Sedative Hypnotics and Anxiolytics Flashcards Preview

Pharmacology Test #6 > Sedative Hypnotics and Anxiolytics > Flashcards

Flashcards in Sedative Hypnotics and Anxiolytics Deck (64)
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1

Stress versus anxiety

stress is something that happens to you and anxiety is a reaction to stress that the brain produces

2

Amygdala

part of the limbic system; ancient, primitive structure; conditioned fear in rodents; anxiety in humans

3

Anxiety disorders

GAD; phobias; OCD; eating disorders; panic attacks; mixed anxiety-depression; PTSC

4

Sedation

reduced responsiveness, calming effect

5

hypnosis

drug-induced sleep

6

Anesthesia

drug-induced amnesia, analgesia, unconsciousness, lsot muscle tone

7

Coma

unconsciousness for 6+ hours, no sleep cycles, non-responsive to pain, light/sound

8

Major inhibitor neurotransmitter in the CNS

GABA

9

What is GABA produced from

glutamate

10

GABA activates

GABAA type ligand gated Cl- channels, and GABAB and GABAC receptors which are GPCRs

11

Most sedative/hypnotics act at which receptors

act at the GABA-A receptor complex (ligand-gated chloride channel) through via different pharmacological mechanisms

12

How many GABA molecules are required to bind and activate a GABA-A receptor?

2 GABA molecules

13

Cl- influx through the GABA receptor does what to the cell membrane?

hyperpolarizes the cell membrane

14

Where do benzodiazepines bind?

at a site distinct from the GABA binding site

15

What does binding of a BZD molecule enhance?

enhances the activity of GABA in activating the receptor, but binding of BZD has no activity on its own

16

What type of binding does BZDs exhibit?

allosteric

17

How does the addition of a BZD or barbiturate when GABA is present enhance the action of GABA?

BZD largely increases the frequency of channel openings whereas barbiturates increase the duration of openings

18

What do molecules with inverse agonist action at the BZD site do when they bind to the BZD site?

they make it harder for GABA to open the channel (negative allosteric modulation), which is the opposite of what BZDs do

19

What is a GABA(A) receptor agonist

an agonist at the GABA binding site

20

What does a BZD site agonist do?

facilitates the action of GABA

21

What does a BZD site antagonist do?

antagonizes the action of BZD agonists without antagonizing the action of barbiturates

22

What is a BZD site inverse agonist

negative allosteric modulator of GABAAR function

23

Benzodiazepines

1. Alprazolam
2. Flurazepam
3. Midozolam
4. Flumazenil

24

How do benzodiazepines work?

potentiate GABA throughout the CNS

25

Metabolism of benzodiazepines

extensively metabolized with many active metabolites

26

What are benzodiazepines potentiated by?

potentiated by other CNS depressants as well as alcohol

27

What is the potential risk associated with benzodiazepines?

significant potential for psychological and physical dependence - people can become addicted to drugs such as Xanax and sleep pills

28

Clinical use of Midazolam

for acute seizure control, pre-surgery anxiolysis, amnesia and sedation;
rapid onset, fast recovery

29

Clinical use of Alprazolam

mainly for panic, GAD;
rapid acting, moderate duration

30

Clinical use of Flurazepam

long duration, next-day sedation is possible;
for insomnia and those who need help maintaining sleep