Induction Drugs Flashcards

1
Q

Gold standard for IV anesthetics

A

Barbs

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2
Q

barbituric acid is composed of

A

urea + malonic acid

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3
Q

Barbs: sedative & hypnotic properties are determined by alterations in which carbon atoms?

A

2 & #5

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4
Q

Name the oxybarbiturates

A

Methohexital
Phenobarbital
Pentobarbital
Secobarbital

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5
Q

The characteristic effect of methohexital due to methyl group on the nitrogen

A

Increased risk of excitatory phenomenon, seizures, and hiccoughs

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6
Q

The phenyl group at the #5 position for Phenobarbital leads to what drug effect?

A

increased anticonvulsant properties

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7
Q

How do pentobarbital and secobarbital differ in chemical structure from the other oxybarbiturates?

A

O2 atom at the #2 carbon atom

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8
Q

Name the two Thiobarbiturates.

A

Thiopental
Thiamylal

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9
Q

How does the chemical structure of thiobarbiturates differ, and what does this mean for the drug characteristics?

A

There is sulfur at the #2 carbon atom. This leads to increased lipid solubility and hypnotic potency.

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10
Q

Barbs MOA

A

Increase affinity for GABA. Barbs can also mimic GABA and activate chloride channels even with no GABA present.

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11
Q

How does the metabolism of oxybarbs and thiobarbs differ?

A

Oxybarbs = Liver
Thiobarbs = Liver, Kidney, Brain

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12
Q

Intra-arterial injection of which barb can lead to cyanosis and gangrene?

A

Thiobarb

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13
Q

What effect does sustained delivery of barbs have on liver enzymes, and which medication is the biggest culprit?

A

Liver enzymes are induced leading to increased metabolism of drugs. Phenobartibal is the most potent liver enzyme inducer.

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14
Q

Liver enzyme induction accelerates the metabolism of which drugs?

A

oral anticoagulants
phenytoin
TCA
corticosteroids
bile salts
vitamin K

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15
Q

What is Porphyria, and what drug class is avoided by patients presenting with it?

A

The autosomal dominant disease leads to defective heme metabolism. This leads to neurological damage, peripheral and autonomic neuropathies, and psychiatric manifestations.
Barbiturates should be avoided.

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16
Q

Why are barbiturates bad for patients with AIP?

A

Barbiturates accelerate heme production. AIP presents as a defect in heme metabolism which leads to excessive accumulation of heme, eventually leading to acute attacks and death.

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17
Q

Categorize the BZ by their elimination half-life.

A

Short: Midazolam
Intermediate: Lorazepam
Long: diazepam

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18
Q

T 1/2 of Midazolam?

A

<6 hours

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19
Q

T 1/2 of Lorazepam?

A

6-24 hours

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20
Q

T 1/2 of Diazepam?

A

24-37 hours

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21
Q

BZ MOA

A

BZ bind to GABBA-A receptors and modulates their activity (enhances affinity). GABA is required as BZ are unable to open chloride channels without them.

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22
Q

The imidazole ring found in BZ requires what state to increase lipid solubility, and under what circumstances does this occur?

A

Closed state, and occurs at physiological pH.

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23
Q

Which BZ are preferred for increased age and liver disease, and why?

A

Lorazepam, oxazepam, temazepam.
These are metabolized by glucuronidation, which is not effected by age or liver disease.

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24
Q

A symptom of BZ withdrawal in the elderly presents as what?

A

Confusion

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25
Long-term use of BZ leads to two significant things in the patient population.
Tolerance & cognitive decline
26
BZ produce more _____ than sedation.
amnesia
27
PO administration of which drug has a high first-pass hepatic extraction.
Midazolam
28
Drugs that inhibit CYP450 enzymes and prolong metabolism include (5).
Fentanyl Erythromycin CCB Antifungals Cimetidine
29
CNS effects include anterograde amnesia.
Midazolam
30
Respiratory effects of Midazolam
decreased TV increased RR
31
May increase cardiac output in CHF patients.
Midazolam
32
Modest CV effects include decreased ABP and increased HR.
Midazolam
33
Most common preoperative sedative in adults and children.
Midazolam
34
Used prophylactically to raise seizure threshold when performing regional blocks
BZ
35
Avoid this bz medication in pregnant patients
Midazolam
36
Po administration results in 100% bioavailability.
Diazepam
37
Mixing with NS or water for dilution results in cloudiness.
Diazepam
38
This medication crosses the placenta, resulting in fetal concentrations equal to or greater than the mother
Diazepam
39
Which active metabolite of a BZ contributes to sustained drug effects and return of drowsiness 6-8 hours after administration?
Desmethyldiazepam
40
Which drug can decrease LVED pressure with small doses?
Diazepam
41
Minimal CV effects with this drug. They equate to natural sleep.
Diazepam
42
Used to produce skeletal muscle relaxation in lumbar disc disease.
Diazepam
43
This BZ is the most potent sedative and amnesic.
Lorazepam
44
BZ with a slower onset due to lower lipid solubility.
Lorazepam
45
This is the only BZ that has no active metabolites.
Lorazepam
46
Contraindicated in patients on antiepileptic drugs.
Flumazenil
47
Propofol induction dose
1.5-2.5mg/kg
48
Propofol onset of action
30 seconds
49
This drug promotes bacterial growth
Propofol
50
This drug contains metabisulfate, known to exacerbate asthma and trigger sulfate allergies.
Generic propofol
51
This drug is a low lipid emulsion that is preservative-free, however, there remains significant pain with injection
Ampofol
52
This drug produces formaldehyde byproducts leading to perineum burning.
Fospropofol
53
A propofol syringe needs discarding after how many hours?
6
54
The mixing of what two drugs lead to fat emboli
Propofol + Lidocaine
55
Propofol pKa
11
56
Propofol EHL
0.5-1.5 hours
57
Propofol Vd
1000-4000 L
58
How is the induction dose of propofol adjusted for elderly patients, and why?
Decrease the dose by 25-50%. Elderly patients have experience increased drug effects and decreased clearance of the drug.
59
Off-Label uses for Propofol
Antiemetic Antipruritic Anticonvulsant diminish bronchoconstriction
60
Which drug contains a preservative resulting in allergies and bronchoconstriction.
Propofol (Diprivan)
61
Propofol: MAC v. GA dosages
MAC: 25-100mcg/kg/min GA: 100-300mcg/kg/min
62
Hypnosis with Propfol lasts how long?
5-10 minutes
63
Propofol respiratory effects
decreased TV, RR, and response to hypoxia
64
How does a propofol dose of 2-2.5mcg/kg impact CV.
40% drop in BP, CO, SVR, and reduced myocardial consumption.
65
Propofol CV effects
decreased BP, HR unchanged, blunted baroreceptor reflex
66
What is propofol infusion syndrome?
high doses of propofol + steroids = multi-organ failure, AKI (rhabdo)
67
Etomidate pKa
4.24
68
Etomidate induction dose
0.2-0.4mg/kg
69
Etomidate has two isomeric forms. Which isomer has hypnotic/sedative properties?
S (+)
70
Etomidate metabolism
Liver enzymes & plasma esterases
71
Flumazenil has no effect on this non-barb drug.
Etomidate
72
Etomidate EHL
2-5 hours
73
Etomidate: special CNS considerations
It causes myoclonus and may activate seizures.
74
Drug known for its hemodynamic stability
Etomidate
75
Etomidate respiratory effects
decreased TV, increased RR, decreased response to CO2, hiccoughs, emergence excitement
76
High incidence of PONV
Etomidate
77
Good drug to use for patients with reactive airway disease.
Etomidate
78
First choice drug category for alcohol detox.
BZ
79
Ketamine induction dose
1-2mg/kg
80
Only agent producing dissociate anesthesia
Ketamine
81
Drug contains potent analgesic properties
Ketamine
82
Ketamine pKa
7.5
83
This drug is not extensively protein-bound, unlike other induction agents.
Ketamine
84
Commercial preparations given as a racemic mixture
Ketamine
85
Ketamine EHL
2-3 hours
86
What are the effects of norketamine?
1/3-1/5 potency, which leads to prolonged drug effects
87
Ketamine MOA
NMDA antagonist minor GABA action
88
Suppresses inflammatory mediators which improve blood flow
Ketamine
89
Ketamine CNS effects
increase CBF, CMRO2, ICP antidepressant, potentiates NDNMB, emergence delirium, nystagmus
90
Emergence delirium with Ketamine is more prevelent in what patient population?
Women 15 years of age and older with a history of personality disorder or dreaming, and with doses of 2mg/kg or more.
91
What can attenuate emergence delirium seen with Ketamine?
Midazolam
92
Ketamine respiratory effects
Bronchodilation increased secretions
93
Ketamine CV effects
increased BP, HR, CO release of NE, and inhibits uptake increased PVR and RV workload
94
It acts as a direct myocardial depressant and is not recommended for patients with CAD.
Ketamine
95
Ketamine LOC
30-60 seconds
96
Ketamine return of consciousness time v. return of awareness
consciousness 10-20minutes awareness 60-90 minutes
97
Ketamine chemical compound is a derivative of?
PCP
98
Chronic Ketamine use causes what metabolic phenomenon to occur?
Enzyme induction which quickens the metabolism of ketamine leading to drug tolerance
99
Dexmedetomidine MOA
Alpha 2 adrenergic agonist
100
Decreased SNS activity seen with dexmedetomidine is caused by?
Decrease in NE levels
101
Dexmedetomidine EHL
2-3 hours
102
Dexmedetomidine dosing
Loading: 1mcg/kg (10min) maintenance: 0.2-1mcg/kg/hr
103
Dexmedetomidine adverse effects
hypotension hypertension (loading phase) Nausea Bradycardia Anemia Hypothermia
104
Exercise extreme cause in using this drug with patients diagnosed with severe heart block and/or severe ventricular dysfunction.
Dexmedetomidine
105
Dexmedetomidine: CSHF of a 4 min infusion v. a 250 min infusion
4 min = 10 min 250 min = 8 hours