Sedative-Hypnotic Agents

Question 1

Benzodiazepenes for acute anxiety (7)

Answer 1

all -zepam, -zepate, (except 2). Use MADLOT for time to peak blood levels

• Alprazolam (Xanax)
• Chlordiazepoxide (Librium)
• Clonazepam (Klonopin)
• Clorazepate (Tranxene)
• Diazepam (Valium)
• Lorazepam (Ativan)
• Oxazepam (Serax)

Question 2

Midazolam

Answer 2

BZ for presurgical sedation- short T1.5

Question 3

Benzodiazepenes mechanism

Answer 3

-Bind part of GABAa channel, increase frequency of opening

Question 4

Benzodiazepenes advantages (4), disadvantages (3)

Answer 4

Ad:
1) rapid onset (so only acute anxiolytic)
2) high TI, flumazenil can easily reverse
3) low risk of drug interactions
4) minimal CV/autonomic side effects
Dis:
1) Dependence risk
2) CNS depression
3) anterograde amnesia

Question 5

BZ Interactions, Side effects, Overdose symptoms

Answer 5

Interactions: other CNS depressants (other sedatives, anti-anxiety, antihistamines, anti-cholinergics, alcohol)
Side effects: drowsiness, impaired judgement/motor skills, amnesia, dependence/withdrawal (anxiety, insomnia, CNS convulsions), lethargy, exhaustion, EtoH intoxication presentation
OD symptoms: respiratory depression, can kill if aspirate vomit. Treat with flumazenil

Question 6

Flumazenil

Answer 6

First line treatment for BZ overdose

• binds at same site and directly opposes BZs and hypnotics
• need repeat administration since 1/2 life is only 1-2h, BZs are days

Question 7

Antidepressants for General Anxiety Disorder - SSRIs (4)

Answer 7

FLew to PARis to ESCape SERvice
Fluoxetine (Prozac)
Paroxitine (Paxil)
Sertraline (Zoloft)
Escitalopram (Lexapro)

-like SSRI/SNRI, takes weeks for action, so chronic anxiolytic

Question 8

Antidepressants for General Anxiety Disorder - SNRIs (2)

Answer 8

Duloxetine (Cymbalta)
Venlafaxine (Effexor)

-like SSRI/SNRI, takes weeks for action, so chronic anxiolytic

Question 9

Buspirone

Answer 9

-anxiolytic without sedation/hypnotic effects- not GABA based
-mechanism: partial agonist at 5HT1a receptors
-second line anxiolytic since inconsistent efficacy
-like SSRI/SNRI, takes weeks for action, so chronic anxiolytic
Side effects: minimal
Drug interactions: CYP3A4 inducers/inhibitors, MAOIs

Question 10

Hypnotics drug types used for Insomnia (4)

Answer 10

• BZs
• non-BZ (ZEZ)
• Non-GABA (Ramelteon, Suvorexant)

Question 11

Hypnotics for Insomnia- BZs (5)

Answer 11

-zolams and -zepams

• Triazolam
• Temazepam
• Estazolam
• Quazepam
• Flurazepam

Question 12

Non-BZ Hypnotics for Insomnia (3)

Answer 12

Zaleplon (Sonata)
Zolpidem (Ambien)
Eszapiclone (Lunesta)
-rapid onset, little day-after effects, but dependency/withdrawal/rebound like BZs

Question 13

Ramelteon

Answer 13

Melatonin agonist

-not controlled since no withdrawal/rebound like other hypnotics. But also not as good success rate

Question 14

Suvorexant

Answer 14

Orexin antagonist
-No GABAergic CNS side effects like BZs
-risk of abuse/dependence like BZs
Side effects: sleep driving, amnesia