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B.Consumption of caffeinated beverages, prescribed drugs,
over-the-counter medications, and illegal substances
should be sought.
III.Pharmacologic management
A.Hypnotics are the primary drugs used in the management
of insomnia. These drugs include the benzodiazepines and
the benzodiazepine receptor agonists in the
imidazopyridine or pyrazolopyrimidine classes.
Recommended dosages of hypnotic medications
(elderly dosages are in parentheses)
Benzodiaz- Recom- Tmax Elimi- Re-
epine mended nation cepto
hypnotics dose, mg half- r se-
life lectiv
ity
Benzodiazepine receptor agonists
Zolpidem 5-10 (5) 1.6 2.6 Yes
(Ambien)
Zaleplon (So- 5-10 (5) 1 1 Yes
nata)
Hypnotic Medications
Estazolam 1-2 (0.5-1) 2.7 17.1 No
(ProSom)
Flurazepam 15-30 (15) 1 47.0- No
(Dalmane) 100
Triazolam 0.250 1.2 2.6 No
(Halcion) (0.125)
Temazepam 7.5-60 0.8 8.4 No
(Restoril) (7.5-20)
Quazepam 7.5-15.0 2 73 No
(Doral) (7.5)
B.Zolpidem (Ambien) and zaleplon (Sonata) have the
advantage of achieving hypnotic effects with less
tolerance and fewer adverse effects.
C.The safety profile of these benzodiazepines and
benzodiazepine receptor agonists is good; lethal
overdose is rare, except when benzodiazepines are
taken with alcohol. Sedative effects may be enhanced
when benzodiazepines are used in conjunction with other
central nervous system depressants.
D.Zolpidem (Ambien) is a benzodiazepine agonist with
a short elimination half-life that is effective in inducing
sleep onset and promoting sleep maintenance. Zolpidem
may be associated with greater residual impairment in
memory and psychomotor performance than zaleplon.
E.Zaleplon (Sonata) is a benzodiazepine receptor
agonist that is rapidly absorbed (TMAX = 1 hour) and has
a short elimination half-life of 1 hour. Zaleplon does not
impair memory or psychomotor functioning at as early as
2 hours after administration, or on morning awakening.
Zaleplon does not cause residual impairment when the
drug is given in the middle of the night. Zaleplon can be
used at bedtime or after the patient has tried to fall asleep
naturally.
F.Benzodiazepines with long half-lives, such as
flurazepam (Dalmane), may be effective in promoting
sleep onset and sustaining sleep. These drugs may have
effects that extend beyond the desired sleep period,
however, resulting in daytime sedation or functional
impairment. Patients with daytime anxiety may benefit
from the residual anxiolytic effect of a long-acting
benzodiazepine administered at bedtime.
Benzodiazepines with intermediate half-lives, such as
temazepam (Restoril), facilitate sleep onset and mainte-
nance with less risk of daytime residual effects.
G.Benzodiazepines with short half-lives, such as
triazolam (Halcion), are effective in promoting the
initiation of sleep but may not contribute to sleep mainte-
nance.
H.Sedating antidepressants are sometimes used as an
alternative to benzodiazepines or benzodiazepine
receptor agonists. Amitriptyline (Elavil), 25-50 mg at
bedtime, or trazodone (Desyrel), 50-100 mg, are
common choices.
References: See page 255.
Nicotine Dependence
Smoking causes approximately 430,000 smoking deaths each
year, accounting for 19.5% of all deaths. Daily use of nicotine
for several weeks results in physical dependence. Abrupt
discontinuation of smoking leads to nicotine withdrawal within
24 hours. The symptoms include craving for nicotine,
irritability, frustration, anger, anxiety, restlessness, difficulty
in concentrating, and mood swings. Symptoms usually last
about 4 weeks.
I.Drugs for treatment of nicotine dependance
A.Treatment with nicotine is the only method that produces
significant withdrawal rates. Nicotine replacement comes
in three forms: nicotine polacrilex gum (Nicorette), nicotine
transdermal patches (Habitrol, Nicoderm, Nicotrol), and
nicotine nasal spray (Nicotrol NS) and inhaler (Nicotrol).
Nicotine patches provide steady-state nicotine levels, but
do not provide a bolus of nicotine on demand as do sprays
and gum.
B.Bupropion (Zyban) is an antidepressant shown to be
effective in treating the craving for nicotine. The symptoms
of nicotine craving and withdrawal are reduced with the use
of bupropion, making it a useful adjunct to nicotine replace-
ment systems.
Treatments for nicotine dependence
Drug Dosage Comments
Nicotine gum 2- or 4-mg Available OTC; poor
(Nicorette) piece/30 min compliance
Nicotine patch 1 patch/d for 6- Available OTC; local
(Habitrol, 12 wk, then taper skin reactions
Nicoderm for 4 wk
CQ)
Nicotine nasal 1-2 doses/h for Rapid nicotine deliv-
spray 6-8 wk ery; nasal irritation
(Nicotrol NS) initially
Nicotine in- 6-16 cartridges/d Mimics smoking be-
haler (Nicotrol for 12 wk havior;
Inhaler) provides low doses
of nicotine
Bupropion 150 mg/day for 3 Treatment initiated 1
(Zyban) d, then titrate to wk before quit day;
300 mg contraindicated with
seizures, anorexia,
heavy alcohol use
C.Nicotine polacrilex (Nicorette) is available OTC. The
patient should use 1-2 pieces per hour. A 2-mg dose is
recommended for those who smoke fewer than 25
cigarettes per day, and 4 mg for heavier smokers. It is
used for 6 weeks, followed by 6 weeks of tapering.
Nicotine gum improves smoking cessation rates by about
40%-60%. Drawbacks include poor compliance and
unpleasant taste.
D.Transdermal nicotine (Habitrol, Nicoderm, Nicotrol)
doubles abstinence rates compared with placebo, The
patch is available OTC and is easier to use than the gum.
It provides a plateau level of nicotine at about half that of
what a pack-a-day smoker would normally obtain. The
higher dose should be used for 6-12 weeks followed by
4 weeks of tapering.
E.Nicotine nasal spray (Nicotrol NS) is available by
prescription and is a good choice for patients who have
not been able to quit with the gum or patch or for heavy
smokers. It delivers a high level of nicotine, similar to
smoking. Nicotine nasal spray doubles the rates of
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