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Pharmacology > Exam 1 - Drug-Receptor Interactions > Flashcards

Exam 1 - Drug-Receptor Interactions Flashcards

1
Q

receptor-mediated mechanism

A

most drugs act via interactions with receptors

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2
Q

non-receptor mediated mechanism

A

some drugs do not act by interaction with receptors (antacid)

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3
Q

What do drugs bind to within the body?

A

endogenous components of cells recognize and bind to specific drugs

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4
Q

endogenous

A

normally present within the body

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5
Q

exogenous

A

from outside the body

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6
Q

What is the importance of frug-receptor interactions?

A

alters the activity of the receptor and alteration of receptor activity produces the observed effect of the drug

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7
Q

Emax

A

the maximum effect or response that a drug can produce when it binds to its target

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8
Q

ED50

A

the dose of a drug the produces a therapeutic effect in 50% of the population

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9
Q

TD50

A

the dose of a drug the produces a toxic effect in 50% of the population

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10
Q

LD50

A

the dose of a drug the produces a lethal effect in 50% of the population

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11
Q

efficacy

A

measurement of the magnitude of response a drug elicits

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12
Q

potency

A

measurement of the amount of drug required to produce a certain response

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13
Q

therapeutic index

A

ratio that compares the toxic dose of a drug its effective dose, indicating the safety margin of the drug
* T.I. = TD50 / ED50

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14
Q

What does a high therapeutic index signify?

A

a wider margin of safety between therapeutic and toxic effects (good)

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15
Q

What does a low therapeutic index signify?

A

a smaller margin of safety between therapeutic and toxic effects (bad)

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16
Q

agonist

A

a drug that, by itself, produces a response

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17
Q

antagonist

A

a drug that, by itself, produces no response but prevents the agonist response

18
Q

What is the general Emax of a full agonist?

A

biggest Emax

19
Q

What is the general Emax of a partial agonist?

A

lesser Emax

20
Q

What is the general Emax of an antagonist?

A

0 Emax

21
Q

What is the general Emax of an inverse agonist?

A

negative Emax

22
Q

intrinsic efficacy

A

refers to the ability of a drug to activate a receptor and produce a biological response once it binds
* indicates how effectively a drug can elicit its intended effect relative to other compounds at the same receptor

23
Q

competitive antagonist

A

binds reversibly to the same receptor site as an agonist without activating the receptor
* effect can be overcome by increasing the concentration of the agonist
* no change in Emax

24
Q

non-competitive antagonist

A

bind either to the same site or to a different site on the receptor, causing a change in receptor function
* CANNOT be reversed by increasing agonist concentration
* reduction in Emax

25
Q

What are examples of pharmacological antagonist?

A
  • competitive antagonist
  • non-competitive antagonist
  • partial antagonist
26
Q

chemical antagonist

A

substance that directly interacts with an agonist or another drug in a chemical reaction
* neutralizing or inactivating it before it can bind to its receptor or exert its effect

27
Q

physiological antagonist

A

a substance that produces an opposite physiological effect to that of an agonist but acting on a different receptor
* counter agonists action through independent mechanism rather than direct competition for the same receptor

28
Q

receptor specific drug

A

interacts with only a single receptor sub-type
* rare

29
Q

receptor selective drug

A

interacts with several receptor sub-types but has a preference for one of them
* common

30
Q

additive effect

A

response to two drugs together is the sum of both responses

31
Q

synergist effect (potentiation)

A

response to two drugs together is greater than the sum of each response

32
Q

idiosyncratic drug response

A

unusual or atypical response seen in only a small % of people

33
Q

hypersensitivity

A

allergic response

34
Q

tolerance

A

decreased response
* takes hours/days to develop

35
Q

refractoriness

A

decreased response
* often used to mean no response at all, similar to extreme tolerance

36
Q

desired effects

A

effects that produce a therapeutic response

37
Q

side effects

A

undesired effects

38
Q

adverse effects

A

serious medical consequences

39
Q

toxic effects

A

causing damage to an organ or whole organism

40
Q

What are the four basic sources of side/adverse effects?

A
  1. chemical properties
  2. drug that interacts with multiple receptor types (dirty drugs)
  3. drug that interacts with single receptor type but multiple subtypes of that receptor
  4. drug that interacts with single receptor subtype but receptor is in multiple tissues or acts via multiple effectors
41
Q

What is a goal of pharmacology in regards to specificity?

A

eliminate undesirable effects by increasing receptor specificty of drugs

Pharmacology (12 decks)

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