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Pharmacology > Anxiolytic and hypnotic drugs > Flashcards

Anxiolytic and hypnotic drugs Flashcards

1
Q

Anxiolytic drugs

A
  1. Buspirone
  2. Hydroxyzine
  3. Diphenhydramine
  4. Doxylamine
  5. Barbiturates (thiopental, phenobarbital)
  6. Antidrepessants:
    - SSRIs (fluoxetine, paroxetine, sertraline)
    - SNRIs (venlafaxine)
  7. Antiepileptics:
    - gabapentin
    - tiagabin
    - valproate
  8. B-adrenoceptors antagonists - propranolol
  9. Atypical antipsychotics (olanzapine, risperidone)
  10. BZP
    - long-acting (clonazepam, diazepam, flurazepam, lorazepam)
    - intermediate-acting (temazepam)
    - short-acting (zolpidem, zoplicon, oxazepam, flumazenil)
    - others (alprazolam, midazolam, flunitrazepam)
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2
Q

Hypnotic drugs

A
  1. BZP - short-acting:
    • lorazepam
    • zolpidem
    • temazepan
    • zopiclon
  2. Antihistamines:
    • difenhydramine
    • promethazine
  3. Others:
    • chloral hydrate
    • meprobamate
    • methaqualone
    • eszopiclone
    • ramelteon
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3
Q

BZP

A

Are lipohilic, well absoorbed, many accumulate gradually in body fat.

  • Oral adm
  • i.v. in status epilepticus - clonazepam and kidazolam in anaesthasia

Metabolism:

  • all are metabolized and excreted in urine
  • different action duration
    • short = hypnotics w/ decrease hangover effect on wakening
    • intermediate
    • long = anxiolytics and anticonvulsants
  • several are converted to their active metabolite

MOA:

  • target GABA-A Rs
  • enhance GABA response by opening GABA activated chloride channels
  • influx Cl -> hyperpolarization -> spreads and inhibits AP
  • act allosterically to increase affinity to GABA

Pharmacological effects:

  • all BZP have anticonvulsive effect!
  • in general: decrease anxiety and aggression (limbic system), induce sleep, sedation, decrease mm tone and coordination (high doses - SC), anterograde amnesia (premedication before surgery)

AE:

  1. acute toxicity
    • BZP are less dangerous than other anxiolytics / hypnotics
    • in over dose cause prolonged sleep, w/out serious depression of resp and cardiac function
    • but combined w/ alcohol -> life-threatnening resp depression
  2. unwanted effects:
    • drowsiness, confusion, amnesia, cognitive impairement
    • used w/ caution in liver disease
    • long-acting, aren’t used as hypnotics anymore
  3. tolerance:
    • marked when BZP are continuously used as antiepileptics
    • is associated w/ decrease in GABA R density and duration of R occupancy
    • develops w/in 1-2 weeks continuous use
  4. dependence:
    • physiological and physical
    • abrupt discontinuation -> withdrawal syndrome (confusion, tremor, anxiety, insomnia, agitation, restlesness, tinnitus, weight loss) -> should be withdrawn gradually!
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4
Q

Clonazepam

A

Long-acting BZP

TU: acute anxiety

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5
Q

Diazepam

A

Long-acting BZP

TU:

  • acute anxiety
  • epilepsy (grand mal and status epilepticus)
  • lacohol withdrawal
  • spasticity (decrease muscle tone)
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6
Q

Flurazepam

A

Long-acting BZP

TU: hypnotic treatment of insomnia

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7
Q

Lorazepam

A

Long-acting BZP

TU:

  • acute anxiety
  • short-acting for insomnia
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8
Q

Temazepam

A

Intermediate-acting BZP

TU: for pts w/ frequent wakening (1-2hs before bedtime)

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9
Q

Zolpidem, Zoplicon and Oxazepam

A

Short-acting BZP

TU: to treat insomnia (decrease hangover effect on wakening)

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10
Q

Flumazenil

A

Short-acting BZP

TU: only used if respiration is very depressed

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11
Q

Alprazolam

A

TU:

  • for short and long-term
  • treatment of anxiety, but withdrawal in approx 30%
  • drug of choice for panic disorders
  • minor invasive procedures = conscious sedation (w/out unpleasant memories -> amnesia)

So effects are for:

  • anxiety disorders
  • sleep disorders
  • mm disorders
  • anticonvulsive
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12
Q

Buspirone

A 
Generalized anxiety (not phobias)
Efficacy similar to BZP
Actions mediated by 5-HT1A R
Some affinity for: DA2, 5-HT2A Rs
No mm relaxing / anticonvulsive properties

Advantages:

  • less side effects
  • minimal sedation
  • no loss of coordination
  • unlikely dependance

Disadvantage: slow onset of action

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13
Q

Hydroxyzin

A

Antihistamine w/ anti-emetic effect
Sedation prior to dental procedures
In pts w/ anxiety and w/ history of drug abuse (together)

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14
Q

Antidepressants

A

In treatment of anxiety

E.g.:

  • venlafaxin
  • duloxetin
  • MAOIs
  • SSRIs
  • TCA
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15
Q

Barbiturates

A

Formerly used as anxiolytics and hypnotics but were replaced by BZP.

Several disadvantages:

  • great tolerance
  • enzyme induction
  • physical dependence
  • low ratio btw lethal and effective doses
  • no antagonist

TU:

  • thiopental -> i.v. for anaesthesia
  • phenobarbital -> anticonvulsant
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16
Q

Zolpidem and Zoplicon

A 
Hypnotics
Act similar to BZP
Short-acting
Lack anxiolytic activity
Metabolized by CYP3A4
Few withdrawal effects
Minimal rebound insomnia
17
Q

Eszopiclone

A

Hypnotic

Effective for up to 6 months compared to placebo

18
Q

Ramelteon

A

Hypnotic
Selective agonist at melatonin (induce and promote sleep)
1ry complaint -> falling asleep -> indication
No dependence / withdrawal effects
Can be administered long-term

Pharmacology (10 decks)

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