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BPS > Kruse DSA: Sedative Hypnotics > Flashcards

Kruse DSA: Sedative Hypnotics Flashcards

1
Q

What are the benzos that DONT end is pam or lam?

A
  • Chlordiazepoxide

- Clorazepate

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2
Q

Benzo antagonist

A

-Flumazenil

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3
Q

Barbiturates

A
  • end in “bital”

- except for Thiopental

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4
Q

What are the newer sedative-hypnotic drugs?

A
  • Buspirone
  • Exzopiclone
  • Meprobamate
  • Ramelteon
  • Zaleplon
  • Zolpidem
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5
Q

What is a sedative?

A
  • a drug that decrases CNS activity, moderates excitement, and calms the recipient
  • Anxiolytic because it reduces anxiety
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6
Q

What is a hypnotic?

A
  • a drug that produces drowiness and facilitates the onset and maintenance ofa state of sleep
  • recipient can be aroused easily from it
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7
Q

MOA of benzodiazepenes?

A

-promote the binding of major inhibitory NT GABA to the GABAa receptor and enhance the GABA induced ion currents

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8
Q

Do benzos have a low capacity to produce fatal CNS depression?

A
  • yes

- so they are preferred over barbiturates

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9
Q

Barbiturates MOA:

A

-Bind to GABAa receptors and potentiate GABA induced chloride currents
=Can activate the cahnnel directly by acting as a GABA mimetic at high concentrations
=narrow therapeutic index and it is often not possible to achieve a desired effect without evidence of general depression of the CNS

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10
Q

What is absorption rate dependent on?

A

-the lipid solubility

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11
Q

What enzyme does the phase 1 rxn for benzos?

A
  • CYP3A4

- then glucuronidation (phase 2)

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12
Q

Which benzos would be good to use in someone who has hepatic insufficiency?

A

-oxazepam and lorazepam

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13
Q

What is the result of GABAa receptor activation?

A
  • increased Cl- influx

- reduced number of AP’s

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14
Q

What do benzodiazepines do to the GABA concentration-response curve?

A
  • shift it to the left
  • less GABA required to activate the receptor
  • benzos just enhace the effect of GABA allosterically
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15
Q

Barbiturates MOA

A
  • increase the duration of GABA-gated chloride channel openings
  • less selective
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16
Q

Which drugs are agonists only when the alpha 1 subunit of the GABA receptor is included?

A

-Eszopiclone, zaleplon, and zopidem

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17
Q

the GABA antagonist

A

-flumazenil

18
Q

inverse agonists

A
  • negative allosteric modulators of GABA receptor

- ex: B-carboline class of compounds

19
Q

Which drug will increase total sleep time?

A

-eszopiclone

20
Q

what is the usual cause of death due to overdose of sedative hypnotics?

A

-depression of the medullary respiratory center

21
Q

what is tolerance?

A

-decrease in responsiveness to a drug following repeated exposure and a common feature of sedative hypnotic use

22
Q

what is dependence?

A

-the compulsive use of a substance despite significant problems resulting from such use

23
Q

What doe Flumazenil do?

A

-binds to benzo binding sit eon GABAa receptors and acts as a competitive antagonist

24
Q

what drugs does flumazenil block the action of?

A

-benzos, zolpidem, zaleplon, and eszopiclone

=does not block CNS effects of other sedative hypnotics, ethanol, opioids, or general anesthetics

25
Q

adverse effects of flumazenil?

A

-agitation, confusion, dizziness, nausea

26
Q

What are benzos widely used for

A

-the management of acute anxiety states (situational anxiety)

27
Q

Benzodiazepine advantages in treating anxiety-

A
  • high therapeutic index
  • availability of flumazenil for overdose
  • low risk of drug interactions based on liver enzyme induction
  • minimal effects on cardiovascular or autonomic functions
28
Q

which benzo is approved for tx of muscle spasticity?

A

-diazepam

29
Q

What are the direct toxic actions of the sedative hypnotics?

A
  • result from dose-related depression of the CNS
  • Low doses may lead to drowsiness, impaired judgement, and diminished skills that can lead to impacts on driving ability job performance, and personal relationships
30
Q

Which pts have more common increased sensitivity to sedative hypnotics?

A

-pts with CV disease, resp disease, or hepatic impairment

31
Q

What condition makes barbiturates contraindicated?

A

-pts with hx of acute intermittent porphyria or other kinds of porphyria

32
Q

what do we have to watch out for with drug interactions and sedative hypnotics?

A

-CYP 450 inhibitors

33
Q

What is Ramelteon approved for?

A

-tx of insomnia characterized by difficulty with sleep onset

34
Q

MOA for Ramelteon?

A

-agonist at MT1 and MT2 melatonin receptors located in the suprachiasmatic nuclei of the brian

35
Q

What pts do we have to be careful with when using ramelteon?

A

-pts with hepatic impairment

36
Q

What is the parent drug of Ramelteon metabolized by?

A

-CYP1A2

37
Q

What do we have do not coadminister with Ramelteon?

A
  • Fluvxamine (SSRI)

- inhibitor of CYP1A2

38
Q

Buspirone

A

approved for the tx of generalized anxiety disorder

  • no sedation, hypnotic, euphoric, anticonvulsant, or muscle relaxant effects
  • metabolized by CYP3A4, watch out for hepatic impairment
39
Q

adverse effects of buspirone?

A

-tachycardia, palpitation, nervousness, GI distress, paresthesias, and dose-dependent papillary constriction

40
Q

Meprobamate

A
  • Approved for the short term relief of anxiety
  • good preop agent used to releive anxiety and provide sedation
  • Active metabolite of the drug carisoprodol

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