Pharm tx of anxiety- Craviso Flashcards
HOw long do you have to have anxiety for GAD?
What are the three main neurotransmitters that you want to affect for tx of GAD?
6 months
Noradrenergic, serotonergic, Gabaergic (benzoes)
Which do you use more often for GAD, benzos or antidepressants?
Why?
antidepressants
-better efficacy for anxiety and for comorid disorders (i.e depression)
Do non benzos and antidepressants have their effects occur immediately or does it take several weeks?
How do you remedy this?
takes several weeks
-give benzo in combo with non benzos or antidepressants for INITIAL tx where benzos will be effective until to non benzo and antidepressants become effective
What is buspirone (buspar)?
What is it used for?
Is it for long or short term tx and are the effects immediate?
Partial agonist at 5HT1A receptor
- GAD and alcoholisms
- long term tx
- effects take several weeks
What are the adverse SEs of Buspirone?
dizziness, light-headedness, insomnia, headache and nausea
What antidepressants do you use for GAD?
Venlafaxine (effexor) blocks reuptake of 5-HT and NE
Duloxetine (cymbalta) Blocks reuptake 5HT and NE
Paroxetine (paxil) Blocks reuptake of 5HT
What other type of anxiety can you treat with benzos and why?
situational anxiety (because you will use them only for a small amount of time ie. in that particular situation)
What is the mechanism of action of benzos?
bind to site on GABAa receptor and enhances GABA Induced Cl conductance and opens the Cl channel more often thus inducing more inhibition
Chlordiazepoxide and Diazepam will go through 2 phases of metabolism, what will happen during the first phase?
they will form metabolites that will act the same as their parent compound thus acted as long lived pharmacologically active metabolites (i.e long lived benzoes)
What are the 2 benzos that form long-lived pharmacologically active metabolites?
DIAZEPAM (Valium) - t1/2 100 hours
CHLORDIAZEPOXIDE (Librium) - t1/2 100 hours
What are the three benzos that have short-lived active metabolites or no active metabolites?
ALPRAZOLAM (Xanax) – t1/2 = 14 hours; metabolized to a short-lived metabolite; most potent benzodiazepine
LORAZEPAM (Ativan) - t1/2 = 14 hours; also very potent; not metabolized
OXAZEPAM (Serax) - t1/2 = 9 hours; not metabolized
What is the most potent benzo?
alprazolam
Whats the deal with alcohol and benzos?
they exhibit cross dependence so you can use benzos to manage ethanol withdrawal
Which benzo do you want to use to treat alcohol withdrawal and why?
Diazepam if liver status hasnt been compromised cuz you want to just give it once and have it last a long time instead of having to keep administering it
Who are particularly sensitive to benzos and what can this cause?
elderly
confusional states in elderly
What are some symptoms of benzo use in elderly?
- dizziness and ataxia (dose-related)
- cognitive impairment
- anterograde amnesia (particularly with very short-acting)
- paradoxical reactions in some such as anxiety, and irritability/hostility
-when using clinically effective doses of long-acting benzo-diazepines – can lead to cumulative effects
What is the drug that you want to give to the elderly? why?
oxazepam (serax) because it has a short half life
Benzos and alcohol is a bad idea, why?
because depressants have additive effects
What is flunitrazepam (rohypnol)
it is the date rape drug and a really potent benzo
What can happen if you abruptly stop benzos?
you can get seizures as well as anxiety, agitation, irritability, insomnia (rebound effect on slow wave sleep and rem sleep), tremor and headache
Benzo withdrawal symptoms are more intense with (blank) acting benzodiazepines as well as with (blank) drugs. What are some examples of these?
short-acting
higher potency
Lorazepam and Alprazolam (have high receptor affinity)
What are therapeutic uses of benzos?
- anxiolytics (limited short term use)
- managing alcohol and barbituate withdrawal
- anticonvulsants (e.g lorazepam for status epilepticus
- preanesthetic adjuncts (midazolam)
- muscle relaxants (diazepam)
Why do you use zolpidem (ambien) instead of benzos for sedative-hypnotics?
because it only binds to BZ1 receptors because they have alpha 1 subunits and thus wont work as anxiolytics or cause cause cognitive impairments
What benzo works as a muscle relaxant?
Diazepam (valium)
What benzo works as a preanesthetic adjunct?
Midazolam (versed)
What benzo works as an anticonvulsant for status epilepticus?
Lorazepam (ativan)
What is a non-selective competitive antagonist of bz receptor (blocks action of benzos and BZ1 receptor agonists such as zolpidem)
It partialy or completely reverses most central effects (sedation; impairment of recall, etc)
-has no effect in the absence of benzos
Flumazenil (romazicon)
How do you give flumazenil (romazicon)?
IV only!
When do you use flumazenil (romazicon)?
Hasten recovery following use of these drugs in anesthetic and diagnostic procedures
and reverse the sedation of BZ receptor agonist overdose
What is the onset and half life like in flumazenil (romazicon)?
Why is this important?
Has a rapid onset of action (1-2 minutes; peak effect between
6 – 10 minutes) but a short half-life (0.7-1.3 hours)
If using this to treat benzo overdose you might accidently throw them into withdrawal!!!!
What are barbituates used for?
as general anesthetics (thiopental) and anticonvulsants (phenobarbital)
-killin people (i.e execution and final exit drugs)
What is the MOA of barbituates?
faciliatate GABAergic inhibitory neurotransmission at GABAa receptors BUT act a different site than benzos
Why are barbituates more potent than benzos?
THey act at a different site than benzo and increase the length of time the Cl- channel is open which increases the influx of Cl-
AND
reduce the glutamate-induced depolarization via AMPA and kainate receptors
AND
depress sensory cortex and decrease motor activity
What is this:
Sweating, trembling, palpitations, shortness of breath, choking
sensation, chest discomfort, nausea, dizziness, chills or hot flushes, fear of going crazy; individuals may confuse a panic attack with a heart attack.
Panic disorder
What do you use to treat panic disorder?
Antidepressants
and
Benzodiazepines
How do you treat panic disorder?
give benzos for short amount of time and give antidepressents and then ween off benzos once the antidepressant effect come into action
What are the SSRIs used in panic disorders?
- fluoxetine (prozac)
- Paroxetine (paxil)
- Sertraline (zoloft)
- Venlafaxine (effexor)
What are the benzos you use for panic disorder?
Alprazolam (xanax)
Lorazepam (ativan)
When do you use lorazepam (ativan) for panic disorders?
Use it IV to stop severe panic attack
How do you treat social anxiety disorder (social phobia)?
Venlafaxine (effexor)
Paroxetine (paxil)
How do you treat performance anxiety (stage fright)?
Propranolol (inderal) to prevent palpitations, tachycardia, tremors etc. (beta adrenergic receptor blocker)
How do you treat obsessive-compulsive disorder?
Fluoxetine (prozac)
Paroxetine (paxil)
Sertraline (zoloft)
How do you treat PTSD?
Paroxetine (paxil)
Sertraline (zoloft)
