Anxiolytics

Question 1

Gold standard for treatment of anxiety disorders

Answer 1

SSRI or SNRI or TCA

Question 2

What drugs are SSRI’s contraindicated with

Answer 2

MAOIs

Question 3

How should you dose SSRI

Answer 3

Start low, gradually increase

Question 4

Are SSRIs safe to take with pregnancy

Answer 4

Not really - category C - they could be harmful, but we’re not sure

Question 5

What is the only SSRI does not lead to discontinuation syndrome?

Answer 5

Fluoxetine (Prozac)

Question 6

SNRI’s can be used for anxiety disorder

Answer 6

Venlaxafine (Effexor)

Duloxetine (Cymbalta)

Question 7

MAOI’s can be used for anxiety disorder

Answer 7

Tranylcypromine (Parnate)

Phenelzine (Nardil)

Question 8

Imipramine (Tofranil)

Clomipramine (Anafranil)

Answer 8

TCA’s can be used for specific anxiety disorders:

Imipramine (Tofranil) - panic disorders
Clomipramine (Anafranil) - OCD

Question 9

What antidepressant should be avoided to treat anxiety disorder?

Answer 9

Buproprion (Wellbutrin)

Question 10

How long does it take for these medications to start working?

Answer 10

2-4 weeks - has to be gradually increased, has to be taken daily

Question 11

Barbiturates (-barbital)

Mechanism?

Answer 11

Bind within GABA-mediated chloride ion channel and increase chloride ion conductance into cell by increasing DURATION of opening, hyperpolarizes neuron, reduces excitability of neurons, depresses CNS

Increases chloride ion conductance INDEPENDENTLY of GABA

Question 12

Are barbiturates dangerous in overdose? High potential for dependence?

Answer 12

YES and YES- fatal

Question 13

Benzodiazepines

Mechanism?

Answer 13

Bind to BZD receptors associated with GABA receptor, enhancing GABA’s ability to increase chloride ion conductance

GABA increases FREQUENCY of opening, hyperpolarizes neuron, reduces excitability of neurons, depresses CNS

Question 14

Which is less dangerous - benzodiazepines or barbiturates and why?

Answer 14

Benzodiazepines - they compete with GABA, so GABA availability is the rate-limiting step

Question 15

When are benzodiazepines dangerous?

Answer 15

When mixed with other CNS depressants like alcohol - avoid giving to alcoholic patients

Question 16

What drug can you give to reverse effect of benzodiazepines in overdose?

Answer 16

Flumazenil (benzodiazepine receptor antagonist)

Question 17

Side FX of benzodiazepines?

Answer 17

Ataxia and falls in elderly
Confusion, memory impairment
Paradoxical excitation
REM suppression
Dependence and abuse potential

Question 18

BZD1 (CNS) receptor

Answer 18

sleep

Question 19

BZD2 (CNS) receptor

Answer 19

confusion, cognition, motor control

Question 20

BZD3 (peripheral) receptor

Answer 20

muscle relaxation

Question 21

Alprazolam (Xanax)

Answer 21

Benzodiazepine

Fast onset of action, but short duration of effect

As a result, not good for treating anxiety

Question 22

Diazepam (Valium)

Answer 22

Benzodiazepine

Fast onset of action, longer duration of effect

Question 23

Clonazepam (Klonopin)

Answer 23

Benzodiazepine

Slow onset of action, long duration of effect

Question 24

Lorazepam (Ativan)
Oxazepam (Serax)
Temazepam (Restoril)

Answer 24

Benzodiazepines that do not require oxidation for elimination (no liver required):

Good for patients w/ liver impairment

Question 25

Zolpidem (Ambien)
Zaleplon (Sonata)
Eszopiclone (Lunesta)

Answer 25

• Zolpidem (Ambien) - mid-range acting
• Zaleplon (Sonata) - shortest acting
• Eszopiclone (Lunesta) - longest acting

Selective BZD receptor agonists

Question 26

Buspirone (Buspar)

Answer 26

Non-BZD, non-barbiturate anxiolytic

Partial agonist at 5-HT1A receptor

No abuse potential

Side FX: dizziness, headache, nausea

Question 27

Propranolol (Inderal)

Metoprolol (Toprol)

Answer 27

Beta-blockers used for stage fright