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27 Cards in this Set
- Front
- Back
- 3rd side (hint)
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What are 5 key sites of opiod action?
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cortex
thalamus hypothalamus periaqueductal gray area (PAG) (very important area) substantia gelatinosa |
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Match the endogenous opioid with its receptor:
1. endorphins 2. dynorphins 3. enkephalins (& endorphins) |
Mu (endorphins)
Kappa (dynorphins) Delta (enkephalin) |
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What are the effects of binding MOR's?
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analgesia (supraspinal)
euphoria respiratory depression dependence miosis GI effects (constipation) |
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Name the main KOR types?
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Buprenorphine and pentazoncine
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What are the strong opioid agonists?
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Strongest to weakest:
fentanyl methadone morphine meperidine codeine (moderate agonist) |
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What are the presynaptic and postsynaptic effects in opioid signal transduction?
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Pre- synaptic: decreased cAMP, Ca++ influx, glutamate release
Post-synaptic: increased K+ efflux |
Long version:
Pre: agonist binds mu --> + Gi protein --> -adenylyl cyclase --> dec cAMP --> dec. Ca++ influx --> no glutamate release --> no pain Post: agonist binds mu --> Gi --> open K+ channel --> K+ efflux --> hyperpol --> AMPA-R driven AP not generated |
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What is a full Mu agonist?
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morphine
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What are 2 top drugs for moderate pain?
Severe pain? |
moderate: codeine & tramadol
severe: morphine also methadone |
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Mu full antagonist
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naloxone
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1. How does morphine depress respiration?
2. What are 3 contraindications related to this dilemma? |
1. depress sensitivity to CO2 in the brainstem (dose-dep for rate, minute vol, & tidal exchange)
2. contra: brain injury, emphysema, HF |
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Opioid receptor and actions of Kappa (KOR) receptors
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Analgesia (spinal)
Sedation Miosis GI effects |
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Tolerance does not develop to what two effects of morphine?
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constipation
miosis (pin point pupils) |
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Opioid receptor and actions of Delta (DOR) receptors
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Analgesia (supraspinal and spinal)
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What are precautions for giving nursing mothers tylenol w/ codeine?
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codeine gets converted to morphine which gets metabolized via UGT (M36/M6G), CYP (Nor-M), & dehydrogenase (hydromorphone). The neonate cannot process these quickly --> bad --> maybe dead
Prescribe codeine ONLY 2-3 days |
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What is the DOC for anesthesia & breakthrough pain?
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Fentanyl
strong!, lipophilic (rapid distribution) transmucosal (breakthrough pain w/morphine- lollipop)) Transdermal patch (slow onset/delivery) |
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Rank the following from shortest to fastest based on onset/duration:
meperidine morphine fentanyl |
shortest to longest:
fentanyl meperidine morphine |
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What analgesic is useful in obstetric setting (labor) but is difficult to detect for abuse.
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Meperidine: short acting on uterus
Eyes: dilation (no pinpoint to detect abuse) Normeperidine is a toxic metabolite! seizures! |
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What are the 3 active metabolites of morphine?
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M6G
M3G hydromorphone |
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What opioid is useful for moderate pain & cough?
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codeine
(dextromethophan relieves cough independently of opioid receptors) |
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What drug is useful for maintenance & detox from heroin?
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methadone (long 1/2 life - 27 hrs vs. 2 hrs for morphine)
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What drug is a kappa agonist, mu/delta antagonist, causes supra-spinal analgesia, can precipitate withdrawal, & has SE's of tachycardia & hallucinations?
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pentazocine (mixed agonist/antag)
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What drug is a partial mu agonist, causes analgesia, can precipitate withdrawal, and is used as an OFFICE-based detox/maintenance drug?
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Buprenorphine
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What is the antidote for opioid overdose?
What is MOA? Negatives? |
naloxone: reverses coma/resp. depression (acts in 1 min for 1-2 hr duration) (given IV)
naltrexone has longer duration (48 hrs) antidoes can precipitate withdrawal! Occupy but do not activate Mu receptors |
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What opioids can be used as anti-diarrheals?
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loperamide & diphenoxylate
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In what system of brain do the mu opioids alter?
Main contra-indications for morphine? |
limbic system- emotion/euphoria
- also respiratory areas - BRAIN TRAUMA/INJURY , emphysema, heart failure |
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Which drug is DOC for doctors to abuse?
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meperidien due to non- dilation of pupils
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Why is heroin such a menace?
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Penetrates blood-brain barrier rapidly--> exaggerated euphoira--> addiction liability
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