Questão 1
Questão
Sleep Hygiene: ASLEEP
• Avoid [blank_start]alcohol, caffeine and nicotine[blank_end]
• [blank_start]Sleep (and sex)[blank_end] should be the only use of the bed
• Leave [blank_start]laptops, TVs and paperwork[blank_end] out of the bedroom
• [blank_start]Exercise[blank_end] regularly and be outdoors during the day
• Early rising - avoid [blank_start]sleeping in and daytime naps[blank_end]
• Plan for bedtime
Responda
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alcohol, caffeine and nicotine
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Sleep (and sex)
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laptops, TVs and paperwork
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Exercise
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sleeping in and daytime naps
Questão 2
Questão
Lack of sleep
• Irritability
• [blank_start]Daytime[blank_end] sleepiness
• [blank_start]Low[blank_end] energy/motivation
• Physical discomfort
• Impaired [blank_start]cognitive function[blank_end]
Responda
-
Daytime
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Low
-
cognitive function
Questão 3
Questão
Insomnia - “Repeated inability to initiate and maintain sleep.”
- Transient, [blank_start]2-3[blank_end] days - likely cause [blank_start]acute[blank_end] situational or environmental stress (shift work, jet lag)
- Short term, <[blank_start]3[blank_end] weeks - likely cause [blank_start]ongoing[blank_end] personal stress
- Long term, >3 weeks - likely causes psychiatric illness, behavioural, medical reasons
Questão 4
Questão
Neurotransmitter effects:
1. Cortical arousal regulated by - (match NT to location)
[blank_start]Noradrenaline[blank_end] (locus coeruleus)
[blank_start]Cholinergic[blank_end] pathways (brainstem)
[blank_start]Histamine[blank_end] (tuberomamillary nucleus)
[blank_start]Serotonin[blank_end] (raphe nucleus)
2. Promote wakefulness: orexins/hypocretins ([blank_start]peptide neurotransmitters[blank_end])
3. Sleep induced by: [blank_start]GABA, melatonin and galanin[blank_end]
Questão 5
Questão
GABA
- Gamma-aminobutyric acid, major inhibitory neurotransmitter, decreases [blank_start]neuronal excitability[blank_end] and therefore CNS function
- Drugs potentiating GABA [blank_start]transmission[blank_end]
1. Hypnotic ([blank_start]sleep inducing[blank_end] properties)
2. Sedative (moderating excitement and [blank_start]calming[blank_end])
3. [blank_start]Anxiolytic[blank_end] (anxiety-relieving)
Responda
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neuronal excitability
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transmission:
-
sleep inducing
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calming
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Anxiolytic
Questão 6
Questão
Drag and drop pharmacotherapies people take for insomnia into the right boxes.
Responda
-
Dietary supplements
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OTC/sleep aids
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Sedating medications
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Insomnia meds
Questão 7
Questão
Benzodiazepine receptor agonists e.g. [blank_start]triazolam, temazepam[blank_end].
Indicated for acute insomnia.
• Dose related [blank_start]hypnotic[blank_end] effects
• Facilitate [blank_start]onset and duration[blank_end] of sleep
• Alter NREM:REM
• [blank_start]Rebound[blank_end] insomnia
• Caution in pulmonary/respiratory disease: [blank_start]respiratory and CV[blank_end] depression risk.
Responda
-
triazolam, temazepam
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hypnotic
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onset and duration
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Rebound
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respiratory and CV
Questão 8
Questão
Pharmacodynamics of benzos:
- [blank_start]Positive allosteric[blank_end] modulator of GABA(A) R (most [blank_start]abundant[blank_end] R in CNS)
- ‘[blank_start]tonic[blank_end]’ inhibition
- [blank_start]hyper[blank_end]polarisation via Cl-
- makes excitation [blank_start]less[blank_end] likely
Pharmacokinetics of benzos:
- Potency: hydrophobicity
- Plasma protein [blank_start]binding[blank_end] (less free drug concentration).. so less potency in vivo
- E.g.: [blank_start]Diazepam[blank_end] - rapid onset, long acting, vs [blank_start]midazolam[blank_end] rapid onset, short acting, temazepam and triazolam very [blank_start]short[blank_end] half life, nitrazepam [blank_start]long[blank_end] half life
- Caution: increased potency with low [blank_start]albumin[blank_end] (e.g. haemodilution, liver dysfunction)
- Metabolised by CYP3A4 (Caution: impaired [blank_start]hepatic[blank_end] function)
Responda
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Positive allosteric
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abundant
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tonic
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hyper
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less
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binding
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Diazepam
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midazolam
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short
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long
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albumin
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hepatic
Questão 9
Questão
Non-benzodiazepine hypnotics: zalepon, zolpidem, zopiclone
• [blank_start]Different[blank_end] chemical class, similar mechanism
• Postsynaptic GABA(A) Rs - binding site [blank_start]distinct[blank_end] from benzo site
• Increased [blank_start]Cl- influx[blank_end] causes hyperpolarisation
• Rapidly [blank_start]absorbed[blank_end], metabolized by liver
• Short t1/2 ~ [blank_start]1-6[blank_end]h
Unwanted effects: Incoordination, drowsiness, dizziness, confusion, amnesia
Responda
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Different
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distinct
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Cl- influx
-
absorbed
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1-6
Questão 10
Questão
Benzos and Zs have problems as short term and long-term therapy:
[blank_start]Sedation, drowsiness, muscle relaxation[blank_end] - affects driving, machinery operation, [blank_start]falls[blank_end] in elderly
[blank_start]Abusable[blank_end] (rapid onset, short duration, high potency) and dependence risks.
Questão 11
Questão
Alternate medications for sleep (off label use):
ACh, NA, 5-HT, and DA promote wakefulness, so antagonists of these can be sedating:
- Antidepressants (e.g. [blank_start]amitriptyline, mirtazapine, doxepin[blank_end])
- Antipsychotics (e.g. [blank_start]quetiapine[blank_end])
GABA [blank_start]agonists[blank_end] are sleep promoting:
- Anxiolytics (e.g. alprazolam, [blank_start]clonazepam[blank_end])
Histamine is a potent wake-promoting neurotransmitter, so [blank_start]antagonists[blank_end] at H1 receptors have sedating properties:
- [blank_start]Promethazine, diphenhydramine[blank_end]. Long [blank_start]duration[blank_end] of action = daytime drowsiness.
Unwanted effects: headache, psychomotor impairment, [blank_start]antimuscarinic[blank_end] effects, paradoxical excitation (children, elderly)
Melatonin:
-• Produced in the [blank_start]pineal[blank_end] gland
• Under control of circadian system (SCN)
• Late evening [blank_start]rise[blank_end] = arousal [blank_start]declines[blank_end], facilitates sleep onset
• Prescription except when supplied: for primary insomnia (adults [blank_start]55[blank_end] years or older, up to [blank_start]13[blank_end] weeks), by a NZ registered, trained pharmacist, in the original pack. Tablets 3mg or MR 2mg.
Responda
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amitriptyline, mirtazapine, doxepin
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quetiapine
-
agonists
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clonazepam
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antagonists
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Promethazine, diphenhydramine
-
duration
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antimuscarinic
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pineal
-
rise
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declines
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55
-
13