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
Q

what are the effects of sufentanil on the heart

A

bradycardia- decreases co

26
Q

what is the skeletal muscle rigidity seen with fentanyls

A

obstruction at the level of the glottis- resolved with intubation

27
Q

alfentaily is comparable to

A

fentanyl

28
Q

what prolongs alfentanil elimination

A

cirrhosis of the liver- renal failure not an issue

29
Q

alfentanil- how much of the drug exists in nonionized form

A

90%- meaning it has rapid effect and is a result of the low PKA.

30
Q

what is a main concern with administering alfentanil

A

it has a 10 fold inter individual variability in systemic clearance

31
Q

clinical use of alfentanil

A

rapid onset and off set

unlike other opioids- supplemental doses decrease systemic blood pressure that is increased after painful stimulation.

32
Q

remifentanil potency is similar to

A

fentanyl

33
Q

remifentail is unique why

A

it is susceptible to hydrolysis by nonspecific plasma and tissue esterase to inactive metabolites.

34
Q

how do you dose remifentanil

A

lean body mass

35
Q

how fast does remifentanil reach a steady state

A

10 minutes

36
Q

is remifentanil effected by renal or hepatic failure

A

no due to esterase metabolsim

37
Q

what case can you think of that requires profound analgesic effect transiently and remifentanil should be used

A

retrobulbar block.

38
Q

before turning off remifentanil infusion what must occur

A

a longer acting opioid should be administered to ensure analgesia when the patient awakens

39
Q

how much does cardiopulmonary bypass decrease clearance of remifentanil

A

20%

40
Q

phenoxabenzamine dose

A

0.5-1mg/kg PO prior to surgery

41
Q

phentolamine dose

A

0.1-2mg/min

30-70mcg/kg iv

42
Q

drugs used to treat pheochromocytoma

A

phenoxabenzamine
phentolamine
proazosin

43
Q

propofol iv dose

A

1.5-2.5mg/kg

44
Q

propofol elimination half time

A

0.5-1.5hr

45
Q

propofol mechanism of action

A

gaba activating opening of the chloride channel with resulting hyper polarization of cell membrane

46
Q

how is propofol cleared

A

clearance of propofol from the plasma exceeds hepatic blood flow- possibly into the lungs.

excreted by the kidneys

47
Q

what is the major metabolic pathway for propofol

A

glucuronidation

48
Q

who requires a smaller does of propofol

A

elderly patients require a lower induction dose as a result of a small central distribution volume and decreased clearance rate.

49
Q

alfentanil dose

A

50-150mcg/kg

infusion 0.1-0.3mcg/kg/min

50
Q

remifentanil dose

A
  1. 5-1mcg/kg/min induction

0. 05-0.8mcg/kg/min maintenance

51
Q

propofol does not alter sa or av node function making it an acceptable drug for what proceudre

A

ablation

52
Q

ketamine increases cerebral blood by what percent

A

60%

53
Q

nifidepine excessive myocardial depression in which patients

A

beta blocked, aortic stenosis, left ventricular dysfunction

54
Q

nifedipine activates baroreceptors leading to what

A

increased heart rate

55
Q

nifedipine venous capacitance response

A

minimal effects on venous capacitance vessels

56
Q

SE nifedipine

A

flushing vertigo and headache

57
Q

amiodarone half time

A

29 days

58
Q

volume distribution of amiodarone

A

large

59
Q

what is the metabolite of amiodarone

A

desethylamiodarone longer half time than the drug result in accumulation.

60
Q

how long can amiodarone last

A

60 days

61
Q

amiodarone increases plasma concentrations of

A
dig
procainamide
quinidine
warfarin
cyclosporine