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Brain and Behavior Part 2 > IV Anesthetics: Sedatives and Hypnotics > Flashcards

IV Anesthetics: Sedatives and Hypnotics Flashcards

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1
Q

Review: What are the 5 A’s of surgical anesthesia?

A 
Amnesia
Anesthesia
Analgesia
Akinesia (not moving)
Areflexia (lack of autonomic reflexes)
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2
Q

7 uses of sedatives and hypnotics other than general anesthesia for surgery? (probs not necessary to memorize)

A 
ICU sedation
Procedural sedation
Seizure treatment
Generalized anxiety disorder, panic disorder
EtOH withdrawal
Insomnia
Muscle spasms
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3
Q

5-6 neurotransmitters that sedatives and hypnotics work on?

A 
GABA/galanin
Histamine
Serotonin
Norepinephrine
Acetylcholine
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4
Q

What are the 2 major principles to think about in the pharmacokinetics of IV anesthetics?

A

Drug redistribution

Context-sensitive half time

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5
Q

Review: What makes up the well-vascularized central compartment (in pharmacokinetics)?

A

Brain, Heart, Kidney

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6
Q

What’s the difference between distribution and elimination half life? Which one matters more?

A

Distribution half life: Time it takes drug in central compartment to be reduced by 50%, due to distributing into other compartments, esp. muscle and fat.
Elimination half life: Time it takes total drug in body to be reduced by 50%.
Distribution half life is what actually matters, as that represents the drug being where it does its job.

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7
Q

What is context-sensitive half time? Why does it happen?

A

The longer you infuse a drug, the longer it takes to eliminate once to stop infusing it.
This happens because the drug accumulates in fat over time, which will be released when the infusion is stopped.

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8
Q

What do you do different with sedatives / hypnotics that have a context-sensitive half life that increases sharply with infusion duration?

A

Usually don’t give them IV. Better suited for PO, suppository, IM etc.

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9
Q

What’s the preferred drug of anesthesia induction?

A

Propofol

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10
Q

What’s the redistribution half life of propofol? (roughly)

A

2-8 minutes. Really short. Even though the elimination half life is 4 - 24 hours, the drug effect goes away very quickly.

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11
Q

Special fact about propofol metabolism?

A

It’s partially metabolized extrahepatic-ly, including in the lungs.

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12
Q

Is the central compartment for pharmacokinetics lareger in children vs. adults? How about older adults vs. young adults?

A

Largest in children. “Kids are all head.”

Smallest in older adults.

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13
Q

MoA of propofol? (roughly)

A

Potentiates GABA-A receptor. (Also affects alpha 2 adrenal receptors, NMDA glutamate receptors, and glycine receptors)

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14
Q

Does propofol cause analgesia?

A

No. It has no effect on pain, only consciousness. You need to give something else for that.

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15
Q

What’s the effect of propofol on blood pressure? How? (3 things) On heart rate?

A 
Decreased blood pressure via..
- vasodilation
- decreased sympathetic tone
- myocardial depression (maybe)
Heart rate is decreased.
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16
Q

3 respiratory effects of propofol?

A

Decrease tidal volume +/- increased RR. (hypopnea or apnea).
Decreased response to high CO2 / low O2.
Bronchodilation.
(note similarities to respiratory effects of inhaled anesthetics)

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17
Q

2 neurological effects of propofol?

A

Decreased metabolic rate -> “burst suppression”

Decreased cerebral blood flow -> “brain relaxation” (the brain actually shrinks, useful in neurosurgery)

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18
Q

Adverse effects of propofol? Name 4.

A

Pain on injection.
Propofol-related infusion syndrome (PRIS) = metabolic acidosis with long-term use.
Hypertriglyceridemia and pancreatitis (propofol is suspended in fat).
Decreased PMN chemotaxis.

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19
Q

2 absolute contraindications to propofol?

A

Allergy to propofol.

Allergy to egg protein.

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20
Q

Relative contraindications for propofol? (2 main ones)

A

Hemodynamic instability (due to cardiovascular effects).
Hx of awareness under anesthesia.
(and, Dr. Lane-Fall notes, using it on your own at home)

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21
Q

What killed Michael Jackson?

A

Taking too much propofol at home.

22
Q

5 reasons why people abuse propofol?

A 
Rapid onset/offset
Potent hypnotic
Increases dopamine in nucleus accumbens -> euphoria, feeling of well-being
Sexual dreams
Not scheduled by DEA
(Don't do it.)
23
Q

What’s the main reason why people opt for etomidate?

A

Patient has hemodynamic instability / undergoing cardiac surgery.

24
Q

How is etomidate different from propofol in its effects? (name 4-5)

A 
Causes adenocortical suppression.
Minimal to moderate cardiovascular effects.
Minimal to moderate respiratory effects.
Can cause seizures.
Worse nausea/vomiting than propofol.
25
Q

What are the 2 major adverse effects of etomidate?

A

Nausaea/vomiting (moreso than propofol).

Adrenal suppression.

26
Q

1 absolute and 3 relative contraindications for etomidate?

A

Absolute: Allergy to etomidate.
Relative:
-adrenal insufficiency
-critical illness, especially septic shock
-history of post-operative nausea/vomiting

27
Q

What anesthetic is also used for lethal injection?

A

Thiopental.

28
Q

What class of drug is thiopental a member of? (or, at least, is friends with?) What’s their common MoA?

A

Barbituates. Potentiate GABA receptors by stabilizing the open conformation of the Cl- channel.

29
Q

What’s worth of note about the metabolism of thiopental? (2 things)

A

It induces it the enzymes that biotransform it, thus may need to give higher doses after giving for a long duration.
Exhibits zero-order kinetics “at supratherapeutic doses” -> linear elimination.

30
Q

To people with which rare condition must you never give thiopental?

A

People with acute intermitted porphyria. (we didn’t even cover this in MDTI)

31
Q

Physiological effects of thiopental (and a similar drug, methohexital)?

A

Very similar to propofol.

Except- methohexital is more predisposing to seizures.

32
Q

4 adverse effects of thiopental?

A

Garlic/onion taste. (must be a similar enough sulfur-containing molecule)
Tissue irritation, possibly necrosis.
Stimulation of porphyrin formation.
Anti-analgesic effect.

33
Q

Absolute contraindications to thiopental? (name 2)

A

Allergy to thiopental.

Acute intermittent porphyria.

34
Q

Relative contraindications for thiopental? (name 2)

A

Hemodynamic instability. (like propofol)

Questionable IV access (i.e. you don’t want this irritating stuff getting into tissues)

35
Q

Which street drug is ketamine most like? Which receptor do they act on?

A

Most like PCP. Both antagonist NMDA receptor.

36
Q

How is the distribution half life of ketamine compare to the other sedatives / hypnotics discussed?

A

At 11 - 16 minutes, it’s slightly longer (but still not that long).

37
Q

What’s special about the metabolism of ketamine?

A

One of its metabolites, norketamine, has desirable analgesic effects.

38
Q

MoA of ketamine? (more than one thing)

A 
Primarily: NMDA antagonist.
But it's dirty also has affects on...
GABA (+)
Nicotinic AChR (-)
5HT-3 (+) <- a serotonin receptor
Opiate receptors (+)
39
Q

Does ketamine decrease sympathetic tone?

A

No. It increases it - can actually cause hypertension and tachycardia.

40
Q

Does ketamine suppress respiration?

A

No. Which makes it nice for additional pain relief without using opioids.

41
Q

What are 4 undesirable affects of ketamine?

A

Dysphoria.
++ salivation and lacrimation. (makes intubation a pain)
Sympathetic simulation -> increased myocardial work.
Increased ICP. (bad for neurosurgery)

42
Q

Absolute contraindication for ketamine?

A

Ketamine allergy. (if there’s only one, it must be that)

43
Q

Relative contraindications for ketamine? *(name 4)

A

Psychosis
Extremely compromised myocardial function
Inability to tolerate tachycardia, hypertension.
Intracranial hypertension.

44
Q

What drugs can mitigate the dissociative effects of ketamine?

A

Benzodiazepines.

45
Q

What drug reverses the effects of benzodiazepines?

A

Flumazenil

46
Q

What drug reverses the effects of opiods?

A

naloxone / naltrexone

47
Q

How are alpha-2 adrenoreceptor antagonists (dexmedetomidine and clonidine) useful?

A

Inducing actual sleep / sedation during which the patient can respond / be aroused. Useful for awake craniotomy.

48
Q

What effect do dopamine antagonists (droperidol and haloperidol) have? (very simply)

A

Induce catatonia - people don’t move. But they are conscious and remember.

49
Q

What’s the sedative in Tylenol PM?

A

diphenhydramine aka Benadryl. (due to its antihistamine activity?)

50
Q

What hypnotic / sedative is great if you don’t want / get get IV access?

A

Ketamine.

Brain and Behavior Part 2 (58 decks)

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