 13

What is constitutive activity? Explain in depth to help with understanding.

Answer 13

Within a normal receptor pool, there are innactive forms of the receptor (Ri) and activated forms of the receptor (Ra). This means that there is some level of baseline receptor activity formed by the Ra receptors. This baseline level/effect is called constitutive, or basal, activity.

*antagonist cannot lower effects below this constitutive/basal activity level

Question 14

Progressively inhibits a response in the presence of a fixed concentration of Agonist

Answer 14

Competitive Antagonists

Question 15

Forms a covalent bond and the receptor is unavailable to bind with an agonist

Answer 15

Irreversible Antagonists

Question 16

A drug that creates an ionic bond with another drug

Answer 16

Chemical Antagonists

Question 17

Use of a drug to interrupt endogenous regulatory pathways mediated by different receptors

Answer 17

Physiologic Antagonists

Question 18

Inverse agonists have a much higher affinity for the R__ form of receptors

Answer 18

Ri (inactivated form)

Question 19

Conventional full agonist drugs have a much higher affinity for the R__ form of receptors

Answer 19

Ra (activated)

Question 20

Partial agonists have an __________ affinity for both Ra and Ri forms

Answer 20

intermediate

Question 21

(T/F) Conventional antagonist have an equal affinity to both Ra and Ri receptor forms

Answer 21

True

Question 22

(t/f) allosteric activators/inhibitors act at the same site on the receptor as the drug

Answer 22

False

Allosteric activators/inhibitors act a different site on the receptor

Question 23

Which drug-receptor bond is the weakest

Answer 23

Hydrophobic

Question 24

Most common drug-receptor bond

Answer 24

electrostatic

Question 25

Strogest drug-receptor bond. Often irreversible

Answer 25

Covalent

Question 26

A signal triggering molecule on a target protein

Answer 26

Ligand

Question 27

Mediate actions of endogenous chemical signals

Answer 27

Regulatory Proteins

Question 28

Inhibited or activated by binding to a drug

Answer 28

Enzymes

Question 29

Available receptors after the max effect of a drug is achieved

Answer 29

Spare receptors

Question 30

Measured by the concentration of drug that is needed for DR binding

Answer 30

Affinity

Question 31

The ability of the DR complex to activate ST (signal transduction)

Answer 31

Efficacy

Question 32

The measure of the magnitude/intensity of a BR produced by the EC100 relative to the maximal attainable response produced in a target tissue

Answer 32

Intrinsic activity

Question 33

Effective Concentration or Effective Dose required to produce 50% of that drug’s maximal response

Answer 33

EC50 or ED50