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Opioid Analgesia - Steve Fitzjohn

Anna mph Neuropharmacology Degree Inglés 36 fichas

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  1. 1Define nociceptionDetection of noxious stimuli
  2. 2Give 4 examples of substances which cause pain signalsH+
    Histamine
    NGF
    Prostaglandin
  3. 3Where do first order neurons of the lateral spinothalamic pathway synapse?Substantia gelatinosa
  4. 4Where do second order neurons of the lateral spinothalamic tract decussate?Spinal Cord
  5. 5How to voltage gated calcium channel blockers work?Reduce transmission from primary to secondary neuron
  6. 6How do cannaboid CB1 receptor agonists reduce pain?Inhibit activation of primary neuron
  7. 7How do non-steroidal anti-inflammatory drugs reduce pain?Prevent action of prostaglandin
  8. 8Define OpiateNaturally occurring agonists of opioid receptors
  9. 9Define opioidAny drug that acts on the opioid receptor
  10. 10What subtype of G protein are most opioid receptor actions mediated through?Gi/o
  11. 11What does the 'a' subunit do when the Gi/o protein is activated?Decreases cAMP
  12. 12What are the two main effects of BY subunit?i) Inhibits Ca2+ voltage gated channel, reducing influx of calcium, preventing neurotransmitter release
    ii) Activates voltage gated K+ channel, increased outward K+ current leads to reduced postsynaptic excitability
  13. 13Summarise the 3 main effects of opioid receptors?1) Inhibit transmitter release
    2) Inhibit neuronal firing
    3) Disinhibition (removal of inhibitory influence causes excitation)
  14. 14Which amino acid forms the main structural part of opioids?Tyrosine
  15. 15Which opioid receptors does y-endorphin bind to?u/d
  16. 16met-enkephalind/u
  17. 17Leu-enkephalind/u (partial at u)
  18. 18dynorphink
  19. 19Which subtype of receptor doesn't allow exogenous receptors to bond? What is the start of the endogenous peptide that does bond?ORL1
    Phenalamine
  20. 20Which drug is a non-selective antagonist at all opioid receptor subtypes?Naloxone
  21. 21Which subtype of receptor is the most important target for analgesia?u
  22. 22What are the four main behavioural responses to u receptor activation?analgesia, euphoria, respiratory depression, constipation
  23. 23What are the four main behavioural responses of k receptor activation?Analgesia, dysphoria/hallucinations, no respiratory depression, diuresis
  24. 24What are the three main behavioural of delta receptor activation?Analgesia, antidepressant, proconvulsant
  25. 25What other important side effects are caused by opioids? (4)Addiction, tolerance, nausea/vomiting, sedation
  26. 26What are the three main general problems with opiods?Side effects
    Breakthrough pain
    Neuropathic pain is resistant to opioids
  27. 27How are opioids most important pre and post synaptically?Pre synaptically: Inhibition of VG Ca2+ channels
    Post-synaptically: Activation of VG K+ channels
  28. 28Name two places in the CNS where injection of opioids reduces pain?1) Dorsal horn of spinal cord
    2) Peri Aquaductal Grey
  29. 29How does injecting into PAG reduces pain?Activation of descending inhibitory pathways
  30. 30Explain in terms of GABAergic neurons and projection neurons how opioids cause disinhibition and how this causes analgesia.Tonically active GABAergic can be stopped from firing by opioids. Disinhibits projection neuron which was inhibited by GABAergic neuron. Second order projection neuron is then able to inhibit second order neurons in the spinal cord and prevent pain transmission.
  31. 31How do opioids induce euphoria?Disinhibition to Ventral Tegmental Area (VTA)
    Enhances dopamine release in the nucleus accumbens
  32. 32Which receptors are mainly responsible for analgesia, addiction/withdrawal to morphine?u
  33. 33What are the three main uses for opioids?Pain Relief
    Treatment of severe diarrhoea
    Cough supression
  34. 34What are the four types of pain opioids treat?Acute
    Chronic (eg cancer)
    During surgery
    Post-operative surgery
  35. 35What is BuprenorphinePartial agonist
  36. 36What are the clinical uses of Buprenorphine? (high and low doses) (3)1)Treatment of morphine addiction at high doses
    2)Treatment of moderate acute pain lower doses
    3) Treatment of moderate chronic pain at even lower doses

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Degree Neuropharmacology Fichas sobre Opioid Analgesia - Steve Fitzjohn, creado por Anna mph el 14/12/2015.
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