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COENZYME Q10

Coenzyme Q10 (CoQ10

) is an antioxidant involved in the mitochondrial electron

transport chain and has been shown to be reduced in patients with PD.

125 A futility

analysis in untreated PD patients treated with CoQ10

failed to show statistical

significance but met the threshold for futility. Two subsequent phase III trials of early

PD patients failed to show symptomatic or neuroprotective benefits.

125–127

In an

evaluation of 600 patients with early PD, subjects were randomized to receive either

1,200 or 2,400 mg of CoQ10 daily in addition to 1,200 IU of α-tocopherol. The study

was terminated prematurely due to failure to meet prespecified futility endpoints and

trend in adverse outcomes compared to placebo.

127 Due to the lack of data supporting

CoQ10, K.B. should be counseled to avoid its use.

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CREATINE AND MINOCYCLINE

Similar to CoQ10

, creatine is thought to play a role in mitochondrial energy

production and has been shown to protect from MPTP-induced dopamine depletion

in animal models.

128 Minocycline is an anti-infective agent that also displays antiinflammatory effects and is hypothesized to alter the neuroinflammatory response that

occurs because dopaminergic neurons are lost in PD. Minocycline has been shown to

be protective in MPTP animal models of PD.

128

The use of both creatine and minocycline in PD was examined in a futility-design

study, in which patients with early PD not requiring therapy were randomly assigned

to receive creatine 10 g/day, minocycline 200 mg/day, or placebo.

128 After 12

months, the mean change in the total UPDRS could not be rejected as futile and met

criteria for further clinical testing. A long-term follow-up of this trial found that by

18 months, patients requiring symptomatic treatment did not differ but significantly

more patients on minocycline discontinued therapy prematurely (23% vs. 9% of

creatine and 6% of placebo patients). Given the unresolved issues surrounding the

induction of antibiotic resistance with long-term use of an agent such as minocycline

and concerns for tolerability, it is generally not recommended. A long-term,

randomized, double-blind, placebo-controlled trial of creatine 10 g/day versus

placebo in early treated PD was terminated early for futility based upon an interim

analysis. The trial concluded that treatment with creatine for at least 5 years does not

support its use in PD.

129 Given the lack of data supporting these agents, they should

be avoided in K.B.

FUTURE THERAPIES

With developments in PD research and biopharmaceutical technology, new treatment

targets and modalities are constantly being investigated. Such targets include

transcription factors, proteins, and their mutations. Novel pharmaceutical and

biologic technologies under development include small-molecule drug delivery, such

as with glial-cell-derived neurotrophic factor, stem cell therapies, and nerve cell

grafts.

Nonmotor Symptoms of Parkinson’s Disease

Although PD is mostly recognized for its cardinal features of motor dysfunction,

nonmotor symptoms are an important part of the disease throughout all stages and are

a key determinant of quality of life.

130 More than 98% of patients with PD have at

least one nonmotor symptom; the average per patient is nearly eight, with the number

and impact increasing with disease duration and severity.

131 Common nonmotor

symptoms include autonomic dysfunction (e.g., gastrointestinal disorders, orthostatic

hypotension, sexual dysfunction, urinary incontinence, sialorrhea, seborrhea, and

constipation), sleep disorders (e.g., RLS, PLMS, excessive daytime somnolence,

insomnia, REM sleep behavior disorder), fatigue, and psychiatric disorders (e.g.,

dementia, depression, and anxiety).

131

In one longitudinal study of patients with PD,

the most common nonmotor symptoms were psychiatric symptoms (68%, most

commonly anxiety), fatigue (58%), leg pain (38%), insomnia (37%), urinary

symptoms (35%), drooling (31%), and difficulty concentrating (31%).

131 Regular

screening for these nonmotor symptoms should occur. L.M. has a history of

depression treated with citalopram that could be attributable to PD, and his therapy

should be periodically evaluated. The forgetfulness and decreased memory described

by L.M. could be early signs of cognitive decline and warrant close observation. The

management of several commonly encountered nonmotor symptoms is reviewed

below.

DEMENTIA

CASE 59-3

QUESTION 1: J.D. is a 74-year-old man with advanced PD, Hoehn and Yahr

2

stage 4. During the last year,

his family has noticed that he is increasingly forgetful and anxious. Twice recently, he left home alone for brief

periods, and called 9-1-1 because he thought someone was trying to break into the house. He also calls his

daughter 2 or 3 times each day, often repeating the same questions and forgetting that he called her earlier. His

wife is his primary caregiver, and he is nearly entirely reliant on her for help in performing ADLs. He scored 20

(below normal) on his most recent Mini-Mental Status Examination, and his family reports that he is no longer

interested in social activities or hobbies. Neuropsychiatric testing is performed and demonstrates a significant

depressive component to his dementia. Subsequent recommendations from the neuropsychiatrist are that he

receives 24-hour supervision, along with participation in structured leisure activities, such as adult day care,

several hours/week to help relieve his wife’s caregiver burden. How should the progressive cognitive decline

that J.D. is experiencing be treated?

The prevalence of dementia in patients with PD is high; 48% to 80% of patients

may develop dementia during the disease course, at a rate approximately 6 times

greater than healthy individuals.

17

,

132 One longitudinal study of 136 incident cases of

PD followed for 20 years found that nearly 100% eventually exhibited dementia.

133

The prevalence of cognitive decline and dementia among patients with PD ranges

from 10% to 30% and may be associated with a more rapid progression of diseaserelated disability.

6 Successful management of cognitive impairment in patients with

PD first requires that all potentially reversible causes and underlying contributing

factors be addressed. These include treating infections, dehydration, and metabolic

abnormalities, as well as eliminating unnecessary medications (particularly

anticholinergics, sedatives, and anxiolytics) that can exacerbate dementia or

delirium.

Experience with cholinesterase inhibitors for treating cognitive impairment in PD

indicates marginal improvements with their use.

134–136 Two randomized, controlled

trials of donepezil have failed to show consistent benefit, whereas galantamine has

only been evaluated in a single open-label trial.

137

,

138 Rivastigmine was found to

provide clinically meaningful (moderate or marked improvement on the Alzheimer’s

Disease Cooperative Study–Clinician’s Global Impression of Change) benefit to

significantly more patients than placebo in a large, randomized, placebo-controlled

trial and has demonstrated sustained cognitive benefit for up to 48 weeks.

136

,

139

,

140 As

a result, rivastigmine was FDA-approved for the management of mild-to-moderate

dementia in PD and is therefore the drug of choice. Compared with placebo, the

cholinesterase inhibitors often result in statistically significant changes on cognitive

scales; though, their impact on function and disposition is unclear.

A cholinesterase inhibitor such as rivastigmine may be considered for patients

such as J.D., although he must be monitored closely for signs of deterioration of

motor function such as worsening of tremor.

137 Cholinesterase inhibitors are

associated with other adverse events that may be overlooked and attributed to the PD

itself, including sialorrhea, excessive lacrimation, incontinence, nausea, vomiting,

and orthostasis. Perhaps more important than any medication therapy, adequate social

support for J.D. should be ensured. Because he becomes further dependent on family

members for assistance with ADLs, the increased needs of the caregiver(s) should

also be considered. In the case of J.D., attending

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adult day care several times weekly, if available, would provide a structured,

supervised environment for interaction with others, as well as providing a rest

period for his caregiver. Dementia is a leading cause of nursing home placement for

patients with PD.

137

DEPRESSION/ANXIETY

CASE 59-3, QUESTION 2: How should anxiety and depression be treated in J.D.?

Despite being one of the strongest predictors of quality of life in PD patients,

depression is often poorly recognized and inadequately treated.

137 This is likely

because depression and PD share overlapping features that often confound the

identification of depression. Withdrawal, lack of motivation, flattened affect,

decreased physical activity, and bradyphrenia are examples of overlapping

features.

137

Treatment of depression in PD should first focus on providing adequate treatment

of the symptoms of PD by attempting to restore mobility and independence,

particularly in patients whose depression can be attributed to lengthy off periods.

Antiparkinsonian drugs, such as pramipexole, can be associated with moodenhancing effects independent of their ability to reduce time in the off state.

137 Small

trials and case reports have shown that depression in patients with PD can be

successfully treated with antidepressant drugs, including tricyclic agents such as

amitriptyline, desipramine, nortriptyline, bupropion, and selective serotonin reuptake

inhibitors (SSRIs) such as citalopram and paroxetine.

137 Given the overall lack of

high-quality trials, it is difficult to know whether expected benefits reflect class

responses or are unique to the individual agents studied. Importantly, the potential for

adverse effects should always be considered. For example, some SSRIs, such as

fluoxetine, can be activating. Although this may be beneficial in patients who are

apathetic or withdrawn, it may worsen symptoms in patients with PD who are

agitated. Selective serotonin reuptake inhibitors have additionally been noted to

worsen PD tremor in approximately 5% of patients.

141 With tricyclic antidepressants,

care must be taken to observe for anticholinergic side effects that may worsen PD

symptoms, such as impaired cognition, delayed gastric emptying (which may reduce

levodopa effectiveness by increasing levodopa degradation in the gut), urinary

problems, orthostatic hypotension, and increased risk of falls. Additionally,

consideration should be taken for drug interactions and the risk for serotonin

syndrome with concomitant MAO-B inhibitors. Electroconvulsive therapy may be

considered in refractory cases, but may adversely affect cognition.

Based on his symptoms, it is reasonable to start J.D. on an antidepressant. Clinical

experience suggests a good initial choice for balancing efficacy and safety is an

SSRI, such as citalopram. As with other patients with depression, the choice of agent

should be individualized based on other pragmatic factors such as cost, potential for

adverse effects, and personal or family history of response to prior agents.

Regardless of which agent or class of antidepressant is selected, therapy should be

started at the lowest dose and gradually titrated to effect. He should be monitored

closely for side effects, particularly anticholinergic symptoms with tricyclic

antidepressants, and for any adverse effects on mobility. He should be observed

carefully for changes in parkinsonian symptoms, including development of

extrapyramidal symptoms, as well as any signs of psychomotor agitation. Short-term

use of benzodiazepines, such as lorazepam or alprazolam, may also provide relief of

anxiety symptoms, but must be used cautiously due to adverse effects on cognition

and risk of falling.

142 Generally, anxiety symptoms should improve with treatment of

the underlying depression.

PSYCHOSIS

In PD, the incidence of psychotic symptoms increases with age, cognitive

impairment, and disease duration.

143 Other risk factors include higher age at PD

onset, high doses of dopaminergic drugs, and REM sleep behavior disorder.

144

Symptoms are often more pronounced at night (the “sundowning” effect), and

hallucinations are typically visual. As with the management of cognitive impairment,

it is important to eliminate or minimize any potential causative factors, particularly

anticholinergic medications that could be contributing to the hallucinations or

delirium. In some patients, reducing the dose of levodopa improves mental function

and also provides satisfactory control of motor features. If it is not possible to

achieve a balance between preserving motor control and decreasing neuropsychiatric

symptoms through reduction in levodopa dosage, antipsychotics may be considered.

Older antipsychotic medications, such as haloperidol, perphenazine, and

chlorpromazine, block striatal dopamine D2

receptors and may exacerbate

parkinsonian symptoms. Therefore, these agents are not recommended. Newer

atypical antipsychotics are more selective for limbic and cortical D3

, D4

, and D5

receptors; they have minimal activity at D2

receptors and may control symptoms

without worsening parkinsonism. Of these agents, clozapine has the best evidence of

efficacy in patients with PD without adversely affecting motor function and should be

preferentially considered.

137 However, its use is complicated by the need for frequent

monitoring of white blood cell counts because of the risk of agranulocytosis. Other

newer agents, particularly quetiapine, appear promising and have controlled

psychosis without worsening parkinsonism.

17

,

137 Risperidone and olanzapine have

also been studied, but both worsened parkinsonism and were inferior to clozapine in

patients with PD.

137

,

145 Aripiprazole, also a newer atypical antipsychotic, has been

associated with worsening motor function in patients with PD, whereas experience

with ziprasidone has yielded mixed results.

146

AUTONOMIC DYSFUNCTION

Patients with PD frequently experience dysautonomia, including orthostasis, erectile

dysfunction, constipation, nocturia, sensory disturbances, dysphagia, seborrhea, and

thermoregulatory imbalances. Management of these symptoms is generally

supportive, and appropriate medical interventions similar to those used in other

geriatric patients can be used to treat these symptoms whenever encountered. In some

cases, fludrocortisone or midodrine can be considered if orthostatic hypotension is

severe, although these drugs have not been well studied in PD patients specifically.

130

Other possibly effective treatments for symptoms of autonomic dysfunction include

sildenafil for erectile dysfunction and polyethylene glycol for constipation.

130

A new atypical antipsychotic, pimavanserin, was FDA-approved in April 2016

based on results from one randomized, placebo-controlled trial. This agent’s

mechanism of action is unique, acting through serotonin receptors, and as such it

avoids interaction with dopamine receptors responsible for the worsening of PD

symptoms with other antipsychotics. It is not without its own risks, including

cardiovascular and paradoxical worsening of psychosis.

147

FALLS

Patients with PD and their caregivers should be counseled on the prevention of falls

because they can result in serious morbidity and mortality. Falls generally result from

one of several factors, including postural instability, freezing and festination,

levodopa-induced dyskinesia, symptomatic orthostatic hypotension, coexisting

neurologic or other medical disorders, and environmental factors. Prevention

remains the best strategy and includes environmental precautions, such as proper

lighting, use of handrails, removing tripping hazards, and incorporating physical and

occupational

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therapy. Reversible causes of postural or gait instability should be addressed

whenever suspected. Patients with PD are advised to take a vitamin D supplement to

reduce their risk of fracture with future falls.

17

SLEEP DISORDERS

Sleep disorders may occur at any time during the disease course and may even

precede motor symptom development.

17

In excessive daytime drowsiness, a common

sleep disorder in PD, treatment with modafinil may be considered.

130 Other sleep

disorders such as insomnia, sleep fragmentation owing to PD symptoms, RLS, and

REM sleep disorder (characterized by vivid dreams that are often acted out,

especially if frightening) are common and a source of decreased quality of life. When

sleep dysfunction can be directly attributed to PD symptoms, such as akinesia,

tremor, dyskinesia, or nightmares, dosage adjustment of dopaminergic medications is

indicated. Proper sleep hygiene should be encouraged. Insomnia symptoms unrelated

to PD symptoms are treated similar to non-PD patients and can be managed

supportively.

RESTLESS LEGS SYNDROME AND PERIODIC

LIMB MOVEMENTS OF SLEEP

Clinical Presentation

CASE 59-4

QUESTION 1: J.J., a 47-year-old woman, presents to her family physician complaining of daytime fatigue and

difficulty sleeping at night because of “jumpy legs.” She reports being able to sleep only 4 to 5 hours/night

because of the leg restlessness and feels unrefreshed after sleep. On further questioning, she describes the

sensation in her legs as being like “bugs crawling under the skin.” The sensation is not painful. She explains that

the symptoms worsen in the evening and at night and are partially relieved with walking. She recalls that her

mother had similar symptoms. Her spouse notes that she often “kicks” him in her sleep. Review of her medical

history shows an otherwise healthy postmenopausal woman. What signs and symptoms are suggestive of RLS

in J.J.? What laboratory tests or diagnostic procedures should be performed in J.J. to evaluate her condition?

RLS, also known as Willis–Ekbom disease, is a disabling sensorimotor disorder

estimated to affect approximately 2% of the adult population.

148 Although most

patients with mild symptoms will not require treatment, RLS can be associated with

adverse health outcomes, including sleep-onset insomnia, missed or late work,

anxiety, depression, marital discord, and even suicide in severe cases.

Four essential criteria have been established by the International Restless Legs

Syndrome Study Group to diagnose RLS (Table 59-6).

149 The pathognomonic trait of

RLS is an almost irresistible urge to move the legs (akathisia), often associated with

uncomfortable paresthesias or dysesthesias felt deep inside the limbs. Patients

describe the sensation as “creepy-crawly” or “like soda water in the veins.”

150 The

symptoms may occur unilaterally or bilaterally, affecting the ankle, knee, or entire

lower limb. With progressive disease, symptoms can begin earlier in the day, and

progressive involvement of the arms or trunk may occur. Temporary or partial relief

of symptoms can be achieved with movement. If patients attempt to ignore the urge to

move the legs, akathisia will progressively intensify until either they move their legs

or the legs jerk involuntarily.

150 Symptoms usually manifest in a circadian pattern

with onset or worsening during nighttime hours (usually between 6 PM and 4 AM, with

peak symptoms between midnight and 4 AM). The circadian pattern persists even in

patients with inverted sleep–wake cycles. As a result of their symptoms, patients

with RLS become “nightwalkers,” spending significant time walking, stretching, or

bending the legs in an effort to relieve symptoms.

Table 59-6

Clinical Features of Restless Legs Syndrome (RLS)

Essential Criteria

Urge to move legs, associated with paresthesias or dysesthesias

Relief of symptoms with movement

Onset or exacerbation of symptoms at rest

Onset or worsening of symptoms during nighttime

Supportive Clinical Features

Accompanying sleep disturbance (sleep-onset insomnia)

Periodic leg movements

Positive response to dopaminergic therapy

Positive family history of RLS

Otherwise normal physical examination

RLS, restless legs syndrome.

The symptoms described by J.J. are an example of a classic presentation of RLS.

The prevalence of RLS increases with age and appears to be slightly more common

in women.

151 She describes “creepy-crawly” sensations that are relieved partially

with walking, a core feature of RLS. Her symptoms are worse during the evening

hours. J.J. reports that her mother suffered from similar symptoms. The observation

of a familial tendency suggests a genetic component, and several chromosomal loci

have been linked to the disease.

152 A strong family history of RLS appears to

correlate with an early age of onset (<45 years), whereas presentation at a later age

is associated with more neuropathy and accelerated disease progression.

150

Most cases of RLS are considered primary or idiopathic; therefore, the diagnosis

does not require elaborate laboratory tests or diagnostic procedures. Several

conditions are associated with RLS and include iron deficiency, pregnancy, and endstage renal disease. Several medications and substances are known aggravators of

RLS, including medications with antidopaminergic properties, such as

metoclopramide and prochlorperazine. Nicotine, caffeine, and alcohol can aggravate

RLS through their own ability to interfere with quality of sleep. Additionally, SSRIs,

tricyclic antidepressants, and commonly used over-the-counter antihistamines, such

as diphenhydramine, can trigger or worsen RLS symptoms.

152 Hypotensive akathisia,

leg cramps, and other conditions such as arthritis, which can cause positional

discomfort with extended periods of sitting in one position, can mimic RLS. These

conditions are easily distinguished from RLS because they are usually localized to

certain joints or muscles, do not have a circadian pattern, and are not associated with

an uncontrollable urge to move.

With an otherwise unremarkable physical examination and medical history,

specific laboratory tests that should be performed in J.J. are limited to serum ferritin

and percent transferrin saturation (total iron-binding capacity) to rule out iron

deficiency anemia. Several studies have documented a relationship between low

ferritin concentrations and increased symptom severity.

153 J.J. is postmenopausal, so

a pregnancy test is not necessary. Polysomnography is not usually indicated unless

there is clinical suspicion for sleep apnea or if sleep remains disrupted despite

treatment of

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RLS. When clinical suspicion from the physical examination or medical history

suggests a possible peripheral nerve or radiculopathy cause, a routine neurologic

panel should be obtained.

152

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