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24 Cards in this Set
- Front
- Back
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opioid receptors
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-Mu: most important
-analgesia, respiratory depression, sedation, euphoria, physical dependence, decrease in GI motility(s/e and problem) -Kappa: -analgesia, sedation, decrease GI motility Delta -possibly psychotomimetic side effects (psychiatric s/e) |
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Pure opioid agonist
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activate mu and kappa receptors
-strong (morphine etc) -most severe pain -moderate strength (codeine etc) |
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Agonist-antagonist
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-activate either mu or kappa and antagonize other and always antagonize pure agonist
-activation of delta may cause psychotomimetic effects -if given after pure agonist, the mix will decrease pain relief -pentazocine, etc |
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Pure opioid antagonist
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antagonize (block) both mu and kappa
-used to reverse respiratory depression and sedation -to treat overdose (antidote) |
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Morphine
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opioid analgesic
-used for relief of moderate and severe pain -decreases sensation and emotional reaction to pain -mimics actions of endogenous opioid peptides at mu and kappa receptors ADVERSE EFFECTS: -respiratory depression-tolerance develops -constipation-little or no tolerance -sedation -orthostatic hypotension -urinary retention- care w/ BPH and anticholinergics (not anti-muscarinic-it's by a different mechanism) -miosis (little tolerance) DOSE FORMS: -oral: -immediate release tablet, capsule, liquid (fastest), soluble tablet, controlled/sustained release tablet and capsule, extended release-24 hr duration -rectal suppository (some use sustained release of tables as suppository) -soluble for injection |
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Fentanyl
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opioid analgesic
DOSE FORMS: -injection -transdermal patch (takes 12-24 hrs for full effect, lasts 48-96 hrs, 4 strengths) -Iontophoretic transdermal system (ITS) (by electrical charge) -transmucosal (lozenge, lozenge on a stick, new buccal tablet) only for breakthrough pain in patients already on/tolerant to opioids S/E similar to morphine |
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Meperidine (Demerol)
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potent opioid
-short acting |
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Methadone
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potent opioid
-long acting -used in detox |
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Alfentanil + sufentanyl
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potent opioid
-similar to fentanyl |
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Remifentanyl
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potent opioid
-very rapid and short acting |
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Codeine
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moderately potent opioid
-dose/compliance limiting SE (GI) -maximal efficacy of asprin and acetaminophen -combination of above--additive effect -by itself no more effective |
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Oxycodone
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moderately potent opioid
-slightly more maximally effective than codeine -immediate acting form alone + combination -sustained release form (OxyContin) controversial b/c it's abused |
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Hydrocodone
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moderately potent opioid
-close to oxycodone, available only in combination |
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Propoxyphene
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moderately potent opioid
-low potency and low maximal efficacy -combined with aspirin + acetaminophen -most physicians avoid it, it's not very effectice |
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Naloxone (Narcan)
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opioid antagonist
-treatment for opioid overdose -competitve blockade of mu and kappa receptors -also used to reverse post-op and newborn opioids |
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Pentazocine
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Agonist-antagonist agent
-poster boy for psychotomimetic -oral tablet form contains .5 mg naloxone -also available as oral combo + injection -frequent psychotomimetic reactions |
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Nalbuphine
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Agonist-antagonist agent
-frequent psychotomimetic reactions |
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Butophanol
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Agonist-antagonist agent
-Increases cardiac work (not used for AMI) -Nasal spray + injection (some give it orally) |
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Buprenorphine
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Agonist-antagonist agent
-different actions and mu and kappa receptor compared to others |
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Naltrexone
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opioid antagonist
-some use in maintenance after detoxification, like methadone, but less successfully because it does not prevent craving |
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Methylnaltrexone
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New opioid antagonist
-selective mu antagonist -indicated for opioid induced constipation in patients on long term opioid refractory to laxatives -injection (can't block mu receptors in brain b/c of quarternary ammonium-little CNS penetration) |
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Alvimopan
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New opioid antagonist
-selective mu antagonist -doesn't get into brain -indicated only for opioid related post-op ileus (decreased GI activity) -short term use -strictly controlled + for in-patients only -not yet indicated for opioid constipation -has lots of S/E |
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Tramadol
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Non-opioid central analgesic
-controlled substance -unusual mech of action -weak mu agonist -also works by inhibitionof NE and serotonin reuptake in spinal neurons -similar maximal efficacy to codeine + ASA or APAP S/E: relatively common- dizziness, dysphoria and seizures are possible |
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Ziconotide
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Non-opioid central analgesic
-new agent given by intrathecal injection (like epideral) -no action at opioid receptors and no opioid actions (including no tolerance, physical dependence, respiratory depression, withdrawal syndrome) -only for those intolerant or unresponsive to other methods -frequent and potentially troublesome s/e's |
