Anxiolytic and Sedatives Flashcards
Define sedative
Agent that exerts a calming effect
Define hypnotic
Agent that produces drowsiness and encourages onset and maintenance of sleep
Define anxiolytic
Agent that relieves anxiety, reduces tension and irritability
Define tolerance
Decreased responsiveness to repeated doses
Define physiologic anxiety
- Expected, normal, transient response to stress
- Necessary for adaptation and coping
- Differs from fear
When is anxiety pathological?
- Has no or minimal recognizable environmental trigger
- Exceeds patient’s capacity to bear discomfort
- Persistent symptoms
- Results in functional impairment
Drugs that may induce anxiety-like symptoms
SSRIs Bronchodilators DA agonists Sympathomimetics Stimulants Thyroid hromone Herbals (ephedra, ginseng, St. John's wort)
Treatment of GAD
- SSRIs or Venlafaxine (1st)
- Buspirone
- BZDs
- Psychotherapy
Treatment of panic disorder
- SSRIs or Venlafaxine (1st)
- BZDs
- Psychotherapy
Treatment of PTSD
- SSRIs (1st)
- BZDs (not common)
- CBT
Treatment of OCD
- SSRIs (1st)
- Clomipramine (serotonergic TCA)
- BZDs have NO role in OCD
Treatment of social anxiety disorders
- B blockers (situational)
- SSRIs or Venlafaxine (generalized)
- BZDs NOT recommended
BZD use in OCD
NO use
BZD use in social anxiety disorders
NOT recommended
How do BZDs work?
Enhance GABA binding on Cl channel causing hyperpolarization
Effects of BZDs
- Anxiolytic
- Sedative and hypnotic
- Anterograde amnesia
- Anticonvulsant
- Muscle relaxant
- Cross tolerance w/alcohol
Therapeutic uses of BZDs
- Anxiety treatment
- Muscular disorders
- Seizures
- Sleep disorders (tolerance to sedative effects develops within 2 wks of continuous use)
- Pre-anesthetics
- Withdrawal from alcohol
BZD metabolism
- Hepatic
- Many have active metabolites
Which BZDs do NOT have active metabolites?
LOT
- Lorazepam
- Oxazepam
- Temazepam
BZDs ADEs
- Sedation (CNS depression)
- Amnesia
- Impaired judgment
- Diminished motor skills (driving caution)
- Resp depression at very high doses or combined w/alcohol
- Elderly more sensitive (so give lower dose)
Who is more likely to abuse BZDs?
Previous drug abusers
What agents have more potential for abuse/withdrawal?
Those with rapid onset and/or elimination
BZDs vs. barbiturates
BZDs are generally safer than barbiturates (esp for overdose situations)
Antidote for BZD overdose?
Flumazenil
Which BZDs are used for anxiety disorders?
LADCCC
- Lorazepam
- Alprazolam
- Diazepam
- Clonazepam
- Clorazepate
- Chlordiazepoxide
What is Buspirone?
5HT1A partial agonist
Buspirone MOAs
- Anxiolytic effects w/o marked sedation
- NO anticonvulsant or muscle relaxant properties
- NO cross tolerance w/ETOH or BZDs
What is Buspirone used for?
GAD (2nd line)
Buspirone ADEs
Dizzy
Nausea
Headaches
Alternative treatments for anxiety
- Non-pharm (counseling, exercise, avoid caffeine/stimulants)
- Antidepressants (SSRIs, Venlafaxine)
- Hydroxyzine
Difficulty falling asleep relates to:
Sleep latency
Difficulty staying asleep relates to:
Total sleep time
Agents used for insomnia
- BZDs
- Non BZD hynpotics (Z drugs, barbiturates)
- Antihistamines
- Melatonin agonist
- Sedating antidepressants
- Orexin receptor blocker (Suvorexant)
How do BZDs work in insomnia?
- Decrease time to fall asleep
- Decrease REM sleep
- Increase Stage 2 (non-REM) sleep
BZDs used in insomnia
- Triazolam
- Flurazepam
- Temazepam
What are non-BZD hypnotics?
Zolpidem (Ambien)
Zaleplon (Sonata)
Eszopiclone (Lunesta)
Phenobarbital
What is phenobarbital now primarily used to treat?
Seizure disorders
Phenobarbital may cause coma:
- At high doses
- In combo w/other CNS depressants
- No specific antidote
What agent can be used to treat insomnia in patients prone to substance abuse?
Trazodone
What is Doxepin and what is it used for?
- TCA (H1 blocker)
- Marketed for insomnia (initiation and maintenance of sleep) as “Silenor”
What is Ramelteon and what is it used for?
- Melatonin receptor agonists
- Decreases sleep latency
- NO risk of abuse
- CYP450 metabolized
Antihistamine use for insomnia
- Mildly effective
- Tolerance develops within 3 days of continuous use
- Anticholinergic ADEs
What is Suvorexant?
- Orexin receptor blocker (plays a role in keeping people awake)
- Approved for treating difficulty in falling and staying asleep
- Only placebo controlled studies have been done
Suvorexant ADEs
- Complex sleep behaviors
- Next day drowsiness
