anxiolytics - benzos Flashcards

0
Q

which of the benzos have active metabolites that have a T1/2 up to 100hrs?

A

CD on Fire

  1. chlordiazepoxide
  2. diazepam
  3. flurazepam
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1
Q

name all the benzodiazepines (7): in order from shortest to longest T1/2:

A
  1. midazolam (1.9hr)
  2. triazolam (2.9hr)
  3. alprazolam (12hr)
  4. lorazepam (14hr)
  5. chlordiazepoxide
  6. diazepam
  7. flurazepam
    MTAL CD on Fire!
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2
Q

which of the benzos are directly metabolized to inactive glucuronides?

A

lorazepam (maybe midazolam, triazolam, alprazolam)

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3
Q

which of the benzos have to get oxidized via the P450 microsomal system in the liver, then conjugated to become inactive?

A

CD on Fire

  1. chlordiazepoxide
  2. diazepam
  3. flurazepam
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4
Q

where do the benzos bind/work?

A

GABAa receptors (binds btwn a1-y2 subunits); GABAa agonists

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5
Q

which benzos are not use to tx short-term depression, but instead used as an anesthesia (has calming effects, and produces anterograde amnesia)?

A

midazolam

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6
Q

which benzos is used for anticonvulsant and muscle relaxant, in addition to typical benzo’s use: short-term depression, maintenance of bipolar, severe bipolar?

A

diazepam, lorazepam

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7
Q

which benzo is typically used for sedation, anticonvulsant, and to PREVENT W/D SEIZURES AND SYMPTOMS IN ALCOHOLICS?

A

lorazepam

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8
Q

what are the SE’s of benzos?

A
  1. daytime sedation and drowsiness
  2. anterograde amnesia
  3. synergistic depression of CNS with other drugs
  4. psychologic and physiologic dependence with chronic use
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9
Q

can u die from benzo OD? why/why not?

A

no, b/c have ceiling effect. only augments GABA but potentiating Cl- channel opening; does not directly open Cl- channels.

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10
Q

what toxin binds noncompetitively at GABAa Cl- channels and in doing so, produces convulsions?

A

picrotoxin, GABAa antagonist

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11
Q

drug that is a non-benzo receptor agonist?

A

zolpidem

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12
Q

BDZ-1 selective agonist

A

zolpidem

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13
Q

benzodiazepine antagonist and specifically, competitive non-selective antagonist

A

flumazenil

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14
Q

drug used to produce sedation (calming/anxiolytic) and hypnosis (sleepiness) without muscle relaxation or anticonvulsant activity?

A

zolpidem

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15
Q

drug used for benzo ODs?

A

flumazenil

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16
Q

SE: sleep walking/driving/eating, next morning impairment

A

zolpidem

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17
Q

SE: might have life-threatening w/d sx, and siezures in mixed ODs, nonuniform in reversal of respiratory depression

A

flumazenil

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18
Q

which disorders do you not use SSRI’s as first line tx (what do you use instead)?

A

acute anxiety/benzos

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19
Q

for what disorders do you use SSRIs and/or benzos?

A

GAD, panic disorder

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20
Q

what disorder do you use SSRIs?

A

OCDs

21
Q

which drug relieves anxiety (is anxiolytic) without marked sedation?

A

buspirone

22
Q

at what receptor does buspirone work on?

A

partial agonist at 5HT1a receptors;;;;no interaction with GABAa receptor complex

23
Q

what are the two barbiturates?

A
  1. thiopental

2. phenobarbitol

24
Q

what are the two barbiturate GABAa agonists?

A
  1. thiopental

2. phenobarbitol

25
Q

which barbiturate is highly lipid soluble, fast on, fast off?

A

thiopental

26
Q

which barbiturate is less lipid soluble, slower onset and slower elimination?

A

phenobarbitol

27
Q

which one for inducing anesthesia and which one for antiepileptic/anticonvulsant?

A

thiopental, phenobarbitol

28
Q

SE of barbs?

A

daytime sedation, drowsiness, dose dependent depression of CNS, psychologic and physiologic dependence if chronic use

29
Q

which barbs are life threatening when w/d abruptly?

which one is dosed based on lean body mass?

A

thiopental and phenobarbitol, thiopental

30
Q

drugs for inducing sleep?

A

triazolam, zolpidem

31
Q

drugs for sedation (calming, antianxiety, anxiolytic)?

A

shorter acting benzos: alprazolam, lorazepam

32
Q

anticonvulsants (3)

A

lorazepam
diazepam
phenobarbital

33
Q

mm relaxation (inhibitory effects on polysynaptic reflexes and inter-neuron transmissions

A

diazepam

34
Q

which disorders do you not use SSRI’s as first line tx (what do you use instead)?

A

acute anxiety/benzos

35
Q

for what disorders do you use SSRIs and/or benzos?

A

GAD, panic disorder

36
Q

what disorder do you use SSRIs?

A

OCDs

37
Q

which drug relieves anxiety (is anxiolytic) without marked sedation?

A

buspirone

38
Q

at what receptor does buspirone work on?

A

partial agonist at 5HT1a receptors;;;;no interaction with GABAa receptor complex

39
Q

what are the two barbiturates?

A
  1. thiopental

2. phenobarbitol

40
Q

what are the two barbiturate GABAa agonists?

A
  1. thiopental

2. phenobarbitol

41
Q

which barbiturate is highly lipid soluble, fast on, fast off?

A

thiopental

42
Q

which barbiturate is less lipid soluble, slower onset and slower elimination?

A

phenobarbitol

43
Q

which one for inducing anesthesia and which one for antiepileptic/anticonvulsant?

A

thiopental, phenobarbitol

44
Q

SE of barbs?

A

daytime sedation, drowsiness, dose dependent depression of CNS, psychologic and physiologic dependence if chronic use

45
Q

which barbs are life threatening when w/d abruptly?

which one is dosed based on lean body mass?

A

thiopental and phenobarbitol, thiopental

46
Q

drugs for inducing sleep?

A

triazolam, zolpidem

47
Q

drugs for sedation (calming, antianxiety, anxiolytic)?

A

shorter acting benzos: alprazolam, lorazepam

48
Q

anticonvulsants (3)

A

lorazepam
diazepam
phenobarbital

49
Q

mm relaxation (inhibitory effects on polysynaptic reflexes and inter-neuron transmissions

A

diazepam