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PHRM824 > EXAM2 > Flashcards

EXAM2 Flashcards

1
Q

Science of interactions of chemical compounds with biological systems

A

Pharmacology

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2
Q

The study of the biochemical and physiological effects of drugs and the mechanisms of their actions, including the correlation of their actions and effects with their chemical structure

A

Pharmacodynamics

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3
Q

The study of the absorption, distribution, biotransformation, and elimination of xenobiotics

A

Pharmacokinetics

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4
Q

Which of the following statements are true:
Pharmacodynamics are a subset of pharmacokinetics
OR
Pharmacokinetics are a subset of pharmacodynamics?

A

FIRST: Pharmacodynamics are a subset of pharmacokinetics

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5
Q

What is the “cornerstone of pharmacology” that explains how the organism interacts with a drug and initiates a chain of biochemical events which results in observed effects?

A

drug receptor

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6
Q

Drug whose interaction with the receptor stimulates a biological response

A

agonist

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7
Q

Orthosteric or Allosteric:
agonist, antagonist, partial agonist, and inverse agonists

A

Orthosteric

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8
Q

Orthosteric or Allosteric:
Site where the native ligand binds

A

Orthosteric

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9
Q

PAM is an allosteric _____, while NAME is an allosteric _____

A

activator, inhibitor

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10
Q

What are the receptor and drug reactions to full, partial, antagonist, and inverse agonist?

A

Full: R active, D active
Partial: R active, D partial
Antagonist: R both, D both
Inverse agonist: R inactive, D inactive

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11
Q

Orthosteric or Allosteric:
Positive (PAM) and Negative (NAM)

A

Allosteric

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12
Q

What happens when a drug binds to SERT?

A

Blocking leads to more serotonin in the synapse (SSRIs)

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13
Q

What happens to serotonin with an MAOI?

A

Increased serotonin

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14
Q

How many serotonin receptors in the body?

A

14

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15
Q

What inhibitor breaks down serotonin in the synapse, where in its absence serotonin increases?

A

MAO

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16
Q

Why is Buprenorphine affective for drug addiction?

A

Stays on drug’s receptor longer, decreasing effect of drug from binding sites

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17
Q

True or False: Drugs only modify cellular function

A

TRUE

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18
Q

True or False: Drugs have a single effect

A

FALSE

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19
Q

Which site of drug action is used for the following:
-Neutralization of gastric acid by antacids
-cholestyramine resin being used to reduce cholesterol absorption

A

Extracellular

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20
Q

Which site of drug action is used for the following:
-Drugs used to treat infections
-Drugs used for cancer chemotherapy
-Hormones such as estrogen

A

Intracellular site

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21
Q

Which site of drug action is used for the following:
Many drugs:
-Acetylcholine and muscarinic or nicotinic receptors
-Catecholamines and alpha and beta receptors
-Growth factors (EGF/FGF) and GF receptors

A

Surface of the cell

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22
Q

Most receptors are ______

A

Proteins

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23
Q

Receptors determine the quantitative relationship between ____ or concentration of drug and pharmacologic _____

A

Receptors determine the quantitative relationship between dose or concentration of drug and pharmacologic effects

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24
Q

Receptors are responsible for _______ of drug action

A

selectivity

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25
Q

Drugs that bind to a receptor and stimulate a biological response

A

agonists

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26
Q

Drugs that bind to a receptor without altering receptor function

A

antagonists

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27
Q

_____ is one of the determinants of potency

A

Affinity

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28
Q

relationship between affinity and potency

A

direct

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29
Q

The ability of the drug to interact with the receptor

A

affinity

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30
Q

The way affinity is measured

A

KD

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31
Q

Assessing signaling event associated with receptor activity

A

Functional assay

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32
Q

As doses increase, the incremental response ______

A

decreases

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33
Q

Which part of the concentration response curve measures efficacy?

A

Max Response

34
Q

If EC50=20nM, what are the concentrations of EC90? EC10?

A

EC90= 200 nM
EC10= 2 nM

35
Q

What are the log values of EC10 and EC90 if EC50=10^-10?

A

EC10= 10^-11
EC90= 10^-9

36
Q

What are the ways affinity is measured?

A

Ki and KD

37
Q

Equation for Law of Mass Action and their receptor availability

A

[D][R]/[DR] or k(off)/k(on) =KD

38
Q

What value determines association rate? What does it measure?

A

Ka- how fast a drug jumps onto receptor [k(on) [D][R] ]

39
Q

What value determines dissociation rate? What does it measure?

A

Kd- how fast drug jumps off receptor [k(off) [DR] ]

40
Q

Coming off a receptor slowly on a graph shows (higher/lower) affinity

A

higher

41
Q

At what value of [D] is unoccupied [R]=occupied [DR]?

A

When D occupies half of the receptors

42
Q

In the Law of Mass Action, binding is (reversible/irreversible), [D] and [R] are either ____ or ____, and receptor sites have (value) affinity and are (dependent/independent)

A

Binding is reversible, [D] and [R] are either free or bound, and receptor sites have equal affinity and are independent

43
Q

How can KD be measured from Bmax?

A

Half of Bmax is KD

44
Q

What is the measure for number of receptors in a system?

A

Bmax

45
Q

How to find the Bmax given a saturation binding assay?

A

Total-Non Specific= Specific

46
Q

How test (radioactive) ligand/drugs compete for same sight as labeled ligand

A

Heterologous competition assays

47
Q

Can you find KD with IC50?

A

Yes: Cheng-Prusoff equation

48
Q

What is the Cheng-Prusoff equation? (NEED TO MEMORIZE)!!

A

Ki=IC50/[1+L/KD]

49
Q

What parameter is NOT required to calculate Ki from a drug/binding curve?
A. KD of radioligand
B. Bmax value
C. IC50 value of test compound
D. Concentration of radioligand [L]

A

B. Bmax
Reason: not in Cheng-Prusoff equation

50
Q

What is the correlation on a drug/concentration plot between affinity and IC50 value?

A

Inverse: High affinity=low IC50 value

51
Q

How do we find the most DOR/MOR/KOR selectivity? Least selective?

A

Most: highest selectivity ratio
Least: least/closest selectivity ratio

52
Q

Which of the following is NOT true?
A. Pharmacology is the science of interactions of chemical compounds with biological systems
B. The drug receptor is the cornerstone of pharmacology
C. Drugs are defined by action (e.g. agonist or antagonist)
D. Antibodies are in increasing use as drugs
E. Pharmacodynamics is the study of the absorption, distribution, biotransformation, and elimination or xenobiotics

A

E. Pharmacokinetics definition!

53
Q

Which of the following is NOT true?
A. Most drugs have a single effect
B. Agonist and antagonists have overlapping binding sites
C. Allosteric modulators can have both positive and negative effects on agonists

A

A.

54
Q

Which of the following statements regarding Bmax is not true?
A. Bmax is an estimated of number of receptors in a given tissue
B. Bmax values are determined through saturation binding studies
C. Bmax values are not regulated by drug treatment
D. Bmax values are independent of the ligand
E. Bmax can influence downstream signaling events

A

C. Bmax values are not regulated by drug treatment

55
Q

Partial agonist are also ____ ______

A

partial antagonist

56
Q

Causes response that is greater than the endogenous ligand

A

super agonist

57
Q

On the ligand spectrum, drives response in opposite direction

A

partial inverse agonist

58
Q

The dose of a drug required to produce a particular effect of given intensity

A

potency

59
Q

On a graph, where is the most potency? The most efficacy?

A

Most potency is furthest left, most efficacious is highest

60
Q

On a graph, where is the most potency? The most efficacy?

A

Most potency is furthest left, most efficacious is highest

61
Q

The biological response resulting from the drug-receptor interaction

A

efficacy

62
Q

A strong agonist has (low/high) affinity and (low/high) efficacy

A

high affinity and high efficacy

63
Q

Which drug property is more important: efficacy or potency?

A

Efficacy

64
Q

Identify constitutive and endogenous activity

A

Constitutive: absent
Endogenous: absent

65
Q

Identify constitutive and endogenous activity

A

Constitutive: present
Endogenous: absent

66
Q

Identify constitutive and endogenous activity

A

Constitutive: absent
Endogenous: present

67
Q

Identify constitutive and endogenous activity

A

Constitutive: present
Endogenous: present

68
Q

What are the three types of receptor antagonism?

A

Competitive, non-competitive, and irreversible

69
Q

Reversible or equilibrium antagonism by increasing the dose of agonist

A

competitive antagonism

70
Q

Competitive antagonist has _____ but lacks _____

A

has affinity, lacks efficacy

71
Q

Plot determining affinity of agonist to a receptor through functional analysis of competitive antagonist

A

Schild Plot

72
Q

Which assay shows specific binding %

A

receptor-binding assay

73
Q

Which assay shows maximal release %?

A

Functional assay

74
Q

Type of antagonist that cannot be completely reversed by increasing the concentration of agonist; produces its effect at a site of the receptor other than the site used by the agonist

A

Noncompetitive Antagonist

75
Q

Increasing antagonist concentrations ____ the KD and ________ Emax of the agonist

A

increase, decrease

76
Q

What happens to the curve of a competitive antagonist vs an irreversible antagonist

A

non-competitive shifts down on graph

77
Q

Spare receptors result in EC50 being (equal, less, or greater) than KD?

A

EC50<KD

78
Q

When two drugs influence a physiological system but in opposite directions.

A

Functional (physiological) antagonism

79
Q

Which of the following is NOT true regarding spare receptors?
A. It is system/tissue dependent
B. Allow a noncompetitive antagonist to look like a competitive antagonist
C. Spare receptors are independent of effector numbers
D. May differ between signaling pathways with the same receptor

A

C. Spare receptors are independent of effector numbers

80
Q

Which of the following is NOT true regarding antagonists?
A. Irreversible and allosteric antagonists have similar effects on the dose response curves of agonists
B. In the absence of space receptors, a noncompetitive antagonist increases the Emax
C. Irreversible antagonists typically bind the Orthosteric site
D. Antagonist affinity can be estimated using a Schild plot

A

B. In the absence of space receptors, a noncompetitive antagonist increases the Emax

81
Q

Chemical reaction occurring between an agonist and an antagonist to form an inactive product

A

chemical antagonism

PHRM824 (6 decks)

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