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Pharm Exam 1 > Drug Receptors and Pharmacodynamics > Flashcards

Drug Receptors and Pharmacodynamics Flashcards

1
Q

Simple explanation of Pharmacodynamics

A

What the drug does to the body

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2
Q

Drugs must interact with a _____ to exert an effect

A

molecular target

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3
Q

_____: the component of a cell or organism that interacts with a drug and initiates the chain of events leading to the drug’s observed effects

A

Receptors

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4
Q

Drug interaction with molecular targets is the initiating event in a multistep process that ultimately alters ______ function

A

Tissue

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5
Q

Receptors (regulatory proteins) that are targets for drugs can also be the targets
for ______, such as neurotransmitters and hormones

A

endogenous substances

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6
Q

______ - measure of how tightly or strongly a drug (ligand) binds to a receptor

A

Affinity

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7
Q

Receptors mediate the actions of pharmacologic _____ and _____

A

agonists and antagonists

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8
Q

______- drugs that bind to receptors and produce some effect or signal from the tissue. It is similar to the response produced by endogenous agents. They posses intrinsic activity

A

Agonists

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9
Q

______- drugs that bind to receptors but do not produce an effect or signal. They possess no intrinsic activity. They block responses from the tissue

A

Antagonists

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10
Q

______- the ability of a drug to evoke a response or effect in a target by altering some activity in the target

A

Intrinsic activity

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11
Q

______- the strength of a single drug-receptor interaction that evokes a response

A

Efficacy

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12
Q

_____- the concentration or dose of a drug required to produce 50% of the drug’s max effect

A

Potency

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13
Q

Types of receptors (4)

A
  • Regulatory proteins- best-characterized receptors
  • Enzymes- generally inhibited by drug binding
  • Transport proteins- can be useful drug targets
  • Structural proteins
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14
Q

Two types of dose response curves:

A

1) Graded dose-response curve
-drug concentration v. percentage of maximal effect
- log of drug concentration v. percentage of max. effect
2) Quantal dose-response curve

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15
Q

Maximal response that can be produced by a drug on a graded dose-response curve

A

Emax

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16
Q

The concentration of drug that produces 50% of maximal effect on a graded dose response curve

A

EC50

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17
Q

What does the logarithmic graded dose response curve accomplish?

A

Expands the scale at lower concentration and compresses the scale at higher concentrations (sigmoid curve)

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18
Q

T/F If Kd is low, binding affinity is high

A

T

19
Q

Which of these drugs is the most potent?

A

B

20
Q

Therapeutic index - the ratio of the ____ to ____

A

TD50 to ED50

21
Q

______: the range between the minimum toxic dose and the minimum therapeutic dose

A

Therapeutic window

22
Q

What do ED50, TD50 and LD50 illustrate?

A
  • ED50- dose at which 50% of individuals exhibit the specified quantal event (median effective dose)
  • TD50- median toxic dose
  • LD50- median lethal dose
23
Q

T/F all receptors have to be occupied to exhibit a full response

A

F - you cannot directly correlate physiological responses to binding

24
Q

An antagonist that binds to the receptor in a reversible mass-action manner is referred to as a ____ ____

A

competitive antagonist

25
Q

What is happening in the graph on the left?

A
  • Reversible binding to the receptor
  • Can be overcome by increasing the agonist concentration
  • The maximal response of the agonist is not decreased
  • The agonist dose-response curve in the presence of a competitive antagonist is displaced to the right
25
Q

the degree of inhibition produced by a competitive antagonist depends on the ____ of the antagonist

A

Concentration

26
Q

the clinical response to a competitive antagonist depends on the concentration of the competing _____

A

Agonist

27
Q

_____ Bind irreversibly to receptors

A

Non-competitive antagonists

28
Q

What does an allosteric antagonist do?

A
  • Bind at a site on the receptor
    different than the agonist binding site
    • or - effect
29
Q

Chemical vs. Physiologic antagonists

A

Chemical- does not utilize receptors
- Example: heparin (Neg charge) can be counteracted by protamine (Pos charge). It makes the other drug unavailable for interactions with blood clotting proteins.
* Physiologic- between endogenous regulatory pathways. less specific, harder to control than receptor specific antagonist
- Example: glucocorticoid hormones v. insulin

30
Q

What do partial agonists do?

A

Produce a lower response, at full receptor occupancy, than full agonists
* Competitively inhibit the responses produced by full agonist

31
Q

How do lipid soluble agents work?

A

Move directly through the plasma membrane into the cell
- intracellular receptors
- Steroids, thyroid hormone (receptors stimulate transcription of genes)
- lag time to onset of effects
- effects persist longer

32
Q

How do ligand-regulated transmembrane proteins work?

A

Regulates intracellular enzyme activity
- Example: insulin, epidermal growth
factor

33
Q

How do cytokine receptors work?

A

Have extracellular and intracellular domains and form dimers
Examples: growth hormone, erythropoietin, types of interferon

34
Q

What is this an example of?

A

Cytokine receptor

35
Q

What is this an example of?

A

Ligand-regulated transmembrane

36
Q

How do ion channels work?

A

Many of the most useful drugs act on ion channels
* Drugs can mimic or block the actions of natural agonists
Examples: acetylcholine,
serotonin, GABA, glutamate

37
Q

What is this channel called?

A

Ion channels

38
Q

How do G proteins and 2nd messangers work?

A

Extracellular ligands that increase the intracellular concentration of 2nd messengers

39
Q

3 components of transmembrane signaling

A

-agonist binding
-activation of G protein
-G protein changes activity of
effector enzyme/ion channel

40
Q

______: caused by genetic differences in metabolism or by immunologic mechanisms, including allergic reactions

A

Idiosyncratic drug response

41
Q

_____: responsiveness diminishes rapidly

A

Tachyphylaxis

42
Q

What does clinical selectivity mean with regards to drugs?

A

No drug causes only a single, specific effect
* Unlikely that a drug binds only to a single type of receptor
* Biochemical processes are coupled to many other biochemical functions

43
Q

Clinically, selectivity is considered by separating effects into

A

1) beneficial or therapeutic
2) toxic or adverse

Pharm Exam 1 (7 decks)

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