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43 Cards in this Set
- Front
- Back
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What are the mu opioid agonists?
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-Morphine
-Oxycodone -Meperidine -Fentanyl -Methadone -Codeine -Heroine |
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Which opioid is less efficacious than the others in alleviating pain?
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Codeine
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What can develop in therapy using any of the opioids?
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Both Tolerance and Dependence can develop
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Why do the abuse liabilities for different opioids differ?
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Because they exhibit different pharmacokinetics - potency and duration of action.
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What is the prototype STRONG analgesic?
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Morphine
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What is the natural source of morphine and what receptor binds it?
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-Poppy
-Mu receptor |
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What administration method results in higher potency of morphine? Why?
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Parenteral; oral administration is 1/3 as potent due to significant FPE
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What is the duration of analgesia achieved by morphine?
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4-5 hrs
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What active drugs are derived from Heroine?
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Monoacetylmorphine and morphine
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How does diacetylmorphine compare to normal morphine? What is the result of this?
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More lipophilic - gets to the CNS much more rapidly
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Is heroine used clinically? Why?
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No - it has no advantage over giving morphine, but has a much greater abuse liability.
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What is PCA?
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Patient controlled analgesia
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What is O-methyl morphine?
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Codeine
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What is related to Codeine?
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Oxycodone
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Which is able to achieve the analgesic effects of Morphine?
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ONLY oxycodone - not codeine
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What pain is each used for?
-Codeine -Oxycodone |
Codeine = mild to mod
Oxycodone = mod to severe |
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What mu agonist has a shorter duration of action than Morphine?
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Meperidine
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What does Meperidine's shorter duration of action make it good for?
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Reducing pain during Endoscopy and other short procedures
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What is Meperidine NOT useful for and why?
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Not for post-surgical pain bc repeated use causes toxic metabolites to accumulate
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What can the toxic metabolites of Normeperidine cause?
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-Fever
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What drug interacts with Meperidine? Resulting in?
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MAOI's - Fever/hypertensive crisis
(remember, Don't give Meperidine to a Parkinson pt on Selegiline) |
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What compound related to Morphine can never achieve the same analgesic effects of it?
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Codeine
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What type of pain can Codeine treat?
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Mild to moderate
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What Codeine-like drug can achieve the efficacy of morphine?
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Oxycodone
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What is the probly with oxycodone?
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It has a major abuse potential (ie brett favre)
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Where Meperidine is a Phenylpiperidine, Methadone is:
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A phenylheptylamine
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How does the potency of Methadone compare to Morphine?
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Equipotent
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How is Methadone administered?
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Orally (little FPE)
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How does Methadone differ from Morphine?
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Longer duration of action
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What are 2 things Methadone is used for treating?
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-Opioid abuse
-Chronic pain |
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What opioid is 100X as potent as morphine?
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Fentanyl
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What is the duration of action of Fentanyl and how is it administered?
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-SHORT acting (1-1.5 hrs)
-Injectable or Transdermal patch |
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What happens when Fentanyl is injected?
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It results in anesthesia
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What is the transdermal patch of Fentanyl used for?
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Treatment of chronic pain
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What are the 2 MIXED action agonist/antagonist opioids?
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-Nalbuphine
-Buprenorphine |
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What receptor activity does Nalbuphine have?
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-Mu antagonist
-Kappa agonist |
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How does the activity/effect of Nalbuphine compare to that of Morphine?
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-Similar efficacy and potency so similar strong analgesic effects
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How does Nalbuphine DIFFER from morphine?
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-Less euphoria
-Lower abuse potential |
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How is Nalbuphine administered?
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Only by injection
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What is Nalbuphine used for?
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Precipitating withdrawal in Opioid dependent patients
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What is the receptor activity of Buprenorphine?
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-Mu partial agonist
-Full kappa antagonist |
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What are 2 uses of Buprenorphine?
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-Treats mod-severe pain
-Treats opioid dependence when in combo with naloxone (oral) |
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How does the potency of Buprenorphine compare to morphine?
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Buprenorphine is more potent
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