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Behavioral Science > Kruse Sedative-Hypnotics > Flashcards

Kruse Sedative-Hypnotics Flashcards

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1
Q

Dose dependent depression of CNS function: What are the curves of barbituates and alcohol v. benzos and new hypnotics?

Which has steeper dose-response curve?

A

Barbituates/alcohol have a linear and **steeper increase making them more dangerous than curved plateau of benzos/newer hypnotics.

CNS effects with increasing dose: Sedation to hypnosis to anesthesia to coma.

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2
Q

MOA of ___:
Bind to specific allosteric GABA-A receptor subunits at CNS synapses enhancing increase in FREQUENCY of GABA-mediated ___ ion channel opening; enhance membrane hyperpolarization.
They increase frequency of channel openings by shifting the dose-response curve to the left. This means what?

A

Benzodiazepines

GABA mediated Chloride ion channel opening (increase FREQUENCY)

Shift dose response curve to the left means that less GABA required to activate the receptor

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3
Q

These clinical symptoms dictate use of what drug? Anxiety, hypnosis, night terrors and sleepwalking, spasticity, anticonvulsant for status epilepticus, alcohol detoxification (eg, DTs), general anesthesia

A

Benzos

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4
Q

MOA of___:

Facilitate GABA-A action by increasing the DURATION of __ channel opening

A

Barbituates - chloride

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5
Q

MOA of misc nonbenzo sedative-hypnotics:

  • eszopiclone, zaleplon, and zolpidem
  • ramelteon
A
  • affect alpha1 subunit of GABA-A receptors (like benzos)

- activates MT1 and MT2 receptors

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6
Q

All sedative-hypnotics cross into three areas.

A

CNS (BBB), placental barrier, breast milk

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7
Q

Absorption of sedative-hypnotics depends on what solubility.

Metabolization of sedative-hypnotics (esp benzo and newer hypnotics) depends on what?

A

lipid solubility

metab depends on liver CYP3A4

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8
Q

Triazolam, thiopental, and newer hypnotics - relative lipid solubility and what this means for onset.

A

very soluble, so fast acting (good for anesthesia)

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9
Q

CYP__ for hepatic metabolism of benzos. Most undergo Phase __ reactions.

Are benzos with longer half lives or shorter half lives more likely to cause cumulative effects (drowsiness)?

A

CYP3A4

Phase 1 >Phase 2 (glucuronidation)

Longer 1/2 live has more cumulative dose (think postanesthetic respiratory depression).

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10
Q

Patient with a preexisting disease needs benzo for anxiety, so you give oxazepam and lorazepam? What condition are these indicated?

A

Because oxazepam and lorazepam only have to go through one hepatic metabolization step before being excreted.

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11
Q

The only barbituate excreted unchanged (not as a glucuronide conjugate). What pH can change its elimination rate?

A

Phenobarbital

Alkalinization of urine can increase elim rate.

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12
Q

Biotransformation of eszopiclone, zolpidem, zaleplon is through CYP___

A

CYP3A4

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13
Q

Phenobarbital (barbituate) and meprobamate (new sedative-hypnotic drug) have what special characteristic that affects bioavailability.

A

They can INDUCE hepatic CYP450 after long-term use, which can increase their/other drug metabolism.

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14
Q

Two fastest onset benzos.
Three int/longer onset benzos.

What does this mean for admin to patients with addiction problems?

A

Fast: Alprazolam and Diazepam (also, clorazepate and flurazepam) –> addictive

Slower: clonazepam, lorazepam, oxazepam –> not as addictive

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15
Q

GABA-A receptors are responsible for most ___ transmission in the CNS

A

inhibitory (CNS influx into neuron = polarization)

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16
Q

Benzos and Barbituates:

Cl influx –> _(hypo/hyper)__polarization of neurons —> _(increased/decreased)__ number of AP = ___ state of CNS

A

Cl influx –> HYPERpolarization of neurons —> DECREASED number of AP = DEPRESSED state of CNS

17
Q

Flumazenil (antagonist) blocks the actions of benzos, eszopiclone, zaleplon, and zolpidem. But it does not block what three things with different binding sites?

A

Barbituates, meprobamate, ethanol, meprobamate, buspirone, ramelteon

18
Q

Anxiety treated by S-H induced ___.

Hypnosis induces ___

A

sedation

sleep

19
Q

persistent postanesthetic respiratory depression de to what drug class?

A

Benzos, which have long half lives

20
Q

eszopiclone, zaleplon, and zolepidm have what anticonvulsant activity?

A

none

21
Q

Drug that binds to benzo binding site on GABA-A receptors and acts as a competative antagonist

A

Flumazenil.

22
Q

Drug used to treat benzo overdose and shorten recovery following benzo anesthetic

A

Flumazenil

23
Q

Concomitant treatment of anxiety:
____ on short term relief (acute panic attacks)
____ for long term treatment

A

Short term - benzo

Long term - SSRI

24
Q

Two risks of using benzos for sleep problems.

A

Can cause daytime sedation

Risk of developing tolerance and anterograde amnesia.

25
Q

Most commonly used agents for sleep problems:

  • which for helping fall asleep
  • which for helping staying asleep
A

Help falling asleep - zaleplon and zolpidem OR ramelteon

Help staying asleep - eszopliclone

26
Q

What class is contraindicated in porphyria?

A

barbitates

27
Q

Ramelteon MOA

do not admin with what SSRI?

A

Agonist at MT1 and MT2 receptors in suprachiasmic nucleus of the brain.

Fluvoxamine inhibits CYP1A2

28
Q

Drug used for generalized anxiety disorder that does not cause sedation, hypnotic, euphoric, anticonvulsant, or muscle relaxant effects (limited psychomotor impariment, making it less addictive).

What is the onset - fast or slow?

A

buspirone

Slow onset - 1 to 2 weeks

(AE=tachycardia, palpitations, nervousness, GI distress, paresthesias, dose dependent papillary construction)

29
Q

Drug used for short term relief of anxiety and sedation. But has a high abuse and dependence potential.

A

Meprobamate

30
Q

Toxicities/risk of ___:

extensions of CNS depressant effects. Dependence liability

A

benzos

31
Q

Toxicities/risk of ___:
Toxicity shows agitation,
confusion. Possible withdrawal
symptoms in benzodiazepine dependence

A

flumazenil

32
Q

Toxicities/risk of ___:
Toxicity shows extensions of
CNS depressant effects. Dependence liability greater than benzodiazepines

 Interactions: additive CNS
depression with ethanol
and many other drugs
 Induction of hepatic drug metabolizing
enzymes
A

barbituates

33
Q 
Toxicities/risk of \_\_\_:
Toxicity shows extensions of
CNS depressant effects
 Dependence liability
 Interactions: additive CNS depression with ethanol
A

eszopliclone, zaleplon, zolpidem

34
Q

Toxicities/risk of ___:
Toxicity shows dizziness, fatigue, endocrine changes
 Interactions: Fluvoxamine inhibits metabolism

A

ramelteon

35
Q

Toxicities/risk of ___:
 Toxicity shows tachycardia,
paresthesias, gastrointestinal distress
 Interactions: CYP3A4 inducers and inhibitor

A

buspirone

Behavioral Science (16 decks)

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