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37 Cards in this Set
- Front
- Back
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What is pain?
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"An unpleasant sensory and emotional experience associated with actual or potential tissue damage, or described in terms of such damage"
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What is analgesia?
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absence of pain in response to stimulation which would normally be painful.
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What is released in injury or tissue damage?
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bradykinin (BK)
prostaglandins (PG) |
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What do BK and PG do?
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They sensitize nociceptors,
leads to substance P release |
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What is the role of substance P?
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- It act on mast cells to degranulate and release histamine (excites nociceptors)
- dilation of peripheral blood vessels (edema...BK) |
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What is a drug that produces sleep?
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Narcotic
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What is a drug that is derived from opium?
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Opiate
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What is a drug that binds to opioid receptors?
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Opioid
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What are 5 types of drugs used in acute pain?
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1. Acetaminophen
2. ASA, NSAIDS 3. Opiod analgesics 4. Combination preparations (acetaminophen + codeine) 5. Local anesthetics |
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What are the 4 types of opioid receptors?
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Mu1
Mu2 Delta Kappa |
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What receptor does morphine work on?
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Mu1, Mu2
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What receptor do enkephalins work on?
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Delta
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What receptor does dynorphin A work on?
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Kappa
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What are some sites of action for opioids?
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Brain
Brainstem Spinal cord Primary afferent neurons Medullary respiratory center Medullary chemoreceptor zone GI tract |
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Do opioids hyperpolarize or stimulate action potential?
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Opioids hyperpolarize postsynaptic neurons by opening K+ channels
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How do opioids reduce inflammatory transmitter release?
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Presynaptically close the Ca2+ channels
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T/F: Opioids activate inhibitory enkephalin interneurons in the dorsal horn of the spinal cord
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True
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T/F: Opioids inhibit glycinergic interneurons
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False
Opioids inhibit GABAergic interneurons (that normally suppress descending pathways) |
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What are 4 methods opioids can come from?
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1. Natural alkaloids extracted from opium (morphine)
2. Synthetic opioids (methadone) 3. Endogenous opioid peptides (enkephalins) 4. Synthetic opioid peptides (DAMGP) (last 2 not used clinically) |
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What are: beta-endorphin, leu-enkephalin, dynorphin?
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Endogenous opioid peptides
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What is the proposed action of kappa receptor binding?
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- spinal analgesia
- sedation |
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What is the proposed action of delta receptor binding?
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spinal analgesia
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What is the proposed action of mu1 receptor binding?
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supraspinal analgesia
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What is the proposed action of mu2 receptor binding?
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respiratory depression
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What are the 3 modes of delivery?
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1. systemic (PO, IV, PR...)
2. neuraxial (spinal, epidural) 3. local (intra-articular) |
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Which drug has better oral bioavailability: morphine, codeine?
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Codeine (60%)
(morphine = 25%) |
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Which drug has high lipid solubility and BBB penetration?
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Heroin
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What two drugs are metabolized to morphine?
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Heroin
Codeine |
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How is morphine metabolized?
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to morphine-3-glucuronide (excitatory and toxic)
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How is morphine excreted?
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90% glucuronides (urine)
10% unchanged (bile, feces) |
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What are some central effects of opioids?
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analgesia (hyperalgesia)
euphoria (dysphoria) sedation respiratory depression nausea/vomiting |
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What are some peripheral effects of opioids?
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histamine release (mast cell degranulation)
hypotension (vasodilation) bradycardia constipation |
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T/F: there are only 3 therapeutic uses for opioids.
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False
1. Analgesia (morphine) 2. Cough suppression (codeine) 3. Antidiarrheal therapy (loperamide) 4. Acute pulmonary edema (IV morphine) |
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What are naloxone and naltrexone?
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Antagonists at mu/delta/kappa receptors
(they rapidly reverse agonist effects - used for overdose) |
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What is tolerance?
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Increase in dose required to produce a given pharmacologic effect.
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What is dependence?
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Occurrence of withdrawal symptoms (physical) and/or craving for the drug (psychological).
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What are some contraindications for opioids?
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- respiratory disease
- drug interactions (MAO inhibitors, sedatives) - pregnancy |
