Drug Receptor Interactions 2 Flashcards

1
Q

What is the equation for the response?

A

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2
Q

What are spare receptors?

A

The extra receptors if less than 100% of receptors are required to evoke a maximum response

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3
Q

What is efficacy?

A

Max response achievable from a drug. This can be obtained by occupying less than 100% of the receptors

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4
Q

What is the difference between efficacious drugs?

A

very efficacious drugs will require to occupy few receptors to give a response than less efficacious

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5
Q

What are some of the features of partial agonists?

A
  • Low efficacy so never produce max response - They can decrease the response of a full agonist as they give a smaller response than if all full agonists were bound
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6
Q

What is a competitive antagonist?

A

A drug that binds reversibly with receptors to form a complex but this complex does not evoke a response

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7
Q

What is the equilibrium dissociation constant for an antagonist?

A

K(A). It is the concentration of antagonist that makes is necessary to add twice as much agonist to produce response

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8
Q

What direction is a Log-Dose response curve displaced by a competitive antagonist

A

To the right as more agonist is needed to required to produce max response, however the linear sections remain parallel

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9
Q

What is the Schild Equation

A

Where r is the ratio by which D must be increased to overcome competition by A

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10
Q

What is pA(2)

A

A way of comparing the affinity of an antagonist. It is equal to -log(base10) of K(A)

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11
Q

What are irreversible competitive antagonists?

A

The bind to the receptor site but dissociate so slowly that it is basically irreversible. Therefore the effects of these are not reversed by adding more agonist

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12
Q

Describe the effects of the irreversable competative antagonists on the log Dose-response curves and this effect over time

A

The curve is decreased. And over time this curve decreases more as agonists come on and off receptors this allows more antagonists to bind.

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13
Q

Describe some of the features of allosteric modulators

A
  • Bind to allosteric sites which are regulatory - Modify efficacy or affinity - Potentiate or inhibit
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14
Q

Name an example of allosteric modulator

A

Non competitive antagonist. They work by blocking the access of the agonist to its binding site through steric hindrance

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15
Q

What is an inverse agonist?

A

This dampens the response. They bind to the active sire and cause a reduction in the activity of the drug

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16
Q

What are the effects of antagonist on an inverse agonist

A