Anti-anxiety drugs Flashcards
What is general anxiety disorder?
Excessive/unreasonable/irrational anxiety about normal life circumstances
Interferes with normal daily functioning and rarely includes panic attacks
What is panic disorder?
Recurrent, unexpected panic attack characterized by intense fear/discomfort
Rapid onset may include palpitations, shaking, and numbness
On going worrying, avoidance of people/pleaces associated with previous panic attacks
What is obsessive compulsive disorder?
Need to check things repeatedly, perform rituals/routines- like hand washing
What is post traumatic stress disorder?
Stress disorder that can develop after experiencing a traumatic event
- Combat, car accident, phsyical/sexual assault
Anxiety is a core symptom that can be exacerbated by reminders of post trauma
What is social anxiety disorder?
persistent, irrational fear of one or more social situations
Blushing sweating trembling palpitations, nausea, panic attacks
Benzodiazepines are used for?
GAD and PD
SSRIS are used for?
GAD, PD, OCD,PTSD, SAD
TCA are used for?
PD
Venlafaxine (SNRI) are used for?
GAD
Buspirone is a what and used for?
5-HT1A and its used for GAD
Clomipramine is what and used for what?
TCA used for OCD
How do benzodiazepines work?
They act on GABA A receptors
How do GABA receptors work?
They increase chloride clearance and inhibit neuronal firing
Where do benzos bind on the GABA A receptors?
Between gamma2 and alpha 1
What other things bind to the GABA A receptors?
Ethanol
General anesthetics
Barbiturates
What is the antidote to benzodiazepines?
Fumazenil- it its a benzo antagonist, reverse its effects
What the different subunits of the GABA A receptors?
Alpha 1-6
BZ1 on alpha 1= sedation/hypnosis
BZ2 alpha 2,3,5= anxiolytics
Alpha 4 and 6 are non-BZ
As you increase the dose of benzos….
You increase the severity of sedation…. to coma and death
What is a major difference of benzos?
Anxiolytic Vs hyponsis
What meds are anxiolytic?
Alprazolam
Clonazepam
Diazepam
Lorazepam
Oxazepam
What meds of hypontics?
Flurazepam
Temazepam
Estazolam
Triazolam
In regards to pharmacokinetics, large variations in the rate of drug onset is do to what 3 reasons?
- Individual differences in pts
- Rate of absorption
- Amount of protein binding.
Lipophilic BZ like diazepam have a more rapid onset (-20 min) than less lipopihlic BS like oxazepam (3hrs)
In regards to pharmacokinetics, large variations in the duration of the drug effect depends on?
- Rate of metabolism (age)
- Deposition in body tissues
For example, many BS have active metabolites that prolongs their duration
For example, diazepam accumulates in fat which prolongs its duration.
What was the first BZ discovered?
Chloradiazepoxide, it has a half life of 24-48 hrs.
What does the chloradiazepoxide have such a long half life?
Active metabolites
What are the 3 BZ that do not have active metabolites?
Lorazepam
Temazepam
OXazepam
What are the 3 BZs without active metabolites good for?
Good for patients with lowered liver function, patients who can’t rely on their liver enzymes to break down the meds
What is the class of inactive metabolites called?
gluconoride conjugates
What is the difference in prescriptions of BZ for an elderly patient versus a young adult?
Elderly patient should always receive a lower dose.
What are the adverse effects of BZs?
Sedation
Black box warning for alcohol/opioid use
Paradoxical excitation
sleep disturbances
allergic reactions
Who is more likely and less likely to develop sedation adverse effect when taking a BZ?
More likely to occur in elderly, less likely if pt has hx of ethanol, barbiturate, or heavy smokers
How can the severe adverse effects of BZ be reversed?
Flumazenil- BZ antagonist
Who has a higher chance of developing the rare, paradoxical excitation adverse effect of BZ?
The very young and elderly, it reduces seizure threshold.
Who are more likely to develop the allergic reaction associated with BZ?
Elderly, smokers, and women on oral contraceptives or people getting repeated injections
Are BZ abused?
Yes and no.
BZ can be used in addition to other addications like opiods, alcohol or stimulants.
Its not usually abused by itself
Does it take awhile for tolerance to build up?
No, tolerance can be profound. A pt can go from 5 mg/day to 1000mg/day for diazepam and not be abusing it.
It can lead to a greater sedative than anxiolytic effect
What happens if someone stops taking a BZ cold turkey?
Withdraw can happen.
it requires dose tapering.
SSRIs are the drug of choice for which disorders?
PD
PTSD
SAD
SSRI are the second line for which disorder?
GAD- if BZ fail
OCD- if clomipramine fails
Which part of the brain plays an important role in emotional processing, in regard to fear and axiety?
Amygdala- this is where SSRIs are said to work
Which three SSRIs are shown efficacy treating most forms of anxiety?
Fluoxetine
Citalopram
Escritalpram
Fluoxetine is?
SERT selective uptake inhibitor (5-HT2CR Antagonist)
Has a delayed therapeutic effect- around 5 weeks
Works for OCD and PD
Citalopram is…
SERT selective uptake inhibitor
Used for PD
Escitalopram is…
SERT selective uptake inhibitor
S-enantiomer of citalopram which is thought to be responsible for most of the anti-depressant effect
Used for GAD
What is Busprione?
It was an antipsychotic drug that was found to help lower anxiety in patients.
It’s a 5-HT1AR Agonist and DA D2 like R antagonist
It takes 1-3 weeks to work
What is Buspirone used for?
GAD and PTSD
