Pharmacodynamics Flashcards

1
Q

Define ‘affinity’

A

Mathetmatically represented as 1/Kd (dissociation constant). If the receptors have a high affinity for the ligand, the Kd will be low (takes a low concentration of ligand to bind to half of the receptors)

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2
Q

Define ‘selectivity’

A

a drug’s ability to preferentially bind to certain receptors

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3
Q

Define ‘specificity’

A

The number of different mechanisms involved; a high specificity involves binding to a small subset of receptors and not eliciting a large host of reactions

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4
Q

Define ‘inverse agonist’

A

An agent which binds to the same receptor as an agonist, but induces a pharmacological response which opposes the agonist

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5
Q

Give an example of a drug which is a positive allosteric modifier

A

Benzodiazepines

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6
Q

Define ‘physiologic antagonism’

A

Occurs when two drugs acting on different receptors and pathways exert opposing actions on the same system, leading to no net response

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7
Q

Define ‘efficacy’

A

the maximum effect of a drug

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8
Q

Define ‘potency’

A

The concentration/dose of a drug required to produce 50% of the drug’s maximal effect (EC50). It is used as a comparative measure between drugs where different doses are needed to produce the same effect.

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9
Q

Define ‘median inhibitory concentration’

A

The concentration of an antagonist that reduces a specified response to 50% of the maximal possible effect.

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10
Q

Define ‘hysteresis’

A

Where the value of a physical property lags behind changes in the effect causing it i.e. the relationship between drug concentration and its effect is not direct

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11
Q

Define ‘counter-clockwise hysteresis’

A

The effect can increase with time for a given drug: Sensitisation (up-regulation of receptors), distribution delay to the site of the effect, an agonistic metabolite may be formed, slow receptor kinetics, and time-dependent protein binding

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12
Q

Define ‘clockwise hysteresis’

A

The measured effect decreases with time for a given drug concentration e.g. tolerance (down-regulation of receptors), disequilibrium between arterial and venous circulation, generation of an antagonistic metabolite, feedback regulation, time-dependent protein binding

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