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Fentanyl Class

Pharm (Test 2)

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