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40 Cards in this Set
- Front
- Back
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Thre main proteins cleaved to make endogenous opiods
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POMC
Proenkephalin Prodynorphin |
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Three major biologically active opiods?
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Metenkephalin
Leu-enkephalin Dynorphin A and B |
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the main receptor subtype of medical relevance
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mu
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Ion channel effects of opiod receptor activation
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increase potasium going out
decrease calcium coming in net effect, inhibition both pre and post synaptically |
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Endogenous opiods and PCP
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endogenous opiods don't bind to PCP receptor sites!
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allodynia
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pain cause by previously inocuous stimuli
Prostoglandins sensitize nervers to sensation from stretch, head, chemicals |
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Drugs that can be combine with opiods to increased efficacy
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SSRI b/c serotonin modulates opiod interneurons in the dorsal colum
NSAIDS b/c prostoglandins sensitize nociceptors |
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Why you don't administer O2 to a patient on morphin
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Morphin depresses response to hypercapnia, so high C02 and carotid O2 are main resp drive. Giving pure O2 depresses drive and can cause resp failure
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Tx for first dose nausea with morphine
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Procholorperazine or chlorpromazine
Patients generally becomes refractory to nauses after initial dose |
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Morphines effect on autonomin system
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Depress sympathetic tone causing vasodilation
May cause orthostasis in normal people or worse in hypovolemic |
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GI effects of morphine
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Acts on nerve plexi and reduce propulsive contraction and increase spasm. Atropine lowers spasm so Atropine + morphine good anti-diarrheal
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Tx for actue morphine poisioning
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repeat injection of naloxone
Naloxone may precipitate withdrawal if patient is dependent on morphine |
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withdrawl from opiods vs withdrawls from ehtanol/barbits
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morphine withdrawls is less severe
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Codeine
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Fully absorbed orally unlike morphine (1/5) so is as effect as parenterally
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hydromorphone, oxymorphone
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like morphine but more potent
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oxycodone and hydrocodone
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used as antitussive and alagesic mixtures
equal to morphine but better absorbed orally |
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Heroin
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prodrug for morphine that rapidly, rapidly crosses BBB
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Leveorphanol
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optical isomer is dextromorpha
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Meperidine
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Demerol
Preferred opiate for OB because it has less constipation, urine retention, fetal resp depression and does not prolong labor |
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Mechanism of action for Meperidine
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Broken to meperidinic acid (analgesia) and normeperidine (excitatory) in the liver
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Naloxone with meperidine
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Naloxone blocks the analgesic properties of meperidine, but not the excitatory, so it can lead to convulsions
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Diphenoxylate
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Lomotil
Insoluable so no absorbed. With atropine, works as a good antidiarrheal with no CNS effects |
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Fentanyl
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80 potentcy of morphine
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Methadone
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Morphine plus
Little higher oral absorbed Longer half life Less withdrawl |
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Propoxyphene
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slightly less effective than codeine but less addictive because you get toxic before you get high of codeine
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1-acetylmethadol
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long lasting opiod in depot form used for treatment of opiate addiction
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long lasting opiate in depot form for tx of opiate addiction
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1-acetylmethadol
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less effective than codein but it has less addictive potential as well
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propoxyphene
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Pentazocin
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kappa agonist, mu antagonist
less respiratory distress than all others but causes nightmares etc at high doses. May precpitate withdrawl in morphine addicts |
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Less respiratory effects than morphine but causes dysphoric effects at high doses
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pentazocin
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Naloxone vs Naltrexone
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Naloxone has no oral availability, naltrexone does with longer effects
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dextromethorphan
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antitussive with no opiod effects except at very high doses
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drug of choice for ob analgesia
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meperidine
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insoluble opiate used with atropine for diarrhea
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diphenoxylate
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80x the potency of morphine
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fentanyl
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opiate of choice for cough
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dextromethorphan
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tx of autonomic symptoms during opiate withdrawl
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clonidine
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Which cause more biliary spasm
Codein, Morphine, Meperidine, Methadone |
Morphine=Meth>Meperidine>Codein
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Duration of action for meperidine vs morphine vs methadone
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Methadone>Morphine>Meperidine
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Respiratory depression of meperidine vs morphine vs methadone
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All have same effect on respiratory depression
Mixed actors like pentazocine have less respiratory depression |
