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Questions and Answers
Which neurotransmitter is NOT mentioned as blocking the transmission of pain signals at the 'pain gate'?
Which neurotransmitter is NOT mentioned as blocking the transmission of pain signals at the 'pain gate'?
- Serotonin
- Opiates
- Norepinephrine
- Dopamine (correct)
Which of the following is used to reverse an overdose?
Which of the following is used to reverse an overdose?
- Pentazocine
- Tramadol
- Buprenorphine
- Naloxone (correct)
Opioids can help influence cognitive and emotional processing.
Opioids can help influence cognitive and emotional processing.
True (A)
Fentanyl and its derivatives are less potent than morphine.
Fentanyl and its derivatives are less potent than morphine.
What is the function of endorphins?
What is the function of endorphins?
What effect does naltrexone have on heroin?
What effect does naltrexone have on heroin?
Opium is derived from the juice of the ______ plant.
Opium is derived from the juice of the ______ plant.
Match the following opioid receptors with their respective endogenous ligands:
Match the following opioid receptors with their respective endogenous ligands:
_______ is a weak Mu antagonist combined with Kappa Agonists and serves as an analgesic.
_______ is a weak Mu antagonist combined with Kappa Agonists and serves as an analgesic.
What is the primary use of gabapentin and pregabalin?
What is the primary use of gabapentin and pregabalin?
Match the following medications with their respective classifications:
Match the following medications with their respective classifications:
Which of the following statements about Suboxone is correct?
Which of the following statements about Suboxone is correct?
Laudanum is a mixture of opioids and caffeine.
Laudanum is a mixture of opioids and caffeine.
Partial Mu Agonists have a higher risk of respiratory depression compared to full agonists.
Partial Mu Agonists have a higher risk of respiratory depression compared to full agonists.
Name one effect of kappa receptors when activated.
Name one effect of kappa receptors when activated.
Flashcards
Pain Pathway
Pain Pathway
The route pain signals travel from sensory nerve endings to brain regions processing pain and the feeling associated with pain.
Opioid Receptors
Opioid Receptors
Specialized protein binding sites in the brain and body, including the spinal cord, that respond to endogenous (produced by the body) or exogenous (drug-derived) opioids.
Analgesia
Analgesia
The relief or lessening of pain.
Mu Opioid Receptor
Mu Opioid Receptor
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Endogenous Opioid
Endogenous Opioid
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Opiate
Opiate
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Descending Antinociceptive Pathways
Descending Antinociceptive Pathways
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Opioid Agonist
Opioid Agonist
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Morphine
Morphine
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Naloxone (Narcan)
Naloxone (Narcan)
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Partial Mu Agonist
Partial Mu Agonist
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Buprenorphine (Subutex)
Buprenorphine (Subutex)
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Suboxone
Suboxone
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Fentanyl
Fentanyl
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Naltrexone
Naltrexone
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Study Notes
Pain Pathways
- Pain signals travel from free nerve endings to the spinal cord, then to the thalamus, and finally to the somatosensory cortex (location of pain).
- Emotional and cognitive aspects of pain are processed through free nerve endings, spinal cord, thalamus, hippocampus, amygdala, and cingulate cortex.
Anti-Pain Pathways
- Anti-pain pathways originate in the midbrain.
- Serotonin and norepinephrine block pain signals at the "pain gate."
- Opioids enhance the effect of serotonin and norepinephrine.
Decreasing Pain with Drugs
- Reducing inflammation (aspirin, NSAIDs)
- Inhibiting nociceptor excitation (gabapentin, pregabalin)
- Decreasing neurotransmitter release (opioids)
- Activating anti-pain pathways (antidepressants, opioids)
- Influencing cognitive and emotional processing (opioids)
Terminology
- Opium: Juice of the opium poppy.
- Narcotic: Any drug inducing sleep.
- Opiate: Drug extracted from opium (e.g., morphine, codeine).
- Opioid: Endogenous ligand binding opioid receptors (e.g., endorphins, enkephalins, dynorphins); now used for both natural and synthetic drugs targeting opioid receptors.
Opium Source and History
- Found in the Papaver somniferum plant.
- Native to Eurasia.
- Used for approximately 7000 years.
- Combined with alcohol to make laudanum.
- Hypodermic injection (1856) led to issues (e.g., "soldiers' disease").
Opioids (e.g., enkephalin)
- Functions: Analgesia, sleep, antitussive, regulates intestinal motility.
- Synthesis: Made from precursor polypeptides, cleaved by proteases.
- Examples of precursor-product pairs: POMC → Endorphin, Proenkephalin → Enkephalin, Proendorphin → Endorphin, Dynorphin.
- Receptors: Metabotropic (MU, KAPPA, DELTA).
- Endogenous ligands: Endorphin, Dynorphin, Enkephalin.
- Exogenous ligands: Morphine, Naloxone, Salvinorin A, Pentazocine (weak mu agonist), Kratom (partial mu agonist).
Opioid Drugs
- Pure Agonists (mu): Morphine, codeine, heroin, methadone, meperidine (Demerol), Fentanyl (80-500x more potent than morphine).
- Mu antagonists: Naloxone (Narcan; overdose reversal), Naltrexone (ReVia, Trexan; treatment to curb heroin effectiveness).
- Partial Mu Agonists: Buprenorphine (Subutex), Tramadol (Ultram; blocks norepinephrine reuptake, releases serotonin, active metabolite extends effects).
- Mixed Agonist-Antagonists: Pentazocine (Talwin; analgesic but dysphoria limits usefulness).
- Suboxone: Buprenorphine + naloxone (orally inactive naloxone, active injected form).
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