Week 10 - Opioids Flashcards
What are opioids?
A large variety of drugs that play a major role in analgesia (ie. pain relief).
What are naturally occurring opioids?
Morphine and codeine.
How are these natural versions extracted?
They are extracted from plants.
What is one of the primary prodrugs of codeine?
Morphine
What are some of the semisynthetic versions of opioids?
Vitolin, Oxycodeine, ——
From what are semisynthetic versions of opioids produced?
They are produced from naturally occurring opioids????
What are some examples of fully synthetic versions of opioids?
fentanyl, heroin, ummmmm
What is the source of the fully synthetic opioids?
it was another synthetic drug that was used as a source.
What is more potent and why - fentanyl or morphine?
F is more potent and
How are opioids generally administered?
The preferred route depends on the particular drug and the purpose of using the drug. Can be taken in through IV, orally, inhalation.
Why heroin preferred over morphine for recreational purposes?
Heroin is able to pass through the BBB much more quickly (it is more lipid soluble).
How are opioids generally metabolized?
In the liver, they are metabolized and many of the metabolites themselves act as opioids.
What are the metabolites of morphine?
a
What are the metabolites of codeine?
a
What are the metabolites of heroin?
a
What are the metabolites of acetylcodeine?
a
What is the endogeneous opioid system?
The system involving neuropeptide transmitters and their receptors and site of actions????
What are neuropeptide transmitters?
a
What are propeptides and how do the neuropeptides form from these propeptides?
a
What are the different propeptides?
a
What are the endogenous opioid peptides (opiopeptins)?
a
What are the different families of opiopeptins?
a
What are the precursor and the peptides of the enkephalins?
a
What are the precursor and the peptides of the endorphins?
a
What are the precursor and the peptides of the dynorphins?
a
What are the different opioid receptors?
a
Where is an effect seen across all opioid receptors?
a
What are the effects of mu receptors on systemic and peripheral sites of actions?
a
What are the effects of kappa receptors on systemic and peripheral sites of actions?
a
What are the effects of delta receptors on systemic and peripheral sites of actions?
a
What receptors does B-endorphin act on?
a
What receptors do Met-enkephalins and leu-enkephalins act on?
a
What receptors does Dynorphin A and B act on?
a
What receptors does Neoendorphines act on
a
What receptors does Nociceptin act on?
a
What is ORL-1 and how does it differ from other opioid receptors?
a
What type of receptors are opioid receptors?
a
What is the end result of opioid receptors being bound to by neuropeptides?
reduce neurotransmission??? reducing metabolic activity within cells
What are some (possible) mechanisms that opioid receptors cause inhibitory action?
Inhibition of adenyl cyclase - a net decrease of adenyl cyclase in the post-synaptic neuron.
Inwardly rectifying the K+ channel.
What is the role of adenyl cyclase?
a
What are GIRK? channels?
a
Which regions of the CNS and PNS do most opioid receptors reside in?
a
What is nociception?
a
How does opioid action influence certain pathways around the brain?*****
a
What are the two nociception pathways?
a
What is the role of the Dorsal horn in nociception?
a
Where do opioids inhibit the pain signal?
a
What are the reinforcing and analgesic effects of opioids?
a
When is glutamate released and when is substance P released when pain signals are initiated?
a
How does adaption to opioids happen? Specifically, how is the inhibitory action of opioids countered?
a
Which opioid receptor do most opioid drugs act on?
a
What are pure opioid receptor agonists?
a
What are partial opioid receptor agonists?
a
What are pure opioid receptor antagonists?
a
What are mixed opioid agonist-antagonists?
a
What are the different phases of opioid agonists and what are the subject effects that characterize these phases?
a
What is the conditioned place preference?
a
What roles do NMDA and glutamate play on morphine action?
a
What are the adverse effects of opioid overdose?
a
What are the acute pharmacological effects of opioids?
- Analgesic
What are the withdrawal symptoms of opioid addiction?
- Reduced pain sensitivity
What are the different detoxication programs for opioid addiction?
a
