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