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Pharmacology 680 > Opioid specific drugs > Flashcards

Opioid specific drugs Flashcards

1
Q

▪ Gold standard or prototype for opioid agonists

-naturally occuring

A

morphine

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2
Q

-what is duration of action for morphine and why?

A

about 4 hours
-Comparatively low lipid solubility
▪ Moves slowly across the blood brain barrier

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3
Q

dose of morphine for anesthetic purposes?

A

0.1 – 0.2 mg/kg used IM as

premedication and IV

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4
Q

what mac level does morphine decrease with ceiling effect?

A

65%

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5
Q

why does only <0.1% of morphine administered enter the CNS at peak plasma
concentrations? (4 reasons)

A

– Low lipid solubility
– High degree of ionization at physiologic pH
– Protein binding
– Rapid conjugation with glucuronic acid

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6
Q

is morphine taken up by lungs?

A

no

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7
Q

morphine clearance?

A

Hepatic clearance is high and dependent on liver blood flow.

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8
Q

what are the two metabolites of morphine?

A

Morphine 3-glucuronide (75-85%) and

morphine 6-glucuronide (M6G) (5-10%)

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9
Q

Metabolites of morphine excreted..

A

renally, so renal failure causes accumulation of M6G and prolonged effect

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10
Q

in women, what are 4 differences to consider when giving morphine?

A

▪ Greater analgesic potency
▪ Slower offset
▪ No effect on apneic threshold
▪ Hypoxic sensitivity decreased

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11
Q

why should you Pretreat morphine with H1 and H2 blockers

A

histamine release is common, wont decrease the release but will block the decrease in SVR and BP

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12
Q

Discovered during search for synthetic atropinelike drug

A

demerol (meperidine)

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13
Q

Causes increase in heart rate, some large airway bronchodilation

really not used for anesthesia in adults

A

demerol

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14
Q

why does demerol cause an increase in N/V?

A

Sensitizes the labyrinthine apparatus

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15
Q

demerol is metabolized by demethylation in the liver to

A

normeperidine (90%) which is excreted by

the kidneys

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16
Q

Dose of demerol used for peds

A

0.5 to 1 mg/kg

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17
Q

Normeperidine side effects

A
  • cns stimulant - seizures
  • hallucinations
  • delirium
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18
Q

Meperidine duration is

A

typically 2-4 hours

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19
Q

(Demerol dose of

> 5 mg/kg) or renal failure can cause

A

seizures

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20
Q

why does demerol suppress postoperative shivering?

A

– May represent stimulation of kappa receptors or
decreased shivering threshold
– May also be related to the alpha2 receptor stimulation

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21
Q 
– Hypertension, tachycardia
– Diaphoresis, hyperthermia
– Confusion, agitation
– Neuromuscular changes – hyperreflexia
– Severe – coma, seizures, coagulopathy,
metabolic acidosis
A

Serotonin syndrome may be caused by

interaction of meperidine with MAOIs, tricyclics

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22
Q

Opioid designed for anesthesia

A

fentanyl

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23
Q

how much more potent is fentanyl than morphine?

A

100x

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24
Q

High lipid solubility of fentanyl explains

A

the rapid onset and greater potency

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25
Q

clinical duration of fentanyl

A

20-40 minutes

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26
Q

___ initial IV dose of fentanyl is taken up by the lungs

A

75%

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27
Q

Repeat doses of fentanyl accumulate in

A 
muscle (large compartment)
and fat (high lipid solubility)
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28
Q

with Repeated doses or an infusion of fentanyl, drug is stored in
the lungs, fat, and muscle causing

A

prolonged analgesia and respiratory depression

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29
Q

how is fentanyl metabolized

A

N-demethylation

Norfentanil most common in humans

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30
Q

3 metabolites of fentanyl

A

– Norfentanyl
– Hydroxyproprionyl-fentanyl
– Hydroxyproprionyl-norfentanyl

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31
Q

Elimination t ½ life of fentanyl is

A

3.1-6.6 hrs

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32
Q

Longer t ½ life of fentanyl is due to

A

o larger volume of distribution as fentanyl can move into tissues more rapidly than morphine.

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33
Q

what 3 reasons do the Elderly have prolonged elimination t ½ life with fentanyl?

A

– Decreases in hepatic blood flow
– Microsomal enzyme activity
– Decreases in albumin production (highly protein bound 79-87%)

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34
Q

what type of surgery is fentanyl duration prolonged with and why?

A

abdominal aortic surgery involving infrarenal aortic cross-clamping.

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35
Q

doses for fentanyl?

A

▪ 1 – 2 mcg/kg IV for analgesia

▪ 2 – 20 mcg/kg IV as a balanced technique to blunt circulatory responses

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36
Q

dose of fentanyl that dependably blunts the sympathetic response of larygoscopy?

A

– 5-8 mcg/kg

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37
Q

dose of fent that significantly reduces the dose of propofol for placement
of an LMA

A

▪ 0.5 mcg/kg

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38
Q

Large doses of fent (50-150 mcg/kg) can reduce MAC by up to

A

80%

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39
Q

Single dose of 3mcg/kg 25-30 minutes prior to incision can reduce iso or des MAC by

A

50%

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40
Q

Small doses (1mcg/kg) reduce MAC by

A

40%

41
Q

Advantages of Fentanyl (3)

A

▪ No direct myocardial depression
▪ No histamine release
▪ Suppresses stress response to surgery

42
Q

Disadvantages of Fentanyl

A

▪ Sympathetic stimulation in response to pain, especially with good LV function
▪ Unreliable amnesia
▪ Post-op respiratory depression

43
Q

▪ Cardiovascular effects of fent

A

– Heart rate decreases more than morphine
▪ Occasional decreases in BP and CO
– No histamine release

44
Q

▪ Muscular effects of fent?

A

– Myoclonus related to depression of inhibitory neurons – seizurelike with no EEG changes

45
Q

neuro effects of fent?

A

moderate increases in ICP (6-9) even

with unchanged PaCO2 bc of vasodilation and an increase in cerebral vascular resistance

46
Q

synergist of fent?

A

benzos, increased resp depression

prop

47
Q

what is a weird side effect caused by fent pre op?

A

reflex coughing

48
Q

Most potent opioid currently available

A

sufentanil

49
Q

what is pulmonary uptake of sufentanil?

A

60%

50
Q

Elimination t ½ life sufentanil?

A

2.5 hours

51
Q

Volume of distribution of sufentanil 1.17 L is smaller due to?

A

greater protein binding than fentanyl (92% v. 79-87%)

52
Q

how is sufentanil metabolized?

A

hepatic via N-dealkylation into inactive

metabolites which are eliminated by both the liver and kidneys

53
Q

why do we not typically use sufentanil for induction?

A
  • stiff chest syndrome
  • may render patient apneic but not unconscious
  • glottic obstruction
54
Q

sufentanil has a longer lasting and greater analgesic effect, what other effect is preferred

A

less respiratory depression

55
Q

what can sufentanil reduce mac by

A

up to 70%

56
Q

dose of sufentanil?

A

1/10 dose of fentanyl

Fent:
▪ 1 – 2 mcg/kg IV for analgesia
▪ 2 – 20 mcg/kg IV as a balanced technique to blunt circulatory responses

57
Q

Use of benzodiazepines along with iv infusion of sufentanil may necessitate

A

a decrease in dose of sufentanil - synergist

58
Q

After infusion for 3 hours, sufentanil will decrease by

A

80% more rapidly than fentanyl and alfentanil.

59
Q

After infusion for 8 hours, sufentanil will decrease by

A

50 % more rapidly than fentanyl or alfentanil.

60
Q

what is sufentanils shorter context sensitive half life due to.. compared to alfent

A

large Vd compared to alfentanil – due to metabolism and redistribution

61
Q

what medication is hard to detect an overdose during a case and why?

A

sufentanil, bp same even with 5x dose

62
Q

why is alfentanil Volume of distribution much smaller (4-6X) than fentanyl

A

due to lower lipid solubility and more protein binding

63
Q

Elimination t ½ life alfentanil

A

1.1-1.6 hrs

64
Q

best choice to give for a single, brief stimulus like laryngoscopy or retrobulbar block

A

alfentanil

65
Q

only 10% of alfentanil ionized at physiologic pH causes (onset alfent vs fent)

A

This causes faster onset or effect-site equilibration.

(A 1.4 mins; F-6.8 mins)

66
Q

this drug is more liable to produce stiff chest and greater euphoria

A

alfentanil

67
Q

Metabolism of alfentanil

A

n-dealkylation to noralfentanil and

amide N-dealkylation to N-phenylpropionamide

68
Q

what makes a standard infusion and dosing regimen difficult to determine with alfentanil?

A

Interindividual variability related to P-450 CYP3A enzyme

69
Q

when should alfentanil infusions be stopped?

A

15-25 mins before emergence

70
Q

Direct laryngoscopy dose alfentanil

A

– 15 mcg/kg 90 sec before blunts SBP and HR response

– 30mcg/kg blunts catecholamine response

71
Q

Induction dose alfentanil

A

– 150-300 mcg/kg given rapidly - unconsciousness

72
Q

Infusion dose of alfentanil with inhaled agent

A

Infusion 25 to 150 mcg/kg/hr

73
Q

difference in alfentanil and fentanyl with blood pressure response with dose given after stimulation

A

BP can be decreased with a dose of alfentanil after the

painful stimulation where fentanyl cannot

74
Q

5X more potent than fentanyl on a mg per mg basis

A

remifentanil

75
Q

Elimination t ½ time remifent

A

6-10 minutes

76
Q

remifentanil Metabolized by

A

nonspecific plasma and tissue esterases to inactive

metabolites which are excreted by the kidneys

77
Q

Context-sensitive half-time of remifent

A

Independent of infusion time
– Approximately 4 minutes
– Must give a longer-acting opioid to ensure analgesia when patient awakens

78
Q

what drug from fent group has greatest decrease in bp

A

remifent

30% decrease in SBP two minutes after administration

79
Q

clinical uses of remifent?

A

– Laryngoscopy
– Retrobulbar block
– Labor and delivery
– Desire rapid recovery – craniotomy, carotid endarterectomy

80
Q

what opioid has smallest Vd?

A

remifent so fast equilibration and fast offset

81
Q

▪ Induction dose remifent

A

1 mcg/kg over 60-90 sec

82
Q

dose if infusing remifent before iv anesthetic dose

A

0.5-1.0
mcg/kg over 10 minutes
Then,
infusion 0.05 to 2.0 mcg/kg/min IV

83
Q

MAC (Sedation case) with remifent dose?

A

0.05 – 0.10 mcg/kg/min with midazolam (2 mg IV)

84
Q

– Suggests acute opioid tolerance

– Tolerance is dose dependent

A

hyperalgesia

seen with remifent

85
Q

why do Patients receiving high doses of remifentanil require high post-op analgesics

A

– Possibly due to alteration in NMDA receptor

86
Q

what two things block opioid tolerance?

A

magnesium and ketamine

87
Q

a decrease in the response to a drug due to its continued administration

A

tolerance

88
Q

an increased response to a stimulus that is normally painful.

A

hyperalgesia

89
Q

Intermediate-acting semi-synthetic opioid

A

dilaudid (hydromorphone)

90
Q

what opioid is best for renal patients

A

dilaudid bc it lacks active metabolites

91
Q

1.5 mg of dilaudid is equivalent to

A

10 mg morphine or 100 mcg fentanyl

92
Q

dose dilaudid

A

0.02-0.06 mg/kg

93
Q

onset and duration of dilaudid

A

Onset: 5 minutes

▪ Duration: 4-5 hours (2-3 hrs ½ life)

94
Q

Metabolism of dilaudid and what opioid is it similar to

A

mostly phase II via glucuronic acid (similar to

morphine)

95
Q

Synthetic opioid

▪ Useful with chronic pain

A

methadone

96
Q

elimination t1/2 of methadone

A

35 hours

97
Q

MOA of tramadol the centrally acting analgesic

A

– Inhibits reuptake of NE and serotonin and inhibits release of presynaptic release of serotonin

98
Q

Advantages of tramadol (3)

A

– Treat shivering
– Minimal ventilatory depressant
– Less likely to cause addiction –

99
Q

disadvantages of tramadol

A

– Interaction w Coumadin, ondansetron
– Seizures
– Nausea and vomiting
-just po, iv not approved in US

Pharmacology 680 (19 decks)

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