Brainscape's Knowledge GenomeTM

Browse over 1 million classes created by top students, professors, publishers, and experts.


See full index

notes to flashcards year 2 - LCRS1 > anxiolytics, sedatives, hypnotics > Flashcards

anxiolytics, sedatives, hypnotics Flashcards

1
Q

how is GABA formed?

A

glutamate –> GABA via glutamate decarboxylase (GAD)

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
2
Q

what can GABA bind to?

A
  • GABAaR on postsynaptic cell –> hyperpolarize cell

- GABAbR on presynaptic cell —> -ve inhibtion of release

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
3
Q

what can GABA be re-uptaken by?

A
  • glial cells: GABA transaminase breaks down GABA into SSA

- pre-synaptic cell: GABA-T breaks down GABA into SSA

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
4
Q

describe GABA metabolism

A
  • GABA –> SSA by GABA-T

- SSA –> succinic acid by SSDH

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
5
Q

where are these enzymes found?

A
  • GAD: cytosol

- GABA-T and SSDH: found in mitochondrial membrane

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
6
Q

what do inhibitors of GABA metabolism lead to?

A
  • more GABA and more inhibition in brain

e. g. sodium valproate, vigabatrin

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
7
Q

What is GABAaR made up of?

A

4 main proteins:

  • GABA-R protein
  • GABA modulin
  • Barbiturate receptor protein
  • benzodiazepine receptor protein
How well did you know this?
1
Not at all
2
3
4
5
Perfectly
8
Q

what are bicuculline and flumazenil?

A

competitive antagonist

  • bicucline (GABA)
  • flumazenil (BDZ)
How well did you know this?
1
Not at all
2
3
4
5
Perfectly
9
Q

what do BDZ and barb need?

A

require GABA to function

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
10
Q

what are the 6 MoA of GABAa-receptor? which ones use each?

A
  1. linkage of GABA-RP, GABA, M, BDZ-RP and opening of Cl- channel (GABA)
  2. initiation of pathway 1 (BDZ)
  3. inc. affinity of binding of GABA/BDZ - reversible (GABA, BDZ)
  4. linkage of Barb-RP and BDZ-RP and opening of Cl- channels
  5. inc. affinity of binding of GABA (Barb)
  6. direct activation of Cl- channel (GABA, Barb)
How well did you know this?
1
Not at all
2
3
4
5
Perfectly
11
Q

what do Barbs and BZDs do to the GABAaR?

A
  • barbs inc. frequency of opening

- BZDs inc. duration of opening

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
12
Q

which is less selective? what does that mean?

A
  • barbs are less selective than BDZs
  • so barbs have less excitatory transmission
  • Barbs are more dangerous = small therapeutic window
How well did you know this?
1
Not at all
2
3
4
5
Perfectly
13
Q

what are the clinical uses of BDZs and Barbs?

A
  • anaesthetics: Barbs only
  • Anticonvulsants: diazepam, clonazepam, phenobarbital
  • anti-spastics: diazepam
  • anxiolytics (long acting): BDSz only, diazepam, oxazepam
  • sedatives/hypnotics (short acting): Barbs and BDZ, oxazepam, amobarbital
How well did you know this?
1
Not at all
2
3
4
5
Perfectly
14
Q

when is oxazepam used?

A

if pt has a hepatic impairment

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
15
Q

define anxiolytics

A

remove anxiety without impairing mental or physical activity

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
16
Q

define sedative

A

reduce mental and physical activity without producing a loss of consciousness

17
Q

define hypnotic

A

induce sleep

18
Q

ideally what should these drugs do?

A
  • large therapeutic window
  • not depress resp
  • produce natural sleep
  • not interact with other drugs
  • not produce hangovers
  • not produce dependence
19
Q

what do the drug names of barbiturates end in?

A
  • tone
  • tal
  • tol
20
Q

describe the structure of barbiturates

A
  • single ring structure with 2 R-groups
  • R groups are -ethyl groups and phenyl/1-methylbutyl
  • drugs have sedative/hypnoticeffet
21
Q

name a barbiturate

A

amobarbital

22
Q

why aren’t these drugs first line?

A
  • small therapeutic window (depress resp)
  • reduce REM sleep = hangovers
  • induce enzymes
  • potentiate effects of other CNS depressants (alcohol)
  • tolerance and dependence issues
23
Q

describe the structure of benzodiazepines

A

triple ring structure

24
Q

what do benzodiazepine drug names end in?

A
  • epam

- epate

25
Q

what do benzodiazepines act on?

A

all GABAa receptors

not GABAb

26
Q

describe the pharmacokinetics of benzodiazepines

A
  • oral/IV admin
  • peak plasma conc at 1 hour
  • extensive liver metabolism
  • excretion in urine (glucuronide conjugates)
27
Q

what are the long and short acting?

A
  • diazepam long acting = 32hr half life

- temazepam (8 hrs) and oxazepam (8 hrs) = short acting

28
Q

what are the advantages of BDZs?

A
  • wide therapeutic window
  • overdose = prolonged sleep
  • flumazenil is BDZ anatgonist so can reverse effect
  • mild effect on REM sleep
  • does not induce liver enzymes
29
Q

what are the unwanted effects of BDZs?

A
  • sedation, confusion, amnesia, ataxia (impaired manual skills)
  • potentiates other CNS depressants
  • tolerance and dependence
30
Q

with which drugs does the free plasma conc. inc. with?

A

aspirin

heparin

31
Q

what is zopiclone?

A
  • sedative/hynotic
  • Z-drug
  • short acting
  • acts on BDZ receptor
  • not BDZs
  • minimal hangover effects but dependency problems
32
Q

what are other anxiolytics?

A
  • antidepressants (SSRIs)
  • anti-epilpetics (valproate)
  • antipsychotic’s (olanzapine)
  • propanolol (improves physical symptoms of anxiety)
  • buspirone (5HT1a receptor agonist with fewer side effects)

notes to flashcards year 2 - LCRS1 (58 decks)

Brainscape helps you reach your goals faster, through stronger study habits.
© 2024 Bold Learning Solutions. Terms and Conditions