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PHARMACOLOGY > PHARMACODYNAMICS 2024 > Flashcards

PHARMACODYNAMICS 2024 Flashcards

1
Q
  • The cellular macromolecule or macromolecule
    complex with which the drug interacts to elicit a
    cellular response.
  • Selective
  • Modifiable
A

DRUG RECEPTOR/ DRUG TARGET

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2
Q

Molecules that translate the drug receptor

interaction into a change in cellular activity

A

EFFECTORS

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3
Q

Binding of ATENOLOL to Beta receptor

stimulates conversion of __

A

ATP to cAMP

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4
Q

Binding of AMLODIPINE to Calcium Channel.

A

ION CHANNELS

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5
Q

Binding of RAMIPRIL to its receptor inhibits ACE

Angiotensin Converting Enzyme

A

ENZYMES

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6
Q

Thiazides (Bendroflumethiazide) block NaCl

transporter at the_____

A

distal convoluted tubule

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7
Q

In partial agonist, the magnitude of biologic effect is directly related to the fraction of_________

A

Active state

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8
Q

In reversible equilibrium, it favors the _____

A

inactive

state.

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9
Q

The strength of the reversible interaction between
a drug and its receptor, as measured by the
dissociation constant

A

DRUG SPECIFICITY

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10
Q
  • Defined as the affinity of one for the other.
  • Both the affinity of a drug for its receptor and its
    intrinsic activity are determined by its chemical
    structure.
A

DISSOCIATION CONSTANT

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11
Q

A drug that interacts with a single type of receptor
that is expressed on only a limited number of
differentiated cells will exhibit_____

A

high specificity.

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12
Q

Once the drug binds to the receptor, it produces a
curve – Receptor Occupancy Theory or Dose
Response Curve and this curve is characterized
by

A

“Hyperbolic Curve”

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13
Q

Response emanates from a receptor occupied by

a drug

A

RECEPTOR OCCUPANCY THEORY

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14
Q

e maximal response that can

be produced by the drug.

A

Emax

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15
Q

the concentration that produces

50% of maximal effect.

A

EC50

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16
Q

refers to the “effect”

A

EC

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17
Q

refers to

“affinity” of the receptor binding.

A

Kd

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18
Q

is the total concentration of
receptor sites (ie, sites bound to the drug
at infinitely high concentrations of free
drug).

A

Bmax

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19
Q

(equilibrium dissociation constant)
represents the concentration of free drug
at which half-maximal binding is
observed.

A

Kd

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20
Q

If the

Kd is low, binding affinity is_____

A

high

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21
Q

If there are 100 receptors, the concentration of the

drug wherein 50% of the receptors are bound

A

Kd

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22
Q

If there are 100 receptors, the concentration

wherein 100% of these receptors are bound

A

Bmax

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23
Q

Refers to the concentration (EC50) or dose
(ED50) of a drug required to produce 50% of that
drug’s maximal effect

A

POTENCY

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24
Q

For this drug, potency is at 1μg, wherein 50% of
half maximal effect is seen. If you give a drug that
would increase the heart rate and the maximum
effect of the drug would be increasing the heart
rate by 50, at what dose wherein you would
appreciate a 25 increase in the heart rate? That is
your_____

A

ED50

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25
Q

In case potency, the lowest dose that produces half maximal effect would be the _____ potent

A

most

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26
Q

A magnitude of response a drug causes when it
interacts with a receptor.

  • Intrinsic Activity
A

MAXIMAL EFFICACY

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27
Q

The best determinant of which drug to choose

clinical effectiveness depends on_____

A

maximal efficacy

28
Q

This parameter reflects the limit of the doseresponse relation on the response axis.

A

maximal efficacy

29
Q

Among Potency and Maximal Efficacy, which is

more important in prescribing drugs?

A

Consider both, but for Clinical Effectiveness,
Maximal Efficacy is more important. When you
prescribe a drug, we are not only after the dosage,
but we’re after the effect of the drug

30
Q

If you are comparing 2 drugs, for example, ARB
and Irbesartan (HPN drugs); They are both
efficacious, but which among the 2 is more potent
based on the dosage, then ____

A

Potency

31
Q

If you are comparing drugs with different
mechanisms and you want to choose which is
better, then

A

EFFICACY

32
Q

In determining the drug of choice what will you

consider is it the potency or efficacy?

A

Efficacy

33
Q

In Potency, you look for the

A

ED50

34
Q

In Efficacy, you look for the

A

Receptor and

Response.

35
Q

A 55-year-old woman with hypertension is to be treated with
a thiazide diuretic. Thiazide A in a dose of 5mg produces the
same decrease in blood pressure as 500mg of Thiazide B.
Which of the following statements best describes these
results?

a. Thiazide A is more efficacious than Thiazide B
b. Thiazide A is about 100 times more potent than
Thiazide B
c. Toxicity of Thiazide A is less than that of Thiazide B
d. Thiazide A has a wider therapeutic window that
Thiazide B

A

Thiazide A is about 100 times more potent than Thiazide B
because it only takes 5mg of Thiazide A to produce the
same efficacy compared to 500mg of Thiazide B.

36
Q

t is used in computing the therapeutic index.

A

QUANTAL DOSE EFFECT CURVES

37
Q

It is the dose at
which 50% of individuals exhibit the specified
quantal effect.

A

Median Effective Dose (ED50)

38
Q

It is the dose
required to produce a particular toxic effect in 50%
of individuals

A

Median Toxic Dose (TD50)

39
Q

If the toxic effect is
the death of the animal. The amount of
drug/substance that when administered to a group
of experimental animals, will kill 50% of the group
in a specified time

A

Median Lethal Dose (LD50)

40
Q
  • Dose of a drug required to produce a desired

effect to that which produces an undesired effect

A

THERAPEUTIC INDEX

41
Q

TI is Defined as the ratio of the______

A

TD50 to the ED50

42
Q

TI formula:

A

Formula = LD50/ ED50

43
Q

refers to the range
wherein the half maximal effect is seen as well as
the adverse effect

A

Therapeutic Window

44
Q

If TI is_____, a slight change in the dosage

can lead to potential adverse effect.

A

low/ narrow

45
Q

If TI is_____, even if there is an increase/
decrease in the dosage of the drug the risk for
adverse effect is lower.

A

large/ wide

46
Q

Penicillin is an example of a drug with _____ TI

A

High

47
Q

Drugs with Low TI:

A 
▪ Antiarrhythmic Drugs - Digoxin
▪ Diabetes - Insulin 
▪ Bronchodilator - Theophylline
▪ Anticoagulant - Warfarin
▪ Antiepileptic - Phenytoin
48
Q

If ED50 is 0.1 and the TD50 is 10 what will be the

Therapeutic Window?

A

0.1 to 10 ug

49
Q

If ED50 is 0.1 and the TD50 is 10 what will be the

Therapeutic Index?

A

10/ 0.1 = 100

50
Q

Determines the ability to fully or partially activate

the receptors

A

INTRINSIC ACTIVITY

51
Q

If a Full Agonist binds to the receptor and
produces and effect similar to your endogenous
ligand, the Intrinsic Activity is

A

1

52
Q

If the drug produces an Intrinsic Activity of 1 and
mimics the effect of your endogenous ligand it is
considered as a

A

Full Agonist.

53
Q

For Partial Agonist, they also bind to the receptor
and mimic the effect of your endogenous ligand
however the Intrinsic Activity of your Partial
Agonist is____

A

above 0 but less than 1.

54
Q

are also agonists however when
they bind to the receptor, they change the
equilibrium/state of your receptor from active to
inactive

A

Inverse Agonist

55
Q

he Intrinsic Activity of your

Inverse Agonist is

A

below 0.

56
Q

For Antagonist, the Intrinsic Activity is

A

0
-because in the absence of agonist your
antagonist will not have any effect.

57
Q

A ligand that binds to a receptor and produces a
conformational change that initiates an
intracellular signal

A

Agonist

58
Q

Continuous administration of agonist after Emax

would lead to

A

Desensitization

59
Q

A ligand that binds to a receptor but does not
produce the conformational change that initiates
an intracellular signal

A

ANTAGONIST

60
Q
  • binding site different from active site that is

bound by endogenous ligand.

A

Allosteric Site

61
Q

Antagonist that binds to allosteric are ALL

A

noncompetitive antagonist

62
Q

reversible -
Compete to the binding site of endogenous
ligand.

A

Competitive antagonist

63
Q

irreversible
because if they bind to active site, they form
covalent bond. Duration of effect will depend
on the regeneration of new receptor

A

Noncompetitive Antagonist

64
Q

Do not bind to receptor bound to your
endogenous ligand. Can be either chemical or
physiologic antagonist.

A

NON – RECEPTOR ANTAGONIST

65
Q

Protamine, a protein that is positively charged at
physiologic pH, can be used clinically to counteract the
effects of heparin, an anti-coagulant that is negatively
charged. This is an example of:

A

a. Chemical Antagonism

-Protamine (a positively charged protein at
physiologic pH) binds heparin (a negatively
charged anticoagulant) making it unavailable for
interactions with proteins involved in the formation
of blood clots.

66
Q

One drug may antagonize the action of a second

by binding to and inactivating the second drug.

A

a. Chemical Antagonism

67
Q

Ted, 50 – year - old diabetic, was rushed to the ER due to
bronchial Asthma in acute exacerbation. He was given
Salbutamol nebulization and Hydrocortisone
(Glucocorticoid). Insulin was administered to oppose the
hyperglycemic effects of glucocorticoid. This is an example
of?

A

Physiologic Antagonism
-(Nonreceptor Antagonism) Hydrocortisone can increase
blood sugar. Insulin was administered to oppose the effect
of the hydrocortisone. Another example: Histamine
(bronchoconstriction) and Epinephrine (Bronchodilation).

PHARMACOLOGY (13 decks)

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