Class #11 - Benzo

Question 1

Dopamine receptors that excite cAMP?

Answer 1

D1 (GPCR)

Question 2

Dopamine receptors that inhibits cAMP?

Answer 2

D2 (GPCR)

Question 3

Dx for schizo act on?

Answer 3

Inhibits D2

Question 4

First effective neuroleptic Dx?

Answer 4

Chlorpromazine

Question 5

Chlopramazine action?

Answer 5

Block D2 receptor

Question 6

New more selective D2 receptor inhibitors Dx name?

Answer 6

Trifluoperazine

Question 7

3 classes of antidepresants?

Answer 7

1. MAOI
2. TCA - block reuptake of amines in synaptic cleft
3. SSRI - Act on 5-HT receptors

Question 8

TCA side effects?

Answer 8

Vascular -> Block Adrenergic receptors; Sedation -> Block H-1 receptors (histamine); GI/Vision -> Block Muscarinic receptors

Question 9

First SSRI?

Answer 9

Fluoxetine (Prozac)

Question 10

How many types of 5-HT receptors?

Answer 10

15, found everywhere, mostly GCPR’s

Question 11

Fluoxetine inhibits on? and is a?

Answer 11

5-HT 3 receptors (Need two molecules of Serotonin to activate), ligand gated ion channel of Na+.

Question 12

Hierarchical vs diffuse connection

Answer 12

Diffuse in brain

Question 13

6 types of anxiety

Answer 13

1. Stress related
2. Generalize anxiety disorders
3. Panic attacks
4. Phobias
5. Secondary anxiety (Eg. Hyperthyroidism)
6. Drug induced

Question 14

Name of benzo comes from?

Answer 14

Benzene ring + 1,4-diazepine ring with 2 Nitrogen atoms

Question 15

5 major effect of Benzo

Answer 15

1. Antianxiety: Hippocampus/amygdala
2. Induce sleep: Cerebral cortex
3. Anticonvulsivant: Cerebellum/hippocampus
4. Musc. relaxation: Spinal cord/cerebellum/brainstem
5. Impairs memory formations (amnesia): Cerebral cortex/hippocampus

Question 16

Benzo lethal dose?

Answer 16

1000 times therapeutic dose

Question 17

Used before benzo for anxiety?

Answer 17

Phenobarbital - Barbiturates

Question 18

Used for stage fright?

Answer 18

b-Blockers

Question 19

Benzo act on which receptor?

Answer 19

GABA a receptors, let Cl- in cell.

Question 20

Most common type of GABA A?

Answer 20

1) 2 alpha1; 2 beta2; 1 gamma2

2) 2 aplha2; 2 beta2; 1gamma2

Question 21

First benzo? 2nd Benzo?

Answer 21

Librium/Chlordiazepoxide

Valium/diazepam

Question 22

Benzo bind where?

Answer 22

Junction between alpha and gamma subunits at an Allosteric site.

Question 23

GABA inhibits?

Answer 23

Serotonin, Acetylcholine, Adrenaline, Dopamine

Question 24

GABA a with subunits alpha 1/2/3 are where?

with alpha 4/5/6 are where? Plus positive modulators.

Answer 24

1. Subsynaptic/synaptic (Phasic inhibition) + Benzo

2. Extrasynaptic (Tonic inhibition) + Neurosteroids, EtOH, general anesthesia

Question 25

Benzo shift dose response curve top?

Answer 25

Left

Question 26

Barbiturate at high dose?

Answer 26

Open GABA a receptors on itself.

Question 27

Benzo vs Barbi in opening o receptors and selectivity

Answer 27

Benzo: Increase frequency and are selective to GABAa
Barbi: Increase duration and are not selective

Question 28

GABA a receptors with alpha 1 subunits =?

alpha 2 subunits =?

Answer 28

1=sedation

2=antianxiety

Question 29

Benzo antagonist=

Answer 29

Flumazenil

Question 30

Benzo inverse agonist=

Answer 30

B-Carboline act on allosteric site but impairs action of gaba = do opposite of benzo

Question 31

GABA b receptors are?

Answer 31

GCPR open K+ion

Question 32

Non-Benzo used for insomnia? binds where?

Answer 32

Zolpidem, bind to alpha 1 subunits on gaba a.