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Pharmacology MidTerm > Benzodiazepines > Flashcards

Benzodiazepines Flashcards

1
Q

Define Anxiety.

A

An unpleasant state of tension, apprehension, and uneasiness… It is a fear that arises from an unknown source.

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2
Q

What are the physical manifestations of anxiety?

A

Sympathetic activation, e.g., tachycardia and sweating.

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3
Q

Do episodes of mild anxiety warrant treatment?

A

No.

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4
Q

Does severe, chronic, and debilitating anxiety warrant treatment?

A

Yes.

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5
Q

What names do anti anxiety medications have?

A

Anxiolytic drugs.
Minor tranquilizers.

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6
Q

What secondary effect do anxiolytics have besides their primary action?

A

Sedative effect.

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7
Q

What is the term for drugs that induce sleep?

A

Hypnotics.

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8
Q

Explain.

A

Benzodiazepines are generally safer because their effects plateau before reaching life-threatening CNS depression.

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9
Q

Compare Drug A and Drug B.

A

Drug A quickly causes deep CNS depression; risky. (e.g., barbiturates and alcohol).

Drug B is safer as its effects are gradual and higher doses are needed for serious CNS depression (e.g., benzodiazepines).

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10
Q

Which class of drugs is most commonly used for treating anxiety? Why?

A

Benzodiazepines.
They are safer and more effective than older classes of medications (barbiturates).

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11
Q

What neurotransmitter receptors do benzodiazepines target?

A

GABA receptors.

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12
Q

How many benzodiazepine receptor subtypes are there?

A

There are two main types: BZ1 and BZ2.

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13
Q

Which subunit is associated with BZ1 receptors?

A

α1

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14
Q

Which subunit is associated with BZ2 receptors?

A

α2

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15
Q

What effect do benzodiazepines have on the affinity of GABA for its receptor?

A

They enhance GABA binding to its GABA-A receptor.

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16
Q

Where are benzodiazepine receptors located?

A

Parallel to GABA receptors.

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17
Q

What is benzodiazepines’ mechanism of action?

A

Benzodiazepines bind to their own specific receptors that are adjacent to GABA-A receptors.

This potentiates the binding of GABA to its own receptor.

This increases chloride ions moving into cells, causing membrane hyperpolarization, reducing action potentials.

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18
Q

Do benzodiazepines bind to the same site that GABA binds to the receptors?

A

No.

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19
Q

What are the adverse effects associated with benzodiazepines?

A

Drowsiness and confusion (most common).
Ataxia at high doses, negatively affecting motor coordination (avoid driving).
Cognitive impairment in the form of decreased long-term recall of new knowledge.

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20
Q

Which patients need to take precautions when using benzodiazepines?

A

Liver disease patients.
Acute-narrow-angle glaucoma patients.
Alcohol and other CNS depressant consumers.

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21
Q

What activities do benzodiazepines NOT exhibit?

A

No antipsychotic or analgesic activity.
They also don’t affect the autonomic nervous system.

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22
Q

Which specific GABA-A receptor subunits are targeted by benzodiazepines for their effects?

A

α1, α2, α3, and α5 subunits.

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23
Q

Which GABA-A receptor subunit is associated with sedation, amnesia, and hypnosis?

A

α1.

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24
Q

Which GABA-A subunits are associated with anxiolytic and muscle relaxant effects?

A

α2 and α3.

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25
Q

Which GABA-A subunit is associated with memory impariment?

A

α5 subunit.

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26
Q

What factors determine the effect of benzodiazepines?

A

Dose and subsequent selectivity.

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27
Q

What therapeutic actions do benzodiazepines exhibit?

A
  1. Anti-anxiety.
  2. Sedative.
  3. Anterograde amnesia.
  4. Anticonvulsant.
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28
Q

When are benzodiazepine anxiolytic?

A

At low doses (α2 subunit).

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29
Q

When are benzodiazepines sedative and hypnotic?

A

All have some sedative properties; some can produce hypnosis at higher doses (α1 subunit).

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30
Q

Which subunit is associated with anterograde amnesia in benzodiazepine use?

A

α1 subunit.

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31
Q

Which subunit is associated with anticonvulsant activity in benzodiazepine use?

A

α1 subunit.

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32
Q

When do benzodiazepines exhibit a muscle relaxing effect?

A

At high doses (α2 subunit).

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33
Q

How are benzodiazepines classified?

A

Based on the duration of action:
1. Long-acting.
2. Intermediate-acting.
3. Short-acting.

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34
Q

List long-acting benzodiazepines.

A

Clonazepam.
Chlordiazepoxide.
Diazepam.
Flurazepam.
Quazepam.

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35
Q

List intermediate-acting benzodiazepines.

A

Alprazolam.
Estazolam.
Lorazepam.
Temazepam.

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36
Q

List short-acting benzodiazepines.

A

Oxazepam.
Triazolam.

37
Q

What is the duration of action of long-acting benzodiazepines?

A

1-3 days.

38
Q

What is the duration of action of intermediate-acting benzodiazepines?

A

10-20 hours.

39
Q

What is the duration of action of short-acting benzodiazepines?

A

3-8 hours.

40
Q

Why are the half-lives of benzodiazepines important?

A

Their half-lives (i.e., duration of action) determine the therapeutic usefulness.

41
Q

Do individual benzodiazepines show big differences in their relative anxiolytic, anticonvulsant, and sedative properties?

A

No (They show small differences in their relative properties).

42
Q

Which types of anxiety are benzodiazepines used for?

A

Generalized anxiety disorder.
Social anxiety.
Performance anxiety.
Post-traumatic stress disorder.

43
Q

Why shouldn’t benzodiazepines be used long-term?

A

They cause addiction.

44
Q

Why are longer-acting benzodiazepines preferred for treating patients who require treatment for prolonged periods of time?

A

Low risk of addiction.

45
Q

Why do benzodiazepines have a small potential for tolerance when used to control anxiety compared to sedative and hypnotic effects?

A

Lower dose is used for anxiety.

46
Q

When does tolerance usually set in with benzodiazepine use?

A

When used for more than two weeks, due to decreased GABA receptor density.

47
Q

Why should benzodiazepines be avoided with alcohol consuming patients?

A

Benzodiazepines potentiate the alcohol effective, causing additive CNS depression.

48
Q

Which substances do benzodiazepines share cross-tolerance with?

A

Ethanol.
Chlordiazepoxide.

49
Q

Which benzodiazepine is effective for short-term and long-term treatment of panic disorders?

A

Alprazolam.

50
Q

What serious risk is associated with alprazolam when it is used to treat panic disorders?

A

Withdrawal reactions occur in about 30% of sufferers.

51
Q

Which benzodiazepine is used to treat skeletal muscle spams, such as the ones that occur in muscle strain and degenerative disorders like multiple sclerosis and cerebral palsy?

A

Diazepam.

52
Q

Which class of benzodiazepines are used for amnesia?

A

Shorter-acting agents.

53
Q

When are short-acting benzodiazepines used to induce amnesia?

A

Before unpleasant procedures, such as endoscopic, bronchoscopic, dental procedures as well as angioplasty.

54
Q

What type of sedation do shorter-acting benzodiazepines cause (when used to induce amnesia)?

A

Conscious sedation.

55
Q

Which benzodiazepine is used as an injection-only inducer of anesthesia?

A

Midazolam.

56
Q

Which benzodiazepines are used to treat grand-mal epileptic seizures and status epilepticus?

A

Diazepam.
Lorazepam.

57
Q

Which benzodiazepines are used to acutely manage alcohol and barbiturate withdrawal and seizures due to cross-tolerance?

A

Chlordiazepoxide.
Clorazepate.
Diazepam.
Oxazepam.

58
Q

What does the sleep cycle consist of?

A

Deep sleep (slow, long).
Rapid eye movement (REM) (faster).

59
Q

What are the characteristics of rapid eye movement (REM) phase of the sleep cycle?

A

Rapid random eye movement.
Low muscle tone.
Vivid dreams.
Heart rate, cardiac pressure, cardiac output, arterial pressure, and breathing rate become irregular.

60
Q

Are all benzodiazepines useful as hypnotic agents?

A

No.

61
Q

How do benzodiazepines affect sleep?

A

Make one fall asleep faster.
Increase stage 2 of non-REM sleep (i.e., REM sleep and slow wave sleep duration is decreased).

62
Q

Which benzodiazepines have a strong hangover effect?

A

Long-acting benzodiazepines.

63
Q

Why are non-benzodiazepine hypnotic drugs (such as zolpidem, and zaleplon) are preferred as hypnotic drugs over benzodiazepines?

A

They do not affect sleep stages.

64
Q

Which long-acting benzodiazepine is most commonly prescribed for sleep disorders?

A

Flurazepam.

65
Q

Which intermediate-acting benzodiazepine is most commonly prescribed for sleep disorders?

A

Temazepam.

66
Q

Which short-acting benzodiazepine is most commonly prescribed for sleep disorders?

A

Triazolam.

67
Q

Which benzodiazepine receptor do benzodiazepines affect when used to treat sleep disorders?

A

BZ1 receptor.

68
Q

Flurazepam, a benzodiazepine used to treat sleep disorders, has an active metabolite, resulting in long half-life.
How does this affect its therapeutic profile?

A

Shortens sleep onset and reduces awakenings.
Extends total sleep time.
Minimally causes rebound insomnia.
However, it leads to daytime drowsiness and drug buildup.

69
Q

Which type of sleep disorder is the benzodiazepine temazepam most effective for?

A

Patients who experience frequent wakening; useful for insomnia caused by the inability to stay asleep.

70
Q

When should temazepam be given when it is used to treat sleep disorders?

A

1-2 hours before the desired bedtime as the peak sedative effect sets in n1 to 3 hours after an oral dose.

This is done so the onset of action is delayed and the time it takes for the patient to fall asleep is not affected.

71
Q

Which type of sleep disorder is the benzodiazepine triazolam most effective for?

A

Helping patients with insomnia (difficulty in going to sleep) to fall asleep.

72
Q

How quickly can tolerance develop with triazolam use?

A

Within a few days.

73
Q

What can happen when triazolam is discontinued?

A

Rebound insomnia.

74
Q

What strategy is recommended to prevent tolerance for triazolam?

A

Take triazolam intermittently, not daily, to prevent tolerance.

75
Q

For what maximum duration should triazolam be prescribed?

A

Not for more than two weeks.

76
Q

What property of benzodiazepines allows for their rapid and complete absorption?

A

Lipophilicity.

77
Q

Through which bodily system are most benzodiazepines metabolized?

A

By hepatic microsomal enzyme system.

78
Q

Name two benzodiazepines suitable for patients with liver dysfunction.

A

Lorazepam.
Oxazepam.

79
Q

Why might the clinical effect of benzodiazepines not align with their half-life?

A

Their clinical effect is terminated by redistribution, not just excretion.

80
Q

Should benzodiazepines be given to pregnant or breastfeeding women? Why or why not?

A

No, they should not; as they can cross the placenta and are excreted in breast milk.

81
Q

What can prolonged use of high doses of benzodiazepines lead to?

A

Psychological and physical dependence.

82
Q

List some withdrawal symptoms from abrupt discontinuation of benzodiazepines.

A

Confusion.
Anxiety.
Agitation.
Restlessness.
Insomnia.
Tension.
Rarely, seizures.

83
Q

Which type of benzodiazepines are more likely to cause abrupt and severe withdrawal symptoms?

A

Short half-life benzodiazepines like triazolam.

84
Q

How do less potent benzodiazepines, such as flurazepam, that are slowly eliminated affect sleep after discontinuation?

A

Induce less abrupt and severe withdrawal reactions.

85
Q

What is the function of flumazenil?

A

Flumazenil acts as an antagonist to GABA-A receptors and reverses the effects of benzodiazepines.

86
Q

How is flumazenil administered?

A

Intravenously.

87
Q

Describe the onset and duration of action of flumazenil.

A

Rapid onset and a short duration of action.

88
Q

Why is flumazenil not typically used for treatment?

A

Its short action does not align with the longer action of most benzodiazepines; it’s mainly used for diagnosis.

89
Q

What are the risks associated with using flumazenil in dependent patients?

A

May precipitate withdrawal symptoms in dependent patients or cause seizures if benzodiazepines were used to control seizures.

Pharmacology MidTerm (8 decks)

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