Sedative Hypnotics

-mildest form of sedation

-diminishes physical and mental response at
lower dosage of certain CNS depressants but
doesn't affect consciousness.
-used mostly at daytime
-increasing the drug may cause hypnotic effect
in w/c is a form of natural sleep.

Sedatives- first prescribed to reduce tension and

anxiety

Hypnotics- one of the most prescribed drugs

because of high incidence of sleep

Types of Hypnotics
short-acting
-useful in achieving sleep because they allow
the client to awaken early in the morning w/out
experiencing lingering effects.
Intermediate-acting
-useful for sustaining sleep
-side effects: residual drowsiness/ hangover in
the morning
 Categories of Sedative Hypnotics
1.Barbiturates
-2000 have been developed but 12 marketed

Classification of Barbiturates

long-acting
-used to control seizures in epilepsy
-ex: phenobarbital and mephobarbital

Mephobarbital (Mabaral)
-to control convulsive episodes of agitation, anxiety
and delirium tremens
-pregnancy category C
-t ½: 34 hrs

intermediate
-asleep sustainers for maintaing long periods of
sleep.
-taken 1 hr for the onset of sleep
-vital signs should be monitored
 Butabarbital soduim (Butisol soduim)
-to relieve anxiety and short term hypnotic
insomnia.
-pregnancy category D
-t ½: 60-120 hrs.
-avoid alcohol w/ barbiturates

short-acting
-used to induce sleep for those who have
difficulty falling asleep.
-ex: secobarbital (seconal) and pentobarbital
sodium (Nembutal)

Secobarbital Sodium (Seconal)

-pregnancy category D
-action: depression of CNS, including the motor
and sensory activities
-therapeutic effects: to treat insomnia, used for
sedation, preoperative medication
-contraindications: respiratory depression, severe
hepatic disease, pregnancy (fetal immaturity)
_special precautions: liver or kidney dysfunction,
elderly, children and debilitated individuals.
Ultrashort-acting
-thiopental sodium (Pentothal), used as general
anesthesia

2. Benzodiazepines
-increases the action of inhibitory
neurotransmitter gamma amino-butyric acid
(GABA) to GABA receptors.
-several benzodiazepines as hypnotics:
ex. Flurazepam Hcl (Dalmane)
-for insomnia, pregnancy category X, t ½ :
2-3 hrs
Temazepam (Restoril)
-treats insomnia and decrease nocturnal
awakenings.
Triazolam (Halcion)
-for management of insomnia
-to avoid tolerance avoid taking >7-10 days
-preganancy category X, t ½: 2-4 h.
Estazolam (ProSom)
-treatment for insomnia
-decreases frequency of nocturnal awakening
-pregnancy cat. X, t ½: 10-24 h.
--all can suppress the stage 4 of NREm sleep
except temazepam

3. Nonbenzodiazepines
-short term treatment 9,10 days) of insomnia
-duration of action: 6-8 h.
-short life: 2-2.5 h
-metabolized in liver to inactivate to 3
metabolites & excreted in bile, urine and feces.
-ex: zolpidem tartrate, ezopiclone (Lunesta),
zaleplon (Sonata)

Zolpidem tartrate (Ambien)

pregnancy category: B
action: depression of CNS and neurotransmitter
inhibition
contraindications: hypersensitivity to
benzodizepine, lactation
adverse reaction: tolerance, psychologic/physical
dependence
side effects: drowsiness, lethargy, hangover, a
bulging fontanels in infants
Chloral Hydrate
-used to induce sleep & decreases nocturnal
awakenings
-doesn't suppresses REM sleep
-taken w/ water to prevent gastric irritation

Sedatives and Hypnotics for older Adults

-indentify first the cause of insomnia in an older
adult
-barbiturates increase CNS depression in
adults& shouldn't be taken for sleep.
-safer than barbiturates: estazolam (ProSom),
temazepam (Restoril) and triazolam (Halcion)
-avoid: flurazepam (Dalmane), quazepam
(Doral), Diazepam (Valium)
 Anesthetics

General anesthetics
-depresses the CNS. Alleviate pain and cause
loss of consciousness

Pathophysiology
1. the lipid structure of the cell membranes is
altered, resulting in impaired physiologic
functions.
2. The inhibitory neurotransmitter GABA is
activated to GABA receptor that pushes
chloride ions into the neurons. This greatly
decreases the fire action potentials of the
neurons
3. the ascending reticular activating system is
altered, and the neurons cease to transmit
information (stimuli) to the brain.
Intravenous Anesthetics
-may be used for general anesthesia
-thiopental sodium (Pentothal): for short term
surgery and rapid stage of induction of anesthesia
-ex: droperidol (Innovar), etomidate (Amidate)
and ketamine hydrochloride (Ketalar)
-midazolam (Versed) and profol (Diprivan):
conscious sedation for minor surgery like
mechanical ventilaton/intubation

Profol (Diprivan)
-supports microbial growth and may risk of
bacterial sepsis, discard vials w/in 6 hrs.
Topical Anesthesia
-decrease the sensitive nerve endings of the
affected area.
-the use is limited to mucous membranes,
broken or unbroken skin surfaces and burns.
-different forms: sol., liquid, spray, ointment,
cream, gel and powder