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24 Cards in this Set
- Front
- Back
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codeine
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opioid agonist. Prodrug, converted to morphine by CYP2D6. in combo with acetaminophen=Tylenol#3. weak, mild, a lot of variablity, not tolerated well. (as in any combo, acetaminophen limits dosing because of toxicty)
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fentanyl (Duragesic)
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opioid agonist. Patch, oral (lollipop, sublingual), epidural, intrathecal/subarachnoid. Really potent, lipid soluble/fast onset
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heroin
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opioid agonist. Diacetyl morphine. Pro drug converted to monoacetyl morphine and morphine in the brain. RAPID onset, analgesia and euphoria.
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hydrocodone (Vicodin)
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opioid agonist. Not active until metabolized to hydromorphone by CYP2D6. Combined with acetaminophen to make Vicodin and Lortab.
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hydromorphone (Dilaudid)
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opioid agonist. IV, PO. 5x more potent than morphine. More lipid soluble, faster onset. Hydromorphone-6-glucuronide less potent than M-6-glucuronide. H-3-G also inactive.
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meperidine (Demerol)
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opioid agonist. IV, PO. Faster onset than morphine, 10x LESS potent. Converted in liver to nor-meperidine which stimulates CNS-convulsions. Nor-meperidine 1/2 life extended (48hrs) in pts with renal failure. Use has decreased despite increased use of other opioids
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morphine
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opioid agonist. Slow onset of action. Clinical duration of single dose is 4 hrs (long). glucuronidation in liver, metabolites excreted in kidney. M-6 glucuronide 10x more potent, active metabolite. M-3-glucuronide inactive metabolite. Inexpensive, familiar. PO needs 3-5 more than IV
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methadone (Dolophine)
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opioid agonist. Oral. Ultra long acting (1/2 life 15-60hrs) used for opioid addiction (to prevent withdrawal). Also for chronic pain because less likely to be abused and pts don’t seem to get as tolerant as fast
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oxycodone (Oxycontin)
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opioid agonist. Metabolized to oxymorphone by CYP2D6. combined with acetaminophen to make percocet. Frequent drug of abuse.. Crushed pills are dangerous
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oxymorphone (Opana)
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opioid agonist. Available in extended release formula
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propoxyphene (Darvon)
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opioid agonist. Pro drug converted to morphine; weak analgesic efficacy (like tylenol#3) combined with acetaminophen=darvocet. [do not use]?
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buprenorphine (Buprenex)
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mixed opiod agonist/antagonist. Partial mu receptor agonist/antagonist. High affinity for mu receptor, kappa receptor agonist. Difficult to reverse agonist effect: useful to treat drug abuse, bad because difficult to provide analgesia for surgery if they have it.
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nalbuphine (Nubain)
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mixed opiod agonist/antagonist. Kappa receptor agonist and mu receptor partial agonist/antagonist. Used to manage short term, acute pain and side effects
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pentazocine (Talwin)
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mixed opiod agonist/antagonist. Kappa receptor agonist and mu receptor partial agonist/antagonist. Used to manage short term, acute pain and side effects
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tramadol (Ultram)
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mixed opiod agonist/antagonist. Partial mu agonist and monoamine uptake inhibitor (potentiates seretonin and norepi) combined with acetaminophen to make Ultracet
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naloxone (Narcan)
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opioid antagonist. Parenteral - prevent/antagonize opioid drugs. Can be used to treat EtOH
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naltrexone (Revia)
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opioid antagonist. Parenteral - prevent/antagonize opioid drugs. Can be used to treat EtOH
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alvimopan (Entereg)
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opioid antagonist. Poorly absorbed orally. Active opioid antagonist antagonizes GI sdie effects of opioids (gets rid of illeus after morphine dosing)
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diphenoxylate (Lomotil)
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antidiarrheal opioid. Poorly absorbed, stay in GI tract. Decrease secretions and motility
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loperamide (Imodium)
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antidiarrheal opioid. Poorly absorbed, stay in GI tract. Decrease secretions and motility
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drugs with active metabolites
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morphine, hydrocodone, oxycodone, codeine, meperidine, heroin, propoxyphene
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CYP 2D6 polymorphism
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rapid vs slow metabolizers (lack fxnl CYP2D6) mean variable response to opioids
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butorphanol
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kappa receptor agonsist and mu receptor partial agonist/antagonist. Used for acute, short term pain.
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mu opioid receptor agonist fxn
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influences motivaitonal-affective component of pain. Brain effects: analgesia, euphoria, resp depression, urinary retention, sedation.
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