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51 Cards in this Set
- Front
- Back
Inhibit synaptic activity of primary afferents and spinal cord pain transmission neurons
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Ascending pathways
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Activation of these receptors close Ca2+ ion channels to inhibit neurotransmitter release
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Presynaptic mu, delta, and kappa receptors
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Activation of these receptors open K+ ion channels to cause membrane hyperpolarization
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Postsynaptic Mu receptors
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All opioids except this agent (which has a muscarinic blocking action) cause pupillary constriction
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Meperidine
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SE of these drugs include dependence, withdrawal syndrome, sedation, euphoria, respiratory depression nausea and vomiting, constipation, biliary spasm, increased ureteral and bladder tone, and reduction in uterine tone
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Opioid Analgesics
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Opioids used in anesthesia
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Morphine and fentanyl
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Opioid used in the management of withdrawal states
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Methadone
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Opioid available trans-dermally
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Fentanyl
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Opioid that can be given PO, by epidural, and IV, which helps to relieve the dyspnea of pulmonary edema
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Morphine
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Use of this opioid with MAOI can lead to hyperpyrexic coma, and with SSRI's can lead to serotonin syndrome
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Meperidine
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Moderate opioid agonists
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Codeine, hydrocodone, and oxycodone
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Weak opioid agonist, poor analgesic, its overdose can cause severe toxicity including respiratory depression, circulatory collapse, pulmonary edema, and seizures
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Propoxyphene
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Partial opioid agonist, considered a strong analgesic, has a long duration of action and is resistant to naloxone reversal
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Buprenorphine
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Opioid antagonist that is given IV and had short DOA
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Naloxone
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Opioid antagonist that is given orally in alcohol dependency programs
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Naltrexone
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These agents are used as antitussive
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Dextromethorphan, Codeine
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These agents are used as antidiarrheal
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Diphenoxylate, Loperamide
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Oral med for increasing pain in met bone CA pt who is receiving oxycodone + acetominophen?
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levorphanol (strong agonist)
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Tolerance doesn't develop to a significant extent with respect to (2)
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constipation, miosis
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The ionic mech involved in inhibition of release of NTs
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decreased influx of Ca ions
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Over-the-counter opioid with antidiarrheal action
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loperamide
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Fentanyl patches used to provide analgesia have caused what SE?
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respiratory depression
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Merperidine plus what drug causes a reaction consisting of tachycardia, HTN, hyperpyrexia and seizures?
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phenelzine (MAOI)
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Merperidine plus SSRI causes what reaction?
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serotonin syndrome
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Genetic polymorphism in drug metab is est to be responsible for variations in analgesic response to what agent?
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codeine
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Morphine is contraindicated or to be used with extreme caution in what 4 clinical situations?
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adrenal insuff, biliary tract surgery, hypothyroidism and late stage labor
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Most likely cause of the following signs and sx in a heroid addict: chills, muscle aches, diarrhea, vomiting, hypervent and hyperthermia
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abstinence syndrome
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Which drug is most effective in alleviating sx of abstinence syndrome?
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buprenorphine
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T or F about nalbuphine? activates mu receptors
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FALSE
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T or F about nalbuphine? doesn't cause resp depression
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FALSE; however is less likely than with mu activators
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T or F about nalbuphine? is nonsedating
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FALSE
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T or F about nalbuphine? pain-relieving action is not superior to that of codeine
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false; superior to codeine but inferior to strong agonists
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T or F about nalbuphine? response to naloxone in overdose may be unreliable
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TRUE
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Which drug doesn't activate opioid receptors and with a single oral dose will block effects of injected heroin for 48 h?
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Naltrexone
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T or F about dextromethorphan? activates kappa receptors
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FALSE; activates mu receptors
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T or F about dextromethorphan? analgesia equivalent to pentazocine
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FALSE; has no analgesic activity
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T or F about dextromethorphan? highly effective antiemetic
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FALSE
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T or F about dextromethorphan? less constipation than codeine
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TRUE
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T or F about dextromethorphan? no abuse potential
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FALSE; causes disorientation, hallucinations, seizures and death in large amounts
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Full agonist drug with good oral bioavail, analgesic activity equivalent to morphine, longer duration of action and milder withdrawal signs:
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methadone
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T or F about propoxyphene? analgesia equivalent to oxycodone
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FALSE; very low analgesic activity
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T or F about propoxyphene? antagonist a mu receptors
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FALSE; weak agonist
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T or F about propoxyphene? causes dose limiting diarrhea
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FALSE
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T or F about propoxyphene? highly effective cough suppressant
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FALSE
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T or F about propoxyphene? seizures in overdose
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TRUE; overdose causes seizures, PE, circulatory collapse, resp depression
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Opioids effect what 3 pain pathways?
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transmission (ascending), modulation (descending) and reactivity (basal ganglia, hypothalamus, limbic and cortex)
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Which opioid has muscarinic blocking acton?
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meperidine
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strong agonists (6)
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morphine, fentanyl, heroin, levorphanol, meperidine, methadone
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weak agonist
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propoxyphene
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mixed agonist-antagonists (4)
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pentazocine, buprenorphine, butorphanol, nalbuphine
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antagonists (3)
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naloxone, nalmefene, naltrexone
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