USMLE Step 1
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| Location of opioid receptors | hypothalamus, immune cells, limbic system, periphery-pain
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| Mu receptor | respiratory depression, euphoria/sedation, physical dependence, decreased GI motility, pupil constriction, ANALGESIA
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| Kappa receptor | analgesia, sedation/dysphoria, pupil constriction
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| Naloxone | MOA: displaces all receptor-bound opiate molecules, reverses opiate OD w/in 30 secs
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| Pentazocine | MOA: opiate used foragonal & antagonal effects on differing receptors, analgesic less so than morphine; ADRs: potent dysphoria-inducing drug, @ high doses + respiratory depression, decreased GI activity, HPTN, hallucinations, nightmares, tachy & dizziness
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| Codeine | MOA: weak mu receptor agonist, weak for analgesia often used in combo w/ ASA or acetaminophen, low abuse potential b/c causes less euphoria than morphine
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| Propoxyphene | MOA: methadone derivative, opioid receptor agonist, weak analgesic, dextro form used analgesic 4 mild-moderate pain vs levo 4 antitussive, combo w/ acetaminophen or ASA; ADRs: w/ EtOH causes severe CNS depression & death, nausea, anorexia & constipation
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| Fentanyl | MOA: opioid STRONG agonist used for strong analgesia, has a rapid onset, short duration (15-30 mins)
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| Methadone | MOA: STRONG opioid agonist, equal potency to morphine, but has longer duration of action = good tx from opioid w/drawl, greatest effect on the mu receptor
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| Heroin | MOA: acetylated morphine due to acetylation able to cross BBB w/ ease = 3x more potent than morphine, causes extreme euphoria
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jerrica_08
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