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Pharmacology Block 2 > Anxiolytics & Hypnotics > Flashcards

Anxiolytics & Hypnotics Flashcards

1
Q

Benzodiazepines

A

Potentiate the effect of GABA at Cl- ion channels

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2
Q

Diazepam

A

-A BZD that is a pos allosteric modulator of GABA A Rs

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3
Q

Propranolol

A

Helps with performance anxiety

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4
Q

GABA shunt

A

Refers to alpha ketoglutarate from the Krebs Cycle, converted to glutamic acid by GABA-transaminase; then subsequently to GABA by glutamic acid decarboxylase (GAD). GABA is then metabolized to form succinic semialdehyde to succinic acid and returns to the Krebs Cycle.

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5
Q

Glutamine loop

A

Glutamine is formed as GABA is transaminated and converted to glutamine. The glutamine is reconverted to glutamate; then decarboxylated by neuronal GAD to GABA

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6
Q

What do BZD not do themselves?

A

open the GABA Cl- channel

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7
Q

The GABA site of the GABA R is distinct from

A

the BDZ site and encompasses alpha-1 and beta-2 subunits

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8
Q

Flumazenil

A

BZD antag

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9
Q

Barbiturates

A
  • Bind to a distinct subunit combination on the GABA receptor
  • At high concentrations can open the channel on their own (without GABA).
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10
Q

BZD and hepatic induction

A

Benzodiazepines do not induce hepatic microsomal enzymes

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11
Q

Diazepam uses

A

anxiety, insomnia, pre-op, muscle relaxant

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12
Q

Chlordiazepoxide uses

A

alcohol detox

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13
Q

Flurazepam, Temazepam and Triazolam use

A

insomnia

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14
Q

Clonazepam

A
  • Panic
  • Anxiety
  • Seizure
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15
Q

Alprazolam

A
  • Short acting BZD
  • Panic
  • Anxiety
  • First line treatment for panic disorder withSSRI
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16
Q

Lorazepam

A
  • Short acting BZD
  • Anxiety
  • Alcohol related seizure
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17
Q

Adverse effects of BDZ

A
  • Sedation
  • Tolerance
  • Physical dependence
  • Self-admin
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18
Q

Toxicity of BZD

A
  • Impaired judgment
  • Slurred speech
  • Incoordination
  • Stupor
  • Respiratory depression
  • Death
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19
Q

Non-BDZ

A
  • Anxiolytic

- Buspirone (5-HT1A R partial agonist)

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20
Q

First line treatment for all anxiety disorders

A

SSRI + BZD

–provides early coverage

21
Q

Cognitive behavioral therapy (CBT)

A

Often used in conjunctive with SSRIs for anxiety

22
Q

When do we see severe respiratory depression

A

When BZD are combined with other sedatives/CNS depressants (like alcohol)

23
Q

GAD first line treatment

A

SSRI, usually venlafaxine, paroxetine or escitalopram

24
Q

Panic disorder first line treatment

A

SSRI + benzodiazepine for immediate action (alprazolam)

25
Q

PTSF (post traumatic stress disorder) first line treatment

A

SSRI, usually paroxetine or sertraline

26
Q

Which BZD are used for sleep?

A

Estazolam, flurazepam, quazepam, temazepam, triazolam

27
Q

Which drugs are typically used for sleep?

A

Eszoiclone, hydroxyzine, zolpidem, zaleplon, ramelteon

28
Q

Describe the adult sleep cycle

A

Duration of about 90 min; includes NREM and REM sleep

29
Q

Melatonin

A

produced in the pineal gland at night

30
Q

Hypnotics

A

Produce drowsiness and promote the onset and maintenance of sleep

31
Q

What are the symptoms of insomnia?

A

Difficulty falling asleep, frequent wakenings, poor quality of sleep

32
Q

What is sleep deprivation?

A

Inadequate opportunity for sleep; sleep itself is relatively normal

33
Q

What is insomnia disorder?

A

Insomnia complaint and significant daytime impairment

34
Q

Short acting BZDs

A

Alprazolam, triazolam, lorazepam, oxazepam

35
Q

Long acting BZDs

A

Flurazepam, clorazepate, prazepam

36
Q

Doxepin

A
  • TCA

- low dose mechanism for insomnia is histamine H1

37
Q

Non-BZD GABA A agonists

A

Eszopiclone, zolpidem, zaleplon

38
Q

Ramelteon

A

Melatonin agonist for sleep

39
Q

Which drugs are sedating antidepressants

A

Trazodone, mirtazapine, amyitriptyline

40
Q

Zolpidem advantges

A

Shorten sleep latency, improve duration, can be used as needed, no negative effect on sleep architecture

41
Q

Zolpidem disadvantages

A

4-6 hr effect, therefore not for middle of the night awakenings, associated with parasomnias

42
Q

Traditional BZD disadvantages

A

Rebound insomnia, memory impairments, loss of coordination, abuse potential, not good for those with respiratory conditions

43
Q

Barbiturates and GABA

A

Increase duration of channel opening, powerful CNS depression; low margin of safety

44
Q

Diphenhydramine

A

Benadryl; sedating antihistamine

45
Q

Anxiety, insomnia, pre-op, muscle

A
  • Long acting BZD

- insomnia

46
Q

Temazepam

A
  • BDZ

- insomnia

47
Q

Triazolam

A
  • Short acting BZD

- Insomnia

48
Q

Oxazepam

A
  • Short acting BZD

- Alcohol detox

49
Q

Zolpidem

A
  • Non-BZD GABA A agonist

- insomnia

Pharmacology Block 2 (4 decks)

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