8 Cns Stimulants

Central Nervous
System Agents
LOURADEL U. ULBATA, MAN RN
CNS
Stimulants
CNS stimulants are drugs
which increase the muscular
(motor) and the mental
(sensory) activities
Their effects vary from the
increase in the alertness and
wakefulness (as with
caffeine) TO the production
of convulsion ( as with
strychnine) or death due to
over stimulation

Behavioral Manifestations of CNS
Stimulation
mild elevation in alertness, decrease in
drowsiness and lessening of fatigue
(Analeptic Effect)
increased nervousness and anxiety -
convulsions.

Molecular Basis of CNS
Stimulation
Imbalance between inhibitory and excitatory
processes as in the brain. This
hyperexcitability of neurons results from:
potentiation or enhancement of excitatory
neurotransmission(e.g. amphetamine)
depression or antagonism of inhibitory
transmission (e.g. Strychnine)
presynaptic control of neurotransmitter
release (e.g. picrotoxin)

Classification of CNS
Stimulants
Analeptic Stimulants
Respiratory Stimulants
Convulsants
Psychomotor Stimulant
Sympathomimetics or
Adrenergic CNS Stimulants
Methylxanthines

Analeptic Stimulants
diverse chemical class of agents
majority can be absorbed orally
have a short duration of action -
primary expression of
pharmacological effect is
convulsions (tonic-clonic)
uncoordinated
pharmacological effect is
terminated through hepatic
metabolism
Possible Common Mechanism of
Action -ability to alter movement of
chloride ions across neuronal
membranes

Doxapram - used to counteract postanesthetic
respiratory depression and for acute
hypercapnia in chronic pulmonary disease.
Used with caution with neonatal apnea
Administered IV
Onset of action: within 20-40 secs
SE: (overdose)
Hypertension
Tachycardia
Trembling
convulsions

Respiratory CNS
Stimulants
Headaches: Migraine and
Cluster
Migraine headaches-
characterized by a unilateral
throbbing head pain,
accompanied by N/V and
photophobia
Cluster headaches-
characterized by severe
unilateral nonthrobbing pain
usually located around the
eye. Usually not associated
with N/V
Preventive Treatment for
migraine

1. Beta adrenergic blockers
2. Anticonvulsants- Valproic
acid (Depakote)
3. Tricyclic antidepressants-
amitriptyline (Elavil)
Treatment or Cessation of
Attacks
Ergotamine tartrate
Nonspecific serotonin agonist and
vasoconstrictor
Should be taken early during a
migraine attack
May cause N and V

Triptans
The most common recently developed group of
drugs for tx of migraines and cluster headches
Prototype: sumatriptan(Imitrex)
Selective serotonin receptor agonist with a short
duration of action
Considered more effective than ergotamine
MOA: causes vasoconstriction of cranial carotid
arteries to relieve migraine attacks
SE: dizziness, fainting, tingling, numbness, warm
sensation, drowsiness
AR: hypotension, heart block, angina, MI, cardiac
arrest

Amphetamines
Stimulates the release of
norepinephrine and dopamine from the
brain and SNS.
Can cause euphoria and alertness
CHARACTERISTICS
all compounds are absorbed well orally
large portion of untransformed amphetamine is
excreted unchanged in the urine. Consequently,
acidifying the urine with ammonium chloride
hastens its clearance, and thus reduces its
reabsorption in the renal tubules.
Overdose: hyperreflexia, tremors, convulsions and
irritability
CV problems: increased heart rate, increased BP,
palpitations and cardiac dysrythmias

Therapeutic Uses:
Narcolepsy
Characterized by falling asleep during waking hours,
such as driving a car or talking with someone. Sleep
paralysis, a condition that is normal during sleep
usually accompanies narcolepsy which affects the
voluntary muscles making the person unable to move
and collapse
Therapeutic uses:
Attention Deficit/Hyperactivity Disorder
May be caused by disregulation of
serotonin, norepinephrine, and dopamine.
Occurs primarily in children, usually before
the age 7, but may continue through
teenage years.
Characteristics involved include
inattentiveness, poor coordination, inability
to concentrate, restlessness, hyperactivity
(excessive and purposeless activity),
inability to complete tasks, and impulsivity.
Pharmacological Actions
The primary effects of an oral dose are
wakefulness, alertness, decrease fatigue; mood
elevation, increased ability to concentrate; an
increase in motor and speech activity.
Amphetamines also diminish the awareness of
fatigue; person may push exertion to the point of
severe damage or even death.

Stimulate the respiratory center,
especially when respiration is
depressed by centrally acting drugs,
(barbiturates and alcohol).
Amphetamine can reverse the marked
sedation and behavioral retardation
resulting from reserpine-like drug.
Depresses appetite by their action on
the lateral hypothalamus rather than
an effect on metabolic rate.

Mechanisms of Action
Releases monoamines at synapses
in the brain and spinal cord.
Inhibits neuronal uptake of
monoamine
Antagonist at certain
adrenoreceptors
May inhibit monoamine oxidase.

Adverse Effects
CNS: Euphoria, dizziness, tremor,
irritability, insomnia, Convulsion (at
higher doses), hyperthermia and
coma
C.V. Cardiac stimulation leads to
headache, palpitations, cardiac
arrhythmias, anginal pain
Other: Weight loss, Psychotic
Reaction which are often
misdiagnosed as schizophrenia.
Addiction - including psychic
dependence, tolerance and physical
dependence.

Drug Interactions:
Tricyclic antidepressant
Antihypertensive Agents
Foods high in tyramine content

Amphetamine-like Drugs or ADHD and
Narcolepsy
Given to increase a childs attention span and
cognitive performance and decrease
impulsiveness, hyperactivity and restlessness
Prototype:
Methylphenidate(Ritalin)
Dexmethypendate (Focalin)
Pemoline (Cylert)
Modafinil(Provigil)- drug for nacolepsy which
increases the amount of time that clients feel
awake

Side Effects:
anorexia, vomiting,
diarrhea, insomnia,
dizziness, nervousness,
restlessness, irritability
Adverse reaction:
tachycardia, growth
suppression,
palpitations, transient
loss of weight in
children, and increased
hyperactivity
Nursing considerations:
Monitor V/S. report
irregularities
Record height, weight, and
growth of children
Observe for withdrawal
symptoms (N and V,
weakness, and headache)
Monitor for side effects

Nursing considerations
Instruct client to take drug with meals
Avoid alcohol consumption
Encourage use of sugarless gum to relieve
dryness of mouth
Monitor weight twice a week
Advise not to drive and use hazardous
equipments when experiencing palpitation,
nervousness, tremors
Instruct client not to discontinue the drug
abruptly
Advise not to eat foods with caffeine
Instruct to eat nutritious food because
drug may cause anorexic effect
Teach to report drug side effects such as
tachycardia and palpitations
CNS
Depressants
CNS Depressants: Classification
They are classified according to their
pharmacological action into:
1- Sedative hypnotics
2- Anaesthetics
Sedativ
e
-
Hypnoti
cs
Mildest form of CNS depression

Diminishes physical and mental responses at
lower dosages of certain CNS depressants but
does not affect consciousness

Sleep
Definition:
Physiological depression of consciousness
Sleep cycle:
Starts with latency period NREM REM cycles of NREM alternate
with REM (about 4 cycles)
NREM REM
- Non rapid eye movement
- Lasts for 90 min.
- Thinking
- Rapid eye movement
- Lasts for 20 min.
- Dreaming
I- Sedative - Hypnotics
Definitions

Sedatives:
Drugs which calm the patient & cause sedation and in large
doses cause sleep

Hypnotics:
Drugs which induce sleep that resembles the natural sleep

Ex. Barbiturates
Sedative Hypnotics
Mechanism of Action
The GABA receptor is a pentameric structure that
forms a Cl
-
channel.

The receptor complex includes distinct binding
sites for benzodiazepines, barbiturates and
GABA-like substances.

GABA transmission exerts an inhibitory effect on
norepinephrine (NE), dopamine (DA), serotonin
(5-HT), and acetylcholine (ACh) pathways.

Sedative-hypnotics
Barbiturates

1-Long acting (12-24 hr)
Ex. Phenobarbital

2-Intermediate acting (8-
12hr)
Ex. Amobarbital
3-Short acting (4-8 hr)
Ex. Pentobarbital
4-Ultrashort acting (0.5-
1hr)
Ex. Thiopental
Non-barbiturates
Benzodiazepines Non- benzodiazepine
MOA:
They have GABA like action opening time
of chloride channels conductance of
chloride ions hyperpolarization

Classification:
1-Long-acting
2-Intermediate-acting
3-Short acting
4-Ultrashort acting

Barbiturates
Prototype:
Short acting: pentobarbital
sodium(Nembutal sodium) for
sedation, sleep, or preanesthetic
Intermediate acting: amobarbital
sodium(Amytal sodium)- sedative
and short term hypnotic, to control
acute convulsive episodes, and for
insomia
Long acting: phenobarbital and
mephobarbital-used to control
seizures
Ultrashort-acting: thiopental
sodium- used as a general
anesthetic

Recognize that continued use of
barbiturate might result in drug abuse
Monitor V/S, esp. RR and BP
Raise side rails
Check for rashes
Administer phenobarbital IV at a rate of
less than 50mg/min. do not mix with other
medications. If to be given IM, use large
muscle such as the gluteus max
Client teaching
Teach client the use on non pharmacological
ways to induce sleep----enjoying a warm bath,
listening to music, drinking warm fluids, and
avoiding drinks with caffeine 6hrs before
bedtime
Instruct to avoid alcohol and antidepressants,
antipsychotics, and narcotic drugs----
respiratory depression
Avoid taking herbs
Advise not to drive or operate a machinery
Instruct to take 30mins before bedtime

Benzodiazepines
Can suppress stage 4 of NREM sleep, which may result
in vivid dreams or nightmares and can delay REM sleep.
Effective for sleep disorders for several weeks longer
than other sedative-hypnotics but should not be longer
than 3-4 weeks as a hypnotic to prevent REM rebound
Prototype:
Alprazolam(Xanax)- for alleviating anxiety that may cause
sleeplessness
Estazolam(ProSom)- for treatment of insomia. Decreases
the frequency of nocturnal wakefulness
Lorazepam(Ativan)-used as a pre operative sedative and
to reduce anxiety
used for short term treatment of insomia
Well absorbed PO, onset 7-27 minutes
MOA: depression of the CNS, neurotransmitter
inhibition

Prototype:
zolpidem(Ambien)
S/E: drowsiness, lethargy, hangover, irritability,
dizziness, anxiety
Adverse reactions:
tolerance, physiologic dependence

Nursing responsibilities:
Monitor V/S. check for respiratory depression
Raise side rails
Observe for side effects (hangover, light-
headedness, dizziness, or confusion)
Teach non pharmacological ways to induce
sleep
Suggest to urinate before taking sedative
hypnotics to prevent sleep disruption
Instruct to avoid alcohol and antidepressants,
antipsychotics, and narcotic drugs----
respiratory depression
Anaesthetics
Definition:
Drugs which cause unconsciousness &
generalized loss of pain sensation, thus
allow surgical procedures to be carried out
Classified as general and local
Ex. thiopental (IV) , halothane (inhalation)

MOA:
Interfering with propagation of nerve impulses
by interfering with electrolytes movement
through the cell membrane

General anesthesia
Is a reversible loss of consciousness induced by
inhibiting neuronal impulses in several areas of the
central nervous system
General anesthetics are agents that block the pain
stimulus at the cortex

Produces a state of the ff:
Analgesia
Amnesia
Unconsciousness characterized by loss of reflexes
and muscle tone

Injection of a solution containing anesthetic
into the tissues at the planned incision site.
Briefly disrupts sensory nerve impulse
transmission form a specific body area or
region.
Types of Local anesthesia
1. Topical anesthesia topical agents are
applied directly to the area of skin or mucous
membrane surfaced to be anesthetized

2. Local infiltration is the injection of an
anesthetic agent directly into the tissue
around an incision, wound, or lesion.

Purposes of Anesthesia
To produce muscle relaxation
To produce analgesia
To produce artificial sleep or to cause loss
of consciousness
To block transmission of nerve impulses
To suppress reflexes

Nursing responsibilities:
Monitor clients postoperative state of
sensorium.
Check preoperative and postoperative urine
output
Record V/S after induction of anesthesia----
may result to hypotension and respiratory
distress
Administer an analgesic or a narcotic-
analgesic with caution until client fully
recovers from the anesthetic

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Central Nervous

Mildest form of CNS depression

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