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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

A

Zolpidem

25
Q

Mechanism of ramelteon (anti-insomnia agent)

A

Melatonin receptor agonist (mimics natural surge of the pineal hormone melatonin at night)

26
Q

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

A

Ramelteon

27
Q

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

A

Buspirone

28
Q

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

A

Propranolol

29
Q

BDZ, Z-drugs, melatonin agonists, but NOT ___ used today for insomnia

A

BARBs

30
Q

BDZ toxic effects

A
  1. Drowsiness
  2. Impaired judgement
  3. Decreased motor skills
  4. Anterograde amnesia
31
Q

Side effect of longer-acting BARB and BDZ agents

A

Hangover effect

32
Q

Caution with elderly taking sedative-hypnotics due to decreased ___

A

Metabolic ability

33
Q

Initial analgesia due to loss of spinal pain neurons; later in this stage also get amnesia

A

Stage I: Analgesis

34
Q

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

A

Stage II: Excitement

35
Q

Progressive loss of reticular activating system, general inhibition of neurons; stage ends when spontaneous respiration ceases

A

Stage III: Surgical anesthesia

36
Q

Spontaneous respiration creases; severe depression of respiratory center in medulla; severe depression of vasomotor center in medulla; IMMINENT DEATH without life support

A

Stage IV: Medullary depression

37
Q

Amount of IA in brain depends on (3):

A
  1. Partial pressure
  2. Ventilation rate
  3. Solubility (blood:gas partition coefficient)
38
Q

Mechanism of nitrous oxide (GA - inhalation)

A

Blocks glutamate (excitatory) ion channel receptors

39
Q

Mechanism of halogenated GA inhalation agents (not nitrous oxide)

A

Multiple sites of action

  • Enhance GABA
  • Increase K+ channel efflux
  • Reduce Na and Ca influx
40
Q

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

A

Minimum alceolar concentration (MAC)

41
Q

Stage III anesthesia involves (3);

A
  1. Suppresion of RAS
  2. Inhibition of spinal reflexes
  3. Loss of consciousness
42
Q

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

A

Malignant hyperthermia

43
Q

Drug that reverses malignant hyperthermia

Prevents Ca release from SR; blocks hypermetabolic reactions and contractions

A

Dantrolene

44
Q

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

A

Halothane

45
Q

Most ideal IA, rapid and smooth induction, little CV or respiratory effects, no toxicity

A

Secoflurane

46
Q

Mechanism of Midazolam (BDZ, but used as PA)

A

BDZ - so GABA enhancement at GABAa receptor-chloride ion channels

47
Q

Mechanism for ketamine (PA)

A

Blocks glutamate receptors

48
Q

Mechanism of propofol (PA)

A

Enhances/act like GABA

49
Q

Mechanism of fentanyl (PA)

A

Potent mu opioid receptor agonsit (opioid analgesic)

50
Q

PA:

Short acting, used for preop sedation, endoscopy

Blackbox warning of respiratory depression mostly when used with other CNS depressants

A

Midazolam

51
Q

PA:

Like PCP, used for induction of anesthesia, increases BP

Delirium and hallucination on recovery

Best in KIDS

A

Ketamine

52
Q

PA:

Short duration of action

Used for induction, rapidly metabolized and eliminated

A

Propofol

53
Q

PA:

Used for cardiac surgery, epidural anesthesia (often with midazolam for IV sedation)

A

Fentanyl

54
Q
A

Neuro System (4 decks)

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