Opioid Pharmacology Flashcards
mechanism of action of opioids presynaptically and postsynaptically
presynaptically they lower calcium influx. Postsynaptically they increase potassium transport into the cell.
what does oxycodone break down into
oxymorphone and hydrocodone, and hydrocodone breaks down into dihydrocodeine and hydromorphone
lipid solubility and onset
more lipid soluble = faster onset
what are the 2 natural opioids
morphine and codeine
mechanism of methadone
Opioid agonist, serotonin-norepinephrine reuptake inhibitor, NMDA antagonist
what are the 3 endogenous opioids
enkephalin, endorphin, dynorphin
relationship between pka and onset
the lower the pka, the faster the onset
what are the 4 fully synthetic opioids
fentanyl, methadone, tramadol, dextropropoxyphene
which opioid receptors cause physical dependence
mu2
what does hydrocodone break down into
dihydrocodeine and hydromorphone
Suboxone =
buprenorphine + naloxone
what 2 drugs break down into hydrocodone
codeine and oxycodone
which opioid receptors result in analgeis
mu1, delta, kappa
which endogenous opioid has the highest affinity for opioid receptors
endorphin
what are the 2 main opioid antagonists
naloxone and naltrexone
what does morphine break down into
hydromorphone
what do opioids activate that results in nausea and vomiting
the chemoreceptor trigger zone
what opioid receptors cause psychomimetic effects
kappa
what are the 4 mixed opioid agonist-antagonists
buprenorphine, pentazocine, butorphanol, nalbuphine
What condition is morphine contraindicated with
renal failure
mechanism of pentazocine, butorphanol, nalbuphine
Opioid agonist-antagonist
most and least lipid soluble opioids
most = fentanyl least = oxycodone
cautionary note of methadone
may cause QT prolongation
what are the 2 opioid contraindicated with MAOIs
tramadol and meperidine
what is tramadol contraindicated with
MAOIs or SSRIs
what does codeine break down into
hydrocodone and morphine, which break up into hydromorphone and dihydrocodeine
which opioid receptors cause respiratory depression
mu2 and kappa
which opioid medication is the only one that has high affinity for delta receptors
methadone
Heroin is aka
diamorphine
mechanism of buprenorphine
Opioid antagonist and partial opioid agonist
mechanism of tramadol
weak mu agonist and weak serotonin-norepinephrine reuptake inhibitor
what does heroin break down into
6-monoacetyl morphine, which breaks down into morphine, which breaks down into hydromorphone
mechanism of codeine
weak opioid agonist
what is the parent drugs of hydromorphone
hydrocodone and morphine
