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18 Cards in this Set
- Front
- Back
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Opiate |
Naturally occurring substances
Agonists only |
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Opioid |
Any substance that interacts with opioid receptor
Agonists/antagonists |
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Classical opioid receptors |
Mu Delta Kappa
ORL1 not important in pain relief |
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Opioid receptor mechanism |
GPCR
Gi/o subunit
Opens potassium channel - hyperpolarisation, inhibit neural firing
Close calcium channel - inhibits transmitter release |
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Descending inhibition |
Removal of inhibitory influence causes excitation |
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Opioid structure always starts with... |
Tyrosine (Tyr) |
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Morphine |
Selective (partial) agonist for μ receptors |
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Naloxone |
μ, δ and K antagonist
Blocks all 3 receptors but more potent at μ |
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Pentazocine |
μ antagonist and K agonist |
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μ receptor effects |
Analgesia Euphoria Respiratory depression Constipation |
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K receptor effects |
Analgesia Dysphoria/hallucinations Diuresis |
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δ receptor effects |
Analgesia Antidepressant Proconvulsant |
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Opioid unwanted effects |
Side effects - nausea, constipation, sedation, respiratory depression
Breakthrough pain
Neuropathic pain resistant |
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Codeine |
Weaker analgesic |
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Oxycodone |
Oral slow release tablets |
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Methadone |
Long acting, suppress withdrawal |
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Fentanyl and remifentanyl |
Anaesthesia and sedation |
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Tramadol |
Weak μ agonist NA uptake inhibitor |
