Pharmacology of Sedative-Hypnotics (anxiety, insomnia, seizures) (Dr. Lei)

What is the MOA of buspirone?

Unknown; may be due to agonist of 5-HT1A & 5-HT2 receptors

What is the MOA of benzodiazepines?

positive allosteric modulation of GABAA

↑ the effects of GABA by increasing GABA affinity for GABAA receptors

What is the MOA of Z drugs/Non-benzodiazepine Receptor Agonists (NBZRAs)?

Non-benzodiazepine hypnotics

Act selectively at benzodiazepine receptors to increase GABA

What is the MOA of Melatonin receptor agonists?

Agonists at MT1 & MT2 melatonin receptors

Promote sleepiness & regulate the circadian rhythm to coordinate the sleep-wake cycle

What is the MOA of orexin receptor antagonists?

Orexin neuropeptide signaling system promotes wakefulness

Antagonists block the orexin neuropeptide signaling system → drowsiness

What is the MOA of doxepin?

Tricyclic antidepressant

Inhibits NE & serotonin reuptake

Blocks Ach & histamine receptors

What is the MOA of antihistamines?

Block H1 histamine receptors

What are the ADEs of buspirone?

Dizziness, drowsiness, headache, lightheadedness, nausea, excitement

What is the warning on buspirone?

serotonin syndrome

What are the contraindications of buspirone?

MAO inhibitors use within past 14 days

What are the ADEs of Z drugs?

Somnolence, dizziness, ataxia, headache, lightheadedness, "pins & needles" feeling on the skin

What are the ADEs of melatonin receptor agonists?

Somnolence, dizziness

What is the warning on ramelteon?

complex sleep behavior

What are the ADEs of orexin receptor antagonists?

Somnolence, headache, dizziness, abnormal dreams

What are the contraindications of orexin receptor antagonists?

Narcolepsy, Strong 3A4 inhibitors

What are the warnings of orexin receptor antagonists?

Worsening depression/suicidal ideation, sleep paralysis, hallucinations, cataplexy-like symptoms, complex sleep behavior, daytime impairment

What are the ADEs of doxepin?

Seizures, somnolence, anticholinergic effects

What are the contraindications of doxepin?

MAOIs

What is the warning on doxepin?

increased suicidal thoughts or actions

What are the ADEs of antihistamines?

Sedation, confusion, paradoxical excitation, peripheral anticholinergic effects

Select the SSRIs & SNRIs used to treat anxiety

Escitalopram (Lexapro)

Fluoxetine (Prozac)

Sertraline (Zoloft)

Duloxetine (Cymbalta, Drizalma Sprinkle)

Venlafaxine XR (Effexor XR)

3 multiple choice options

Select the (possible) 5-HT1A & 5-HT2 receptor agonist used to treat anxiety

Buspirone (Buspar)

3 multiple choice options

Select the benzodiazepines used to treat anxiety

Alprazolam (Xanax XR)

Clonazepam (Klonopin)

Diazepam (Valium)

Lorazepam (Ativan)

3 multiple choice options

Select the benzodiazepines used to treat insomnia

Temazepam (Restoril)

Estazolam

Quazepam

Flurazepam

Triazolam (Halcion)

3 multiple choice options

Select the Z drugs (NBZRAs) used to treat insomnia

Eszopiclone (Lunesta)

Zolpidem (Ambien, Edluar)

Zaleplon (Sonate)

3 multiple choice options

Select the melatonin receptor agonists used to treat insomnia

Melatonin

Ramelteon (Rozerem)

Tasimelteon (Hetlioz)

3 multiple choice options

Select the orexin receptor antagonists used to treat insomnia

Daridorexant (Quviviq)

Lemborexant (DayVigo)

Suvorexant (Belsomra)

3 multiple choice options

Select the TCA used to treat insomnia

doxepin (Silenor)

3 multiple choice options

Select the antihistamines used to treat insomnia

Diphenhydramine (Benedryl)

Doxylamine (Unisom Sleep Tabs)

3 multiple choice options