Anxiolytics Flashcards
Gold standard for treatment of anxiety disorders
SSRI or SNRI or TCA
What drugs are SSRI’s contraindicated with
MAOIs
How should you dose SSRI
Start low, gradually increase
Are SSRIs safe to take with pregnancy
Not really - category C - they could be harmful, but we’re not sure
What is the only SSRI does not lead to discontinuation syndrome?
Fluoxetine (Prozac)
SNRI’s can be used for anxiety disorder
Venlaxafine (Effexor)
Duloxetine (Cymbalta)
MAOI’s can be used for anxiety disorder
Tranylcypromine (Parnate)
Phenelzine (Nardil)
Imipramine (Tofranil)
Clomipramine (Anafranil)
TCA’s can be used for specific anxiety disorders:
Imipramine (Tofranil) - panic disorders
Clomipramine (Anafranil) - OCD
What antidepressant should be avoided to treat anxiety disorder?
Buproprion (Wellbutrin)
How long does it take for these medications to start working?
2-4 weeks - has to be gradually increased, has to be taken daily
Barbiturates (-barbital)
Mechanism?
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
Are barbiturates dangerous in overdose? High potential for dependence?
YES and YES- fatal
Benzodiazepines
Mechanism?
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
Which is less dangerous - benzodiazepines or barbiturates and why?
Benzodiazepines - they compete with GABA, so GABA availability is the rate-limiting step
When are benzodiazepines dangerous?
When mixed with other CNS depressants like alcohol - avoid giving to alcoholic patients
What drug can you give to reverse effect of benzodiazepines in overdose?
Flumazenil (benzodiazepine receptor antagonist)
Side FX of benzodiazepines?
Ataxia and falls in elderly Confusion, memory impairment Paradoxical excitation REM suppression Dependence and abuse potential
BZD1 (CNS) receptor
sleep
BZD2 (CNS) receptor
confusion, cognition, motor control
BZD3 (peripheral) receptor
muscle relaxation
Alprazolam (Xanax)
Benzodiazepine
Fast onset of action, but short duration of effect
As a result, not good for treating anxiety
Diazepam (Valium)
Benzodiazepine
Fast onset of action, longer duration of effect
Clonazepam (Klonopin)
Benzodiazepine
Slow onset of action, long duration of effect
Lorazepam (Ativan)
Oxazepam (Serax)
Temazepam (Restoril)
Benzodiazepines that do not require oxidation for elimination (no liver required):
Good for patients w/ liver impairment
Zolpidem (Ambien)
Zaleplon (Sonata)
Eszopiclone (Lunesta)
- Zolpidem (Ambien) - mid-range acting
- Zaleplon (Sonata) - shortest acting
- Eszopiclone (Lunesta) - longest acting
Selective BZD receptor agonists
Buspirone (Buspar)
Non-BZD, non-barbiturate anxiolytic
Partial agonist at 5-HT1A receptor
No abuse potential
Side FX: dizziness, headache, nausea
Propranolol (Inderal)
Metoprolol (Toprol)
Beta-blockers used for stage fright