Home' Australian Pharmacist : Australian Pharmacist July 2013 Contents 68 Australian Pharmacist July 2013 I ©Pharmaceutical Society of Australia Ltd.
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impairment of motor skills the following
day, which increases the risk of falls.4,12
The major concern about benzodiazepine
use is associated adverse effects,
including cognitive impairment, daytime
drowsiness, lightheadedness, dizziness,
amnesia falls and consequent fractures.12
Furthermore, hypnotic use is associated
with a 60% increase in car accidents, a
risk which is accentuated with concurrent
alcohol use and older age.12
While benzodiazepine use is common
in the elderly, only intermittent, short
term use (maximum of two weeks) is
recommended.13 After short term use,
benzodiazepines can be withdrawn
without problems.4 If benzodiazepine has
been used for several months at or above
therapeutic doses, a gradual withdrawal
of dose by 15% of the starting dose on
a weekly basis is advised to minimise
severity of withdrawal symptoms.4
Withdrawal symptoms include anxiety,
insomnia, irritability and palpitations.4
The imidazopyridine agents are classified
by their chemical structure and are
GABAA receptor agonists with varying
affinities for specific receptor subtypes.
Newer GABA active agents zolpidem,
zaleplon and zopiclone all bind GABAA
receptors and have various onsets of
action and half-lives which ascertain
whether they are used for sleep initiation,
maintenance or both. Comparison of the
onset of action and half-life of the three
drugs is noted in Table 5.11
Zolpidem is an imidazopyridine that binds
preferentially to one benzodiazepine
receptor subtype thought to mediate
hypnotic effects.1 Zolpidem has a short
elimination half-life of two hours, and
for this reason it is less likely to cause
drowsiness the following day.1 A modified
release formulation of zolpidem providing
one layer of rapid onset to initiate sleep
and the other layer providing prolonged
effects for maintenance has been
formulated to circumvent the problem
of the short half-life causing a rebound
effect to during the night, and early
Common adverse effects are daytime
somnolence or fatigue, dry mouth,
headaches, memory disturbance, nausea
and dizziness when used at standard
doses. Zolpidem can also cause sleep
associated behaviour disorders, including
somnambulism and night eating
disorder.15 Tolerance and dose escalation
are uncommon as are long-term
Zaleplon causes less memory loss and
sedation at therapeutic doses than
zolpidem, however both agents cause
hallucinations and visual disturbances.
Zaleplon has a rapid onset, half-life and
elimination and is therefore the drug of
choice for initiating sleep and may be
given to people who repeatedly wake
during the night, given its short duration
Zopiclone has a longer half-life and a high
bioavailability that indicates minimal first
pass effect. It is recommended that the
dosage of zopiclone is reduced by half in
Sleep-wake activity regulation
• Wake up at the same time each day.
• If you are unable to sleep for a long
time, do not stay in bed. Get out of
bed and do something that is not
stimulating, and then return to bed
and try to sleep.
• Avoid oversleeping.
• Avoid midday napping or limit to
10--15 minutes powernaps.
Sleep setting and in uences
• Exercise regularly before going to
• Avoid bright light exposure in late
evening or night.
• Encourage exposure to bright light
• Avoid heavy meals within three
hours of sleep.
• Avoid vigorous physical activity
within three hours before retiring.
• Have a dark, quiet room for sleeping,
avoid using TV, radio, computers or
• Ensure mattress and pillows are
comfortable and supportive.
• Only use the bed for sleep and
• Avoid caffeine after lunch.
• Reduce excessive alcohol intake.
• Avoid smoking especially after
• Avoid illicit drugs.
• Avoid having pets in the bedroom.
• Remove highly illuminated digital
clocks in the bedroom.
Sleep promoting adjuvant
• Encourage a light snack or a warm
milk drink before bed.
• Encourage a warm bath before bed.
• Ensure a comfortable temperature
for sleep and maximum darkness.
Table 3. Sleep hygiene4,7
Rules for stimulus control
1. Lie down intending to go to sleep
only when you are sleepy.
2. Only use bed for sleep, do not read,
watch TV, eat or worry in bed. Sexual
activity is permitted.
3. If unable to sleep, get out of bed
immediately and go to another
room. Stay up as long as you wish
and then return to the bedroom to
sleep. The goal is to associate your
bed with falling asleep quickly so if
it feels like you are in bed for longer
than 10 minutes and have not
fallen asleep, you must follow this
4. If you still cannot fall asleep, repeat
step 3. Do this as often as necessary
throughout the night.
5. Set your alarm clock to get up
at the same time every morning
irrespective of how much sleep you
get during the night. This will help
your body to acquire a consistent
6. Do not nap during the day.
Table 4. Stimulus control
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