Exam #01f - Opioids & Multi-MOA Analgesics Flashcards
Name (2) endogenous opioid peptides?
- endorphins
2. enkephalins
This term is defined as awareness of a sensory stimulus (pain that you can describe)?
sensation
This term is defined as the effect component of pain (how you think about a specific pain)
perception
Opioid receptors are distributed throughout the body including the CNS, PNS, GI tract, immune cells, and lung. What clinical relevance do opioid receptors in immune cells serve?
In vivo, morphine decreases immune function, however, there is no definitive evidence that giving morphine to cancer patients is inhibiting their immune function or giving fatal outcome
True or False - opioid receptors in the lungs cause respiratory depression?
False - nobody is sure why opioid receptors are in the lungs
List the steps of the opioid MOA?
- opioid binds to 7TM-GPCR
- binding activates Gi protein
- Gi inhibits adenylate cyclase
- this decreases [cAMP]
- this decreases intracellular Ca2+
- this results in decreased release of NT
The two primary sites of action of opioids are the presynaptic neuron and postsynaptic neuron. Explain what ions are affected at these two locations?
Presynaptic neuron - opioid binding inhibits Ca2+ influx and inhibits NT release
Postsynaptic neuron - opioid binding enhances K+ efflux and hyperpolarizes neuron
Name the (8) CNS effects of opioid binding to opioid receptors?
- analgesia
- euphoria
- sedation
- respiratory depression
- constipation
- cough suppression
- miosis
- N&V
True or False - all opioids inhibit cough due to opioid receptors in the brain stem and not the lungs?
True
Morphine activity is attributable to its (2) metabolites, morphine 6-glucuronide and morphine 3-glucuronide. Which metabolite can lead to CNS toxicity? If an individual forms one metabolite but not another, do this individual still get analgesic effect?
morphine 3-glucuronide can lead to CNS toxicity
yes
Name the (11) mu opioid receptor (MOR) agonists?
- morphine
- meperidine
- methadone
- hydromorphone
- heroin
- hydrocodone
- oxycodone
- oxymorphone
- fentanyl
- codeine
- buprenorphine
True or False - fentanyl is a good drug for both transdermal and epidural
True
Which MOR agonist is a prodrug for morphine?
Codeine
Which MOR agonist is approved for opioid abuse treatment as a transdermal patch?
Buprenorphine
Name the (2) MOR antagonists?
- Naloxone
2. Naltrexone
Which MOR agonist is used to treat “addicts?”
Methadone
Which MOR agaonist is used in CV surgery?
Fentanyl
Which MOR agonist causes the release of histamine: morphine or fentanyl?
Morphine causes release of histamine, fentanyl does NOT
Which MOR agaonist is used as a cough suppressant?
Codeine
Which (2) opioids are used as antidiarrheals?
- Diphenoxylate + atropine (Lomotil)
2. Loperamide (Imodium)
Which MOR agonist can cause a muscular rigidity SE?
fentanyl
Is Tramadol a centrally acting or peripherally acting analgesic?
Centrally acting
True or False - Tramadol is an NSAID
False - it is NOT
How does Tramadol’s dual mechanism of action differ from Tapentadol’s?
Tramadol - metabolite M1 opioid agonist and non-opioid component is NE & 5-HT reuptake inhibitor
Tapentadol is the same except it is only a NE reuptake inhibitor
