Efficacy and Partial Agonists Flashcards

1
Q

What is efficacy and what does it depend on?

A
  1. The ability of a drug to activate a receptor and cause a response (EFFECT)
  2. Depends on the number of receptors occupied and
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2
Q

What is E max?

A

The maximum response an agonist can achieve

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3
Q

What type of Emax does a partial agonist have?

A

Lower Emax

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4
Q

What is a partial agonist?

A

They partially bind to the receptor sites and can never evoke the maximum Emax response even though 100% of receptor sites may be binded

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5
Q

How is a partial agonist used in medicines and give an example?

A
  1. Used due to less desensitisation compared to normal agonists and can be used as competitive inhibitors against agonists
  2. Buprenorphine- used as a partial agonist as it reduce pain but not give all the other side effects of morphine
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6
Q

What is the term that explains how maximum response can be created without 100% of the receptor sites being binded and explain it?

A
  1. Receptor Reserves- a proportion of receptors in the tissues that are never used
  2. A signal amplification must occur for it to activate
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7
Q

What is the inverse agonist?

A
  1. Has some actions that are similar to agonists but can also have the complete opposite response- it blocks the individual activity of the agonist as well (not just receptors)
  2. Equilibrium between agonist and inverse as they switch between the two
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8
Q

What are state are receptors constantly in? And which do agonists prefer?

A
  1. Constant equilibrium between active and non active state

2. Agonists prefer the active state

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