Antiparkinson Drugs

Objectives
• Briefly discuss the impact of acetylcholine and dopamine on the
brain.

• Describe the pathophysiology of Parkinson's disease.

• Identify the different classes of medications used to manage

Parkinson's disease, and list the drugs in each class.

• Discuss the mechanisms of action, dosages, indications, routes of

administration, contraindications, cautions, drug interactions,
adverse effects, and toxic effects of antiparkinson drugs.

• Develop a nursing care plan that includes all phases of the nursing
process for patients taking antiparkinson drugs. 2
 Parkinson’s Disease (PD)
⬤ Chronic, progressive,
degenerative disorder

⬤ Affects dopamine-producing
neurons in the brain

⬤ Caused by an imbalance of two

neurotransmitters
➢ Dopamine
➢ Acetylcholine (ACh)

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Parkinson’s Disease (cont’d)

Copyright © 2014 by Mosby, an imprint of Elsevier Inc. 4

 Parkinson’s Disease (cont’d)
⬤ A progressive condition
➢ Reduction in the number of dopaminergic terminals
➢ Rapid swings in response to levodopa occur (“on-off
phenomenon”)
• PD worsens
• Dyskinesia
 Difficulty performing voluntary movements.

⬤ “Wearing-off phenomenon”

Copyright © 2014 by Mosby, an imprint of Elsevier Inc. 5

 Levodopa Therapy
⬤ Levodopa is a precursor of dopamine

⬤ Blood-brain barrier does not allow an outside

supply of dopamine to enter, but does allow
levodopa

Copyright © 2014 by Mosby, an imprint of Elsevier Inc. 6

 Drug Therapy for PD
⬤ Aimed at increasing levels of dopamine as long
as there are functioning nerve terminals
remaining

⬤ Antagonizes or blocks the effects of Ach

⬤ Drug therapy does not slow the progression of

the disease

Copyright © 2014 by Mosby, an imprint of Elsevier Inc. 7

 Drug Therapy for PD (cont’d)
Indirect-acting dopamine-receptor agonists
➢ Monoamine oxidase B (MAO-B) inhibitors: selegiline
(Eldepryl), rasagiline

➢ Catechol ortho-methyltransferase (COMT) inhibitors:

entacapone, tolcapone

➢ Dopamine modulator: amantadine

Copyright © 2014 by Mosby, an imprint of Elsevier Inc. 8

 Selective MAOI Therapy
⬤ MAO enzymes break down catecholamines in
the CNS, primarily in the brain

⬤ Selegiline (Eldepryl) and rasagiline (Azilect)

are selective MAO-B inhibitors
➢ Cause an increase in levels of dopaminergic
stimulation in the CNS

Copyright © 2014 by Mosby, an imprint of Elsevier Inc. 9

 Selective MAOI Therapy (cont’d)
selegiline (Eldepryl) & Rasagiline (Azilect)
⬤Used in combination with levodopa or

carbidopa-levodopa

⬤ Used as adjuncts when a patient’s response to

levodopa is fluctuating

⬤Allow the dose of levodopa to be decreased

➢ Delay development of unresponsiveness to levodopa
therapy
Copyright © 2014 by Mosby, an imprint of Elsevier Inc. 10
 Selective MAOI Therapy (cont’d)
Adverse effects are usually mild
➢ Dizziness, insomnia, nausea, diarrhea, chest pain, headache, weight
loss, orthostatic hypotension
Administration/Nursing Interventions
➢ Tablet and orally disintegrating forms
➢ Give before the morning meal
➢ Assist with menu selections
Contraindications
➢ Uncontrolled HTN, suicidal ideation, meperidine (Demerol)
Interactions
➢ Meperidine (Demerol), opioids, other MAOIs, tricyclic or SSRIs
antidepressants
➢ Foods with tyramine
➢ Ephedra, St John’s wort, ginseng, ma huag
➢ Antihypertensive drugs, diuretics and general anesthetics 11
 Tyramine Foods
Milk Products - Cheese (aged) and sour cream
Fruits - Bananas (in large amounts), figs, raisins
Vegetables - Egg plant, avocados, beets, sour kraut
Meats - Aged processed and smoked meat (pepperoni, sausage, salami,
bologna) liver
Fish - Fish, caviar, shrimp paste, salted herring
Legumes - Broad beans pods (Fava), soybeans, tofu
Misc - spoiled foods, processed foods, broths, large amount of nuts, yeast
Alcoholic beverages - beer, red wine, vermouth
Non-tyramine foods, beverages that precipitate similar effects -
Chocolate (contains phenylamine), caffeine containing beverages (coffee,
tea, cola) non-alcoholic beer and wine.

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 Dopamine Modulator
⬤ amantadine (Symmetrel)
➢ Indirect acting

➢ Causes release of dopamine from storage sites at the

end of nerve cells that are still intact

➢ Blocks reuptake of dopamine into the nerve endings,

allowing more to accumulate both centrally and
peripherally

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 Catechol ortho-methyltransferase
(COMT) Inhibitors
⬤ Indirect acting

⬤ tolcapone (Tasmar), entacapone (Comtan)

⬤ Inhibit COMT, the enzyme responsible for the breakdown of

levodopa, the dopamine precursor

⬤ Prolong the duration of action of levodopa; reduce wearing-off

phenomenon

Commonly Reported Adverse Effects: GI up-set and urine discoloration

Interactions: Nonselective MAOIs

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 COMT Inhibitors (cont’d)
tolcapone (Tasmar)
➢ Has caused severe liver failure (Black Box Warning:
Hepatic disease)

➢ Requires monitoring of liver enzymes and labs

• Aspartate Transaminase (AST)
• Alanine Aminotransferase (ALT)
• Aspartate Transaminase (ALP)
• Lactate Dehydrogenase (LDH)
• Bilirubin
• Complete Blood Count (CBC)

➢ FDA announced that this drug is not used unless

other drugs do not work
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 Direct-Acting Dopamine Receptor
Agonists
⬤ Nondopamine dopamine receptor agonists
(NDDRAs)
➢ Ergot derivatives (bromocriptine)
➢ Nonergot drugs - pramipexole (Mirapex), ropinirole

⬤ Dopamine replacement drugs

➢ Levodopa, carbidopa, levodopa/carbidopa (Sinemet)

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 Nondopamine Dopamine Receptor
Agonists
Mechanism of Action
⬤Directly binds and stimulates dopamine receptors
➢ Activate dopamine receptors and stimulate production of more dopamine
pramipexole (Mirapex)
➢ Side effect: dizziness, GI upset, drowsiness, orthostatic hypotension,
muscle weakness, sleep attacks, dyskinesias
➢ Nursing Interventions: Ensure safety, check BP, observe abnormal
muscle movement, monitor serum creatine phosphokinase (CPK)
➢ Interactions:
•Cimetidine
•Metoclopramide and Phenothiazines
•Alcohol and other CNS depressants

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 Dopamine Replacement Drugs
Replacement drugs (presynaptic)
➢ Work presynaptically to increase brain levels of dopamine
➢ Used in the later stages of Parkinson’s Disease

⬤Dopamine must be taken orally

➢ Levodopa is able to cross the blood-brain barrier, and then it is
converted to dopamine

⬤Large doses of levodopa

➢ However, large doses of levodopa needed to get dopamine to
the brain also cause adverse effects

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 Dopamine Replacement Drugs
Replacement drugs
➢ Carbidopa is given with levodopa

➢ Carbidopa does not cross the blood-brain barrier and prevents levodopa
breakdown in the periphery

➢ As a result, more levodopa crosses the blood-brain barrier, where it can

be converted to dopamine
Levodopa/Carbidopa (Sinemet)
Side effects: Nausea / Vomiting, orthostatic or postural hypotension,
darken urine and sweat, psychosis, dyskinesia
Interactions: Traditional antipsychotics and supplements with Vit B6
MAOI antidepressants within 2 weeks
Increase protein meals
Anticholinergic drugs

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 Anticholinergic Therapy
⬤ Anticholinergics block the effects of
acetylcholine (Ach)
➢ Reduce the excessive cholinergic activity
in the brain

⬤ Used to treat muscle tremors and

muscle rigidity associated with PD
➢ These two symptoms are caused by
excessive cholinergic activity

⬤ Does not relieve bradykinesia

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 Anticholinergic Therapy

Acetylcholine is responsible for causing increase salivation, lacrimation,

urination, diarrhea, increase GI motility and emesis.

Anticholinergics will have the opposite effects

➢ Dry mouth
➢ Urinary retention
➢ Decrease GI motility

What would be some nursing Interventions?

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 Anticholinergic Therapy (cont’d)
⬤ benztropine mesylate (Cogentin)

⬤ trihexyphenidyl (generic only)

⬤ Antihistamines also have anticholinergic

properties
➢ diphenhydramine (Benadryl)

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Nursing Implications

Antiparkinson Drugs

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 Nursing Implications
Antiparkinson Drugs
⬤ Perform a thorough assessment, nursing history,
and medication history
⬤ Include questions about the patient’s:

➢ CNS
➢ GI and GU tracts
➢ Psychologic and emotional status

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 Nursing Implications (cont’d)
⬤ Assess for signs and symptoms of PD
➢ Masklike expression
➢ Speech problems
➢ Dysphagia
➢ Rigidity of arms, legs, and neck
⬤ Assess for conditions that may be
contraindications

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 Nursing Implications (cont’d)
⬤ Administer drugs as directed by manufacturer
⬤ Provide patient education regarding PD and the

medication therapy
⬤ Inform patient not to take other medications with

PD drugs unless he or she checks with

physician

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 Nursing Implications (cont’d)
⬤ When starting dopaminergic drugs, assist
patient with walking because dizziness may
occur
⬤ Administer oral doses with food to minimize GI

upset
⬤ Encourage patient to force fluids to at least 3000

mL/day (unless contraindicated)

⬤ Taking levodopa with MAOIs may result in

hypertensive crisis

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 Nursing Implications (cont’d)
⬤ Patient should be taught not to discontinue
antiparkinson drugs suddenly
⬤ Teach patient about expected therapeutic and

adverse effects with antiparkinson drug therapy

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 Nursing Implications (cont’d)
⬤ Entacapone may darken the patient’s urine and
sweat
⬤ Therapeutic effects of COMT inhibitors may be

noticed within a few days; it may take weeks

with other drugs

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 Nursing Implications (cont’d)
⬤ Monitor for response to drug therapy
➢ Improved sense of well-being and mental status
➢ Increased appetite
➢ Increased ability to perform ADLs, to concentrate, and
to think clearly
➢ Less intense parkinsonian manifestations, such as
less tremor, shuffling gait, muscle rigidity, and
involuntary movements

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