Continuum ranging from
relaxation, to sedation, to
anesthesia
Sedatives:
Relaxes the
patient
Hypnotics:
Induces sleep in
the patient
Sedative-hypnotic:
Calms at lower
doses, causes sleep
at higher doses
Tranquilizers:
Produces a calm
or tranquil feeling
Withdrawal can cause
fever; psychosis; seizures;
tachycardia; hypotension;
anorexia; muscle cramps;
memory, concentration,
and orientation
impairment; abnormal
sounds in the ear; blurred
vision; and insomnia,
agitation, and anxiety
Obvious symptoms last
2-4 wks; subtle can last
months
Antidepressants
Treats GAD, OCD,
panic, social phobia,
and PTSD
Can reduce the
negative thoughts
associated
w/anticipatory
component of panic
Can also suppress ANS,
helping pt. remain
calm
SSRIs: Safer
and w/less
sympathomimetic
&
anticholinergic
effects
Atypicals, including
SNRIs: Side effects
include abnormal
dreams, sweating,
constipation, dry
mouth, anorexia,
weight loss, tremor,
abnormal vision, and
loss of sexual desire
TCAs: Annoying
anticholinergic effects,
such as dry mouth,
blurred vision, urine
retention, and
hypertension
Not recommended
for pt. with a history
of heart attack,heart
blocks, or
arrhythmia.
Most are pregnancy
category C or D
Alcohol or other CNS
depressants are off
limtis
Pt. w/ asthma, GI disorders,
alcoholism, schizophrenia, or
bipolar should be cautious
MAOIs: Can cause
orthostatic hypotension,
headache, and diarrhea,
Pt. should strictly
avoid foods
containing tyramine
Potentiate
effects of insulin
& other diabetic
drugs
Rarely used due to
potential for severe
adverse effects
Benzodiazepines
Most widely prescribed
in medicine
Act by binding to GABA
receptor-chloride channel
molecule, which intensifies
effects of GABA
Most are metabolized in
liver & excreted in urine
Does not cause
life-threatening
respiratory depression
unless taken in large
quantities, combined
w/other CNS depressions,
or given to pt. w/sleep
apnea.
Shortens length of
time to get to sleep
and reduces
frequency of
interrupted sleep
Most increase total
sleep time, btut some
reduce stage 3 and
some affect REM
Can be used for seizure
disorders (Valium),
alcohol withdrawal,
central muscle
relaxation, and general
anesthesia.
Many of these have
the same actions
and adverse effects,
and differ primarily
in onset and
duration of action.
Preferred for
short term
treatment of
insomnia
caused by
anxiety.
Class IV drugs
Barbiturates
Treatment of choice for
anxiety and insomnia
prior to introduction of
benzos
Rarely, if ever, given for
anxiety or insomnia
anymore b/c of significant
adverse effects and better
medications
Risk of dependence is high;
withdrawal is severe and
sometimes fatal; OD can
cause profound respiratory
depression, hypotension,
and shock
Several are
class II
Bind to GABA
receptor-chloride
channel and intensify
effects of GABA
Capable of depressing
CNS function at all
levels
When taken for
prolonged periods, they
stimulate microsomal
enzymes.
Simulates their
own metabolism,
as well as that of
hundreds of
other drugs
Tolerance can develop to
this drug and to other CNS
depressants, such as
opioids.
Miscellaneous
Used mainly for
social anxiety:
Valproate (Depakote)
Propranolol (Inderal)
and atenolol
(Tenormin)
Used mainly for
insomnia:
Zaleplon (Sonata)
Eszopiclone (Lunesta)
Zolpiden (Ambien)
Anxiolytic &
hypnotic effect
Hypnotic effect
Buspirone (BuSpar):
Mechanism unclear,
but r/t D2 dopamine
receptors in brain
Agonist effects on
presynaptic dopamine
& high affinity for
serotonin
Less likely than benzos
to affect cognitive &
motor performance
Rarely interacts w/other
CNS depressants
Common side effects:
Dizziness, headache, and
drowsiness
Less of a chance of
dependence. May take a
couple weeks to work.
Anxiolytic effect
Zolpidem (Ambien,
Edluar, Intermezzo):
Class IV, short-term insomnia
treatment
Highly specific to GABA
Produces muscle relaxation
and anti-convulsant effects
when given higher than
therapeutic dose
Rapid onset
Impaired liver or kidney
will increase serum lvl of
drug
Use w/ caution in suicidal
patients b/c intentional
overdose can happen.
Adverse effects may include
nausea, dizziness, diarrhea,
daytime drowsiness, amnesia,
and somnambulism
Rebound insomnia can occur
when discontinued
Long-term use allowed
Escopiclone (Lunesta)
Similar properties to
zolpidem
Longer elimination half
life may give it an
advantage over
zolpidem in
maintaining sleep &
decreasing early
morning waking
More likely to cause
daytime sedation
Zaleplon (Sonata)
Useful for ppl who fall
asleep but wake early
in the morning
Sometimes used for travel
Ramelton (Rozerem)
Melatonin receptior
agonist
Shown to improve sleep
induction
Short onset of action,
lasts as long as XR
zolpidem
Long-term use allowed
Hypnotic effect
Tasimelteon (Hetlioz
Melatonin receptor agonist
Treatment of non-24
hour sleep-wake disorder
Most common effects
are headaches and
uncommon dreams
Avoid concurrent
use w/ fluvoxamine
(Luvox) or rifampin
(Rifandin)