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37 Cards in this Set
- Front
- Back
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What is the active compound in opioid analgesics?
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Morphine
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What drug is used to antagonize the effects of all opioid agents?
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Naloxone
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Is naloxone a competitive or non-competitive antagonist for opioid receptors?
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Naloxone is a competitive inhibitor
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What is the MOA of pentazocine?
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Pentazocine acts as an agonist at Kappa receptors and an antagonist at Mu opioid receptors.
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This category of opioids has an analgesic ceiling effect.
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Mixed agonist/antagonist opioids
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What is the most significant danger associated with using mixed agonist/antagonist opioids?
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Mixed agents such as pentazocine act as antagonists at the Mu receptors. If a patient is currently taking codeine or another Mu agonist this can out compete and cause withdrawal.
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Give an example of a partial opioid agonist.
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Buprenorphine
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T/F Opioids undergo significant first past metabolism.
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True
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Do opioids cross the placenta or the BBB?
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Yes and yes
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Name two opioids that have toxic metabolites.
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Meperidine (normeperidine) and Propoxyphene (norpropoxyphene)
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At what receptor do most currently available opioids act?
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Mu receptors in the brain and spinal cord.
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Give four general effects of opioids.
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Analgesia, Euphoria, Sedation(no amnesia), Respiratory depression, cough suppression, miosis, truncal rigidity, GI, biliary tract, histamine release
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What opioid is most often used as a cough suppressant?
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Codeine
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Which of the opioids are most likely to cause constipation?
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Codeine
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What opioid has the largest effect on histamine release?
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Morphine (addicts will always be messing with their nose bc of this)
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Name four clinical uses for opioids.
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Analgesia, Acute pulmonary edema, Cough, Diarrhea, Anesthesia
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What is the drug of choice for maintenance and/or managed withdrawl from opioids?
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Methadone
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Name the four drugs used for maintenance and/or managed withdrawl from opioids?
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Methadone, LAAM, Buprenorphine, Clonidine(non opioid)
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What is the "gold standard" opioid?
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Morphine (no ceiling, t1/2 >30min., multiple dosage forms, least expensive, high 1st pass)
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Name four phenanthrenes.
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Morphine, Oxymorphone, Hydromorphone, Hydrocodone, Heroin
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What route of administering codeine is contraindicated?
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Codeine should not be given IV because this can cause hypotension
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What are the components of Tylenol #3?
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Acetaminophen and Codeine
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How should you change a pts. dose of codeine when switching from the parenteral to the oral route?
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No change
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What type of opioid is Nalbuphine?
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Nalbuphine is a mixed agonist/antagonist.
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T/F Morphine is more potent than fentanyl.
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False fentanyl is 100x more potent than morphine.
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This opioid is known for causing the "rigid chest" phenomenon.
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Fentanyl. Treat with naloxone or paralyzation.
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These opioids are only useful in the treatment of diarrhea.
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Diphenoxylate and loperamide
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What does the DM on a cough syrup bottle stand for?
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Dextromethorphan
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Dextromethorphan is an isomer of what compound?
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Levorphanol
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What is the only current medical use for dextramethorphan?
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Dextramethorphan is used as an antitussive.
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What is unique about butorphanol?
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Butorphanol is an opioid that can be used as a nasal spray to treat migraine headaches. Don't use in elderly.
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What is the classic mixed agonist-antagonist?
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Pentazocine - agonist at kappa and a weak mu antagonist
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What is the prototype drug for opioid partial agonists?
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Buprenorphine
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What is the problem with giving many opioids po?
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Many opioids undergo extensive 1st past effect.
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Which of morpines metabolites are more active than morphine?
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M6 Gluc
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T/F Buprenorphine is not as strong as morphine.
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False buprenorphine is 25-50x as potent as morphine
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Ehat is the brand name for propoxyphene?
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darvan
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