M&R Session 11 Flashcards
What can altered receptor responsiveness result from?
Change in receptor number
Change in receptor coupling to 2nd messenger
Change in availability of 2nd messenger
Change in cell responsiveness
Which changes causing altered receptor responsiveness are seen clinically?
Change in receptor number
Change in receptor coupling to 2nd messenger
How does suprasensitivity arise?
Agonist deprivation
Excessive antagonist exposure
What is tachyphylaxis?
Decreased sensitivity of a cell to a ligand
How does tachyphylaxis arise?
Excessive exposure to agonist
What is activation of mu-opioid receptors associated with?
Analgesia
Sedation
Euphoria
What is an example of an endogenous opioid?
Endorphins
When are endogenous opiates released?
Stress
How does repeated opioid use cause tachyphylaxis?
Repeated use –> receptors upregulated but amount of 2nd messenger is constant
What can be said about the level of opioid required to elicit a response in tachyphylaxis?
Increased
Why does a patient perceive pain when opioid levels fall?
Molecule leaves receptor and is less likely to be replaced –> 2nd messenger activity falls
What are the typical withdrawal S/S of opiate withdrawal?
Distressing, variable, poorly localised pain
Sweating
Anxiety
Constipation
Why is it preferable to use patient administered analgesia with opiate based treatment?
Will be administered irregularly so no tachyphylaxis hence dose will stay low
How is clinical opioid withdrawal treated?
Decrease dose of opioid Substitute w/ a different class of analgesia
What is phaechromocytoma?
Tumour of the adrenal medulla