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45 Cards in this Set

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  • Back
  • 3rd side (hint)
Mu receptors have what effect on which ion channel?
open K+ channel
What endogenous substance binds to mu receptors?
endorphins
What are the effects of mu receptor agonism?
supraspinal analgesia; spinal analgesia, respiratory depression, euphoria, physical dependence
Kappa receptors have what effect on which ion channel?
close Ca2+ channel
What endogenous substance binds to kappa receptors?
dynorphins
What are the effects of kappa receptor agonism?
spinal analgesia; sedation, some dysphoric and psychotomimetic effects
What endogenous substance binds to delta receptors?
enkephalins
What are the effects of delta receptor agonism?
spinal and supraspinal analgesia
How are opioids administered?
usually orally
Which opioid cannot be given orally?
hydromorphone
How are opioids metabolized and excreted?
by the liver, by the kidney
What are the main CNS effects of opioids? (h for hint)
analgesia, euphoria, miosis, antitussive; sedative at low doses, N/V, increase muscular tone, increase ICP
Hint: MEAT
What are the main peripheral effects of opioids?
hypotension, constipation, urinary retention; prolonged labor, increased release of prolactin, ADH, GH, histamine and decreased release of LH
Which opioids treat diarrhea?
loperamide and diphenoxylate
Which opioids treat cough?
codeine and dextromethorphan
Which opioid treats opioid dependence?
methadone
Which opioid treats pulmonary edema?
morphine
Which two opioids are used for cardiovascular surgery? Why?
morphine and fentanyl b/c they produce minimal cardiac depression
What are the main side effects of opioids?
respiratory depression, constipation, N/V, dysphoria, hypotension, urinary retention, increase in ICP, pruritus
Which drugs do opioids interact with and how?
+ sedatives increases CNS and respiratory depression; + antipsychotics increases sedation, antimuscarinic effects, and alpha block; + MAOI is contraindicated because it will lead to hypertension and hyperpyrexic coma
Morphine, hydromorphone, oxymorphone, heroin
phenanthrenes
methadone, LAAM
phenylheptylamines
meperidine, fentanyl
phenylpiperidines
How is morphine given?
orally or IV
What potency does hydromorphone have with respect to morphine?
higher
What is heroin metabolized to?
morphine
Which other drug class do you give with codeine?
NSAIDs
Name two analogs of codeine.
oxycodone and hydrocodone
What is methadone for?
sever chronic pain and opioid addiction
What is LAAM?
long-acting analog of methadone
What drug class do you give with propoxyphene?
NSAIDs
How is meperidine given? what potency does it have with respect to morphine?
orally or IV; one-tenth
If meperidine is given IV it can cause what dangerous side effect?
tachycardia
Is fentanyl rapid acting or slow acting? What is its primary use?
rapid, anesthesia
What drug do you give with diphenoxylate?
atropine
What are mixed agonist-antagonist opioids?
They antagonize mu receptors but agonize kappa and delta.
Which receptor is pentazocine most active at? If it stimulates sigma receptors what side effect does it cause?
kappa; psychomimetic
What is the only oral mixed agonist-antagonist opioid?
pentazocine
Nalbuphine is a more potent antagonist at which receptor?
mu
Butorphanol is like which other mixed a-a opioid?
pentazocine
Buprenorphine is a partial agonist at which receptor? It is a more potent analgesic than which opioid?
mu; morphine
Opioid antagonists are analogs of which opioid?
morphine
How is naloxone administered? How is it metabolized?
IV, liver
How is naltrexone administered? What makes it different from naloxone? What about nalmefene?
orally, longer action; longer half-life
Tramadol is a weak agonist of which opioid receptor? What does it inhibit? What are its side effects?
mu; reuptake of norepinephrine and serotonin; seizures, dependence, withdrawal symptoms