Anxiolytic Drugs Flashcards

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?

A

α1β2γ2

21
Q

Where do benzodiazepines bind to on the GABAa receptor?

A

α-γ interface

22
Q

Where does GABA bind to on the GABAa receptor?

A

α-β interface

23
Q

Which alpha subunits are insensitive to benzodiazepines?

A

α4

α6

24
Q

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

A

α1

25
Q

At which alpha subunits does the binding of benzodiazepines induce anxiolytic effects?

A

α2

α3

26
Q

Which gamma subunit is required for benzodiazepine binding?

A

γ2

27
Q

Ideal receptor subunit combinations for effective anxiolytic action of benzodiazepines

A

α2β3γ2

α3β1-3γ2

28
Q

What is the mechanism of action of the endogenous benzodiazepine βCCE (ethyl-β-carboline-3-carboxylate)

A

Binds to the benzodiazepine binding site as an inverse agonist
Diazepam binding inhibitor

29
Q

Give an example of a benzodiazepine antagonist

A

Flumazenil

30
Q

when is Flumazenil used

A

Reverse actions of benzodiazepines, for example in patients who become excessively drowsy after BZ admin or after overdose

31
Q

What would happen if Flumazenil was administered to benzodiazepine–naïve patients?

A

Will produce anxiety

32
Q

Give an example of a BARBITUATE used to treat anxiety

A

phenobarbitone

33
Q

Mechanism of action of barbiturates

e.g. phenobarbitone

A

binds to the GABAA receptor

low concentrations prolongs openings produced by GABA

high concentrations it opens the channel (in absence of GABA)

34
Q

Barbiturates are non-selective. Where else do they bind and what is there action?

A

bind to AMPA receptors inhibiting glutamate release

35
Q

why are barbituates no longer used?

A

Produce tolerance and dependence

Produce anaesthesia and death in overdose

36
Q

Give an example of 5-HT1A agonists used to treat anxiety

A

Buspirone (mst comonly used)

ipsapirone

gepirone

37
Q

what is the mechanism of Buspirone?

A

5-HT1A receptor partial agonist

38
Q

What are the benefits of using Buspirone over other anxiolytic drugs?

A
  • less sedation
  • less motor in-coordination
  • No reports of tolerance and physical dependence
39
Q

What are the side effects of Buspirone?

A
  • nausea
  • dizziness
  • headache
  • restlessness
40
Q

What are the disadvantages of Buspirone?

A

Ineffective against panic attacks or severe anxiety

Therapeutic action takes days or weeks to develop

Does not suppress benzodiazepine withdrawal

41
Q

What is the mechanism of action of 5-HT1A agonists like buspirone to relieve anxiety?

A

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
Q

Give an example of an anxiolytic which is a β-adrenoceptor antagonists

A

propanolol

43
Q

What is the effect of propanolol

A

remove the peripheral symptoms of anxiety
palpitations
sweating
tremor

Block peripheral receptors – not a CNS effect

44
Q

Give two examples of antipshychotics used to treat anxiety

A

olanzepine

risperidone

45
Q

When are antipshychotics used to treat anxiety

A

may be used to treat GAD or post-traumatic stress disorder in some cases

46
Q

Give two examples of other hypnotics used to treat anxiety

A

zopiclone

zolpidem

47
Q

What is the mecahnism of action of zopiclone and zolpidem?

A

chemically distinct from benzodiazepines but bind to same site and act in similar way

short lasting

48
Q

Give two examples of antihistamines used to treat anxiety?

A

diphenhydramine (NYTOL)

promethazine

49
Q

What is the side effect of antihistamines?

A

drowsiness