Chapter 13

Central Nervous System

Stimulants and Related Drugs

Copyright © 2017, Elsevier Inc. All rights reserved.

 CNS Stimulants
 Drugs that stimulate a specific area of the brain
or spinal cord
 Neurons contain receptors for excitatory
neurotransmitters, including dopamine
(dopaminergic drugs), norepinephrine
(adrenergic drugs), and serotonin (serotonergic
drugs)
 Sympathomimetic drugs

Copyright © 2017, Elsevier Inc. All rights reserved. 2

 Classification
 Classified according to
 Chemical structural similarities: amphetamines,
serotonin agonists, sympathomimetics, and xanthines
 Site of therapeutic action in the central nervous
system (CNS)
 Major therapeutic uses: anti–attention deficit disorder,
antinarcoleptic, anorexiant, antimigraine, and
analeptic drugs

Copyright © 2017, Elsevier Inc. All rights reserved. 3

Attention Deficit Hyperactivity Disorder
(ADHD)
 Most common psychiatric disorder in children,
affecting 4% to 10% of school-age children
 Boys are affected from two to nine times more
often than girls.
 Primary symptoms of ADHD are inappropriate
ability to maintain attention span or the presence
of hyperactivity and impulsivity.
 Drug therapy for both childhood and adult ADHD
is the same.

Copyright © 2017, Elsevier Inc. All rights reserved. 4

 Narcolepsy
 Incurable neurologic condition in which patients
unexpectedly fall asleep in the middle of normal
daily activities. These “sleep attacks” are
reported to cause car accidents or near-misses
in 70% or more of patients.
 Cataplexy: sudden acute skeletal muscle
weakness. Associated symptom in at least 70%
of narcolepsy cases. It involves sudden acute
skeletal muscle weakness.

Copyright © 2017, Elsevier Inc. All rights reserved. 5

 Obesity
 According to the National Institutes of Health
and the Centers for Disease Control and
Prevention, approximately 30% of Americans are
obese, and nearly two thirds (64.5%) are
overweight.
 More than 72 million obese adults
 Associated health risks

Copyright © 2017, Elsevier Inc. All rights reserved. 6

 Migraine

 Common type of recurring headache, usually

lasting from 4 to 72 hours
 Typical features: pulsatile quality with pain that
worsens with each pulse
 Most commonly unilateral but may occur on both
sides of the head
 Associated symptoms: nausea, vomiting,
photophobia (avoidance of light), and
phonophobia (avoidance of sounds)
 Aura
Copyright © 2017, Elsevier Inc. All rights reserved. 7
 Analeptic-Responsive Respiratory
Depression Syndromes
 Neonatal apnea
 Bronchopulmonary dysplasia
 Postanesthetic respiratory depression
 Drugs: analeptic drugs such as theophylline,
aminophylline, caffeine, and doxapram

Copyright © 2017, Elsevier Inc. All rights reserved. 8

Drugs for Attention Deficit Hyperactivity
Disorder (ADHD) and Narcolepsy
 Amphetamines: methylphenidate
 Nonamphetamine stimulants
 Pemoline and Modafinil
 Atomoxetine: nonstimulant drug that is also used to
treat ADHD
 Lisdexamfetamine (Vyvanse) prodrug for
dextroamphetamine

Copyright © 2017, Elsevier Inc. All rights reserved. 9

 Mechanism of Action
and Drug Effects
 Amphetamines
 Stimulate areas of the brain associated with mental
alertness
 CNS effects
 Mood elevation or euphoria
 Increased mental alertness and capacity for work
 Decreased fatigue and drowsiness
 Prolonged wakefulness

Copyright © 2017, Elsevier Inc. All rights reserved. 10

 Mechanism of Action
and Drug Effects (Cont.)
 Respiratory effects
 Relaxation of bronchial smooth muscle
 Increased respiration
 Dilation of pulmonary arteries

Copyright © 2017, Elsevier Inc. All rights reserved. 11

 Adverse Effects
 Wide range; dose related
 Tend to “speed up” body systems
 Common adverse effects include:
 Palpitations, tachycardia, hypertension, angina,
dysrhythmias, nervousness, restlessness, anxiety,
insomnia, nausea, vomiting, diarrhea, dry mouth,
increased urinary frequency, others

Copyright © 2017, Elsevier Inc. All rights reserved. 12

 Principal Drugs Used to Treat ADHD
and Narcolepsy
 Amphetamines
 Nonamphetamine stimulants
 Atomoxetine: nonstimulant drug also used for
ADHD

Copyright © 2017, Elsevier Inc. All rights reserved. 13

 Amphetamines
 Dextroamphetamine sulfate (Dexedrine)
 Dextroamphetamine saccharate
 Amphetamine sulfate
 Amphetamine aspartate (Adderall): one of the
most commonly prescribed drugs for ADHD

Copyright © 2017, Elsevier Inc. All rights reserved. 14

 Atomoxetine (Strattera)
 Approved for treating ADHD in children older
than 6 years of age and in adults
 In September 2005, the FDA issued a warning
describing cases of suicidal thinking and
behavior in small numbers of adolescent
patients receiving this medication.

Copyright © 2017, Elsevier Inc. All rights reserved. 15

 Audience Response System Question

A teenage boy will be receiving atomoxetine (Strattera) as

part of treatment for ADHD. Which statement about this
drug therapy is accurate?

A. Strattera is highly addictive.

B. Psychotherapy is rarely helpful in cases of ADHD.
C. The patient should be monitored for possible suicidal
thoughts and behavior.
D. Strattera is used to treat narcolepsy as well as ADHD.

Copyright © 2017, Elsevier Inc. All rights reserved. 16

 Methylphenidate (Ritalin)
 First prescription drug indicated for ADHD
 Also used for narcolepsy
 Extended-release dosage forms
 Ritalin SR
 Concerta
 Metadate CD

Copyright © 2017, Elsevier Inc. All rights reserved. 17

 Modafinil (Provigil)
 Use: improvement of wakefulness in patients
with excessive daytime sleepiness associated
with narcolepsy and with shift work sleep
disorder
 Less abuse potential than amphetamines and
methylphenidate
 Schedule IV drug
 Armodafinil (Nuvigil): similar to modafinil

Copyright © 2017, Elsevier Inc. All rights reserved. 18

 Anorexiants
 Used to treat obesity
 Anorexiants
 phentermine (Ionamin)
 benzphetamine (Didrex)
 methamphetamine (Desoxyn)
 diethylpropion (Tenuate)

Copyright © 2017, Elsevier Inc. All rights reserved. 19

 Other Drugs to Treat Obesity
 Orlistat (Xenical): related nonstimulant drug
used to treat obesity
 Mechanism of action: works locally in the small and
large intestines, where it inhibits absorption of caloric
intake from fatty foods.
 lorcaserin (Belviq)
 Qsymia (phentermine and topiramate)

Copyright © 2017, Elsevier Inc. All rights reserved. 20

 Mechanism of Action
 Suppress appetite control centers in the brain
 Increase the body’s basal metabolic rate
 Mobilization of adipose tissue stores
 Enhanced cellular glucose uptake
 Reduce dietary fat absorption

Copyright © 2017, Elsevier Inc. All rights reserved. 21

 Audience Response System Question

A patient wants to take Orlistat (Xenical) to assist in her

weight loss program, but she is wary of its unpleasant
adverse effects. What measure can be suggested to
reduce these effects?

A. Restrict dietary intake of fat.

B. Restrict dietary intake of fiber.
C. Increase intake of dairy products.
D. Avoid intake of carbonated beverages.

Copyright © 2017, Elsevier Inc. All rights reserved. 22

 Adverse Effects
 Possible elevated blood pressure and heart
palpitations
 Anxiety
 Agitation
 Dizziness
 Headache

Copyright © 2017, Elsevier Inc. All rights reserved. 23

 Antimigraine Drugs
 Antimigraine (serotonin agonists; also called
triptans)
 sumatriptan (Imitrex)
 almotriptan (Axert)
 eletriptan (Relpax)
 naratriptan (Amerge)
 rizatriptan (Maxalt)
 zolmitriptan (Zomig)
 frovatriptan (Frova)

Copyright © 2017, Elsevier Inc. All rights reserved. 24

 Antimigraine Drugs (Cont.)
 Ergot alkaloids
 Were the mainstay of treatment of migraine
headaches but have been replaced by the triptans for
first-line therapy
 Dihydroergotamine mesylate (D.H.E. 45): injectable
form and as a nasal spray (Migranal)
 Ergotamine tartrate with caffeine (Cafergot): tablet
form

Copyright © 2017, Elsevier Inc. All rights reserved. 25

 Audience Response System Question

Before administering a serotonin agonist, it is most

important for the nurse to assess the patient for a history of

A. hypertension.
B. allergy to penicillin.
C. chronic bronchitis.
D. cataracts.

Copyright © 2017, Elsevier Inc. All rights reserved. 26

Mechanism of Action and Drug Effects
 Triptans
 Stimulate 5-HT receptors in cerebral arteries, causing
vasoconstriction and reducing headache symptoms
 Reduce the production of inflammatory neuropeptides
 Ergot alkaloids
 Narrow or constrict blood vessels in the brain

Copyright © 2017, Elsevier Inc. All rights reserved. 27

 Adverse Effects

 Triptans
 Vasoconstriction
 Irritation at injection site
 Tingling, flushing
 Ergot alkaloids
 Nausea and vomiting
 Cold or clammy hands and feet
 Muscle pain
 Dizziness
 Others
Copyright © 2017, Elsevier Inc. All rights reserved. 28
 Sumatriptan (Imitrex)

 Original prototype drug for this class

 Seven triptans
 Slight pharmacokinetic differences exist between
some of these products.
 Effects are comparable overall.

Copyright © 2017, Elsevier Inc. All rights reserved. 29

 Analeptics
 Used less frequently
 Still used for neonatal apnea
 Examples
 Doxapram (Dopram)
 Methylxanthines, such as aminophylline, theophylline,
and caffeine

Copyright © 2017, Elsevier Inc. All rights reserved. 30

 Analeptics (Cont.)
 Doxapram (Dopram)
 Treatment of respiratory depression associated with
anesthetic drugs and drugs of abuse, COPD-induced
hypercapnia
 Monitor deep tendon reflexes, in addition to vital signs
and heart rhythm, to prevent overdosage of this drug.

Copyright © 2017, Elsevier Inc. All rights reserved. 31

 Analeptics (Cont.)
 Caffeine
 Found in:
• Over-the-counter drugs: NoDoz
• Combination prescription drugs: Fioricet, Fiorinal
• Foods and beverages
 Use with caution in patients with a history of:
• Peptic ulcer
• Recent myocardial infarction
• Dysrhythmias
Intravenous: caffeine citrate and caffeine sodium
benzoate

Copyright © 2017, Elsevier Inc. All rights reserved. 32

 Mechanism of Action
 Stimulate areas of CNS that control respiration
 Methylxanthines
 Inhibit phosphodiesterase, leading to buildup of cyclic
adenosine monophosphate (cAMP)
 Caffeine
 Antagonizes adenosine receptors

Copyright © 2017, Elsevier Inc. All rights reserved. 33

 Adverse Effects
 Vagal
 Stimulation of gastric secretions, diarrhea, and reflex
tachycardia
 Vasomotor
 Flushing, sweating
 Respiratory
 Elevated respiratory rate
 Musculoskeletal
 Muscular tension and tremors

Copyright © 2017, Elsevier Inc. All rights reserved. 34

 Doxapram (Dopram)
 Used in conjunction with supportive measures in
cases of respiratory depression that involve
anesthetics, drugs of abuse and COPD-
associated hypercapnia.
 To prevent overdose, monitor deep tendon
reflexes, vital signs, and heart rhythm.

Copyright © 2017, Elsevier Inc. All rights reserved. 35

 Nursing Implications
 Assess for:
 Potential contraindications
 Potential interactions, including herbal therapies
 Conditions such as abnormal cardiac rhythms,
seizures, palpitations, liver problems
 For children, assess baseline height and weight.

Copyright © 2017, Elsevier Inc. All rights reserved. 36

 Nursing Implications (Cont.)
 Drugs for ADHD
 Last daily dose should be given 4 to 6 hours before
bedtime to reduce insomnia.
 Take on an empty stomach 30 to 45 minutes before
meals.
 Drug “holidays” may be ordered.
 Instruct parents to keep a journal to monitor the
child’s response to therapy.
 Monitor the child for continued physical growth,
including height and weight.

Copyright © 2017, Elsevier Inc. All rights reserved. 37

 Audience Response System Question

A patient is prescribed an anorexiant. Which statement will

the nurse include in patient teaching?

A. “Take the medication with your evening meal.”

B. “You will need to take this drug for at least 2 years.”
C. “If you develop a dry mouth, stop taking the drug
immediately.”
D. “Avoid intake of caffeine.”

Copyright © 2017, Elsevier Inc. All rights reserved. 38

 Nursing Implications (Cont.)
 Anorexiants
 Follow instructions for diet and exercise.
 Take in the morning.
 Avoid caffeine
 Fat-soluble vitamin supplementation may be needed.

Copyright © 2017, Elsevier Inc. All rights reserved. 39

 Nursing Implications (Cont.)
 Selective Serotonin Receptor Agonists (SSRAs)
 Dissolvable wafers, nasal spray, and self-injectable
forms
 Provide specific teaching about correct administration.
 Instruct patients to keep a journal to monitor response
to therapy.

Copyright © 2017, Elsevier Inc. All rights reserved. 40

 Nursing Implications (Cont.)
 Ergot alkaloids
 Chest pain, confusion, slurred speech, and vision
changes need immediate medical attention.
 Analeptics
 Pay close attention to the ABCs because of the
patient’s diminished sensorium.

Copyright © 2017, Elsevier Inc. All rights reserved. 41

 Nursing Implications (Cont.)
 Monitor for therapeutic responses
 ADHD: decreased hyperactivity, increased attention
span and concentration
 Anorexiant: appetite control and weight loss
 Narcolepsy: decrease in sleepiness
 Serotonin agonist: decrease in frequency, duration,
and severity of migraines
 Monitor for adverse effects

Copyright © 2017, Elsevier Inc. All rights reserved. 42