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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

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2
Q

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

A

short-axoned interneurons

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3
Q

What is GABA synthesised from

A

Glutamate

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4
Q

What enzyme acts on glutamate to form GABA

A

glutamate decarboxylase enzyme, GAD

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5
Q

What is needed for GABA synthesis

A

Glutamate, GAD, vitB6

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6
Q

What is needed for proper functioning of GAD

A

Vit B6

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7
Q

What type of receptor are GABA receptors

A

Chloride ionophores, type 1

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8
Q

What does GABA receptor stimulation cause

A

Chloride influx and hyperpolarisation

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9
Q

What is GABA metabolised into

A

SSA - succinic semialdehyde

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10
Q

What metabolises GABA

A

GABA-T

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11
Q

What is GABA reuptaken by

A

Glial cells and presynaptic terminal

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12
Q

What downregulates GABA release

A

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

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13
Q

What type of receptors are GABAb autoreceptors

A

Type 2 G protein coupled

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14
Q

What metabolises SSA succinic semialdehyde

A

SUCCINIC SEMIALDEHYDE DEHYDROGENASE (SSDH)

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15
Q

What is the product of SSA succinic semialdehyde metabolism

A

Succinic acid

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16
Q

Succinic acid is the metabolic product of what?

A

succinic semialdehyde metabolism by SSADH

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17
Q

Succinic semialdelhyde is the metabolic product of what?

A

GABA by GABA T

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18
Q

Where are GABAT and SSADH enzymes found

A

Mitochondria

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19
Q

What is the use of succinic acid

A

Used in TCA cycle

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20
Q

Sodium valproate actions?

A

GABAT and SSADH inhibitor

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21
Q

Sodium valproate is an example of what type of drug?

A

Anticonvulsant

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22
Q

Vigabatrin actions?

A

Covalent GABAT inhibitor

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23
Q

Vigabatrin is an example of what type of drug?

A

Anticonvulsant

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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
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25
What modulates linkage of the GRP with the benzodiazepine RP
GABA modulin
26
What happens when GABA binds to the GABARP (3)
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
27
What happens when a benzodiazepine binds to the BDZRP (1)
- This enhances the action of GABA on the chloride ion channel and enhances the affinity of GABA binding to GRP
28
What happens if we bind a barbiturate to a BRP (normal and high doses) (2+1)
- 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
What is bicuculline
competitive GABAA receptor antagonist
30
What is - FLUMAZENIL
competitive benzodiazepine antagonist
31
Example of a competitive benzodiazepine antagonist
FLUMAZENIL
32
Example of a competitive GABAA receptor antagonist
bicuculline
33
Explain the allosteric effects of BDZ and barbiturates, what dose is this
Therapeutic doses, neither drug have any activity. They enhance GABAs action
34
BARB/BDZ - which has Cl channel activity at a high dose?
BARB
35
How do BDZ potentiate GABA exactly
Increase frequency of the opening of the Cl channels
36
How do BARBs potentiate GABA exactly
Increase duration of the opening of the Cl channels
37
What drug family Increases duration of the opening of the Cl channels
BARB
38
What drug family Increases frequency of the opening of the Cl channels
BDZ
39
Which is more selective, BDZ or BARB, what does this mean X drug can also be used for
BDZ, so BARBs can also be used for surgical anaesthesia
40
Margin of safety of BARBs? Why
Low selectivity leading to low margin of error
41
Clinical uses of BARBs? (4)
Anaesthetics Anxiolytics Sedatives/hypnotics
42
Clinical uses of BDZ (3)
Anti-spastics Anxiolytics Sedatives/hypnotics
43
Definition of anxiolytic?
REMOVE ANXIETY WITHOUT IMPAIRING MENTAL OR PHYSICAL ACTIVITY (‘MINOR TRANQUILLISERS’)
44
Definition of sedative?
REDUCE MENTAL AND PHYSICAL ACITVITY WITHOUT PRODUCING LOSS OF CONSCIOUSNESS
45
Definition of hypnotic?
INDUCE SLEEp
46
Ideal criteria for anxiolytics/sedatives/hypnotics? (6)
- 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
Example of a barbiturate?
Amobarbital
48
Amobarbital is an example of?
BARB
49
Unwanted effects of BARBs? (6)
- 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
Admin of BDZ?
Oral/IV
51
Lipid solubility of BDZ?
HIgh
52
Plasma protein binding of BDZ?
High
53
What metabolises BDZ?
Liver microsomal enzymes
54
How are BDZ excreted?
In urine as glucoronide conjugates
55
Duration of action of BDZ?
Varied
56
how is a longer duration of action achieved by BDZ?
Active metabolites or a slower metabolism of it
57
T1/2 life of diazepam
32 hours
58
T1/2 life of temazepam
8h
59
T1/2 life of oxazepam
8h
60
Examples of a common anxiolytic Benzo?
diazepam (valium)
61
What are long lasting benzos used for
anxiolytics
62
What are short lasting benzos used for
sedatives/hypnotics
63
Advantages of using BDZ? (3)
- 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
Side effects of benzos? (5)
- 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
Other than BARB and BDZ, what can you use as a sedative/hypnotic
Zopiclone
66
Use of zopiclone
sedative/hypnotic
67
Other than BARB and BDZ, what other classes of drugs can you use as anxiolytics
``` Antidepressants Antiepileptics Antipsychotics Propranolol beta blocker Buspirone ```

Pharmacology and Therapeutics 2 Y2 (24 decks)

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