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46 Cards in this Set
- Front
- Back
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What are the opiate receptors?
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Mu
Delta Kappa N/OFQ |
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What was the endogenous opioid receptor agonists?
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Beta endorphin with Met-enkephalin
Dynorphin with Leu-enkephalin |
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Which four genes code opioid peptides?
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Beta endorphin and ACTH
Enkephalin Dynophine N/OFQ |
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What is the mechanism of opioids?
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G-protein modulated decrease in Ca conductance via cAMP decrease to cause a decrease in nt release
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Which receptor does morphine bind?
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Mu
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Why is morphine much more effective when given parenterally?
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Large first pass hepatic metabolism
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Why does morphine cause itching?
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Causes the release of histamine
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Why does morphine cause pupil constriction?
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CN III stimulation
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What opioids are effectively used for cough?
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Codeine
Dextromethophan |
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What causes respiratory depression with opioid use?
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Decrease response to pCO2 in the brainstem
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Why can O2 administration cause apnea in respiratory depressed opioid users?
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Hypoxic drive is still intact so elevation of oxygen saturation causes then to stop breathing
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What are the cerebral vascular effects of morphine?
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Increase cerebral blood flow due to increase in pCO2 causing vasodilation. Also increases ICP.
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Why would you use morphine for CHF pts?
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Decreases workload and oxygen demand of left heart.
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What are the endocrine effects of morphine?
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Increase in prolactin
Increase in ADH Decrease LH/FSH Decrease ACTH |
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Why can opioids cause hypersensitivity reactions?
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Direct degranulation of mast cells.
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What is the difference between heroin and morphine?
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Heroin is more lipid soluble making it 2.5 times more potent
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Why would you use codeine over morphine?
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Better absorption
Less GI side effects Less dependence Good for cough |
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What are the disadvantages of codeine?
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Not good for severe pain
Potent histamine release No IV use OD can cause seizures |
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What are the advantages of using hydromorphone?
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(dilaudid)
8-10 times more potent Short duration Can give a high dose because its more soluble than morphine |
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What is the relative potency of oxymorphone, oxycodone, and hydrocodone?
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All equal to morphine
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What opioids are good alternatives to morphine if you want to administer orally?
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Oxycodone
Hydrocodone |
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What is dextromethophan used for? What are the benefits over other opioids?
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Antitussive
No GI effects No respiratory depression But also no pain relief |
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What is the drug of choice during delivery? Why?
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Meperidine, increases the force of oxytocin-induced contractions of the uterus and has short duration of action.
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What is the presentation of meperidine abuse? Why?
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Stupor and convulsion due to opiate and atropine-like effects.
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What is the benefit of alphaprodine use over meperidine?
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More rapid onset with shorter duration of action
Good oral effectiveness |
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What is the relative potency of fentanyl? What is the duration of action?
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100 times more than morphine
Half life is 20 mins |
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What is the common usage for fentanyl?
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post-anesthesia
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What are the benefits to sufentanil use over fentanyl?
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More potent: 1000 times more than morphine
More rapid onset |
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What are the pros and cons of remifentanil?
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more rapid than fentanyl but could have shorter half life because it can be metabolized by plasma esterases (8-20 mins)
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What is diphenoxylate used for?
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Diarrhea
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What is loperamide used for? What is the mechanism?
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Diarrhea
Slows motility |
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What allows methadone to have longer action than morphine?
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plasma protein binding
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What is the primary use for methadone?
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Opiate withdrawal management
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What is propoxyphene used for? What are the limitations?
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mild and moderate pain
Limitations: Not anti-inflammatory, antipyretic or antitussive No IV use due to irritation |
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Why would you use a mixed narcotic agonist/antagonist?
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Lower potential for abuse
Not as much respiratory effect |
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What is pentazocine?
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Mixed Narcotic
Mu antagonist Kappa agonist |
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What is the CV effect of pentazocine?
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Increase in rate and BP
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What is nalbuphine? What are the benefits of use?
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Mixed narcotic
Less hypotension than morphine Good for acute MI |
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Which mixed narcotics are more potent than morphine?
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Butophanol
Buprenophine |
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What is different about the respiratory depression caused by mixed narcotics?
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Appear to have a ceiling
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What is the mechanism of Buprenorphine?
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Mixed narcotic
partial mu agonist |
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Why would buprenorphine be used to treat fentanyl-induce respiratory depression?
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Antagonizes without reversing opioid effect
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What are the pure opiate antagonists?
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Naloxone
Naltrexone Nalmefine |
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What is the more effect route for naloxone?
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parenterally
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What is the difference between naloxone and naltrexone?
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naloxone is short duration
naltrexone is long duration and better orally |
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What are the uses for opiate antagonists?
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reverse respiratory depression and prevent drug abuse
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