Central Nervous

System Depressants
 Physiology of Sleep
Hypnotics- are used to induced

Sleep- is a recurrent, normal condition of inertia and

unresponsiveness during which an individual’s overt
and covert responses to stimuli are markedly reduced
-during sleep a person is no longer in sensory contact
with the immediate environment and stimuli that
bombard the senses of sight, hearing, touch, smell, and
the taste during the waking hours.
Types and Stages of Sleep

☺Nonrapid Eye Movement (NREM) Sl

eep

☺Rapid Eye Movement (REM) Sleep

*DIAGRAM
Next
Nonrapid Eye Movement Sleep

-an individual moves through the four stages of non-

REM sleep:
Four stages of non-REM sleep
Stage 1:
♦ Dozing or feelings of drifting off to sleep
♦ Person can be easily awakened
♦ Insomniacs have longer stage 1 periods than
normal
*DIAGRAM
Nonrapid Eye Movement Sleep

Stage 2:
♦ Person is relaxed but can be easily awakened
♦ Has occasional REM and also some slight eyeball
movements
Stage 3:
♦ Deep sleep, difficult to wake person up
♦ Respirations, pulse, and blood pressure may decrease

*DIAGRAM
Nonrapid Eye Movement Sleep

Stage 4:
♦ Sleepwalking or bedwetting may occur
♦ Person very hard to wake up. If awakened, may be very
groogy
♦Dreaming, especially about daily events

Back *DIAGRAM
Rapid Eye Movement (REM) Sleep

♦ individuals experiencing most of their recallable dreams.

♦ children have a few REM sleep periods and have longer

periods of stage 3 and 4 NREM sleep.

♦Older adults experience a decrease in stages 3 and 4 of

NREM sleep and have frequent waking periods.

♦ longer during the sleep process

Rapid Eye Movement (REM) Sleep

♦ If a person is roused from REM sleep, a vivid, bizarre

dream may be recalled.

♦ respirations may be irregular

 Stage 2
(50%)

Stage 1
(2%-5%)
Stage 3
(5%)
Stage 4
REM sleep (10%-15%)

Back
 Physiology of Sleep
Hypnotics- are used to induced

The following occurs during nondreaming sleep

•Blood pressure falls by 10 to 30 mmHg

•Pulse rate is slowed

•Metabolic rate is decreased

•Gastrointestinal tract activity is slowed

•Urine formation is slowed

•Oxygen consumption and carbon dioxide production

 Physiology of Sleep
Hypnotics- are used to induced

are lowered

• Body temperature is decreased slightly

• Respirations are slower and shallower

• Body movement is minimal

 Nonpharmacologic Methods

♦ Arise at specific hour in the morning

♦ take few or no day time naps

♦ avoid drinks that contain caffeine 6 hours before bedtime

♦ avoid heavy meals or strenuous exercise before bedtime

 Nonpharmacologic Methods

♦ take a warm bath, read, listen, to music before

bedtime

♦ decrease exposure to loud noises

♦ avoid drinking copious amounts of fluids before sleep

♦Drink warm milk before bedtime

Sedative-Hypnotics
 S
Anxiety-
e
Anxiety is a state or feeling of apprehension, uneasiness, d
agitation, uncertainty, and resulting from the anticipation of a
some threat or danger, usually of intrapsychic origin, whose t
source are generally unknown or unrecognized.
i
v
Sedatives-
Sedatives are central nervous system (CNS) depressants
e
drugs that were commonly prescribed H
y
-diminishes physical and mental responses at lower p
dosages of certain CNS depressants but does not affect n
consciousness. o
t
i
c
 - reduce
Hypnotics- nervousness,
are used to induced excitability, or irritability by
producing a calming or soothing effects.

Hypnotics- are used to induced sleep.

Two types of Hypnotics:

 Short-acting hypnotics

- are useful in achieving sleep, because they allow the client

to awaken early in the morning without experiencing
lingering side effects.
Intermediate-acting hypnotics
Hypnotics- are used to induced

-are useful for sustaining sleep

-however after using one the client may experience residual

drowsiness, or hangover, in the morning.
 Sedative-Hypnotics

♦ sedatives was first prescribed to reduce tension and

anxiety

♦ hypnotic drug therapy should be short-term to prevent

drug dependence and drug tolerance

♦Clients with severe respiratory disorders should avoid

hypnotics, which could cause an increase in respiratory
distress

♦Hypnotics are contraindicated during pregnancy

 Sedative-Hypnotics

♦Hypnotic effect- increasing the drug dose, not hypnosis but

a form of “natural” sleep

♦ with very high doses anesthesia may be achieved (eg.

Thiopental sodium (Penthotal)
Difference between
Hypnotics- are used to induced sedatives and hypnotics

-the degree of CNS depression induced

- a small dosage may be used for a sedative effect, and

larger dosages may be used for hypnotic effects.
 Sedative-Hypnotics

Categories

ф Barbiturates

ф Benzodiazepines

ф Nonbenzodiazepines
 Barbiturates

-Examples: pentobarbital, secobarbital (Seconal), butabarbital

(Butisol), amobarbital (Amytal), phenobarbital (Levotan)

Classified ♦ long-acting
into:
♦ intermediate-acting

♦ short-acting
Back
♦ ultrashort-acting
 Barbiturates
Mechanism of Action:

 act by enhancing and/or mimicking the synaptic

action of gamma-aminobutyric acid (GABA), an
inhibitory neurotransmitter

 the sedative-hypnotic action of it may be due to

an inhibition of conduction in the reticular formation
resulting in a decrease in the number of impulses
reaching the cerebral cortex
 Barbiturates
Indications:
 adjuncts to anesthesia and treatment of seizure
disorders (e.g. thiopental (Pentothal) and methohexital
(Brevital)

Several are indicated for the treatment of insomnia

(e.g. pentobarbital (Nembutal)

 have been used for their sedative effects in treating

or reducing anxiety and nervousness (e.g. diazepam
(Valium)
 Barbiturates
Pharmacokinetics:
 are readily absorbed after oral rectal and parenteral
administration

Side Effects and Adverse Reactions

 drowsiness, dizziness, hangover effect, nausea,
vomiting, insomnia, constipation, restlessness, faintness,
headache, hypersensitivity reactions (skin rash, edema,
apnea, bronchospasm, Stevensons-Johnson’s syndrome
 older, or debilitated clients, may exhibit confusion,
disorientation, and mental depression
 Barbiturates
Nursing Responsibilities

 avoid giving barbiturates to the clients who are

hypersensitive to them or have respiratory conditions
(involving dyspnea or obstruction), a previous dependency on
barbiturates, or renal or hepatic impairment
 avoid giving barbiturates to children and older adults with a
history of paradoxical reactions(
 Barbiturates
Nursing Responsibilities

 If the client is pregnant or may become pregnant during

therapy, she should discuss barbiturate use with nurse-midwife,
nurse practitioner, or physician

 client should skip the dose if it is close to the next dose and
continue with the regimen, doses should not be doubled
 Barbiturates
Nursing Responsibilities

 inform the client not to take any additional medications

while taking a barbiturate unless the drugs have been approved
by the prescriber or the pharmacist

Back
 Long-acting Barbiturates

-examples are: Phenobarbital and amobarbital

-Require more than 60 minutes for onset and peak over a

period of 10 to 12 hours

- used for treating epilepsy and other chronic neurologic

disorders, as well for sedation in clients with high anxiety
 Long-acting Barbiturates
Phenobarbital ( Luminal)

Therapeutic Effects:

-Depressant and anticonvulsant effects may be related to its

ability to increase and/or mimic the inhibitory activity of
GABA on nerve impulses (depress CNS synaptic transmission
and increase seizure activity threshold in he motor cortex)
-As a sedative it may also interfere with the transmission of
impulses from the thalamus to the brain cortex.
 Long-acting Barbiturates
Phenobarbital ( Luminal)

Contraindications:

-Pregnancy (Category D)

-Hypersensitivity to barbiturates, severe renal, hepatic, cardiac

or respiration impairment
 Long-acting Barbiturates
Phenobarbital ( Luminal)

Side Effects/Adverse Reactions:

- Dizziness - blood dsycrasias

- headache - megaloblastic anemia

- hangover - hypotension

- GI disturbances

- allergic reactions
 Long-acting Barbiturates
Phenobarbital ( Luminal)

Pharmacokinetics:

A: Good

D: Wide, 25-30% protein bound

M: Liver

E: kidneys (25% unchange)

T½: 5-7 days

 Long-acting Barbiturates
Phenobarbital ( Luminal)

Pharmacodynamics:

PO IM IV

Onset 20-60 mins >60 mins 5 mins

Peak Unknown Unknown > 15 mins

Duration 10-12 hours 10-12 hours 10-12 hours

 Long-acting Barbiturates
Phenobarbital ( Luminal)

Indications

- Short treatment of insomnia

-Long term treatment of generalized tonic-clonic and cortical

focal seizures

- emergency control of acute convulsions

-Preanesthetic sedation
 Long-acting Barbiturates
Phenobarbital ( Luminal)

Dosage

-Taken with food

- oral- tablets may be crushed and mixed with fluid or food.

-100-320 mg/day

-Maximum: 600 mg/day

 Long-acting Barbiturates
Phenobarbital ( Luminal)

Stock Dose:

-Tablets: 15, 16, 30, 60, 90, 100 mg

-capsules: 16 mg

-Elixir: 15 mg/5ml, 20 mg/5 ml

-injection: 30, 60, 65, 130 mg/ml

 Long-acting Barbiturates
Phenobarbital ( Luminal)

Available brands in the Philippines:

-Luminal

-Rhea Phenobarbital

Back
Intermediate-acting Barbiturates

Examples: butabarbital (Butisol)

♦are useful as sleep sustainers for maintaining long

periods of sleep

♦ are not prescribed for those who have trouble getting to

sleep

♦Vital signs should be closely monitored in persons who

take it.
Intermediate-acting Barbiturates

♦ have an onset of 45-60 minutes and peak in 6-8 hours.

♦ used as sedative-hypnotics

Back
Short-acting Barbiturates

- Examples: pentobarbital (Nembutal), secobarbital (Seconal)

-produce an effect (onset) in a relatively short time ( 10-15

minutes) and peak over a relatively short period ( 3-4 hours)

-are used for treating insomnia, for preanesthetic sedation, in

combination with other drugs for psychosomatic disorders
Short-acting Barbiturates
Pentobarbital (Nembutal)

Therapeutic Effects:
-General CNS depressant
-depress the cerebral cortex
-alter cerebellar functions
-depress motor output
-can produce excitation, sedation, hypnosis,
anesthesia, and deep coma
Short-acting Barbiturates
Pentobarbital (Nembutal)

Contraindications:
-hypersensitivity to barbiturates
-marked liver impairment
-severe respiratory distress
-previous-addiction to sedative-hypnotic drugs
-pregnancy (fetal damage, neonatal withdrawal
syndrome )
-lactation
Short-acting Barbiturates
Pentobarbital (Nembutal)

Side effects/adverse effects:

- nausea and vomiting - orthostatic hypotension
- light-headedness - palpitations
- delirium - seizures
- agitation - tremors
- visual disturbances
- arrhythmia
Short-acting Barbiturates
Pentobarbital (Nembutal)

Pharmacokinetics:
A: slow rate; moderately protein bound
D: crosses placenta; enters breast milk
M: Hepatic; half life- 15-50 hours
E: Urine
Route of Administration:
IV, IM
Short-acting Barbiturates
Pentobarbital (Nembutal)

Onset of Action: 10-15 minutes

Duration of Action: 3-4 hours

Indications and Dosage:

Adults: hypnotic, 100 mg PO/IV, 150-200 mg

IM, or 120-200 mg rectally at bedtime. Daytime sedative,
20 mg PO or 30 mg rectally 2-4 times daily.
Preoperataive, 100 mg PO or 150 or 200 mg IM.
Anticonvulsant, 100-500 mg IV.
Short-acting Barbiturates

Pentobarbital (Nembutal)
Indications and Dosage:
Children: sedative-preoperative, 2-6 mg/kg or
maximum 100 mg/dose
Stock Dose:
Injection- 50mg/ml

**Not available in the Philippines

Back
Ultrashort-acting Barbiturates

-Example: Thiopental sodium (Penthotal)

-used as a general anesthetic specifically IV anesthetics

Back
Benzodiazepines
-Examples: flurazepam (Dalmane), temazepam (Restoril),
triazolam (Halcion), estazolam (ProSom), and quazepam
(Doral)

-most widely prescribed drugs in clinical medicine, primarily

because of their advantages over the older agents (e.g.
barbiturates, meprobamate, and alcohol)

-has following advantages:

(1) lower fatality rates with acute toxicity and overdose, (2)
lower potential for abuse,
Benzodiazepines

(3) more favorable side effects/adverse reaction profiles, and

(4) fewer potentially serious drug interactions reported when

administered with other
Benzodiazepines
Mechanism of Action:

 can be used to alleviate anxiety

 increase the action of the inhibitory neurotransmitter

gamma-aminobutyric acid (GABA) to the GABA receptors

 neuron excitability is reduced

 (except for temazepam) can suppress stage 4 of NREM

sleep, which may result in vivid dreams or nightmares and can
delay REM sleep
Benzodiazepines
Mechanism of Action:

 do not exert a general CNS depressant

 pharmacologic properties of this class include muscle

relaxant, antianxiety, anticonvulsant, and hypnotic effects

Indications:

-for anxiety disorders - insomnia

- alcohol withdrawal - seizure disorders

- preoperative medication - neuromuscular disease

Benzodiazepines
Pharmacokinetics:

 oral-are readily absorbed from the gastrointestinal tract

 highly protein bound and lipid soluble and are

excreted by the kidney

 the onset of the anticonvulsant, antianxiety, and

muscle relaxant effects of these agents after IV
administration is approximately 1-5 minutes
Benzodiazepines
Pharmacokinetics:

 Onset of action is approximately 15-30 minutes after

IM injection

Side effects:

- Drowsiness - nausea

- Hiccups - vomiting

- lassitude - loss of dexterity

- nausea
Benzodiazepines
Adverse Effects:

-Increased behavioral problems ( anger, decreased ability

to concentrate)

- insomnia

- increased excitability

- hallucinations

- apprehansions
Benzodiazepines
Nursing Responsibilities:

- determine if the client is hypersensitive to any of it

-Pregnant women should usually avoid using this because

their use in the in the first trimester is associated with an
increased risk of congenital anomalies

- careful titration to individual needs is essential in older

adults
Benzodiazepines
Nursing Responsibilities:

-Baseline assessment of the client should include a

description of the client’s underlying conditions and CNS
and mental status, as well as complete blood count (CBC)
and liver function test

- caution the client not to take more than the prescribed

dosage if the medication seems less effective but to
consult the prescriber
Benzodiazepines
Available in the Philippines:

Generic Brand Names

-Bromazepam Lexotan

-Alprazolam Xanor, Xanor XR

-Clonazepam Rivotril

- Clorazepate Tranxene

- Diazepam Valium
Benzodiazepines
Available in the Philippines:

Generic Brand Names

- estazolam Esilgan

- midazolam Dormicum, Pfizer Midazolam

Benzodiazepines
Flurazepam (Dalmane)

Therapeutic Effects:
- potentiates the action of GABA, an inhibitory
neurotransmitter
- effective in patients with recurring insomnia or
poor sleeping habits
Benzodiazepines
Flurazepam (Dalmane)
Contraindications:
-Hypersensitivity to benzodiazepines
- psychoses
- glaucoma
- shock
- Coma
- use cautiously in the elderly or impaired liver or renal
function, debilitation, depression
 Benzodiazepines
Flurazepam (Dalmane)
Adverse Effects:
-Drowsiness - blood dyscrasias
- sedation - nausea
- depression - diarrhea
- lethargy - dyspepsia
- edema - incontinence
- palpitations - Pruritus
Benzodiazepines
Flurazepam (Dalmane)

Pharmacokinetics:
A- well absorbed in the GI tract
D- Crosses placenta, enters breast milk
M- Hepatic; Half life- 47-100 hours
E- Urine
Benzodiazepines
Flurazepam (Dalmane)

Onset of action: Fast

Duration of action: Long acting
Indications and dosage:
Adults: 15-30 mg PO
Children up to 15 years: not recommended
Stock dose: capsules-15, 30 mg

**not available in the Philippines Back

Nonbenzodiazepines

- example: zolpidem (Ambien), eszopiclone (Lunesta),

zalepton (Sonata)

-Differs from the structure of benzodiazepines

- used for short term treatment ( less than 10 days) of

insomnia
Nonbenzodiazepines
Zolpiden (Ambien)

Therapeutic Effects:

-Sedative, anticonvulsant, anxiolytic, and myorelaxant

that act by subunit modulation of the GABA receptor

Contraindications:

-Pregnancy ( Category C)

-Children <15years
Nonbenzodiazepines
Zolpiden (Ambien)

Contraindications:

- hypersensitivity

-Use cautiously with impaired hepatic or renal

functions, addiction-prone patients

- lactation
Nonbenzodiazepines
Zolpiden (Ambien)

Side Effects/Adverse Effects:

- Seizures - vomiting

- hallucinations - general allergic reactions

- morning drowsiness - angioedema

- constipation

- nausea
Nonbenzodiazepines
Zolpiden (Ambien)

Pharmacokinetics:

A- Rapidly absorbed from GI tract. Absolute

bioavailability: 70%. Food reduce both the rate and
extent of GI absorption.

D- Protein binding: 92%. Distributed into breast milk.

Nonbenzodiazepines
Zolpiden (Ambien)

Pharmacokinetics:

M- Undergoes first pass metabolism

E- Excreted in urine and faeces as inactive metabolites.

T½- 2 ½ hours
Nonbenzodiazepines
Zolpiden (Ambien)

Pharmacodynamics:

Onset Rapid

Peak 30 mins- 2 hours

Duration Unknown
Nonbenzodiazepines
Zolpiden (Ambien)

Indication:

-Short-term treatment of insomnia

Dosage:

-before bed time on an empty stomach

-Adult: PO, 10 mg stat before bedtime

Nonbenzodiazepines
Zolpiden (Ambien)

Dosage:

-Elderly, debilitated or hepatic insufficiency patients:

5 mg dose , maximum dose: not exceeding 10 mg

Nonbenzodiazepines
Zolpiden (Ambien)

Stock Dose:

-Tablets: 5, 10 mg

-ER tablets: 6.25, 12.5 mg

-oral spray: 5, 10 mg
 Nonbenzodiazepines

Zolpiden (Ambien)

Available Brands in the Philippines:

-Stilnox

-Ziohex

-Zoldem
Chloral hydrate

- Use to induce sleep and decrease nocturnal awakenings

-It does not suppress REM sleep

-Less occurrence of hang-over, respiratory depression,

and tolerance with it than with other sedative-hypnotics

-Its use is effective in older adults

Chloral hydrate

-Can be given to clients with mild liver dysfunction

- gastric irritation may occur, so the drug must be given

with sufficient water