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Pharm (Test 2)

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Question
Answer
Small doses of fentanyl have a duration of?   20-40 min  
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Small doses of fentanyl have a duration based on...   redistribution  
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Larger doses of fentanyl have a (longer or shorter?) duration?   longer (>40min)  
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Larger doses of fentanyl have a duration based on...   accumulation  
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Fentanyl (is or isn't) taken up by lungs during first-pass.   is (75% of initial IV dose)  
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What happens to the distribution of repeat doses of fentanyl?   accumulate in muscle and fat (d/t high lipid solubility)  
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What is one reason for prolonged duration of large/repeated doses of fentanyl?   mobilization from storage sites when admin. ceases (especially when used in combination w/ volatiles)  
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For infusions <2hrs, the context sensitive half-time of fentanyl is (greater or less?) than that of sufentanil?   less  
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For infusions >2hrs, the context sensitive half-time of fentanyl is (greater or less?) than that of sufentanil?   greater  
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How is fentanyl metabolized?   by N-demethylation  
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What are fentanyl's metabolites? Are they active or inactive?   1)norfentanyl (minimal activity; structurally similar to normeperidine); 2)hydroxypropoinyl-fentanyl (inactive) 3)hydroxypropinyl-norfentanyl (inactive)  
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Which of fentanyl's metabolites is the principle metabolite in humans?   norfentanyl  
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How are fentanyl's metabolites metabolized?   excreted by kidneys in the urine (also 10% of fentanyl)  
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Is fentanyl a good drug of choice for renal failure pts?   yes; metabolites that are metabolized renally are inactive  
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What is the eliminiation 1/2 life of fentanyl?   3.1-6.6 hrs  
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How does fentanyl's eliminiation 1/2 life compare to morphine?   longer than morphine  
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Why does fentanyl have a longer 1/2 life than morphine when it has a shorter duration?   larger volume of distribution; plasma cntn is maintained by redistribution  
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Is the duration of fentanyl prolonged with hepatic cirrhosis?   no  
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What pt variables can prolong the duration of fentanyl?   elderly (decreases in hepatic blood flow; dec. microsomal activity; dec. in albumin production-->highly protein bound); abdominal aortic surgery involving infarenal aortic cross-clamping  
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What is the typical dose of fentanyl given for analgesia?   1-2mcg/kg IV  
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What is a possible dose of fentanyl given to blunt circulatory responses?   2-20mcg/kg IV  
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What dose of fentanyl blocks the sympathetic response during laryngoscopy?   5-8mcg/kg  
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What is a dose of fentanyl to blunt circulatory responses when given with N2O, midazolam, or volatiles?   bolus of 10mcg/kg, then 50-100 mcg/hr  
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What dose of fentanyl can reduce the required dose of propofol for LMA placement?   0.5mcg/kg  
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Fentanyl is (more or less?) effective in reducing MAC of volatile agents than morphine?   more  
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What dose of fentanyl can reduce MAC by 80%?   50-150mcg/kg  
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What dose of fentanyl can reduce MAC by 40%?   1mcg/kg  
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What are 3 advantages of fentanyl?   1)no direct myocardial depression 2)no histamine release 3)suppresses stress response to surgery  
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What are 3 disadvantages of fentanyl?   1)sympathetic stim. in response to pain (especially w/ good LV function) 2)unreliable amnesia 3)post-op resp depression (d/t renarcatization)  
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Fentanyl reduces a pt's HR (more or less?) than morphine?   more  
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True or False: Fentanyl can occasionally reduce a pt's BP and CO   True (not r/t contractility; r/t dec. SVR, dec. preload)  
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What are some neuromuscular affects of fentanyl?   1)myoclonus r/t depression of inhibitory neurons (seizure-like w/ no EEG changes), 2)doses of 30mcg/kg change somatosensory evoke potential, but don't interfere w/ the use and interpretation  
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What affects can fentanyl have on head injury pts?   increases ICP (6-9) even w/ unchanged PaCO2, decreases in MAP and CPP (dec. in BP --> dec. in cerebral vascular resisitance --> vasoldilation -->inc. ICP)  
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What affects of fentanyl are synergistic when given w/ benzo's?   sedation, hypnosis, resp. depression  
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What affect dose fentanyl have on cough?   reflex coughing  
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What is the most potent opioid currently available?   sufentanil  
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Compare sufentanil's potency to fentanyl and morphine.   10X more potent than fentanyl; 1000X more potent than morphine  
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Compare sufentanil's lipid solubility to fentanyl.   more lipid soluble than fentanyl  
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Is sufentanil taken up by lungs in first pass?   yes; 60%  
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Compare sufentanil's elimination 1/2 time to fentanyl.   shorter (2.5 hrs compared to 3.1-6.6 hrs)  
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Compare sufentanil's protein binding to fentanyl.   greater protein binding (so smaller volume of distribution)  
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How is sufentanil metabolized?   hepatic N-dealkylation  
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Are sufentanil's metabolites active or inactive?   inactive  
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How are sufentanil's metabolites metabolized?   elimination by liver and kidneys  
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What is the effect of a pre-induction dose of sufentanil?   apnea w/o loss of consciousness  
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What dose of sufentanil is commonly associated w/ stiff chest?   10-15mcg  
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Compare sufentanil's sedative quality to fentanyl.   more sedative than fentanyl  
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Compare sufentanil's analgesia to fentanyl.   longer lasting analgesia than fentanyl  
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Compare sufentanil's respiratory depression to fentanyl.   less respiratory depression  
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Compare sufentanil's affinity to receptors to fentanyl.   greater  
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Typically, pt who received sufentanil are extubated (sooner or later?) than those who received fentanyl.   20 min sooner  
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Sufentanil can reduce the MAC of volatiles by up to _______%.   70%  
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This MAC reduction of sufentanil is (more or less?) than an equipotent dose of fentanyl.   more  
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Compare a dose of sufentanil than that of fentanyl.   1/10th the dose of fentanyl  
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What is a typical dose of sufentanil?   loading dose of 1mcg/kg, then 1mcg/kg/hr  
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You must turn off an infusion of sufentanil __________min prior to emergence.   30-45 min  
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Using what group of meds can necessitate decreasing the infusion rate of sufentanil.   benzo's  
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Compare sufentanil's context sensitive 1/2 life to that of fentanyl.   after infusion for 3 hrs, sufentanil will dec. by 80% more rapidly than fent; after infusion for 8hrs, sufentanil will dec. by 50% more rapidly than fent.  
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Why is an overdose of sufentanil difficult to diagnose?   the BP at the minimum effective dose and the BP at 5X that dose will be the same  
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What are 2 reasons sufentanil can cause difficult ventilation?   1)stiff chest, 2)glottis obstriction  
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What dose of sufentanil can cause seizures?   1000X effective dose  
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Compare alfentanil's potency to fentanyl.   1/5 as potent as fentanyl  
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Compare alfentanil's volume of distribution to fentanyl.   Smaller (4-6X) than fent  
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Compare alfentanil's lipid solubility to fentanyl.   lower lipid solubility  
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Compare alfentanil's elimination 1/2 life to fentanyl.   shorter (1.1-1.6 hrs)  
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What percent of alfentanil is in ionized form at physiologic pH?   10%  
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Compare alfentanil's onset time to fentanyl.   faster  
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What dose of alfentanil gives maximum catecholamine blunting for laryngoscopy?   30mcg/kg  
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What is one indication for use of alfentanil?   retrobulbar block (eye cases)  
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Compare alfentanil's liability of producing stiff chest to fentanyl.   more liable  
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Compare alfentanil's ability to produce euphoria to fentanyl   more euphoria  
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Describe the metabolism of alfentanil into its metabolites?   N-dealkylation to noralfentanil; amine N-dealkylation to N-phenylpropionamide  
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Are alfentanil's metabolites active or inactive?   inactive  
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_____% of alfentanil is cleared w/in 60 min of administration.   96%  
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What can make standard infusion and dosing of alfentanil difficult?   interindividual variability r/t P-450 and CYP3A enzymes  
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For an infusion <8hrs, alfentanil's context sensitive 1/2 time is (greater or less?) than sufentanil.   less  
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For an infusion >8hrs, alfentanil's context sensitive 1/2 time is (greater or less?) than sufentanil,   greater  
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Alfentanil infusions should be discontinued _______min before emergence   15-25 min  
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What dose of alfentanil blunts SBP and HR response to laryngoscopy?   15mcg/kg 90 sec before  
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What is a typical induction dose of alfentanil?   150-300mcg/kg rapidly  
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What is a typical infusion dose of alfentanil?   150mcg/kg/hr  
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Alfentanil should be given (before or after?) incision.   Before: BP can be decreased w/ a dose after painful stimulation  
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Compare incidence of PONV of alfentanil to sufentanil and fentanyl/   lower than both  
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Compare remifentanyl's potency to fentanyl.   5X more potent  
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What is the eliminiation 1/2 t of remifentanyl?   6-10 min  
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Describe how remifentanil is metabolized into its metabolites.   nonspecific plasma and tissue esterases into inactive metabolites  
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How are remifentanil's metabolites metablized?   excreted by the kidneys  
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True or False: Remifentanil's duration is affected by plasmacholinesterase deficiency.   False  
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Hypothermia slows the clearance of remifentanil by ______%.   20%  
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_____% of remifentanil is eliminated during distribution?   99.8  
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How long dose redistribution of remifentanil take?   0.9 min  
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What is the elimination 1/2 t of remifentanil?   6.3 min  
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True or False: Remifentanil's context sensitive half-time is independent of infusion time.   True  
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What is remifentanil's context sensitive half time?   4 min  
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Pt who received remifentanil have a _____% dec in SBP 2 min after administration.   30%  
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Does remifentanil cause histamine release?   no  
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How long is remifentanil's equilibration time?   10 min  
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The effect site concentration of remifentanil decreases by 50% in ______min.   4  
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Compare remifentanil's volume of distribution to the rest of the fentanyl class.   smallest volume of distribution  
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Which opioid of the fentanyl class has the smallest volume of distribution?   remifentanil  
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What are some clinical uses for remifentanil?   laryngoscopy, retrobulbar block, LandD, desire rapid recovery for quick neuro exam (craniotomy, carotid endarterectomy)  
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What is the infusion dose of remifentanil?   0.5mcg/kg/min  
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What is the induction dose of remifentanil?   1mcg/kg over 60-90 sec  
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