Brainscape's Knowledge GenomeTM

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


See full index

Pharmacology and Therapeutics 2 Y2 > Anxiolytics, Sedatives and Hypnotics > Flashcards

Anxiolytics, Sedatives and Hypnotics Flashcards

1
Q

GABA is the bodies main …

A

Inhibitory NT

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

GABA neurons as a rule are … (axon length and type of neurone)

A

short-axoned interneurons

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

What is GABA synthesised from

A

Glutamate

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

What enzyme acts on glutamate to form GABA

A

glutamate decarboxylase enzyme, GAD

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

What is needed for GABA synthesis

A

Glutamate, GAD, vitB6

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

What is needed for proper functioning of GAD

A

Vit B6

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

What type of receptor are GABA receptors

A

Chloride ionophores, type 1

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
8
Q

What does GABA receptor stimulation cause

A

Chloride influx and hyperpolarisation

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
9
Q

What is GABA metabolised into

A

SSA - succinic semialdehyde

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

What metabolises GABA

A

GABA-T

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
11
Q

What is GABA reuptaken by

A

Glial cells and presynaptic terminal

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

What downregulates GABA release

A

GABAb autoreceptors on presynaptic terminals, downregulate GABA release by negative feedback

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
13
Q

What type of receptors are GABAb autoreceptors

A

Type 2 G protein coupled

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
14
Q

What metabolises SSA succinic semialdehyde

A

SUCCINIC SEMIALDEHYDE DEHYDROGENASE (SSDH)

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

What is the product of SSA succinic semialdehyde metabolism

A

Succinic acid

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

Succinic acid is the metabolic product of what?

A

succinic semialdehyde metabolism by SSADH

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
17
Q

Succinic semialdelhyde is the metabolic product of what?

A

GABA by GABA T

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
18
Q

Where are GABAT and SSADH enzymes found

A

Mitochondria

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
19
Q

What is the use of succinic acid

A

Used in TCA cycle

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
20
Q

Sodium valproate actions?

A

GABAT and SSADH inhibitor

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
21
Q

Sodium valproate is an example of what type of drug?

A

Anticonvulsant

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
22
Q

Vigabatrin actions?

A

Covalent GABAT inhibitor

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
23
Q

Vigabatrin is an example of what type of drug?

A

Anticonvulsant

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
24
Q

4 components of the GABAa receptor complex?

A
  1. GABA receptor protein
  2. Benzodiazepine receptor protein
  3. Barbiturate receptor protein
  4. Chloride channel protein
How well did you know this?
1
Not at all
2
3
4
5
Perfectly
25
Q

What modulates linkage of the GRP with the benzodiazepine RP

A

GABA modulin

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
26
Q

What happens when GABA binds to the GABARP (3)

A

linkage of the GRP with the benzodiazepine RP, mediated by GABA modulin

  • This opens the chloride channel protein, allowing chloride ions to enter the cell and cause hyperpolarization
  • Also enhances the binding of BDZ to BDZRP
How well did you know this?
1
Not at all
2
3
4
5
Perfectly
27
Q

What happens when a benzodiazepine binds to the BDZRP (1)

A
  • This enhances the action of GABA on the chloride ion channel and enhances the affinity of GABA binding to GRP
28
Q

What happens if we bind a barbiturate to a BRP (normal and high doses) (2+1)

A
  • We get enhancement of GABA action of the chloride channel
  • We also get enhanced affinity of GABA binding to the GABARP
  • At high doses, we can get a direct effect of the drug on the chloride channel
29
Q

What is bicuculline

A

competitive GABAA receptor antagonist

30
Q

What is - FLUMAZENIL

A

competitive benzodiazepine antagonist

31
Q

Example of a competitive benzodiazepine antagonist

A

FLUMAZENIL

32
Q

Example of a competitive GABAA receptor antagonist

A

bicuculline

33
Q

Explain the allosteric effects of BDZ and barbiturates, what dose is this

A

Therapeutic doses, neither drug have any activity. They enhance GABAs action

34
Q

BARB/BDZ - which has Cl channel activity at a high dose?

A

BARB

35
Q

How do BDZ potentiate GABA exactly

A

Increase frequency of the opening of the Cl channels

36
Q

How do BARBs potentiate GABA exactly

A

Increase duration of the opening of the Cl channels

37
Q

What drug family Increases duration of the opening of the Cl channels

A

BARB

38
Q

What drug family Increases frequency of the opening of the Cl channels

A

BDZ

39
Q

Which is more selective, BDZ or BARB, what does this mean X drug can also be used for

A

BDZ, so BARBs can also be used for surgical anaesthesia

40
Q

Margin of safety of BARBs? Why

A

Low selectivity leading to low margin of error

41
Q

Clinical uses of BARBs? (4)

A

Anaesthetics
Anxiolytics
Sedatives/hypnotics

42
Q

Clinical uses of BDZ (3)

A

Anti-spastics
Anxiolytics
Sedatives/hypnotics

43
Q

Definition of anxiolytic?

A

REMOVE ANXIETY WITHOUT IMPAIRING MENTAL OR PHYSICAL ACTIVITY (‘MINOR TRANQUILLISERS’)

44
Q

Definition of sedative?

A

REDUCE MENTAL AND PHYSICAL ACITVITY WITHOUT PRODUCING LOSS OF CONSCIOUSNESS

45
Q

Definition of hypnotic?

A

INDUCE SLEEp

46
Q

Ideal criteria for anxiolytics/sedatives/hypnotics? (6)

A
  • Have a wide margin of safety
  • Not depress respiration
  • Produce natural sleep (hypnotics)
  • Not interact with other drugs
  • Not produce ‘hangovers’
  • Not produce dependence
47
Q

Example of a barbiturate?

A

Amobarbital

48
Q

Amobarbital is an example of?

A

BARB

49
Q

Unwanted effects of BARBs? (6)

A
  • Low safety margins Depress respiration, O.D.s can be lethal
  • Alter natural sleep (decrease REM) Hangovers/irritability
  • Enzyme inducers (if co-administered with other drugs that are metabolized with same drug, they’ll effect the metabolism of the other drug)
  • Potentiate effect of other CNS depressants (e.g. alcohol)
  • Tolerance
  • Dependence Withdrawal syndrome (insomnia, anxiety, tremor, convulsions, death)§
50
Q

Admin of BDZ?

A

Oral/IV

51
Q

Lipid solubility of BDZ?

A

HIgh

52
Q

Plasma protein binding of BDZ?

A

High

53
Q

What metabolises BDZ?

A

Liver microsomal enzymes

54
Q

How are BDZ excreted?

A

In urine as glucoronide conjugates

55
Q

Duration of action of BDZ?

A

Varied

56
Q

how is a longer duration of action achieved by BDZ?

A

Active metabolites or a slower metabolism of it

57
Q

T1/2 life of diazepam

A

32 hours

58
Q

T1/2 life of temazepam

A

8h

59
Q

T1/2 life of oxazepam

A

8h

60
Q

Examples of a common anxiolytic Benzo?

A

diazepam (valium)

61
Q

What are long lasting benzos used for

A

anxiolytics

62
Q

What are short lasting benzos used for

A

sedatives/hypnotics

63
Q

Advantages of using BDZ? (3)

A
  • Wide margin of safety:
     O.D. leads to prolonged sleep (this sleep is rousable)
     O.D. can be treated with I.V. FLUMAZENIL (competitive antagonist)
  • Only have a mild effect on REM sleep
  • Do not induce liver enzymes
64
Q

Side effects of benzos? (5)

A
  • Sedation, confusion, amnesia, ataxia (impaired manual skills)
  • Potentiate other CNS depressants (e.g. alcohol, BARBs)
  • Tolerance (less than BARBs – BZs only show ‘tissue’ tolerance)
  • Dependence:
     Withdrawal syndrome similar to BARBs but less intense
     Withdraw them slowly
  • Free plasma concentration of BZs is increased by aspirin, heparin etc.
65
Q

Other than BARB and BDZ, what can you use as a sedative/hypnotic

A

Zopiclone

66
Q

Use of zopiclone

A

sedative/hypnotic

67
Q

Other than BARB and BDZ, what other classes of drugs can you use as anxiolytics

A 
Antidepressants
Antiepileptics
Antipsychotics
Propranolol beta blocker
Buspirone

Pharmacology and Therapeutics 2 Y2 (24 decks)

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