Anxiolytics [3] Flashcards Preview

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Flashcards in Anxiolytics [3] Deck (26):
1

NTs involved in anxiety
(Neuropharmacological targets)

5HT
GABA

2

1st line agent for most anxiety disorders

Antidepressants (SSRI-SNRIs) → increase 5HT

3

Benzodiazepine agonist action and when it is good to use for anxiety

Indirectly Augment GABA Cl- Channels
- good in acute and situational anxiety
- INTENSIFY effect of GABA

- Non-linear, less steep CNS effects (greater dose req. to reach CNS depressant)

4

Barbiturate action and when it is good to use for anxiety

Indirectly Augment GABA Cl- Channels
- rarely used for anxiety
- PROLONG effect of GABA
- less selective
- depresses excitatory NT (Glu)
- IV barb maintain surgical anesthesia ( stage III)

- LINEAR CNS effects

- very easy to overdose and abuse

5

BDZ vs Barbs
Which has greater margin of safety?
Which has higher therapeutic index?
Which one prolongs effect of GABA?
Binds to gamma subunit of GABA R Ion channel?

BDZ (greater dose to achieve CNS depression)
BDZ
Barbs - prolongs in presence of GABA and opens channels directly at higher doses
BDZ

6

BDZ vs General Anesthetics (GA)
- maintain stage III surgical anesthesia
- potentiate GABAa receptor activity
- Low margin of safety
- Low potency
- Inhibition of Excitatory synaptic transmission

GA
Both
GA
GA
GA

7

Non BDZ

"Z drugs"
Eszopiclone
Zaleplon
Zolpidem

- binds only to GABA Cl- channels with a1
- makes you sleepy (w/o anxiolytics)
- reduced potential for dependence

(if you want to relieve anxiety, bind a2-5 - BDZ binds a1, a2-5)

8

BDZ alone are safe, but combined with what is lethal?

Ethanol (can open GABA Cl- channel directly at a nonspecific site)
BDZ open indirectly

Can result in coma (additive effect of CNS depressant)

9

Admin of flumazenil will reverse the toxicities associated with overdose of____

BDZs
(BDZ R antagonist)
- reverses CNS depression

10

What reverses toxicity of morphine?

naloxone blocks binding

11

a1 GABA receptor Cl- channel subunit
- agonist
- location
- action
- side effects

BDZ + Z drugs

Cortex

Sleep, Anticonvulsants
(no anti-anxiety)

Amnesia, Additive CNS depression

12

a2-5 GABA receptor Cl- channel subunit
- agonist
- location
- action
- side effects

BDZ

Limbic system, brain stem

Anxiolytics, myorelaxants
- can treat anxiety, convulsions at dose where pt is still awake

Tolerance, Dependence, Addiction

13

BDZ low dose

Anxiolytics (a2-a5)

14

BDZ high dose

anticonvulsant effects

(a1- higher barbs and BDZ inhibit seizure activity in cortical neurons)

Myorelaxants
- BDZ inhibit spinal cord reflexes
- usually accompanied with sig CNS depression

Sleep

15

Drug of choice for status epilepticus

diazepam

16

which is used for anesthesia induction?
- Barbs or BDZ?

Barbituates: anesthesia induction (phenobarbitol)

BDZ NOT capable of induction (used as adjuncts)

17

dependence of BDZ

psychologic dep
physical dep (chronic use)
withdrawal syndrome

- Most common adverse rxns are extension of CNS depression

18

BDZ ready to be conjugated +inactivated in 1 step

Oxazepam
Lorazepam
Temazepam

conjugation enzymes dont diminish with age
- dont worry about slow metabolism in old people
- can reliably eliminate it with age

(look for O or L)

19

BDZ eliminated by CYP450

Diazepam
- most BDZ
- phase I with subsequent inactivation via conjugation by glucuronidation (phase II)

20

Anterograde Amnesia is common in drugs that

enhance GABA neuronal fxn
(→ indirectly depressing glutamate fxn)
- ie: BDZ

Beneficial use in uncomfortable procedure as pt is able to cooperate w/o any memory afterward
eg: colonscopy

21

Midazolam (versed)

BDZ

antianxiety - act by potentiating GABAa receptors

22

Alprazolam
Lorazepam
Diazepam
___________
Buspirone

Anti -anxiety
BDZs


(Buspirone is a partial 5HT1A partial agonist)

23

Do BDZ result in retrograde or anterograde amnesia?

Anterograde amnesia
- enhance GABA neuronal fxn
(→ indirectly depressing glutamate fxn)

24

Do BDZ or SSRIs work better in anxiety?

SSRI
- BDZ can be used as an adjunct for acute management while SSRI take effect

25

Difference btwn treating anxiety disorders in:
acute panic attack
Mild-moderate symptoms
Severe symptoms

acute: BDZ
mild-mod: SSRI (antidepressant OR CBT)
Severe: SSRI AND CBT

26

Schedules of Barbs vs BDZ

Barbs: sched II
- lower therapeutic index
- higher abuse potential than BDZ
- more likely to result in death by resp. depression
- classic inducers of cytP450
BDZ: sched IV
- hgher a