7 - Sedative-Hypnotics

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1

a. Ramelton

  1. A melatonic receptor agonist

    a. Ramelton

    b. Zalepton

    c. Chloral Hydrate

    d. Dipenhydramine

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a. Zolpidem

  1. DOC for Insomnia

    a. Zolpidem

    b. Buspirone

    c. Ethanol

    d. Chloral Hydrate

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A. Midazolam

  1. A short-acting drug that induces anterograde amnesia

    A. Midazolam

    b Diazepam

    c. Phenobarbital

    d. Chlordiazepoxide

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a. Diazepam

  1. Increases the frequency of chloride channel opening

    a. Diazepam

    b. Atropine

    c. Mephobarbital

    d. Etomidate

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b. Trichloroethanol

  1. What is the active metabolite of chloral hydrate

    a. Acetaldehyde

    b. Trichloroethanol

    c. Formaldehyde

    d. Acetic acid

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SEDATIVES

produce mental relaxation and to reduce the desire for physical activity

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Anxiety

changes in mood (apprehension and fear)

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HYPNOTICS

induce and maintain sleep

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Insomnia

irregular and include longer latency to fall asleep and frequent awakenings

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Benzodiazepines

  • Potentiate GABA

  • (+) BDZ receptor (allosteric site formed by the cleft between α and γ subunits of GABA-A)

  • Increase the frequency of chloride channel opening

  • Result: ↓ in neuronal activity

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Barbiturates

  • Prolong GABA

  • Do NOT bind to BDZ receptor

  • Increase the duration of chloride channel opening

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Sleep, calming effect, drowsiness

Increasing the frequency of chloride channel opening results in

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Respiratory Depression

Increase the duration of chloride channel opening can cause

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Flumazenil

Antidote for benzodiazepines toxicity

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Barbiturates

Which is more toxic?

Benzodiazepines or Barbiturates

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  • Neutralization

  • Hemodialysis

Barbiturates toxicity management

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  • Chlordiazepoxide

  • Diazepam

  • flurazepam

  • Quazepam

Long-Acting Benzodiazepines

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>12hrs

DOA of Long-Acting Benzodiazepines

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Chlordiazepoxide, Diazepam

A Long-Acting Benzodiazepines that is used for severe muscle spasm

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flurazepam

A Long-Acting Benzodiazepines that is used for Insomnia

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  • Estazolam

  • Alprazolam,

  • Clonazepam

  • Temazepam, Lorazepam, Chlonazepam

Intermediate Acting Benzodiazepines

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7-12 hrs

DOA for Intermediate Acting Benzodiazepines

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Estazolam

Intermediate Acting Benzodiazepines for Insomnia

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Alprazolam, Clonazepam

Intermediate Acting Benzodiazepines for panic disorder

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Antidepressant

1st line for panic disorder

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Status Epilepticus

Lorazepam can cause a life threatening condition called:

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  • Triazolam

  • Midazolam

  • Oxazepam

Short Acting Benzodiazepines

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1-6 hrs

DOA for Short Acting Benzodiazepines

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Triazolam

Short Acting Benzodiazepines for Insomnia

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Midazolam

Short Acting Benzodiazepines for anterograde amnesia

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rebound insomnia

Problem for Short Acting Benzodiazepines after discontinuation

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Barbiturates

Seldom use in anxiety or insomnia. Use in Seizures

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Intermitten Porphyria

Barbiturates C/I to:

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Phenobarbital, Mephobarbital

Long-Acting Barbiturates

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Butabarbital, Vinbarbital, Amobarbital

Intermediate-Acting Barbiturates

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Secobarbital, Pentobarbital, Hexobarbital

Short-Acting Barbiturates

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Thiopental, Methohexital, Thiamytal

Ultrashort-Acting Barbiturates

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6-12 hrs

DOA of Long-Acting Barbiturates

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3 hrs

DOA of Short-Acting Barbiturates

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3-6 hrs

DOA of Intermediate-Acting Barbiturates

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<15-20 mins

DOA of Ultrashort-Acting Barbiturates

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  • Z-Drugs

  • Melatonin

  • Chloral Hydrate

  • Antihistaminesp[

Other Sedative Hypnotic Drugs

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Z-Drugs

  • binds to BDZ Receptor 1 (controls sleep & wakefulness)

  • DOC for insomnia (replaced BDZ)

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Zaleplon

A Z drug that is used to promote induction of sleep

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Zolpidem, EsZopiclone

A Z drug that is used to maintain the sleep

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Melatonin

Tx for Jetlags & insomnia for shift-workers

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before

Melatonin is released __ the onset of sleep and produces drowsiness that facilitates sleep

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Lethal injection

Midazolam is used in a form of

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RaMELteon

  • approved to treat sleep-onset insomnia

  • Adv: NO abuse liability, NO rebound insomnia

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Trichloroethanol

Chloral Hydrate active metabolite

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Chloral Hydrate

  • occasionally used for preanesthetic sedation in pediatric patients

  • OBSOLETE

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Antihistamines

A sedative hypnotic drugs that is also used for Insomnia, Mild Anxiety

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Buspirone

  • Tx Generalized Anxiety Disorder

  • ADV: less tolerance, less dependence, less abuse

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  • Buspirone

  • Propranolol

non sedative hypnotic drugs

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Propranolol

A non sedative hypnotic drug that is used for stage fright & performance anxiety

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alpha and gamma sub unit

Benzodiazepine is adjacent to

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alpha and beta sub unit

Barbiturates is adjacent to

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