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Pharmacology (Winter) > Anxiolytics & Hypnotics > Flashcards

Anxiolytics & Hypnotics Flashcards

1
Q

Long-acting BZDs:

A

Diazepam, Flurazepam, Clonazepam,

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2
Q

Intermediate-acting BZDs:

A

Lorazepam, Alprazolam, Temazepam,

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3
Q

Short-acting BZDs:

A

Triazolam

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4
Q

BZD antagonist:

A

Flumazenil

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5
Q

Barbiturates:

A

Thiopental

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6
Q

Other anxiolytic:

A

Buspirone

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7
Q

Other hypnotic:

A

Zopiclone

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8
Q

What are terms “anxiolytic” and “hypnotic”?

A

Anxiolytic (help pt relax)
- Calming effects
- Relief of anxiety

Hypnotic (help pt sleep)
- Promotes drowsiness
- Promotes onset and maintenance of sleep

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9
Q

What drugs are classified as Benzodiazepines (BZDs)?

A

Diazepam, Flurazepam, Clonazepam, Lorazepam, Alprazolam, Temazepam and
Triazolam

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10
Q

What drugs are classified as Barbiturates?

A

Thiopental

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11
Q

What drugs are classified under “Others”?

A

Buspirone (anxiolytic), Zopiclone (hypnotic)

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12
Q

What is the action site of BZDs?

A

GABA-A receptor

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13
Q

What is a GABA-A receptor?

A
  • GABA is the primary inhibitory neurotransmitter in brain;
  • GABA-A receptor is a hetero-oligomeric glycoprotein with 2X α, 2X β and 1X γ subunits.
  • α subunit has 5 isoforms with α1-5
    – α1 — hypnotic
    – α2-5 — sedation, psychomotor effect
  • GABA-A receptor is a chloride channel
    – Activation — chloride influx; hyperpolarizes neurons and decreases neuronal activity.
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14
Q

What is the action sites of the BZDs?

A

GABA-A receptor, Cl- channel

ENHANCE GABA actions (not directly activate receptor), increase Cl- channel opening

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15
Q

What is the action sites of the Barbiturates?

A

GABA-A receptor, Cl- channel

ENHANCE GABA actions; DIRECTLY ACTIVATE receptor at high concentration; inhibit glutamate AMPA receptor

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16
Q

What are the factors that affect rate of onset and duration of BZDs?

A

lipophilicity and biotransformation

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17
Q

What are the factors that affects onset (determined by absorption & distribution) of BZDs?

A

Lipophilicity

MORE LIPOPHILIC = MORE RAPID ONSET OF ACTION

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18
Q

What are the factors that affects duration (determined by biotransformations & excretion) of BZDs?

A

Biotransformation

MANY PHASE I METABOLITES OF BZDs ARE ACTIVE

Half-life of BZDs ↑, Duration ↑

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19
Q

What are the Long-acting BZDs?

A

Diazepam, Flurazepam, Clonazepam,

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20
Q

What are the Intermediate-acting BZDs?

A

Lorazepam, Alprazolam, Temazepam,

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21
Q

What are the Short-acting BZDs?

A

Triazolam

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22
Q

What is the main differences between BZDs?

A

rate of onset and duration of actions

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23
Q

What are BZDs therapeutic uses related to half-life?

A
  • short acting is preferable for hypnotic
  • longer acting preferable for anxiolytic
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24
Q

BZDs with long half-lives:

A

cause cumulative effects with multiple doses

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25
Q

What are the pharmacokinetics of Barbiturates?

A
  • Lipophilic: absorbed and distributed rapidly.
  • Metabolized in the liver, but slowly (with the exception of thiopental)
  • HEPATIC CYT-P450 SYSTEM INDUCERS
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26
Q

Which Barbiturate drugs are Ultra-short-acting (30 min)?

A

thiopental for induction of anesthesia

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27
Q

Which Barbiturate drugs are Short-acting (18-48 hours)?

A

secobarbital, pentobarbital for hypnotic and sedative

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28
Q

Which Barbiturate drugs are Long-acting (4-5 days)?

A

phenobarbital for seizures

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29
Q

What are the therapeutic uses of BZDs?

A

1) For relief of ANXIETY (NOT 1st line drugs for chronic anxiety (SSRIs are 1st line drugs)

2) For treatment of INSOMNIA (increase stage II, but decrease deep sleep)

3) For sedation and amnesia before and during surgical procedures

4) For treatment of epilepsy and seizure states

5) For muscle relaxation in specific neuromuscular disorders (skeletal muscle spasms)

6) For control of ethanol (alcohol) withdrawal symptoms or other sedative-hypnotic withdrawal states

30
Q

What are Barbiturates used for?

A

rarely used, but still used for induction of ANESTHESIA, SEIZURE

31
Q

What are the 6 things that BZDs are used for?

A
  1. For relief of anxiety (sedation)
  2. For tx of insomnia (hypnotic)
  3. For sedation & amnesia before & during surgical procedures
  4. For tx of epilepsy & seizure states - Anticonvulsant

5) Muscle relaxant – for muscle relaxation in skeletal muscle spasms caused by CNS disorder. e.g. diazepam

6) For alcohol withdrawal symptoms or other sedative- hypnotic withdrawal states

32
Q

What are BZDs used for?

A

Used for the management of ACUTE ANXIETY
STATES and for rapid control of panic attacks.

33
Q

Are BZDs the 1st-line drugs for chronic anxiety?

A

NO - Selective serotonin reuptake inhibitors (SSRIs) are first-line drugs FOR LONG-TERM MANAGEMENT of chronic anxiety (Generalized Anxiety Disorder) and panic disorders.

34
Q

What is the drug selection of BZDs for panic disorders & agoraphobia?

A

Alprazolam

35
Q

How do BZDs act as hypnotics?

A
  • decrease the latency to sleep onset and increase Stage II of NREM
  • decrease both slow wave and REM sleep.
36
Q

Which BZD drug?

For difficulty falling asleep, use fast-acting, but shorter duration drug

A

i.e. triazolam

37
Q

Which BZD drug?

For frequent awakenings, falling asleep is not the issue, so use a drug of medium duration

A

i.e. lorazepam, temazepam

38
Q

What dose level should you start with for tx of insomnia (hypnotic) BZDs?

A

Starting with very low doses (to avoid hangover)

39
Q

Why are BZDs used for sedation and amnesia before and during surgical procedures?

A

Produce sedative effects, cause anterograde amnesia

Use before and during medical and surgical procedures.

40
Q

Which BZDs make them 1st choice for sedation and amnesia before and during surgical procedures (Produce sedative effects, cause anterograde amnesia)?

A

midazolam, lorazepam

Use before and during medical and surgical procedures.

41
Q

Which BZDs should be used for treatment of epilepsy and seizure states – Anticonvulsant?

A

(lorazepam, diazepam)
- management of seizures such as generalized tonic-clonic status epilepticus, absence seizures, partial seizures…

42
Q

Why should BZDs be used forMuscle relaxant – for muscle relaxation in skeletal muscle spasms caused by CNS disorder. e.g. diazepam?

A

has useful relaxant effects in skeletal muscle spasticity of central origin

43
Q

Why should BZDs be used for alcohol withdrawal symptoms or other sedative- hypnotic withdrawal states?

A
  • substituting for alcohol or other sedative-hypnotics during withdrawal states
  • reducing the risk of withdrawal-related seizures.
44
Q

What are Barbiturates?

A

CNS depression:
- Sedation →hypnosis →anesthesia →coma
- Higher than BZDs

45
Q

What are the therapeutic uses of Barbiturates?

A
  • Rarely used as sedative and hypnotic. These drugs have largely been replaced by safer agents such as BZDs for the treatment of anxiety and insomnia.
  • Used as anticonvulsant in epilepsy and seizure. Barbiturates (phenobarbital): treatment of generalized tonic-clonic seizures, but not the drugs of first choice
  • As a component of balanced anesthesia Barbiturates (thiopental): Used to induce anesthesia, often followed by inhalation agent
46
Q

What are the general adverse effects of BZDs?

A

Safe, but produce CNS depressive effect on psychomotor and cognitive functions: drowsiness, confusion, anterograde amnesia; potentiate with alcohol, opiates CNS depressants.

47
Q

What is the Tolerance of BZDs?

A

decreased responsiveness to a drug following repeated treatment: down-regulation of brain BZD receptors (pharmacodynamic tolerance); not induction of metabolic enzymes.

48
Q

What is the Dependence of BZDs?

A

an altered physiologic state that requires continuous drug administration to prevent WITHDRAWAL symptoms:
A. Withdrawal symptoms: rebound anxiety, insomnia;
B. Withdrawal symptoms are more common and more severe in patients on BZDs with short half-lives as compared to long-half-lives;
C. Chronic use causes tolerance and dependence: patients on long-term BZD use MUST be tapered.

(severity of withdrawal sx’s is related in part to half-life!)

49
Q

What are the considerations of BZDs?

A
  • Prescriptions should be written for short periods
  • Depressant effects on psychomotor & cognitive functions
  • Used in combo with alcohol or other CNS depressants
  • Older patients, patients with liver diseases
  • Obese patients
  • Unauthorized dosage increases
50
Q

What are the contraindications of BZDs?

A
  • Myasthenia gravis
  • Narrow-angle glaucoma
  • Alcoholism
  • Severe sleep apnea
  • Pregnant or nursing mothers
51
Q

What is Flumazenil? What is the action site of Flumazenil?

A

has a high affinity for BZD binding site - BZD competitive antagonist

52
Q

What are the therapeutic use of Flumazenil?

A
  • Used to reverse the CNS depressant effects of BZD overdose
  • Inhibits effects of BZDs, but DOES NOT inhibit effects of barbiturates, buspirone, ethanol, opioids or general anesthetics

– Given iv, it acts rapidly & has a short half-life (0.7-1.3 hours); if repeated dosing is usually necessary

– Caution: If BZDs given for seizures

53
Q

What are the adverse effects of Barbiturates?

A
  • inducer of metabolic enzymes (metabolic tolerance) & pharmacodynamic tolerance
  • low therapeutic index
  • not safe
  • no antidote (compare with BZDs)

(CNS depression, physical dependence with more severe withdrawal sx’s, popular drug of social abuse)

54
Q

BZDs vs barbiturates

Action site:

A
  • BZDs: Potentiate GABA-A receptor activation 

Barbiturates:
- Potentiate GABA-A receptor activation,  GABA-mimetic at high concentration,  Inhibit glutamate AMPA receptor

55
Q

BZDs vs barbiturates

Pharmacokinetics:

A
  • Lipophilic; rate of onset of action is determined by lipophilicity of individual drug
  • BZDs: Many phase I metabolites of BZDs are active, no effect on Cyt-P450 isoenzymes
  • Barbiturates: hepatic Cyt-P450 system inducers.
56
Q

BZDs vs barbiturates

Therapeutic uses:

A
  • BZDs: anxiety; insomnia; amnesia; epilepsy; muscle spasms; alcohol withdrawal
  • Barbiturates: epilepsy, induction of anesthesia followed by inhalation agent.
57
Q

BZDs vs barbiturates

Adverse effects:

A

Therapeutic index:
- BZDs: Therapeutic index is high, safe
- Barbiturates: Therapeutic index is low, high doses can cause cardiac and vascular depression

Dependence and withdrawal:
- Restlessness, insomnia, weakness, dizziness, nausea, sweating and anxiety.
- BZDs: need to be tapered; Barbiturates: Give BZDs and then need to be tapered

Overdose: BZDs: flumazenil; Barbiturates: No antidote

58
Q

BZDs vs SSRIs in the treatment of anxiety

Action site:

A

BZDs: GABA-A receptor

SSRIs: serotonin transporter

59
Q

BZDs vs SSRIs in the treatment of anxiety

Pharmacokinetics:

A

Onset of anxiolytic effects
- Faster with BZDs than SSRIs

60
Q

BZDs vs SSRIs in the treatment of anxiety

Therapeutic uses:

A
  • Anxiety caused by a temporary stressor may be better treated with a BZD
  • SSRIs: more appropriate for long term anxiety, especially if anxiety may be a symptom of depression
  • Recommended for days or weeks with BZD; months with SSRIs
61
Q

BZDs vs SSRIs in the treatment of anxiety

Adverse effects:

A
  • Therapeutic index: Both are high
  • Drug interactions:
    – SSRIs: due to inhibition of liver enzymes
    – BZDs: CNS depressants including ethanol and
    antihistamines
  • Dependence:
    – BZDs: Rebound anxiety, insomnia after BZD therapy; need to be tapered
    – SSRIs: No dependence
  • Amnesic effects:
    – Produced by BZDs, not SSRIs
62
Q

What are the other anxiolytics & hypnotics?

A

Structurally different from BZDs and barbiturates

Other anxiolytic:
- Buspirone

Other hypnotic:
- Zopiclone

63
Q

What is the action site of Buspirone (Buspar): anxiolytic?

A

partial serotonin receptor agonist

no effect on GABA

64
Q

What are the pharmacokinetics of Buspirone (Buspar): anxiolytic?

A

intermediate onset (takes more than 1 week)

65
Q

What is the therapeutic use of Buspirone (Buspar): anxiolytic?

A

treat anxiety

66
Q

What is the adverse effects of Buspirone (Buspar): anxiolytic?

A

No risk of tolerance & dependence, minimal abuse potential, no withdrawal effects

Consideration: Do not use with monoamine oxidase (MAO) inhibitors

67
Q

What is the action site of Zopiclone (Imovane)?

A

structure is different from BZDs but GABA-A receptor binding site is same with BZDs, enhances GABA-mediated neuronal inhibition

68
Q

What are the pharmacokinetics of Zopiclone (Imovane)?

A

rapidly metabolized

69
Q

What is the therapeutic use of Zopiclone (Imovane)?

A

used for insomnia, not for anxiety, cause less
amnesia, minimal muscle relaxing and anticonvulsant effects

70
Q

What are the adverse effects of Zopiclone (Imovane)?

A

drowsiness, memory impairments, but low risk for tolerance, dependence and withdrawal

Can be antagonized by flumazenil

Pharmacology (Winter) (23 decks)

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