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57 Cards in this Set
- Front
- Back
- 3rd side (hint)
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Which neurotransmitter binds to the delta receptor
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Enkephalin
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Which neurotransmitter binds to the kappa receptor
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Dynorphin
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Which neurotransmitter binds to the mu receptor
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Beta-endorphin
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What is the mechanism of action of medications that activate presynaptic opioid receptors
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Inhibits calcium influx through voltage-gated ion channels thereby inhibiting neurotransmitter release
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None
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What is the mechanism of action of medications that activate postsynaptic opioid receptors
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Increases potassium efflux from cells leading to membrane hyperpolarization and thereby inhibition of neurotransmitter release
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None
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Opioid receptors are coupled to what type of proteins
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Inhibitory G-proteins (inhibits adenylyl cyclase)
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Binding of opioids to which receptor type may be responsible for the dysphoria and hallucinations associated with certain opioids
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Sigma receptor
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What is the prototype opioid analgesic
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Morphine
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None
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Why must caution be taken when using opioids in patients with head injuries
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Opioids may increase intracranial pressure
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Where in the midbrain are opioid receptors located
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Periaqueductal gray region (binding to these receptors leads to activation of descending pathways to the Raphe nuclei thereby decreasing transmission throughout pain pathways)
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None
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Where in the dorsal horn of the spinal cord are opioid receptors located
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Primary afferent fibers (binding to these receptors leads to inhibition of substance P release)
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None
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Are opioid analgesics better at relieving intermittent or persistent pain
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Persistent pain
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None
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What is the mechanism of morphine-induced hypotension and pruritus
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Increased histamine release from mast cells
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None
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Do opioid analgesics increase or decrease gastrointestinal (GI) peristalsis
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Decrease (causes constipation)
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None
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Which two opioids are used specifically to treat diarrhea
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Loperamide
Diphenoxylate |
None
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Which medication is commonly given in combination with diphenoxylate for the treatment of diarrhea
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Atropine
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Which opioid analgesic does not increase the tone of the biliary tract, bladder, and ureter
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Meperidine (antagonizes muscarinic receptors)
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None
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Do opioid analgesics increase or decrease uterine contractions during pregnancy
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Decrease
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None
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Do opioid analgesics cause miosis or mydriasis of the pupils
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Miosis (common sign of opioid overdose is pinpoint pupils)
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None
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What is the mechanism of opioid-induced miosis
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Increased parasympathetic (cholinergic) activity in the pupilary constrictor muscles
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None
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Which opioid analgesic does not cause miosis
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Meperidine (antagonizes muscarinic receptors)
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None
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Which two opioids are used specifically to treat cough
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Codeine; Dextromethorphan (opioids suppress the cough reflex)
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Is dextromethorphan a natural or synthetic opioid
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Synthetic
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What is the mechanism of opioid-induced urinary retention
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Increases antidiuretic hormone (ADH)
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None
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Do opioid analgesics promote emesis or act an antiemetics
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Promote emesis
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None
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What is the mechanism of opioid-induced emesis
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Activation of the chemoreceptor trigger zone (CTZ)
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None
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Where is the CTZ located
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Area postrema
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What is the mechanism of opioid-induced respiratory depression
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Reduced sensitivity of respiratory center to carbon dioxide levels
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None
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What is the most common cause of death in opioid overdose
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Respiratory depression
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None
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What are the two most lipophilic opioids
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Heroin; Fentanyl (these two medications rapidly cross the BBB to produce euphoric effects
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None
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Which opioid is the least lipophilic
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Morphine
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None
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Is morphine metabolized via phase I or phase II reactions
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Phase II (glucuronidation)
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Does morphine-3-glucuronide have analgesic activity
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No
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Does morphine-6-glucuronide have analgesic activity
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Yes
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Which two opioid-induced effects do patients not develop tolerance to
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Constipation; Miosis
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What are the signs and symptoms of opioid withdrawal
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Lacrimation
Rhinorrhea Diaphoresis Yawning Goose bumps Anxiety Muscle spasms Diarrhea Increased pain sensation |
None
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Which medication is used to counteract the respiratory depression seen in opioid overdose
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IV naloxone (may need to give multiple doses as naloxone has a shorter half-life than morphine)
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None
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What is the mechanism of action of naloxone
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Mu-receptor antagonist
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What is the half-life of naloxone
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1-1.5 hours
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What is the half-life of morphine
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2-4 hours
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Which opioid antagonist is given orally to decrease cravings in alcoholism
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Naltrexone
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None
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What is the half-life of naltrexone
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4 hours
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Which opioid analgesic is used to prevent withdrawal symptoms in patients discontinuing heroin use
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Methadone
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None
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Which central-acting α2 agonist is used to prevent withdrawal symptoms in patients discontinuing heroin use
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Clonidine
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Give examples of strong opioid agonists
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Morphine
Heroin Hydromorphone Methadone Meperidine Fentanyl Hydrocodone |
None
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Give examples of weak opioid agonists
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Codeine
Propoxyphene |
None
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Give examples of partial opioid agonists
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Buprenorphine
Pentazocine |
None
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What is the mechanism of action of pentazocine
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Kappa-receptor agonist
Mu-receptor antagonist |
None
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Propoxyphene is a derivative of which opioid analgesic
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Methadone
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None
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Name two synthetic opioid analgesics
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Methadone
Meperidine |
None
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Fentanyl is chemically related to which synthetic opioid analgesic
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Meperidine
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None
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Does morphine have a high or low oral bioavailability
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Low
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Which two opioids should not be given in combination with MAOIs
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Meperidine and Dextromethorphane (these combinations may produce serotonin syndrome)
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What drug do you get by acetylating morphine
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Heroin
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None
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Is codeine itself an active opioid analgesic
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No (must be metabolized via cytochrome P-450 2D6 to active morphine)
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None
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Which medication is commonly given in combination with codeine for the treatment of pain
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Acetaminophen
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Which medication is commonly given in combination with propoxyphene for the treatment of pain
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Acetaminophen
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