Anxiolytic and Hypnotics Flashcards Preview

Neuro Quiz 2 > Anxiolytic and Hypnotics > Flashcards

Flashcards in Anxiolytic and Hypnotics Deck (48)
Loading flashcards...
1

Define sedative

Decreases activity
Moderates
Excitement
Calms
-Doesn't put you to sleep though

2

Define hypnotic

Produces drowsiness
Facilitates onset and maintenance of sleep that resembles natural sleep
Easily aroused sleep

3

GABA is

Major inhibitory NT

4

GABA(A)

Ligand operated
Permeable for Cl- which leads to hyperpolarization

5

GABA(B)

Metabotropic receptor
Inhibits adenylate cyclase, reduces NT release
Mostly in SPINE
Not helpful for anxiety

6

More Cl =

More inhibition = less anxiety

7

****Benzodiazepines MOA

Potentiate the action of GABA which increases the flux of chloride which makes more pronounced hyperpolarization and less excitable neurons
DOES NOT DIRECTLY ACTIVATE GABA(A) RECEPTOR

8

Flunitrazepam (BZ), pentobarbital and ethanol all

Cause sedation, CNS depression, anxiolysis and euphoria

9

GABA(A) has

different subunits

10

BZ are activators of which receptors

alpha 1/2/3/5 (not 4/6

11

Alpha 6 involved in

motor and balance coordination

12

Alpha 1 responsible for

Hypnotic/sedative
Anticonvulsant
Antergrade Amnesia

13

Alpha 2 responsible for

Anxiolysis

14

Pi pi stacking

Week form of bonding between groups when aligned parallel
Weak but multiple can be strong

15

Benzodiazepines are strictly :

allosteric modulators of the GABA(A) receptor
DO NOT directly open the receptor

16

What combination can be lethal?

Benzo and Alcohol

17

Antidote of Benzodiazepines

Flumazenil

18

Flumazenil MOA

Binds to GABA(A) receptor and competitively antagonizes BDZ

19

Overall Effects of BDZ

Reduction of anxiety and aggression
Sedation (little suppression of REM)
Anti-convulsant effect
Anterograde amnesia
Paradoxical effect (excitation)

20

PK of BDZ

Lipophilic
Liver
Active metabolites
No enzymes

21

Dizepam -->

Temazepam --> Oxazepam

22

Dexomoxepam -->

Diazepam

23

Prazepam -->

Diazepam

24

Short half life BZs

Triazolam
Oxazepam

25

Intermediate half life of BZ

Estazolam
Temazepam
Lorazepam
Alprazolam

26

Long half life of BZ

Flurazepam
Diazepam
Quazepam
Nitrazepam
Clonazepam

27

Rapid onset BZ

Triazolam
Estazolam
Flurazepam
Diazepam
Quazepam
Nitrazepam
Clonazepam

28

Slow onset BZ

Oxazepam
Temazepam

29

Intermediate onset of BZ

Lorazepam
Alprazolam

30

Overall side effects BZ

Daytime sedation
Reduction of reaction time
Ataxia, falls
COGNITIVE DEFICITS
Addictive!!!