7 - Sedative-Hypnotics

a. Ramelton

a. Ramelton

1. A melatonic receptor agonist

   a. Ramelton

   b. Zalepton

   c. Chloral Hydrate

   d. Dipenhydramine

a. Zolpidem

2. DOC for Insomnia

   a. Zolpidem

   b. Buspirone

   c. Ethanol

   d. Chloral Hydrate

A. Midazolam

3. A short-acting drug that induces anterograde amnesia

   A. Midazolam

   b Diazepam

   c. Phenobarbital

   d. Chlordiazepoxide

a. Diazepam

4. Increases the frequency of chloride channel opening

   a. Diazepam

   b. Atropine

   c. Mephobarbital

   d. Etomidate

b. Trichloroethanol

5. What is the active metabolite of chloral hydrate

   a. Acetaldehyde

   b. Trichloroethanol

   c. Formaldehyde

   d. Acetic acid

SEDATIVES

produce mental relaxation and to reduce the desire for physical activity

Anxiety

changes in mood (apprehension and fear)

HYPNOTICS

induce and maintain sleep

Insomnia

irregular and include longer latency to fall asleep and frequent awakenings

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

Barbiturates

• Prolong GABA

• Do NOT bind to BDZ receptor

• Increase the duration of chloride channel opening

Sleep, calming effect, drowsiness

Increasing the frequency of chloride channel opening results in

Respiratory Depression

Increase the duration of chloride channel opening can cause

Flumazenil

Antidote for benzodiazepines toxicity

Barbiturates

Which is more toxic?

Benzodiazepines or Barbiturates

• Neutralization

• Hemodialysis

Barbiturates toxicity management

• Chlordiazepoxide

• Diazepam

• flurazepam

• Quazepam

Long-Acting Benzodiazepines

>12hrs

DOA of Long-Acting Benzodiazepines

Chlordiazepoxide, Diazepam

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

flurazepam

A Long-Acting Benzodiazepines that is used for Insomnia

• Estazolam

• Alprazolam,

• Clonazepam

• Temazepam, Lorazepam, Chlonazepam

Intermediate Acting Benzodiazepines

7-12 hrs

DOA for Intermediate Acting Benzodiazepines

Estazolam

Intermediate Acting Benzodiazepines for Insomnia

Alprazolam, Clonazepam

Intermediate Acting Benzodiazepines for panic disorder

Antidepressant

1st line for panic disorder

Status Epilepticus

Lorazepam can cause a life threatening condition called:

• Triazolam

• Midazolam

• Oxazepam

Short Acting Benzodiazepines

1-6 hrs

DOA for Short Acting Benzodiazepines

Triazolam

Short Acting Benzodiazepines for Insomnia

Midazolam

Short Acting Benzodiazepines for anterograde amnesia

rebound insomnia

Problem for Short Acting Benzodiazepines after discontinuation

Barbiturates

Seldom use in anxiety or insomnia. Use in Seizures

Intermitten Porphyria

Barbiturates C/I to:

Phenobarbital, Mephobarbital

Long-Acting Barbiturates

Butabarbital, Vinbarbital, Amobarbital

Intermediate-Acting Barbiturates

Secobarbital, Pentobarbital, Hexobarbital

Short-Acting Barbiturates

Thiopental, Methohexital, Thiamytal

Ultrashort-Acting Barbiturates

6-12 hrs

DOA of Long-Acting Barbiturates

3 hrs

DOA of Short-Acting Barbiturates

3-6 hrs

DOA of Intermediate-Acting Barbiturates

<15-20 mins

DOA of Ultrashort-Acting Barbiturates

• Z-Drugs

• Melatonin

• Chloral Hydrate

• Antihistaminesp[

Other Sedative Hypnotic Drugs

Z-Drugs

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

• DOC for insomnia (replaced BDZ)

Zaleplon

A Z drug that is used to promote induction of sleep

Zolpidem, EsZopiclone

A Z drug that is used to maintain the sleep

Melatonin

Tx for Jetlags & insomnia for shift-workers

before

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

Lethal injection

Midazolam is used in a form of

RaMELteon

• approved to treat sleep-onset insomnia

• Adv: NO abuse liability, NO rebound insomnia

Trichloroethanol

Chloral Hydrate active metabolite

Chloral Hydrate

• occasionally used for preanesthetic sedation in pediatric patients

• OBSOLETE

Antihistamines

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

Buspirone

• Tx Generalized Anxiety Disorder

• ADV: less tolerance, less dependence, less abuse

• Buspirone

• Propranolol

non sedative hypnotic drugs

Propranolol

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

alpha and gamma sub unit

Benzodiazepine is adjacent to

alpha and beta sub unit

Barbiturates is adjacent to