Class 7-sleep Flashcards

Question

BENZODIAZEPINES

Answer 1

GABAA RECEPTOR AGONIST - In the absence of GABA, there is no effect - Simultaneous use of the receptor by benzodiazepines AND GABA = potentialisation GABAA RECEPTOR Includes several sub-units Benzodiazepines are mainly linked to sub-units α, β and γ Example of effect by sub-unit α1 : sedation α2 : anxiolytic α 5 : anterograde amnesia Effects on sleep: decrease sleep onset latency, increase total sleep time Little more time sleep per night (15-30 min) compared to a placebo... and that difference is lost over time.

Answer 2

``` Drowsiness, sedation Weakness Ataxia Dizziness Light-headed feeling Dry mouth Headache Confusion, disorientation Tachycardia, palpitations Anterograde amnesia « Hangover » effect: Administer a shorter-acting BZD Paradoxical effect: Especially children, elderly, behavioral disorder, borderline personality disorder. Stop immediately! Rebound insomnia: Associated with abrupt discontinuation ```

Answer 3

Generally short-term use : 2 weeks | Some benzodiazepines up to 12 weeks

Answer 4

zopicolne, eszopiclone, zolpidem GABAA RECEPTOR AGONIST - More specific affinity for α1 sub-unit (sedation) - Eszopiclone : exact mechanism unknown Effect on sleep: decrease sleep onset latency, increase TST

Answer 5

``` oDaytime drowsiness o Headache o Cognitive disorders o Dizziness o Falls o Alteration of taste o Complex sleep-related behaviors o Less risk of dependence ```

Answer 6

* Sleep apnea * Hepatic failure * Respiratory failure * Somnambulism * Myasthenia gravis

Answer 7

``` Mainly via CYP Increased drowsiness • Alcohol • Antihistamines • Opiates • Some antidepressants • Some antipsychotics ```

Answer 8

Generally short-term use : 7 – 10 days

Answer 9

MECHANISM OF ACTION At low doses : H1 receptor antagonism PHARMACOKINETICS: Improvements in sleep as early as first night Duration of action : 7 hours SIDE EFFECTS: Anticholinergic effects

Answer 10

TRAZODONE (LOW DOSE : 25 – 100 mg HS) | MIRTAZAPINE (LOW DOSE : 7,5 – 15 mg HS)

Answer 11

QUETIAPINE (LOW DOSE : 6,25 mg – 100 mg HS) | Although sedating, not recommended for insomnia unless a comorbid psychiatric disorder exists

Answer 12

CONSIDER IN THE FOLLOWING SITUATIONS Circadian rhythm disorders (e.g. jet lag) Delayed sleep phase disorder Patients with low endogenous melatonin levels DOSING 0,5 – 10 mg HS in many different formulations SIDE EFFECTS Considered safe

Answer 13

MECHANISM OF ACTION: Appears to act on central GABA systems DOSING: 300 – 900 mg HS SIDE EFFECTS : GI upset, headache, restless sleep, bitter taste, heart palpitations, rare cases of hepatotoxicity INTERACTIONS : may interact with medication via CYP

Answer 14

Do not take unless you have sufficient time to devote to sleep (sleep medications generally require at least 7 – 8 hours) Do not combine with alcohol or other CNS depressants, because this can intensify side effects Ask a professional if it is safe to take any newly prescribed medication with this medication to avoid interactions If insomnia does not improve in 7 – 10 days, consult the provider because insomnia may be a symptom of another underlying illness

Answer 15

Start at the lowest effective dose and initiate a short-term duration of treatment (e.g. 1 – 2 weeks) Evidence suggests that pharmacotherapy should be used no longer than a month due to the risk of dependence and tolerance Principles of behavioural management should remain the focus, even if medication is used Long- term use of hypnotics may be appropriate in some cases (e.g. severe refractory insomnia) : regular follow-up and reassessment are beneficial to ensure that comorbidities, tolerance and/or dependence do not emerge Short to intermediate-acting BZD or NBRA If symptoms persist, consider an alternative short to intermediate-acting BZD or NBRA

Answer 16

- ↑ alertness - ↑ energy - ↑ daily function - ↓ risk of falls - ↓ traffic accidents

Answer 17

- Cause serious side effects : confusion, memory problems, falls and hip fractures - ↑ risk of car accidents - Cause addiction - Only help a little

Answer 18

- Recurring episodes of an irresistible need to sleep, fall asleep or nap during the same day. During the previous 3 months, must occur at least 3 times per week - At minimum, occurrence or experience one of the following : - Cataplexy (sudden loss of muscle tone triggered by emotion) episodes at least a few times per week each month - Hypocretin deficiency - REM sleep latency 15 min or less on nighttime PSG or MSLT, revealing a mean sleep latency eight minutes or less

Answer 19

- Excessive daytime sleepiness (EDS): irresistible urge to sleep attacks occur in 100 % of cases - Cataplexy : sudden loss of muscle tone triggered by emotion (e.g. laughing, excitement, anger) - Hallucinations - Sleep paralysis : total or partial paralysis occurring at the onset or termination of sleep in which the muscles are inhibited but the brain is aware of physiologic change

Answer 20

- Hypocretin (also called OX) – deficiency - Dopamine / noradrenaline – hypofunction - Acetylcholine – excess - Histamine neurons – have a role in the «waking action» of OX

Answer 21

- Modafinil (AlertecMD) - If ineffective : stimulants (refer to ADHD class) - Available in the USA : Sodium oxybate (GHB)

Answer 22

MECHANISM OF ACTION UNKNOWN ; HYPOTHESIS : - Binds the DA transporter to inhibit reuptake - ↑ histamine in hypothalamus to stimulate the release of hypocretin CLINICAL EFFECT - ↑ daytime vigilance and ↓ number and duration of daytime sleep episodes with little effect on nocturnal sleep - Similar to traditional CNS stimulants, but with improved tolerability and ↓ risk of abuse and tolerance - Onset of action < 1 hour ; duration 6 – 8 hours

Answer 23

- ↑ blood pressure in initial hypertension - Headache - GI upset - Nausea / vomiting - Anxiety - Insomnie - Dizziness

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Class 7-sleep Flashcards

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