Ch. 47: opioids
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| MOA of opiates? | bind to specific receptors in the CNS, nerve terminals of the periphery, and GI to produce effects that mimic endogenous peptide neurotransmitters
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| primary use of opioids? | relieve intense pain and the anxiety that accompanies it.
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| opiates are abused due to what effects? | euphoric effects
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| where are the opioid receptors? | some in the hypothalamus. when stimulated, hypothalamus becomes more active in neuroendocrine secretion. receptors are on immune cells, role is yet unknown. receptors also in limbic system (area of emotions), amygdala, peripheral sensory fibers
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| what are the two most important opioid receptors? | mu, kappa
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| mu receptor activation produces what? | respiratory depression, euphoria/sedation, physical dependence, decreased GI motility, pupil constriction, strong analgesia
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| kappa receptor activation effects? | analgesia, sedation/dysphora, pupil constriction.
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| do all opioids stimulate or inhibit Gi proteins? | stimulate. they inhibit activation of adenylate cyclase.
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| this displaces all receptor bound opiate molecules. it reverses overdose of opiates. with IV adminstration, it is able to reverse any overdose-induced coma/respiratory depression within thirty seconds. | naloxone
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| has agonal and antagonal effects on differing receptors. it is a potent dysphoria inducing drug. it is analgesic, but less so than morphine and causes much less euphhoria than morphoine does. at higher doses, | pentazocine
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| at higher doses of pentazocine, what happens? | induces respiratory depression, decreased Gi activity, hypertension, hallucinations, nightmares, tachycardia, dizziness
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| weak mu receptor agonist. because it is weak for analgesia, it is often use din combination with aspiriin or acetaminophen. it has low abuse potential because it causes less euphoria than morphine | codeine
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| derivative of methadone, and is an opioid receptor agonist. it is a weaker analgesic than codeine (about half as effective). if used with alcohol, causes severe CNS depression, and even death. | propoxyphene
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| a STRONG opioid agonist. its indicaiton for use is strong analgesia. it has a rapid onset, but short duration (fifteen to thirty minutes) | fentanyl
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| STRONG opioid agonist. it is equal in potency to morphine, but has a longer duration of action, making it an effective drug for treatment of drug withdrawal from opioids. it has greatest effect at the mu receptor | methadone
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| acelyated morphine. becauese of the acetylation, it is able to cross the blood brain barrier with much greater ease. this makes it three times more potent than morphine. it causes extreme euphoria | heroin
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