Part 1
Anxiolytics
Benzodiazepines – act at GABA (Gamma amino butyric acid)
receptor – an inhibitory neurotransmitter
Alprazolam (Xanax)
Lorazepam (Ativan)
Temazepam (Restoril)
Clonazepam (Klonopin)
NEED to know, MOA, indications (pretty much anxiety),
side effects, which receptor is it attaching to? GABA!!!,
what to teach? This can make you tired, so you don’t want
to drive
Increasing GABA DECREASES the effect of neuronal
excitement or decrease neuron firing
1. Reduction in anxiety
2. Muscle relaxation
3. Ataxia
4. Anticonvulsant activity – cannot be used solely as
this
Buspar – (sometimes called an atypical anxiolytic)
Approved for the tx of GAD
1. MOA: acts mainly at the pre-synaptic Serotonin 1a
receptor. It does have some activity at the dopamine
receptor, but be sure to know that it primarily acts
at the serotonin receptor.
2. Also has action at dopamine receptors
Absorbed well orally
1. Should be taken with food to decrease the first-pass
effect
Short half-life, but slow onset of action
Works better for anxiety than depression
Antidepressants
SSRIs – act at the Serotonin receptor
What should you focus on as you study?
Paroxetine (Paxil)
Fluoxetine (Prozac)
Sertraline (Zoloft)
Citalopram (Celexa)
Escitalopram (Lexapro)
1. Indicated for MDD, GAD, OCD, PTSD, Panic Disorder
and more
, 1. They have a class effect, you can expect Paxil to do
the same as Prozac, etc. they have most of the same
side effects
However, Celexa and Lexapro.. very well
tolerated usually, decreased libido,
erectile dysfunction… then we can try a
different one in the same group.
Similar but different enough that it’s
possible to not have side effects with a
different drug
2. MOA: they inhibit the pre-synaptic reuptake of
serotonin
Serotonin is more available
Serotonin is a feel good drug
2. Adverse effects that all SSRIs have in common
Nausea, dry mouth, headache, sexual
side effects
2. Patient education that is important when prescribing
these medications
Take at the same time every day
Can take up to 6 weeks for full effects
Nausea, dry mouth, and headache can
improve after the first week, sexual side
effects usually don’t
3. Well absorbed orally
4. Have significant first-pass effect
5. Metabolized by the CYP450 system
6. Majority eliminated through the urine
7. Symptoms of serotonin syndrome
8. Drug-drug interaction with linezolid (Zyvox)
(antibiotic)
SNRIs – act at the Serotonin and Norepinephrine receptors
Venlafaxine (Effexor)
Duloxetine (Cymbalta)
1. MOA: block serotonin and norepinephrine
transporters, inhibiting the reuptake of
neurotransmitters
Potential for more side effects than
SSRIs
At lower doses, venlafaxine
predominantly affects serotonin
reuptake (not hitting the norepinephrine
inhibition as much) not on the test
Tricyclic antidepressants