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Phar 752 > Anxiolytics and Sedatives > Flashcards

Anxiolytics and Sedatives Flashcards

1
Q

Buspirone mechanism

A 
5HT1a Agonist (along with 6-hydroxybuspirone metabolite)
Alpha-2 Antagonism (due to 1-PP metabolite)
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2
Q

Buspirone metabolism

A

Two routes, both by 3A4:

  • 6-hydroxybuspirone: active as 5HT1a Agonist
  • 1-PP: active as an Alpha-2 Antagonist
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3
Q

Chlordiazepoxide

A

Librium

1st Benzodiazepine; 1960

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4
Q

Diazepam brand name

A

Valium

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5
Q

Diazepam metabolism

A

Two routes:

  • 3-hydroxydiazepam: active as Temazepam (Restoril)
  • N-desmethyldiazepam: active as Nordazepam
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6
Q

Diazepam characteristics

A

More lipophilic than Chlordiazepoxide

  • Faster onset
  • 5-10x more potent
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7
Q

Chlordiazepoxide metabolism

A 
Chlordiazepoxide, N-demethylation to...
N-desmethylchlordiazepoxide, amino group to carbonyl..
Demoxepam, Nitro group reduced...
Nordazepam, 3-position hydroxylation...
Oxazepam.
All of theses are active.
Oxazepam will be glucuronidated.
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8
Q

Clorazepate brand name

A

Tranxene

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9
Q

Clorazepate metabolism

A 
*Prodrug of Nordazepam*
"-ate" for carboxylate group...
Decarboxylation to Nordazepam (active)
Then, 3-hydroxylation to Oxazepam (active)
Then, Glucuronidation (inactive)
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10
Q

Lorazepam brand name

A

Ativan

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11
Q

Lorazepam metabolism

A

Direct Glucuronidation - NO active metabolites.

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12
Q

Lorazepam potency

A

More potent than Oxazepam due to 2-position Cl EWG.

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13
Q

Alprazolam brand name

A

Xanax

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14
Q

Alprazolam metabolism (similar to Triazolam)

A

Two routes, both by 3A4:
- 4-hydroxyalprazolam >
- alpha-hydroxyalprazolam
Both rapidly Glucuronidated; neither significantly contribute to action.

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15
Q

Clonazepam brand name

A

Klonopin

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16
Q

Clonazepam metabolism

A

Reduction of Nitro group to 7-aminoclonazepam (inactive)

Further N-acetylation.

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17
Q

Quazepam brand name

A

Doral

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18
Q

Quazepam metabolism

A

Benzene-Fluoro group to 2-oxoquazepam (active)

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19
Q

Quazepam indication

A

Insomnia

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20
Q

Midazolam brand name

A

Versed

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21
Q

Midazolam metabolism

A

3A4 Hydroxylation at alpha-“M”ethyl group (active)

Further Glucuronidation.

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22
Q

Midazolam indication

A

Preoperative sedation

Induction of anesthesia.

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23
Q

Triazolam brand name

A

Halcion

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24
Q

Triazolam metabolism (similar to Alprazolam)

A

Two routes, both by 3A4:
- 4-hydroxylation
- alpha-hydroxylation
Both rapidly Glucuronidated and excreted.

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25
Q

Flumazenil mechanism

A

Benzodiazepine Antagonist

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26
Q

Flumazenil brand name

A

Romazicon

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27
Q

Flumazenil structural alteration

A

Missing the 5-phenyl group altogether.

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28
Q

Flumazenil metabolism

A

Ester hydrolysis - short half life.

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29
Q

Flumazenil route of administration

A

IV

30
Q

Most important characteristic of Barbituate SAR

A

5,5-disubstitution

31
Q

Butabarbital sodium brand name

A

Butisol sodium

32
Q

Butabarbital sodium C-5 carbons, t1/2, duration

A

6
45-60hrs
6-8hrs

33
Q

Secobarbital brand name

A

Seconal

34
Q

Secobarbital C-5 carbons, other modifications, and duration

A

8
Unsaturation in C-5 side chain
3-4hrs

35
Q

Methohexital sodium C-5 carbons, and other modifications

A

9
Extra N-methyl
Extra unsaturation in C-5 side chains

36
Q

Methohexital sodium characteristics

A

Added features increase lipophilicity, and increase activity.
Rapid onset and very short duration.

37
Q

Methohexital sodium indication

A

Induction of anesthesia

38
Q

Chloral hydrate

A

In water, small amounts go to Trichloroacetylaldehyde.
In presence of NADH, in vivo, goes to THE
- THE believed to be the sedative component.
Some migraine drugs contain Dichlorolphenazone
- Prodrug of Chloral hydrate

39
Q

Meprobamate key point

A

Meprobamate is a 2C19 metabolite of Carisoprodol (soma), a muscle relaxant.

40
Q

Zaleplon brand name

A

Sonata

41
Q

Zaleplon metabolism

A

Major: Aldehyde Oxidase to 5-0xozaleplon (active)
Minor: 3A4 to N-deethylzaleplon (inactive?)

42
Q

Zaleplon notable interaction

A

Cimetidine, an H2-antagonist, inhibits both Aldehyde Oxidase, and CYP-3A4.
Significantly increases t1/2 of Zaleplon.

43
Q

Eszopiclone brand name

A

Lunesta

44
Q

Eszopiclone metabolism

A

Two routes, both by 3A4:

  • N-desmethylzopiclone (inactive)
  • Eszopiclone N-oxide (inactive)
45
Q

Ramelteon brand name

A

Rozerem

46
Q

Ramelteon indication

A

Insomnia - for sleep onset.

47
Q

Ramelteon metabolism

A

One route, by both CYP 1A2 and 2C19

- Hydroxyramelteon metabolites (inactive)

48
Q

Ramelteon notable interaction

A

Fluvoxamine - 1A2/2C19 inhibition.

49
Q

Ramelteon mechanism

A

MT1 and MT2 receptor agonist

50
Q

Tasimelteon indication

A

24hr Sleep Wake disorder

- Usually for blind people (very expensive)

51
Q

Tasimelteon metabolism

A

One route, by both CYP 1A2 and 3A4

- Hydroxy metabolite (inactive)

52
Q

Dexmedetomidine brand name

A

Precedex

53
Q

Dexmedetomidine indication

A

For sedation as an IV clinically.

54
Q

Dexmedetomidine mechanism

A

Alpha-2 Agonist (autoreceptor)

55
Q

Suvorexant brand name

A

Belsomra

56
Q

Suvorexant mechanism

A

Orexin receptor, OX1 and OX2 antagonist

- Orexins promote wakefulness

57
Q

Suvorexant metabolism

A

3A4 hydroxylation (inactive)

58
Q

Gammahydroxybutyrate (GHB) also known as

A

Sodium oxybate (Xyrem)

59
Q

Gammahydroxybutyrate (GHB) mechanism

A

GABA-B modulator.

60
Q

Gammahydroxybutryate (GHB) key point

A

Restricted distribution program due to potential for abuse.

  • Applies to chemicals that can be used in it’s synthesis as well: 1,4-butanediol, and Gammabutyrolactone.
  • Both are GHB prodrugs.
61
Q

What is Oxazepam?

A

Figure out.

62
Q

Gammahydroxybutyrate (GHB) Indication

A

To treat excessive daytime sleepiness in narcolepsy patients, by helping them sleep.
Taken at bedtime, then 2.5-4hrs later.
Helps establish regular wake/sleep cycles.

63
Q

Zolpidem tartrate brand name

A

Ambien

64
Q

Zolpidem tartrate metabolism

A

3A4 aromatic ring methyl hydroxylation

- primary alcohol to carboxylate (inactive)

65
Q

Zolpidem tartrate dosing consideration

A

Max of 5mg in women, slower clearance.

66
Q

Z-Drug mechanism

A

Bind GABA receptors with an Alpha-1 subunit.

67
Q

Eszopliclone good for

A

Sleep onset and maintenance.

68
Q

Zolpidem tartrate good for

A

Sleep onset and maintenance.

69
Q

Zaleplon good for

A

Sleep onset only.

70
Q

Suvorexant good for

A

Sleep onset and maintenance.

71
Q

Triazolam consideration

A

Not to be used in elderly.

72
Q

If you had to use a BZD in an elderly patient…

A

Use Temazepam (Restoril)

Phar 752 (12 decks)

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