opioids Flashcards

1
Q

name the active metabolite of demerol/meperidine

A

normeperidine

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2
Q

name the active metabolite of morphine

A

morphine 6 gluconoridation

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3
Q

name the side effects of meperidine

A

increases HR
delirium & seizures- from the active metabolite
serotonin syndrome- especially if patient is taking an MAOI
mydriasis

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4
Q

fentanyl what is it structurally related to

A

meperidine

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5
Q

how much fentanyl gets stored in the lungs initially due to first pass pulmonary uptake

A

75%

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6
Q

what is the concern with the large amount of fentanyl that gets stored in the lungs.

A

it limits the initial amount of drug that reaches the systemic circulation and may play an important role in determining the pharmacokinetic profile of fentanyl.

it also means when it gets stopped after several repeated doses- plasma concentration does not decrease rapidly.

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7
Q

does hepatic cirrhosis prolong elimination half time of fentanyl

A

no- somewhat surprising

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8
Q

what occurs when the continuous infusion of fentanyl increases beyond two hours

A

the context sensitive half time of this opioid becomes greater than sufentanil.

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9
Q

elimination of what two drugs is prolonged by cardiopulmonary bypass

A

fentanyl and alfentanil

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10
Q

iv dose of fentanyl

A

1-2mcg/kg- per hammon we give 50-100mcg

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11
Q

what is the clinical use of fentanyl

A

blunt response to intubation or sudden changes in surgical stimulation

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12
Q

if we inject an opioid such as fentanyl before painful surgical stimulation- how will that benefit the patient post op

A

it will decrease the amount of postoperative analgesia required.

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13
Q

side effects of fentanyl

A

persistent recurrent depression of ventilation
secondary peaks- 1 from acid gastric fluid ion trapping then getting absorbed back into circulation- 2 washout from the lungs.

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14
Q

what is more prominent with fentanyl than morphine and may lead to occasional decreases in blood pressure and cardiac output

A

bradycardia

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15
Q

rapid administration of fentanyl, sufentanil and alfentil may result in

A

seizure like activity

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16
Q

administration of fentanyl and sufentanil to head injury patients has been associated with…

A

modest increases in ICP (6-9mmhg)

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17
Q

what is different about the increase in ICP evoked by sufentanil (and fentanyl)

A

decrease BP - vasodilation auto regulation decreases cerebral vascular resistance increasing ICP

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18
Q

sufentanil is how much more potent than fentanyl

A

5-10x more potent

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19
Q

how much pulmonary first pass uptake does sufentanil undergo

A

60%

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20
Q

protein binding of sufentanil

A

92%

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21
Q

dose of sufentanil

A

0.1-0.4mcg/kg

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22
Q

when do you see an increase plasma concentration of sufentanil

A

chronic renal failrue

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23
Q

clinical use of sufentanil

A

longer period of analgesia

less depression of ventilation compared to fentanyl

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24
Q

what does sufentanil do to the brain

A

decrease in cerebral metabolic oxygen requirements and cerebral blood flow is decreased or unchanged.

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25
what are the effects of sufentanil on the heart
bradycardia- decreases co
26
what is the skeletal muscle rigidity seen with fentanyls
obstruction at the level of the glottis- resolved with intubation
27
alfentaily is comparable to
fentanyl
28
what prolongs alfentanil elimination
cirrhosis of the liver- renal failure not an issue
29
alfentanil- how much of the drug exists in nonionized form
90%- meaning it has rapid effect and is a result of the low PKA.
30
what is a main concern with administering alfentanil
it has a 10 fold inter individual variability in systemic clearance
31
clinical use of alfentanil
rapid onset and off set | unlike other opioids- supplemental doses decrease systemic blood pressure that is increased after painful stimulation.
32
remifentanil potency is similar to
fentanyl
33
remifentail is unique why
it is susceptible to hydrolysis by nonspecific plasma and tissue esterase to inactive metabolites.
34
how do you dose remifentanil
lean body mass
35
how fast does remifentanil reach a steady state
10 minutes
36
is remifentanil effected by renal or hepatic failure
no due to esterase metabolsim
37
what case can you think of that requires profound analgesic effect transiently and remifentanil should be used
retrobulbar block.
38
before turning off remifentanil infusion what must occur
a longer acting opioid should be administered to ensure analgesia when the patient awakens
39
how much does cardiopulmonary bypass decrease clearance of remifentanil
20%
40
phenoxabenzamine dose
0.5-1mg/kg PO prior to surgery
41
phentolamine dose
0.1-2mg/min | 30-70mcg/kg iv
42
drugs used to treat pheochromocytoma
phenoxabenzamine phentolamine proazosin
43
propofol iv dose
1.5-2.5mg/kg
44
propofol elimination half time
0.5-1.5hr
45
propofol mechanism of action
gaba activating opening of the chloride channel with resulting hyper polarization of cell membrane
46
how is propofol cleared
clearance of propofol from the plasma exceeds hepatic blood flow- possibly into the lungs. excreted by the kidneys
47
what is the major metabolic pathway for propofol
glucuronidation
48
who requires a smaller does of propofol
elderly patients require a lower induction dose as a result of a small central distribution volume and decreased clearance rate.
49
alfentanil dose
50-150mcg/kg | infusion 0.1-0.3mcg/kg/min
50
remifentanil dose
0. 5-1mcg/kg/min induction | 0. 05-0.8mcg/kg/min maintenance
51
propofol does not alter sa or av node function making it an acceptable drug for what proceudre
ablation
52
ketamine increases cerebral blood by what percent
60%
53
nifidepine excessive myocardial depression in which patients
beta blocked, aortic stenosis, left ventricular dysfunction
54
nifedipine activates baroreceptors leading to what
increased heart rate
55
nifedipine venous capacitance response
minimal effects on venous capacitance vessels
56
SE nifedipine
flushing vertigo and headache
57
amiodarone half time
29 days
58
volume distribution of amiodarone
large
59
what is the metabolite of amiodarone
desethylamiodarone longer half time than the drug result in accumulation.
60
how long can amiodarone last
60 days
61
amiodarone increases plasma concentrations of
``` dig procainamide quinidine warfarin cyclosporine ```