1. Central Nervous System Stimulants and Related Drugs
Chapter 13
Central Nervous System Stimulants and Related Drugs
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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
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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
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4. 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.
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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.
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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
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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
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8. Analeptic-Responsive Respiratory Depression Syndromes
Neonatal apnea
Bronchopulmonary dysplasia
Postanesthetic respiratory depression
Drugs: analeptic drugs such as theophylline, aminophylline, caffeine, and doxapram
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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
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10. 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
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11. Mechanism of Action and Drug Effects (Cont.)
Respiratory effects
Relaxation of bronchial smooth muscle
Increased respiration
Dilation of pulmonary arteries
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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
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13. Principal Drugs Used to Treat ADHD and Narcolepsy
Amphetamines
Nonamphetamine stimulants
Atomoxetine: nonstimulant drug also used for ADHD
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Amphetamines
Dextroamphetamine sulfate (Dexedrine)
Dextroamphetamine saccharate
Amphetamine sulfate
Amphetamine aspartate (Adderall): one of the most commonly prescribed drugs for ADHD
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15. 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.
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16. 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?
Strattera is highly addictive.
Psychotherapy is rarely helpful in cases of ADHD.
The patient should be monitored for possible suicidal thoughts and behavior.
Strattera is used to treat narcolepsy as well as ADHD.
Correct answer: C
Rationale: Prescribers are advised to work with parents to monitor closely for suicidal thoughts and behavior. In addition, psychosocial problems within the patient’s family should be addressed if needed. Strattera is not addictive, and it is not used to treat narcolepsy.
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17. Methylphenidate (Ritalin)
First prescription drug indicated for ADHD
Also used for narcolepsy
Extended-release dosage forms
Ritalin SR
Concerta
Metadate CD
Correct answer: C
Rationale: Prescribers are advised to work with parents to monitor closely for suicidal thoughts and behavior. In addition, psychosocial problems within the patient’s family should be addressed if needed. Strattera is not addictive, and it is not used to treat narcolepsy.
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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
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Anorexiants
Used to treat obesity
Anorexiants
phentermine (Ionamin)
benzphetamine (Didrex)
methamphetamine (Desoxyn)
diethylpropion (Tenuate)
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20. 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)
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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
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22. 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?
Restrict dietary intake of fat.
Restrict dietary intake of fiber.
Increase intake of dairy products.
Avoid intake of carbonated beverages.
Correct answer: A
Rationale: Restricting dietary intake of fat to less than 30% of total calories can help reduce some of the GI adverse effects of Orlistat, which include oily spotting, flatulence, and fecal incontinence in 20% to 40% of patients.
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Adverse Effects
Possible elevated blood pressure and heart palpitations
Anxiety
Agitation
Dizziness
Headache
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Antimigraine Drugs
Antimigraine (serotonin agonists; also called triptans)
sumatriptan (Imitrex)
almotriptan (Axert)
eletriptan (Relpax)
naratriptan (Amerge)
rizatriptan (Maxalt)
zolmitriptan (Zomig)
frovatriptan (Frova)
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25. 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
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26. Audience Response System Question
Before administering a serotonin agonist, it is most important for the nurse to assess the patient for a history of
hypertension.
allergy to penicillin.
chronic bronchitis.
cataracts.
Correct answer: A
Rationale: The nurse should complete a thorough cardiac history as well as measurement of blood pressure and pulse rate and rhythm. If a patient has a history of hypertension, there is risk of further increases in blood pressure to dangerous levels with use of these drugs and thus the need for careful assessment and documentation. In fact, these drugs are generally not prescribed for patients with migraines who also have coronary artery disease unless a thorough cardiac evaluation has been performed.
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27. 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
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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
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29. Sumatriptan (Imitrex)
Original prototype drug for this class
Seven triptans
Slight pharmacokinetic differences exist between some of these products.
Effects are comparable overall.
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Analeptics
Used less frequently
Still used for neonatal apnea
Examples
Doxapram (Dopram)
Methylxanthines, such as aminophylline, theophylline, and caffeine
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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.
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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
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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
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Adverse Effects
Vagal
Stimulation of gastric secretions, diarrhea, and reflex tachycardia
Vasomotor
Flushing, sweating
Respiratory
Elevated respiratory rate
Musculoskeletal
Muscular tension and tremors
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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.
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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.
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37. 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.
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38. Audience Response System Question
A patient is prescribed an anorexiant. Which statement will the nurse include in patient teaching?
“Take the medication with your evening meal.”
“You will need to take this drug for at least 2 years.”
“If you develop a dry mouth, stop taking the drug immediately.”
“Avoid intake of caffeine.”
Correct answer: D
Rationale: Caffeine in any form must be avoided by patients taking anorexiants. These medications should be taken in the morning to prevent interference with sleep. The drugs are taken on a short-term basis. Dry mouth frequently develops and can be managed by sucking ice chips and keeping a bottle of water nearby at all times. These drugs should not be abruptly stopped because a rebound increase in appetite may develop.
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39. Nursing Implications (Cont.)
Anorexiants
Follow instructions for diet and exercise.
Take in the morning.
Avoid caffeine
Fat-soluble vitamin supplementation may be needed.
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40. 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.
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41. 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.
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42. 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
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