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26 Cards in this Set
- Front
- Back
Physiology of pain (Excitatory example)
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substance P in primary sensory afferents
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Physiology of pain (Inhibitory example)
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GABA, endogenous opiod peptides
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Endogenous opiod peptides
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Inhibitory transmitters which modify pain transmission and perception: endogenous analgesics.
Modulate hormonal fluctuations. Pentapeptides are name of them. Located on presynaptic and postsynaptic sites in pain pathways. |
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Opiod receptors ___ neuronal activity
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inhibit
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Endogenous opiod peptides are ____ during stress or anticipation
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released
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Mu receptors (Morphine)
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mediate analgesia, well-being (euphoria), respiratory depression, physical dependence.
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Delta receptors
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Mediate tolerance and analgesia.
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Kappa receptors
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analgesia, sedation, and psychotic effects, miosis
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Morphine and exogenous opioid analgesics
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Opiod receptor agonists!!
Inhibit pain pathway from peripheral sensory receptors to limbic system. Pattern of effect depends on agonist activity. Concentrated in the GI tract. |
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Codeine, propoxyphene, oxycodone, hydrocodone
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Partial mu agonists.
Are mild to moderate agonists with lower efficacy. |
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Mechanism, Indications, and Disadvantages of Pentazocine (Talwin)
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Mixed agonist/antagonist opiod.
Analgesia due primarily to kappa receptor agonist activity. Only partial agonist or perhaps antagonist at mu receptor. Get ceiling effect analgesic and some respiratory depression with dependence Dysphoria, anxiety and hallucination may occur. |
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What receptor does the analgesia come from for Pentazocine (Talwin)?
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kappa receptor
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Is Pentazocine (Talwin) a mixed, agonist, or antagonist?
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Mixed
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Mechanism of Naloxone (Narcan)
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Pure competitive Antagoinst. Has highest affinity for mu receptors.
Used to treat overdoses, accelerate postop recovery, or treat dependence |
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What drug is used to treat overdoeses, accelerate postop recovery, or treat dependence of opiod?
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Naloxone (Narcan). It occupies the opiod receptor wihtout producing a pharmacological effect.
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Mechanism of Morphine
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With pain allows for analgesia, euphoria, drowsiness, and mental clouding.
Without pain can lead to nausea, apathy, dysphoria. Leads to pupillary constirction. Respiratory depression due to action on the brain stem. |
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Indications of Morphine
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Used against continuous dull pain.
Suppresses the cough reflex. Decreases glandular secretions in GI tract. Depresses propulsive perstalsis, increases non-propulsive contractions. |
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Advantages of Morphine
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Used for diarrhea by allowing increased water absorption from small and large intestines.
Only effect is by oral absorption. |
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Disadvantages of Moprhine
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Constipation.
Easily crosses placental and fetal BBB. Develop tolerance. When crushed lose the effect. Get abrupt withdrawal causing abstinence syndrome. |
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What drug is the receptor antagonist that prevents constpatin but does not penetrate the CNS?
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methyl naltrexone (Relistor)
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Mechanism of Methadone
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Longer duration of action and a longer but less intense withdrawal sydrome than morphine.
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Indications of Methadone
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Used in heroin detoxification and maintenance programs.
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Mechanism and Indications for Meperidine (Demerol)
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More consistent oral absorption than morphine.
Indicated for labor pain. |
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Disadvantages of Meperidine (Demerol)
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May produce CNS excitation and convulsion.
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Advantages of Mepridine (Demerol)
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Fewer GI and GU tract effects.
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Fentanyl (Sublimaze)
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Used as an adjunct for sedation and anxiolytic properties.
Used alone for cardiovascular surgery. Lollipop by way of buccal/transmucosal administration. |