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NR565 Week 3 Midterm Study Guide
Advanced Pharmacology Fundamentals (Chamberlain University)
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Week 3: Midterm Study Guide
Sunday, May 18, 2025 9:47 AM
Week 3:
Chapter 24: Opioid analgesics, opioid antagonists, and nonopioid centrally acting analgesics
Pain
• Agonist-Antagonist Opioid Action
○ Acts as an agonists at K receptors and as an antagonist at µ receptors
○ Because of the limited agonist actions at µ receptors, these drugs produce little to no euphoria, and limited
respiratory depression
○ In supratherapeutic doses, the drugs can cause unpleasant reactions such as anxiety, nightmares, and
hallucinations
• Agonist-Antagonist Opioids
○ Pentazocine, nalbuphine, butorphanol, buprenorphine
○ Have a lower potential for abuse, produces less respiratory depression, and are less powerful than
analgesics.
○ Prototype: Pentazocine
○ These drugs should never be administered to someone who is physically dependent on pure opioid agonists
as it will precipitate withdrawal
○ Pure opioid agonists can still reverse these drugs as well.
• Opioid Peptides
○ The body has three families of peptides that have opioid-like properties:
§ Enkephalins
§ Endorphins
§ Dynorphins
○ Endogenous opioid peptides are found in the CNS and in peripheral tissues and serve has
neurotransmitters, neurohormones, and neuromodulators
§ However, their precise physiologic role is not fully understood
• Opioid Receptors
○ Three main classes
§ µ (Mu) -- Most important receptor pharmacologically, because opioid analgesics act primarily by
activating this receptor
• Activation of this site causes:
o Analgesia
o Respiratory depression
o Sedation
o Euphoria
o Physical dependence
o Decreased GI motility
§ K (Kappa) -- Opioid analgesics produce weak activation of these receptors
• Activation of these receptors causes:
o Analgesia
o Sedation
o Decreased GI motility
§ δ (Delta)
• Opioid analgesics do not interact with these receptors
• Opioids: Classification of Drugs
○ An opioid is any drug, natural, or synthetic, that has actions similar to those of morphine
○ Opiates are more specific and only applies to compounds present in opium
○ Drugs that act at opioid receptors are classified on the basis of how they affect receptor function
○ At each type of receptor, a drug can act in one of three ways:
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Agonist
NR565 Week 3 Midterm Study Guide
Advanced Pharmacology Fundamentals (Chamberlain University)
Scan to open on Studocu
Studocu is not sponsored or endorsed by any college or university
Downloaded by CHUNXU XIA ()
, lOMoARcPSD|46788506
Week 3: Midterm Study Guide
Sunday, May 18, 2025 9:47 AM
Week 3:
Chapter 24: Opioid analgesics, opioid antagonists, and nonopioid centrally acting analgesics
Pain
• Agonist-Antagonist Opioid Action
○ Acts as an agonists at K receptors and as an antagonist at µ receptors
○ Because of the limited agonist actions at µ receptors, these drugs produce little to no euphoria, and limited
respiratory depression
○ In supratherapeutic doses, the drugs can cause unpleasant reactions such as anxiety, nightmares, and
hallucinations
• Agonist-Antagonist Opioids
○ Pentazocine, nalbuphine, butorphanol, buprenorphine
○ Have a lower potential for abuse, produces less respiratory depression, and are less powerful than
analgesics.
○ Prototype: Pentazocine
○ These drugs should never be administered to someone who is physically dependent on pure opioid agonists
as it will precipitate withdrawal
○ Pure opioid agonists can still reverse these drugs as well.
• Opioid Peptides
○ The body has three families of peptides that have opioid-like properties:
§ Enkephalins
§ Endorphins
§ Dynorphins
○ Endogenous opioid peptides are found in the CNS and in peripheral tissues and serve has
neurotransmitters, neurohormones, and neuromodulators
§ However, their precise physiologic role is not fully understood
• Opioid Receptors
○ Three main classes
§ µ (Mu) -- Most important receptor pharmacologically, because opioid analgesics act primarily by
activating this receptor
• Activation of this site causes:
o Analgesia
o Respiratory depression
o Sedation
o Euphoria
o Physical dependence
o Decreased GI motility
§ K (Kappa) -- Opioid analgesics produce weak activation of these receptors
• Activation of these receptors causes:
o Analgesia
o Sedation
o Decreased GI motility
§ δ (Delta)
• Opioid analgesics do not interact with these receptors
• Opioids: Classification of Drugs
○ An opioid is any drug, natural, or synthetic, that has actions similar to those of morphine
○ Opiates are more specific and only applies to compounds present in opium
○ Drugs that act at opioid receptors are classified on the basis of how they affect receptor function
○ At each type of receptor, a drug can act in one of three ways:
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Agonist
