DRUGS ACTING ON THE NERVOUS

SYSTEM

Mrs. MICHELLE A. IDURIA, RN,MAN

Lecturer
• Moods and emotions flow the
various thoughts, feelings and
actions of individuals which are
communicated throughout the
central nervous system by
chemical neurotransmitters
Major Neurotransmitters
• Gamma-aminobutyric acid (GABA)
• Serotonin
• Dopamine
• Norepinephrine
• Acetylcholine
Gamma –aminobutyric acid
• Associated with regulation ox anxi
ety
• Reduced level, may result to anxiet
y
Serotonin
• Associated with arousal and gener
al activity levels of the CNS
• Regulates sleep, wakefulness and
mood as well as the delusions, hall
ucinations and withdrawal of schiz
ophrenia
 Dopamine containing
neurons
• Involved in regulation of and cogni
tion, emotional responses and moti
vation
Dopamine neurotransmitters
• Associated with schizophr
enia and other psychoses
Norepinephrine
• Associated with control of arousa
l , attention,vigilance, mood, affec
t and anxiety
• Involved with thinking, planning,
and interpreting
 Acetylcholine
• Plays a role in sleep and wakef
ulness
• “ faulty release, reuptake or elimin
ation of neurotransmitters may lea
d to imbalance of neurotransmissi
on, hence, mental and behavioral d
isorders may follow”
ANXIOLYTIC AGENTS
Anxiety
• State of apprehension, tension
or uneasiness that stems from
anticipation of danger, source
of which is unknown or
unrecognized
Primary anxiety
• Not caused by a medical condition
or drug
Secondary anxiety
• Related to selected drugs, medical
or psychiatric disorders
Non pharamacologic measures
• Relaxation technique
• Psychotherapy
• Support group
Pharmacologic
• Benzodiazepines –used as anti con
vulsants, sedative-hypnotics, pre o
perative drugs and anxiolytics
Benzodiazepines
• Enhance the action of gamma
aminobutyric acid (GABA), an
inhibitory neurotransmitter within
the CNS
Examples:
• Lorazepam ( Ativan)
• Diazepam ( Valium )
• Chlordiazepoxide
( Librium)
Librium (PO, IV,IM)
• First benzodiazepine widely us
ed for its sedative effect
Lorazepam (PO, IV, IM)
• Mild to moderate anxiety
• Control alcohol
withdrawal syndrome
Diazepam (PO, IV, IM)
• Anxiety
• Muscle spasm
• Epileptics
• Pre operative sedation
Pharmacokinetics
• Lipid soluble
• Absorbed readily in the GI tract
• Highly protein bound
• Excreted in the urine
• Classified as Controlled substance
schedule IV
Pharmacodynamics
• Must be prescribed no more
than 3 to 4 months
Side effects
• Sedation
• Dizziness
• Headache
• Dry mouth
• Blurred vision
• Urinary incontinence
• constipation
Adverse reactions
• Leukopenia
• Drug tolerance
• Physical dependency
Antidote for overdose
• Flumazenil (Romazicon) IV
Client teaching
• Adivise not to drive or operate a da
ngerous equipment
• Instruct not consume alscohol
• Inoform that effective response is 1
-2 weeks
• Encourage compliance and not to
abruptly stop taking the medicatio
n
ANTIDEPRESSANTS AND
MOOD STABILIZERS
Depression
• Characterized by mood
changes and loss of interest in
normal activities
Reactive depression
• Sudden onset after a precipitati
ng event
Major depression
• Loss of interest in work and home
and inability to complete tasks
Bipolar disorder
• Manic –depressive illness
• Swings between two moods –e
uohoric and dysphoric
Antidepressant agents
• Tricyclic antidepressants
• Selective serotonin inhibitor
• Monoamine oxidase inhibitor
• Atypical antidepressants
Tricyclic antidepressant
• To treat major depression
• Block the uptake of the
neurotransmitters
norepinephrine and serotonin
in the brain
Examples
• Amitriptyline ( Elavil) (PO)
• Doxepin ( Sinequan) (PO)
• Trimipramine ( Surmontil) (PO)
Side effects
• Orthostatic hypotension
• Sedation
• Anticholinergic effects
• Cardiac toxicity- most serious adverse
reaction
• seizures
Side effects
• Allergic reaction
• Blood dyscracia
• Sexual dysfunction
SELECTIVE SEROTONIN
REUPTAKE INHIBITORS
SSRI
• Blocks the reuptake of serotonin in
the nerve terminal of the CNS
• Do not block the uptake of
dopamine, norepinephrine nor
block cholinergic receptors
• Well absorbed in the GI tract
SSRI
• Major depression
• Obsessive compulsive
• Panic
• Phobias
• PTSD
Examples
• Fluoxetine ( Prozac)
• Sertraline ( Zoloft)
• Paroxetine ( Paxil))
• Citalopram ( Celexa)
Side effects
• Dry mouth
• Blurred vision
• Insomnia
• Headache
• Nervousness
• Anorexia
• Nausea
• Diarrhea
• Suicidal ideation
• Decrease in sexual arousal
MONOAMINE OXIDASE
INHIBITOR
Monoamine Oxidase (MAO)
Inhibitor
• Monoamine –an enzyme that
inactivates norepinephrine,
dopamine, epinephrine and
serotonin
• As effective as TCA
Examples:
• Tranylcypromine ( Parnate)-PO
• Isocarboxazid ( Marplan)
• Phenelzine sulfate ( Nardil)
Drug and food interaction
• Any drug that is CNS stumulant, or
sympathomimetics,
vasoconstrictors or cold
medication containing
phenylephrine can cause
HYPERTENSIVE CRISIS
Food Interaction
• Food that contains tyramine:
cheese, cream. Yogurt, coffee,
chocolate,, bananas, raisins, Italian
beer and red wine can cause
HYPERTENSIVE CRISIS
Client teachings
• Compliance is important
• Effectiveness is 1-2 weeks after therapy
• Not to consume alcohol
• Not to abruptly stop the drug
• Take with food if GI distress occurs
 ANTIPSYCHOTIC
AGENTS/NEUROLEPTICS
• PSYCHOSIS
Losing contact with reality
• Difficulty in processing information an
coming to a conclusion
• Delusions
• Hallucinations
• Incoherence
• Catatonia
• Aggressive violent behavior
Mechanism of action
• Blocks the action of dopamine
Phenothiazines(IM,PO,IV,SQ)
• Chlorpromazine ( Thorazine)
Fluphenazine ( prolixin)-PO,IM,
• Perphenazine ( Trilafon)
• Thioridazine ( Mellaril)
Phenothiazines
• Highly protein bound
• Excretion of metabolites is slow
• Full therapeutic effect evident in 3
to 6 weeks
Non phenothiazines
• Most common is haloperidol
( Haldol)
• Alters the effects of dopamine by
blocking dopamine receptors
• Potent 0.5 to 5 gm
• With long half life
Long acting preparations
• Every 2-4 weeks
• Use large gauge needle
• Z track technique
• Injection site should not be
massaged
• Sites must be rotated
Side effects
• Drowsiness ( most common)
• Anticholinergic effects
• Extrapyramidal syndrome
( pseudoparkinsonism, dystonia,
tardive dyskinesia
 Nursing interventions/Client
teaching
• Monitor VS
• Observe for EPS
• Record intake and output
• Instruct client to take drugs as ordered
• Inform of when improvement in
condition is evident
• Remain with the client while taking the
medication
• Discuss family planning
• Taech smoking cessation
• Obtain lab test _WBC for 3 months
• Inform that tolerance may develop
over a period of days or weeks
 DRUGS FOR
NEUROMUSCULAR
DISORDERS
Neuromuscular disorders:
• Myasthenia gravis
• Multiple sclerosis
• Muscle spasm
Myasthenia gravis
• Results from lack of acetylcholine
receptor sites
• Weakness and fatigue of skeletal
muscles
• autoimmune
 Acetylcholinesterase
inhibitors/cholinesterase inhibitors
• Inhibit the action of the enzyme
• More acetylcholine is available
causing muscle contraction
Example
• Neostigmine ( Prostigmin)
• Short half life ( given every 2 to 4
hours)
• Pyridostigmine ( Mestinon)
• Intermediate half life ( given every
3-6 hours)
Cholinergic crisis
• Results from overdosing
• Severe headache
• Paralysis
• Arrest
• Antidote: Atropine sulfate
Tensilon test(edrophonium chloride)
• If muscle weakness becomes more
severe- overdosing (cholinergic cri
sis)
• If muscle weakness improves-unde
rdosing (myasthenic crisis)
Side effects
• GI disturbances
• Increased salivation and tearing
• Constricted pupils
• Blurred vision
• Bradycardia
• Hypotension
Multiple sclerosis
• Autoimmune disease
• Attacks myelin sheath of nerve
fibers
• Weakness and spascticity
Treatment

• Glucocorticoids
( prednisone)
• Biologic response modifiers
• Immunosuppressants
( Cytoxan)
 Client
• Medications teaching
should not be abruptly
stopped
• Advise not to drive or operate
machineries
• Teach to avoid alcohol
• Warn that this is contraindicated to
pregnant women
DRUGS ACTING ON
THE AUTONOMIC
NERVOUS SYSTEM
Autonomic Nervous System
• Also called visceral system
• Acts on the smooth muscle and
glands
• Control and regulate the heart,r
espiratory system, GI tract, bla
dder, eyes and glands
2 sets of neurons in the ANS
• afferent neurons- sends impulses t
o the CNS where they are interpret
ed
• Efferent neurons- receive the impul
ses from the brain and transmit tho
se impulses through the spinal cor
d to the effector organ cells
Efferent pathways
• Sympathetic nervous system
• Parasympathetic nervous syste
m
Sympathetic Nervous System
• Called adrenergic system
• Adrenergic receptor organ cells ar
e:
• Alpha 1
• Alpha 2
• Beta 1
• Beta 2
Parasympathetic Nervous System

• Called cholinergic system

Sympathetic Nervous Parasympathetic
system Nervous System
Dilates pupils Constrict pupils
Dilates bronchioles Constrict bronchioles
Relaxes smooth muscle Contracts smooth
(GI tract) muscle of stomach,
intestine and bladder

Constrict blood vessels Dilates blood vessels

Increases heart rate Decreases heart rate

Relaxes smooth muscle Increases peristalsis
of GI tract
Sympathetic Parasympathetic
nervous system Nervous system
Relaxes bladder Constrict
muscle bladder
Relaxes uterine
muscle
Increases
salivation
ADRENERGIC/ADRENERGIC
BLOCKERS
 Adrenergics/sympathomimetics/
adrenergic agonists
• Drugs that stimulate the sympatheti
c nervous system
• Act on the receptor cells
Norepinephrine
• SNS neurotransmitter
 Effects of adrenergic at receptor sites

RECEPTOR PHYSIOLOGIC
RECEPTORS
ALPHA 1 increases force of
heart contraction
Vasoconstriction
increases blood
pressure
Mydriasis occur
Decrease salivation
Increses urinary
relaxation and urinary
sphincter contraction
Receptor Physiologic response
ALPHA 2 •Inhibits the release of
norepinephrine
•Dilates blood vessels
•Produce hypotension
•Decrease gastrointestinal
motility and tone
BETA 1 •Increases heart rate and
force of contraction
•Increases renin secretion
•Increases blood pressure
receptor Physiologic response
BETA 2 •Dilates bronchioles
•Promotes
gastrointestinal and
uterine relaxation
•Promotes
glycogenolysis
•Increase blood flow in
skeletal muscles
Classification of sympathomimetics
Classification Action Examples
Direct Stimulate Epinephrine
acting adrenergic Norepinephrin
receptor e
Indirect Stimulate the amphetamine
acting release of
norepinephrine
from the
terminal nerve
endings
Mixed Ephedrine
 Epinephrine
• Non selective
• Acts on Alpha1, beta 1 and beta 2 a
drenergic sites
Pharmacokinetics
• Maybe administered SQ, IV, topicall
y or inhalation, intracardiac
• Metabolized in the liver
• Excreted in the urine
Pharmacodynamics
• Used to treat anaphylaxis
• Inotropic
• Increases cardiac output
• Increases systolic BP, heart rate
• bronchodilation
• High doses may result to cardiac dy
srhythmias
• Onset and peak are rapid
OTHER ADRENERGIC DRUGS
• norepinephrine (Levophed)- IV---for shock
• Dopamine (Intropin)- IV---to correct hypotensi
on
• Phenylephrine—instillation—nasal decongest
ant
• Phenylpropanolamine---PO---nasal decongest
ant
• Albuterol (ventolin)---to relieve bronchospas
m
• Terbutaline sulfate---PO--IV
 CLIENT HEALTH
EDUCATION/NURSING
RESPONSIBILITY
NURSING RESPONSIBILITY
• Record client’s vital signs
• Check urinary output and assess bladd
er distention
• Offer food when giving the drug
• Evaluate blood glucose level
Client teaching
• Instruct client to read the label of O
TC meds
• Advise nursing mothers not to take
these drugs
• Explain rebound congestion
• Encourage to report side effects
 ADRENERGIC
BLOCKERS/ANTAGONISTS
Adrenergic Blockers
• Also called antagonists, sympatholy
tics
• Blocks the effect of adrenergic neur
otransmitters
Receptor Responses
ALPHA 1 Effects of Adrenergic blockers at
Vasodilation
Decrease BP
receptors
Miosis
Suppresses ejaculation
Reduces contraction of
smooth muscle in the bladder
and prostate gland
BETA 1 Decreases heart rate,
reduces force of contraction
BETA 2 Constricts bronchioles
Contracts uterus
Inhibits glycogenolysis
Alpha adrenergic blockers
• Selective alpha blockers-blocks alp
ha 1
• Non selective-blocks alpha 1 and al
pha2
 Selective apha adrenergic blockers

• Terazosin ( Hytrin)---PO---for hypert

ension
• Prazosin Hcl ( Minipress)----PO—m
ild to mod hpn
• Doxazosin mesylate ( Regitine)---IM
/IV---peripheral vascular disorder an
d hypertensive emergency
BETA ADRENERGIC
BLOCKERS
Beta blockers
• Selective
• Non selective beta blockers
Non selective beta blockers
drugs Route Uses
Propranolol PO Angina
(Inderal) pectoris,MI,
hypertension,
dysrhythmia
Nadolol ( PO Hypertension,
Corgard) angina
pectoris
Carvedilol ( PO hypertension
Coreg)
Penbutolol ( PO Mild to mod
Levatol) hypertension
Pharmacokinetics of propranolol

• Well absorbed in the GI tra

ct
• Crosses blood brain barri
er and placenta
• Metabolized in the liver
• Half life of 3-6 hours
Pharmacodynamics
• Decreases heart rate
• Decreases blood pressure
• Constriction of bronchial tubul
es
Selective Beta Adrenergic Blockers
Drug route Uses
Metropolol Po/IV hpn,angina,
tartrate MI,
(Lopressor) bradycardia,
dizziness
Atenolol ( PO
Tenormin)
Betaxolol ( PO Hypertensio
Kerlone) n ang
glaucoma
 NURSING
RESPONSIBILITIES/CLIENT
EDUCATION
Nursing responsibilities
• Obtain VS and ECG
• Assess whether with respiratory
problems
• Record and I and O
• Note other drugs that the client i
s taking
 Client Education
• Advise client not to abruptly stop a beta blo
cker
• Instruct to comply with the drug regimen
• Monitor blood sugar level if in insulin thera
py
• Teach how to monitor pulse and blood pres
sure
• Drugs may cause decrease libido
• Mood changes
• Slowly rise from bed
CHOLINERGICS AND ANTI
CHOLINERGICS
Cholinergics /parasympathomimetics
• Mimics PNS acetylcholine
Two types of receptors
• Muscarinic – stimulates smoot
h muscle, slows heart rate
• Nicotinic- affects skeletal musc
les
 Effects of Cholinergic Drugs
Body tissue Response
Cardiovascular •Decreases heart rate
•Lowers blood pressure

GI Increases tone and motility

Increased peristalsis
OCULAR miosis
GLANDULAR Increases salivation
BRONCHIAL Bronchial contraction.
Increase secretion
STRIATED MUSCLE Maintains muscle strength
and tone
Direct acting cholinergics
• Acts on the receptor site to stimulate
response
• Eg Bethanechol chloride ( Urecholin
e)-used primarily to increase urinatio
n
• Metoclopramide Hcl ( Reglan)-increa
ses gastric emptying
Indirect acting cholinergics
• Also called Cholinesterase inhibit
or/acetylcholinesterase inhibitor,a
nticholinesterase
• Do not act on the receptors
• Inhibit or inactivate cholinesterase
Example

• Drugs used to increase muscle tone

for clients with myathenia gravis ( e
drophonium Cl or Tensilon)
 NURSING
RESPONSIBILITY/CLIENT
EDUCATION
Nursing responsibilities
• Monitor VS
• Record I and O
• Administer 1 hour before or 2 hours after m
eal
• Check AST
• Check for side effects
• Auscultate for breath sounds
• Have the antidote ready
• Excessive perspiration may occur
• Beware of cholinergic crisis
ANTICHOLINERGICS
 Anticholinergics
/parasympatholytics/cholinergic blocking
agents

• Inhibit action of acetylcholine by occ

upying the acetylcholine receptors
• Sympathetic nervous system domina
tes
• Opposite effects of cholinergic drugs
 Atropine Sulfate
• Derived from Belladonna plant
• Act on the muscarinic receptor,little
on nicotinic receptor
Atropine Sulfate
• Pre operative medication to decreas
e salivary secretions
• Antispasmodic to treat PUD
• Increase heart rate in case of brady
cardia
 Pharmacokinetics
• Well absorbed orally and parenteral
ly
• Crosses blood brain barrier
• Short half life
• What do you think are side e
ffects and adverse reactions
of atropine sulfate
OTHER SIDE EFFECTS
• Nausea
• Headache
• Dry skin
• Abdominal distention
• Impotence
• Photophobia
• coma
Nursing interventions
• Monitor VS
• Determine I & O
• Record bowel sound
• Raise side rails
• Provide mouth care
• Advise client to avoid hot environme
nt
• Instruct not to drive a motor vehicle