Pharmacodynamics - receptors, clinical Flashcards
What are the types of GPCRs located in the bronchi of the lungs?
B2 adrenoceptors
M3 muscarinic recetors
What does activation of the M3 muscarinic receptors in the bronchi cause?
Bronchoconstriction
What does activation of the B2 adrenoceptors in the bronchi cause?
Bronchodilation
How is asthma treated?
Giving B2 adrenoceptor agonists
What is functional antagonism?
Two drugs acting on two different types of receptors to cause opposing effects
What properties must the B2 adrenoceptor agonists have when treating asthma? Why?
Must be specific for B2 adrenoceptors
So that they don’t bind to and activate B1 adrenoceptors in the heart
giving increased heart rate and force of contraction
What are some examples of B2 adrenoceptor agonists used to treat asthma?
Salbutamol
Salmeterol
What are the advantages of partial agonists over full agonists?
Give a more controlled response
Can act as antagonist against high levels of full agonist
What binds to the mu-opioid receptor?
Opioids duh
What are the uses of opioids?
Pain relief
Recreational use
What are the risks of opioids?
Addictive
Can cause respiratory depression
What are some examples of opioids?
Morphine
Diamorphine
Buprenorphine
Which of morphine, diamorphine and buprenorphine are partial agonists and which are full agonists?
Morphine and diamorphine - full agonists
Buprenorphine - partial agonist
What might happen to someone who is addicted to morphine/diamorphine who takes buprenorphine? Why?
Withdrawal symptoms
Because buprenorphine doesn’t give the maximum response that morphine/diamorphine do
and will antagonise morphine/diamorphine
What are the uses of buprenoprhine clinically?
Given for pain relief
less risk of addiction, respiratory depression compared to morphine, diamorphine etc.
Can be used to help people addicted to morphine/diamorphine withdraw from them
