Transmitters and Receptors Flashcards Preview

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Flashcards in Transmitters and Receptors Deck (32):
1

5 places that CNS drugs can act on

1. Synthesis
2. Storage
3. Release
4. Inactivation: Re-uptake/Metabolism
5. Receptor

2

Problems with drug in the CNS re: mechanisms:

molecular mechanisms known
therapeutic mechanism not always known.

3

SSRI, Cocaine and Anti-AChE affect what?

reuptake of NTs

4

Cocaine and amphetamines affect NA but also:

dopaminergic
serotonergic

5

Which drug in epilepsy limits excitatory nerve activation?

phenytoin: binds to OPEN sodium channel, decrease Glutamate action

6

What drug enhances inhibitory input for epilepsy?

benzodiazepines enhance GABA receptor activity

7

Two NTs implicated for sedation/anxiety?

GABA
Serotonin

8

3 NTs implicated for anxiety?

serotonin
NA
Neuropeptide Y

9

NT implicated for Sedation in children

Histamine

10

Benzodiazepines used in treating what 5 main things:

epilepsy
anxiety
sleep disorders
premedication
acute alcohol withdrawal

11

Beta-adrenoceptor antagonists do what for anxiety?

block physical signs
nothing for CNS though

12

4 clinically recognized anxiety disorders?

general anxiety
panic disorder
phobia
PTSD

13

Barbiturates, hypnotic/anxiolytics used much today?

pretty much obsolete

14

What is Zolpidem?

direct non-benzodiazepine GABA agonist at orthosteric site

15

What do barbiturates do? why bad?

General depressants
toxic: narrow therapeutic window
induce liver enzymes
abrupt withdrawal = death
addictive

16

2 situations where you anxiolytics/hypnotics are still used?

anaesthetic
anticonvulsant

17

Why choose benzodiazepines over barbiturates?

wider therapeutic index
less cardioresp depression
less addictive
'safer' in overdose

18

benzodiazepines interact with GABA A or GABA B receptors?

GABA A receptor only

19

three ways benzodiazepines interact with GABA A receptor?

1. modulate orthosteric ligand affinity
2. modulate orthosteric ligand efficacy
3. modulate receptor activation level

20

benzodiazepines modulate at which site?

allosteric modulators

21

diazepam a benzodiazepines does what to the GABA A receptor?

1. increase frequency of Cl- channel opening
2. increase sensitivity with no change to maximal response

22

difference between benzodiazepines and barbituates in terms of receptor channel? how does this affect overdose?

1. benzodiazepines: open and close/frequency: hits ceiling, safer
2. barbituates: keeps the channel open, can overdose easily

23

why are allosteric modulators better?3 big ones:

1. increase therapeutic window
2. positive modulation of ENDOGENOUS agonist, not exogenous
3. more receptor subtype selectivity

24

unwanted side effects of benzodiazepines?

drowsiness
confusion
impaired coordination

25

disadvantages of benzodiazepines?

interact with alcohol,
antihistamines/barbituates
withdrawal,
dependence

26

Can you take the same dose of benzodiazepines always?

develop tolerance: need to increase dose

27

How long is short vs. long acting benzodiazepines?

short: 6-12 hours
Long: >24 hours

28

Does low potency matter?

only if awkward to administer, low potency does not = inferior drugs

29

what is pharmacological efficacy?

strength of receptor activation: full vs. partial agonist

30

what is clinical efficacy?

strength of beneficial effect

31

benzodiazepines vs. barbituates: 3 big points in terms of efficacy/potency

1. both affect GABA receptors
2. Benzo: increase channel frequency (increase potency)
3. barbituates increase duration of Cl- channel opening (increase efficacy)

32

What is Buspirone? where does it act?

non benzo anxiolytic: partial agonist at 5HT1 receptors