Nuts and Bolts of Therapeutics Flashcards

1
Q

Drug-receptor interactions depend on…

A
  1. Chemical composition
  2. Stereochemical disposition (chirality)
  3. Ability for drug to reach receptor binding zone
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2
Q

Affinity

A

Probability of the the drug occupting a receptor at any given time - affected by other drugs, ageing and genetic mutations

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3
Q

Selectivity

A

The degree to which a drug acts on a given site relative to other sites

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4
Q

Efficacy

A

The relative ability of a drug-receptor complex to produce the maximum functional response

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5
Q

Agonist

A

Chemical binds to a receptor and activates it to produce a biological response

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6
Q

Partial Agonist

A

Chemical still binds to receptor but only has partial efficacy

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7
Q

Antagonist

A

Chemical binds and blocks/dampens agonist-mediated responses rather than provoking a biological response

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8
Q

Potency

A

Measure of drug activity - the amount required to produce an effect of given intensity

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9
Q

Tolerance

A

Decreased response to drug with repeated doses

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10
Q

Mechanisms of tolerance

A
  1. Decreased receptor numbers (downregulation)
  2. Decreased receptor binding affinity
  3. Modulation of downstream response to initial signal
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11
Q

On-target response

A

Drug intended to modulate the function of a specific receptor in a particular tissue

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12
Q

Off-target response

A

Drug and/or metabollites modulate the function of a target for which it was not intended

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13
Q

Therapeutic index

A

Ratio of the dose that produces toxicity to the dose that produces a clinically desired or effective response in a group of individuals

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14
Q

Dose

A

Total quantity of an active agent taken in or absorbed at any one time

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15
Q

Main routes of drug administration

A
  1. Enteral - substance given by GIT - desired effect is systemic (oral, NG, ND, enema)
  2. IV - 100% availability
  3. Parental - desired effect is systemic but drug not given via GIT (transdermal, tansmucousal, inhalation)
  4. Topical - local effect (transcutaneous/cream, inhalation)
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