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pharmacology Neuro > Anxiolytic Drugs > Flashcards

Anxiolytic Drugs Flashcards

(49 cards)

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1
Q

Give an example of an ANTIDEPRESSANT which is a Selective serotonin (5-HT) reuptake inhibitor (SSRI) used to treat anxiety

A

citalopram

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2
Q

Give an example of an ANTIDEPRESSANT which is a serotonin/noradrenaline reuptake inhibitor (SNRI) used to treat anxiety

A

venlafaxine

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3
Q

What is a disadvantage of using ANTIDEPRESSANTS to treat anxiety?

A

the onset of action is delayed

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4
Q

Are ANTIDEPRESSANTS anxiolytic, sedative, or hypnotic?

A

Anxiolytics

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5
Q

Give two examples of older ANTIDEPRESSANTS used to treat anxiety

A

MAOIs

Tricyclics

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6
Q

The disadvantages of using older ANTIDEPRESSANTS to treat anxiety

A

more side effects

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7
Q

What are the clinical uses of BENZODIAZEPINES

A
  • anti-anxiety
  • sedative
  • hypnotic
  • anticonvulsant
  • muscle relaxant
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8
Q

What are the side effects of BENZODIAZEPINES

A
  • drowsiness
  • confusion
  • amnesia
  • impaired motor coordination
  • lack of depth perception
  • reduced REM sleep
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9
Q

What is the half life and therapeutic usefulness of the BENZODIAZEPINE Zolpidem?

A

1-2h

hypnotic

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10
Q

What is the half life and therapeutic usefulness of the BENZODIAZEPINE Triazolam

A

2-4h

hypnotic

withdraw from UK market due to side effects

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11
Q

What is the half life and therapeutic usefulness of the BENZODIAZEPINE Loprazolam

A

6-12h

hypnotic and anxiolytic

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12
Q

What is the half life and therapeutic usefulness of the BENZODIAZEPINE Nitrazepam

A

16-40h

hypnotic and anxiolytic

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13
Q

What is the half life and therapeutic usefulness of the BENZODIAZEPINE Diazepam

A

20-40h

anxiolytic and anticonvulsant

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14
Q

Describe the tolerance of BENZODIAZEPINES in relation to their anticonvulsant, anxiolytic, and hypnotic uses.

A
  • greatest to anticonvulsant action
  • may occur to anxiolytic action
  • little to hypnotic actions
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15
Q

Do BENZODIAZEPINES induce a physical or psychological dependance?

A

physical

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16
Q

In the use of BENZODIAZEPINES what does withdrawal induce with physical dependance?

A
  • anxiety
  • dizziness
  • tinnitus
  • tremor
  • weight loss
  • sleep disturbances
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17
Q

What occurs if BENZODIAZEPINES are taken with alcohol

A

respiratory depression

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18
Q

What is the mechanism of action of BENZODIAZEPINES

A

1) Bind to GABAa receptor
2) Enhance the affinity of GABA binding
3) Increase the probability of channel opening
4) increase Cl- into cell leading to hyperpolarisation 5)inhibition of nerve cell

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19
Q

What is the structure of the GABAa receptor?

A

It is a ligand gated chloride channel with a pentameric structure

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20
Q

What is the most abundant GABAa receptor?

21
Q

Where do benzodiazepines bind to on the GABAa receptor?

Study These Flashcards
A

α-γ interface

22
Q

Where does GABA bind to on the GABAa receptor?

Study These Flashcards
A

α-β interface

23
Q

Which alpha subunits are insensitive to benzodiazepines?

24
Q

At which alpha subunit does the binding of benzodiazepines induce sedation and amnesia?

25
At which alpha subunits does the binding of benzodiazepines induce anxiolytic effects?
α2 | α3
26
Which gamma subunit is required for benzodiazepine binding?
γ2
27
Ideal receptor subunit combinations for effective anxiolytic action of benzodiazepines
α2β3γ2 α3β1-3γ2
28
What is the mechanism of action of the endogenous benzodiazepine βCCE (ethyl-β-carboline-3-carboxylate)
Binds to the benzodiazepine binding site as an inverse agonist Diazepam binding inhibitor
29
Give an example of a benzodiazepine antagonist
Flumazenil
30
when is Flumazenil used
Reverse actions of benzodiazepines, for example in patients who become excessively drowsy after BZ admin or after overdose
31
What would happen if Flumazenil was administered to benzodiazepine–naïve patients?
Will produce anxiety
32
Give an example of a BARBITUATE used to treat anxiety
phenobarbitone
33
Mechanism of action of barbiturates | e.g. phenobarbitone
binds to the GABAA receptor low concentrations prolongs openings produced by GABA high concentrations it opens the channel (in absence of GABA)
34
Barbiturates are non-selective. Where else do they bind and what is there action?
bind to AMPA receptors inhibiting glutamate release
35
why are barbituates no longer used?
Produce tolerance and dependence Produce anaesthesia and death in overdose
36
Give an example of 5-HT1A agonists used to treat anxiety
Buspirone (mst comonly used) ipsapirone gepirone
37
what is the mechanism of Buspirone?
5-HT1A receptor partial agonist
38
What are the benefits of using Buspirone over other anxiolytic drugs?
- less sedation - less motor in-coordination - No reports of tolerance and physical dependence
39
What are the side effects of Buspirone?
- nausea - dizziness - headache - restlessness
40
What are the disadvantages of Buspirone?
Ineffective against panic attacks or severe anxiety Therapeutic action takes days or weeks to develop Does not suppress benzodiazepine withdrawal
41
What is the mechanism of action of 5-HT1A agonists like buspirone to relieve anxiety?
5-HT1a receptors are somatodendritic autoreceptors on raphe neurones 5-HT1a receptors on 5-HT containing nerves desensitize Eventually 5-HT release is enhanced
42
Give an example of an anxiolytic which is a β-adrenoceptor antagonists
propanolol
43
What is the effect of propanolol
remove the peripheral symptoms of anxiety palpitations sweating tremor Block peripheral receptors – not a CNS effect
44
Give two examples of antipshychotics used to treat anxiety
olanzepine risperidone
45
When are antipshychotics used to treat anxiety
may be used to treat GAD or post-traumatic stress disorder in some cases
46
Give two examples of other hypnotics used to treat anxiety
zopiclone zolpidem
47
What is the mecahnism of action of zopiclone and zolpidem?
chemically distinct from benzodiazepines but bind to same site and act in similar way short lasting
48
Give two examples of antihistamines used to treat anxiety?
diphenhydramine (NYTOL) promethazine
49
What is the side effect of antihistamines?
drowsiness

pharmacology Neuro (14 decks)

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