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61 Cards in this Set

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  • Back
How much does an opioid agonist-antagonist decrease MAC?
8-20%
Dose of Nalmefene (Revex)?

Agonist/Antagonist...?
0.25mcg/kg IV q 2 to 5 min

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