Exam 2: Hypnotics Flashcards
BZD MOA
bind to GABAa receptors, allosteric site
BZD AE overview (4)
- daytime sedation
- psychomotor impairment
- cognitive deficits
- anterograde amnesia
BZD cautions (10)
- older adults
- tolerance and dependence within 4-6 weeks of use
- withdrawal
- rebound insomnia
- AVOID IN HX OF DRUG USE
- AVOID W/ ALCOHOL USE OR OPIOD USE
- BOXED WARNING W OPIODS
- AVOID IN SLEEP APNEA
- AVOID IN PREGNANCY
- can worsen depression, PTSD, suicidal ideation
BZD drugs (2)
- tamezepam
- 7.5-50mg dose
- sleep onset/maintenance
- slow onset - Triazolam
- 0.125-0.25 mg
- rapid onset
- sleep onset use
BZE Adverse Effects (7)
- CNS depression
- sedation
- respiratory depression - psychomotor impairment
- ataxia
- falls in elderly - Confusion
- Agression
- Disinhibition
- Amnesia
- anterograde
- retrograde - Dependence and abuse
Non-BZD Receptor Agonist
Z-Drugs
MOA
Bind to GABAa receptor, allosteric site
-more selective subunits
Z-drugs
Adverse effects (4)
- Daytime sedation
- cognitive deficits
- amnesia
- complex sleep behaviors
Z-drugs
Cautions (6)
- older adults
- tolerance and rebound insomnia < BZDs
- rx for significant withdrawal
- AVOID concomitant CNS depressants, including alcohol and opioids
- can worsen depression, suicidal ideation
- BOXED WARNING:
April 2019
-serious injuries or death in 66 patients, caused by parasomnias
Z-Drug pearls (1)
Rapid onset; food delays by 1-2 hours
Melatonin Agonist
MOA (1)
- melatonin analogue; binds melatonin 1 & 2 receptors (hypothalamus)
Melatonin Agonist Sleep Benefits (3)
- Regulates circadian rhythms (phase shifting)
- direct effect on decreasing sleep latency
- no effect on sleep maintenance
Melatonin Agonist AE (4)
- HA
- Dizziness
- daytime somnolence
- GI upset
Melatonin Agonist Caution (2)
- may increase prolactin level in men & women
2. decreased testosterone levels in men
Melatonin Agonist Pearls (5)
- SAFE in sleep apnea, COPD, hx of substance use disorder
- may require 3 weeks of nightly use for maximum effect on sleep onset
- high-fat meal decreased effectiveness
- affected by CYP1A2 and CYP3A4 inhibition/induction
- brand-only $$$
Orexin Agonist MOA
Antagonism or orexin receptor 1 and 2 in the hypothalamus
-when activated they promote waking
Orexin Agonist Adverse Effects (7)
- daytime solomnce
- sleep paralysis
- cataplexy
- abnormal thinking
- hallucination
- CNS depression
- sleep-related activities
Cautions Orexin Agonist (4)
- potential to worse depression/suicidal ideation
- CONTRAINDICATED IN NARCOLEPSY
- Potential for abuse,
AVOID USE IN ALCOHOL - AVOID USE WITH STRONG CYP3A 4 inhibitors
Orexin Agonist Pearls
- onset delayed with food
- plan for 7 hours of sleep time
- brand-only $$$
Antidepressants MOA (3)
- Histamine H antagonism, “selective” at low doses
- serotonin 5HT2c antagonism
- Alpha-1 blockade (trazodone)
Antidepressants benefits/effect on sleep (3)
- primarily sleep maintenance
- not dependence, minimal tolerance
- not well studied in patients without depression
Antidepressants cautions (4)
- side effects vary widely between medications
- daytime somnolence/sedation is a possible side effect of each of the agents commonly used for sleep
- sedative effect within 1-2 weeks
- insomnia doses generally not effective for treatment of depression
Antihistamines MOA
- histamine H1 antagonism
Antihistamines benefits
may be effective for transient insomnia; latency and maintenance
Cautions Antihistamines (4)
- Tolerance to hypnotic effect; after 10 days
- increased dose does not equal increased response
- anticholinergic; CNS depression, next-day residual effects
- AVOID: narrow-angle glaucoma, acute asthma, urinary obstruction
Pearls Antihistamines (2)
- in a variety OTC products
2. some combo products contain antihistamines
Melatonin OTC MOA
- M1, M2, M3 receptors
Melatonin OTC Side effects
minimal, some daytime somnolence
Valerian OTC MOA
increases GABA
Valerican OTC SE
minimal, some diarrhea
Kava/chamomile/wuling MOA
*possible effects on GABA, 5HT, or glutamate
Kava/chamomile/wuline AE
hapatotoxicity (KAVA)
-rest similar to placebo
Gabapentin Role/ Risks
- not recommended
1. role: insomnia with consistent alcohol use disorder
- Rx: Dizziness, N/V
- mortality rx with opioids
- Rx dependency and abuse
Atypical Antipsychotics
role/rx
- NOT recommended
1. quetiapine, olanzapine
2. Role: insomnia with schizophrenia, Bipolar, or depressive d/o
- rx:
- metabolic effects
- movement d/o
- anticholingeric
- QTc prolongation
- orthostatic hypotension
- increased mortality in elderly patients with dementia-related psychosis
