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CNS Depressants > CNS Depressants > Flashcards

CNS Depressants Flashcards

1
Q

GABA A Receptor Complex

A

Cl channel within the CNS that is opened by GABA.

  • there are five accesory receptors that can be activated with drugs (benzo, barb, ETOH) to speed the influx of Cl
  • as it becomes more negative (hyperpolarized) it becomes harder to depolarize and conduct the AP
  • Each CNS depressant activates different combinations of these accessory sites to produce different profiles of CNS depression by making it easier for GABA to bind
  • All CNS depressants are POSITIVE ALLOSTERIC MODULATORS of the GABA A receptor
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2
Q

Dose Dependency in CNS Depressants

A
  • Every CNS depressant can cause the full range of CNS depression (anxiolysis to death) depending on how the accessory sites affect hyperpolarization and dose
  • order of CNS depression is anxiolysis, euphoria, sedation, muscle relaxation, anticonvulsant, coma, and death
  • It is very costly to get drugs approved for different indications, so keep in mind that any CNS depressant can achieve any effect of CNS depression.
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3
Q

Barbiturates (general aspects)

A
  • are classified by rate and duration of action

- At higher doses Barbs can open the channel spontaneously, which gives them a narrow therapeutic window

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4
Q

Pharmacokinetics of Barbiturates

A
  • Rate of distribution depends on lipid solubility
  • metabolized more slowly with hepatic impairment (risk of OD)
  • tolerance, physical dependence, psychological dependence
  • additive effect with other CNS depressants
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5
Q

Ultrashort Acting Barbiturates

A

sodium thiopental, thiamylal, methylhexital

  • these are primarily used for induction of anesthesia
  • very lipid soluble so they enter and leave the brain quickly (very fast onset)
  • HL range from 4-12 hours (although therapeutic effect is long gone, drug remains in body)
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6
Q

Short to Intermediate Acting Barbiturates

A

-these are rarely used today
secobarbital- first sedative/hypnotic
pentobarbital- first anxiolytic

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7
Q

Long Acting Barbiturates

A

phenobarbital- anticonvulsant with 80-120 hour HL

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8
Q

Side Effects of Barbiturates

A

CNS and respiratory depression (more pronounced than Benzo), tolerance, dependence, abuse

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9
Q

Withdrawal from CNS depressants

A
  • withdrawal symptoms are the opposite of therapeutic effect (CNS hyperstimulation)
  • withdrawal is a life threatening occurrence (can seize to death)
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10
Q

Benzodiazepines (general aspects)

A
  • unlike Barbs, these cannot open the Cl channel alone
  • have a wider therapeutic window and better SE profile than Barb
  • more likely to pass out before apnea occurs
  • have a reversal agent
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11
Q

Flumazenil

A

aka romazicon

  • reversal agent for benzos
  • outcompetes other benzos at the site but has no effect
  • 1 hour HL (many benzos have much longer HL, so may need repeated doses of flumazenil
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12
Q

Pharmacokinetics of Benzodiazepines

A
  • MOA is similar to that of barbs
  • benzos are metabolized to less effective, but still potent, metabolites
  • therefore, drugs that need to be repeatedly metabolized have longer HLs
  • temazepam, oxazepam, and lorazepam only need a phase II reaction to become inactive so they are most gentle on liver
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13
Q

Short Acting Benzodiazepine

A

midazolam and triazolam

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14
Q

midazolam

A
  • short acting benzodiazepine
  • used for conscious sedation and same-day surgery
  • comes in a sucker (children)
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15
Q

triazolam

A
  • short acting benzodiazepine

- approved as sedative/hypnotic but is often used for conscious sedation

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16
Q

Intermediate acting Benzodiazepine

A

lorazepam, oxazepam, temazepam, alprazolam, chlordiazepoxide

17
Q

lorazepam

A
  • intermediate acting benzodiazepine
  • used for a wide variety of anxiety issues
  • most water soluble which makes it easy for IV or IM injection
  • first choice for status epilepticus
  • part of the B52
18
Q

oxazepam

A
  • intermediate acting benzodiazepine

- used for short term or situational anxiety that is debilitating (afraid of flying but must take a flight)

19
Q

temazepam

A
  • intermediate acting benzodiazepine

- sedative hypnotic for sleep maintenance disorder

20
Q

alprazolam

A
  • intermediate acting benzodiazepine
  • used for anxiety, depression, and panic disorder
  • is very widely prescribed and many practitioners become concerned with dependency
  • it is key to give clear administration instructions rather than “prn anxiety”
21
Q

chlordiazepoxide

A
  • intermediate acting benzodiazepine
  • the oldest benzo (that’s why it doesn’t end in pam or lam)
  • used for anxiety but rarely seen
22
Q

Long acting benzodiazepine

A

diazepam and clonazepam

23
Q

diazepam

A
  • long acting benzodiazepine
  • manages anxiety with a long HL
  • also commonly used in status epilepticus, but is more viscous than lorazepam
24
Q

clonazepam

A
  • long acting benzodiazepine
  • manages anxiety with a long HL
  • can be used for aggressive behavior/sundowning
25
Q

Uses of Benzodiazepine

A
  • used for the widest range of CNS effects because they are much safer than barbs
  • anxiety, sedation, muscle relaxant, anticonvulsant, and anesthesia induction agent
26
Q

Adverse Effects of Benzodiazepines

A
  • CNS depression, anterograde amnesia, respiratory depression (less pronounced than barbs), tolerance, dependence, abuse
  • Have additive effects with other CNS depressants
27
Q

anxiety disorder

A

generalized anxiety disorder- constantly increased anxiety, muscle tension, and autonomic hyperactivity
panic disorder- recurrent and discrete periods of of intense anxiety, fear, and discomfort with autonomic arousal

28
Q

Treatment of Anxiety Disorder

A
  • depends on type and severity of anxiety
  • alprazolam is only one approved for panic disorder
  • benzos are used for immediate anxiolysis and to reduce the sympathetic response
  • for generalized, buspirone is a good first choice (no dependence, long effect) SE include HA, nausea, dizziness
  • for panic, an SSRI or tricyclic is a good first choice
  • beta blocker can be used for performance anxiety
29
Q

Treatment of Insomnia

A

benzos, non-benzos, antidepressants, antihistamines, melatonin, and meprobamate/carisoprodol
-chloral hydrate SHOULD NOT BE USED

30
Q

benzos used for insomnia

A

triazolam and temazepam

31
Q

non-benzodiazepines used for insomnia

A
  • these work at the benzo binding site but have different structure
  • zolpidem, zaleplon, eszopiclone
32
Q

antidepressants used for insomnia

A

trazadone and doxepin

33
Q

antihistamines used for insomnia

A

hydroxyzine and diphenhydramine

-OTC meds with PM

34
Q

melatonin for insomnia

A

-binds to MT receptor and has long onset

35
Q

meprobamate and carisoprodol for insomnia

A

meprobamate- originally an anxiolytic that became sedative-hypnotic
carisoprodol- skeletal muscle relaxant that is metabolized to meprobamate. Has abuse potential.

36
Q

causes of insomnia

A

stress, illness, drugs, ETOH, jet lag

37
Q

Monitored anesthesia care and its fundamental elements

A
  • combination of local anesthesia, sedation, and analgesia

- fundamental elements include safe sedation, control of anxiety, and pain control

38
Q

Conscious Sedation

A
  • depress the LOC without compromising airway or ability to respond to stimuli
  • good conscious sedation should be safe, cheap, readily absorbed, fast acting, wear off quickly, be reversible, not irritate GI, and be rapidly excreted

CNS Depressants (1 decks)

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