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Pharmacology > Drug Receptor Interactions > Flashcards

Drug Receptor Interactions Flashcards

1
Q

Approximately how many applications are there for novel drugs every year?

A

40

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2
Q

What is a novel drug?

A

entirely new molecular entities

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3
Q

What is the primary source of information regarding the efficacy and safety of new drugs?

A

drug companies will be the primary source of new information

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4
Q

True or False: All drug targets are neuroreceptors

A

false

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5
Q

The binding forces involved in drug-receptor interactions are usually a combination of _____ interactions that result in _______ ________.

A

weak, irreversible binding

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6
Q

What is Kd?

A

the dissociation constant: the drug concentration required to produce half-maximal occupancy of the receptor population

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7
Q

What is concentration dependence?

A

the percentage of receptors bound by or occupied by a drug increases as the concentration of that drug increases

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8
Q

What is saturability?

A

once all of the receptors are bound by a drug, further increases of drug concentration cannot increase the percentage of receptors bound by the drug

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9
Q

What does a small dissociation constant (Kd) mean?

A

the drug is tightly interacting with its receptor

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10
Q

What is affinity?

A

the force that impels certain molecules to bind to or unite with certain others to form complexes or compounds

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11
Q

A high affinity drug produces a _____ dissociation constant.

A

low

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12
Q

What is specificity?

A

the selectivity of a drug for a particular receptor

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13
Q

What kind of drug has complete specificity?

A

a drug that binds only on particular drug receptors

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14
Q

What is competitive inhibition of binding?

A

when two (reversibly binding) drugs which both bind to the same population of receptors are present simultaneously, the two drugs compete to bind to those receptors

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15
Q

How does competitive inhibition of binding effect Kd?

A

it will appear to increase it (decrease affinity)

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16
Q

What is non-competitive inhibition of binding?

A

when a drug binds irreversibly to a receptor, other drugs which normally bind to that receptor cannot displace it

17
Q

What is allosteric modulation of binding?

A

binding of a drug to a receptor may be increased or decreased by a second drug that does not actually bind to the same site on the receptor

18
Q

In allosteric modulation of binding, how is the affinity affected?

A

the total number of receptors is not changed, but the affinity of the receptor for the first drug is changed

19
Q

What is efficacy?

A

a percentage of the maximum response that can be mediated by a receptor-effector system (maximum response=complete efficacy)

20
Q

What is a full agonist?

A

something that produces the maximum response that can be elicited by those receptors

21
Q

What is a partial agonist?

A

something that produces a response, but it is smaller than the maximum response that can be elicited by other agonists at the same receptors

22
Q

Which is more effective, a full agonist or a partial agonist?

A

a full agonist

23
Q

What is an antagonist?

A

something that binds to the receptor, but does not activate the effector system - blocks activation

24
Q

What is potency?

A

a relative measure of drug activity, the concentration (or dose) of a drug required to produce an effect compared with the concentration (or dose) required for other agents to produce the same effect

25
Q

What is EC50?

A

the concentration of a drug required to produce 50% of that drug’s maximum response

26
Q

If there is a low Kd what is the affinity?

A

high

27
Q

If there is a low EC50 what is the potency?

A

high

28
Q

What does a cumulative dose-response releationship show?

A

the percentage of patients that reach a certain response threshold at or below that dose

29
Q

What is ED50?

A

the effective dose - the dose required to elicit the therapeutic response in 50% of the population

30
Q

What are the therapeutic effects?

A

the desired effects

31
Q

What are the side effects?

A

the undesired effects

32
Q

Name 2 scenarios in which side effects can happen.

A

Sometimes the same receptor that produces the desired therapeutic effect also produces undesired effects
sometimes the drug binds to other targets because the drug is dirty

33
Q

What is LD50?

A

the lethal dose in half of the patients

Pharmacology (16 decks)

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