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Pharmacology Exam 2 > IV Anesthetics > Flashcards

IV Anesthetics Flashcards

(128 cards)

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1
Q

What is the chemical name for Propofol?

A

2,6-diisopropylphenol

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2
Q

What preservatives are found in the generic formulation of Propofol and what are the clinical implications?

A

sodium metabisulfite-bronchospasm
benzyl alcohol-avoid in infants

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3
Q

What is the mechanism of action of Propofol?

A

direct GABA-A agonist
change in Cl- conductance
neuronal hyperpolarization

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4
Q

What is the dose of propofol for induction? Infusion?

A

Induction: 1.5-2.5 mg/kg
Infusion: 25-200 mcg/kg/min

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5
Q

What is the onset of propofol?

A

30-60 seconds

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6
Q

What is the duration of propofol?

A

5-10 minutes

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7
Q

How is propofol cleared?

A

Liver P450 enzymes and extrahepatic metabolism mostly in the lungs
*clearance exceeds liver blood flow

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8
Q

What is the active metabolite of propofol?

A

none

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9
Q

What are the cardiovascular effects of propofol?

A

decreased BP, SVR, venous tone, preload, myocardial contractility

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10
Q

What are the respiratory effects of propofol?

A

shifts CO2 curve down and to the right (less sensitive to CO2)
respiratory depression
inhibits hypoxic ventilatory drive

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11
Q

What are the CNS effects of Propofol?

A

decreased CMRO2, CBF, ICP, IOP
NO ANALGESIA
anticonvulsant properties
myoclonus may occur
rarely seizures may occur

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12
Q

What are some other properties of propofol that are relevant?

A

antioxidant properties
change the color of urine (green-phenol, cloudy-increased uric acid)
antipruritic: 10 mg IV (spinal opioids and cholestasis)
antiemetic: 10-20 mg

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13
Q

What are the risk factors for propofol infusion syndrome?

A

propofol dose >4 mcg/kg/hr
propofol infusion duration >48 hours
sepsis
continuous catecholamine infusions
high dose steroids
significant cerebral injury

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14
Q

What are the clinical signs of propofol infusion syndrome?

A

acute refractory bradycardia leading to asystole plus at least one:
-metabolic acidosis
-rhabdomyolysis
-enlarged or fatty liver
-renal failure
-hyperlipidemia
-lipemia (early sign)

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15
Q

How do you treat propofol infusion syndrome?

A

discontinue propofol, maximize gas exchange, cardiac pacing, PDE inhibitors, glucagon, ECMO, CRRT

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16
Q

How long is a propofol syringe good for? Tubing?

A

syringe: 6 hours
tubing: 12 hours

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17
Q

What is the chemical name for fospropofol?

A

phosphono-O-methyl-2,6-diisopropylphenol

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18
Q

How does the formulation of Fospropofol differ from Propofol?

A

made in an aqueous solution which prevents burning and doesn’t support microbial growth

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19
Q

What is Fospropofol’s mechanism of action?

A

-prodrug metabolized to Propofol by alkaline phosphatase
-GABA-A agonist

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20
Q

What is the dose of Fospropofol?

A

initial bolus: 6.5 mg/kg
repeat bolus: 1.6 mg/kg

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21
Q

What is the onset of Fospropofol?

A

5-13 minutes

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22
Q

What is the duration of Fospropofol?

A

15-45 minutes

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23
Q

How is Fospropofol cleared?

A

same as propofol
liver P450 enzymes and extrahepatic metabolism mostly in the lungs

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24
Q

What is Fospropofol metabolized into?

A

Propofol, formaldehyde, and phosphate

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25
What is a major side effect of Fospropofol?
genital and anal burning
26
What is the chemical name for ketamine?
2-(o-cholophenyl)-2 (methylamino) cycloheanone hydrochloride
27
What medication class is Ketamine from?
arylcyclohexylamine
28
What is the formulation for Ketamine?
racemic mixture of 1, 5, or 10% solutions
29
What is the mechanism of action for Ketamine?
NMDA receptor antagonist (antagonizes glutamate) secondary receptors: opioid, MAO, serotonin, NE, muscarinic, Na+ channels
30
What is the dose of Ketamine?
induction: 1-2 mg/kg maintenance: 1-3 mg/kg analgesia: 0.1-0.5 mg/kg IM: 4-8 mg/kg PO: 10 mg/kg
31
What is the onset of Ketamine?
IV: 30-60 seconds IM: 2-4 minutes PO: variable
32
What is the duration of Ketamine?
10-20 minutes (60-90 minutes to full orientation)
33
How is Ketamine cleared?
liver P450 enzymes
34
What effect does chronic ketamine use have?
induces the enzymes that metabolize it leading to rapid escalation in tolerance
35
What is the active metabolite of Ketamine?
Norketamine (1/3-1/5 potency) excreted in the urine
36
What are the cardiovascular effects of Ketamine?
increased SNS tone, CO, HR, SVR, PVR myocardial depressant
37
What are the respiratory effects of Ketamine?
bronchodilation increased oral and pulmonary secretions no effect on upper airway muscle tone, airway reflexes, respiratory drive, CO2 response curve
38
What are the CNS effects of Ketamine?
increased CMRO2, ICP, CBF, & EEG activity possible increased IOP nystagmus or blepharospasm emergence delirium (prevent w/benzos)
39
True or False: Ketamine relieves somatic pain more than visceral pain.
True
40
What is the chemical name for Etomidate?
R-1-methyl-1-(a-methylbenzyl) imidazole -5-carboxylate
41
What medication class is Etomidate from?
Imidazole
42
When given in physiologic pH, is Etomidate more lipid or water-soluble?
lipid soluble
43
What are the two formulations of Etomidate?
35% Propylene glycol (more painful) lipid emulsion (less painful)
44
What is the mechanism of action of Etomidate?
GABA-A agonist
45
What is the dose of Etomidate?
0.2-0.4 mg/kg
46
What is the onset of Etomidate?
30-60 seconds
47
What is the duration of Etomidate?
5-15 minutes
48
How is Etomidate cleared?
Liver (P450 enzymes) & non-specific plasma esterases
49
True or False: With Etomidate, rapid awakening is due to redistribution.
True
50
What is the active metabolite of Etomidate?
none
51
What are the cardiovascular effects of Etomidate?
minimal change in HR, SV, & CO decreased SVR & BP no block to SNS from laryngoscopy
52
What are the respiratory effects of Etomidate?
mild respiratory depression
53
What are the CNS effects of Etomidate?
decreased CMRO2, CBF, ICP cerebral perfusion pressure same NO ANALGESIA
54
Does Etomidate increase the risk of seizures?
no hx of seizures: no increased risk hx of seizures: increased risk of seizures and seizure-like activity
55
Why is Etomidate use avoided in patients with Addison's disease or sepsis?
Etomidate inhibits 11-beta-hydroxylase and 17-beta-hydroxylase which are required for cortisol and aldosterone synthesis
56
True or False: Nausea and vomiting rates are more common with Etomidate than with other induction agents.
True as high as 30-40%
57
What are thiobarbiturates?
sulfur molecule in the 2nd position increases lipid solubility & potency ex. Thiopental, Thiamylal
58
What are oxybarbiturates?
oxygen molecule in the 2nd position ex. Methohexital, Pentobarbital
59
What does adding a methyl group to the nitrogen of barbiturates do?
lowers the seizure threshold and increases potency ex. Methohexital
60
What does adding a methyl group to the nitrogen of barbiturates do?
decreases seizure threshold and increases potency ex. Methohexital
61
What is the chemical name for Thiopental?
5-ethyl-5-(1-methylbutyl)-2-thiobarbituric acid
62
What medication class does Thiopental come from?
barbiturate
63
What is the formulation of Thiopental?
water soluble precipitates when mixed with acidic solution
64
What is the mechanism of action of Thiopental?
GABA-A agonist low dose: increases affinity for GABA for receptor high dose: directly stimulates GABA-A receptor
65
What is the dose for Thiopental?
adults: 2.5-5 mg/kg peds: 5-6 mg/kg
66
What is the onset of Thiopental?
30-60 seconds
67
What is the duration of action of Thiopental?
5-10 minutes
68
How is Thiopental cleared?
Liver (P450 enzymes) *repeated doses>tissue accumulation>prolonged wake up and hangover effect
69
True or False: With Thiopental, rapid awakening is determined by redistribution.
True
70
What is the active metabolite of Thiopental?
low dose: none high dose: Pentobarbital
71
What are the cardiovascular effects of Thiopental?
hypotension (vasodilation, decreased preload, myocardial depression) reflex tachycardia (maintains CO)
72
What are the respiratory effects of Thiopental?
shifts CO2 curve to right respiratory depression bronchoconstriction (histamine release)
73
What are the CNS effects of Thiopental?
decreased CMRO2, CBF, ICP, EEG NO ANALGESIA focal neuroprotection
74
What occurs with intra-arterial injection of Thiopental?
intense vasoconstriction, crystal formation, inflammation > tissue necrosis
75
How do you treat intra-arterial injection of Thiopental?
phentolamine or phenoxybenzamine stellate ganglion block or brachial plexus block
76
Which barbiturate is the gold standard for electroconvulsive therapy? What is the dose?
Methohexital 1-1.5 mg/kg
77
Which barbiturate is excreted unchanged in the urine?
Phenobarbital *not metabolized by P450 enzymes
78
What is acute intermittent porphyria?
caused by a defect in heme synthesis that promotes the accumulation of heme precursors
79
What is AIP made worse by?
stimulation of ALA synthase emotional stress prolonged NPO status CYP450 induction
80
What are the signs and symptoms of AIP?
severe abdominal pain N/V anxiety/confusion/psychosis coma skeletal muscle weakness bulbar weakness
81
What drugs should be avoided in patients with AIP?
barbiturates etomidate ketamine ketorolac amiodarone calcium channel blockers birth control pills
82
How do you treat AIP?
HYDRATION glucose supplementation heme arginate prevent hypothermia
83
What drugs are safe in patients with AIP?
volatile anesthetics nitrous oxide NMBs NMB reversals narcotics midazolam ondansetron vasopressors beta-blockers
84
What is the chemical name for Dexmedetomidine?
(S)-4-(1-(2,3-dimethylphenyl)ethyl)-1H-imidazole monohydrochloride
85
What medication class is Dexmedetomidine from?
Imidazole
86
What is the formulation of Dexmedetomidine?
water soluble Vial: 100 mcg/mL Infusion: 4 mcg/mL
87
What is the mechanism of action of Dexmedetomidine?
alpha-2 agonist of presynaptic nerve sedation: inhibits the locus coerulus in the pons analgesia: dorsal horn of spinal cord
88
What is the dose of Dexmedetomidine?
loading: 1 mcg/kg over 10 minutes maintenance: 0.4-0.7 mcg/kg/hr
89
What is the onset of Dexmedetomidine?
10-20 minutes with loading dose
90
What is the duration of Dexmedetomidine?
10-30 minutes after infusion stopped
91
How is Dexmedetomidine cleared?
Liver (P450 enzymes)
92
What is the active metabolite of Dexmedetomidine?
none
93
What are the cardiovascular effects of Dexmedetomidine?
hypotension bradycardia
94
What side effect does rapid administration of Dexmedetomidine cause?
short-lived hypertension alpha-2 stimulation in vasculature before SNS tone reduction in CNS
95
What are the respiratory effects of Dexmedetomidine?
NO respiratory depression
96
What are the CNS effects of Dexmedetomidine?
decreased CBF ANALGESIA NO change: CMRO2, ICP resembles sleep not reliable amnestic anti-shivering (impairs thermoregulatory response)
97
Why is Dexmedetomidine good for neuro surgery?
does not impair evoked potentials useful for "wake-up" test for scoliosis
98
How can you give Dexmedetomidine to a child without an IV?
nasal or buccal route 3-4 mcg/kg 1 hour before surgery
99
What is the chemical name for Midazolam?
8-chloro-6-(2-fluorophenyl)-1-methyl-4-H-imidazo(1,5-a)(1,4) benzodiazepine
100
What medication class is Midazolam from?
Benzodiazepine
101
What is the formulation of Midazolam?
imidazole ring
102
When given in physiologic pH, is Midazolam more lipid or water-soluble?
lipid soluble
103
What is the mechanism of action of Midazolam?
GABA-A agonist increased frequency of channel opening
104
What is the dose of Midazolam?
IV sedation: 0.01-0.1 mg/kg IV induction: 0.1-0.4 mg/kg PO sedation peds: 0.5-1 mg/kg
105
What is the onset of Midazolam?
30-60 seconds
106
What is the duration of action of Midazolam?
IV: 20-60 minutes
107
How is Midazolam cleared?
Liver and intenstine by P450 enzymes
108
What is the active metabolite of Midazolam?
1-hydroxymidazolam 1/2 potent, rapidly conjugated to inactive renal failure prolongs the effect
109
What are the cardiovascular effects of Midazolam?
minimal effects for sedation decreased SVR and BP for induction
110
What are the respiratory effects of Midazolam?
minimal effects for sedation respiratory depression for induction (COPD patients more sensitive) opioids potentiate respiratory depression
111
What are the CNS effects of Midazolam?
minimal effects on CMRO2 & CBF for sedation decreased CMRO2 and CBF for induction anterograde amnesia anticonvulsant anxiolysis spinally mediated skeletal muscle relaxation NO ANALGESIA
112
Why does Diazepam remain in the body for so long?
undergoes enterohepatic recirculation t1/2=43 hours
113
What are good uses for Diazepam?
anticonvulsant prevention of emergence delirium after ketamine antispasmodic (muscle spasticity)
114
Why is Lorazepam limited for being an anticonvulsant?
it has a slow onset
115
What is the relative potency (greatest to least): diazepam lorazepam midazolam
lorazepam > midazolam > diazepam LMD sounds like L & D
116
What is added to diazepam and lorazepam to enhance water solubility?
Propylene glycol *causes venous irritation (diazepam > lorazepam)
117
What is the dose for remimazolam?
induction: 2.5-5 mg over 1 minute for maintenance: 2.5 mg over 15 seconds Q2min
118
What is the half-time of Remimazolam?
0.5-2 minutes
119
How is Remimazolam cleared?
non-specific plasma esterases
120
What are the benefits of Remimazolam over Midazolam?
faster onset of action, deeper sedation, faster recovery
121
What are the benefits of Remimazolam over Propofol?
less respiratory depression and better cardiopulmonary stability
122
What is the reversal for Remimazolam?
Flumazenil
123
What is the mechanism of action of Flumazenil?
competitive GABA-A antagonist
124
What is the duration of action of Flumazenil?
30-60 minutes
125
What is the dose of Flumazenil?
initial: 0.2 mg IV 0.1 mg increments Q1min
126
How is reversal of benzodiazepines different from reversal of opioids?
Flumazenil does NOT increase SNS tone, anxiety, or neuroendocrine evidence of stress
127
What side effects can occur when giving Flumazenil to a benzodiazepine-dependent patient?
signs of withdrawal including seizures
128
True or False: Flumazenil usually reverses sedative effects with greater effect than amnestic effects.
True

Pharmacology Exam 2 (5 decks)

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