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B&B Week 6 Flashcards > Lecture 15: Pharmacology and Intravenous Anesthetics > Flashcards

Lecture 15: Pharmacology and Intravenous Anesthetics Flashcards

1
Q

What are the 5 A’s of amnesia?

A
  1. amnesia
  2. anesthesia
  3. analgesia
  4. akinesia
  5. areflexia
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2
Q

When do you give sedatives or hypnotics?

A
  • ICU sedation
    • procedural sedation
    • seizure treatment
    • generalized anxiety disorder, panic disorder
    • ethanol withdrawal
    • insomnia
    • muscle spasms
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3
Q

What neurotransmitters are involved in sedation/hypnotics?

A 
GABA
Histamine
Serotonin
Norepinephrine
Acetylcholine
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4
Q

What is Hypnosis?

A

Leads to a state of unconsciousness (cause sleep)

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5
Q

What is sedation?

A

Leads to a decrease activity; calming, relaxing effect; does not necessarily induce sleep though it does at high doses

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6
Q

What are the Pharmacokinetic characteristics?

A

i. Route of administration
ii. Elimination
iii. Metabolism
iv. Distribution

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7
Q

What is the difference between drug elimination and redistribution?

A

Redistribution = measurement used to gauge the length of effect of drug in body
-as soon as drug redistributes, the drug effect is gone
Elimination doesn’t say anything about how long effects last)

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8
Q

When you give drug to patient, where does it go first?

A

Central compartment

Most well perfused (brain, kidney, liver)

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9
Q

Where does the drug go after the central compartment?

A

Fat (slowly equilibrating compartment)

Muscle (rapid equilibrating compartment)

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10
Q

How does drug stop working?

A

Because it has decreased concentration in central compartment…so you can have drug in body while it doesn’t do shit
That’s why redistribution is more important than elimination half-life

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11
Q

What is the context-sensitive half time?

A

The half-time of the drug depends on how long you give it

The longer you infuse a drug, the longer it takes to eliminate

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12
Q

What drugs have the longest context-sensitive half-time? Significance?

A

The ones that are most stored in fat (because the fat will release drugs into plasma once it has decreased in concentration in central compartment)
This means that the higher the context-sensitive half-time, the less likely you’re going to want to give this guy intravenously UNLESS you want to knock people out for a long ass time

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13
Q

What are the characteristics of pharmacodynamics?

A
  1. Receptor agonist, antagonist, partial agonist
  2. Genetic variability in receptor density and sensitivity
  3. Dosre response
  4. efficacy, potency, toxicity
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14
Q

What are examples of drugs with long context-sensitive half-times? Significance?

A
  1. Diazepam (longest)
  2. Thiopental
    You don’t want to give them because it is harder to control
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15
Q

What is the problem with fat soluble drugs?

A

We never get a steady state, because the drug distributes from plasma, to perfused tissues, muscle groups, then fat groups

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16
Q

What are key features of propofol?

A 
Milk of amnesia
Contraindicated in Egg allergy
Killed Michael Jackson
Used for the induction/maintenance of general anesthesia
Acts through GABA
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17
Q

Why is propofol a drug of abuse?

A
  1. Increases dopamine concentrations in nucleus accumbens
  2. Euphoria, feeling of well-being, like cocaine
  3. Sexual dreams
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18
Q

What are the adverse effects of propofol?

A
  1. VERY PAINFUL on injection
  2. propofol related infusion syndrome (PRI)
  3. Hypertriglyceridemia (because a calorie source) and pancreatitis
  4. decreased poly chemotaxis
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19
Q

What are the ABSOLUTE contraindications? Relative contraindications?

A
  1. egg protein and allergy to propofol
  2. hemodynamic instability (hypotension)
  3. awareness under anesthesia (for TIVA)
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20
Q

What is the redistribution half-life of propofol? Significance?

A

2-8 minutes

That means patient wakes up in 2-8 minutes

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21
Q

How is propofol metabolized?

A

Hepatic, renal

Glucuronidated or sulfated prior to excretion

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22
Q

For a kid how much propofol do you need vs. an elderly person?

A

Kid needs MORE propofol because more head in proportion of body…elderly person needs less

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23
Q

What is the MOA of propofol?

A
  • it potentiates the effects of GABA

- does NOT affect pain…only affects consciousness

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24
Q

What are the physiological effects?

A 
Loss of consciousness
HYPOtension
-vasodilation/sympathetic tone
Apnea
-bronchodilation, decreased response to hypercarbia and hypoxia
DECREASED respiration
-DECREASED cerebral metabolic rate
-DECREASED cerebral blood flow
Kind of like desflurane except desflurane has increased cerebral blood flow
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25
Q

What do you need to know about etomidate?

A

Used for INDUCTION of general anesthesia
Used for known or anticipated hemodynamic instability
Used for illness, cardiac anesthesia

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26
Q

What is the MOA of etomidate?

A

Potentiates the effects of GABA
No effects on pain
Causes adrenocortical suppression

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27
Q

What are the pharmacokinetic features of etomidate?

A

Redistribution = 2-8 minutes
Elimination = 3-5 hours (but this doesn’t say anything about how long effects last)
Metabolized by liver and excreted in urine/bile

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28
Q

What are the physiologic effects of etomidate?

A

It does NOT fuck with cardiovascular system so no hypotension
It does NOT fuck with respiratory system so no respiratory depression
Can cause seizures
Same neurologic effects as propofol (decreased metabolism and blood flow in brain)

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29
Q

What are the adverse effects of etomidate?

A
  • adrenal suppression

- INCREASED postop NAUSEA/vomiting relative to propofol

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30
Q

What are the absolute contraindications of etomidate?

A 
Allergy to etomidate
Relative: adrenal insufficiency
-critical illness
-history of postop nausea/vomiting
Therefore it is NOT abusable lmao
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31
Q

What is thiopental?

A 
A BARBITURATE
Used in the second world war and in lethal injections
Related to phenobarbital, pento barbital
Acidic motherfuckerr
Cousins used for seizure therapy lol
Potentiates effect on GABA
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32
Q

What do you need to know about thiopental?

A

Used for INDUCTION general anesthesia

-related to drugs that help induce seizures

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33
Q

What are the pharmacokinetic features of thiopental?

A

5-10 half life redistribution
Metabolism: in the liver and excreted into kidneys
It is an EXCEPTION to rule of hepatic metabolism because it is largely unchanged when excreted in kidney
-zero order kinetics at high doses

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34
Q

Which IV anesthetic is not metabolized in the liver?

A

Thiopental

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35
Q

What are the contraindications of thiopental?

A

Acute Intermittent Porphyria

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36
Q

What is the MOA of thiopental?

A

Barbiturates bind to post-synaptic GABA receptor

  • increase the duration of chloride channel opening when GABA binds
  • activates chloride flow in absence of GABA
How well did you know this?
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37
Q

What are the physiologic effects of thiopental?

A

Same as propofol

Exception: Methohexital DECREASES seizure threshold relative to other induction agents

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38
Q

What are the adverse effects of thiopental?

A

Garlic/onion taste

  • tissue irritation/necrosis
  • stimulation of porphyrin formation
  • ANTI-analgesic effect
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39
Q

What are absolute contraindications in thiopental? Relative contraindications?

A

ACUTE INTERMITTENT PORPHYRIA
Allergy to thiopental
And
Hemodynamic instability/questionable IV access

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40
Q

What drug is ketamine most like?

A

PCP (phencyclidine)

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41
Q

What is porphyrin?

A

A group of organic compounds

Example: heme

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42
Q

What does Ketamine do to you?

A

Causes dissociative hypnosis
A lot like PCP or Phencyclidine…PCP allows you to have dissociative hypnosis
Used as recreational drug
S-enantiomer has all the nice effects
R-enantiomer has all the negative effects

How well did you know this?
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43
Q

What is the key delineating factor of ketamine?

A

You don’t have to give it IV (can give it PO, IM, intranasal, etc.)
It is DIFFERENT from the other three IV anesthetics (etomidate, propofol, thiopental)
Has analgesic effect

44
Q

What are pharmokinetics of ketmamine?

A

11-16 mins of redistribution half-life
Elimination = 203 hours
Metabolism = hepatic degradation

45
Q

What are the desirable properties of ketamine?

A 
IV, PO, IM intranasal
Analgesic (only IV anesthetic that is analgesic)
Hypnotic/amnestic 
Maintains sympathetic tone…HYPERtension
POTENT bronchodilator/analgesic 
Preserves respiration
46
Q

What is the MOA of ketamine?

A

Primary NMDA receptor ANTAGONIST

47
Q

What are the undesirable properties of ketamine?

A

Increase salivation/lacrimation
Causes dysphoria (a state of unhappiness)
Increase intracranial pressure
Increased myocardial work

48
Q

What are the adverse effects?

A

Salivation
Dysphoria/dissociation
Sympathetic stimulation (tachycardia and hypertension)

49
Q

Absolute contraindications of ketamine? Relative contraindications?

A 
Allergy to ketamine
And
Psychosis
Compromised myocardial function
Intracranial hypertension
50
Q

What are examples of other sedative/hypnotics

A
  1. benzodiazepines (important)
  2. opioids (important)
  3. alpha-2 adrenoreceptor antagonists
  4. dopamine antagonists
  5. antihistamines
  6. Z-drugs
  7. Melatonin agonists
  8. general anesthetics like halothane, flurane
51
Q

What is the sedative ingredient in Tylenol PM?

A

Diphenhydramine

-a sedative

52
Q

What is diphenhydramine?

A

The sedative ingredient in Tylenol

53
Q

What are the delineating factors of Propofol?

A
  • rapid onset/offset
    • used for anesthetic induction, TIVA (total intravenous anesthetic), ICU sedation
    • partially metabolized by EXTRAhepatic tissues
    • causes hemodynamic instability
54
Q

What are the delineating factors of Etomidate?

A
  • drug of choice in hemodynamically compromised patients (little physiological effects)
    • causes adrenocortical suppression
    • causes NAUSEA and VOMITING
55
Q

What are the delineating factors Thiopental

A
  • very similar to propofol in pharmacokinetic properties

- contraindicated in porphyria

56
Q

What are the delineating factors of Ketamine?

A
  • causes sympathetic stimulation
    • potent analgesic
    • causes dissociative anesthesia and dysphoria
    • contraindicated in psychosis
    • does NOT REQUIRE IV access (can be given PO)
57
Q

Why do IV induction agents cause hypotension?

A

Decrease vasomotor tone
Decrease cardiac output
Myocardial depression

58
Q

What anesthetic do you give A 25 yo man with developmental delay, claustrophobia, fear of needles and no IV access presenting for inguinal hernia repair?

A

Ketamine

59
Q

How does drug stop working?

A

Because it has decreased concentration in central compartment…so you can have drug in body while it doesn’t do shit
That’s why redistribution is more important than elimination half-life

60
Q

What is the context-sensitive half time?

A

The half-time of the drug depends on how long you give it

The longer you infuse a drug, the longer it takes to eliminate

61
Q

What drugs have the longest context-sensitive half-time? Significance?

A

The ones that are most stored in fat (because the fat will release drugs into plasma once it has decreased in concentration in central compartment)
This means that the higher the context-sensitive half-time, the less likely you’re going to want to give this guy intravenously UNLESS you want to knock people out for a long ass time

62
Q

What are the characteristics of pharmacodynamics?

A
  1. Receptor agonist, antagonist, partial agonist
  2. Genetic variability in receptor density and sensitivity
  3. Dosre response
  4. efficacy, potency, toxicity
63
Q

What are examples of drugs with long context-sensitive half-times? Significance?

A
  1. Diazepam (longest)
  2. Thiopental
    You don’t want to give them because it is harder to control
64
Q

What is the problem with fat soluble drugs?

A

We never get a steady state, because the drug distributes from plasma, to perfused tissues, muscle groups, then fat groups

65
Q

What are key features of propofol?

A 
Milk of amnesia
Contraindicated in Egg allergy
Killed Michael Jackson
Used for the induction/maintenance of general anesthesia
Acts through GABA
66
Q

Why is propofol a drug of abuse?

A
  1. Increases dopamine concentrations in nucleus accumbens
  2. Euphoria, feeling of well-being, like cocaine
  3. Sexual dreams
67
Q

What are the adverse effects of propofol?

A
  1. VERY PAINFUL on injection
  2. propofol related infusion syndrome (PRI)
  3. Hypertriglyceridemia (because a calorie source) and pancreatitis
  4. decreased poly chemotaxis
68
Q

What are the ABSOLUTE contraindications? Relative contraindications?

A
  1. egg protein and allergy to propofol
  2. hemodynamic instability (hypotension)
  3. awareness under anesthesia (for TIVA)
69
Q

What is the redistribution half-life of propofol? Significance?

A

2-8 minutes

That means patient wakes up in 2-8 minutes

70
Q

How is propofol metabolized?

A

Hepatic, renal

Glucuronidated or sulfated prior to excretion

71
Q

For a kid how much propofol do you need vs. an elderly person?

A

Kid needs MORE propofol because more head in proportion of body…elderly person needs less

72
Q

What is the MOA of propofol?

A
  • it potentiates the effects of GABA

- does NOT affect pain…only affects consciousness

73
Q

What are the physiological effects?

A 
Loss of consciousness
HYPOtension
-vasodilation/sympathetic tone
Apnea
-bronchodilation, decreased response to hypercarbia and hypoxia
DECREASED respiration
-DECREASED cerebral metabolic rate
-DECREASED cerebral blood flow
Kind of like desflurane except desflurane has increased cerebral blood flow
74
Q

What do you need to know about etomidate?

A

Used for INDUCTION of general anesthesia
Used for known or anticipated hemodynamic instability
Used for illness, cardiac anesthesia

75
Q

What is the MOA of etomidate?

A

Potentiates the effects of GABA
No effects on pain
Causes adrenocortical suppression

76
Q

What are the pharmacokinetic features of etomidate?

A

Redistribution = 2-8 minutes
Elimination = 3-5 hours (but this doesn’t say anything about how long effects last)
Metabolized by liver and excreted in urine/bile

77
Q

What are the physiologic effects of etomidate?

A

It does NOT fuck with cardiovascular system so no hypotension
It does NOT fuck with respiratory system so no respiratory depression
Can cause seizures
Same neurologic effects as propofol (decreased metabolism and blood flow in brain)

78
Q

What are the adverse effects of etomidate?

A
  • adrenal suppression

- INCREASED postop NAUSEA/vomiting relative to propofol

79
Q

What are the absolute contraindications of etomidate?

A 
Allergy to etomidate
Relative: adrenal insufficiency
-critical illness
-history of postop nausea/vomiting
Therefore it is NOT abusable lmao
80
Q

What is thiopental?

A 
A BARBITURATE
Used in the second world war and in lethal injections
Related to phenobarbital, pento barbital
Acidic motherfuckerr
Cousins used for seizure therapy lol
Potentiates effect on GABA
81
Q

What do you need to know about thiopental?

A

Used for INDUCTION general anesthesia

-related to drugs that help induce seizures

82
Q

What are the pharmacokinetic features of thiopental?

A

5-10 half life redistribution
Metabolism: in the liver and excreted into kidneys
It is an EXCEPTION to rule of hepatic metabolism because it is largely unchanged when excreted in kidney
-zero order kinetics at high doses

83
Q

Which IV anesthetic is not metabolized in the liver?

A

Thiopental

84
Q

What are the contraindications of thiopental?

A

Acute Intermittent Porphyria

85
Q

What is the MOA of thiopental?

A

Barbiturates bind to post-synaptic GABA receptor

  • increase the duration of chloride channel opening when GABA binds
  • activates chloride flow in absence of GABA
86
Q

What are the physiologic effects of thiopental?

A

Same as propofol

Exception: Methohexital DECREASES seizure threshold relative to other induction agents

87
Q

What are the adverse effects of thiopental?

A

Garlic/onion taste

  • tissue irritation/necrosis
  • stimulation of porphyrin formation
  • ANTI-analgesic effect
88
Q

What are absolute contraindications in thiopental? Relative contraindications?

A

ACUTE INTERMITTENT PORPHYRIA
Allergy to thiopental
And
Hemodynamic instability/questionable IV access

89
Q

What drug is ketamine most like?

A

PCP (phencyclidine)

90
Q

What is porphyrin?

A

A group of organic compounds

Example: heme

91
Q

What does Ketamine do to you?

A

Causes dissociative hypnosis
A lot like PCP or Phencyclidine…PCP allows you to have dissociative hypnosis
Used as recreational drug
S-enantiomer has all the nice effects
R-enantiomer has all the negative effects

92
Q

What is the key delineating factor of ketamine?

A

You don’t have to give it IV (can give it PO, IM, intranasal, etc.)
It is DIFFERENT from the other three IV anesthetics (etomidate, propofol, thiopental)
Has analgesic effect

93
Q

What are pharmokinetics of ketmamine?

A

11-16 mins of redistribution half-life
Elimination = 203 hours
Metabolism = hepatic degradation

94
Q

What are the desirable properties of ketamine?

A 
IV, PO, IM intranasal
Analgesic (only IV anesthetic that is analgesic)
Hypnotic/amnestic 
Maintains sympathetic tone…HYPERtension
POTENT bronchodilator/analgesic 
Preserves respiration
95
Q

What is the MOA of ketamine?

A

Primary NMDA receptor ANTAGONIST

96
Q

What are the undesirable properties of ketamine?

A

Increase salivation/lacrimation
Causes dysphoria (a state of unhappiness)
Increase intracranial pressure
Increased myocardial work

97
Q

What are the adverse effects?

A

Salivation
Dysphoria/dissociation
Sympathetic stimulation (tachycardia and hypertension)

98
Q

Absolute contraindications of ketamine? Relative contraindications?

A 
Allergy to ketamine
And
Psychosis
Compromised myocardial function
Intracranial hypertension
99
Q

What are examples of other sedative/hypnotics

A
  1. benzodiazepines (important)
  2. opioids (important)
  3. alpha-2 adrenoreceptor antagonists
  4. dopamine antagonists
  5. antihistamines
  6. Z-drugs
  7. Melatonin agonists
  8. general anesthetics like halothane, flurane
100
Q

What is the sedative ingredient in Tylenol PM?

A

Diphenhydramine

-a sedative

101
Q

What is diphenhydramine?

A

The sedative ingredient in Tylenol

102
Q

What are the delineating factors of Propofol?

A
  • rapid onset/offset
    • used for anesthetic induction, TIVA (total intravenous anesthetic), ICU sedation
    • partially metabolized by EXTRAhepatic tissues
    • causes hemodynamic instability
103
Q

What are the delineating factors of Etomidate?

A
  • drug of choice in hemodynamically compromised patients (little physiological effects)
    • causes adrenocortical suppression
    • causes NAUSEA and VOMITING
104
Q

What are the delineating factors Thiopental

A
  • very similar to propofol in pharmacokinetic properties

- contraindicated in porphyria

105
Q

What are the delineating factors of Ketamine?

A
  • causes sympathetic stimulation
    • potent analgesic
    • causes dissociative anesthesia and dysphoria
    • contraindicated in psychosis
    • does NOT REQUIRE IV access (can be given PO)
106
Q

Why do IV induction agents cause hypotension?

A

Decrease vasomotor tone
Decrease cardiac output
Myocardial depression

107
Q

What anesthetic do you give A 25 yo man with developmental delay, claustrophobia, fear of needles and no IV access presenting for inguinal hernia repair?

A

Ketamine

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