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49 Cards in this Set
- Front
- Back
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What are some uses of opioids?
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Tx of diarrhea, acute pulmonary edema, antitussive, pain relief (dull, visceral pain)
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What receptor does morphine have an affinity for?
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mu
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What receptor does codeine have an affinity for?
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mu
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What is deacetylated morphine?
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Heroine
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What makes an anolog of morphine have agonist properties?
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alterations to nCH3 (n-methyl group) on C17
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Why does the brain have opiod receptors?
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Endorphins are endogenous
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What receptor does Beta-endorphin show an affinity for?
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mu
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What receptor does leu/met-enkephalin show an affinity for?
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delta
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What receptor does dynorphin show affinity for?
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kappa
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What forms from prepropiomelanocortin?
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Beta endorphin
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What forms from preproenkephalin?
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leu/met-enkephalin
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What forms from preprodynorphin?
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dynorphin
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What is the mechanism of morphine at spinal sites?
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Closing of Ca channels to prevent presynaptic NT release and hyperpolarizing post-synaptic membranes by opening K channels
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What maintains pain sensitivity?
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GABA (morphine upsets what GABA is doing)
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How do opiods activate pain inhibitory neurons at the brainstem?
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inhibity GABA activity
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What does morphine do to the pain threshold?
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Increase it
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What is the structure of an opiod receptor?
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7 transmembrane regions and g-protein coupled activity
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What opioid has a ceiling effec with limitation for severe pain?
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Codeine
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What produces pleasure?
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> dopamine at nucleus accumbens
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What would the pupil do with use of opioids?
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miosis
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What does morphine do to the endocrine system?
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> ADH (water retention)
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What drug is useful in MI or in patients with pulmonary edema?
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Morphine
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What does morphine do to the GI system?
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Spastic paralysis (constipation) and < peristalsis
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Where would you see MINIMAL tolerance to morphine?
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Miosis (constriction), constipation, convulsions
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The BBB is significant for which drug?
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Morphine (thus heroin crosses much faster)
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Most of heroin is excreted in how long?
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24 hours
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Ultram
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Tramadol
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Dolophine
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Methadone
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What receptor does methadone primarily act on?
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mu
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Which opioid has an extended duration of 8 hours?
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Methadone
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Darvon
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Prophozyphene
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What receptor does Meperidine (Demerol) primarily act on?
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mu
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What is the significance of normeperidine?
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1st metabolite of Meperidine (Demerol) that causes seizures when accumulated
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Which lasts longer, naloxone or naltrexone?
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Naltrexone
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What is an opioid antagonist that lasts 1-2 hours given orally to prevent relapse?
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Naloxone
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Nalorphine
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partial agonist
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Pentazocine (Talwin)
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partial agonist
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What is given to dx physical dependence?
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Nalorphine
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What is the drug of choice if addiction problem exisits?
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Pentazocine
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Butorphanol (Stadol)
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partial agonist
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Nalbuphine (Nubaine)
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partial agonist
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Buprenorphine (Buprenex)
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Partial agonist
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What has been found useful in reducing craving for heroin or cocaine during the withdrawal period?
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Buprenorphine (Buprenex)
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What drug should you choose for moderate pain?
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Codeine
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The drug of choice for bilary/renal colic?
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Meperidine
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Widely used as a substitute for heroin?
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methadone
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Used in IV to reverse respiratory depression in opioid OD?
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Naloxone or nalmefene
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Dyspnea due to L ventricular failure is relieved by what?
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morphine
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What should you use for diarrhea?
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loperamide or diphenoxylate
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