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Neuro-pharmacology > Benzodiazepines > Flashcards

Benzodiazepines Flashcards

1
Q

Meprobamate (MPB)

A

MPB was an early non-barbiturate anxiolytic

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2
Q

MPB potentiates GABAA and acts as

A

a weak
partial agonist at the GABA site

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3
Q

Meprobamate (MPB) Eventually withdrawn due to

A

abuse potential and
narrow safety margin

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4
Q

Chlordiazepoxide found to have

A

sedative,
anxiolytic, and anticonvulsant effects

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5
Q

(Valium)

A

diazepam

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6
Q

BZD Effects

A

Anxiolytic and anticonvulsant

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7
Q

BZD Effects - sedation

A

less potent than barbiturates

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8
Q

BZD & muscles

A

Muscle relaxant

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9
Q

BZD Not effective as _____ but

A

anaesthetics BUT can be used as relaxants for pre-surgical anaesthesia

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10
Q

Midazolam

A

is a short-acting BZD used for brief
surgical procedures with local anaesthetic

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11
Q

Midazolam recovery

A

Recovery in a few hours with anterograde
amnesia – creates the illusion of anaesthesia

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12
Q

BZD Effects Lower incidence of (3)

A

tolerance,
less severe withdrawal,
greater safety margin than barbiturates

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13
Q

BZD use - like

A

Like barbiturates, the effects of BZDs vary with their rate of onset and duration of effect in the body.

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14
Q

BZDs have more rapid

A

onset and
termination of effect with increased
lipophilicity.

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15
Q

BZDs often have active

A

e metabolites
generated by type I metabolism

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16
Q

BZD Pharmacology

A

Some of the effects of BZDs relate to their slow metabolism and number of active metabolites

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17
Q

duration of effect of Benzos list

A

Oxazepam < Diazepam < Flurazepam

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18
Q

Diazepam half life

A

1-3 days but metabolites can be active and go on to have effects

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19
Q

Nordazepam results from _____ and has a half life of

A

Demethylation of Diazepam - half life of 2-7 days

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20
Q

Oxazepam results from _____ and has a half life of

A

oxidation and Demethylation of diazepam - half life of 4-15 days

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21
Q

temazepam results from _____ and has a half life of

A

oxidation of diazepam - half life of 4-18 days

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22
Q

prolonged action of metabolites

A

is beneficial for
anxiolytic and anticonvulsant use

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23
Q

Long elimination of metabolites reduces

A

reduces the
withdrawal syndrome

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24
Q

BZD metabolism - Short-acting BZDs

A

Enter the brain quickly due to high lipophilicity
Terminate quickly due to depot binding in fatty
tissues

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25
Q

BZD metabolism - Short-acting BZDs

A
  • Enter the brain quickly due to high lipophilicity
  • Terminate quickly due to depot binding in fatty
    tissues
  • Tend to have ‘hangover’ effects due to slow release
    from fatty tissues
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26
Q

BZD metabolism - Long-acting BZDs

A
  • Slower onset due to lower lipophilicity
  • Not readily taken up into fatty tissues
  • Multiple active metabolites
  • Long elimination half-lives
  • Reduced withdrawal effects due to slow decline in
    systemic levels
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27
Q

BZD receptor - BZD are

A

positive allosteric modulators at
the GABAA receptor

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28
Q

BZD site of GABAA is often referred to as

A

the BZD receptor

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29
Q

Many types of interactions at the BZD
receptor

A
  • Agonists (+ allosteric modulator of GABAA)
  • Partial agonists
  • Antagonists
  • Inverse agonists (- allosteric modulator of
    GABAA)
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30
Q

Classic benzodiazepines act as

A

positive allosteric modulators of
GABA-A

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31
Q

BZD binding increases the

A

response of the channel to lower concentrations of GABA

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32
Q

BZD increase the frequency of

A

channel opening

33
Q

Unlike barbiturates BZDs do not

A

have GABA mimetic activity

34
Q

The BZD site has for many years been considered an ‘orphan receptor’

A

The existence of a natural ligand for
the BZD site is proposed

35
Q

Several compounds have been
identified that bind the BZD site - termed

A

‘endozepines’

36
Q

β-carbolines

A

Small molecule inverse agonists at the
BZD site

37
Q

β-carbolines list

A
  • β-CCE
  • β-CCM
  • DMCM
38
Q

Diazepam-binding inhibitor (DBI)

A

Protein inverse agonist at the BZD site

39
Q

The BZD site of GABAA is able to elicit
both

A

h positive and negative allosteric
modulation of GABA activity.

40
Q

Negative allosteric modulators exert

A

biological effects as inverse agonists of
the BZD site

41
Q

Inverse agonists bind and exert - biological effect

A

biological effect that is opposite that of
agonists.

42
Q

Effects of BZD classes - Typical agonists: Classical BZD anxiolytics

A

Diazepam, lorazepam, flunitrazepam

43
Q

Typical agonists: Exert

A

positive allosteric modulation on GABAA

44
Q

Typical agonists: effects

A

Anxiolytic, sedative-hypnotic, anti-convulsant

45
Q

Competitive antagonists exert

A

Exert no effect at the BZD site but displace agonist binding

46
Q

Competitive antagonists: Flumazenil

A

used to treat BZD overdose

47
Q

Inverse agonists

A

Negative allosteric modulators of GABAA

48
Q

Inverse agonists - effects

A

Anxiogenic

49
Q

Inverse agonists - Principally experimental compounds, no

A

therapeutic benefit

50
Q

To date most proposed endozepines function as

A

inverse agonists at the BZD site

51
Q

Endozepines are

A

anxiogenic

52
Q

In animal studies endozepines increase (3)

A

agitation,
increase distress vocalizations,
and increase aggressive behaviours

53
Q

In human volunteers, endozepine administration increased (3)

A

muscle tension,
autonomic hyperactivity,
extreme apprehension

54
Q

The function of endozepines supports the model that the

A

BZD receptor site plays
a natural role in anxiogenesis

55
Q

BZD drugs may in fact

A

antagonize endozepine-induced anxiety

56
Q

BZD tolerance and dependence - tolerance

A

No metabolic tolerance develops (no enzyme
induction)

57
Q

Rapid tolerance develops to

A

muscle relaxant and
sedative effects (pharmacodynamic)

58
Q

Very little tolerance develops to

A

anxiolytic effects

59
Q

Many adverse side effects of BZDs when used because

A

anxiolytics are transient and dissipate as the
tolerance develops to the sedative effects

60
Q

Animal models of dependence show BZDs to have

A

low risk of dependence

61
Q
  • Dependence seems to be problematic in
A

n human
clinical use and abuse

62
Q

Convergent site of action with

A

barbiturates and
alcohol

63
Q

Convergent site of action with barbiturates and alcohol

A

Cross-tolerance and potential for drug
interactions

64
Q

BZDs interact with alcohol and pose

A

e increased
risk of toxicity and abuse when co-administered

65
Q

, BZDs are effective at treating

A

alcohol
withdrawal in chronic alcoholics

66
Q

BZDs have increased risk of adverse events in

A

elderly patients due to decreased liver function

67
Q

BZDs tend to _____ in elderly patients
causing adverse events

A

bioaccumulate

68
Q

Rebound effects

A

Rebound insomnia
Anxiety

69
Q

Withdrawal effects: (4)

A
  • Fearfulness
  • Tremors
  • Agitation
  • Muscle spasms
70
Q

Withdrawal easily managed with a

A

a long-acting BZD such as diazepam and slow weaning off the drug

71
Q

Adverse intoxication can occur

A

at higher doses

72
Q

Adverse intoxication can occur at higher doses (4)

A
  • Disorientation
  • Cognitive impairments
  • Amnesia
  • Sedation
73
Q

Paradoxical effects at high doses

A
  • Aggression
  • Irritability
  • Anxiety
74
Q
  • Overdose can be managed by
A

BZD
competitive antagonist

75
Q

BZD
competitive antagonist

A

Flumazenil displaces BZDs but has a
short half-life

76
Q

Overdose can present with

A

unconsciousness but respiratory
depression is only seen when
another drug is present

77
Q

Overdose can present with
unconsciousness but respiratory
depression is only seen when
another drug is present

A

Common with alcohol

78
Q

Triazolam is a

A

short-acting BZD with rapid clearance
used to treat insomnia (less hangover sedating effects)

79
Q

Triazolam causes people

A

to do violent things

Neuro-pharmacology (26 decks)

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