Pharmacology - Opioids
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- 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
- 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