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Pharmacology (2014-2018) > Principles of pharmacodynamics > Flashcards

Principles of pharmacodynamics Flashcards

1
Q

True about drug-receptor interactions

A. With the ligand, the receptor is always active
B. Without the ligand, the receptor is always inactive
C. The receptor only produces its effect when activated by the agonist
D. Constitutive action is by unbound receptor in active conformation

A

C

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2
Q

The binding of acetylcholine to its nicotinic receptor leads to

A. Hyperpolarization
B. Exit of Cl- ions
C. Failure of generation of action potential
D. Depolarization

A

D

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3
Q

Which of the following receptors is expected to have the quickest biologic response after the ligand has bound to the binding site?

A. Ion channel
B. GPCR
C. Cytoplasmic/intracellular receptor
D. Enzyme-linked

A

A

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4
Q

Glucagon acts through what receptor?

A. Ionophore
B. G-protein coupled
C. Tyrosine kinase
D. Cytoplasmic/intracellular

A

B

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5
Q

Anesthetics like tubocurarine induce skeletal muscle relaxation by:

A. Induce entry of Na+
B. Inhibit entry of Na+
C. Induce exit of Na+
D. Inhibit exit of Na+

A

B

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6
Q

Allosteric activators produce an action that may be described as:

A. Greater than agonist alone
B. Equal to agonist
C. Less than agonist alone
D. Opposite to agonist

A

A

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7
Q

Tamoxifen is a partial estrogen agonist. As a partial agonist, it

A. Produces the same effects as estrogen on all tissues in high doses
B. Antagonizes estrogen in breast tissue and agonizes estrogen effect on bones
C. Agonizes estrogen effects but antagonizes estrogen effects at higher levels/doses
D. Induces conformational change in estrogen to inactivate it

A

B

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8
Q

The mode of action of this drug is mediated by G-protein coupled receptor

A. The hormone insulin
B. The glucocorticoid prednisone
C. Salbutamol
D. Diazepam

A

C

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9
Q

Which of the following drugs has a non-receptor mediated mechanism of action?

A. Epinephrine
B. Mannitol
C. Ipatropium (anti-adrenergic)
D. Carbamezapine

A

B

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10
Q

Which of the following is the expected outcome when receptors are continuously and chronically exposed to agonists?

A. Up-regulation of receptors
B. Formation of B-arrestin
C. Down-regulation of receptors
D. Increased sensitivity to agonist action leading to greater biologic effect

A

C

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11
Q

The binding of diazepam to its receptor causes the following events

A. Separation of Gs alpha protein from G-beta and G-gamma protein subunits
B. Autophosphorylation of the beta-subunit of the receptor
C. Direct opening of the ionophore channel causing exit of sodium
D. Conformotional change of GABA receptor causing improved GABA binding and action

A

D

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12
Q

The binding of a ligand or drug on the cytoplasmic/nuclear receptor lead to biologic effects that are

A. Expected within seconds to minutes
B. Terminated once drug concentration becomes low or zero
C. Delayed but once these manifest, are also short-lived
D. Persistent for hours or days even when the drug has been eliminated from the body

A

D

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13
Q

What type of receptor is used by EGF and other growth factors?

A. Enzyme linked
B. G-coupled protein
C. Ligand-gated ion channel
D. Intracellular/nuclear receptor

A

A

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14
Q

The effector molecules of a G-coupled receptor like the muscarinic receptor is

A. Adenylyl cyclase
B. Phospholipase C
C. Tyrosine kinase
D. Chloride channel

A

A

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15
Q

Receptors have these characteristics except

A. Are responsible for the selectivity of drug action
B. Can create new functions by its binding to ligands
C. Can mediate the actions of the pharmacologic agonists and antagonists
D. Are generally macromolecular molecules which possess stereospecificity
E. Can largely determine the quantitative relationship between drug dose or concentration and pharmacologic effects

A

B

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16
Q

Drug-receptor interactions are subject to the following

A. Downregulation such as desensitization
B. Upregulation such as hyperactivity
C. No regulation
D. A and B only
E. AOTA
A

D

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17
Q

The 3 most important characteristics of a drug

A. Potency, safety, equality
B. Efficacy, safety, quality
C. Efficacy, safety, affordability
D. Potency, efficacy, quality

E. Efficacy, safety, accessibility

A

B

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18
Q

What are the indices in the graded dose response curve?

A. Efficacy, potency, slope, variation
B. Frequency of individual response
C. Maximum effect, location of the curve on the horizontal axis
D. A and B
E. A and C
A

E

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19
Q

The best dose response curve (where it is easiest to analyze mathematically) can be signified

A. Sigmoid curve
B. Standing curve
C. Reclining curve
D. Gaussian curve
E. Hyperbolic curve
A

A

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20
Q

Antagonism

A. Is characterized by affinity to a receptor but no intrinsic activity
B. Can be classified into competitive or irreversible and non-competitive or reversible
C. Can be classified into competitive or reversible and non-competitive or irreversible
D. A and C
E. B and C

A

D

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21
Q

The quantal dose-response curve

A. Has the shape of a Gaussian or normal curve
B. Is an all or none curve
C. Reflects the frequency of population response to drug dose
D. Reflects the variation of population response to drug dose
E. AOTA

A

E

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22
Q

Patient with asthma presents with bronchoconstriction. Which drug casues delayed but prolonged bronchodilation?

A. Glucocorticoid through GCPR
B. b-adrenergic through GCPR
C. Glucocorticoid through enzyme-linked receptor
D. Glucocorticoid inside cytoplasmic/nuclear receptor

A

D

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23
Q

The action of mannitol of decreasing intracranial pressure is mediated by this type of receptor:

    A. Ionotropic
    B. Metabotropic
    C. GPCK
    D. NOTA
A

D

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24
Q

Use of an allosteric activatior with another drug will result in:

    A. Decreased efficacy of drug
    B. Increased efficacy of drug
    C. Decreased potency of drug
    D. Increased potency of drug
A

B

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25
Q

When acetylcholine binds to nicotine receptors:

   A. Open Na+ channels
   B. Generate CAMP
   C. Gene expression
   D. Activate tyrosine kinase
A

A

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26
Q

Glucocorticoid hydrocotisone binds to the following receptor:

    A. Ionotropic
    B. GPCR
    C. Tyrosine kinase
    D. Cytoplasmic/nuclear receptor
A

C

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27
Q

Benzodiazepine, after binding to its target receptor, causes what changes?

     A. Separation of the Gsa subunit from Gb and Gγ protein subunits
     B. Autophosphorylation of the beta subunit of the receptor
     C. Direct opening of ionophore channel causing exit of sodium
     D. Conformational change of GABA receptor causing improved GABA binding
A

D

28
Q

The ff. contribute to the development of desensitization/tachyphylaxis:

    A. Endocytosis of receptors
    B. Phosphorylation
    C. Compensation
    D. Exocytosis of receptors
A

A

29
Q

While receptors regulate biochemical and physiological activity, they are also subject to regulatory mechanisms, such as:

   A. Upregulation due to synthesis of new receptors
   B. Upregulation due to continued stimulation
   C. Downregulation due to covalent bonding and destruction of receptors.
   D. A & C
   E. AOTA
A

D

30
Q

Potency is:

    A. Effectiveness of drug relative to dose
    B. Importance is considered where ease of administration ends
    C. Sigmoid on the horizontal axis
    D. B and C
    E. All of the above
A

E

31
Q

Anesthetics that work similarly with tubocurarine induce skeletal muscle relaxation through the following

A. Inhibit exit of Na through NaCh receptor
B. Allow exit
C. Inhibiting the entry of sodium across the cell membranes of the nicotinic acetylcholine receptor
D. Allow exit

A

C

32
Q

What effect does an allosteric activator exert on a drug?

A. Decrease the efficacy of a drug
B. Increase in the efficacy of the drug
C. Effect depends on the drug
D. None of the above

A

B

33
Q

Binding of acetylcholine its receptors triggers this cellular event:

A. The opening of sodium channels
B. Chloride ion enters cell
C. Hyperpolarization of the membrane
D. G-protein is activated

A

A/D

34
Q

What type of receptors does the mineralocoticod aldosterone bind to?

A. Ion channel
B. GPCR
C. Tyrosine kinase linked
D. Cytoplasmic/nuclear

A

D

35
Q

The following are proposed mechanisms for the development of tolerance and desensitization, except:

A. Endocytosis of receptors
B. Phosphorylation of G protein-coupled receptors
C. Changes in components of response distal to the receptor
D. Exocytosis of the receptor-vesicle complex

A

D

36
Q

Receptors which regulate biochemical and physiological functions are in themselves subject to regulatory homeostatic control, which come in the form of:

A. Upregulation
B. Downregulation or desensitization
C. Both

A

C

37
Q

The semilogarithmic graded dose response curve has the following characteristics:

A. It is a sigmoid curve
B. It consists of 4 parameters: slope, potency, variability, maximal effect
C. The magnitude of the response decreases with greater concentration of the unbound drug at the receptor site
D. A & B only

A

D

38
Q

Nicotinic subunit receptor responsible for gate opening upon Ach binding

A. Alpha
B. Beta
C. Gamma
D. Delta

A

A

39
Q

Compared to the sigmoid curve of a full agonist in the log dose vs. response curve, the curve in the presence of a partial agonist:

A. will shift to the right
B. will shift to the left
C. Emax will be higher
D. Emax will be lower

A

D

The partial agonist has lower Emax than the full

agonist. “The partial agonist produces a lower response at

full receptor occupancy. The partial agonist’s inability to

produce maximal effect, even when present at high

concentrations that saturate binding to all receptors, is not

due to decreased affinity for binding to receptors but

indicated by the fact that partial agonist competitively inhibits

the responses produced by full agonists.” (Basic and Clinical

Pharmacology 11th ed. By Katzung, page 19)

40
Q

Compared to the sigmoid curve of a full agonist in the log dose vs. response curve, the curve in the presence of a competitive antagonist:

A. will shift to the right
B. will shift to the left
C. Emax will be higher
D. Emax will be lower

A

A

Reversible competitive antagonism shifts the

dose response curve to the right, causing the drug to behave

as if it were less pontent.

41
Q

Compared to the sigmoid curve of a full agonist in the log dose vs. response curve, the curve in the presence of a noncompetitive antagonist:

A. will shift to the right
B. will shift to the left
C. Emax will be higher
D. Emax will be lower

A

D

Irreversible noncompetitive antagonism

decreases maximal response.

42
Q

Agonist binding has both affinity and efficacy, antagonist binding also has both affinity and efficacy.

A. True
B. False

A

B

43
Q

The presence of spare receptors will allow an agonist to achieve full efficacy even in the presence of non-competitive agonists. T/F

A

T

44
Q

The most important concept in pharmacodynamics is the

A. Therapeutic triangle
B. Scatchard plot
C. semi-log dose response curve
D. presence of agonist/antagonist
E. All of the above
A

C

45
Q

The Scatchard plot

A. Is a graphic representation used in the analysis of binding phenomena in which concentration of bound ligand divided by that of the free ligand bound ligand is plotted against concentration of bound ligand

B. Is a straight line plot for one binding site (may also represent several binding sites) where the x axis intercept is B (bound drug) and the slope is -1/Kd (negative reciprocal of the dissociation/association constant)

C. Defines an equation for calculating the affinity constant of a ligand with a protein or receptor

D. Is a curve of B/F (bound ligand/free ligand) versus B (bound ligand)

E. All of the above

A

E

46
Q

The three most important properties of a drug product are

A. efficacy, safety, quality
B. efficacy, lack of significant toxicity and quality
C. potency, safety and quality
D. a and b
E. a and c
A

D

47
Q

What are “orphan” receptors?

A

Receptor with presently unknown ligands

48
Q

What are “spare” receptors?

A

Receptors are said to be “spare” for a given pharmacologic response if it is possible to elicit a maximal biologic response at a concentration of agonist that does not result in occupancy of the full complement of available receptors.

49
Q

What are the two types of antagonists?

A

Reversible competitive antagonist and irreversible competitive antagonist

50
Q

The binding of GABA to its receptor leads to this effect

A. Opening of voltage gated sodium channel

B. Hyperpolarization of plasma membrane

C. Generation of action potential

D. Release of calcium from ER and mitochondria

A

B

51
Q

Chloride enters the cell through channel

B. ATP is converted to cAMP

C. Expression of genes for transcription of actin and myosin

D. Activation of Tyrosine kinase

A

B

52
Q

Binding of an agonist to the GABA receptor (e.g. gabapentin used in seizures) will result into the

cellular response:

A. Opening of sodium channels

B. Hyperpolarization of the cell membrane

C. Generation of a membrane potential

D. Release of intracellular calcium

A

B

53
Q

Binding of beta blockers (eg. Propanolol) to beta receptors

A. Bronchodilation

B. Bronchoconstriction

C. Tachycardia

D. Positive ionotropic response

A

B

54
Q
  1. Inhibition of estrogen binding to cytosolic receptor is an intervention to achieve this therapeutic goal:

A. Inhibition of cellular division

B. Facilitiation of glucose transport across membrane

C. Triggering of selective gene expression

D. Pleiotropic response

A

A

55
Q

The action of this drug is mediated by intracellular nuclear receptors

A. insulin

B. estrogen

C. mannitol

D. salbutamol

A

B

56
Q

Which is TRUE of Drug Action?

A. All drug molecules exert a chemical influence on

cells initially through receptors.

B. Specificity of drug receptor interaction is reciprocal.

C. Occupation of receptor always transforms the

receptor t to an active conformational state.

D. Drug is effective if it affects the most number of

tissues and cells as possible.

A

B

57
Q

Which receptor modulates the allergic receptor

A. Beta adrenergic receptor

B. Histamine-1 receptor

C. Opiate receptor
D. Angiotensin converting enzyme converting

receptor

A

B

58
Q

G-protein coupled receptors are the most

common receptor acted on by drugs?

A. True

B. False

A

A

59
Q

13.Covalent bonds are usually irreversible.

A. True

B. False

A

A

60
Q

The log-dose effect relationship shows:

a. a hyperbolic curve
b. a sigmoid curve
c. the four characteristics – potency, efficacy, slope

and variability

d. a and c
e. b and c

A

E

61
Q

Classes of drugs are best described according to:

a. source whether natural or synthetic
b. chemical structure
c. therapeutic use and therapeutic effect
d. all of the above
e. b and c

A

C

62
Q

Margin of safety is measured by

a. Therapeutic indexwhich is the ration of toxic dose

50 over effectivedose 50

b. Standard safety margin utilizing 100 experimental

animals

c. Standard safety margin utilizing 1000 experimental

animals

d. Distance between the minimum effective dose and

the maximum effective dose which is just ahairline

away from the minimum toxic dose

E. ALL OF THE ABOVE

A

A

63
Q

For Epinephrine to achieve ionotropic and

chronotropic effects, it must react with which type of

receptors?

A. Ion channel-linked receptors

B. GPCR

C. Cytosolic receptor

D. Enzyme-linked receptors

A

B

64
Q

Binding of Salbutamol to beta-2 adrenergic

receptor triggers this intracellular event:

A. Chloride ion enters the cell

B. Conversion of ATP to cAMP

C. Increase membrane conductance to potassium

ions

D. Selective gene expression

A

B

65
Q

Binding of atropine to cholinergic receptor in

bronchial smooth muscles triggers the physiologic

response:

A. Sequestration of calcium by ER

B. Binding of cytosolic calcium to calmodulin

C. Myosin and actin interaction inhibited

D. GDP is replaced by GTP in the alpha-subunit of G

protein

A

C

66
Q

Binding of insulin to its membrane-bound receptor

leads to this cellular response

A. Facilitated diffusion of potassium across plasma

membrane

B. Phosphorylation of effector proteins

C. Signal transduction and amplification by generating

cAMP and Ca2+

D. Hyperpolarization of the plasma membrane

A

B

67
Q

Binding of estrogen to cytosolic receptor is the

target of antineoplasm intervention

A. Inhibit cellular division

B. Apoptosis

C. Necrosis

D. Inhibit pleomorphic activity

A

A

Pharmacology (2014-2018) (23 decks)

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