CENTRAL NERVOUS

SYSTEM AGENTS
CARMENCITA R. PACIS PhD, MAN
 LEARNING OBJECTIVES:
At the end of the course unit (CU), learners will be able to:
• Understand the basic concept of drugs affecting the
• Central Nervous System
• Classify Neurotransmitters that affect nervous function
• Comprehend the basic impulse transmission in the nervous
system to understand pharmacodynamics of drugs affecting
the nervous system
• Identify classifications of drugs affecting the CNS
• Describe the specific actions of drugs and its adverse effects.
• Understand the pharmacokinetics of drugs affecting the
nervous system
• Determine specific nursing considerations or precautions in
safe drug administration
• Provide appropriate health drug education related to drug
therapy
• Use available clinical evidence that can ensure safe
medication administration
 CENTRAL NERVOUS SYSTEM (CNS)
MEDICATIONS

A. CNS
Stimulants
• STIMULANT – a
substance that
quickens the activity of
the CNS by increasing
the rate of neuronal
discharge or by
blocking an inhibitory
neurotransmitter.
• Classification: CNS Stimulants
• Amphetamines
• Anorexiants
• Analeptics
 1. AMPHETAMINES AND
AMPHETAMINE-LIKE DRUGS
Action: stimulate the release
of norepinephrine, which
causes increased alertness,
less fatigue and elevate the
mood.
Common drugs:
• Methylphenidate
(Ritalin, Concerta) – for
ADHD most commontly
• Dextroamphetamine
sulfate (Dexedrine,
adderall)
• Methamphetamine HCL
(Desoxyn)
 METHYLPHENIDATE
• Methylphenidate (MPH) non-competitively
blocks the reuptake of dopamine and
noradrenaline into the terminal by blocking
dopamine transporter (DAT) and
noradrenaline transporter (NAT),
increasing levels of dopamine and
noradrenaline in the synaptic cleft.
• Attention Deficit hyperactivity Disorder
(ADHD) - Childhood condition involving
inattention, impulsivity and
hyperactivity
• Amphetamine increase attention span
while decreasing the hyperactivity
 METHAMPHETAMINE
HYDROCHLORIDE

• CLASSES - Psychostimulants, Amphetamines

• Desoxyn/Methamphetamine Hydrochloride Oral Tab:
5mg
• significantly increased the overall amount of
glutamate.
Other Uses:
Narcolepsy -
Characterized by sudden
sleep attack
Endogenous obesity -
Obesity resulting from
dysfunction of the
endocrine or metabolic
systems. Amphetamines
suppress the appetite
Mental depression –
elevate the mood.
Nursing Implications:
• Weight reduction diet and exercise
program should accompany the use of
these agents for obesity. Short term is
recommended
• Do not abruptly stop taking the drugs
• Do not try to make up dose if one is
skipped
• Avoid other stimulants while on these
drugs
• Avoid taking the last dose after 4 to 6
PM to prevent insomnia
 2. ANOREXIANTS
Action: suppress the appetite by acting on the
hypothalamus
Use: weight reduction when accompanied by medical
complications
Tolerance and abuse are possible
Common drugs:
• Benzphetamine HCL (Didrex)
• Diethylpropion (tenuate, Tepanil, Dospan)
• Phenmetrazine HCL (Preludin)
• Phentermine HCL ( Adipex-P, lonamin)
• Dextroamphetamine sulfate (Dexedrine)
 BENZPHETAMINE HCL
• similar to that of amphetamines. Amphetamines
stimulate norepinephrine and dopamine release in
nerve endings in the lateral hypothalamic feeding
centre, decreasing appetite.
 PHENTERMINE
• Phentermine (Adipex): Phentermine is
the most commonly prescribed
weight loss medication. It is an
adrenergic agonist that increases the
release of norepinephrine in the
hypothalamus. Norepinephrine
release induces appetite suppression
and increases resting energy
expenditure.
 3. ANALEPTICS
Action: stimulates the CNS by acting on the cerebral
cortex and the medulla
Uses:
• Respiratory stimulation→ primary use
Common drugs:
• Methylxanthines: theophylline (used for asthma),
theobromide
• Respiratory stimulant: Doxapram HCL (Dopram)
• Caffeine induces dopamine and glutamate release in
the shell of the nucleus accumbens.
 THEOPHYLLINE
• Theophylline relaxes the
smooth muscle of the
bronchial airways and
pulmonary blood vessels and
reduces airway
responsiveness to histamine,
methacholine, adenosine,
and allergen.
• Beta 2 agonist -
bronchodilation
 DOXAPRAM
• Doxapram is a respiratory
stimulant with analeptic activity.
Doxapram, independent of
oxygen levels, directly stimulates
the peripheral carotid
chemoreceptors, possibly by
inhibiting the potassium
channels of type I cells within
the carotid body, thereby
stimulating catecholamines
release.
Major side Effects:
CV: dysrhythmias, heart attacks, tachycardia, HPN,
tachypnea
• Caffeinism: restlessness, insomia, nervousness, muscle
twitching, headache
• Seizures
• Tolerance and abuse

Nursing implication
• Monitor the dietary intake of caffeine
• Assess respiratory and CV systems
• Watch for withdrawal symptoms: nausea, vomiting,
headache
• Avoid other foods and drinks that contain stimulants
 CNS DEPRESSANTS
• Sedative-hypnotics
• Anesthetics
• Anticonvulsants
• Anxiolytics
• Antidepressants
 1. SEDATIVE-HYPNOTICS
• SEDATIVE- agent that produces a state of calmness
• HYPNOTIC- an agent given at bedtime to induce
sleep (usually in a larger dosage than a sedative)
CATEGORIES OF SEDATIVE-HYPNOTICS:
a. Barbiturates
Action: stimulating the inhibitory neurotransmitter
system in the brain called the [gamma]-
aminobutyric acid (GABA) system.
Uses:

Major side Effects:

• Excessive CNS depression: dizziness, drowsiness, hang-over
effect, convulsion
• Rebound insomnia, respiratory depression
• Anxiety, hypersensitivity
• Interacts with alcohol and narcotics which may further
depress the CNS
Nursing implications:
• Teach safety precautions to clients
• Assess level of consciousness,
respiratory status, and effectiveness
of the agent
• Hold if respirations is <10/min.
• Do not abruptly stop the medication
for those on chronic use.
 b. Benzodiazepines
Common drugs:
• flurazepam (Dalmane)
• estozolam (Esilgan)
• temazapam
• triazolam
• quazepam
• Action: increase in GABA (inhibitor)→
calming effect – decrease anxiety, induce
sleep, hypnotic therapy
 2. ANESTHETICS
ANESTHESIA- the loss of sensation as a result
of reversible CNS depression
MOA - inhibit or block excitatory ligand-
gated ion channels and enhance the
sensitivity of inhibitory ion channels such
as GABA receptor.
1. Barbiturates - depress nerve synapses in
the reticular activating system, the portion
of the nervous system responsible for the
level of consciousness
• e.g. thiopental sodium (Penthotal)
2. Benzodiazepine - act by facilitating the
binding of the inhibitory neurotransmitter
GABA at various GABA receptors throughout
the CNS.
• diazepam, lorazepam, midazolam
3. Ketamine hydrochloride - Antagonism of
the NMDA receptor is responsible for the
anesthetic, analgesic, and psychotomimetic
effects
• for children and patients with hypotension
• used for short surgical procedures
4. Propofol - positive modulation of the
inhibitory function of the neurotransmitter
gama-aminobutyric acid (GABA) through
GABA-A receptors.
• can cause respiratory depression
Major side effects: hangover effect,
apnea, laryngospasm,
bronchospasm, coughing, CVS
depression
Nursing implication
• Have emergency equipment and IV fluids
ready
• Know each individual drug
• Practice and stress safety measures
• Monitor vital signs
• Monitor elimination and status (urine
output)
3. Anticonvulsants
• ANTICONVULSANT – substance that prevents, reduces,
or stops the severity of epileptic or other convulsive
disorders.
• Mechanisms:
• Suppress sodium influx →
prolonging channel
inactivation → prevents
neuron firing
• Suppress calcium influx →
prevents electric current
generated
• Increase the action of GABA
 NURSING CONSIDERATIONS
• CNS: dizziness
• Eat food with drug
• Antacids decrease
• Support group for epileptics
• Alert tag indicating specific drug
• Report adverse effects
3. ANXIOLYTICS OR
ANTIANXIETY DRUGS
• Action: to enhance the effect of GABA (Gamma
AminoButyric Acid), an inhibitory neurotransmitter to
decrease impulses in the synapses of the brain,
therefore decreasing conduction of rapid impulses
causing symptoms of anxiety.depression of the CNS,
produces relaxation.
• Common Drugs:
• Benzodiazepines: diazepam (Valium)
Alprazolam (Xanor)
Lorazepam (Ativan)
 NURSING CONSIDERATIONS
• Avoid abrupt discontinuation after prolonged use
• Not given if BP is decreased, with renal/hepatic
dysfunction, or history of drug abuse
• Xanax (Alprazolam), Ativan (Lorazepam), Serax (
Oxazepam ) - examples with brand names
• Increase in 3Ds - drowsiness, dizziness, and decrease in
BP
• Enhance action of GABA
• Teach to rise slowly from supine
• Yes, alcohol and caffeine should be avoided
4. ANTIDEPRESSANTS AND
MOOD STABILIZERS
• a. Tricyclic antidepressants
(TCAs)
• Common drugs: amitriptyline
doxepin imipramine
(Torfranil)
• Action: increases
neurotransmitter
concentration levels of NE
and serotonin.
• Major side effects:
sedation, othostatic
hypotension,
anticholinergic effect
• Nursing implication
• It will take 1 to 3 weeks
before the drug will take
effect.
• Drug can mask suicidal
tendencies.
• Institute safety measures.
• b. Monoamine oxidase inhibitors
(MAOIs)
• Common drugs: phenelzine
sulfate
• Tranylycpromine sulphate
• Isocarboxazid
• Action: inhibit MAO enzymes
(present in the brain, blood
platelets, liver, spleen and
kidneys) that metabolizes NE and
serotonin.
• Uses: 2nd line antidepressant
• Side effects: hypertensive
crisis (if given with
tyramine rich foods like
cheese, yogurt, red
wines), CNS stimulation
(anxiety,agitation,
mania), orthostatic
hypotension.
C. Selective serotonin reuptake
inhibitors (SSRIs)
• Common drugs: fluoxetine (Prozac)
• Sertraline (Zoloft)
• Paroxetine (Seroxat)
• Action: antidepressant response is
from the inhibition of the serotonin
uptake
• Uses: depression, obsessive-
compulsive disorders disorders
• Side effects: nausea, diarrhea,
CNS stimulation insomnia,
headache, nervousness,
dizziness), skin rash
• Nursing implication:
• administer with meals to reduce
nausea
• use cautiously in patients with
impaired renal function