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61 Cards in this Set
- Front
- Back
How much does an opioid agonist-antagonist decrease MAC?
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8-20%
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Dose of Nalmefene (Revex)?
Agonist/Antagonist...? |
0.25mcg/kg IV q 2 to 5 min
Antagonist |
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How is Nalmefene (Revex) metabolized?
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Conjugation
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Which has a longer duration of action Naloxone or Nalmefene?
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Nalmafene
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This antagonist has a sustained antagonism for as long as 24 hours when taken PO and is thus a good treatment option for addicts.
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Naltrexone
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Name opioids that are antagonists and what receptor they act on.
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Naloxone, Naltrexone and Nalmafene are all mu antagonists
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Dose and Duration of action of Naloxone (Narcan)?
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IV 1-5 mcg/kg
Infusion 5mcg/kg/h Duration: 30-45 minutes T 1/2: 60-90 minutes |
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Nausea, vomiting, increased SNS activity, reversal of analgesia, pulmonary edema and cardiac dysrhythmias are all side effects of what opioid antagonist?
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Naloxone (Narcan)
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Opioid agonist-antagonists, what receptors do they act on.
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Bind to Mu receptors as partial agonists or competitive antagonist. Partial agonist effects on kappa and delta receptors
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Name opioid agonist-antagonists.
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Pentazocine (Talwin), Butorphanol (Stadol), Nalbuphine (Nubain), Buprenorphine (Buprenex), Nalorphine, Dezocine (Dalgon)
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Which opioid agonist-antagonist has a high affinity for Mu1 receptors and moderate affinity for delta receptors with a ceiling effect?
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Dezocine (Dalgon)
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Which opioid agonist-antagonist has a high incidence of dysphoria?
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Nalorphine
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Which opioid agonist-antagonist has a s.e. of prolonged resp. depression and is resistant to naloxone?
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Buprenorphine (Buprenex)
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Which opioid agonist-antagonist can be placed epidurally & is highly lipid soluble which can lead to delayed resp. depression?
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Buprenorphine (Buprenex)
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What is the most common s.e. for Nalbuphine (Nubain)?
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Sedation
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Which opioid agonist-antagonist does not increase HR, BP or PAP?
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Nalbuphine (Nubain)
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Which opioid agonist-antagonist has a low affinity for Mu receptors and a moderate affinity for kappa receptors?
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Butorphanol (Stadol)
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Which opioid agonist-antagonist is a derivative of benzomorphan?
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Pentazocine (Talwin)
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Pentazocine has agonist effects on what receptor(s)?
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Delta and Kappa
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Which opioid agonist-antagonist has high risk of dependence?
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Pentazocine (Talwin)
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Which opioid agonist-antagonist has s.e. of sedation, N/V, dysphoria, diaphoresis, dizziness and an increase in plasma catecholamines?
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Pentazocine (Talwin)
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Synthetic opioid by the acetylation of morphine.
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Heroin
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This opioid does not posess antipyretic, antiinflammatory, or antitussive properties.
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Propoxyphene
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This synthetic opioid would be appropriate only for addicts.
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Methadone (Dolophine)
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This opioid is 10x more potent than morphine (Chris has never seen it used)?
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Oxymorphone (Numorphan)
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What is the onset, peak and duration of Hydromorphone (Dilaudid)?
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Onset 15-30 min
Peak 30-90 min Duration 4-5 hours |
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This opioid has more sedation, less eurphoria and is 5x more potent than morphine?
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Hydromorphone
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This opioid is demethylated in the liver and excreted by the kidneys?
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Codeine (methylmorphine)
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This opioid is an antitussive at 15mg and an analgesic at 60mg PO?
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Codeine (methylmorphine)
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Side effects of this opioid include N/V, minimal sedation, constipation, physical dependence?
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Codeine (methylmorphine)
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Codeine (Methylmorphine) is created by substitution of what?
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Substitution of a methyl group for the hydroxyl group on C 3 of morphine
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What is the onset, peak and duration of IV Remifentanil (Ultiva)?
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Onset 1 min
Peak 1 min Duration 5-10 min |
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Place in order from highest to lowest Context Sensitive 1/2 times Alfentanil/Fentanil/Remifentanil/Sufentanil.
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Fentanil > Alfentanil > Sufentanil > Remifentanil
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This opioid agonist has an ester linkage making it susceptible to hydrolysis?
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Remifentanil (Ultiva)
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This opioid agonist is specific to Mu receptors, has a small Vd and its clearance is not affected by renal or hepatic failure?
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Remifentanil (Ultiva)
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This might be a good opioid agonist for a 'wake up test'?
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Remifentanil (Ultiva)
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What are the recommended doses for Remifentanil (Ultiva)?
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IV: 1mcg/kg IV over 60 sec Infusion: 0.5-1mcg/kg IV over 10 min
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Which opioid agonist should be avoided in untreated Parkinson's patients, why?
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Alfentanil (Alfenta)
It decreases the central dopamine transmission |
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This opioid agonist (and dose) blunts BP and HR response to intubation? (and dose) blunts catecholamine response?
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Alfentanil 15mcg/kg
Alfentanil 30mcg/kg |
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This opioid agonist is metabolized by N-dealkylation of Piperidine and Amide independently?
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Alfentanil (Alfenta)
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This opioid agonist is 96%cleared hepatically within 60 minutes.
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Alfentanil (Alfenta)
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Alfentanil's effects are prolonged with_________, because of alterations in P-450 activity?
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Erythromycin
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With initial dose, which opioid agonist has first-pass pulmonary uptake of:
10%/60%/75% |
Alfentanil (Alfenta) 10%
Sufentanil (Sufenta) 60% Fentanyl 75% |
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What is the onset, peak and duration of Alfentanil?
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Onset immediate
Peak immediate Duration (fast?) |
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What % of Alfentanil exists in the non ionized form and does it have a low or high pKa?
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90%
low pKa |
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Which opioid agonist is useful when you want to avoid coughing and bucking on emergence?
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Sufentanil (Sufenta)
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This opioid agonist is metabolized by N dealkylation and O demethylation?
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Sufentanil (Sufenta)
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Protein binding by opioid agonist, place in order from highest to lowest: Fentanyl/ Sufentanil/ Alfentanil/ Remifentanil/ Morphine/ Meperidine
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Sufentanil 93%
Alfentanil 92% Fentanyl 84% Remifentanil 80% Meperidine 70% Morphine 35% |
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This opioid agonist is 5-10x more potent than Fentanyl?
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Sufentanil (Sufenta)
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What are the clinical doses for low dose analgesia/ med. dose (surgical anesthesia)/ high dose (alone for surgical anesthesia) of Fentanyl?
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Low dose 1-2mcg/kg IV
Med dose 2-20mcg/kg IV High dose 50-100mcg/kg IV |
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This opioid agonist is metabolized by N-demethylation?
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Fentanyl (Sublimaze)
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What is the onset, peak and duration of Fentanyl?
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Onset 2-5 min
Peak 20-30 min Duration 0.5-1 hour |
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This opioid agonist is 75-125x more potent than morphine? Why?
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Fentanyl b/c of its high lipid solubility
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Describe Serotonin Syndrome and which drugs are associated with this fatal interaction?
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HTN, tachycardia, hyperpyrexia, convulsions
Meperidine and MAOIs or SSRIs |
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Side effects of this opioid agonist include: respiratory depression, orthostatic hypotension, increased HR, and mydriasis.
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Meperidine (Demerol)
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What opioid agonist and agonist-antagonist suppress post op shivering? How?
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Meperidine and Butorphanol Stimulate Kappa receptors
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What happens with high doses of Meperidine?
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Negative cardiac inotropic effects and histamine release
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What is the onset, peak and duration of Meperidine?
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Onset 5 min
Peak 30-60 min Duration 2-4hours |
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What opioid agonists are derived from phenylpieridine?
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Meperidine, Fentanyl, Sufentanil, Alfentanil, Remifentanil
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Which opioid agonist acts on mu and kappa receptors?
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Meperidine (Demerol)
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What is the onset, peak and duration of Morphine?
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Onset 20 min
Peak 30-60 min Duration 4-6 hours |