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Psych Pharm > Sedative- Hypnotics (Anxiolytics) > Flashcards

Sedative- Hypnotics (Anxiolytics) Flashcards

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1
Q

What are the Benzodiazepines

A

Alprazolam, Chlordiazepoxide, Clonazepam, Clorazepate, Diazepam, Lorazepam, Oxazepam, Prazepam

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2
Q

What are the non-benzodiazepine anxiolytics

A

Buspirone, Propanolol

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3
Q

What is the mechanism of action of Benzodiazepines

A

They act as allosteric agonists, they do not activate the receptor independently of the natural ligand. They potentiate effects of GABA

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4
Q

What is Flumazenil and what does it do/used for

A

Flumazenil is a competitive antagonist that blocks the effects of benzodiazepines

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5
Q

Which drugs are metabolized to N-desmethyldiezapam (nordiazepam)

A 
Clorazepate
Diazepam
Chlordiazepoxide
Prazepam
Halazepam
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6
Q

Of the drugs that are metabolized to nordiazepam, which is not directly metabolized to this but must first undergo other phases of metabolism?

A

Chlordiazepoxide

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7
Q

What are the active metabolites of Chlordiazepoxide?

A

N-desmethylchlordiazepoxide
Demoxepam
Nordiazepam

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8
Q

What is N-desmethyldiazepam (nordiazepam) metabolized to, and by what process does this occur?

A

Oxazepam via Hydroxylation

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9
Q

Which Benzodiazepines are not metabolized to Oxazepam?

A

Alprazolam and Lorazepam

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10
Q

What is the active metabolite of Alprazolam?

A

a-hydroxyalprazolam

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11
Q

Which drug is converted directly to a Glucuronide conjugate?

A

Lorazepam

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12
Q

Are benzodiazepines safe for pregnancy? What Pregnency catagory are they in?

A

No. Catagory D

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13
Q

Which Benzodiazepines have a Rapid onset of action?

A

Clorazepate
Diazepam
Flurazepam
Triazolam

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14
Q

Which Fast acting Benzo has the shortest half life?

A

Triazolam (It is the only Rapid onset Benzo with a short t1/2, all others have long t1/2)

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15
Q

Which Benzos have a slow onset of action?

A

Oxazepam
Prazepam
Temazepam

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16
Q

Which slow acting Benzo has a short half life?

A

Oxazepam

17
Q

Which slow acting Benzo has a long half life?

A

Prazepam

18
Q

Withdrawal reactions occur after abrupt discontinuation of Benzos. Which benzos should be tapered?

A

Short half life benzos should be tapered.

Triazolobenzodiazepines (Alprazolam, Estazolam, and Triazolam)

19
Q

Which Benzo is most used for panic attacks? Why?

A

Alprazolam because it also has antidepressant effects similar to TCAs.

20
Q

Which Benzo produces muscle relaxation in clinical doses?

A

Diazepam

21
Q

Which Benzos are used to treat Alcohol withdrawal?

A

Chlordiazepoxide
Diazepam
Lorazepam

22
Q

Which Benzo do you use to treat Alcohol withdrawal in a person with hepatic impairment?

A

Lorazepam because it undergoes Renal metabolism as well

23
Q

Which subunits on the GABA receptor do Benzos bind to, to enhance inhibitory action of GABA?

A

a1, a2, a3 or a5 AND y subunit

24
Q

What is the chronological order in which the tolerance to benzos develop

A
  1. Sedative and Hypnotic effect
  2. Anticonvulsant effect
  3. RARELY IF EVER TO ANXIOLYTIC EFFECT
    (the time which tolerance develops varies by drug)
25
Q

What is the mechanism for tolerance to Benzos

A
  1. Receptor uncoupling
  2. Receptor sub-unit down-regulation
  3. Sensitization of glutamatergic system
  4. Crosstalk from other G-protein receptor systems
26
Q

Which Benzos can be administered by injection?

A

Diazepam

Lorazepam

27
Q

What patient populations do you need to be careful prescribing Benzos to? Why?

A

Older patients, especially those with COPD because Benzos cause respiratory depression

28
Q

In a patient who is experiencing respiratory depression from Benzos, what drug do you give to offset the effects?

A

Flumazenil

29
Q

What is the mechanism of action of Buspirone?

A

Supresses seretonergic while enhancing noradrenergic and dopaminergic activities

30
Q

What is Buspirone used for?

A

Equally effective as Benzos as anxiolyitc

Has no anticonvulsant, muscle relaxant, or sedative effect

31
Q

What is propanolol used for (not cardio)

A

performance anxiety or stage fright

32
Q

What is the problem with using buspirone?

A

It has a VERY slow onset, and takes weeks to see clinical effect

33
Q

Describe mechanism of Propanolol to reduce stage fright (not mechanism of action)

A

supresses somatic and autonomic symptoms of anxiety but does not alter emotional symptoms

Psych Pharm (3 decks)

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