Opioids Flashcards
What is the main function of opioids?
analgesia
Where can you find naturally occurring opioids?
in alkaloids found in the opium poppy
What are opiates?
opiates are the naturally occurring opioid
What caused a surge in US opioid use?
end of the civil war; soldier’s disease
production of hypodermic syringe
What is heroin?
a semi-synthetic opioid
What is the potency of heroin?
5x more potent than morphine as it is more lipid soluble due to addition of 2 acetyl groups
What is the pharmacological effect of heroin?
identical to morphine as it is largely metabolised into morphine
How does administration affect the pharmacological effect?
oral; analgesia but no euphoria/rush
IV/smoking/snorting; analgesia and euphoria
What are the major clinical effects of opioids?
analgesia euphoria conditioned place preference reduced gastrointestinal motility cough suppression
What are the major side effects of opioids?
reduced gastrointestinal motility
respiratory depression
nausea/vomiting
What are the effects of repeated opioid administration?
sensitisation
tolerance
withdrawal
What opioid effects can become sensitised?
stimulant effects; with VTA administration
rewarding effects
What opioid effects can become tolerated?
analgesia
euphoria
respiratory depression
What withdrawal effects are seen with opioid use?
symptoms are opposite to the acute effects
How can respiratory depression be reversed?
administration of naloxone
What is saturable binding?
the maximum effects observed in opioids suggests that there is a finite number of mechanisms on which opioids can act
How can we predict analgesic effects in humans from animal studies?
opioids causing contractions of the intestine in the guinea pig predicts human analgesia
What are the endogenous ligands/peptides that act on μ receptors?
endorphins
endomorphins
What propertied/precursor peptide is used to create μ peptides?
POMC
unknown
What are the endogenous ligands/peptides that act on δ receptors?
enkephalin
endorphin