Sedative Hypnotic Drugs

Question 1

Sedative Drug

Answer 1

Also called anxiolytic drug
Reduces a person’s response to external stimuli (reduces anxiety and has a calming effect with minimal depression of motor or mental functions)
All of these drugs cause sedation (so the same drug often used as both anti-anxiolytic (low dose) and hypnotic (high dose))

Question 2

Hypnotic Drug

Answer 2

Induces drowsiness and a sleep like state

Question 3

Anxiety

Answer 3

Changes in mood, physiological arousal and increased perceptual acuity
Symptoms: tachycardia, sweating, trembling, palpitations, unpleasant state of tension, apprehension, uneasiness

Question 4

Therapeutic uses of BZ

Answer 4

Anxiety disorders (less susceptible to tolerance than sedative-hypnotic effects)
Muscular disorders
Seizures
Alchohol withdrawal
Sleep disorders (use ones with shorter duration of action)

Question 5

Buspirone

Answer 5

MOA mediated in part by 5HT1A receptors
Also affinity for DA2 receptors
Treat anxiety disorders
Little sedation
No anti-convulsant or muscle-relaxant properties
Slow onset of efficacy

Question 6

Zolpidem

Answer 6

Unrelated to BZ
Has hypnotic actions
Binds to BZ receptor and increases GABA-mediated inhibition
Short term treatment of insomnia

Question 7

Ramelton

Answer 7

Activates melatonin receptors in the suprachiasmatic nuclei of CNS
Decreases the latency of sleep onset
Minimal rebound insomnia and abuse potential

Question 8

Orexin Antagonists (Suvorexant)

Answer 8

Hypnotic

Antagonist at orexin receptors

Question 9

Benzodiazepine Metabolism

Answer 9

Extensively metabolized by the hepatic system to ACTIVE compounds
The apparent half-life represents the combined actions of the parent drug and its metabolites
Excreted in the urine as glucuronides or oxidized metabolites
The long acting BZ go through Desmethyldiazepam

Question 10

Abuse, Tolerance, and Adverse Reactions to BZ

Answer 10

Psychological and physiological dependence
Tolerance - Short half life (wake up early), day time anxiety, amnesia and confusion
Adverse: Drowsiness and confusion, ataxia and cognitive impairment at higher doses
Withdrawal symptoms: Confusion, anxiety, agitation, restlessness, insomnia, and tension

Question 11

Barbiturates Metabolism

Answer 11

Well absorbed orally
Wide distribution throughout body
Metabolized in liver to INACTIVE metabolites that are excreted in urine
A lot of tolerance, physical dependence, severe withdrawal, coma and resp depression

Question 12

Therapeutic Uses of Barbiturates

Answer 12

Anesthesia - influenced by duration of action
Anticonvlusant - phenobarbitol used to manage seizures
Anxiety - can be used as a mild sedative for anxiety and insomnia (most replaced by BZ)