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Neuro System > Sedative-Hypnotics, General Anesthetics > Flashcards

Sedative-Hypnotics, General Anesthetics Flashcards

1
Q

Sedative-hyponotics are used for what 2 purposes?

A
  1. Sedation - anxiolytic effect
  2. Hyponisis - anti-insomnia effect
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2
Q

Absorption of benzodiazapines correlates with ___

A

Lipophilicity

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3
Q

Lipid solubility with BDZs affects CNS entry. ___ has the highest lipid solubility (thus fastest CNS entry). All BDZ cross breast milk and placenta.

A

Diazepam

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4
Q

Metabolism for benzodiazapines is important, as most have ___

A

Active metabolites

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5
Q

Benzodiazapines with NO active metabolites (4)

A
  1. Oxazepam
  2. Temazepam
  3. Lorazepam
  4. Clonazepam

(out the liver cleared)

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6
Q

Mechanism of benzodiazapines, barbiturates, and EtOH

A

Bind to allosteric site on the GABAa receptor-Cl ion channel complex → increase action of GABA

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7
Q

Withdrawl of benzodiazapines and barbiturates may lead to ___

A

REM rebound (bizzare dreams)

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8
Q

___ and ___ are BDZs used in IV sedation and anesthetic adjucants, but not BDZ capable to stage III surgical anesthesia alone.

A

Midazolam

Diazepam

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9
Q

BDZ:

Medium duration of action

Indicated for anxiety and panic disorder

Prone to drug dependence

A

Alprazolam

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10
Q

BDZ:

Long-acting BDZ

Used for anxiety, alcohol detox, seizures, and muscle spasms

IV formualtion

A

Diazepam

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11
Q

BDZ:

Medium duration of action

No active metabolite (good for elderly)

Used for anxiety and seizures

A

Lorazepam

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12
Q

BDZ competitive antagonist, used in BDZ OD and given IV (barbiturates do not have antagonist and are therefore more dangerous)

A

Flumazenil

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13
Q

All barbuturates are absorbed rapidly and are highly ___

A

Lipid soluble

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14
Q

Metabolites of all BARBs are ___

All BARBs self-induce ___ (especially phenobarbital)

A

Inactive

Hepatic drug metabolizing systems

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15
Q

What is the major difference between the mechanism of BDZs and BARBs?

A

BARBs work in absense of GABA (thus have no ceiling effect like BDZs)

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16
Q

Pentobarbital and other BARBs can produce ___, however used mainly as adjunct parenteral agents.

A

Stage III anesthesia

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17
Q

Due to a lack of ceiling effect, toxic doses of BARBs may lead to ___

A

Respiratory/circulatory collapse

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18
Q

BARB:

Used to treat insomnia, largely replaced by BDZ and Z-drugs (e.g., zolpidem)

A

Pentobarbital

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19
Q

BARB:

Used to treat seizure disorders, largely replaced by newer agents

A

Phenobarbital

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20
Q

Mechanism of antihistamines (sedative-hypnotics)

A

Antagonists at histamine H1 receptors in brain → reduce ACh neurotransmission in RAS

Block direct histamine-mediated arousal in cortical neurons

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21
Q

Antihistamine (sedative-hypnotic)

First-generation - used as sedative-hypnotics

Often found as OTC sleep-aid drugs and in combo with other agents

A

Diphenhydramine

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22
Q

Antihistamine (sedative-hypnotic)

Prescription ONLY

Used as anxiolytic and pre-op sedative

A

Hydroxyzine

23
Q

Mechanism of zolpidem (anti-insomnia agent)

A

Like BDZ, but more selective at GABAa receptors with alpha-1 subunit only

24
Q

1 sleep med in the world

Anti-insomnia agent

Rapid onset with short elimination half-life

Less morning hangover effect

Less impact on sleep cycles

Little tolerance to hypnotic effects and no withdrawl effects

25
Mechanism of ramelteon (anti-insomnia agent)
Melatonin receptor agonist (mimics natural surge of the pineal hormone **melatonin at night**)
26
Anti-insomnia agent No apparent abuse properties Indicated for sleep-onset insomnia only Approved for long-term used No evidence of rebound insomnia with cessation Only non-scheduled prescription drug available for treatment of insomnia
Ramelteon
27
Non-sedating anxiolytic agent Not chemically related to BDZ or BARBs **No anticonvulsant or muscle relaxant effects** High affinity for 5-HT1a receptors Indicated for management of anziety disorders or the **short-term** relief of anxiety symptoms
Buspirone
28
Non-sedating anxiolytic agent Not chemically related to BDZ or BARBs (non-selective beta-blocker) No anticonvulsant or muscle relaxant effects Off-label use for acute situational or **performance anxiety**
Propranolol
29
BDZ, Z-drugs, melatonin agonists, but NOT ___ used today for insomnia
BARBs
30
BDZ toxic effects
1. Drowsiness 2. Impaired judgement 3. Decreased motor skills 4. Anterograde amnesia
31
Side effect of longer-acting BARB and BDZ agents
Hangover effect
32
Caution with elderly taking sedative-hypnotics due to decreased \_\_\_
Metabolic ability
33
Initial analgesia due to loss of spinal pain neurons; later in this stage also get amnesia
Stage I: Analgesis
34
Stage of excitement of delirium often with struggling due to inhibition of smaller CNS inhibitory neurons; definitely amnesic; respiration is irregular; vomiting, retching or incontinence may occur; stage ends when regular respiration resumes
Stage II: Excitement
35
Progressive loss of reticular activating system, general inhibition of neurons; stage ends when spontaneous respiration ceases
Stage III: Surgical anesthesia
36
Spontaneous respiration creases; severe depression of respiratory center in medulla; severe depression of vasomotor center in medulla; IMMINENT DEATH without life support
Stage IV: Medullary depression
37
Amount of IA in brain depends on (3):
1. Partial pressure 2. Ventilation rate 3. Solubility (blood:gas partition coefficient)
38
Mechanism of nitrous oxide (GA - inhalation)
Blocks glutamate (excitatory) ion channel receptors
39
Mechanism of halogenated GA inhalation agents (not nitrous oxide)
Multiple sites of action * **Enhance GABA** * Increase K+ channel efflux * Reduce Na and Ca influx
40
A way to compare potency among inhalation agents (GA) Defined: The minimal alveolar concentration which produces immobility to surgical incision in 50% of patients. Lower value = more potent
Minimum alceolar concentration (MAC)
41
Stage III anesthesia involves (3);
1. Suppresion of RAS 2. Inhibition of spinal reflexes 3. Loss of consciousness
42
Uncontrolled hypermetabolix reaction that occurs in skepetal muscle May occur with any GA inhalation except nitrous oxide Appears to be a genetic defect in the Ca uptake in the SR
Malignant hyperthermia
43
Drug that reverses malignant hyperthermia Prevents Ca release from SR; blocks hypermetabolic reactions and contractions
Dantrolene
44
GA - inhalation Prototypical halogenated IA Most potent Rate of induction and recovery slow Sensitizes the heart to catecholamines so greatest risk for **cardiac arrhythmias** Fatal **hepatitis**
Halothane
45
Most ideal IA, rapid and smooth induction, little CV or respiratory effects, no toxicity
Secoflurane
46
Mechanism of Midazolam (BDZ, but used as PA)
BDZ - so GABA enhancement at GABAa receptor-chloride ion channels
47
Mechanism for ketamine (PA)
Blocks glutamate receptors
48
Mechanism of propofol (PA)
Enhances/act like GABA
49
Mechanism of fentanyl (PA)
Potent mu opioid receptor agonsit (opioid analgesic)
50
PA: Short acting, used for **preop sedation, endoscopy** Blackbox warning of respiratory depression mostly when used with other CNS depressants
Midazolam
51
PA: Like PCP, used for induction of anesthesia, increases BP **Delirium and hallucination** on recovery Best in **KIDS**
Ketamine
52
PA: **Short duration of action** Used for induction, rapidly metabolized and eliminated
Propofol
53
PA: Used for cardiac surgery, epidural anesthesia (often with midazolam for IV sedation)
Fentanyl
54

Neuro System (4 decks)

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