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Focus on
PHARMACOLOGY
ESSENTIALS FOR HEALTH PROFESSIONALS
CHAPTER
17
Drugs Used to
Treat Central
Nervous System
Conditions
Figure 17-1 The central nervous system (CNS) includes the brain and spinal cord. The
peripheral nervous system includes the nerves throughout the body that exit from the
spinal cord.
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Figure 17-2
The spinal cord.
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CNS Stimulants: Uses
• Diverse group of pharmacologic agents
• Exact mechanism of action is not clear
but may stimulate cerebral cortex and
increase activity of norepinephrine,
dopamine, and other catecholamines at
CNS synapses.
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CNS Stimulants: Uses
• Indirect-acting sympathomimetics are
used to treat attention deficit–
hyperactivity disorder (ADHD); very
few other therapeutic uses.
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CNS Stimulants: Adverse Effects
• Common: headache, palpitations,
cardiac dysrhythmias, hypertension,
nervousness, nausea
• Highly addictive and widely abused
outside therapeutic therapy (especially
methamphetamine)
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CNS Stimulants:
Contraindications
• Do not use in patients with a history of
drug abuse, severe agitation,
hyperthyroidism, diabetes mellitus,
moderate to severe hypertension,
advanced arteriosclerosis, angina
pectoris, cardiovascular disorders, or
glaucoma.
• Safety in pregnancy and lactation not
established.
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CNS Stimulants:
Patient Information
• Advise patients that taking CNS
stimulants for a long time can cause
withdrawal symptoms.
• Advise families of children with ADHD
to seek counseling. Drug therapy alone
is insufficient.
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Sedatives and Hypnotics
• Sedatives: diminish activity of CNS;
used to relieve anxiety
• Hypnotics: induce sleep; used for
short-term treatment of insomnia
• Difference between two drug classes is
in the dosage
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Hypnotics and Sleep
• No currently available hypnotics induce
what can be termed “natural” sleep.
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Table 17-1
Commonly Used Benzodiazepines
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Table 17-1 (continued) Commonly Used Benzodiazepines
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Benzodiazepines: Uses
• Mechanism of action appears related to
their ability to increase the action of
neurotransmitter GABA.
• Indicated for generalized anxiety
disorders, panic disorders, insomnia,
some types of seizures, muscle
relaxation
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Benzodiazepines:
Adverse Effects
• Common: drowsiness, ataxia, impaired
judgment, rebound insomnia, tolerance
• Serious (with overdosage): CNS and
respiratory depression, hypotension,
coma
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Benzodiazepines:
Contraindications
• Do not use in pregnancy, severe liver
or kidney disorders, or in hyperactive
children.
• Interact with alcohol, omeprazole to
cause increased CNS depression
• Interact with cimetidine, disulfiram,
hormonal contraceptives, theophylline,
ranitidine
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Benzodiazepines:
Patient Information
• Educate patients about relaxation
techniques and to avoid caffeine,
especially close to bedtime.
• Advise patients not to abruptly stop
medication.
• Warn patients to avoid alcohol and
other CNS depressants.
• Advise patients to avoid driving.
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Oral Contraceptives
• Warn women taking benzodiazepines
and oral contraceptives that increased
sedative effects may occur because
high levels of benzodiazepines may
accumulate in the blood plasma.
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Barbiturates: Uses
• Classified as CNS agents,
anticonvulsants, and sedative-hypnotics
• May work by inhibiting reticularactivating system, thereby interfering
with impulse transmission of cerebral
cortex
• Used to treat insomnia and for some
types of seizures
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Barbiturates: Adverse Effects
• Common: sedation, nausea, vomiting,
constipation, diarrhea, bradycardia
• Serious: respiratory depression,
circulatory shock, renal or hepatic
damage
• Addiction
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Barbiturates: Contraindications
• Do not use in patients with familial
history of porphyria or with severe
respiratory or kidney disease; and in
pregnancy or lactation.
• Interact with alcohol, oral
anticoagulants, corticosteroids, oral
contraceptives
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Barbiturates:
Patient Information
• Instruct patients in relaxation
techniques.
• Advise patients not to stop the
medication suddenly.
• Warn patients not to drink alcohol or
drive while taking barbiturates.
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Epilepsy
• Permanent, recurrent seizure disorder
• Seizure: periodic attack of disturbed
cerebral function
– Generalized tonic-clonic (previously grand
mal)
– Generalized absence (previous petit mal)
– Generalized myoclonic
– Partial
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Table 17-2
Most Commonly Prescribed Antiseizure Drugs
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Table 17-2 (continued) Most Commonly Prescribed Antiseizure Drugs
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Table 17-2 (continued) Most Commonly Prescribed Antiseizure Drugs
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Phenytoin (Dilantin): Uses
• Most common hydantoin
• Reduces voltage, frequency, spread of
electrical discharges within motor
cortex
• Used for partial, tonic-clonic,
psychomotor, and nonepileptic seizures
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Phenytoin: Adverse Effects
• Common: blurred vision, dizziness,
drowsiness, fatigue, thrombocytopenia,
aplastic anemias
• Excess dosages: confusion, delirium,
psychosis
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Phenytoin: Contraindications
• Avoid in patients with hypoglycemic
seizures, sinus bradycardia, or heart
block, and in pregnancy or lactation.
• Use cautiously in patients with impaired
liver or kidney function, alcoholism,
blood disorders, or hypotension.
• Lower the dosage in elderly patients.
• Numerous drug–drug interactions
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Phenytoin: Patient Information
• Advise patients that urine may turn
pink or red-brown.
• Instruct patients with diabetes to
frequently check blood glucose levels.
• Advise patients to use good oral
hygiene to prevent gingival
hyperplasia.
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Valproic Acid (Depakote): Uses
• Action may be related to increased
bioavailability of GABA to neurons.
• Used to treat simple and complex
absence seizures
• Has been used for other generalized
seizures
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Valproic Acid: Adverse Effects
• Common: nausea, vomiting,
hypersalivation, abdominal cramps,
sedation, drowsiness, possible
prolonged bleeding time
• Serious: liver failure, life-threatening
pancreatitis
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Valproic Acid: Contraindications
• Safe use during pregnancy not
established.
• Increases effects of CNS depressants
• Interacts with aspirin, warfarin,
cimetidine, and other drugs
• May alter thyroid function and urine
ketone tests
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Valproic Acid:
Patient Information
• Advise patients to swallow capsules
whole or add liquid form to foods or
liquids to improve taste.
• Instruct patients to take with meals to
reduce GI upset.
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Ethosuximide: Uses
• Blocks calcium channels to stabilize
neuronal excitability, raising threshold
of uncontrolled cerebral discharges
• Used to control absence and myoclonic
seizures and akinetic epilepsy
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Ethosuximide: Adverse Effects
• Common: drowsiness, hiccups, ataxia,
dizziness, headache, euphoria,
restlessness, anxiety, blurred vision,
aggressiveness, agranulocytosis,
gingival hyperplasia, nausea, vomiting,
anorexia
• Serious: aplastic anemia
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Ethosuximide: Contraindications
• Avoid use in severe liver or kidney
disease.
• Safety not established in pregnancy,
lactation, or children younger than 3
years.
• Interacts with primidone,
carbamazepine, and isoniazid
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Ethosuximide:
Patient Information
• Advise patients about possibility of
blood disorders.
• Instruct patients to report sore throat,
fever, or bruising.
• Warn patients against driving.
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Carbamazepine (Tegretol): Uses
• Promotes sodium efflux, which reduces
neuronal excitability, but leaves motor
cortex relatively unaffected
• Used for partial and tonic-clonic
seizures and trigeminal neuralgia
• Also used to treat depression and
bipolar disorder
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Carbamazepine:
Adverse Effects
• Common: blood disorders, altered
urination, liver or kidney dysfunctions,
confusion and agitation in elderly
patients especially, blurred vision,
dizziness, drowsiness, fatigue
• Serious: severe cardiovascular
disturbances
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Carbamazepine:
Contraindications
• Avoid in patients with cardiac or liver
impairment.
• Use extremely cautiously in pregnancy.
• Interacts with antineoplastic agents,
antiretroviral protease inhibitors,
barbiturates, calcium channel blockers,
corticosteroids, and many more drugs
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Carbamazepine:
Patient Information
• Inform patients that blood disorders
may occur.
• Advise patients to report sore throat,
mucosal ulceration, petechiae, or
bruising of unknown cause.
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Parkinson’s Disease
• Occurs mostly in elderly individuals
• Nervous system disorder characterized
by movement abnormalities such as
tremor of head and extremities,
difficulty coordinating fine muscle
movement, hypokinesia (inability or
slowness in initiating movements)
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Cause of Parkinson’s Disease
• Unknown, but a CNS defect leads to it
• Substantia nigra is important to
initiation and control of muscular
movement
• Lack of dopaminergic activity in
substantia nigra leads to imbalance
between dopamine and acetylcholine
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Figure 17-3
Normal (A) and abnormal (B) balance between dopamine and
acetylcholine.
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Parkinsonism
• Refers to symptoms produced by
certain drugs, poisons, and traumatic
lesions in the basal ganglia
• Also called secondary parkinsonism
• Symptoms may be temporary.
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Treatment of
Parkinson’s Disease
• No cure available
• Drug therapy manages symptoms.
• Pharmacotherapy attempts to
rebalance dopamine and acetylcholine
by:
– Decreasing muscarinic activity
– Increasing dopaminergic activity by
blockings its breakdown or mimicking its
action
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Kava
• Patients who have Parkinson’s disease
should not take the natural product
kava, which is often taken as a dietary
supplement to reduce stress and
anxiety.
• Antipsychotics, barbiturates,
benzodiazepines, and CNS depressants
should not be taken with kava.
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Table 17-3
Anticholinergic Drugs Used for Parkinson’s Disease
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Anticholinergic Drugs: Uses
• Work by inhibiting muscarine receptors
and blocking effect of acetylcholine
• Only centrally acting anticholinergics
are used (benztropine and
trihexyphenidyl)
• Can be used to treat parkinsonism
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Anticholinergics:
Adverse Effects
• Common: anxiety, agitation, confusion,
dry mouth, decreased sweating and
heat release
• Serious: urticaria, urine retention,
paresthesias, sinus tachycardia
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Anticholinergics:
Contraindications
• Safe use in pregnancy not established.
• Should not be given with other
antimuscarinics
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Anticholinergics:
Patient Information
• Instruct patients to avoid alcohol.
• Advise patients to consume a high-fiber
diet to help ease constipation.
• Warn patients to avoid driving because
the drug causes drowsiness.
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Table 17-4
Dopaminergic Drugs Used for Parkinson’s Disease
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Table 17-4 (continued) Dopaminergic Drugs Used for Parkinson’s Disease
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Dopaminergics: Uses
• Precise mechanism unknown; but
dopaminergics are precursors of
dopamine
• Most commonly used is levodopa
(Larodopa)
• Used to treat Parkinson’s disease and
parkinsonism associated with
manganese and carbon monoxide
poisoning
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Dopaminergics:
Adverse Effects
• Common: dyskinesia, hallucinations,
mental confusion
• Long-term: loss of efficacy
• Abrupt discontinuation: neuroleptic
malignant syndrome (tachycardia,
muscular rigidity, fever, mental status
changes, diaphoresis, tachypnea)
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Dopaminergics:
Contraindications
• Use cautiously in cardiac disease.
• Should not be used in patients with a
history of allergy to these substances.
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Dopaminergics:
Patient Information
• Instruct patients to take with food to
avoid GI upset and avoid foods rich in
vitamin B6 (beans and cereals).
• Advise patients to use good oral
hygiene.
• Warn patients not to discontinue the
drug abruptly.
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Schizophrenia
• Chronic psychiatric disease
• Positive symptoms: exaggerations of
normal functioning, such as
hallucinations and delusions
• Negative symptoms: terse speech,
social withdrawal, apathy, anhedonia
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Antipsychotic Drugs
• Typical
– Examples: chlorpromazine (Thorazine),
haloperidol (Haldol)
• Atypical
– Examples: clozapine (Clozaril), olanzapine
(Zyprexa), risperidone (Risperdal)
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Table 17-5
Common Typical and Atypical Antipsychotic Drugs
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Table 17-5 (continued) Common Typical and Atypical Antipsychotic Drugs
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Table 17-5 (continued) Common Typical and Atypical Antipsychotic Drugs
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Table 17-5 (continued) Common Typical and Atypical Antipsychotic Drugs
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Antipsychotics: Uses
• Act by blocking postsynaptic
dopaminergic receptors
• Used to decrease the positive
symptoms of schizophrenia
• Some agents are effective antiemetic
and antinausea agents
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Antipsychotics:
Adverse Effects
• Common: sedation, dry mouth, sexual
dysfunction, akathisia, bradykinesia,
tardive dyskinesia
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Antipsychotics:
Contraindications
• Contraindicated in comatose patients
who have received large amounts of
CNS depressant drugs
• Contraindicated in patients with known
drug allergies to these agents
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Antipsychotics:
Patient Information
• Advise family members about adverse
effects.
• Suggest using hard candy or ice chips
for a dry mouth.
• Warn patient not to drive a car until
effects are known.
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Lithium: Uses
• Mechanism of action is unclear.
• Used in control and prophylaxis of
acute mania and in acute manic phase
of mixed bipolar disorder
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Lithium: Adverse Effects
• Common: nausea, tremors
• Overdosage: vomiting, diarrhea,
dizziness, headache, drowsiness,
tinnitus, disorientation, short-term
memory loss
• Toxic levels: kidney and heart damage
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Lithium: Contraindications
• Avoid in pregnancy and in patients with
thyroid disorders.
• Interacts with carbamazepine,
haloperidol, and phenothiazines
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Lithium: Patient Information
• Advise patients to drink plenty of fluids.
• Instruct patients to contact their
physician if diarrhea or fever develops.
• Warn patients not to drink excessive
caffeinated beverages and to avoid hot
weather.
• Warn patients not to drive until effects
are known.
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Depression
• Major depression affects about 5 to 6%
of Americans.
• Symptoms include feelings of doom,
lack of self-worth, inability to sense
pleasure, loss of energy, inability to
concentrate, changes in sleep habits,
thoughts of suicide.
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Antidepressants
• Tricyclic antidepressants (TCAs)
• Monoamine oxidase inhibitors (MAOIs)
• Selective serotonin reuptake inhibitors
(SSRIs)
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Table 17-6
Classifications of Antidepressants
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Table 17-6 (continued) Classifications of Antidepressants
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Mechanism of Action
of Diazepam Animation
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action of diazepam.
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TCAs: Uses
• Increase effects of norepinephrine and
serotonin in the CNS by blocking
reuptake by neurons
• Used to treat endogenous depression
and reactive depression
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TCAs: Adverse Effects
• Common: dry mouth, blurred vision,
constipation, urine retention,
tachycardia, mental confusion,
sedation, postural hypotension
• Serious: may precipitate hyperpyrexic
crisis, tachycardia, or seizures
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TCAs: Contraindications
• Avoid in patients during acute recovery
from myocardial infarction or with
severe renal and hepatic impairment.
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TCAs: Patient Information
• Warn patients not to stop medication
abruptly.
• Advise patients to take at bedtime to
promote a normal sleep pattern.
• Instruct patients to report severe
postural hypotension.
• Educate patients that the drugs must
be taken continually to be effective.
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TCAs and Other Medications
• Instruct patients to consult their
physicians about taking any other
medications, including OTC drugs, with
TCAs.
• Instruct patients to contact their
physicians if allergic reactions occur
while taking these medications.
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Effect of TCAs on Prostate Gland
• Elderly men with enlarged prostate
glands are at a higher risk for urine
retention when taking TCAs.
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St. John’s Wort
• The natural product interacts with
TCAs, MAOIs, SSRIs, alcohol, and foods
high in tyramine or catecholamines.
• Women should not use St. John’s wort
during pregnancy or lactation.
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SSRIs: Uses
• Act by primarily blocking serotonin
reuptake
• Used to treat depression, geriatric
depression, obsessive-compulsive
disorder, bulimia nervosa, premenstrual
dysphoric disorder
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SSRIs: Adverse Effects
• Common: headache, nausea, vomiting,
tremor, insomnia, dizziness, diarrhea
• Serious: cardiac toxicity and death
from overdose
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SSRIs: Contraindications
• Do not use concurrently with MAOIs or
thioridazine.
• Do not use in pregnancy or in children
younger than 7 years.
• Use cautiously in patients with hepatic
or renal impairment, renal failure,
lactation, cardiac disease, and diabetes
mellitus.
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SSRIs: Patient Information
• Advise patients to drive carefully while
taking antidepressants, especially at
the beginning of therapy.
• Instruct patients to take in the morning
with food to minimize insomnia and GI
upset.
• Warn patients to avoid alcohol.
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Monoamine Oxidase Inhibitors
(MAOIs): Uses
• May act by preventing natural
breakdown of neurotransmitters
• Used as second- or third-line
antidepressants, depressive phase of
bipolar disorder, and severe exogenous
depression
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MAOIs: Adverse Effects
• Common: orthostatic hypotension,
nausea, constipation, dry mouth,
diarrhea, dizziness, vertigo, headache
• Serious: hypertensive crisis
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MAOIs: Contraindications
• Avoid in patients with epilepsy, liver
disease, and serious cardiovascular
disease.
• These drugs interact with many other
drugs and with foods containing
tyramine (cheese, yogurt, beef, coffee,
tea, caffeinated sodas, chocolate, red
wine).
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MAOIs: Patient Information
• Instruct patients to avoid foods that
contain tyramine and provide a list of
these foods.
• Inform patients that effectiveness
occurs after about 2 weeks of therapy.
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