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pain reliever. A drug that inhibits painful stimuli or the perception of pain. |
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a drug that is physically addictive with repeated use. Narcotic analgesics are similar to opium (opiate drugs). |
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are derived from the poppy plant |
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similar in structure to morphine |
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Prevent or interrupt moderate to severe pain of any origin without a loss of consciousness |
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during or after surgical procedures |
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any etiology from back pain to cancer pain |
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extracted from poppy seeds (Papaver somniferum) |
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Euphoria Analgesia Sedation Relief from diarrhea Cough suppression |
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drug extracted from the exudate of the poppy |
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is a natural or synthetic drug that binds to opioid receptors prod“opioid” ucing agonist effects |
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derivatives of thenaturally occurring plant substance opium (semi-synthetic)OR synthetic substances that produce the same pharmacologic effects as opium |
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phenanthrene morphine 10% codeine 0.5% thebaine 0.2% |
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heroin oxymorphone Hydromorphone |
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meperidine methadone morphinians benzamorphans |
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Morphine Heroin Hydromorphone Fentanyl Codeine Hydrocodone |
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Pain is composed of two elements |
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Definition
localized stimulation of peripheral nerves through damage or inflammation and recognition of pain within the CNS that can intensify the reaction to pain |
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the mechanism whereby pain peripheral stimuli are transmitted to the central nervous system. |
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Polymodal nociceptors (PMN) |
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Definition
the main type of peripheral sensory neuron that responds to pain stimuli. |
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Definition
endings respond to thermal, mechanical and chemical stimuli. |
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Activation of peripheral nociceptive fibers |
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Definition
causes release of substance P and other pain-signaling neurotransmitters from nerve terminals in the dorsal horn of the spinal cord |
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Release of pain-signaling neurotransmitters |
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Definition
regulated by endogenous endorphins or by exogenous opioid agonists by acting presynaptically to inhibit substance P release, causing analgesia |
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analgesics relieve pain by selectively acting on receptors within the CNS |
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decrease anxiety reduce the reaction to pain interrupt pain signal transmission within the spinal cord |
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they are at areas concerned with pain and receptor locations beginning with highest concentration areas |
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Opioid Receptors location |
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Definition
cerebral cortex,amygdala, septum, thalamus, hypothalamus, midbrain, spinal cord |
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Definition
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action of endorphins produced in the brain and spinal cord by selectively stimulating receptors |
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receptors mediate analgesia, euphoria, and respiratory depression |
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receptors mediate sedation, dysphoria |
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receptors mediate hallucinations, and increased respiration and blood pressure |
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show poor analgesia and little addictive potential |
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May regulate mu receptor activity Believed to cause hallucinations |
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Located outside spinal cord Responsible for central interpretation of pain |
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Located throughout CNS Responsible for respiratory depression, spinal analgesia, physical dependence, and euphoria |
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Only modest analgesia Little or no respiratory depression Little or no dependence Dysphoric effects |
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Definition
has affinity for binding plus efficacy |
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Definition
has affinity for binding but no efficacy; blocks action of endogenous and exogenous ligands |
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Definition
produces an agonist effect at one receptor and an antagonist effect at another |
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has affinity for binding but low efficacy |
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Morphine *Heroin *Hydromorphone *Fentanyl *Codeine |
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Drowsiness and lethargy Apathy Cognitive impairment Sense of tranquility |
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Depression of respiration |
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Main cause of death from opioid overdose Combination of opioids and alcohol is especially dangerous |
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Opioids suppress the “cough center” in the brain |
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pupillary constriction in the presence of analgesics is characteristic of opioid use |
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Stimulation of receptors in an area of the medulla called the chemoreceptor trigger zone causes nausea and vomiting Unpleasant side effect, but not life threatening |
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Gastrointestinal symptoms |
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Opioids relieve diarrhea as a result of their direct actions on the intestines |
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Opioids can release histamines causing itching or more severe allergic reactions including bronchoconstriction Opioids can affect white blood cell function and immune function |
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Pharmacological Effects on CNS |
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Definition
Change in mental alertness, sedation (μ, κ) Change mood, euphoria (µ) or dysphoria (κ) Stimulation of chemoreceptor trigger zone initiating nausea and vomiting Dose dependent depression of the vomiting center Depression of respiratory centers (µ) Headache Cough suppressant (antitussive) Secretion of antidiuretic hormone |
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