Pharm tx of anxiety- Craviso Flashcards

1
Q

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?

A

6 months

Noradrenergic, serotonergic, Gabaergic (benzoes)

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2
Q

Which do you use more often for GAD, benzos or antidepressants?
Why?

A

antidepressants

-better efficacy for anxiety and for comorid disorders (i.e depression)

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3
Q

Do non benzos and antidepressants have their effects occur immediately or does it take several weeks?
How do you remedy this?

A

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

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4
Q

What is buspirone (buspar)?
What is it used for?
Is it for long or short term tx and are the effects immediate?

A

Partial agonist at 5HT1A receptor

  • GAD and alcoholisms
  • long term tx
  • effects take several weeks
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5
Q

What are the adverse SEs of Buspirone?

A

dizziness, light-headedness, insomnia, headache and nausea

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6
Q

What antidepressants do you use for GAD?

A

Venlafaxine (effexor) blocks reuptake of 5-HT and NE
Duloxetine (cymbalta) Blocks reuptake 5HT and NE
Paroxetine (paxil) Blocks reuptake of 5HT

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7
Q

What other type of anxiety can you treat with benzos and why?

A

situational anxiety (because you will use them only for a small amount of time ie. in that particular situation)

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8
Q

What is the mechanism of action of benzos?

A

bind to site on GABAa receptor and enhances GABA Induced Cl conductance and opens the Cl channel more often thus inducing more inhibition

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9
Q

Chlordiazepoxide and Diazepam will go through 2 phases of metabolism, what will happen during the first phase?

A

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)

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10
Q

What are the 2 benzos that form long-lived pharmacologically active metabolites?

A

DIAZEPAM (Valium) - t1/2  100 hours

CHLORDIAZEPOXIDE (Librium) - t1/2  100 hours

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11
Q

What are the three benzos that have short-lived active metabolites or no active metabolites?

A

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

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12
Q

What is the most potent benzo?

A

alprazolam

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13
Q

Whats the deal with alcohol and benzos?

A

they exhibit cross dependence so you can use benzos to manage ethanol withdrawal

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14
Q

Which benzo do you want to use to treat alcohol withdrawal and why?

A

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

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15
Q

Who are particularly sensitive to benzos and what can this cause?

A

elderly

confusional states in elderly

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16
Q

What are some symptoms of benzo use in elderly?

A
  • 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

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17
Q

What is the drug that you want to give to the elderly? why?

A

oxazepam (serax) because it has a short half life

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18
Q

Benzos and alcohol is a bad idea, why?

A

because depressants have additive effects

19
Q

What is flunitrazepam (rohypnol)

A

it is the date rape drug and a really potent benzo

20
Q

What can happen if you abruptly stop benzos?

A

you can get seizures as well as anxiety, agitation, irritability, insomnia (rebound effect on slow wave sleep and rem sleep), tremor and headache

21
Q

Benzo withdrawal symptoms are more intense with (blank) acting benzodiazepines as well as with (blank) drugs. What are some examples of these?

A

short-acting
higher potency

Lorazepam and Alprazolam (have high receptor affinity)

22
Q

What are therapeutic uses of benzos?

A
  • anxiolytics (limited short term use)
  • managing alcohol and barbituate withdrawal
  • anticonvulsants (e.g lorazepam for status epilepticus
  • preanesthetic adjuncts (midazolam)
  • muscle relaxants (diazepam)
23
Q

Why do you use zolpidem (ambien) instead of benzos for sedative-hypnotics?

A

because it only binds to BZ1 receptors because they have alpha 1 subunits and thus wont work as anxiolytics or cause cause cognitive impairments

24
Q

What benzo works as a muscle relaxant?

A

Diazepam (valium)

25
Q

What benzo works as a preanesthetic adjunct?

A

Midazolam (versed)

26
Q

What benzo works as an anticonvulsant for status epilepticus?

A

Lorazepam (ativan)

27
Q

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

A

Flumazenil (romazicon)

28
Q

How do you give flumazenil (romazicon)?

A

IV only!

29
Q

When do you use flumazenil (romazicon)?

A

Hasten recovery following use of these drugs in anesthetic and diagnostic procedures
and reverse the sedation of BZ receptor agonist overdose

30
Q

What is the onset and half life like in flumazenil (romazicon)?
Why is this important?

A

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!!!!

31
Q

What are barbituates used for?

A

as general anesthetics (thiopental) and anticonvulsants (phenobarbital)
-killin people (i.e execution and final exit drugs)

32
Q

What is the MOA of barbituates?

A

faciliatate GABAergic inhibitory neurotransmission at GABAa receptors BUT act a different site than benzos

33
Q

Why are barbituates more potent than benzos?

A

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

34
Q

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.

A

Panic disorder

35
Q

What do you use to treat panic disorder?

A

Antidepressants
and
Benzodiazepines

36
Q

How do you treat panic disorder?

A

give benzos for short amount of time and give antidepressents and then ween off benzos once the antidepressant effect come into action

37
Q

What are the SSRIs used in panic disorders?

A
  • fluoxetine (prozac)
  • Paroxetine (paxil)
  • Sertraline (zoloft)
  • Venlafaxine (effexor)
38
Q

What are the benzos you use for panic disorder?

A

Alprazolam (xanax)

Lorazepam (ativan)

39
Q

When do you use lorazepam (ativan) for panic disorders?

A

Use it IV to stop severe panic attack

40
Q

How do you treat social anxiety disorder (social phobia)?

A

Venlafaxine (effexor)

Paroxetine (paxil)

41
Q

How do you treat performance anxiety (stage fright)?

A

Propranolol (inderal) to prevent palpitations, tachycardia, tremors etc. (beta adrenergic receptor blocker)

42
Q

How do you treat obsessive-compulsive disorder?

A

Fluoxetine (prozac)
Paroxetine (paxil)
Sertraline (zoloft)

43
Q

How do you treat PTSD?

A

Paroxetine (paxil)

Sertraline (zoloft)